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Assay Detail

CHEMBL887415

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

Binding
Binding affinity to human AR
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Androgen receptor (CHEMBL1871)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Tandem optimization of target activity and elimination of mutagenic potential in a potent series of N-aryl bicyclic hydantoin-based selective androgen receptor modulators.
Hamann LG, Manfredi MC, Sun C, Krystek SR, Huang Y, Bi Y, Augeri DJ, Wang T, Zou Y, Betebenner DA, Fura A, Seethala R, Golla R, Kuhns JE, Lupisella JA, Darienzo CJ, Custer LL, Price JL, Johnson JM, Biller SA, Zahler R, Ostrowski J.
Bioorg Med Chem Lett (2007) 17 : 1860 -1864
PubMed 17292608 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 26 8.27 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL231122 1 9.15
CHEMBL398226 1 8.92
CHEMBL390849 1 8.89
CHEMBL230052 1 8.82
CHEMBL229264 1 8.68
CHEMBL230694 1 8.54
CHEMBL394592 1 8.52
CHEMBL425646 1 8.49
CHEMBL397217 1 8.48
CHEMBL230695 1 8.43
CHEMBL231015 1 8.37
CHEMBL389607 1 8.35
CHEMBL394593 1 8.21
CHEMBL388421 1 8.11
CHEMBL231014 1 8.10
CHEMBL231327 1 8.10
CHEMBL395502 1 8.09
CHEMBL389606 1 8.07
CHEMBL231328 1 7.85
CHEMBL397274 1 7.68
CHEMBL439873 1 7.62
CHEMBL388210 1 7.47
CHEMBL230053 1 7.32
CHEMBL230594 1 -
CHEMBL389805 1 -
CHEMBL231121 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL231122 Ki = 0.7 nM 9.15
CHEMBL398226 Ki = 1.2 nM 8.92
CHEMBL390849 Ki = 1.3 nM 8.89
CHEMBL230052 Ki = 1.5 nM 8.82
CHEMBL229264 Ki = 2.1 nM 8.68
CHEMBL230694 Ki = 2.9 nM 8.54
CHEMBL394592 Ki = 3.0 nM 8.52
CHEMBL425646 Ki = 3.2 nM 8.49
CHEMBL397217 Ki = 3.3 nM 8.48
CHEMBL230695 Ki = 3.7 nM 8.43
CHEMBL231015 Ki = 4.3 nM 8.37
CHEMBL389607 Ki = 4.5 nM 8.35
CHEMBL394593 Ki = 6.1 nM 8.21
CHEMBL388421 Ki = 7.8 nM 8.11
CHEMBL231014 Ki = 8.0 nM 8.10
CHEMBL231327 Ki = 7.9 nM 8.10
CHEMBL395502 Ki = 8.1 nM 8.09
CHEMBL389606 Ki = 8.5 nM 8.07
CHEMBL231328 Ki = 14.0 nM 7.85
CHEMBL397274 Ki = 21.0 nM 7.68
CHEMBL439873 Ki = 24.0 nM 7.62
CHEMBL388210 Ki = 34.0 nM 7.47
CHEMBL230053 Ki = 48.0 nM 7.32
CHEMBL230594 Ki - -
CHEMBL389805 Ki - -
CHEMBL231121 Ki - -