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Assay Detail

CHEMBL3395778

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

Binding
Inhibition of p38alpha (unknown origin) assessed as phosphorylation of ATF-2 by ELISA
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Tetra-substituted pyridinylimidazoles as dual inhibitors of p38α mitogen-activated protein kinase and c-Jun N-terminal kinase 3 for potential treatment of neurodegenerative diseases.
Muth F, Günther M, Bauer SM, Döring E, Fischer S, Maier J, Drückes P, Köppler J, Trappe J, Rothbauer U, Koch P, Laufer SA.
J Med Chem (2015) 58 : 443 -456
PubMed 25475894 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 34 6.64 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3394106 1 7.52
CHEMBL3394121 1 7.47
CHEMBL3394097 1 7.44
CHEMBL3394125 1 7.44
CHEMBL3394107 1 7.41
CHEMBL3394102 1 6.91
CHEMBL3394120 1 6.89
CHEMBL3394112 1 6.87
CHEMBL3394095 1 6.85
CHEMBL3394126 1 6.84
CHEMBL3394122 1 6.84
CHEMBL3394119 1 6.82
CHEMBL3394104 1 6.79
CHEMBL3394105 1 6.78
CHEMBL3394124 1 6.74
CHEMBL3394100 1 6.72
CHEMBL3394103 1 6.68
CHEMBL3394117 1 6.68
CHEMBL3394108 1 6.65
CHEMBL3394098 1 6.61
CHEMBL3394094 1 6.53
CHEMBL3394101 1 6.47
CHEMBL3394118 1 6.45
CHEMBL3394123 1 6.45
CHEMBL3394110 1 6.38
CHEMBL3394114 1 6.35
CHEMBL3394113 1 6.21
CHEMBL3394093 1 6.19
CHEMBL3394116 1 6.18
CHEMBL3394109 1 6.14

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3394106 IC50 = 30.0 nM 7.52
CHEMBL3394121 IC50 = 34.0 nM 7.47
CHEMBL3394097 IC50 = 36.0 nM 7.44
CHEMBL3394125 IC50 = 36.0 nM 7.44
CHEMBL3394107 IC50 = 39.0 nM 7.41
CHEMBL3394102 IC50 = 123.0 nM 6.91
CHEMBL3394120 IC50 = 128.0 nM 6.89
CHEMBL3394112 IC50 = 135.0 nM 6.87
CHEMBL3394095 IC50 = 140.0 nM 6.85
CHEMBL3394126 IC50 = 146.0 nM 6.84
CHEMBL3394122 IC50 = 146.0 nM 6.84
CHEMBL3394119 IC50 = 153.0 nM 6.82
CHEMBL3394104 IC50 = 164.0 nM 6.79
CHEMBL3394105 IC50 = 165.0 nM 6.78
CHEMBL3394124 IC50 = 181.0 nM 6.74
CHEMBL3394100 IC50 = 191.0 nM 6.72
CHEMBL3394117 IC50 = 208.0 nM 6.68
CHEMBL3394103 IC50 = 211.0 nM 6.68
CHEMBL3394108 IC50 = 223.0 nM 6.65
CHEMBL3394098 IC50 = 246.0 nM 6.61
CHEMBL3394094 IC50 = 297.0 nM 6.53
CHEMBL3394101 IC50 = 335.0 nM 6.47
CHEMBL3394118 IC50 = 356.0 nM 6.45
CHEMBL3394123 IC50 = 354.0 nM 6.45
CHEMBL3394110 IC50 = 416.0 nM 6.38
CHEMBL3394114 IC50 = 451.0 nM 6.35
CHEMBL3394113 IC50 = 612.0 nM 6.21
CHEMBL3394093 IC50 = 642.0 nM 6.19
CHEMBL3394116 IC50 = 655.0 nM 6.18
CHEMBL3394109 IC50 = 723.0 nM 6.14
CHEMBL3394111 IC50 = 764.0 nM 6.12
CHEMBL3394096 IC50 = 1666.0 nM 5.78
CHEMBL3394099 IC50 = 1699.0 nM 5.77
CHEMBL3394115 IC50 = 2184.0 nM 5.66