General Information of This Payload
Payload ID
PAY0HYAIC
Name
GRM payload C1
Synonyms
GRM payload C1
   Click to Show/Hide
Formula
C28H32FNO6
Isosmiles
O=C1C=C2CC[C@H]3[C@@H]4C[C@@H](O[C@H]5C6=CC=C(N)C=C6)[C@@](C(CO)=O)(O5)[C@@]4(C)C[C@H](O)[C@]3(F)[C@@]2(C)C=C1
InChI
InChI=1S/C28H32FNO6/c1-25-10-9-18(32)11-16(25)5-8-19-20-12-23-28(22(34)14-31,26(20,2)13-21(33)27(19,25)29)36-24(35-23)15-3-6-17(30)7-4-15/h3-4,6-7,9-11,19-21,23-24,31,33H,5,8,12-14,30H2,1-2H3/t19-,20-,21-,23+,24+,25-,26-,27-,28+/m0/s1
InChIKey
ACTDQNDKLAACFG-FMIHUGCCSA-N
Pharmaceutical Properties
Molecule Weight
497.563
Polar area
119.08
Complexity
1160.923654
xlogp Value
2.9637
Heavy Count
36
Rot Bonds
3
Hbond acc
7
Hbond Donor
3
Each Antibody-drug Conjugate Related to This Payload
Full Information of The Activity Data of The ADC(s) Related to This Payload
38283215 ADC 8 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50)
0.44 ug/mL
High TNF expression (TNF +++)
Method Description
ADC1-ADC27 with a DAR value of ~4 were screened in a GRE luciferase reporter assay in K562 cells over expressing mTNF and wild-type K562 cells to assess potency resulting from targeted delivery vs. nonspecific uptake. All the ADCs were inactive in the wild-type cells, suggesting the activity seen in mTNF over expressed cells was through targeted ADC uptake followed by intracellular release of compound C1.

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In Vitro Model Blast phase chronic myelogenous leukemia, BCR-ABL1 positive, Chronic myeloid leukemia K562 cells (TNF) CVCL_0004
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50) > 34 ug/mL Negative TNF expression (TNF-)
Method Description
ADC1-ADC27 with a DAR value of ~4 were screened in a GRE luciferase reporter assay in K562 cells over expressing mTNF and wild-type K562 cells to assess potency resulting from targeted delivery vs. nonspecific uptake. All the ADCs were inactive in the wild-type cells, suggesting the activity seen in mTNF over expressed cells was through targeted ADC uptake followed by intracellular release of compound C1.

   Click to Show/Hide
In Vitro Model Blast phase chronic myelogenous leukemia, BCR-ABL1 positive, Chronic myeloid leukemia K562 cells (wt) CVCL_0004
38283215 ADC 20 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50)
0.48 ug/mL
High TNF expression (TNF +++)
Method Description
ADC1-ADC27 with a DAR value of ~4 were screened in a GRE luciferase reporter assay in K562 cells over expressing mTNF and wild-type K562 cells to assess potency resulting from targeted delivery vs. nonspecific uptake. All the ADCs were inactive in the wild-type cells, suggesting the activity seen in mTNF over expressed cells was through targeted ADC uptake followed by intracellular release of compound C1.

   Click to Show/Hide
In Vitro Model Blast phase chronic myelogenous leukemia, BCR-ABL1 positive, Chronic myeloid leukemia K562 cells (TNF) CVCL_0004
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50) > 26 ug/mL Negative TNF expression (TNF-)
Method Description
ADC1-ADC27 with a DAR value of ~4 were screened in a GRE luciferase reporter assay in K562 cells over expressing mTNF and wild-type K562 cells to assess potency resulting from targeted delivery vs. nonspecific uptake. All the ADCs were inactive in the wild-type cells, suggesting the activity seen in mTNF over expressed cells was through targeted ADC uptake followed by intracellular release of compound C1.

   Click to Show/Hide
In Vitro Model Blast phase chronic myelogenous leukemia, BCR-ABL1 positive, Chronic myeloid leukemia K562 cells (wt) CVCL_0004
38283215 ADC 7 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50)
0.51 ug/mL
High TNF expression (TNF +++)
Method Description
ADC1-ADC27 with a DAR value of ~4 were screened in a GRE luciferase reporter assay in K562 cells over expressing mTNF and wild-type K562 cells to assess potency resulting from targeted delivery vs. nonspecific uptake. All the ADCs were inactive in the wild-type cells, suggesting the activity seen in mTNF over expressed cells was through targeted ADC uptake followed by intracellular release of compound C1.

