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Assay Detail

CHEMBL4003428

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

Binding
Inhibition of GST-His tagged human p38alpha expressed in Escherichia coli assessed as reduction in ATF2 phosphorylation measured after 60 mins by ELISA
21
Total Activities
21
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

Tri- and Tetrasubstituted Pyridinylimidazoles as Covalent Inhibitors of c-Jun N-Terminal Kinase 3.
Muth F, El-Gokha A, Ansideri F, Eitel M, Döring E, Sievers-Engler A, Lange A, Boeckler FM, Lämmerhofer M, Koch P, Laufer SA.
J Med Chem (2017) 60 : 594 -607
PubMed 27977190 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 7.43 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4062023 1 9.10
CHEMBL4086457 1 8.70
CHEMBL4082212 1 8.52
CHEMBL4092555 1 8.52
CHEMBL4069805 1 8.40
CHEMBL4074524 1 7.77
CHEMBL4085536 1 7.77
CHEMBL4093282 1 7.66
CHEMBL4072555 1 7.58
CHEMBL4063964 1 7.46
CHEMBL4077018 1 7.44
CHEMBL4066691 1 7.42
CHEMBL4101953 1 7.33
CHEMBL4071770 1 7.00
CHEMBL4092482 1 6.90
CHEMBL4104351 1 6.83
CHEMBL4094220 1 6.66
CHEMBL4077684 1 6.62
CHEMBL4082278 1 5.71
CHEMBL4100292 1 5.23
CHEMBL4101252 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4062023 IC50 = 0.8 nM 9.10
CHEMBL4086457 IC50 = 2.0 nM 8.70
CHEMBL4082212 IC50 = 3.0 nM 8.52
CHEMBL4092555 IC50 = 3.0 nM 8.52
CHEMBL4069805 IC50 = 4.0 nM 8.40
CHEMBL4074524 IC50 = 17.0 nM 7.77
CHEMBL4085536 IC50 = 17.0 nM 7.77
CHEMBL4093282 IC50 = 22.0 nM 7.66
CHEMBL4072555 IC50 = 26.0 nM 7.58
CHEMBL4063964 IC50 = 35.0 nM 7.46
CHEMBL4077018 IC50 = 36.0 nM 7.44
CHEMBL4066691 IC50 = 38.0 nM 7.42
CHEMBL4101953 IC50 = 47.0 nM 7.33
CHEMBL4071770 IC50 = 100.0 nM 7.00
CHEMBL4092482 IC50 = 126.0 nM 6.90
CHEMBL4104351 IC50 = 149.0 nM 6.83
CHEMBL4094220 IC50 = 217.0 nM 6.66
CHEMBL4077684 IC50 = 241.0 nM 6.62
CHEMBL4082278 IC50 = 1952.0 nM 5.71
CHEMBL4100292 IC50 = 5920.0 nM 5.23
CHEMBL4101252 IC50 > 10000.0 nM -