Reaction Details |
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Target | Vascular endothelial growth factor receptor 2 |
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Ligand | BDBM16673 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_943682 (CHEMBL2344826) |
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IC50 | 2600±n/a nM |
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Citation | Yang, LL; Li, GB; Ma, S; Zou, C; Zhou, S; Sun, QZ; Cheng, C; Chen, X; Wang, LJ; Feng, S; Li, LL; Yang, SY Structure-activity relationship studies of pyrazolo[3,4-d]pyrimidine derivatives leading to the discovery of a novel multikinase inhibitor that potently inhibits FLT3 and VEGFR2 and evaluation of its activity against acute myeloid leukemia in vitro and in vivo. J Med Chem56:1641-55 (2013) [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 2 |
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Name: | Vascular endothelial growth factor receptor 2 |
Synonyms: | FLK-1b | Fetal liver kinase 1b | Kinase insert domain receptor | Kinase insert domain receptor-B | Protein-tyrosine kinase receptor flk-1b | VEGFR-2 | VEGFR-2 homolog B | VGFR2_DANRE | Vascular endothelial growth factor receptor 2 homolog B | flk1b | kdr | kdrb | si:ch211-254j6.1 |
Type: | PROTEIN |
Mol. Mass.: | 153046.15 |
Organism: | Danio rerio |
Description: | ChEMBL_943682 |
Residue: | 1357 |
Sequence: | MAKTSYALLLLDILLTFNVAKAIELRFVPDPPTLNITEKTIKINASDTLQITCRGRQILE
WSTPHNRTSSETRLTISDCSGDGLFCSTLTLSKAVANETGEYRCFYKSLPKEDGKTSVAV
YVFIQDYRTPFVRIAQDYDVVFIREGEQVVIPCLVSVEDLNVTLYTKYPVKELSTDGKEV
IWDSRRGFILPSRVVSYAGVVYCQTTIRNETFQSSPYIVAVVGYKIYDLTLSPQHERLTV
GERLILNCTAHTELNVGIDFQWTFPHEKRSVNGSMSTSRYKTSSNKKKLWNSLELSNTLT
VENVTLNDTGEYICTASSGQMQKIAQASLIVYEKPFIALSDQLWQTVEAKAGDAEAKILV
KYYAYPEPAVRWYKNDQLIVLRDEYRMKFYRGVHLTIYGVTEKDAGNYTVVMTNKITKEE
QRRTFQLVVNDLPRIFEKDVSLDRDVHMYGSSPTLTCTASGGSSPVTIKWQWMPREDCPV
RFLPKSDTRMAKCDKWREMSNNTGKNPLISQTSVDERTLKTISTLKIQKAVDHALYRCIA
TNKMGQDQRVIVFQVTRFLNLSVLPSSSPIEGQDVIMRCVADRLLYYNLRWYRVANVANH
DPPPAAVPCDTLTLSHLHQPNVTVSGLQGTNVTLDMPIPNATMMDQGLYACQVEIVGTNE
KTCLLHNLRLRALEMSRIVTNLTDQRVNVSDSTTLVCEVSGTPTPTIVWTKDNQTVMEGS
GVILKRSNRVLTIQRVKKEDSGLYICTACNQQGCESSEARISVDGAEEKMNVELIMPIGA
VVIAMFLWLLIVFVIRNRKRPNDGDLKTGYLSIILDSDDMPMDEHCERLTYDASKWEFPR
DRLKLGEPLGRGAFGQVVEATAYGIEKATTCTTVAVKMLKEGATSSEYRALMSELKILIH
IGHHLNVVNLLGACTKQGGPLMVIVEYCKHGNLSSYLKSKRGEYSPYKKRTPRMPNRREV
QQDEDPREGDLGLGTSTRLDICTGTAVCTRTGEQTYKTLQDEQESSDWDHLTMEDLISYS
FQVAKGMEFLASRKCIHRDLAARNILLSENSVVKICDFGLARDVYKDPDYVRKGDARLPL
KWMAPETIFDRVYTTQSDVWSFGVLLWEIFSLGASPYPGVCIDESFCRRLKEGTRMRAPD
YATPEIYQTMLDCWLDRPLDRPTFTQLVEHLGNLLQASAQQDGKDYIPLTNGEMEEELVA
PHLNVTSKRSFYAGNTEAQLHYDNAPPLGFPQQMNSSGVPVNMTGFVDIPLEHTTVMDGH
VDCGVGLSREQMKALDRQAQRPLNFSPLLRCKSKESLASESSNQTSGYQSGYHSDDAEAP
IYANEEMILKRDIRKKPPLPKRNDKFSAEVRYSAPPV
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BDBM16673 |
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n/a |
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Name | BDBM16673 |
Synonyms: | 4-[4-({[4-chloro-3-(trifluoromethyl)phenyl]carbamoyl}amino)phenoxy]-N-methylpyridine-2-carboxamide | 4-[4-[[4-chloro-3-(trifluoromethyl)phenyl]carbamoylamino]phenoxy]-N-methyl-picolinamide;tosylic acid | BAY 43-9006 | BAY 439006 | BAY439006 | CHEMBL1336 | Hit compound, 8 | Nexavar | Sorafenib | Sorafenib, 4 | US10183928, Sorafenib | US10202365, Compound Sorafenib | US10227329, Compound Sorafenib | US10584114, Compound Sorafenib | US10774070, Compound Sorafenib | US10980809, Example Sorafenib | US11279688, Compound Sorafenib | US11505527, Compound Sorafenib | US9029401, Sorafenib | US9469639, Sorafenib | US9902709, Comparative example 1 | Xarelto | cid_216239 |
Type | Small organic molecule |
Emp. Form. | C21H16ClF3N4O3 |
Mol. Mass. | 464.825 |
SMILES | CNC(=O)c1cc(Oc2ccc(NC(=O)Nc3ccc(Cl)c(c3)C(F)(F)F)cc2)ccn1 |
Structure |
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