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Assay Detail

CHEMBL654087

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Functional
Transcriptional activation in CV-1 cells expressing human glucocorticoid receptor
12
Total Activities
12
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

Glucocorticoid receptor (CHEMBL2034)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Nonsteroidal selective glucocorticoid modulators: the effect of C-10 substitution on receptor selectivity and functional potency of 5-allyl-2,5-dihydro-2,2,4-trimethyl-1H-[1]benzopyrano[3,4-f]quinolines.
Kym PR, Kort ME, Coghlan MJ, Moore JL, Tang R, Ratajczyk JD, Larson DP, Elmore SW, Pratt JK, Stashko MA, Falls HD, Lin CW, Nakane M, Miller L, Tyree CM, Miner JN, Jacobson PB, Wilcox DM, Nguyen P, Lane BC.
J Med Chem (2003) 46 : 1016 -1030
PubMed 12620078 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 12 7.23 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL131 PREDNISOLONE 4.0 1 8.10
CHEMBL267940 1 7.77
CHEMBL440454 1 7.50
CHEMBL266282 AL-43 1 7.48
CHEMBL267231 1 7.46
CHEMBL268239 1 7.21
CHEMBL8394 1 6.91
CHEMBL7671 1 6.89
CHEMBL8209 1 6.71
CHEMBL266709 1 6.26
CHEMBL8639 1 -
CHEMBL8360 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL131 PREDNISOLONE EC50 = 8.0 nM 8.10
CHEMBL267940 EC50 = 17.0 nM 7.77
CHEMBL440454 EC50 = 32.0 nM 7.50
CHEMBL266282 AL-43 EC50 = 33.0 nM 7.48
CHEMBL267231 EC50 = 35.0 nM 7.46
CHEMBL268239 EC50 = 61.0 nM 7.21
CHEMBL8394 EC50 = 123.0 nM 6.91
CHEMBL7671 EC50 = 130.0 nM 6.89
CHEMBL8209 EC50 = 195.0 nM 6.71
CHEMBL266709 EC50 = 550.0 nM 6.26
CHEMBL8639 EC50 > 300.0 nM -
CHEMBL8360 EC50 > 300.0 nM -