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Assay Detail

CHEMBL872286

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

Binding
Binding affinity for human p38 MAP kinase expressed in Escherichia coli using [gamma-33P]ATP; n=4
17
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

MAP kinase p38 (CHEMBL2094115)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

5-Cyanopyrimidine derivatives as a novel class of potent, selective, and orally active inhibitors of p38alpha MAP kinase.
Liu C, Wrobleski ST, Lin J, Ahmed G, Metzger A, Wityak J, Gillooly KM, Shuster DJ, McIntyre KW, Pitt S, Shen DR, Zhang RF, Zhang H, Doweyko AM, Diller D, Henderson I, Barrish JC, Dodd JH, Schieven GL, Leftheris K.
J Med Chem (2005) 48 : 6261 -6270
PubMed 16190753 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 9.23 10.33

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL194813 1 10.33
CHEMBL363643 1 10.30
CHEMBL196741 1 10.24
CHEMBL197206 1 10.24
CHEMBL195532 1 9.82
CHEMBL197351 1 9.80
CHEMBL274257 2 9.39
CHEMBL198876 1 9.39
CHEMBL382954 1 9.21
CHEMBL383137 1 9.01
CHEMBL370783 1 8.82
CHEMBL383172 1 8.80
CHEMBL198872 1 8.72
CHEMBL198456 1 7.85
CHEMBL196230 1 7.82
CHEMBL198198 1 7.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL194813 Ki = 0.047 nM 10.33
CHEMBL363643 Ki = 0.05 nM 10.30
CHEMBL196741 Ki = 0.057 nM 10.24
CHEMBL197206 Ki = 0.057 nM 10.24
CHEMBL195532 Ki = 0.15 nM 9.82
CHEMBL197351 Ki = 0.16 nM 9.80
CHEMBL274257 Ki = 0.41 nM 9.39
CHEMBL198876 Ki = 0.41 nM 9.39
CHEMBL274257 Ki = 0.42 nM 9.38
CHEMBL382954 Ki = 0.61 nM 9.21
CHEMBL383137 Ki = 0.97 nM 9.01
CHEMBL370783 Ki = 1.5 nM 8.82
CHEMBL383172 Ki = 1.6 nM 8.80
CHEMBL198872 Ki = 1.9 nM 8.72
CHEMBL198456 Ki = 14.0 nM 7.85
CHEMBL196230 Ki = 15.0 nM 7.82
CHEMBL198198 Ki = 16.0 nM 7.80