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Assay Detail

CHEMBL4357706

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

Binding
Inhibition of recombinant human His-tagged FGFR1 (308 to 731 residues) expressed in baculovirus expression system using tyrosine-4 peptide as substrate incubated for 1 hr by Z'-LYTE assay
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Fibroblast growth factor receptor 1 (CHEMBL3650)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-Based Design of a Potent and Selective Covalent Inhibitor for SRC Kinase That Targets a P-Loop Cysteine.
Du G, Rao S, Gurbani D, Henning NJ, Jiang J, Che J, Yang A, Ficarro SB, Marto JA, Aguirre AJ, Sorger PK, Westover KD, Zhang T, Gray NS.
J Med Chem (2020) 63 : 1624 -1641
PubMed 31935084 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 6.74 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4538743 1 7.92
CHEMBL4574265 1 7.77
CHEMBL4563120 1 7.70
CHEMBL3883384 1 7.27
CHEMBL4562024 1 7.14
CHEMBL4442889 1 7.05
CHEMBL4460150 1 6.92
CHEMBL4462060 1 6.43
CHEMBL4528820 1 6.41
CHEMBL4569421 1 5.98
CHEMBL4475369 1 5.17
CHEMBL4515441 1 5.08
CHEMBL4436957 1 -
CHEMBL4453645 1 -
CHEMBL4442593 1 -
CHEMBL4561015 1 -
CHEMBL4592277 1 -
CHEMBL4443649 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4538743 IC50 = 12.0 nM 7.92
CHEMBL4574265 IC50 = 17.0 nM 7.77
CHEMBL4563120 IC50 = 20.0 nM 7.70
CHEMBL3883384 IC50 = 54.0 nM 7.27
CHEMBL4562024 IC50 = 72.0 nM 7.14
CHEMBL4442889 IC50 = 89.0 nM 7.05
CHEMBL4460150 IC50 = 119.0 nM 6.92
CHEMBL4462060 IC50 = 373.0 nM 6.43
CHEMBL4528820 IC50 = 391.0 nM 6.41
CHEMBL4569421 IC50 = 1050.0 nM 5.98
CHEMBL4475369 IC50 = 6710.0 nM 5.17
CHEMBL4515441 IC50 = 8340.0 nM 5.08
CHEMBL4436957 IC50 > 10000.0 nM -
CHEMBL4453645 IC50 > 3330.0 nM -
CHEMBL4442593 IC50 > 10000.0 nM -
CHEMBL4561015 IC50 > 10000.0 nM -
CHEMBL4592277 IC50 > 10000.0 nM -
CHEMBL4443649 IC50 > 10000.0 nM -