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Assay Detail

CHEMBL5329971

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

ADMET
Inhibition of human CYP11B1 expressed in human NCI-H295 cells incubated for 48 hrs by radioimmuno assay
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Homo sapiens
Cell Type NCI-H295
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Fluorinated aldosterone synthase (CYP11B2)-inhibitors for differential diagnosis between bilateral and unilateral conditions of primary aldosteronism.
Maier P, Heinze B, Gabor S, Reese S, Hahner S, Schirbel A.
Bioorg Med Chem Lett (2023) 96 : 129501 -129501
PubMed 37804995 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 6.92 7.81

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5413320 1 7.81
CHEMBL5408597 1 7.68
CHEMBL5402622 1 7.62
CHEMBL5409957 1 7.61
CHEMBL5413659 1 7.32
CHEMBL5417708 1 7.25
CHEMBL5414558 1 7.19
CHEMBL287677 DEXFADROSTAT 2.0 1 6.99
CHEMBL5418063 1 6.97
CHEMBL5400111 1 6.81
CHEMBL5412612 1 6.80
CHEMBL5398781 1 6.64
CHEMBL5420707 1 6.59
CHEMBL5426685 1 6.56
CHEMBL5401923 1 6.49
CHEMBL5405085 1 6.33
CHEMBL5410140 1 6.33
CHEMBL5438181 1 6.27
CHEMBL5405763 1 6.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5413320 IC50 = 15.5 nM 7.81
CHEMBL5408597 IC50 = 20.8 nM 7.68
CHEMBL5402622 IC50 = 23.7 nM 7.62
CHEMBL5409957 IC50 = 24.3 nM 7.61
CHEMBL5413659 IC50 = 47.8 nM 7.32
CHEMBL5417708 IC50 = 56.0 nM 7.25
CHEMBL5414558 IC50 = 64.8 nM 7.19
CHEMBL287677 DEXFADROSTAT IC50 = 102.0 nM 6.99
CHEMBL5418063 IC50 = 106.0 nM 6.97
CHEMBL5400111 IC50 = 156.0 nM 6.81
CHEMBL5412612 IC50 = 157.0 nM 6.80
CHEMBL5398781 IC50 = 229.0 nM 6.64
CHEMBL5420707 IC50 = 258.0 nM 6.59
CHEMBL5426685 IC50 = 276.0 nM 6.56
CHEMBL5401923 IC50 = 324.0 nM 6.49
CHEMBL5405085 IC50 = 469.0 nM 6.33
CHEMBL5410140 IC50 = 462.0 nM 6.33
CHEMBL5438181 IC50 = 532.0 nM 6.27
CHEMBL5405763 IC50 = 595.0 nM 6.22