   Click to Show/Hide
In Vitro Model Blast phase chronic myelogenous leukemia, BCR-ABL1 positive, Chronic myeloid leukemia K562 cells (TNF) CVCL_0004
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50) > 50 ug/mL Negative TNF expression (TNF-)
Method Description
ADC1-ADC27 with a DAR value of ~4 were screened in a GRE luciferase reporter assay in K562 cells over expressing mTNF and wild-type K562 cells to assess potency resulting from targeted delivery vs. nonspecific uptake. All the ADCs were inactive in the wild-type cells, suggesting the activity seen in mTNF over expressed cells was through targeted ADC uptake followed by intracellular release of compound C1.

   Click to Show/Hide
In Vitro Model Blast phase chronic myelogenous leukemia, BCR-ABL1 positive, Chronic myeloid leukemia K562 cells (wt) CVCL_0004
38283215 ADC 23 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50)
0.53 ug/mL
High TNF expression (TNF +++)
Method Description
ADC1-ADC27 with a DAR value of ~4 were screened in a GRE luciferase reporter assay in K562 cells over expressing mTNF and wild-type K562 cells to assess potency resulting from targeted delivery vs. nonspecific uptake. All the ADCs were inactive in the wild-type cells, suggesting the activity seen in mTNF over expressed cells was through targeted ADC uptake followed by intracellular release of compound C1.

   Click to Show/Hide
In Vitro Model Blast phase chronic myelogenous leukemia, BCR-ABL1 positive, Chronic myeloid leukemia K562 cells (TNF) CVCL_0004
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50) > 36 ug/mL Negative TNF expression (TNF-)
Method Description
ADC1-ADC27 with a DAR value of ~4 were screened in a GRE luciferase reporter assay in K562 cells over expressing mTNF and wild-type K562 cells to assess potency resulting from targeted delivery vs. nonspecific uptake. All the ADCs were inactive in the wild-type cells, suggesting the activity seen in mTNF over expressed cells was through targeted ADC uptake followed by intracellular release of compound C1.

   Click to Show/Hide
In Vitro Model Blast phase chronic myelogenous leukemia, BCR-ABL1 positive, Chronic myeloid leukemia K562 cells (wt) CVCL_0004
38283215 ADC 12 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50)
0.54 ug/mL
High TNF expression (TNF +++)
Method Description
ADC1-ADC27 with a DAR value of ~4 were screened in a GRE luciferase reporter assay in K562 cells over expressing mTNF and wild-type K562 cells to assess potency resulting from targeted delivery vs. nonspecific uptake. All the ADCs were inactive in the wild-type cells, suggesting the activity seen in mTNF over expressed cells was through targeted ADC uptake followed by intracellular release of compound C1.

   Click to Show/Hide
In Vitro Model Blast phase chronic myelogenous leukemia, BCR-ABL1 positive, Chronic myeloid leukemia K562 cells (TNF) CVCL_0004
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50) > 38 ug/mL Negative TNF expression (TNF-)
Method Description
ADC1-ADC27 with a DAR value of ~4 were screened in a GRE luciferase reporter assay in K562 cells over expressing mTNF and wild-type K562 cells to assess potency resulting from targeted delivery vs. nonspecific uptake. All the ADCs were inactive in the wild-type cells, suggesting the activity seen in mTNF over expressed cells was through targeted ADC uptake followed by intracellular release of compound C1.

   Click to Show/Hide
In Vitro Model Blast phase chronic myelogenous leukemia, BCR-ABL1 positive, Chronic myeloid leukemia K562 cells (wt) CVCL_0004
38283215 ADC 26 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50)
0.55 ug/mL
High TNF expression (TNF +++)
Method Description
ADC1-ADC27 with a DAR value of ~4 were screened in a GRE luciferase reporter assay in K562 cells over expressing mTNF and wild-type K562 cells to assess potency resulting from targeted delivery vs. nonspecific uptake. All the ADCs were inactive in the wild-type cells, suggesting the activity seen in mTNF over expressed cells was through targeted ADC uptake followed by intracellular release of compound C1.

   Click to Show/Hide
In Vitro Model Blast phase chronic myelogenous leukemia, BCR-ABL1 positive, Chronic myeloid leukemia K562 cells (TNF) CVCL_0004
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50) > 19 ug/mL Negative TNF expression (TNF-)
Method Description
ADC1-ADC27 with a DAR value of ~4 were screened in a GRE luciferase reporter assay in K562 cells over expressing mTNF and wild-type K562 cells to assess potency resulting from targeted delivery vs. nonspecific uptake. All the ADCs were inactive in the wild-type cells, suggesting the activity seen in mTNF over expressed cells was through targeted ADC uptake followed by intracellular release of compound C1.

