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Assay Detail

CHEMBL4057958

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

Binding
Inhibition of FGR (unknown origin)
6
Total Activities
6
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

Tyrosine-protein kinase Fgr (CHEMBL4454)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of 3-morpholino-imidazole[1,5-a]pyrazine BTK inhibitors for rheumatoid arthritis.
Boga SB, Alhassan AB, Liu J, Guiadeen D, Krikorian A, Gao X, Wang J, Yu Y, Anand R, Liu S, Yang C, Wu H, Cai J, Zhu H, Desai J, Maloney K, Gao YD, Fischmann TO, Presland J, Mansueto M, Xu Z, Leccese E, Knemeyer I, Garlisi CG, Bays N, Stivers P, Brandish PE, Hicks A, Cooper A, Kim RM, Kozlowski JA.
Bioorg Med Chem Lett (2017) 27 : 3939 -3943
PubMed 28720503 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 7.17 7.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4077588 1 7.66
CHEMBL4076024 1 7.55
CHEMBL4060757 1 7.41
CHEMBL4062498 1 7.16
CHEMBL4069387 1 6.69
CHEMBL4075954 1 6.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4077588 IC50 = 22.0 nM 7.66
CHEMBL4076024 IC50 = 28.0 nM 7.55
CHEMBL4060757 IC50 = 39.0 nM 7.41
CHEMBL4062498 IC50 = 69.0 nM 7.16
CHEMBL4069387 IC50 = 203.0 nM 6.69
CHEMBL4075954 IC50 = 268.0 nM 6.57