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Assay Detail

CHEMBL4050076

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

Functional
Antiproliferative activity human A375 cells after 72 hrs by cell titer-glo luminescence assay
12
Total Activities
12
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

Design, synthesis and evaluation of derivatives based on pyrimidine scaffold as potent Pan-Raf inhibitors to overcome resistance.
Wang L, Zhang Q, Zhu G, Zhang Z, Zhi Y, Zhang L, Mao T, Zhou X, Chen Y, Lu T, Tang W.
Eur J Med Chem (2017) 130 : 86 -106
PubMed 28242553 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 5.57 6.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4080362 1 6.17
CHEMBL1229517 VEMURAFENIB 4.0 1 6.16
CHEMBL4075036 1 5.99
CHEMBL4101717 1 5.74
CHEMBL4085294 1 5.64
CHEMBL4066939 1 5.57
CHEMBL4063679 1 5.55
CHEMBL4060531 1 5.44
CHEMBL4082425 1 5.43
CHEMBL4104590 1 5.33
CHEMBL4060057 1 4.97
CHEMBL1336 SORAFENIB 4.0 1 4.87

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4080362 IC50 = 680.0 nM 6.17
CHEMBL1229517 VEMURAFENIB IC50 = 700.0 nM 6.16
CHEMBL4075036 IC50 = 1020.0 nM 5.99
CHEMBL4101717 IC50 = 1810.0 nM 5.74
CHEMBL4085294 IC50 = 2270.0 nM 5.64
CHEMBL4066939 IC50 = 2680.0 nM 5.57
CHEMBL4063679 IC50 = 2830.0 nM 5.55
CHEMBL4060531 IC50 = 3600.0 nM 5.44
CHEMBL4082425 IC50 = 3740.0 nM 5.43
CHEMBL4104590 IC50 = 4730.0 nM 5.33
CHEMBL4060057 IC50 = 10600.0 nM 4.97
CHEMBL1336 SORAFENIB IC50 = 13640.0 nM 4.87