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Assay Detail

CHEMBL680190

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Binding
Binding affinity for glucocorticoid receptor
11
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Glucocorticoid receptor (CHEMBL2034)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and characterization of non-steroidal ligands for the glucocorticoid receptor: selective quinoline derivatives with prednisolone-equivalent functional activity.
Coghlan MJ, Kym PR, Elmore SW, Wang AX, Luly JR, Wilcox D, Stashko M, Lin CW, Miner J, Tyree C, Nakane M, Jacobson P, Lane BC.
J Med Chem (2001) 44 : 2879 -2885
PubMed 11520196 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 7.79 8.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL99046 3 8.68
CHEMBL131 PREDNISOLONE 4.0 1 8.62
CHEMBL419158 2 8.48
CHEMBL97206 1 8.40
CHEMBL318409 1 8.03
CHEMBL95644 1 7.96
CHEMBL317983 1 7.75
CHEMBL99128 1 5.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL99046 Ki = 2.1 nM 8.68
CHEMBL131 PREDNISOLONE Ki = 2.4 nM 8.62
CHEMBL419158 Ki = 3.3 nM 8.48
CHEMBL97206 Ki = 4.0 nM 8.40
CHEMBL99046 Ki = 4.7 nM 8.33
CHEMBL318409 Ki = 9.3 nM 8.03
CHEMBL95644 Ki = 11.0 nM 7.96
CHEMBL317983 Ki = 18.0 nM 7.75
CHEMBL419158 Ki = 95.0 nM 7.02
CHEMBL99046 Ki = 240.0 nM 6.62
CHEMBL99128 Ki = 1800.0 nM 5.75