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Assay Detail

CHEMBL4040336

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

ADMET
Androgenic activity at human androgen receptor expressed in African green monkey CV-1 cells assessed as increase in interaction between VP16-fused AR-NTD and GAL4-fused AR-LBD after 17 hrs by luciferase reporter gene assay
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Androgen receptor (CHEMBL1871)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-Based Approach To Identify 5-[4-Hydroxyphenyl]pyrrole-2-carbonitrile Derivatives as Potent and Tissue Selective Androgen Receptor Modulators.
Unwalla R, Mousseau JJ, Fadeyi OO, Choi C, Parris K, Hu B, Kenney T, Chippari S, McNally C, Vishwanathan K, Kilbourne E, Thompson C, Nagpal S, Wrobel J, Yudt M, Morris CA, Powell D, Gilbert AM, Chekler ELP.
J Med Chem (2017) 60 : 6451 -6457
PubMed 28696695 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 26 6.84 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4095364 1 9.15
CHEMBL386630 TESTOSTERONE 4.0 1 8.96
CHEMBL4104046 1 7.54
CHEMBL4095883 1 5.92
CHEMBL4065842 1 5.81
CHEMBL4079377 1 5.81
CHEMBL4088158 1 5.81
CHEMBL4087256 1 5.70
CHEMBL4073399 1 -
CHEMBL4100251 1 -
CHEMBL4066319 1 -
CHEMBL4087674 1 -
CHEMBL4074927 1 -
CHEMBL4068562 1 -
CHEMBL4091403 1 -
CHEMBL4069026 1 -
CHEMBL4062016 1 -
CHEMBL4074555 1 -
CHEMBL4072730 1 -
CHEMBL4073869 1 -
CHEMBL4088572 1 -
CHEMBL4060340 1 -
CHEMBL4080698 1 -
CHEMBL4098744 1 -
CHEMBL4061510 1 -
CHEMBL4103641 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4095364 EC50 = 0.71 nM 9.15
CHEMBL386630 TESTOSTERONE EC50 = 1.1 nM 8.96
CHEMBL4104046 EC50 = 28.9 nM 7.54
CHEMBL4095883 EC50 = 1205.8 nM 5.92
CHEMBL4065842 EC50 = 1542.6 nM 5.81
CHEMBL4079377 EC50 = 1550.9 nM 5.81
CHEMBL4088158 EC50 = 1556.0 nM 5.81
CHEMBL4087256 EC50 = 2014.9 nM 5.70
CHEMBL4073399 EC50 > 10000.0 nM -
CHEMBL4100251 EC50 > 10000.0 nM -
CHEMBL4066319 EC50 > 10000.0 nM -
CHEMBL4087674 EC50 > 10000.0 nM -
CHEMBL4074927 EC50 > 10000.0 nM -
CHEMBL4068562 EC50 > 10000.0 nM -
CHEMBL4091403 EC50 > 10000.0 nM -
CHEMBL4069026 EC50 > 10000.0 nM -
CHEMBL4062016 EC50 > 10000.0 nM -
CHEMBL4074555 EC50 > 10000.0 nM -
CHEMBL4072730 EC50 > 10000.0 nM -
CHEMBL4073869 EC50 > 10000.0 nM -
CHEMBL4088572 EC50 > 10000.0 nM -
CHEMBL4060340 EC50 > 10000.0 nM -
CHEMBL4080698 EC50 > 10000.0 nM -
CHEMBL4098744 EC50 > 10000.0 nM -
CHEMBL4061510 EC50 > 10000.0 nM -
CHEMBL4103641 EC50 > 10000.0 nM -