   Click to Show/Hide
In Vitro Model Blast phase chronic myelogenous leukemia, BCR-ABL1 positive, Chronic myeloid leukemia K562 cells (wt) CVCL_0004
38283215 ADC 27 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50)
0.55 ug/mL
High TNF expression (TNF +++)
Method Description
ADC1-ADC27 with a DAR value of ~4 were screened in a GRE luciferase reporter assay in K562 cells over expressing mTNF and wild-type K562 cells to assess potency resulting from targeted delivery vs. nonspecific uptake. All the ADCs were inactive in the wild-type cells, suggesting the activity seen in mTNF over expressed cells was through targeted ADC uptake followed by intracellular release of compound C1.

   Click to Show/Hide
In Vitro Model Blast phase chronic myelogenous leukemia, BCR-ABL1 positive, Chronic myeloid leukemia K562 cells (TNF) CVCL_0004
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50) > 42 ug/mL Negative TNF expression (TNF-)
Method Description
ADC1-ADC27 with a DAR value of ~4 were screened in a GRE luciferase reporter assay in K562 cells over expressing mTNF and wild-type K562 cells to assess potency resulting from targeted delivery vs. nonspecific uptake. All the ADCs were inactive in the wild-type cells, suggesting the activity seen in mTNF over expressed cells was through targeted ADC uptake followed by intracellular release of compound C1.

   Click to Show/Hide
In Vitro Model Blast phase chronic myelogenous leukemia, BCR-ABL1 positive, Chronic myeloid leukemia K562 cells (wt) CVCL_0004
38283215 ADC 10 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50)
0.6 ug/mL
High TNF expression (TNF +++)
Method Description
ADC1-ADC27 with a DAR value of ~4 were screened in a GRE luciferase reporter assay in K562 cells over expressing mTNF and wild-type K562 cells to assess potency resulting from targeted delivery vs. nonspecific uptake. All the ADCs were inactive in the wild-type cells, suggesting the activity seen in mTNF over expressed cells was through targeted ADC uptake followed by intracellular release of compound C1.

   Click to Show/Hide
In Vitro Model Blast phase chronic myelogenous leukemia, BCR-ABL1 positive, Chronic myeloid leukemia K562 cells (TNF) CVCL_0004
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50) > 50 ug/mL Negative TNF expression (TNF-)
Method Description
ADC1-ADC27 with a DAR value of ~4 were screened in a GRE luciferase reporter assay in K562 cells over expressing mTNF and wild-type K562 cells to assess potency resulting from targeted delivery vs. nonspecific uptake. All the ADCs were inactive in the wild-type cells, suggesting the activity seen in mTNF over expressed cells was through targeted ADC uptake followed by intracellular release of compound C1.

   Click to Show/Hide
In Vitro Model Blast phase chronic myelogenous leukemia, BCR-ABL1 positive, Chronic myeloid leukemia K562 cells (wt) CVCL_0004
38283215 ADC 5 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50)
0.72 ug/mL
High TNF expression (TNF +++)
Method Description
ADC1-ADC27 with a DAR value of ~4 were screened in a GRE luciferase reporter assay in K562 cells over expressing mTNF and wild-type K562 cells to assess potency resulting from targeted delivery vs. nonspecific uptake. All the ADCs were inactive in the wild-type cells, suggesting the activity seen in mTNF over expressed cells was through targeted ADC uptake followed by intracellular release of compound C1.

   Click to Show/Hide
In Vitro Model Blast phase chronic myelogenous leukemia, BCR-ABL1 positive, Chronic myeloid leukemia K562 cells (TNF) CVCL_0004
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50) > 23 ug/mL Negative TNF expression (TNF-)
Method Description
ADC1-ADC27 with a DAR value of ~4 were screened in a GRE luciferase reporter assay in K562 cells over expressing mTNF and wild-type K562 cells to assess potency resulting from targeted delivery vs. nonspecific uptake. All the ADCs were inactive in the wild-type cells, suggesting the activity seen in mTNF over expressed cells was through targeted ADC uptake followed by intracellular release of compound C1.

   Click to Show/Hide
In Vitro Model Blast phase chronic myelogenous leukemia, BCR-ABL1 positive, Chronic myeloid leukemia K562 cells (wt) CVCL_0004
38283215 ADC 22 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50)
0.72 ug/mL
High TNF expression (TNF +++)
Method Description
ADC1-ADC27 with a DAR value of ~4 were screened in a GRE luciferase reporter assay in K562 cells over expressing mTNF and wild-type K562 cells to assess potency resulting from targeted delivery vs. nonspecific uptake. All the ADCs were inactive in the wild-type cells, suggesting the activity seen in mTNF over expressed cells was through targeted ADC uptake followed by intracellular release of compound C1.

