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Assay Detail

CHEMBL2423499

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
32
Total Activities
32
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

Cushing's syndrome: development of highly potent and selective CYP11B1 inhibitors of the (pyridylmethyl)pyridine type.
Emmerich J, Hu Q, Hanke N, Hartmann RW.
J Med Chem (2013) 56 : 6022 -6032
PubMed 23869452 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 32 7.27 8.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2417616 1 8.89
CHEMBL2417553 1 8.70
CHEMBL2417614 1 8.30
CHEMBL2417635 1 8.22
CHEMBL2417637 1 8.10
CHEMBL2417626 1 7.96
CHEMBL2417622 1 7.92
CHEMBL934 METYRAPONE 4.0 1 7.82
CHEMBL2417621 1 7.68
CHEMBL2417625 1 7.68
CHEMBL2417620 1 7.55
CHEMBL2417633 1 7.50
CHEMBL2417619 1 7.48
CHEMBL2417613 1 7.42
CHEMBL2417615 1 7.29
CHEMBL2417627 1 7.22
CHEMBL2011253 1 7.17
CHEMBL2417623 1 7.16
CHEMBL2417632 1 7.06
CHEMBL2417634 1 7.01
CHEMBL428780 1 6.97
CHEMBL2417624 1 6.91
CHEMBL2417612 1 6.90
CHEMBL2417628 1 6.82
CHEMBL2011262 1 6.74
CHEMBL2417636 1 6.62
CHEMBL2417638 1 6.37
CHEMBL2417630 1 6.21
CHEMBL2417617 1 5.99
CHEMBL2417631 1 5.95

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2417616 IC50 = 1.3 nM 8.89
CHEMBL2417553 IC50 = 2.0 nM 8.70
CHEMBL2417614 IC50 = 5.0 nM 8.30
CHEMBL2417635 IC50 = 6.0 nM 8.22
CHEMBL2417637 IC50 = 8.0 nM 8.10
CHEMBL2417626 IC50 = 11.0 nM 7.96
CHEMBL2417622 IC50 = 12.0 nM 7.92
CHEMBL934 METYRAPONE IC50 = 15.0 nM 7.82
CHEMBL2417621 IC50 = 21.0 nM 7.68
CHEMBL2417625 IC50 = 21.0 nM 7.68
CHEMBL2417620 IC50 = 28.0 nM 7.55
CHEMBL2417633 IC50 = 32.0 nM 7.50
CHEMBL2417619 IC50 = 33.0 nM 7.48
CHEMBL2417613 IC50 = 38.0 nM 7.42
CHEMBL2417615 IC50 = 51.0 nM 7.29
CHEMBL2417627 IC50 = 60.0 nM 7.22
CHEMBL2011253 IC50 = 68.0 nM 7.17
CHEMBL2417623 IC50 = 69.0 nM 7.16
CHEMBL2417632 IC50 = 87.0 nM 7.06
CHEMBL2417634 IC50 = 98.0 nM 7.01
CHEMBL428780 IC50 = 107.0 nM 6.97
CHEMBL2417624 IC50 = 124.0 nM 6.91
CHEMBL2417612 IC50 = 125.0 nM 6.90
CHEMBL2417628 IC50 = 151.0 nM 6.82
CHEMBL2011262 IC50 = 181.0 nM 6.74
CHEMBL2417636 IC50 = 240.0 nM 6.62
CHEMBL2417638 IC50 = 427.0 nM 6.37
CHEMBL2417630 IC50 = 610.0 nM 6.21
CHEMBL2417617 IC50 = 1015.0 nM 5.99
CHEMBL2417631 IC50 = 1122.0 nM 5.95
CHEMBL2417629 IC50 = 1711.0 nM 5.77
CHEMBL2417618 IC50 > 5000.0 nM -