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Assay Detail

CHEMBL2390352

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Binding
Antagonist activity at human androgen receptor LBD expressed in human MDA-kb2 cells by luciferase reporter gene assay
ChEMBL ↗
41
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type MDA-kb2
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

The systematic structure-activity relationship to predict how flavones bind to human androgen receptor for their antagonistic activity.
Tamura H, Yoshioka M, Hasegawa M, Hosoda A, Matsugi M, Akamatsu M.
Bioorg Med Chem (2013) 21 : 2968 -2974
PubMed 23611768 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 41 6.06 6.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2386405 — — 2 6.72
CHEMBL2386396 — — 2 6.60
CHEMBL2386393 — — 2 6.48
CHEMBL2386404 — — 2 6.44
CHEMBL2386395 — — 2 6.44
CHEMBL274471 — — 2 6.34
CHEMBL2386394 — — 2 6.11
CHEMBL16807 5-HYDROXYFLAVONE — 2 6.08
CHEMBL2386397 — — 2 6.07
CHEMBL484662 — — 2 6.07
CHEMBL2386401 — — 2 5.97
CHEMBL2386406 — — 2 5.92
CHEMBL2386392 — — 2 5.91
CHEMBL143978 — — 2 5.79
CHEMBL2386399 — — 2 5.70
CHEMBL2386408 — — 2 5.45
CHEMBL16972 — — 2 4.96
CHEMBL144330 — — 1 -
CHEMBL2386398 — — 1 -
CHEMBL2386400 — — 1 -
CHEMBL2386402 — — 1 -
CHEMBL2386403 — — 1 -
CHEMBL2386407 — — 1 -
CHEMBL2386409 — — 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2386405 — IC50 = 190.55 nM 6.72
CHEMBL2386405 — IC50 = 190.0 nM 6.72
CHEMBL2386396 — IC50 = 251.19 nM 6.60
CHEMBL2386396 — IC50 = 250.0 nM 6.60
CHEMBL2386393 — IC50 = 330.0 nM 6.48
CHEMBL2386393 — IC50 = 331.13 nM 6.48
CHEMBL2386395 — IC50 = 360.0 nM 6.44
CHEMBL2386404 — IC50 = 360.0 nM 6.44
CHEMBL2386395 — IC50 = 363.08 nM 6.44
CHEMBL2386404 — IC50 = 363.08 nM 6.44
CHEMBL274471 — IC50 = 460.0 nM 6.34
CHEMBL274471 — IC50 = 457.09 nM 6.34
CHEMBL2386394 — IC50 = 770.0 nM 6.11
CHEMBL2386394 — IC50 = 776.25 nM 6.11
CHEMBL16807 5-HYDROXYFLAVONE IC50 = 831.76 nM 6.08
CHEMBL16807 5-HYDROXYFLAVONE IC50 = 840.0 nM 6.08
CHEMBL484662 — IC50 = 851.14 nM 6.07
CHEMBL2386397 — IC50 = 851.14 nM 6.07
CHEMBL2386397 — IC50 = 850.0 nM 6.07
CHEMBL484662 — IC50 = 860.0 nM 6.07
CHEMBL2386401 — IC50 = 1071.52 nM 5.97
CHEMBL2386401 — IC50 = 1070.0 nM 5.97
CHEMBL2386406 — IC50 = 1202.26 nM 5.92
CHEMBL2386406 — IC50 = 1200.0 nM 5.92
CHEMBL2386392 — IC50 = 1230.27 nM 5.91
CHEMBL2386392 — IC50 = 1240.0 nM 5.91
CHEMBL143978 — IC50 = 1610.0 nM 5.79
CHEMBL143978 — IC50 = 1621.81 nM 5.79
CHEMBL2386399 — IC50 = 1990.0 nM 5.70
CHEMBL2386399 — IC50 = 1995.26 nM 5.70
CHEMBL2386408 — IC50 = 3548.13 nM 5.45
CHEMBL2386408 — IC50 = 3580.0 nM 5.45
CHEMBL16972 — IC50 = 11100.0 nM 4.96
CHEMBL16972 — IC50 = 11220.18 nM 4.95
CHEMBL2386409 — IC50 - — -
CHEMBL144330 — IC50 - — -
CHEMBL2386398 — IC50 - — -
CHEMBL2386400 — IC50 - — -
CHEMBL2386402 — IC50 - — -
CHEMBL2386403 — IC50 - — -
CHEMBL2386407 — IC50 - — -