   Click to Show/Hide
In Vitro Model Blast phase chronic myelogenous leukemia, BCR-ABL1 positive, Chronic myeloid leukemia K562 cells (TNF) CVCL_0004
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50) > 50 ug/mL Negative TNF expression (TNF-)
Method Description
ADC1-ADC27 with a DAR value of ~4 were screened in a GRE luciferase reporter assay in K562 cells over expressing mTNF and wild-type K562 cells to assess potency resulting from targeted delivery vs. nonspecific uptake. All the ADCs were inactive in the wild-type cells, suggesting the activity seen in mTNF over expressed cells was through targeted ADC uptake followed by intracellular release of compound C1.

   Click to Show/Hide
In Vitro Model Blast phase chronic myelogenous leukemia, BCR-ABL1 positive, Chronic myeloid leukemia K562 cells (wt) CVCL_0004
38283215 ADC 2 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50)
0.74 ug/mL
High TNF expression (TNF +++)
Method Description
ADC1-ADC27 with a DAR value of ~4 were screened in a GRE luciferase reporter assay in K562 cells over expressing mTNF and wild-type K562 cells to assess potency resulting from targeted delivery vs. nonspecific uptake. All the ADCs were inactive in the wild-type cells, suggesting the activity seen in mTNF over expressed cells was through targeted ADC uptake followed by intracellular release of compound C1.

   Click to Show/Hide
In Vitro Model Blast phase chronic myelogenous leukemia, BCR-ABL1 positive, Chronic myeloid leukemia K562 cells (TNF) CVCL_0004
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50) > 50 ug/mL Negative TNF expression (TNF-)
Method Description
ADC1-ADC27 with a DAR value of ~4 were screened in a GRE luciferase reporter assay in K562 cells over expressing mTNF and wild-type K562 cells to assess potency resulting from targeted delivery vs. nonspecific uptake. All the ADCs were inactive in the wild-type cells, suggesting the activity seen in mTNF over expressed cells was through targeted ADC uptake followed by intracellular release of compound C1.

   Click to Show/Hide
In Vitro Model Blast phase chronic myelogenous leukemia, BCR-ABL1 positive, Chronic myeloid leukemia K562 cells (wt) CVCL_0004
38283215 ADC 14 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50)
0.78 ug/mL
High TNF expression (TNF +++)
Method Description
ADC1-ADC27 with a DAR value of ~4 were screened in a GRE luciferase reporter assay in K562 cells over expressing mTNF and wild-type K562 cells to assess potency resulting from targeted delivery vs. nonspecific uptake. All the ADCs were inactive in the wild-type cells, suggesting the activity seen in mTNF over expressed cells was through targeted ADC uptake followed by intracellular release of compound C1.

   Click to Show/Hide
In Vitro Model Blast phase chronic myelogenous leukemia, BCR-ABL1 positive, Chronic myeloid leukemia K562 cells (TNF) CVCL_0004
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50) > 50 ug/mL Negative TNF expression (TNF-)
Method Description
ADC1-ADC27 with a DAR value of ~4 were screened in a GRE luciferase reporter assay in K562 cells over expressing mTNF and wild-type K562 cells to assess potency resulting from targeted delivery vs. nonspecific uptake. All the ADCs were inactive in the wild-type cells, suggesting the activity seen in mTNF over expressed cells was through targeted ADC uptake followed by intracellular release of compound C1.

   Click to Show/Hide
In Vitro Model Blast phase chronic myelogenous leukemia, BCR-ABL1 positive, Chronic myeloid leukemia K562 cells (wt) CVCL_0004
38283215 ADC 25 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50)
0.79 ug/mL
High TNF expression (TNF +++)
Method Description
ADC1-ADC27 with a DAR value of ~4 were screened in a GRE luciferase reporter assay in K562 cells over expressing mTNF and wild-type K562 cells to assess potency resulting from targeted delivery vs. nonspecific uptake. All the ADCs were inactive in the wild-type cells, suggesting the activity seen in mTNF over expressed cells was through targeted ADC uptake followed by intracellular release of compound C1.

   Click to Show/Hide
In Vitro Model Blast phase chronic myelogenous leukemia, BCR-ABL1 positive, Chronic myeloid leukemia K562 cells (TNF) CVCL_0004
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50) > 50 ug/mL Negative TNF expression (TNF-)
Method Description
ADC1-ADC27 with a DAR value of ~4 were screened in a GRE luciferase reporter assay in K562 cells over expressing mTNF and wild-type K562 cells to assess potency resulting from targeted delivery vs. nonspecific uptake. All the ADCs were inactive in the wild-type cells, suggesting the activity seen in mTNF over expressed cells was through targeted ADC uptake followed by intracellular release of compound C1.

