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Assay Detail

CHEMBL5130159

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

ADMET
Inhibition of human CYP11B1 expressed in Chinese hamster V79 MZh cells using [14C]-deoxycorticosteron as substrate measured after 6 hrs by phosphoimager analysis
37
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
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

Design, Synthesis, and Biological Evaluations of Pyridyl 4,5,6,7-Tetrahydro-4,7-Methanobenzo[<i>d</i>]isoxazoles as Potent and Selective Inhibitors of 11β-Hydroxylase.
Yin L, Pan Y, Xue Y, Chen X, You T, Huang J, Xu Q, Hu Q.
J Med Chem (2022) 65 : 11876 -11888
PubMed 35975976 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 37 7.34 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5198576 1 8.70
CHEMBL5177141 1 8.22
CHEMBL3099695 OSILODROSTAT 4.0 1 8.22
CHEMBL5175710 1 8.10
CHEMBL5184829 1 8.05
CHEMBL5209512 1 7.92
CHEMBL5186306 1 7.82
CHEMBL5201480 1 7.77
CHEMBL5174912 1 7.77
CHEMBL5204043 1 7.66
CHEMBL5203687 1 7.60
CHEMBL5171157 1 7.51
CHEMBL5204850 1 7.50
CHEMBL5175708 1 7.46
CHEMBL5195761 1 7.43
CHEMBL5196347 1 7.34
CHEMBL5186765 1 7.34
CHEMBL5175784 1 7.31
CHEMBL5171873 1 7.24
CHEMBL5199220 1 7.19
CHEMBL5197879 1 7.10
CHEMBL5197102 1 7.08
CHEMBL5185819 1 7.07
CHEMBL5202317 1 7.02
CHEMBL5202486 1 7.01
CHEMBL5183554 1 6.97
CHEMBL5204984 1 6.95
CHEMBL5189860 1 6.94
CHEMBL5192747 1 6.89
CHEMBL5171092 1 6.87

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5198576 IC50 = 2.0 nM 8.70
CHEMBL5177141 IC50 = 6.0 nM 8.22
CHEMBL3099695 OSILODROSTAT IC50 = 6.0 nM 8.22
CHEMBL5175710 IC50 = 8.0 nM 8.10
CHEMBL5184829 IC50 = 9.0 nM 8.05
CHEMBL5209512 IC50 = 12.0 nM 7.92
CHEMBL5186306 IC50 = 15.0 nM 7.82
CHEMBL5201480 IC50 = 17.0 nM 7.77
CHEMBL5174912 IC50 = 17.0 nM 7.77
CHEMBL5204043 IC50 = 22.0 nM 7.66
CHEMBL5203687 IC50 = 25.0 nM 7.60
CHEMBL5171157 IC50 = 31.0 nM 7.51
CHEMBL5204850 IC50 = 32.0 nM 7.50
CHEMBL5175708 IC50 = 35.0 nM 7.46
CHEMBL5195761 IC50 = 37.0 nM 7.43
CHEMBL5196347 IC50 = 46.0 nM 7.34
CHEMBL5186765 IC50 = 46.0 nM 7.34
CHEMBL5175784 IC50 = 49.0 nM 7.31
CHEMBL5171873 IC50 = 57.0 nM 7.24
CHEMBL5199220 IC50 = 65.0 nM 7.19
CHEMBL5197879 IC50 = 79.0 nM 7.10
CHEMBL5197102 IC50 = 83.0 nM 7.08
CHEMBL5185819 IC50 = 86.0 nM 7.07
CHEMBL5202317 IC50 = 96.0 nM 7.02
CHEMBL5202486 IC50 = 97.0 nM 7.01
CHEMBL5183554 IC50 = 106.0 nM 6.97
CHEMBL5204984 IC50 = 113.0 nM 6.95
CHEMBL5189860 IC50 = 115.0 nM 6.94
CHEMBL5192747 IC50 = 128.0 nM 6.89
CHEMBL5171092 IC50 = 135.0 nM 6.87
CHEMBL5189922 IC50 = 138.0 nM 6.86
CHEMBL5175297 IC50 = 153.0 nM 6.82
CHEMBL5175134 IC50 = 157.0 nM 6.80
CHEMBL5196053 IC50 = 167.0 nM 6.78
CHEMBL5203488 IC50 = 179.0 nM 6.75
CHEMBL5173465 IC50 = 183.0 nM 6.74
CHEMBL5195876 IC50 = 189.0 nM 6.72