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Assay Detail

CHEMBL916636

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Functional
Agonist activity at human androgen receptor expressed in CV1 cells by transcriptional activation assay
ChEMBL ↗
68
Total Activities
32
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CV-1
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Androgen receptor (CHEMBL1871) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel series of potent, nonsteroidal, selective androgen receptor modulators based on 7H-[1,4]oxazino[3,2-g]quinolin-7-ones.
Higuchi RI, Arienti KL, López FJ, Mani NS, Mais DE, Caferro TR, Long YO, Jones TK, Edwards JP, Zhi L, Schrader WT, Negro-Vilar A, Marschke KB.
J Med Chem (2007) 50 : 2486 -2496
PubMed 17439112 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Efficacy 34 - -
EC50 34 8.13 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1445 FLUOXYMESTERONE 4.0 2 9.52
CHEMBL224263 — — 2 8.96
CHEMBL227784 — — 2 8.85
CHEMBL227394 — — 2 8.72
CHEMBL389481 — — 2 8.64
CHEMBL227590 — — 2 8.62
CHEMBL226558 — — 2 8.57
CHEMBL227440 — — 2 8.57
CHEMBL227645 — — 2 8.49
CHEMBL227783 — — 2 8.46
CHEMBL227088 — — 2 8.42
CHEMBL224207 — — 2 8.41
CHEMBL390728 — — 2 8.39
CHEMBL27769 STANOLONE 2.0 2 8.24
CHEMBL226559 — — 2 8.23
CHEMBL388997 — — 2 8.22
CHEMBL224204 — — 2 8.19
CHEMBL375907 — — 2 8.11
CHEMBL227408 — — 6 8.11
CHEMBL227305 — — 2 8.00
CHEMBL226609 — — 2 7.85
CHEMBL376360 — — 2 7.82
CHEMBL227030 — — 2 7.75
CHEMBL227749 — — 2 7.58
CHEMBL227695 — — 2 7.57
CHEMBL390746 — — 2 7.52
CHEMBL388831 — — 2 7.51
CHEMBL268589 — — 2 7.33
CHEMBL227463 — — 2 7.28
CHEMBL227033 — — 2 6.88

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1445 FLUOXYMESTERONE EC50 = 0.3 nM 9.52
CHEMBL224263 — EC50 = 1.1 nM 8.96
CHEMBL227784 — EC50 = 1.4 nM 8.85
CHEMBL227394 — EC50 = 1.9 nM 8.72
CHEMBL389481 — EC50 = 2.3 nM 8.64
CHEMBL227590 — EC50 = 2.4 nM 8.62
CHEMBL227440 — EC50 = 2.7 nM 8.57
CHEMBL226558 — EC50 = 2.7 nM 8.57
CHEMBL227645 — EC50 = 3.2 nM 8.49
CHEMBL227783 — EC50 = 3.5 nM 8.46
CHEMBL227088 — EC50 = 3.8 nM 8.42
CHEMBL224207 — EC50 = 3.9 nM 8.41
CHEMBL390728 — EC50 = 4.1 nM 8.39
CHEMBL27769 STANOLONE EC50 = 5.7 nM 8.24
CHEMBL226559 — EC50 = 5.9 nM 8.23
CHEMBL388997 — EC50 = 6.0 nM 8.22
CHEMBL224204 — EC50 = 6.4 nM 8.19
CHEMBL227408 — EC50 = 7.8 nM 8.11
CHEMBL375907 — EC50 = 7.8 nM 8.11
CHEMBL227408 — EC50 = 8.9 nM 8.05
CHEMBL227305 — EC50 = 10.0 nM 8.00
CHEMBL226609 — EC50 = 14.0 nM 7.85
CHEMBL376360 — EC50 = 15.0 nM 7.82
CHEMBL227030 — EC50 = 18.0 nM 7.75
CHEMBL227749 — EC50 = 26.0 nM 7.58
CHEMBL227695 — EC50 = 27.0 nM 7.57
CHEMBL390746 — EC50 = 30.0 nM 7.52
CHEMBL388831 — EC50 = 31.0 nM 7.51
CHEMBL227408 — EC50 = 44.0 nM 7.36
CHEMBL268589 — EC50 = 47.0 nM 7.33
CHEMBL227463 — EC50 = 52.0 nM 7.28
CHEMBL227033 — EC50 = 133.0 nM 6.88
CHEMBL27769 STANOLONE Efficacy = 100.0 % -
CHEMBL1445 FLUOXYMESTERONE Efficacy = 124.0 % -
CHEMBL226609 — Efficacy = 75.0 % -
CHEMBL390728 — Efficacy = 100.0 % -
CHEMBL390754 — EC50 > 10000.0 nM -
CHEMBL390754 — Efficacy < 20.0 % -
CHEMBL227088 — Efficacy = 58.0 % -
CHEMBL227030 — Efficacy = 56.0 % -
CHEMBL227695 — Efficacy = 65.0 % -
CHEMBL224204 — Efficacy = 92.0 % -
CHEMBL388997 — Efficacy = 69.0 % -
CHEMBL227590 — Efficacy = 83.0 % -
CHEMBL227749 — Efficacy = 46.0 % -
CHEMBL227645 — Efficacy = 70.0 % -
CHEMBL227440 — Efficacy = 96.0 % -
CHEMBL375907 — Efficacy = 62.0 % -
CHEMBL226558 — Efficacy = 85.0 % -
CHEMBL390746 — Efficacy = 49.0 % -