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Assay Detail

CHEMBL1768362

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

Binding
Inhibition of human CYP11B2 expressed in hamster V79 MZh cells assessed as conversion of [4-14C]-11-deoxycorticosterone substrate by HPTLC assay
33
Total Activities
33
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 11B2, mitochondrial (CHEMBL2722)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Fine-tuning the selectivity of aldosterone synthase inhibitors: structure-activity and structure-selectivity insights from studies of heteroaryl substituted 1,2,5,6-tetrahydropyrrolo[3,2,1-ij]quinolin-4-one derivatives.
Lucas S, Negri M, Heim R, Zimmer C, Hartmann RW.
J Med Chem (2011) 54 : 2307 -2319
PubMed 21384875 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 33 8.54 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1765214 1 9.70
CHEMBL1765215 1 9.70
CHEMBL1765207 1 9.22
CHEMBL1765220 1 9.15
CHEMBL1765222 1 9.05
CHEMBL1765208 1 9.05
CHEMBL9298 FADROZOLE 2.0 1 9.00
CHEMBL1765209 1 9.00
CHEMBL1765205 1 8.96
CHEMBL1765232 1 8.92
CHEMBL1765229 1 8.92
CHEMBL1765219 1 8.89
CHEMBL1765228 1 8.85
CHEMBL1765221 1 8.85
CHEMBL1765210 1 8.66
CHEMBL1765224 1 8.64
CHEMBL1765226 1 8.62
CHEMBL1765206 1 8.62
CHEMBL446083 1 8.59
CHEMBL1765223 1 8.44
CHEMBL1765211 1 8.37
CHEMBL1765212 1 8.36
CHEMBL1765227 1 8.34
CHEMBL1765213 1 8.23
CHEMBL1765230 1 7.80
CHEMBL1765225 1 7.75
CHEMBL457425 1 7.66
CHEMBL62811 1 7.55
CHEMBL1765231 1 7.48
CHEMBL1765217 1 7.25

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1765214 IC50 = 0.2 nM 9.70
CHEMBL1765215 IC50 = 0.2 nM 9.70
CHEMBL1765207 IC50 = 0.6 nM 9.22
CHEMBL1765220 IC50 = 0.7 nM 9.15
CHEMBL1765222 IC50 = 0.9 nM 9.05
CHEMBL1765208 IC50 = 0.9 nM 9.05
CHEMBL9298 FADROZOLE IC50 = 1.0 nM 9.00
CHEMBL1765209 IC50 = 1.0 nM 9.00
CHEMBL1765205 IC50 = 1.1 nM 8.96
CHEMBL1765232 IC50 = 1.2 nM 8.92
CHEMBL1765229 IC50 = 1.2 nM 8.92
CHEMBL1765219 IC50 = 1.3 nM 8.89
CHEMBL1765228 IC50 = 1.4 nM 8.85
CHEMBL1765221 IC50 = 1.4 nM 8.85
CHEMBL1765210 IC50 = 2.2 nM 8.66
CHEMBL1765224 IC50 = 2.3 nM 8.64
CHEMBL1765226 IC50 = 2.4 nM 8.62
CHEMBL1765206 IC50 = 2.4 nM 8.62
CHEMBL446083 IC50 = 2.6 nM 8.59
CHEMBL1765223 IC50 = 3.6 nM 8.44
CHEMBL1765211 IC50 = 4.3 nM 8.37
CHEMBL1765212 IC50 = 4.4 nM 8.36
CHEMBL1765227 IC50 = 4.6 nM 8.34
CHEMBL1765213 IC50 = 5.9 nM 8.23
CHEMBL1765230 IC50 = 16.0 nM 7.80
CHEMBL1765225 IC50 = 18.0 nM 7.75
CHEMBL457425 IC50 = 22.0 nM 7.66
CHEMBL62811 IC50 = 28.0 nM 7.55
CHEMBL1765231 IC50 = 33.0 nM 7.48
CHEMBL1765217 IC50 = 56.0 nM 7.25
CHEMBL1765218 IC50 = 89.0 nM 7.05
CHEMBL1765216 IC50 - -
CHEMBL1765233 IC50 - -