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Assay Detail

CHEMBL989836

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
27
Total Activities
27
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

In vivo active aldosterone synthase inhibitors with improved selectivity: lead optimization providing a series of pyridine substituted 3,4-dihydro-1H-quinolin-2-one derivatives.
Lucas S, Heim R, Ries C, Schewe KE, Birk B, Hartmann RW.
J Med Chem (2008) 51 : 8077 -8087
PubMed 19049427 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 27 6.08 8.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL451505 1 8.16
CHEMBL9298 FADROZOLE 2.0 1 8.00
CHEMBL456390 1 7.48
CHEMBL457856 1 7.06
CHEMBL499007 1 6.72
CHEMBL461884 1 6.54
CHEMBL457646 1 6.47
CHEMBL509971 1 6.28
CHEMBL511329 1 6.24
CHEMBL459970 1 6.13
CHEMBL446083 1 6.13
CHEMBL508155 1 6.11
CHEMBL448743 1 6.09
CHEMBL460178 1 5.94
CHEMBL457640 1 5.78
CHEMBL461457 1 5.70
CHEMBL462093 1 5.40
CHEMBL459969 1 5.36
CHEMBL461458 1 5.31
CHEMBL457425 1 5.29
CHEMBL457858 1 5.27
CHEMBL459071 1 5.22
CHEMBL461885 1 5.22
CHEMBL62811 1 5.17
CHEMBL462092 1 4.87
CHEMBL457639 1 -
CHEMBL456391 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL451505 IC50 = 6.9 nM 8.16
CHEMBL9298 FADROZOLE IC50 = 10.0 nM 8.00
CHEMBL456390 IC50 = 33.0 nM 7.48
CHEMBL457856 IC50 = 87.0 nM 7.06
CHEMBL499007 IC50 = 191.0 nM 6.72
CHEMBL461884 IC50 = 290.0 nM 6.54
CHEMBL457646 IC50 = 339.0 nM 6.47
CHEMBL509971 IC50 = 525.0 nM 6.28
CHEMBL511329 IC50 = 580.0 nM 6.24
CHEMBL459970 IC50 = 745.0 nM 6.13
CHEMBL446083 IC50 = 742.0 nM 6.13
CHEMBL508155 IC50 = 769.0 nM 6.11
CHEMBL448743 IC50 = 819.0 nM 6.09
CHEMBL460178 IC50 = 1145.0 nM 5.94
CHEMBL457640 IC50 = 1671.0 nM 5.78
CHEMBL461457 IC50 = 1977.0 nM 5.70
CHEMBL462093 IC50 = 3964.0 nM 5.40
CHEMBL459969 IC50 = 4371.0 nM 5.36
CHEMBL461458 IC50 = 4921.0 nM 5.31
CHEMBL457425 IC50 = 5177.0 nM 5.29
CHEMBL457858 IC50 = 5402.0 nM 5.27
CHEMBL459071 IC50 = 5952.0 nM 5.22
CHEMBL461885 IC50 = 5970.0 nM 5.22
CHEMBL62811 IC50 = 6746.0 nM 5.17
CHEMBL462092 IC50 = 13378.0 nM 4.87
CHEMBL457639 IC50 - -
CHEMBL456391 IC50 - -