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Assay Detail

CHEMBL4230002

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

Binding
Inhibition of BRAF V600E mutant (unknown origin) after 20 mins by immunoblotting assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Effects of rigidity on the selectivity of protein kinase inhibitors.
Assadieskandar A, Yu C, Maisonneuve P, Liu X, Chen YC, Prakash GKS, Kurinov I, Sicheri F, Zhang C.
Eur J Med Chem (2018) 146 : 519 -528
PubMed 29407977 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 7.54 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3736320 1 8.40
CHEMBL4248365 1 7.89
CHEMBL1229517 VEMURAFENIB 4.0 1 7.68
CHEMBL4249028 1 7.62
CHEMBL4242050 1 7.36
CHEMBL4243230 1 7.34
CHEMBL4237900 1 7.29
CHEMBL4247506 1 7.19
CHEMBL4250674 1 7.06

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3736320 IC50 = 4.0 nM 8.40
CHEMBL4248365 IC50 = 13.0 nM 7.89
CHEMBL1229517 VEMURAFENIB IC50 = 21.0 nM 7.68
CHEMBL4249028 IC50 = 24.0 nM 7.62
CHEMBL4242050 IC50 = 44.0 nM 7.36
CHEMBL4243230 IC50 = 46.0 nM 7.34
CHEMBL4237900 IC50 = 51.0 nM 7.29
CHEMBL4247506 IC50 = 65.0 nM 7.19
CHEMBL4250674 IC50 = 87.0 nM 7.06