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Assay Detail

CHEMBL1769806

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

Binding
Inhibition of 17,20 lyase activity in Sprague-Dawley rat testicular microsomes
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Testis
Subcellular Microsomes
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Steroid 17-alpha-hydroxylase/17,20 lyase (CHEMBL4430)
Type SINGLE PROTEIN
Organism Rattus norvegicus

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 7.35 8.08

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1766170 1 8.08
CHEMBL1765101 1 8.00
CHEMBL1766187 1 7.85
CHEMBL1766169 1 7.82
CHEMBL1766176 1 7.77
CHEMBL1766171 1 7.72
CHEMBL1766191 1 7.72
CHEMBL1766180 1 7.62
CHEMBL1766177 1 7.62
CHEMBL1766184 1 7.60
CHEMBL1766174 1 7.55
CHEMBL1766175 1 7.54
CHEMBL1766189 1 7.48
CHEMBL1766172 1 7.48
CHEMBL1766178 1 7.31
CHEMBL1766182 1 7.28
CHEMBL1766183 1 7.21
CHEMBL1766179 1 7.15
CHEMBL1766185 1 7.09
CHEMBL1766173 1 6.92
CHEMBL1766181 1 6.68
CHEMBL1766186 1 6.50
CHEMBL1766192 1 6.35
CHEMBL1766188 1 6.11
CHEMBL1766190 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1766170 IC50 = 8.3 nM 8.08
CHEMBL1765101 IC50 = 10.0 nM 8.00
CHEMBL1766187 IC50 = 14.0 nM 7.85
CHEMBL1766169 IC50 = 15.0 nM 7.82
CHEMBL1766176 IC50 = 17.0 nM 7.77
CHEMBL1766171 IC50 = 19.0 nM 7.72
CHEMBL1766191 IC50 = 19.0 nM 7.72
CHEMBL1766180 IC50 = 24.0 nM 7.62
CHEMBL1766177 IC50 = 24.0 nM 7.62
CHEMBL1766184 IC50 = 25.0 nM 7.60
CHEMBL1766174 IC50 = 28.0 nM 7.55
CHEMBL1766175 IC50 = 29.0 nM 7.54
CHEMBL1766189 IC50 = 33.0 nM 7.48
CHEMBL1766172 IC50 = 33.0 nM 7.48
CHEMBL1766178 IC50 = 49.0 nM 7.31
CHEMBL1766182 IC50 = 53.0 nM 7.28
CHEMBL1766183 IC50 = 62.0 nM 7.21
CHEMBL1766179 IC50 = 71.0 nM 7.15
CHEMBL1766185 IC50 = 81.0 nM 7.09
CHEMBL1766173 IC50 = 120.0 nM 6.92
CHEMBL1766181 IC50 = 210.0 nM 6.68
CHEMBL1766186 IC50 = 320.0 nM 6.50
CHEMBL1766192 IC50 = 450.0 nM 6.35
CHEMBL1766188 IC50 = 770.0 nM 6.11
CHEMBL1766190 IC50 > 1000.0 nM -