   Click to Show/Hide
In Vitro Model Blast phase chronic myelogenous leukemia, BCR-ABL1 positive, Chronic myeloid leukemia K562 cells (wt) CVCL_0004
38283215 ADC 16 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50)
0.8 ug/mL
High TNF expression (TNF +++)
Method Description
ADC1-ADC27 with a DAR value of ~4 were screened in a GRE luciferase reporter assay in K562 cells over expressing mTNF and wild-type K562 cells to assess potency resulting from targeted delivery vs. nonspecific uptake. All the ADCs were inactive in the wild-type cells, suggesting the activity seen in mTNF over expressed cells was through targeted ADC uptake followed by intracellular release of compound C1.

   Click to Show/Hide
In Vitro Model Blast phase chronic myelogenous leukemia, BCR-ABL1 positive, Chronic myeloid leukemia K562 cells (TNF) CVCL_0004
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50) > 50 ug/mL Negative TNF expression (TNF-)
Method Description
ADC1-ADC27 with a DAR value of ~4 were screened in a GRE luciferase reporter assay in K562 cells over expressing mTNF and wild-type K562 cells to assess potency resulting from targeted delivery vs. nonspecific uptake. All the ADCs were inactive in the wild-type cells, suggesting the activity seen in mTNF over expressed cells was through targeted ADC uptake followed by intracellular release of compound C1.

   Click to Show/Hide
In Vitro Model Blast phase chronic myelogenous leukemia, BCR-ABL1 positive, Chronic myeloid leukemia K562 cells (wt) CVCL_0004
38283215 ADC 13 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50)
0.81 ug/mL
High TNF expression (TNF +++)
Method Description
ADC1-ADC27 with a DAR value of ~4 were screened in a GRE luciferase reporter assay in K562 cells over expressing mTNF and wild-type K562 cells to assess potency resulting from targeted delivery vs. nonspecific uptake. All the ADCs were inactive in the wild-type cells, suggesting the activity seen in mTNF over expressed cells was through targeted ADC uptake followed by intracellular release of compound C1.

   Click to Show/Hide
In Vitro Model Blast phase chronic myelogenous leukemia, BCR-ABL1 positive, Chronic myeloid leukemia K562 cells (TNF) CVCL_0004
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50) > 50 ug/mL Negative TNF expression (TNF-)
Method Description
ADC1-ADC27 with a DAR value of ~4 were screened in a GRE luciferase reporter assay in K562 cells over expressing mTNF and wild-type K562 cells to assess potency resulting from targeted delivery vs. nonspecific uptake. All the ADCs were inactive in the wild-type cells, suggesting the activity seen in mTNF over expressed cells was through targeted ADC uptake followed by intracellular release of compound C1.

   Click to Show/Hide
In Vitro Model Blast phase chronic myelogenous leukemia, BCR-ABL1 positive, Chronic myeloid leukemia K562 cells (wt) CVCL_0004
38283215 ADC 6 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50)
0.82 ug/mL
High TNF expression (TNF +++)
Method Description
ADC1-ADC27 with a DAR value of ~4 were screened in a GRE luciferase reporter assay in K562 cells over expressing mTNF and wild-type K562 cells to assess potency resulting from targeted delivery vs. nonspecific uptake. All the ADCs were inactive in the wild-type cells, suggesting the activity seen in mTNF over expressed cells was through targeted ADC uptake followed by intracellular release of compound C1.

   Click to Show/Hide
In Vitro Model Blast phase chronic myelogenous leukemia, BCR-ABL1 positive, Chronic myeloid leukemia K562 cells (TNF) CVCL_0004
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50) > 50 ug/mL Negative TNF expression (TNF-)
Method Description
ADC1-ADC27 with a DAR value of ~4 were screened in a GRE luciferase reporter assay in K562 cells over expressing mTNF and wild-type K562 cells to assess potency resulting from targeted delivery vs. nonspecific uptake. All the ADCs were inactive in the wild-type cells, suggesting the activity seen in mTNF over expressed cells was through targeted ADC uptake followed by intracellular release of compound C1.

   Click to Show/Hide
In Vitro Model Blast phase chronic myelogenous leukemia, BCR-ABL1 positive, Chronic myeloid leukemia K562 cells (wt) CVCL_0004
38283215 ADC 4 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50)
0.84 ug/mL
High TNF expression (TNF +++)
Method Description
ADC1-ADC27 with a DAR value of ~4 were screened in a GRE luciferase reporter assay in K562 cells over expressing mTNF and wild-type K562 cells to assess potency resulting from targeted delivery vs. nonspecific uptake. All the ADCs were inactive in the wild-type cells, suggesting the activity seen in mTNF over expressed cells was through targeted ADC uptake followed by intracellular release of compound C1.

