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Assay Detail

CHEMBL4043792

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Functional
Antiproliferative activity against human FGFR2-amplified SUM52 cells after 5 days by SRB assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type SUM52
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

2-Oxo-3, 4-dihydropyrimido[4, 5-d]pyrimidinyl derivatives as new irreversible pan fibroblast growth factor receptor (FGFR) inhibitors.
Li X, Guise CP, Taghipouran R, Yosaatmadja Y, Ashoorzadeh A, Paik WK, Squire CJ, Jiang S, Luo J, Xu Y, Tu ZC, Lu X, Ren X, Patterson AV, Smaill JB, Ding K.
Eur J Med Chem (2017) 135 : 531 -543
PubMed 28521156 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 8.70 9.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4060079 1 9.24
CHEMBL4096041 1 9.19
CHEMBL4069509 1 9.19
CHEMBL4092508 1 9.11
CHEMBL4100258 1 9.10
CHEMBL4088313 1 9.08
CHEMBL4068733 1 9.00
CHEMBL4079538 1 8.96
CHEMBL4103795 1 8.96
CHEMBL4092354 1 8.70
CHEMBL2216830 1 8.54
CHEMBL4077029 1 8.48
CHEMBL4096738 1 8.40
CHEMBL189584 PD-173074 1 7.91
CHEMBL4084614 1 6.65

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4060079 IC50 = 0.57 nM 9.24
CHEMBL4096041 IC50 = 0.65 nM 9.19
CHEMBL4069509 IC50 = 0.65 nM 9.19
CHEMBL4092508 IC50 = 0.77 nM 9.11
CHEMBL4100258 IC50 = 0.8 nM 9.10
CHEMBL4088313 IC50 = 0.84 nM 9.08
CHEMBL4068733 IC50 = 1.0 nM 9.00
CHEMBL4079538 IC50 = 1.1 nM 8.96
CHEMBL4103795 IC50 = 1.1 nM 8.96
CHEMBL4092354 IC50 = 2.0 nM 8.70
CHEMBL2216830 IC50 = 2.9 nM 8.54
CHEMBL4077029 IC50 = 3.3 nM 8.48
CHEMBL4096738 IC50 = 4.0 nM 8.40
CHEMBL189584 PD-173074 IC50 = 12.3 nM 7.91
CHEMBL4084614 IC50 = 224.0 nM 6.65