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Assay Detail

CHEMBL874034

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

Binding
Binding affinity towards human glucocorticoid receptor (GR) was determined using [3H]dexamethasone as radioligand in SF-1 cells
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type SF-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
Ki 36 7.90 9.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL273658 1 9.24
CHEMBL8140 1 9.02
CHEMBL8007 1 8.72
CHEMBL7655 1 8.70
CHEMBL267231 1 8.66
CHEMBL7781 1 8.64
CHEMBL268239 1 8.64
CHEMBL131 PREDNISOLONE 4.0 1 8.62
CHEMBL266282 AL-43 1 8.60
CHEMBL7843 1 8.55
CHEMBL7988 1 8.42
CHEMBL7817 1 8.39
CHEMBL8360 1 8.38
CHEMBL267940 1 8.36
CHEMBL8394 1 8.28
CHEMBL7987 1 8.27
CHEMBL8027 1 8.27
CHEMBL8637 1 8.18
CHEMBL7671 1 8.16
CHEMBL440454 1 8.15
CHEMBL8209 1 8.03
CHEMBL8329 1 7.92
CHEMBL274208 1 7.92
CHEMBL266488 1 7.86
CHEMBL267670 1 7.75
CHEMBL266709 1 7.56
CHEMBL415309 1 7.47
CHEMBL8639 1 7.47
CHEMBL8055 1 7.29
CHEMBL8026 1 7.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL273658 Ki = 0.58 nM 9.24
CHEMBL8140 Ki = 0.95 nM 9.02
CHEMBL8007 Ki = 1.9 nM 8.72
CHEMBL7655 Ki = 2.0 nM 8.70
CHEMBL267231 Ki = 2.2 nM 8.66
CHEMBL7781 Ki = 2.3 nM 8.64
CHEMBL268239 Ki = 2.3 nM 8.64
CHEMBL131 PREDNISOLONE Ki = 2.4 nM 8.62
CHEMBL266282 AL-43 Ki = 2.5 nM 8.60
CHEMBL7843 Ki = 2.8 nM 8.55
CHEMBL7988 Ki = 3.8 nM 8.42
CHEMBL7817 Ki = 4.1 nM 8.39
CHEMBL8360 Ki = 4.2 nM 8.38
CHEMBL267940 Ki = 4.4 nM 8.36
CHEMBL8394 Ki = 5.2 nM 8.28
CHEMBL7987 Ki = 5.42 nM 8.27
CHEMBL8027 Ki = 5.32 nM 8.27
CHEMBL8637 Ki = 6.6 nM 8.18
CHEMBL7671 Ki = 6.9 nM 8.16
CHEMBL440454 Ki = 7.0 nM 8.15
CHEMBL8209 Ki = 9.3 nM 8.03
CHEMBL8329 Ki = 12.0 nM 7.92
CHEMBL274208 Ki = 12.1 nM 7.92
CHEMBL266488 Ki = 13.9 nM 7.86
CHEMBL267670 Ki = 18.0 nM 7.75
CHEMBL266709 Ki = 27.6 nM 7.56
CHEMBL8639 Ki = 33.8 nM 7.47
CHEMBL415309 Ki = 34.0 nM 7.47
CHEMBL8055 Ki = 51.0 nM 7.29
CHEMBL8026 Ki = 65.0 nM 7.19
CHEMBL8139 Ki = 88.0 nM 7.06
CHEMBL8340 Ki = 140.0 nM 6.85
CHEMBL7844 Ki = 400.0 nM 6.40
CHEMBL7966 Ki = 487.0 nM 6.31
CHEMBL8359 Ki = 2100.0 nM 5.68
CHEMBL8131 Ki = 6000.0 nM 5.22