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

CHEMBL4013835

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

Unclassified
Chemical reactivity of the compound assessed as BME adduct formation after 2 hrs by LC-MS analysis
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Unclassified
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

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
Kd 7 4.37 4.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4089842 1 4.37
CHEMBL4099992 1 4.37
CHEMBL4064081 1 -
CHEMBL4068509 PRN-1371 1.0 1 -
CHEMBL4095844 1 -
CHEMBL4061766 1 -
CHEMBL4081984 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4089842 Kd = 43000.0 nM 4.37
CHEMBL4099992 Kd = 43000.0 nM 4.37
CHEMBL4064081 Kd = 291000.0 nM -
CHEMBL4068509 PRN-1371 Kd = 164000.0 nM -
CHEMBL4095844 Kd = 933000.0 nM -
CHEMBL4061766 Kd = 4140000.0 nM -
CHEMBL4081984 Kd = 951000.0 nM -