Reaction Details |
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Target | Fibroblast growth factor receptor 1 |
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Ligand | BDBM301310 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_2188243 (CHEMBL5100325) |
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IC50 | 0.900000±n/a nM |
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Citation | Shvartsbart, A; Roach, JJ; Witten, MR; Koblish, H; Harris, JJ; Covington, M; Hess, R; Lin, L; Frascella, M; Truong, L; Leffet, L; Conlen, P; Beshad, E; Klabe, R; Katiyar, K; Kaldon, L; Young-Sciame, R; He, X; Petusky, S; Chen, KJ; Horsey, A; Lei, HT; Epling, LB; Deller, MC; Vechorkin, O; Yao, W Discovery of Potent and Selective Inhibitors of Wild-Type and Gatekeeper Mutant Fibroblast Growth Factor Receptor (FGFR) 2/3. J Med Chem65:15433-15442 (2022) [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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BDBM301310 |
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n/a |
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Name | BDBM301310 |
Synonyms: | 3-(2,6-difluoro-3,5-dimethoxyphenyl)-1-ethyl-8-(morpholin-4-ylmethyl)-1,3,4,7-tetrahydro-2H-pyrrolo[3',2':5,6]pyrido[4,3-d]pyrimidin-2-one | US10131667, Example 126 | US11053246, Example 126 | US11407750, Compound 6 | US9611267, Example 126 |
Type | Small organic molecule |
Emp. Form. | C24H27F2N5O4 |
Mol. Mass. | 487.4991 |
SMILES | CCN1C(=O)N(Cc2cnc3[nH]c(CN4CCOCC4)cc3c12)c1c(F)c(OC)cc(OC)c1F |
Structure |
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