General Information of This Payload
Payload ID
PAY0LFXNZ
Name
B63
Synonyms
B63
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Target Eukaryotic peptide chain release factor GTP-binding subunit ERF3A (GSPT1)
Structure
Formula
C27H30ClN5O5
Isosmiles
O=C1C(C=CC(CNC(NC(C=C2)=CC(Cl)=C2CCCOC3CNC3)=O)=C4)=C4CN1C(CCC5=O)C(N5)=O
InChI
InChI=1S/C27H30ClN5O5/c28-22-11-19(5-4-17(22)2-1-9-38-20-13-29-14-20)31-27(37)30-12-16-3-6-21-18(10-16)15-33(26(21)36)23-7-8-24(34)32-25(23)35/h3-6,10-11,20,23,29H,1-2,7-9,12-15H2,(H2,30,31,37)(H,32,34,35)
InChIKey
XSSRZNVPRIWHLV-UHFFFAOYSA-N
Pharmaceutical Properties
Molecule Weight
540.02
Polar area
128.87
Complexity
1216.594577
xlogp Value
2.3437
Heavy Count
38
Rot Bonds
9
Hbond acc
6
Hbond Donor
4
The activity data of This Payload
Standard Type Value Units Cell line Disease Model Cell line ID Reference
Half maximal inhibitory Concentration (lC50) <10 nM
HL-60 cells
Adult acute myeloid leukemia
CVCL_0002 
[1]
Half maximal inhibitory Concentration (lC50) <10 nM
HL-60 cells
Adult acute myeloid leukemia
CVCL_0002 
[1]
Half maximal inhibitory Concentration (lC50) <10 nM
SK-BR-3 cells
Breast adenocarcinoma
CVCL_0033 
[1]
Half maximal inhibitory Concentration (lC50) <10 nM
SK-BR-3 cells
Breast adenocarcinoma
CVCL_0033 
[1]
Half maximal inhibitory Concentration (lC50) <10 nM
NCI-H929 cells
Plasma cell myeloma
CVCL_1600 
[1]
Half maximal inhibitory Concentration (lC50) <10 nM
NCI-H929 cells
Plasma cell myeloma
CVCL_1600 
[1]
Half maximal inhibitory Concentration (lC50) 10-50 nM
Ramos cells
Burkitt lymphoma
CVCL_0597 
[1]
Half maximal inhibitory Concentration (lC50) 10-50 nM
Ramos cells
Burkitt lymphoma
CVCL_0597 
[1]
Half maximal inhibitory Concentration (lC50) 10-50 nM
NCI-H82 cells
Lung small cell carcinoma
CVCL_1591 
[1]
Half maximal inhibitory Concentration (lC50) 10-50 nM
NCI-H82 cells
Lung small cell carcinoma
CVCL_1591 
[1]
Each Antibody-drug Conjugate Related to This Payload
Full Information of The Activity Data of The ADC(s) Related to This Payload
wO2024222841A1 ADC66 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
6.613 pM
High CD33 expression (CD33+++)
Method Description
Cytotoxicity of ADC to MV4-11 cells
In Vitro Model Childhood acute monocytic leukemia MV4-11 cells CVCL_0064
wO2024222841A1 ADC65 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
6.699 pM
High CD33 expression (CD33+++)
Method Description
Cytotoxicity of ADC to MV4-11 cells
In Vitro Model Childhood acute monocytic leukemia MV4-11 cells CVCL_0064
wO2024169913A1 ADC01-06-4 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
0.02107 nM
High HER2 expression (HER2+++)
Method Description
Cytotoxicity of ADC to SK-BR-3 cells
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
wO2024169913A1 ADC04-07-8 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
0.04488 nM
High DLL3 expression (DLL3+++)
Method Description
Cytotoxicity of ADC to NCI-H82 cells
In Vitro Model Lung small cell carcinoma NCI-H82 cells CVCL_1591
References
Ref 1 Antibody-drug conjugate
Ref 2 Domide molecular glue derivative and use thereof