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Assay Detail

CHEMBL4136222

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

Binding
Inhibition of MAPK p38 (unknown origin)
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Design, synthesis and biological evaluation of novel benzimidazole amidines as potent multi-target inhibitors for the treatment of non-small cell lung cancer.
Bistrović A, Krstulović L, Harej A, Grbčić P, Sedić M, Koštrun S, Pavelić SK, Bajić M, Raić-Malić S.
Eur J Med Chem (2018) 143 : 1616 -1634
PubMed 29133046 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 7.19 9.09

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1738839 1 9.09
CHEMBL1232784 1 8.70
CHEMBL258202 1 8.46
CHEMBL476351 GW775608X 1 8.22
CHEMBL257341 1 8.19
CHEMBL4168810 1 8.05
CHEMBL1929215 1 7.75
CHEMBL1929238 1 7.66
CHEMBL4166018 1 7.36
CHEMBL218962 1 7.30
CHEMBL119385 NEFLAMAPIMOD 2.0 1 7.16
CHEMBL1929195 1 7.12
CHEMBL5416410 DASATINIB 4.0 1 7.00
CHEMBL1738943 1 6.23
CHEMBL1233784 1 5.72
CHEMBL1929210 1 5.64
CHEMBL1232634 1 5.62
CHEMBL941 IMATINIB 4.0 1 4.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1738839 IC50 = 0.82 nM 9.09
CHEMBL1232784 IC50 = 2.0 nM 8.70
CHEMBL258202 IC50 = 3.5 nM 8.46
CHEMBL476351 GW775608X IC50 = 6.0 nM 8.22
CHEMBL257341 IC50 = 6.5 nM 8.19
CHEMBL4168810 IC50 = 9.0 nM 8.05
CHEMBL1929215 IC50 = 18.0 nM 7.75
CHEMBL1929238 IC50 = 22.0 nM 7.66
CHEMBL4166018 IC50 = 44.0 nM 7.36
CHEMBL218962 IC50 = 50.0 nM 7.30
CHEMBL119385 NEFLAMAPIMOD IC50 = 70.0 nM 7.16
CHEMBL1929195 IC50 = 76.0 nM 7.12
CHEMBL5416410 DASATINIB IC50 = 100.0 nM 7.00
CHEMBL1738943 IC50 = 586.0 nM 6.23
CHEMBL1233784 IC50 = 1900.0 nM 5.72
CHEMBL1929210 IC50 = 2300.0 nM 5.64
CHEMBL1232634 IC50 = 2400.0 nM 5.62
CHEMBL941 IMATINIB IC50 = 70000.0 nM 4.16