   Click to Show/Hide
In Vitro Model Blast phase chronic myelogenous leukemia, BCR-ABL1 positive, Chronic myeloid leukemia K562 cells (TNF) CVCL_0004
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50) > 50 ug/mL Negative TNF expression (TNF-)
Method Description
ADC1-ADC27 with a DAR value of ~4 were screened in a GRE luciferase reporter assay in K562 cells over expressing mTNF and wild-type K562 cells to assess potency resulting from targeted delivery vs. nonspecific uptake. All the ADCs were inactive in the wild-type cells, suggesting the activity seen in mTNF over expressed cells was through targeted ADC uptake followed by intracellular release of compound C1.

   Click to Show/Hide
In Vitro Model Blast phase chronic myelogenous leukemia, BCR-ABL1 positive, Chronic myeloid leukemia K562 cells (wt) CVCL_0004
38283215 ADC 21 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50)
0.86 ug/mL
High TNF expression (TNF +++)
Method Description
ADC1-ADC27 with a DAR value of ~4 were screened in a GRE luciferase reporter assay in K562 cells over expressing mTNF and wild-type K562 cells to assess potency resulting from targeted delivery vs. nonspecific uptake. All the ADCs were inactive in the wild-type cells, suggesting the activity seen in mTNF over expressed cells was through targeted ADC uptake followed by intracellular release of compound C1.

   Click to Show/Hide
In Vitro Model Blast phase chronic myelogenous leukemia, BCR-ABL1 positive, Chronic myeloid leukemia K562 cells (TNF) CVCL_0004
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50) > 50 ug/mL Negative TNF expression (TNF-)
Method Description
ADC1-ADC27 with a DAR value of ~4 were screened in a GRE luciferase reporter assay in K562 cells over expressing mTNF and wild-type K562 cells to assess potency resulting from targeted delivery vs. nonspecific uptake. All the ADCs were inactive in the wild-type cells, suggesting the activity seen in mTNF over expressed cells was through targeted ADC uptake followed by intracellular release of compound C1.

   Click to Show/Hide
In Vitro Model Blast phase chronic myelogenous leukemia, BCR-ABL1 positive, Chronic myeloid leukemia K562 cells (wt) CVCL_0004
38283215 ADC 1 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50)
0.92 ug/mL
High TNF expression (TNF +++)
Method Description
ADC1-ADC27 with a DAR value of ~4 were screened in a GRE luciferase reporter assay in K562 cells over expressing mTNF and wild-type K562 cells to assess potency resulting from targeted delivery vs. nonspecific uptake. All the ADCs were inactive in the wild-type cells, suggesting the activity seen in mTNF over expressed cells was through targeted ADC uptake followed by intracellular release of compound C1.

   Click to Show/Hide
In Vitro Model Blast phase chronic myelogenous leukemia, BCR-ABL1 positive, Chronic myeloid leukemia K562 cells (TNF) CVCL_0004
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50) > 50 ug/mL Negative TNF expression (TNF-)
Method Description
ADC1-ADC27 with a DAR value of ~4 were screened in a GRE luciferase reporter assay in K562 cells over expressing mTNF and wild-type K562 cells to assess potency resulting from targeted delivery vs. nonspecific uptake. All the ADCs were inactive in the wild-type cells, suggesting the activity seen in mTNF over expressed cells was through targeted ADC uptake followed by intracellular release of compound C1.

   Click to Show/Hide
In Vitro Model Blast phase chronic myelogenous leukemia, BCR-ABL1 positive, Chronic myeloid leukemia K562 cells (wt) CVCL_0004
38283215 ADC 3 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50)
0.95 ug/mL
High TNF expression (TNF +++)
Method Description
ADC1-ADC27 with a DAR value of ~4 were screened in a GRE luciferase reporter assay in K562 cells over expressing mTNF and wild-type K562 cells to assess potency resulting from targeted delivery vs. nonspecific uptake. All the ADCs were inactive in the wild-type cells, suggesting the activity seen in mTNF over expressed cells was through targeted ADC uptake followed by intracellular release of compound C1.

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In Vitro Model Blast phase chronic myelogenous leukemia, BCR-ABL1 positive, Chronic myeloid leukemia K562 cells (TNF) CVCL_0004
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50) > 15 ug/mL Negative TNF expression (TNF-)
Method Description
ADC1-ADC27 with a DAR value of ~4 were screened in a GRE luciferase reporter assay in K562 cells over expressing mTNF and wild-type K562 cells to assess potency resulting from targeted delivery vs. nonspecific uptake. All the ADCs were inactive in the wild-type cells, suggesting the activity seen in mTNF over expressed cells was through targeted ADC uptake followed by intracellular release of compound C1.

