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Assay Detail

CHEMBL620387

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

Functional
Ability to induce human IL-6 assay in A549 lung carcinoma cell line.
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type A549
Confidence 9 — Direct 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
EC50 22 8.12 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL310570 1 9.00
CHEMBL81111 1 8.72
CHEMBL311662 1 8.66
CHEMBL310365 1 8.57
CHEMBL81591 1 8.54
CHEMBL312041 1 8.52
CHEMBL82546 1 8.49
CHEMBL79335 1 8.36
CHEMBL131 PREDNISOLONE 4.0 1 8.35
CHEMBL312399 1 8.07
CHEMBL309243 1 8.03
CHEMBL79807 1 8.01
CHEMBL83110 1 7.99
CHEMBL419479 1 7.94
CHEMBL310420 1 7.86
CHEMBL420767 1 7.84
CHEMBL313062 1 7.84
CHEMBL311034 1 7.81
CHEMBL81397 1 7.71
CHEMBL440877 1 7.62
CHEMBL313400 1 7.50
CHEMBL309909 1 7.27

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL310570 EC50 = 1.0 nM 9.00
CHEMBL81111 EC50 = 1.9 nM 8.72
CHEMBL311662 EC50 = 2.2 nM 8.66
CHEMBL310365 EC50 = 2.7 nM 8.57
CHEMBL81591 EC50 = 2.9 nM 8.54
CHEMBL312041 EC50 = 3.0 nM 8.52
CHEMBL82546 EC50 = 3.2 nM 8.49
CHEMBL79335 EC50 = 4.4 nM 8.36
CHEMBL131 PREDNISOLONE EC50 = 4.5 nM 8.35
CHEMBL312399 EC50 = 8.6 nM 8.07
CHEMBL309243 EC50 = 9.3 nM 8.03
CHEMBL79807 EC50 = 9.7 nM 8.01
CHEMBL83110 EC50 = 10.2 nM 7.99
CHEMBL419479 EC50 = 11.4 nM 7.94
CHEMBL310420 EC50 = 13.9 nM 7.86
CHEMBL420767 EC50 = 14.3 nM 7.84
CHEMBL313062 EC50 = 14.4 nM 7.84
CHEMBL311034 EC50 = 15.5 nM 7.81
CHEMBL81397 EC50 = 19.5 nM 7.71
CHEMBL440877 EC50 = 24.2 nM 7.62
CHEMBL313400 EC50 = 31.3 nM 7.50
CHEMBL309909 EC50 = 54.2 nM 7.27