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Assay Detail

CHEMBL683497

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Binding
Compound was tested for inhibitory activity towards human glucocorticoid receptor
23
Total Activities
23
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

Novel N-arylpyrazolo[3,2-c]-based ligands for the glucocorticoid receptor: receptor binding and in vivo activity.
Ali A, Thompson CF, Balkovec JM, Graham DW, Hammond ML, Quraishi N, Tata JR, Einstein M, Ge L, Harris G, Kelly TM, Mazur P, Pandit S, Santoro J, Sitlani A, Wang C, Williamson J, Miller DK, Thompson CM, Zaller DM, Forrest MJ, Carballo-Jane E, Luell S.
J Med Chem (2004) 47 : 2441 -2452
PubMed 15115388 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 8.26 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL310570 1 9.10
CHEMBL79335 1 8.96
CHEMBL312399 1 8.82
CHEMBL313062 1 8.72
CHEMBL312041 1 8.72
CHEMBL311662 1 8.60
CHEMBL82546 1 8.55
CHEMBL419479 1 8.47
CHEMBL309243 1 8.41
CHEMBL310420 1 8.38
CHEMBL79807 1 8.21
CHEMBL79378 1 8.20
CHEMBL83110 1 8.17
CHEMBL310365 1 8.14
CHEMBL313400 1 8.10
CHEMBL81591 1 8.08
CHEMBL420767 1 8.06
CHEMBL81111 1 8.05
CHEMBL81397 1 8.02
CHEMBL440877 1 7.78
CHEMBL311034 1 7.69
CHEMBL309909 1 7.60
CHEMBL312627 1 7.11

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL310570 IC50 = 0.8 nM 9.10
CHEMBL79335 IC50 = 1.1 nM 8.96
CHEMBL312399 IC50 = 1.5 nM 8.82
CHEMBL313062 IC50 = 1.9 nM 8.72
CHEMBL312041 IC50 = 1.9 nM 8.72
CHEMBL311662 IC50 = 2.5 nM 8.60
CHEMBL82546 IC50 = 2.8 nM 8.55
CHEMBL419479 IC50 = 3.4 nM 8.47
CHEMBL309243 IC50 = 3.9 nM 8.41
CHEMBL310420 IC50 = 4.2 nM 8.38
CHEMBL79807 IC50 = 6.2 nM 8.21
CHEMBL79378 IC50 = 6.3 nM 8.20
CHEMBL83110 IC50 = 6.7 nM 8.17
CHEMBL310365 IC50 = 7.2 nM 8.14
CHEMBL313400 IC50 = 7.9 nM 8.10
CHEMBL81591 IC50 = 8.4 nM 8.08
CHEMBL420767 IC50 = 8.8 nM 8.06
CHEMBL81111 IC50 = 9.0 nM 8.05
CHEMBL81397 IC50 = 9.5 nM 8.02
CHEMBL440877 IC50 = 16.6 nM 7.78
CHEMBL311034 IC50 = 20.4 nM 7.69
CHEMBL309909 IC50 = 24.9 nM 7.60
CHEMBL312627 IC50 = 77.3 nM 7.11