infigratinib [Ligand Id: 7877] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1852688 (Bgj-398, BGJ-398, BGJ398, Infigratinib, MVP-BGJ398, NVP-BGJ398) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| fibroblast growth factor receptor 1/Fibroblast growth factor receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3650] [GtoPdb: 1808] [UniProtKB: P11362] | ||||||||
| ChEMBL | Biochemical Kinase Assay : Recombinant FGFR1 (2.5 nM), or FGFR4 (12 nM) was prepared as a mixture with substrate KKKSPGEYVNIEFG (SEQ ID NO:1) (20 μM, FGFR1 substrate); Poly [E,Y]4:1 (0.2 mg/ml, FGFR2,3,4 substrate)] in kinase reaction buffer (20 mM HEPES-HCl, pH 7.5, 10 mM MgCl2, 2 mM MnCl2, 1 mM EGTA, 0.02% Brij35, 0.1 mM Na3VO4, 0.02 mg/ml BSA, 2 mM DTT, and 1% DMSO). Compound was added to the enzyme/substrate mixture using acoustic technology and pre-incubated for 0, 15, or 60 minutes at room temperature. After compound pre-incubation, 33P-γ-ATP was added at a final concentration of 10 μM to initiate kinase reactions. Reactions were incubated for 120 minutes at room temperature. | B | 9 | pIC50 | 1 | nM | IC50 | US-9434697-B2. Pyrimidine FGFR4 inhibitors (2016) |
| ChEMBL | Inhibition of recombinant FGFR1 (unknown origin) using peptidic substrates in presence of ATP by Kinase-Glo luminescent kinase assay | B | 9 | pIC50 | 1 | nM | IC50 | Eur J Med Chem (2017) 126: 476-490 [PMID:27914362] |
| ChEMBL | Inhibition of FGFR1 (unknown origin) | B | 9.05 | pIC50 | 0.9 | nM | IC50 | Eur J Med Chem (2021) 220: 113499-113499 [PMID:33940465] |
| GtoPdb | - | - | 9.05 | pIC50 | 0.9 | nM | IC50 | J Med Chem (2011) 54: 7066-83 [PMID:21936542] |
| ChEMBL | Inhibition of N-terminal GST-tagged human FGFR1 cytoplasmic domain (398-822 AA) expressed in baculovirus using FAM-labelled peptide as substrate pre-incubated for 10 mins followed by substrate addition by mobility shift assay | B | 9.23 | pIC50 | 0.59 | nM | IC50 | Eur J Med Chem (2020) 187: 111943-111943 [PMID:31846829] |
| fibroblast growth factor receptor 2/Fibroblast growth factor receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4142] [GtoPdb: 1809] [UniProtKB: P21802] | ||||||||
| GtoPdb | - | - | 8.85 | pIC50 | 1.4 | nM | IC50 | J Med Chem (2011) 54: 7066-83 [PMID:21936542] |
| ChEMBL | Inhibition of FGFR2 (unknown origin) | B | 8.85 | pIC50 | 1.4 | nM | IC50 | Eur J Med Chem (2021) 220: 113499-113499 [PMID:33940465] |
| ChEMBL | Inhibition of recombinant FGFR2 (unknown origin) using peptidic substrates in presence of ATP by Kinase-Glo luminescent kinase assay | B | 9 | pIC50 | 1 | nM | IC50 | Eur J Med Chem (2017) 126: 476-490 [PMID:27914362] |
| fibroblast growth factor receptor 3/Fibroblast growth factor receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2742] [GtoPdb: 1810] [UniProtKB: P22607] | ||||||||
| GtoPdb | - | - | 9 | pIC50 | 1 | nM | IC50 | J Med Chem (2011) 54: 7066-83 [PMID:21936542] |
| ChEMBL | Inhibition of recombinant GST fused FGFR3 (unknown origin) using poly(EY) 4:1 as substrate in presence of [gamma-32P]ATP after 10 mins by scintillation counting method | B | 9 | pIC50 | 1 | nM | IC50 | Eur J Med Chem (2017) 126: 476-490 [PMID:27914362] |
| ChEMBL | Inhibition of FGFR3 (unknown origin) | B | 9 | pIC50 | 1 | nM | IC50 | Eur J Med Chem (2021) 220: 113499-113499 [PMID:33940465] |
| fibroblast growth factor receptor 4/Fibroblast growth factor receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3973] [GtoPdb: 1811] [UniProtKB: P22455] | ||||||||
| ChEMBL | Inhibition of phosphorylated FGFR4 (388 to 802 residues) (unknown origin) using 5-Fluo-Ahx-KKKKEEIYFFFG-NH2 as substrate after 60 mins by microfluidic mobility shift assay | B | 7.15 | pIC50 | 71 | nM | IC50 | Medchemcomm (2017) 8: 1604-1613 [PMID:30108871] |
