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Assay Detail

CHEMBL2173450

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Functional
Antiproliferative activity against human A375 cells expressing B-Raf V600E mutant and wild type Ras
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type A-375
Confidence 1 — Organism
Curated By Autocuration

Target

A-375 (CHEMBL613859)
Type CELL-LINE
Organism Homo sapiens

Publication

Conformation-specific effects of Raf kinase inhibitors.
Wang X, Kim J.
J Med Chem (2012) 55 : 7332 -7341
PubMed 22808911 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 6.27 6.51

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1229517 VEMURAFENIB 4.0 1 6.51
CHEMBL1197798 1 6.51
CHEMBL477989 SB590885 1 6.43
CHEMBL1230020 PLX-4720 1 6.30
CHEMBL1336 SORAFENIB 4.0 1 5.62
CHEMBL525191 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1229517 VEMURAFENIB IC50 = 310.0 nM 6.51
CHEMBL1197798 IC50 = 310.0 nM 6.51
CHEMBL477989 SB590885 IC50 = 370.0 nM 6.43
CHEMBL1230020 PLX-4720 IC50 = 500.0 nM 6.30
CHEMBL1336 SORAFENIB IC50 = 2400.0 nM 5.62
CHEMBL525191 IC50 < 500.0 nM -