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Assay Detail

CHEMBL3388885

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

Binding
Inhibition of human CYP11B2 expressed in hamster V79MZh cells using [1,2-3H]-11-deoxycorticosterone as substrate
35
Total Activities
35
Compounds Tested
2
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 11B2, mitochondrial (CHEMBL2722)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Potent 11β-hydroxylase inhibitors with inverse metabolic stability in human plasma and hepatic S9 fractions to promote wound healing.
Zhu W, Hu Q, Hanke N, van Koppen CJ, Hartmann RW.
J Med Chem (2014) 57 : 7811 -7817
PubMed 25176013 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 6.64 8.30
Inhibition 10 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3337694 1 8.30
CHEMBL3337695 1 8.10
CHEMBL3287169 1 7.22
CHEMBL934 METYRAPONE 4.0 1 7.14
CHEMBL3337676 1 7.07
CHEMBL3337683 1 6.71
CHEMBL3337679 1 6.69
CHEMBL3337673 1 6.62
CHEMBL3337664 1 6.60
CHEMBL3337691 1 6.59
CHEMBL3337684 1 6.58
CHEMBL3337677 1 6.53
CHEMBL3337666 1 6.50
CHEMBL3337681 1 6.49
CHEMBL3337685 1 6.46
CHEMBL3337689 1 6.37
CHEMBL3337686 1 6.33
CHEMBL3337667 1 6.30
CHEMBL3337678 1 6.29
CHEMBL3337680 1 6.26
CHEMBL3337690 1 6.25
CHEMBL3337687 1 6.22
CHEMBL3286405 1 6.22
CHEMBL3337672 1 6.07
CHEMBL3337665 1 6.07
CHEMBL3337671 1 -
CHEMBL3337670 1 -
CHEMBL3337674 1 -
CHEMBL3337688 1 -
CHEMBL3337669 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3337694 IC50 = 5.0 nM 8.30
CHEMBL3337695 IC50 = 8.0 nM 8.10
CHEMBL3287169 IC50 = 60.0 nM 7.22
CHEMBL934 METYRAPONE IC50 = 72.0 nM 7.14
CHEMBL3337676 IC50 = 85.0 nM 7.07
CHEMBL3337683 IC50 = 196.0 nM 6.71
CHEMBL3337679 IC50 = 205.0 nM 6.69
CHEMBL3337673 IC50 = 239.0 nM 6.62
CHEMBL3337664 IC50 = 251.0 nM 6.60
CHEMBL3337691 IC50 = 259.0 nM 6.59
CHEMBL3337684 IC50 = 260.0 nM 6.58
CHEMBL3337677 IC50 = 295.0 nM 6.53
CHEMBL3337666 IC50 = 320.0 nM 6.50
CHEMBL3337681 IC50 = 322.0 nM 6.49
CHEMBL3337685 IC50 = 344.0 nM 6.46
CHEMBL3337689 IC50 = 429.0 nM 6.37
CHEMBL3337686 IC50 = 469.0 nM 6.33
CHEMBL3337667 IC50 = 500.0 nM 6.30
CHEMBL3337678 IC50 = 519.0 nM 6.29
CHEMBL3337680 IC50 = 555.0 nM 6.26
CHEMBL3337690 IC50 = 557.0 nM 6.25
CHEMBL3337687 IC50 = 607.0 nM 6.22
CHEMBL3286405 IC50 = 608.0 nM 6.22
CHEMBL3337672 IC50 = 850.0 nM 6.07
CHEMBL3337665 IC50 = 850.0 nM 6.07
CHEMBL3337668 Inhibition = 34.0 % -
CHEMBL3337693 Inhibition = 47.0 % -
CHEMBL3337692 Inhibition = 28.0 % -
CHEMBL3337675 Inhibition = 7.0 % -
CHEMBL3337682 Inhibition = 47.0 % -
CHEMBL3337669 Inhibition = 41.0 % -
CHEMBL3337688 Inhibition = 22.0 % -
CHEMBL3337674 Inhibition = 10.0 % -
CHEMBL3337670 Inhibition = 8.0 % -
CHEMBL3337671 Inhibition = 38.0 % -