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Assay Detail

CHEMBL2340955

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

Binding
Inhibition of human CYP11B1 expressed in hamster V79MZh cells using [1,2-3H]-11-deoxycorticosterone as substrate
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type V79MZh
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Modulation of cytochromes P450 with xanthone-based molecules: from aromatase to aldosterone synthase and steroid 11β-hydroxylase inhibition.
Gobbi S, Hu Q, Negri M, Zimmer C, Belluti F, Rampa A, Hartmann RW, Bisi A.
J Med Chem (2013) 56 : 1723 -1729
PubMed 23363058 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 7.49 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2333326 1 9.30
CHEMBL2333334 1 8.26
CHEMBL9298 FADROZOLE 2.0 1 8.20
CHEMBL78322 1 8.17
CHEMBL2333333 1 7.88
CHEMBL442373 1 7.87
CHEMBL2333327 1 7.72
CHEMBL307160 1 7.65
CHEMBL2333332 1 7.61
CHEMBL2333330 1 7.59
CHEMBL2333329 1 7.10
CHEMBL2333331 1 7.03
CHEMBL1083652 1 7.00
CHEMBL2333328 1 6.81
CHEMBL2333335 1 6.57
CHEMBL2333336 1 6.38
CHEMBL2333337 1 6.11

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2333326 IC50 = 0.5 nM 9.30
CHEMBL2333334 IC50 = 5.5 nM 8.26
CHEMBL9298 FADROZOLE IC50 = 6.3 nM 8.20
CHEMBL78322 IC50 = 6.7 nM 8.17
CHEMBL2333333 IC50 = 13.1 nM 7.88
CHEMBL442373 IC50 = 13.4 nM 7.87
CHEMBL2333327 IC50 = 19.2 nM 7.72
CHEMBL307160 IC50 = 22.3 nM 7.65
CHEMBL2333332 IC50 = 24.4 nM 7.61
CHEMBL2333330 IC50 = 25.4 nM 7.59
CHEMBL2333329 IC50 = 80.1 nM 7.10
CHEMBL2333331 IC50 = 92.5 nM 7.03
CHEMBL1083652 IC50 = 99.1 nM 7.00
CHEMBL2333328 IC50 = 156.3 nM 6.81
CHEMBL2333335 IC50 = 268.4 nM 6.57
CHEMBL2333336 IC50 = 415.8 nM 6.38
CHEMBL2333337 IC50 = 785.3 nM 6.11