Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL4013830

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

Functional
Antiproliferative activity against human SNU16 cells over-expressing FGFR2 after 72 hrs by Presto-Blue assay
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type SNU-16
Confidence 1 — Organism
Curated By Autocuration

Target

SNU-16 (CHEMBL613529)
Type CELL-LINE
Organism Homo sapiens

Publication

Discovery of the Irreversible Covalent FGFR Inhibitor 8-(3-(4-Acryloylpiperazin-1-yl)propyl)-6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-(methylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (PRN1371) for the Treatment of Solid Tumors.
Brameld KA, Owens TD, Verner E, Venetsanakos E, Bradshaw JM, Phan VT, Tam D, Leung K, Shu J, LaStant J, Loughhead DG, Ton T, Karr DE, Gerritsen ME, Goldstein DM, Funk JO.
J Med Chem (2017) 60 : 6516 -6527
PubMed 28665128 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 26 8.43 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4102642 1 9.52
CHEMBL4099992 1 9.30
CHEMBL4064081 1 9.05
CHEMBL4064756 1 8.92
CHEMBL4062003 1 8.92
CHEMBL4061286 1 8.85
CHEMBL4099578 1 8.82
CHEMBL4083740 1 8.74
CHEMBL4086567 1 8.68
CHEMBL4081984 1 8.66
CHEMBL4068509 PRN-1371 1.0 1 8.59
CHEMBL4095844 1 8.47
CHEMBL4089842 1 8.47
CHEMBL4061766 1 8.46
CHEMBL4066763 1 8.46
CHEMBL4092456 1 8.42
CHEMBL4084708 1 8.39
CHEMBL4088057 1 8.33
CHEMBL4095783 1 8.28
CHEMBL4083151 1 8.17
CHEMBL4073347 1 7.96
CHEMBL4091839 1 7.77
CHEMBL4065128 1 7.58
CHEMBL4102058 1 7.57
CHEMBL4084079 1 7.47
CHEMBL4100201 1 7.29

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4102642 IC50 = 0.3 nM 9.52
CHEMBL4099992 IC50 = 0.5 nM 9.30
CHEMBL4064081 IC50 = 0.9 nM 9.05
CHEMBL4064756 IC50 = 1.2 nM 8.92
CHEMBL4062003 IC50 = 1.2 nM 8.92
CHEMBL4061286 IC50 = 1.4 nM 8.85
CHEMBL4099578 IC50 = 1.5 nM 8.82
CHEMBL4083740 IC50 = 1.8 nM 8.74
CHEMBL4086567 IC50 = 2.1 nM 8.68
CHEMBL4081984 IC50 = 2.2 nM 8.66
CHEMBL4068509 PRN-1371 IC50 = 2.6 nM 8.59
CHEMBL4095844 IC50 = 3.4 nM 8.47
CHEMBL4089842 IC50 = 3.4 nM 8.47
CHEMBL4061766 IC50 = 3.5 nM 8.46
CHEMBL4066763 IC50 = 3.5 nM 8.46
CHEMBL4092456 IC50 = 3.8 nM 8.42
CHEMBL4084708 IC50 = 4.1 nM 8.39
CHEMBL4088057 IC50 = 4.7 nM 8.33
CHEMBL4095783 IC50 = 5.3 nM 8.28
CHEMBL4083151 IC50 = 6.8 nM 8.17
CHEMBL4073347 IC50 = 11.0 nM 7.96
CHEMBL4091839 IC50 = 17.0 nM 7.77
CHEMBL4065128 IC50 = 26.0 nM 7.58
CHEMBL4102058 IC50 = 27.0 nM 7.57
CHEMBL4084079 IC50 = 34.0 nM 7.47
CHEMBL4100201 IC50 = 51.0 nM 7.29