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Assay Detail

CHEMBL5168103

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

Binding
Inhibition of wild type FGFR1 (unknown origin) using Poly (Glu,Tyr) 4:1 as substrate incubated for 60 mins in presence of ATP by ELISA
36
Total Activities
36
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

Discovery of 1,6-Naphthyridin-2(1<i>H</i>)-one Derivatives as Novel, Potent, and Selective FGFR4 Inhibitors for the Treatment of Hepatocellular Carcinoma.
Zhang X, Wang Y, Ji J, Si D, Bao X, Yu Z, Zhu Y, Zhao L, Li W, Liu J.
J Med Chem (2022) 65 : 7595 -7618
PubMed 35635004 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 36 6.39 8.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5175788 1 8.38
CHEMBL5180280 1 8.08
CHEMBL5185308 1 7.77
CHEMBL5181533 1 7.52
CHEMBL5186034 1 7.34
CHEMBL5202677 1 7.31
CHEMBL5189122 1 7.28
CHEMBL5200589 1 7.09
CHEMBL5193663 1 7.01
CHEMBL5192973 1 6.72
CHEMBL5204828 1 6.66
CHEMBL5173719 1 6.62
CHEMBL5173193 1 6.55
CHEMBL5186125 1 6.28
CHEMBL5172762 1 6.20
CHEMBL5188086 1 6.10
CHEMBL5191143 1 6.10
CHEMBL4514636 FISOGATINIB 2.0 1 6.02
CHEMBL5176617 1 6.01
CHEMBL5203036 1 5.85
CHEMBL5190597 1 5.71
CHEMBL5192694 1 5.60
CHEMBL5170061 1 5.55
CHEMBL5184648 1 5.52
CHEMBL5200584 1 5.51
CHEMBL5189713 1 5.43
CHEMBL5194694 1 5.39
CHEMBL5186071 1 5.39
CHEMBL5179371 1 5.38
CHEMBL5206076 1 5.37

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5175788 IC50 = 4.2 nM 8.38
CHEMBL5180280 IC50 = 8.3 nM 8.08
CHEMBL5185308 IC50 = 17.0 nM 7.77
CHEMBL5181533 IC50 = 30.4 nM 7.52
CHEMBL5186034 IC50 = 45.7 nM 7.34
CHEMBL5202677 IC50 = 48.5 nM 7.31
CHEMBL5189122 IC50 = 52.8 nM 7.28
CHEMBL5200589 IC50 = 80.8 nM 7.09
CHEMBL5193663 IC50 = 96.6 nM 7.01
CHEMBL5192973 IC50 = 192.0 nM 6.72
CHEMBL5204828 IC50 = 221.0 nM 6.66
CHEMBL5173719 IC50 = 240.8 nM 6.62
CHEMBL5173193 IC50 = 281.0 nM 6.55
CHEMBL5186125 IC50 = 527.0 nM 6.28
CHEMBL5172762 IC50 = 637.0 nM 6.20
CHEMBL5188086 IC50 = 799.0 nM 6.10
CHEMBL5191143 IC50 = 791.0 nM 6.10
CHEMBL4514636 FISOGATINIB IC50 = 950.0 nM 6.02
CHEMBL5176617 IC50 = 983.0 nM 6.01
CHEMBL5203036 IC50 = 1422.0 nM 5.85
CHEMBL5190597 IC50 = 1952.0 nM 5.71
CHEMBL5192694 IC50 = 2490.0 nM 5.60
CHEMBL5170061 IC50 = 2799.0 nM 5.55
CHEMBL5184648 IC50 = 3000.0 nM 5.52
CHEMBL5200584 IC50 = 3069.0 nM 5.51
CHEMBL5189713 IC50 = 3731.0 nM 5.43
CHEMBL5186071 IC50 = 4041.0 nM 5.39
CHEMBL5194694 IC50 = 4028.0 nM 5.39
CHEMBL5179371 IC50 = 4129.0 nM 5.38
CHEMBL5206076 IC50 = 4300.0 nM 5.37
CHEMBL5202150 IC50 > 5000.0 nM -
CHEMBL5196437 IC50 > 5000.0 nM -
CHEMBL5176243 IC50 > 5000.0 nM -
CHEMBL5193780 IC50 > 5000.0 nM -
CHEMBL5188499 IC50 > 5000.0 nM -
CHEMBL5204303 IC50 > 5000.0 nM -