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Assay Detail

CHEMBL681744

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

Binding
Binding affinity was determined for human glucocorticoid receptor(hGR).
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Glucocorticoid receptor (CHEMBL2034)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and biological activity of novel nonsteroidal progesterone receptor antagonists based on cyclocymopol monomethyl ether.
Hamann LG, Farmer LJ, Johnson MG, Bender SL, Mais DE, Wang MW, Crombie D, Goldman ME, Jones TK.
J Med Chem (1996) 39 : 1778 -1789
PubMed 8627601 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 30 5.88 9.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1276308 MIFEPRISTONE 4.0 1 9.17
CHEMBL384467 DEXAMETHASONE 4.0 1 8.26
CHEMBL103 PROGESTERONE 4.0 1 7.52
CHEMBL1908373 ONAPRISTONE 2.0 1 7.38
CHEMBL53549 1 5.99
CHEMBL48746 1 5.90
CHEMBL50454 1 5.78
CHEMBL51669 1 5.75
CHEMBL417729 1 5.75
CHEMBL48858 1 5.66
CHEMBL54270 1 5.66
CHEMBL51788 1 5.64
CHEMBL51933 1 5.62
CHEMBL51639 1 5.61
CHEMBL50849 1 5.59
CHEMBL299828 1 5.57
CHEMBL48358 1 5.56
CHEMBL299778 1 5.43
CHEMBL50619 1 5.39
CHEMBL49978 1 5.36
CHEMBL48745 1 5.34
CHEMBL50023 1 5.27
CHEMBL296156 1 5.20
CHEMBL299512 1 5.17
CHEMBL49754 1 5.08
CHEMBL50786 1 5.08
CHEMBL2113712 1 5.07
CHEMBL49966 1 -
CHEMBL50534 1 -
CHEMBL299766 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1276308 MIFEPRISTONE Ki = 0.68 nM 9.17
CHEMBL384467 DEXAMETHASONE Ki = 5.5 nM 8.26
CHEMBL103 PROGESTERONE Ki = 30.5 nM 7.52
CHEMBL1908373 ONAPRISTONE Ki = 41.8 nM 7.38
CHEMBL53549 Ki = 1036.0 nM 5.99
CHEMBL48746 Ki = 1261.0 nM 5.90
CHEMBL50454 Ki = 1657.0 nM 5.78
CHEMBL51669 Ki = 1777.0 nM 5.75
CHEMBL417729 Ki = 1766.0 nM 5.75
CHEMBL48858 Ki = 2206.0 nM 5.66
CHEMBL54270 Ki = 2199.0 nM 5.66
CHEMBL51788 Ki = 2286.0 nM 5.64
CHEMBL51933 Ki = 2379.0 nM 5.62
CHEMBL51639 Ki = 2465.0 nM 5.61
CHEMBL50849 Ki = 2570.0 nM 5.59
CHEMBL299828 Ki = 2670.0 nM 5.57
CHEMBL48358 Ki = 2781.0 nM 5.56
CHEMBL299778 Ki = 3697.0 nM 5.43
CHEMBL50619 Ki = 4109.0 nM 5.39
CHEMBL49978 Ki = 4417.0 nM 5.36
CHEMBL48745 Ki = 4532.0 nM 5.34
CHEMBL50023 Ki = 5424.0 nM 5.27
CHEMBL296156 Ki = 6386.0 nM 5.20
CHEMBL299512 Ki = 6812.0 nM 5.17
CHEMBL49754 Ki = 8215.0 nM 5.08
CHEMBL50786 Ki = 8356.0 nM 5.08
CHEMBL2113712 Ki = 8511.0 nM 5.07
CHEMBL49966 Ki 10000.0 nM -
CHEMBL50534 Ki > 10000.0 nM -
CHEMBL299766 Ki > 10000.0 nM -