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Assay Detail

CHEMBL1035784

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

Binding
Inhibition of human recombinant GST-tagged p38alphaMAPK-induced ATF2 phosphorylation
17
Total Activities
17
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

3-amino-7-phthalazinylbenzoisoxazoles as a novel class of potent, selective, and orally available inhibitors of p38alpha mitogen-activated protein kinase.
Pettus LH, Xu S, Cao GQ, Chakrabarti PP, Rzasa RM, Sham K, Wurz RP, Zhang D, Middleton S, Henkle B, Plant MH, Saris CJ, Sherman L, Wong LM, Powers DA, Tudor Y, Yu V, Lee MR, Syed R, Hsieh F, Tasker AS.
J Med Chem (2008) 51 : 6280 -6292
PubMed 18817364 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 9.24 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL495118 1 9.70
CHEMBL522689 1 9.70
CHEMBL495493 1 9.52
CHEMBL493496 1 9.52
CHEMBL494916 1 9.52
CHEMBL523374 1 9.40
CHEMBL523516 1 9.40
CHEMBL494917 1 9.40
CHEMBL495084 1 9.40
CHEMBL495492 1 9.30
CHEMBL494305 1 9.30
CHEMBL521860 1 9.22
CHEMBL522877 1 9.15
CHEMBL495290 1 9.10
CHEMBL492661 1 8.96
CHEMBL524054 1 8.70
CHEMBL493707 1 7.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL495118 Ki = 0.2 nM 9.70
CHEMBL522689 Ki = 0.2 nM 9.70
CHEMBL495493 Ki = 0.3 nM 9.52
CHEMBL493496 Ki = 0.3 nM 9.52
CHEMBL494916 Ki = 0.3 nM 9.52
CHEMBL523374 Ki = 0.4 nM 9.40
CHEMBL523516 Ki = 0.4 nM 9.40
CHEMBL494917 Ki = 0.4 nM 9.40
CHEMBL495084 Ki = 0.4 nM 9.40
CHEMBL495492 Ki = 0.5 nM 9.30
CHEMBL494305 Ki = 0.5 nM 9.30
CHEMBL521860 Ki = 0.6 nM 9.22
CHEMBL522877 Ki = 0.7 nM 9.15
CHEMBL495290 Ki = 0.8 nM 9.10
CHEMBL492661 Ki = 1.1 nM 8.96
CHEMBL524054 Ki = 2.0 nM 8.70
CHEMBL493707 Ki = 16.0 nM 7.80