Reaction Details |
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Target | Fibroblast growth factor receptor 1 |
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Ligand | BDBM81377 |
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Substrate/Competitor | n/a |
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Meas. Tech. | In Vitro Activity Kinase Assay |
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IC50 | 9.2±0.0 nM |
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Kd | 2.8±0.0 nM |
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Citation | Zhou, W; Hur, W; McDermott, U; Dutt, A; Xian, W; Ficarro, SB; Zhang, J; Sharma, SV; Brugge, J; Meyerson, M; Settleman, J; Gray, NS A structure-guided approach to creating covalent FGFR inhibitors. Chem Biol17:285-95 (2010) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Fibroblast growth factor receptor 1 |
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Name: | Fibroblast growth factor receptor 1 |
Synonyms: | BFGFR | Basic fibroblast growth factor receptor 1 | Basic fibroblast growth factor receptor 1 (FGFR1) | CD_antigen=CD331 | CEK | FGFBR | FGFR-1 | FGFR-1 Tyrosine Kinase | FGFR-1, (FL) | FGFR1 | FGFR1_HUMAN | FLG | FLT2 | Fibroblast growth factor receptor (FGFR) | Fibroblast growth factor receptor 1 (FGFR-1) | Fibroblast growth factor receptor 1 (FGFR1) | Fms-like tyrosine kinase 2 | HBGFR | N-sam | VEGF-receptor 2 and Fibroblast growth factor receptor 1 | bFGF-R | c-fgr |
Type: | Receptor |
Mol. Mass.: | 91861.70 |
Organism: | Homo sapiens (Human) |
Description: | P11362 |
Residue: | 822 |
Sequence: | MWSWKCLLFWAVLVTATLCTARPSPTLPEQAQPWGAPVEVESFLVHPGDLLQLRCRLRDD
VQSINWLRDGVQLAESNRTRITGEEVEVQDSVPADSGLYACVTSSPSGSDTTYFSVNVSD
ALPSSEDDDDDDDSSSEEKETDNTKPNRMPVAPYWTSPEKMEKKLHAVPAAKTVKFKCPS
SGTPNPTLRWLKNGKEFKPDHRIGGYKVRYATWSIIMDSVVPSDKGNYTCIVENEYGSIN
HTYQLDVVERSPHRPILQAGLPANKTVALGSNVEFMCKVYSDPQPHIQWLKHIEVNGSKI
GPDNLPYVQILKTAGVNTTDKEMEVLHLRNVSFEDAGEYTCLAGNSIGLSHHSAWLTVLE
ALEERPAVMTSPLYLEIIIYCTGAFLISCMVGSVIVYKMKSGTKKSDFHSQMAVHKLAKS
IPLRRQVTVSADSSASMNSGVLLVRPSRLSSSGTPMLAGVSEYELPEDPRWELPRDRLVL
GKPLGEGCFGQVVLAEAIGLDKDKPNRVTKVAVKMLKSDATEKDLSDLISEMEMMKMIGK
HKNIINLLGACTQDGPLYVIVEYASKGNLREYLQARRPPGLEYCYNPSHNPEEQLSSKDL
VSCAYQVARGMEYLASKKCIHRDLAARNVLVTEDNVMKIADFGLARDIHHIDYYKKTTNG
RLPVKWMAPEALFDRIYTHQSDVWSFGVLLWEIFTLGGSPYPGVPVEELFKLLKEGHRMD
KPSNCTNELYMMMRDCWHAVPSQRPTFKQLVEDLDRIVALTSNQEYLDLSMPLDQYSPSF
PDTRSSTCSSGEDSVFSHEPLPEEPCLPRHPAQLANGGLKRR
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BDBM81377 |
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n/a |
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Name | BDBM81377 |
Synonyms: | FIIN-1 |
Type | Small organic molecule |
Emp. Form. | C30H35Cl2N7O4 |
Mol. Mass. | 628.549 |
SMILES | CCNCCCCNc1ncc2CN(C(=O)N(Cc3cccc(NC(=O)C=C)c3)c2n1)c1c(Cl)c(OC)cc(OC)c1Cl |
Structure |
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