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Assay Detail

CHEMBL1013119

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

Binding
Inhibition of human c-RAF at 10 uM
13
Total Activities
13
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

RAF proto-oncogene serine/threonine-protein kinase (CHEMBL1906)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis, and biological evaluation of novel Tri- and tetrasubstituted imidazoles as highly potent and specific ATP-mimetic inhibitors of p38 MAP kinase: focus on optimized interactions with the enzyme's surface-exposed front region.
Laufer SA, Hauser DR, Domeyer DM, Kinkel K, Liedtke AJ.
J Med Chem (2008) 51 : 4122 -4149
PubMed 18578517 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Inhibition 9 - -
IC50 4 6.31 7.25

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL430419 1 7.25
CHEMBL303144 1 6.09
CHEMBL67658 1 5.58
CHEMBL494666 1 -
CHEMBL103667 DORAMAPIMOD 2.0 1 -
CHEMBL10 SB-203580 1 -
CHEMBL481943 1 -
CHEMBL480952 1 -
CHEMBL518964 1 -
CHEMBL519617 1 -
CHEMBL493669 1 -
CHEMBL494871 1 -
CHEMBL307435 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL430419 IC50 = 56.0 nM 7.25
CHEMBL303144 IC50 = 810.0 nM 6.09
CHEMBL67658 IC50 = 2600.0 nM 5.58
CHEMBL494666 Inhibition = 31.0 % -
CHEMBL103667 DORAMAPIMOD Inhibition = 79.0 % -
CHEMBL10 SB-203580 Inhibition = 85.0 % -
CHEMBL481943 Inhibition = - % -
CHEMBL480952 Inhibition = - % -
CHEMBL518964 Inhibition = 7.0 % -
CHEMBL519617 Inhibition = 53.0 % -
CHEMBL493669 Inhibition = 19.0 % -
CHEMBL494871 Inhibition = 36.0 % -
CHEMBL307435 IC50 > 1000.0 nM -