Payload Information

General Information of This Payload
Payload ID
PAY0HAUVI
Name
US12209180B2 P2
Synonyms
P2
   Click to Show/Hide
Structure
Formula
C34H45N3O2
Isosmiles
C[C@]12CCC[C@](C)(C(NC([C@]3(C)[C@]4([H])CCC(C=CC(N)=C5)=C5[C@]4(CCC3)C)=O)=O)[C@]1([H])CCC6=C2C=C(N)C=C6
InChI
InChI=1S/C34H45N3O2/c1-31-15-5-17-33(3,27(31)13-9-21-7-11-23(35)19-25(21)31)29(38)37-30(39)34(4)18-6-16-32(2)26-20-24(36)12-8-22(26)10-14-28(32)34/h7-8,11-12,19-20,27-28H,5-6,9-10,13-18,35-36H2,1-4H3,(H,37,38,39)/t27-,28-,31-,32-,33+,34+/m1/s1
InChIKey
OHDCWFWNGOONHA-PFQVMFNOSA-N
Pharmaceutical Properties
Molecule Weight
527.753
Polar area
98.21
Complexity
1316.006986
xlogp Value
6.2146
Heavy Count
39
Rot Bonds
2
Hbond acc
4
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
H1H21234N-N297Q-LP1 [Investigative]
 ADC Info 
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 Effective Concentration (EC50)
0.738 nM
Positive MSR1 expression (MSR1+++/++)
Method Description
Anti-MSR1-LXR Agonist Conjugate Activity in Differentiated THP-1/LXR-Luc cells
In Vitro Model Acute monoblastic/monocytic leukemia, Childhood acute monocytic leukemia THP-1/LXR-Luc cells CVCL_5115
H1H21234N-N297Q-LP2 [Investigative]
 ADC Info 
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 Effective Concentration (EC50)
0.868 nM
Positive MSR1 expression (MSR1+++/++)
Method Description
Anti-MSR1-LXR Agonist Conjugate Activity in Differentiated THP-4/LXR-Luc cells
In Vitro Model Acute monoblastic/monocytic leukemia, Childhood acute monocytic leukemia THP-1/LXR-Luc cells CVCL_5115
H1H21234N-N297Q-LP4 [Investigative]
 ADC Info 
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 Effective Concentration (EC50)
0.923 nM
Positive MSR1 expression (MSR1+++/++)
Method Description
Anti-MSR1-LXR Agonist Conjugate Activity in Differentiated THP-2/LXR-Luc cells
In Vitro Model Acute monoblastic/monocytic leukemia, Childhood acute monocytic leukemia THP-1/LXR-Luc cells CVCL_5115
H1H21234N-N297Q-LP5 [Investigative]
 ADC Info 
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 Effective Concentration (EC50)
1.2 nM
Positive MSR1 expression (MSR1+++/++)
Method Description
Anti-MSR1-LXR Agonist Conjugate Activity in Differentiated THP-3/LXR-Luc cells
In Vitro Model Acute monoblastic/monocytic leukemia, Childhood acute monocytic leukemia THP-1/LXR-Luc cells CVCL_5115
H1H21234N-N297Q-LP12 [Investigative]
 ADC Info 
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 Effective Concentration (EC50)
1.3 nM
Positive MSR1 expression (MSR1+++/++)
Method Description
Anti-MSR1-LXR Agonist Conjugate Activity in Differentiated THP-4/LXR-Luc cells
In Vitro Model Acute monoblastic/monocytic leukemia, Childhood acute monocytic leukemia THP-1/LXR-Luc cells CVCL_5115
References
Ref 1 Bis-octahydrophenanthrene carboxamide derivatives and protein conjugates thereof for use as LXR agonists