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Assay Detail

CHEMBL1769807

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

Binding
Inhibition of human 17,20 lyase activity
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Steroid 17-alpha-hydroxylase/17,20 lyase (CHEMBL3522)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

17,20-Lyase inhibitors. Part 3: Design, synthesis, and structure-activity relationships of biphenylylmethylimidazole derivatives as novel 17,20-lyase inhibitors.
Kaku T, Tsujimoto S, Matsunaga N, Tanaka T, Hara T, Yamaoka M, Kusaka M, Tasaka A.
Bioorg Med Chem (2011) 19 : 2428 -2442
PubMed 21429754 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 7.30 7.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1766169 1 7.75
CHEMBL1766170 1 7.72
CHEMBL1766180 1 7.68
CHEMBL1766191 1 7.66
CHEMBL1766176 1 7.62
CHEMBL1766189 1 7.58
CHEMBL1766187 1 7.58
CHEMBL1766174 1 7.57
CHEMBL1766175 1 7.55
CHEMBL1766172 1 7.48
CHEMBL1766182 1 7.44
CHEMBL1766183 1 7.42
CHEMBL1766184 1 7.40
CHEMBL1766178 1 7.36
CHEMBL1766185 1 7.35
CHEMBL1766171 1 7.31
CHEMBL1766173 1 7.27
CHEMBL1766186 1 7.11
CHEMBL1766190 1 7.04
CHEMBL1766177 1 6.92
CHEMBL1765101 1 6.89
CHEMBL1766181 1 6.82
CHEMBL1766179 1 6.80
CHEMBL1766192 1 6.62
CHEMBL1766188 1 6.47

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1766169 IC50 = 18.0 nM 7.75
CHEMBL1766170 IC50 = 19.0 nM 7.72
CHEMBL1766180 IC50 = 21.0 nM 7.68
CHEMBL1766191 IC50 = 22.0 nM 7.66
CHEMBL1766176 IC50 = 24.0 nM 7.62
CHEMBL1766189 IC50 = 26.0 nM 7.58
CHEMBL1766187 IC50 = 26.0 nM 7.58
CHEMBL1766174 IC50 = 27.0 nM 7.57
CHEMBL1766175 IC50 = 28.0 nM 7.55
CHEMBL1766172 IC50 = 33.0 nM 7.48
CHEMBL1766182 IC50 = 36.0 nM 7.44
CHEMBL1766183 IC50 = 38.0 nM 7.42
CHEMBL1766184 IC50 = 40.0 nM 7.40
CHEMBL1766178 IC50 = 44.0 nM 7.36
CHEMBL1766185 IC50 = 45.0 nM 7.35
CHEMBL1766171 IC50 = 49.0 nM 7.31
CHEMBL1766173 IC50 = 54.0 nM 7.27
CHEMBL1766186 IC50 = 77.0 nM 7.11
CHEMBL1766190 IC50 = 92.0 nM 7.04
CHEMBL1766177 IC50 = 120.0 nM 6.92
CHEMBL1765101 IC50 = 130.0 nM 6.89
CHEMBL1766181 IC50 = 150.0 nM 6.82
CHEMBL1766179 IC50 = 160.0 nM 6.80
CHEMBL1766192 IC50 = 240.0 nM 6.62
CHEMBL1766188 IC50 = 340.0 nM 6.47