   Click to Show/Hide
In Vitro Model Blast phase chronic myelogenous leukemia, BCR-ABL1 positive, Chronic myeloid leukemia K562 cells (wt) CVCL_0004
38283215 ADC 19 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50)
1.03 ug/mL
High TNF expression (TNF +++)
Method Description
ADC1-ADC27 with a DAR value of ~4 were screened in a GRE luciferase reporter assay in K562 cells over expressing mTNF and wild-type K562 cells to assess potency resulting from targeted delivery vs. nonspecific uptake. All the ADCs were inactive in the wild-type cells, suggesting the activity seen in mTNF over expressed cells was through targeted ADC uptake followed by intracellular release of compound C1.

   Click to Show/Hide
In Vitro Model Blast phase chronic myelogenous leukemia, BCR-ABL1 positive, Chronic myeloid leukemia K562 cells (TNF) CVCL_0004
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50) > 13 ug/mL Negative TNF expression (TNF-)
Method Description
ADC1-ADC27 with a DAR value of ~4 were screened in a GRE luciferase reporter assay in K562 cells over expressing mTNF and wild-type K562 cells to assess potency resulting from targeted delivery vs. nonspecific uptake. All the ADCs were inactive in the wild-type cells, suggesting the activity seen in mTNF over expressed cells was through targeted ADC uptake followed by intracellular release of compound C1.

   Click to Show/Hide
In Vitro Model Blast phase chronic myelogenous leukemia, BCR-ABL1 positive, Chronic myeloid leukemia K562 cells (wt) CVCL_0004
38283215 ADC 15 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50)
1.05 ug/mL
High TNF expression (TNF +++)
Method Description
ADC1-ADC27 with a DAR value of ~4 were screened in a GRE luciferase reporter assay in K562 cells over expressing mTNF and wild-type K562 cells to assess potency resulting from targeted delivery vs. nonspecific uptake. All the ADCs were inactive in the wild-type cells, suggesting the activity seen in mTNF over expressed cells was through targeted ADC uptake followed by intracellular release of compound C1.

   Click to Show/Hide
In Vitro Model Blast phase chronic myelogenous leukemia, BCR-ABL1 positive, Chronic myeloid leukemia K562 cells (TNF) CVCL_0004
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50) > 29 ug/mL Negative TNF expression (TNF-)
Method Description
ADC1-ADC27 with a DAR value of ~4 were screened in a GRE luciferase reporter assay in K562 cells over expressing mTNF and wild-type K562 cells to assess potency resulting from targeted delivery vs. nonspecific uptake. All the ADCs were inactive in the wild-type cells, suggesting the activity seen in mTNF over expressed cells was through targeted ADC uptake followed by intracellular release of compound C1.

   Click to Show/Hide
In Vitro Model Blast phase chronic myelogenous leukemia, BCR-ABL1 positive, Chronic myeloid leukemia K562 cells (wt) CVCL_0004
38283215 ADC 17 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50)
1.08 ug/mL
High TNF expression (TNF +++)
Method Description
ADC1-ADC27 with a DAR value of ~4 were screened in a GRE luciferase reporter assay in K562 cells over expressing mTNF and wild-type K562 cells to assess potency resulting from targeted delivery vs. nonspecific uptake. All the ADCs were inactive in the wild-type cells, suggesting the activity seen in mTNF over expressed cells was through targeted ADC uptake followed by intracellular release of compound C1.

   Click to Show/Hide
In Vitro Model Blast phase chronic myelogenous leukemia, BCR-ABL1 positive, Chronic myeloid leukemia K562 cells (TNF) CVCL_0004
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50) > 50 ug/mL Negative TNF expression (TNF-)
Method Description
ADC1-ADC27 with a DAR value of ~4 were screened in a GRE luciferase reporter assay in K562 cells over expressing mTNF and wild-type K562 cells to assess potency resulting from targeted delivery vs. nonspecific uptake. All the ADCs were inactive in the wild-type cells, suggesting the activity seen in mTNF over expressed cells was through targeted ADC uptake followed by intracellular release of compound C1.

   Click to Show/Hide
In Vitro Model Blast phase chronic myelogenous leukemia, BCR-ABL1 positive, Chronic myeloid leukemia K562 cells (wt) CVCL_0004
38283215 ADC 24 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50)
1.26 ug/mL
High TNF expression (TNF +++)
Method Description
ADC1-ADC27 with a DAR value of ~4 were screened in a GRE luciferase reporter assay in K562 cells over expressing mTNF and wild-type K562 cells to assess potency resulting from targeted delivery vs. nonspecific uptake. All the ADCs were inactive in the wild-type cells, suggesting the activity seen in mTNF over expressed cells was through targeted ADC uptake followed by intracellular release of compound C1.

