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Assay Detail

CHEMBL4399243

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

Functional
Cytotoxicity against human MCF7 cells expressing VEGFR2 and wild type BRAF measured after 48 hrs by sulforhodamine B assay
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type MCF7
Confidence 1 — Organism
Curated By Autocuration

Target

MCF7 (CHEMBL387)
Type CELL-LINE
Organism Homo sapiens

Publication

Novel potent substituted 4-amino-2-thiopyrimidines as dual VEGFR-2 and BRAF kinase inhibitors.
Abdel-Mohsen HT, Omar MA, El Kerdawy AM, Mahmoud AEE, Ali MM, El Diwani HI.
Eur J Med Chem (2019) 179 : 707 -722
PubMed 31284081 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 26 4.46 5.36

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1336 SORAFENIB 4.0 1 5.36
CHEMBL4573547 1 4.88
CHEMBL4448435 1 4.78
CHEMBL4561629 1 4.76
CHEMBL4558790 1 4.76
CHEMBL4471650 1 4.71
CHEMBL4453308 1 4.70
CHEMBL4549103 1 4.64
CHEMBL4474922 1 4.61
CHEMBL4449189 1 4.57
CHEMBL4557976 1 4.55
CHEMBL4566054 1 4.49
CHEMBL4574832 1 4.43
CHEMBL4434973 1 4.42
CHEMBL4438418 1 4.31
CHEMBL4450118 1 4.27
CHEMBL4539297 1 4.27
CHEMBL4465126 1 4.26
CHEMBL4590013 1 4.18
CHEMBL4547466 1 4.17
CHEMBL4474945 1 4.17
CHEMBL4469216 1 4.16
CHEMBL4470636 1 4.16
CHEMBL4570955 1 4.13
CHEMBL4441990 1 4.09
CHEMBL4467107 1 4.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1336 SORAFENIB IC50 = 4330.0 nM 5.36
CHEMBL4573547 IC50 = 13020.0 nM 4.88
CHEMBL4448435 IC50 = 16540.0 nM 4.78
CHEMBL4561629 IC50 = 17180.0 nM 4.76
CHEMBL4558790 IC50 = 17200.0 nM 4.76
CHEMBL4471650 IC50 = 19610.0 nM 4.71
CHEMBL4453308 IC50 = 19980.0 nM 4.70
CHEMBL4549103 IC50 = 23010.0 nM 4.64
CHEMBL4474922 IC50 = 24370.0 nM 4.61
CHEMBL4449189 IC50 = 26880.0 nM 4.57
CHEMBL4557976 IC50 = 28210.0 nM 4.55
CHEMBL4566054 IC50 = 32110.0 nM 4.49
CHEMBL4574832 IC50 = 37160.0 nM 4.43
CHEMBL4434973 IC50 = 37800.0 nM 4.42
CHEMBL4438418 IC50 = 49040.0 nM 4.31
CHEMBL4450118 IC50 = 53240.0 nM 4.27
CHEMBL4539297 IC50 = 53630.0 nM 4.27
CHEMBL4465126 IC50 = 55190.0 nM 4.26
CHEMBL4590013 IC50 = 66140.0 nM 4.18
CHEMBL4547466 IC50 = 67550.0 nM 4.17
CHEMBL4474945 IC50 = 67070.0 nM 4.17
CHEMBL4469216 IC50 = 68510.0 nM 4.16
CHEMBL4470636 IC50 = 69050.0 nM 4.16
CHEMBL4570955 IC50 = 73270.0 nM 4.13
CHEMBL4441990 IC50 = 81250.0 nM 4.09
CHEMBL4467107 IC50 = 80310.0 nM 4.09