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Assay Detail

CHEMBL1776378

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

Binding
Inhibition of p38 alpha MAPK in human whole blood assessed as phosphorylation of ATF-2 by immunosorbent non-radioactive enzyme assay
49
Total Activities
49
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Tissue Blood
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Mitogen-activated protein kinase 14 (CHEMBL260)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Chiral sulfoxides as metabolites of 2-thioimidazole-based p38α mitogen-activated protein kinase inhibitors: enantioselective synthesis and biological evaluation.
Bühler S, Goettert M, Schollmeyer D, Albrecht W, Laufer SA.
J Med Chem (2011) 54 : 3283 -3297
PubMed 21449619 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 49 7.45 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1773433 1 8.70
CHEMBL1773432 1 8.70
CHEMBL1773437 1 8.52
CHEMBL1773436 1 8.40
CHEMBL1773438 1 8.40
CHEMBL480962 1 8.30
CHEMBL1773499 1 8.22
CHEMBL1271554 1 8.05
CHEMBL1773506 1 7.96
CHEMBL1773503 1 7.96
CHEMBL1773502 1 7.92
CHEMBL1773505 1 7.92
CHEMBL1773434 1 7.92
CHEMBL10 SB-203580 1 7.82
CHEMBL1773509 1 7.77
CHEMBL1773421 1 7.75
CHEMBL1773510 1 7.72
CHEMBL1773504 1 7.68
CHEMBL1773435 1 7.62
CHEMBL1773520 1 7.60
CHEMBL1773508 1 7.58
CHEMBL482086 1 7.57
CHEMBL1773511 1 7.57
CHEMBL1773500 1 7.54
CHEMBL1773514 1 7.51
CHEMBL1773439 1 7.47
CHEMBL1773507 1 7.47
CHEMBL1773515 1 7.44
CHEMBL1773425 1 7.43
CHEMBL1773512 1 7.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1773433 IC50 = 2.0 nM 8.70
CHEMBL1773432 IC50 = 2.0 nM 8.70
CHEMBL1773437 IC50 = 3.0 nM 8.52
CHEMBL1773436 IC50 = 4.0 nM 8.40
CHEMBL1773438 IC50 = 4.0 nM 8.40
CHEMBL480962 IC50 = 5.0 nM 8.30
CHEMBL1773499 IC50 = 6.0 nM 8.22
CHEMBL1271554 IC50 = 9.0 nM 8.05
CHEMBL1773506 IC50 = 11.0 nM 7.96
CHEMBL1773503 IC50 = 11.0 nM 7.96
CHEMBL1773502 IC50 = 12.0 nM 7.92
CHEMBL1773505 IC50 = 12.0 nM 7.92
CHEMBL1773434 IC50 = 12.0 nM 7.92
CHEMBL10 SB-203580 IC50 = 15.0 nM 7.82
CHEMBL1773509 IC50 = 17.0 nM 7.77
CHEMBL1773421 IC50 = 18.0 nM 7.75
CHEMBL1773510 IC50 = 19.0 nM 7.72
CHEMBL1773504 IC50 = 21.0 nM 7.68
CHEMBL1773435 IC50 = 24.0 nM 7.62
CHEMBL1773520 IC50 = 25.0 nM 7.60
CHEMBL1773508 IC50 = 26.0 nM 7.58
CHEMBL482086 IC50 = 27.0 nM 7.57
CHEMBL1773511 IC50 = 27.0 nM 7.57
CHEMBL1773500 IC50 = 29.0 nM 7.54
CHEMBL1773514 IC50 = 31.0 nM 7.51
CHEMBL1773507 IC50 = 34.0 nM 7.47
CHEMBL1773439 IC50 = 34.0 nM 7.47
CHEMBL1773515 IC50 = 36.0 nM 7.44
CHEMBL1773425 IC50 = 37.0 nM 7.43
CHEMBL1773512 IC50 = 40.0 nM 7.40
CHEMBL1773521 IC50 = 45.0 nM 7.35
CHEMBL1773501 IC50 = 50.0 nM 7.30
CHEMBL321415 IC50 = 50.0 nM 7.30
CHEMBL1773513 IC50 = 61.0 nM 7.21
CHEMBL109331 IC50 = 65.0 nM 7.19
CHEMBL1773429 IC50 = 69.0 nM 7.16
CHEMBL1773430 IC50 = 77.0 nM 7.11
CHEMBL1773519 IC50 = 95.0 nM 7.02
CHEMBL1773431 IC50 = 141.0 nM 6.85
CHEMBL1773427 IC50 = 161.0 nM 6.79
CHEMBL1773517 IC50 = 168.0 nM 6.78
CHEMBL432798 IC50 = 188.0 nM 6.73
CHEMBL1773428 IC50 = 197.0 nM 6.71
CHEMBL1773518 IC50 = 200.0 nM 6.70
CHEMBL1773516 IC50 = 207.0 nM 6.68
CHEMBL1773426 IC50 = 403.0 nM 6.39
CHEMBL1773423 IC50 = 1030.0 nM 5.99
CHEMBL1773422 IC50 = 1072.0 nM 5.97
CHEMBL1773424 IC50 = 1265.0 nM 5.90