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Assay Detail

CHEMBL648070

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Functional
Antagonistic activity against human androgen receptor (hAR) in CV-1 cells using cotransfection assay
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type CV-1
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Androgen receptor (CHEMBL1871)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

4-Alkyl- and 3,4-dialkyl-1,2,3,4-tetrahydro-8-pyridono[5,6-g]quinolines: potent, nonsteroidal androgen receptor agonists.
Higuchi RI, Edwards JP, Caferro TR, Ringgenberg JD, Kong JW, Hamann LG, Arienti KL, Marschke KB, Davis RL, Farmer LJ, Jones TK.
Bioorg Med Chem Lett (1999) 9 : 1335 -1340
PubMed 10340624 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 6.92 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL286684 1 7.92
CHEMBL281028 1 7.80
CHEMBL27297 1 7.70
CHEMBL2113248 1 7.54
CHEMBL2113247 1 7.20
CHEMBL282866 1 7.14
CHEMBL27413 1 6.67
CHEMBL285602 1 6.60
CHEMBL283449 1 6.59
CHEMBL418198 1 5.57
CHEMBL390728 1 5.34
CHEMBL280865 1 -
CHEMBL27769 STANOLONE 2.0 1 -
CHEMBL27812 1 -
CHEMBL431493 1 -
CHEMBL27945 1 -
CHEMBL27276 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL286684 IC50 = 12.0 nM 7.92
CHEMBL281028 IC50 = 16.0 nM 7.80
CHEMBL27297 IC50 = 20.0 nM 7.70
CHEMBL2113248 IC50 = 29.0 nM 7.54
CHEMBL2113247 IC50 = 63.0 nM 7.20
CHEMBL282866 IC50 = 73.0 nM 7.14
CHEMBL27413 IC50 = 216.0 nM 6.67
CHEMBL285602 IC50 = 251.0 nM 6.60
CHEMBL283449 IC50 = 259.0 nM 6.59
CHEMBL418198 IC50 = 2710.0 nM 5.57
CHEMBL390728 IC50 = 4580.0 nM 5.34
CHEMBL280865 IC50 > 10000.0 nM -
CHEMBL27769 STANOLONE IC50 > 10000.0 nM -
CHEMBL27812 IC50 > 10000.0 nM -
CHEMBL431493 IC50 > 10000.0 nM -
CHEMBL27945 IC50 > 10000.0 nM -
CHEMBL27276 IC50 > 10000.0 nM -