Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL887414

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

Functional
Agonist activity at human AR
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
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
EC50 26 7.81 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL398226 1 9.22
CHEMBL229264 1 9.15
CHEMBL394592 1 9.00
CHEMBL389607 1 8.77
CHEMBL231122 1 8.77
CHEMBL390849 1 8.77
CHEMBL231014 1 8.66
CHEMBL425646 1 8.64
CHEMBL230052 1 8.55
CHEMBL230694 1 8.44
CHEMBL397274 1 8.21
CHEMBL397217 1 7.44
CHEMBL231015 1 7.33
CHEMBL389606 1 7.28
CHEMBL231328 1 7.10
CHEMBL439873 1 7.01
CHEMBL395502 1 6.66
CHEMBL230053 1 6.46
CHEMBL230695 1 6.31
CHEMBL394593 1 6.22
CHEMBL231327 1 5.97
CHEMBL231121 1 -
CHEMBL389805 1 -
CHEMBL230594 1 -
CHEMBL388421 1 -
CHEMBL388210 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL398226 EC50 = 0.6 nM 9.22
CHEMBL229264 EC50 = 0.7 nM 9.15
CHEMBL394592 EC50 = 1.0 nM 9.00
CHEMBL389607 EC50 = 1.7 nM 8.77
CHEMBL231122 EC50 = 1.7 nM 8.77
CHEMBL390849 EC50 = 1.7 nM 8.77
CHEMBL231014 EC50 = 2.2 nM 8.66
CHEMBL425646 EC50 = 2.3 nM 8.64
CHEMBL230052 EC50 = 2.8 nM 8.55
CHEMBL230694 EC50 = 3.6 nM 8.44
CHEMBL397274 EC50 = 6.2 nM 8.21
CHEMBL397217 EC50 = 36.0 nM 7.44
CHEMBL231015 EC50 = 47.0 nM 7.33
CHEMBL389606 EC50 = 52.0 nM 7.28
CHEMBL231328 EC50 = 79.0 nM 7.10
CHEMBL439873 EC50 = 98.0 nM 7.01
CHEMBL395502 EC50 = 221.0 nM 6.66
CHEMBL230053 EC50 = 345.0 nM 6.46
CHEMBL230695 EC50 = 487.0 nM 6.31
CHEMBL394593 EC50 = 607.0 nM 6.22
CHEMBL231327 EC50 = 1080.0 nM 5.97
CHEMBL231121 EC50 - -
CHEMBL389805 EC50 > 10000.0 nM -
CHEMBL230594 EC50 > 10000.0 nM -
CHEMBL388421 EC50 > 10000.0 nM -
CHEMBL388210 EC50 > 10000.0 nM -