| ChEMBL | Inhibition of recombinant non-phosphorylated FGFR4 kinase domain (442 to 753) (unknown origin) expressed in Sf9 insect cells using 5-Fluo-Ahx-KKKKEEIYFFFG-NH2 peptide as substrate in presence of ATP measured after 60 mins by caliper microfluidic mobility shift assay | B | 7.15 | pIC50 | 71 | nM | IC50 | J Med Chem (2020) 63: 12542-12573 [PMID:32930584] |
| ChEMBL | Inhibition of non-phosphorylated N-terminal His6-tagged FGFR4 C477A mutant (G442 to E753 residues) (unknown origin) expressed in sf9 cells using 5-Fluo-Ahx-KKKKEEIYFFFG-NH2 as substrate after 60 mins by microfluidic mobility shift assay | B | 7.19 | pIC50 | 64 | nM | IC50 | Medchemcomm (2017) 8: 1604-1613 [PMID:30108871] |
| ChEMBL | Inhibition of wild type non-phosphorylated N-terminal His6-tagged FGFR4 (G442 to E753 residues) (unknown origin) expressed in sf9 cells using 5-Fluo-Ahx-KKKKEEIYFFFG-NH2 as substrate after 60 mins by microfluidic mobility shift assay | B | 7.21 | pIC50 | 62 | nM | IC50 | Medchemcomm (2017) 8: 1604-1613 [PMID:30108871] |
| GtoPdb | - | - | 7.22 | pIC50 | 60 | nM | IC50 | J Med Chem (2011) 54: 7066-83 [PMID:21936542] |
| ChEMBL | Inhibition of FGFR4 (unknown origin) | B | 7.22 | pIC50 | 60 | nM | IC50 | Eur J Med Chem (2021) 220: 113499-113499 [PMID:33940465] |
| ChEMBL | Inhibition of recombinant FGFR4 (unknown origin) using peptidic substrates in presence of ATP by Kinase-Glo luminescent kinase assay | B | 7.22 | pIC50 | 60 | nM | IC50 | Eur J Med Chem (2017) 126: 476-490 [PMID:27914362] |
| ChEMBL | Biochemical Kinase Assay : Recombinant FGFR1 (2.5 nM), or FGFR4 (12 nM) was prepared as a mixture with substrate KKKSPGEYVNIEFG (SEQ ID NO:1) (20 μM, FGFR1 substrate); Poly [E,Y]4:1 (0.2 mg/ml, FGFR2,3,4 substrate)] in kinase reaction buffer (20 mM HEPES-HCl, pH 7.5, 10 mM MgCl2, 2 mM MnCl2, 1 mM EGTA, 0.02% Brij35, 0.1 mM Na3VO4, 0.02 mg/ml BSA, 2 mM DTT, and 1% DMSO). Compound was added to the enzyme/substrate mixture using acoustic technology and pre-incubated for 0, 15, or 60 minutes at room temperature. After compound pre-incubation, 33P-γ-ATP was added at a final concentration of 10 μM to initiate kinase reactions. Reactions were incubated for 120 minutes at room temperature. | B | 7.89 | pIC50 | 13 | nM | IC50 | US-9434697-B2. Pyrimidine FGFR4 inhibitors (2016) |
| ChEMBL | Inhibition of non-phosphorylated N-terminal His6-tagged FGFR4 C552A mutant (G442 to E753 residues) (unknown origin) expressed in sf9 cells using 5-Fluo-Ahx-KKKKEEIYFFFG-NH2 as substrate after 60 mins by microfluidic mobility shift assay | B | 9.09 | pIC50 | 0.82 | nM | IC50 | Medchemcomm (2017) 8: 1604-1613 [PMID:30108871] |
| fibroblast growth factor receptor 4/Fibroblast growth factor receptor 4 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3839] [GtoPdb: 1811] [UniProtKB: Q03142] | ||||||||
| ChEMBL | Inhibition of FGFR4 in mouse BAF3 cells assessed as reduction in cell viability incubated for 2 days by cell proliferation assay | B | 6.24 | pIC50 | 581 | nM | IC50 | J Med Chem (2020) 63: 12542-12573 [PMID:32930584] |
| ChEMBL | Inhibition of FGFR4 in mouse BAF3 cells assessed as decrease in FGFR4 phosphorylation incubated for 40 mins | B | 6.27 | pIC50 | 541 | nM | IC50 | J Med Chem (2020) 63: 12542-12573 [PMID:32930584] |
| SMO/Smoothened homolog in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5971] [GtoPdb: 239] [UniProtKB: Q99835] | ||||||||
| ChEMBL | Displacement of [3H]-cyclopamine from SMO V404M mutant in gefitinib resistant human HCC827 cells by scintillation counting | B | 7.33 | pKi | 46.5 | nM | Ki | J Med Chem (2017) 60: 7447-7458 [PMID:28787156] |
| kinase insert domain receptor in Human [GtoPdb: 1813] [UniProtKB: P35968] | ||||||||
| GtoPdb | - | - | 6.74 | pIC50 | 180 | nM | IC50 | J Med Chem (2011) 54: 7066-83 [PMID:21936542] |
ChEMBL data shown on this page come from version 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]
