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Assay Detail

CHEMBL2169296

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of human CYP11B1 expressed in hamster V79 MZh cells using deoxycorticosterone substrate
19
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type V79 MZh
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cytochrome P450 11B1, mitochondrial (CHEMBL1908)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel imidazol-1-ylmethyl substituted 1,2,5,6-tetrahydropyrrolo[3,2,1-ij]quinolin-4-ones as potent and selective CYP11B1 inhibitors for the treatment of Cushing's syndrome.
Yin L, Lucas S, Maurer F, Kazmaier U, Hu Q, Hartmann RW.
J Med Chem (2012) 55 : 6629 -6633
PubMed 22788843 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 7.72 8.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2163638 1 8.85
CHEMBL2163639 3 8.82
CHEMBL2163640 1 8.47
CHEMBL2163637 1 8.19
CHEMBL2163651 1 7.89
CHEMBL2163636 1 7.77
CHEMBL2163641 1 7.72
CHEMBL2163650 1 7.70
CHEMBL2163644 1 7.57
CHEMBL2163643 1 7.54
CHEMBL2163642 1 7.40
CHEMBL2163646 1 7.40
CHEMBL2163649 1 7.30
CHEMBL2163648 1 7.16
CHEMBL2163645 1 6.96
CHEMBL2163647 1 6.84
CHEMBL2163652 1 6.36

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2163638 IC50 = 1.4 nM 8.85
CHEMBL2163639 IC50 = 1.5 nM 8.82
CHEMBL2163639 IC50 = 2.2 nM 8.66
CHEMBL2163640 IC50 = 3.4 nM 8.47
CHEMBL2163637 IC50 = 6.5 nM 8.19
CHEMBL2163639 IC50 = 10.3 nM 7.99
CHEMBL2163651 IC50 = 13.0 nM 7.89
CHEMBL2163636 IC50 = 17.0 nM 7.77
CHEMBL2163641 IC50 = 19.0 nM 7.72
CHEMBL2163650 IC50 = 20.0 nM 7.70
CHEMBL2163644 IC50 = 27.0 nM 7.57
CHEMBL2163643 IC50 = 29.0 nM 7.54
CHEMBL2163642 IC50 = 40.0 nM 7.40
CHEMBL2163646 IC50 = 40.0 nM 7.40
CHEMBL2163649 IC50 = 50.0 nM 7.30
CHEMBL2163648 IC50 = 70.0 nM 7.16
CHEMBL2163645 IC50 = 110.0 nM 6.96
CHEMBL2163647 IC50 = 144.0 nM 6.84
CHEMBL2163652 IC50 = 438.0 nM 6.36