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Assay Detail

CHEMBL4331498

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

Binding
Inhibition of BRAF (unknown origin)
6
Total Activities
6
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

Serine/threonine-protein kinase B-raf (CHEMBL5145)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of potent Pan-Raf inhibitors with increased solubility to overcome drug resistance.
Wang L, Zhang Y, Zhang Q, Zhu G, Zhang Z, Duan C, Lu T, Tang W.
Eur J Med Chem (2019) 163 : 243 -255
PubMed 30529543 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 7.91 8.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3577124 LY-3009120 1.0 1 8.82
CHEMBL1229517 VEMURAFENIB 4.0 1 8.16
CHEMBL4438236 1 8.03
CHEMBL1336 SORAFENIB 4.0 1 7.65
CHEMBL4436132 1 7.40
CHEMBL4586402 1 7.37

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3577124 LY-3009120 IC50 = 1.5 nM 8.82
CHEMBL1229517 VEMURAFENIB IC50 = 6.9 nM 8.16
CHEMBL4438236 IC50 = 9.4 nM 8.03
CHEMBL1336 SORAFENIB IC50 = 22.6 nM 7.65
CHEMBL4436132 IC50 = 39.6 nM 7.40
CHEMBL4586402 IC50 = 43.1 nM 7.37