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Assay Detail

CHEMBL929947

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Binding
Inhibition of human p38alpha
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

The discovery of (R)-2-(sec-butylamino)-N-(2-methyl-5-(methylcarbamoyl)phenyl) thiazole-5-carboxamide (BMS-640994)-A potent and efficacious p38alpha MAP kinase inhibitor.
Hynes J, Wu H, Pitt S, Shen DR, Zhang R, Schieven GL, Gillooly KM, Shuster DJ, Taylor TL, Yang X, McIntyre KW, McKinnon M, Zhang H, Marathe PH, Doweyko AM, Kish K, Kiefer SE, Sack JS, Newitt JA, Barrish JC, Dodd J, Leftheris K.
Bioorg Med Chem Lett (2008) 18 : 1762 -1767
PubMed 18313298 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 26 7.71 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL255482 1 8.70
CHEMBL258203 1 8.64
CHEMBL257995 1 8.49
CHEMBL255698 1 8.47
CHEMBL258201 1 8.46
CHEMBL258202 1 8.46
CHEMBL403200 1 8.42
CHEMBL257994 1 8.39
CHEMBL255288 1 8.38
CHEMBL257996 1 8.35
CHEMBL258223 1 8.27
CHEMBL403141 1 7.89
CHEMBL258418 1 7.66
CHEMBL255254 1 7.55
CHEMBL254169 1 7.47
CHEMBL255428 1 7.44
CHEMBL258403 1 7.41
CHEMBL254365 1 7.28
CHEMBL186177 1 7.21
CHEMBL255931 1 6.96
CHEMBL258247 1 6.96
CHEMBL404446 1 6.89
CHEMBL403140 1 6.85
CHEMBL254168 1 6.80
CHEMBL255719 1 6.57
CHEMBL402943 1 6.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL255482 IC50 = 2.0 nM 8.70
CHEMBL258203 IC50 = 2.3 nM 8.64
CHEMBL257995 IC50 = 3.2 nM 8.49
CHEMBL255698 IC50 = 3.4 nM 8.47
CHEMBL258201 IC50 = 3.5 nM 8.46
CHEMBL258202 IC50 = 3.5 nM 8.46
CHEMBL403200 IC50 = 3.8 nM 8.42
CHEMBL257994 IC50 = 4.1 nM 8.39
CHEMBL255288 IC50 = 4.2 nM 8.38
CHEMBL257996 IC50 = 4.5 nM 8.35
CHEMBL258223 IC50 = 5.4 nM 8.27
CHEMBL403141 IC50 = 13.0 nM 7.89
CHEMBL258418 IC50 = 22.0 nM 7.66
CHEMBL255254 IC50 = 28.0 nM 7.55
CHEMBL254169 IC50 = 34.0 nM 7.47
CHEMBL255428 IC50 = 36.0 nM 7.44
CHEMBL258403 IC50 = 39.0 nM 7.41
CHEMBL254365 IC50 = 53.0 nM 7.28
CHEMBL186177 IC50 = 62.0 nM 7.21
CHEMBL255931 IC50 = 110.0 nM 6.96
CHEMBL258247 IC50 = 110.0 nM 6.96
CHEMBL404446 IC50 = 130.0 nM 6.89
CHEMBL403140 IC50 = 140.0 nM 6.85
CHEMBL254168 IC50 = 160.0 nM 6.80
CHEMBL255719 IC50 = 270.0 nM 6.57
CHEMBL402943 IC50 = 330.0 nM 6.48