   Click to Show/Hide
In Vitro Model Blast phase chronic myelogenous leukemia, BCR-ABL1 positive, Chronic myeloid leukemia K562 cells (TNF) CVCL_0004
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50) > 19 ug/mL Negative TNF expression (TNF-)
Method Description
ADC1-ADC27 with a DAR value of ~4 were screened in a GRE luciferase reporter assay in K562 cells over expressing mTNF and wild-type K562 cells to assess potency resulting from targeted delivery vs. nonspecific uptake. All the ADCs were inactive in the wild-type cells, suggesting the activity seen in mTNF over expressed cells was through targeted ADC uptake followed by intracellular release of compound C1.

   Click to Show/Hide
In Vitro Model Blast phase chronic myelogenous leukemia, BCR-ABL1 positive, Chronic myeloid leukemia K562 cells (wt) CVCL_0004
38283215 ADC 11 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50)
1.4 ug/mL
High TNF expression (TNF +++)
Method Description
ADC1-ADC27 with a DAR value of ~4 were screened in a GRE luciferase reporter assay in K562 cells over expressing mTNF and wild-type K562 cells to assess potency resulting from targeted delivery vs. nonspecific uptake. All the ADCs were inactive in the wild-type cells, suggesting the activity seen in mTNF over expressed cells was through targeted ADC uptake followed by intracellular release of compound C1.

   Click to Show/Hide
In Vitro Model Blast phase chronic myelogenous leukemia, BCR-ABL1 positive, Chronic myeloid leukemia K562 cells (TNF) CVCL_0004
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50) > 50 ug/mL Negative TNF expression (TNF-)
Method Description
ADC1-ADC27 with a DAR value of ~4 were screened in a GRE luciferase reporter assay in K562 cells over expressing mTNF and wild-type K562 cells to assess potency resulting from targeted delivery vs. nonspecific uptake. All the ADCs were inactive in the wild-type cells, suggesting the activity seen in mTNF over expressed cells was through targeted ADC uptake followed by intracellular release of compound C1.

   Click to Show/Hide
In Vitro Model Blast phase chronic myelogenous leukemia, BCR-ABL1 positive, Chronic myeloid leukemia K562 cells (wt) CVCL_0004
38283215 ADC 9 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50)
1.49 ug/mL
High TNF expression (TNF +++)
Method Description
ADC1-ADC27 with a DAR value of ~4 were screened in a GRE luciferase reporter assay in K562 cells over expressing mTNF and wild-type K562 cells to assess potency resulting from targeted delivery vs. nonspecific uptake. All the ADCs were inactive in the wild-type cells, suggesting the activity seen in mTNF over expressed cells was through targeted ADC uptake followed by intracellular release of compound C1.

   Click to Show/Hide
In Vitro Model Blast phase chronic myelogenous leukemia, BCR-ABL1 positive, Chronic myeloid leukemia K562 cells (TNF) CVCL_0004
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50) > 44 ug/mL Negative TNF expression (TNF-)
Method Description
ADC1-ADC27 with a DAR value of ~4 were screened in a GRE luciferase reporter assay in K562 cells over expressing mTNF and wild-type K562 cells to assess potency resulting from targeted delivery vs. nonspecific uptake. All the ADCs were inactive in the wild-type cells, suggesting the activity seen in mTNF over expressed cells was through targeted ADC uptake followed by intracellular release of compound C1.

   Click to Show/Hide
In Vitro Model Blast phase chronic myelogenous leukemia, BCR-ABL1 positive, Chronic myeloid leukemia K562 cells (wt) CVCL_0004
38283215 ADC 18 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50)
1.69 ug/mL
High TNF expression (TNF +++)
Method Description
ADC1-ADC27 with a DAR value of ~4 were screened in a GRE luciferase reporter assay in K562 cells over expressing mTNF and wild-type K562 cells to assess potency resulting from targeted delivery vs. nonspecific uptake. All the ADCs were inactive in the wild-type cells, suggesting the activity seen in mTNF over expressed cells was through targeted ADC uptake followed by intracellular release of compound C1.

   Click to Show/Hide
In Vitro Model Blast phase chronic myelogenous leukemia, BCR-ABL1 positive, Chronic myeloid leukemia K562 cells (TNF) CVCL_0004
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50) > 20 ug/mL Negative TNF expression (TNF-)
Method Description
ADC1-ADC27 with a DAR value of ~4 were screened in a GRE luciferase reporter assay in K562 cells over expressing mTNF and wild-type K562 cells to assess potency resulting from targeted delivery vs. nonspecific uptake. All the ADCs were inactive in the wild-type cells, suggesting the activity seen in mTNF over expressed cells was through targeted ADC uptake followed by intracellular release of compound C1.

   Click to Show/Hide
In Vitro Model Blast phase chronic myelogenous leukemia, BCR-ABL1 positive, Chronic myeloid leukemia K562 cells (wt) CVCL_0004
References
Ref 1 Impact of dipeptide on ADC physicochemical properties and efficacy identifies Ala-Ala as the optimal dipeptide