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Assay Detail

CHEMBL808554

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

Binding
Inhibition of recombinant steroid 5-alpha-reductase type I
26
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

3-oxo-5-alpha-steroid 4-dehydrogenase 1 (CHEMBL1787)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-activity relationships for inhibition of type 1 and 2 human 5 alpha-reductase and human adrenal 3 beta-hydroxy-delta 5-steroid dehydrogenase/3-keto-delta 5-steroid isomerase by 6-azaandrost-4-en-3-ones: optimization of the C17 substituent.
Frye SV, Haffner CD, Maloney PR, Hiner RN, Dorsey GF, Noe RA, Unwalla RJ, Batchelor KW, Bramson HN, Stuart JD.
J Med Chem (1995) 38 : 2621 -2627
PubMed 7629802 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 26 8.40 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2115222 2 9.70
CHEMBL445627 1 9.70
CHEMBL283123 1 9.52
CHEMBL421735 1 9.30
CHEMBL283430 1 9.22
CHEMBL87805 1 8.89
CHEMBL88032 1 8.82
CHEMBL314309 1 8.52
CHEMBL90440 1 8.51
CHEMBL328670 1 8.47
CHEMBL88485 1 8.44
CHEMBL327702 1 8.40
CHEMBL314725 1 8.38
CHEMBL87082 1 8.34
CHEMBL89327 1 8.30
CHEMBL314977 1 8.28
CHEMBL314953 1 8.17
CHEMBL89557 1 8.17
CHEMBL87021 1 8.12
CHEMBL25516 1 8.10
CHEMBL277224 1 8.06
CHEMBL89240 1 7.58
CHEMBL88494 1 7.57
CHEMBL280155 1 6.62
CHEMBL314069 1 5.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL445627 Ki = 0.2 nM 9.70
CHEMBL2115222 Ki = 0.2 nM 9.70
CHEMBL283123 Ki = 0.3 nM 9.52
CHEMBL421735 Ki = 0.5 nM 9.30
CHEMBL283430 Ki = 0.6 nM 9.22
CHEMBL2115222 Ki = 0.6 nM 9.22
CHEMBL87805 Ki = 1.3 nM 8.89
CHEMBL88032 Ki = 1.5 nM 8.82
CHEMBL314309 Ki = 3.0 nM 8.52
CHEMBL90440 Ki = 3.1 nM 8.51
CHEMBL328670 Ki = 3.4 nM 8.47
CHEMBL88485 Ki = 3.6 nM 8.44
CHEMBL327702 Ki = 4.0 nM 8.40
CHEMBL314725 Ki = 4.2 nM 8.38
CHEMBL87082 Ki = 4.6 nM 8.34
CHEMBL89327 Ki = 5.0 nM 8.30
CHEMBL314977 Ki = 5.3 nM 8.28
CHEMBL89557 Ki = 6.7 nM 8.17
CHEMBL314953 Ki = 6.8 nM 8.17
CHEMBL87021 Ki = 7.5 nM 8.12
CHEMBL25516 Ki = 8.0 nM 8.10
CHEMBL277224 Ki = 8.8 nM 8.06
CHEMBL89240 Ki = 26.0 nM 7.58
CHEMBL88494 Ki = 27.0 nM 7.57
CHEMBL280155 Ki = 240.0 nM 6.62
CHEMBL314069 Ki = 1100.0 nM 5.96