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Assay Detail

CHEMBL5030898

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

Functional
Antiproliferative activity against human A-375 cells harboring BRAF mutant assessed as reduction in cell viability incubated for 24 hrs by Click-iT EdU cell proliferation imaging assay
7
Total Activities
7
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

Targeting KRAS Mutant Cancers via Combination Treatment: Discovery of a 5-Fluoro-4-(3<i>H</i>)-quinazolinone Aryl Urea pan-RAF Kinase Inhibitor.
Huestis MP, Dela Cruz D, DiPasquale AG, Durk MR, Eigenbrot C, Gibbons P, Gobbi A, Hunsaker TL, La H, Leung DH, Liu W, Malek S, Merchant M, Moffat JG, Muli CS, Orr CJ, Parr BT, Shanahan F, Sneeringer CJ, Wang W, Yen I, Yin J, Siu M, Rudolph J.
J Med Chem (2021) 64 : 3940 -3955
PubMed 33780623 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 7.20 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5094268 1 8.10
CHEMBL3577124 LY-3009120 1.0 1 7.55
CHEMBL5090624 1 7.32
CHEMBL5079215 1 7.07
CHEMBL5094514 1 7.03
CHEMBL4780060 1 6.95
CHEMBL5075174 1 6.39

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5094268 IC50 = 8.0 nM 8.10
CHEMBL3577124 LY-3009120 IC50 = 28.3 nM 7.55
CHEMBL5090624 IC50 = 47.4 nM 7.32
CHEMBL5079215 IC50 = 85.3 nM 7.07
CHEMBL5094514 IC50 = 92.6 nM 7.03
CHEMBL4780060 IC50 = 112.0 nM 6.95
CHEMBL5075174 IC50 = 405.0 nM 6.39