Reaction Details |
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Target | Vascular endothelial growth factor receptor 1 |
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Ligand | BDBM50391643 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_847957 (CHEMBL2150257) |
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IC50 | >10000±n/a nM |
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Citation | Kawakita, Y; Miwa, K; Seto, M; Banno, H; Ohta, Y; Tamura, T; Yusa, T; Miki, H; Kamiguchi, H; Ikeda, Y; Tanaka, T; Kamiyama, K; Ishikawa, T Design and synthesis of pyrrolo[3,2-d]pyrimidine HER2/EGFR dual inhibitors: improvement of the physicochemical and pharmacokinetic profiles for potent in vivo anti-tumor efficacy. Bioorg Med Chem20:6171-80 (2012) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Vascular endothelial growth factor receptor 1 |
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Name: | Vascular endothelial growth factor receptor 1 |
Synonyms: | FLT | FLT1 | FRT | Flt-1 | Fms-like tyrosine kinase 1 | Platelet-derived growth factor receptor beta (PDGFRB) | Tyrosine-protein kinase FRT | Tyrosine-protein kinase receptor FLT | VEGFR-1 | VEGFR1 | VGFR1_HUMAN | Vascular endothelial growth factor receptor (VEGFR) | Vascular endothelial growth factor receptor 1 (FLT1) | Vascular endothelial growth factor receptor 1 (VEGFR1) | Vascular endothelial growth factor receptor 1 and 2 (Flt-1 and KDR) | Vascular endothelial growth factor receptor 1 precursor | Vascular permeability factor receptor | fms-related tyrosine kinase 1 | vascular endothelial growth factor/vascular permeability factor receptor |
Type: | Receptor Tyrosine Kinase |
Mol. Mass.: | 150800.23 |
Organism: | Homo sapiens (Human) |
Description: | P17948 |
Residue: | 1338 |
Sequence: | MVSYWDTGVLLCALLSCLLLTGSSSGSKLKDPELSLKGTQHIMQAGQTLHLQCRGEAAHK
WSLPEMVSKESERLSITKSACGRNGKQFCSTLTLNTAQANHTGFYSCKYLAVPTSKKKET
ESAIYIFISDTGRPFVEMYSEIPEIIHMTEGRELVIPCRVTSPNITVTLKKFPLDTLIPD
GKRIIWDSRKGFIISNATYKEIGLLTCEATVNGHLYKTNYLTHRQTNTIIDVQISTPRPV
KLLRGHTLVLNCTATTPLNTRVQMTWSYPDEKNKRASVRRRIDQSNSHANIFYSVLTIDK
MQNKDKGLYTCRVRSGPSFKSVNTSVHIYDKAFITVKHRKQQVLETVAGKRSYRLSMKVK
AFPSPEVVWLKDGLPATEKSARYLTRGYSLIIKDVTEEDAGNYTILLSIKQSNVFKNLTA
TLIVNVKPQIYEKAVSSFPDPALYPLGSRQILTCTAYGIPQPTIKWFWHPCNHNHSEARC
DFCSNNEESFILDADSNMGNRIESITQRMAIIEGKNKMASTLVVADSRISGIYICIASNK
VGTVGRNISFYITDVPNGFHVNLEKMPTEGEDLKLSCTVNKFLYRDVTWILLRTVNNRTM
HYSISKQKMAITKEHSITLNLTIMNVSLQDSGTYACRARNVYTGEEILQKKEITIRDQEA
PYLLRNLSDHTVAISSSTTLDCHANGVPEPQITWFKNNHKIQQEPGIILGPGSSTLFIER
VTEEDEGVYHCKATNQKGSVESSAYLTVQGTSDKSNLELITLTCTCVAATLFWLLLTLFI
RKMKRSSSEIKTDYLSIIMDPDEVPLDEQCERLPYDASKWEFARERLKLGKSLGRGAFGK
VVQASAFGIKKSPTCRTVAVKMLKEGATASEYKALMTELKILTHIGHHLNVVNLLGACTK
QGGPLMVIVEYCKYGNLSNYLKSKRDLFFLNKDAALHMEPKKEKMEPGLEQGKKPRLDSV
TSSESFASSGFQEDKSLSDVEEEEDSDGFYKEPITMEDLISYSFQVARGMEFLSSRKCIH
RDLAARNILLSENNVVKICDFGLARDIYKNPDYVRKGDTRLPLKWMAPESIFDKIYSTKS
DVWSYGVLLWEIFSLGGSPYPGVQMDEDFCSRLREGMRMRAPEYSTPEIYQIMLDCWHRD
PKERPRFAELVEKLGDLLQANVQQDGKDYIPINAILTGNSGFTYSTPAFSEDFFKESISA
PKFNSGSSDDVRYVNAFKFMSLERIKTFEELLPNATSMFDDYQGDSSTLLASPMLKRFTW
TDSKPKASLKIDLRVTSKSKESGLSDVSRPSFCHSSCGHVSEGKRRFTYDHAELERKIAC
CSPPPDYNSVVLYSTPPI
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BDBM50391643 |
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n/a |
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Name | BDBM50391643 |
Synonyms: | CHEMBL2148052 | CHEMBL2148053 |
Type | Small organic molecule |
Emp. Form. | C25H25Cl2N5O4S |
Mol. Mass. | 562.468 |
SMILES | CC(C)(C(=O)NCCn1ccc2ncnc(Nc3ccc(Oc4cccc(Cl)c4)c(Cl)c3)c12)S(C)(=O)=O |
Structure |
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