Reaction Details Report a problem with these data
Target
Vascular endothelial growth factor receptor 3
Ligand
BDBM50318958
Substrate
n/a
Meas. Tech.
ChEMBL_635340 (CHEMBL1119653)
IC50
5±n/a nM
Citation
Hudkins, RL; Zulli, AL; Underiner, TL; Angeles, TS; Aimone, LD; Meyer, SL; Pauletti, D; Chang, H; Fedorov, EV; Almo, SC; Fedorov, AA; Ruggeri, BA 8-THP-DHI analogs as potent Type I dual TIE-2/VEGF-R2 receptor tyrosine kinase inhibitors. Bioorg Med Chem Lett 20:3356-60 (2010) [PubMed] Article
More Info.:
Target
Name:
Vascular endothelial growth factor receptor 3
Synonyms:
FLT-4 | FLT4 | Fms-like tyrosine kinase 4 | Focal adhesion kinase 1/vascular endothelial growth factor receptor 3 | VEGFR-3 | VEGFR3 | VGFR3_HUMAN | Vascular endothelial growth factor receptor | Vascular endothelial growth factor receptor 3 (VEGFR-3) | Vascular endothelial growth factor receptor 3 (VEGFR3)
Type:
Protein
Mol. Mass.:
152749.58
Organism:
Homo sapiens (Human)
Description:
P35916-2
Residue:
1363
Sequence:
MQRGAALCLRLWLCLGLLDGLVSGYSMTPPTLNITEESHVIDTGDSLSISCRGQHPLEWAWPGAQEAPATGDKDSEDTGVVRDCEGTDARPYCKVLLLHEVHANDTGSYVCYYKYIKARIEGTTAASSYVFVRDFEQPFINKPDTLLVNRKDAMWVPCLVSIPGLNVTLRSQSSVLWPDGQEVVWDDRRGMLVSTPLLHDALYLQCETTWGDQDFLSNPFLVHITGNELYDIQLLPRKSLELLVGEKLVLNCTVWAEFNSGVTFDWDYPGKQAERGKWVPERRSQQTHTELSSILTIHNVSQHDLGSYVCKANNGIQRFRESTEVIVHENPFISVEWLKGPILEATAGDELVKLPVKLAAYPPPEFQWYKDGKALSGRHSPHALVLKEVTEASTGTYTLALWNSAAGLRRNISLELVVNVPPQIHEKEASSPSIYSRHSRQALTCTAYGVPLPLSIQWHWRPWTPCKMFAQRSLRRRQQQDLMPQCRDWRAVTTQDAVNPIESLDTWTEFVEGKNKTVSKLVIQNANVSAMYKCVVSNKVGQDERLIYFYVTTIPDGFTIESKPSEELLEGQPVLLSCQADSYKYEHLRWYRLNLSTLHDAHGNPLLLDCKNVHLFATPLAASLEEVAPGARHATLSLSIPRVAPEHEGHYVCEVQDRRSHDKHCHKKYLSVQALEAPRLTQNLTDLLVNVSDSLEMQCLVAGAHAPSIVWYKDERLLEEKSGVDLADSNQKLSIQRVREEDAGRYLCSVCNAKGCVNSSASVAVEGSEDKGSMEIVILVGTGVIAVFFWVLLLLIFCNMRRPAHADIKTGYLSIIMDPGEVPLEEQCEYLSYDASQWEFPRERLHLGRVLGYGAFGKVVEASAFGIHKGSSCDTVAVKMLKEGATASEHRALMSELKILIHIGNHLNVVNLLGACTKPQGPLMVIVEFCKYGNLSNFLRAKRDAFSPCAEKSPEQRGRFRAMVELARLDRRRPGSSDRVLFARFSKTEGGARRASPDQEAEDLWLSPLTMEDLVCYSFQVARGMEFLASRKCIHRDLAARNILLSESDVVKICDFGLARDIYKDPDYVRKGSARLPLKWMAPESIFDKVYTTQSDVWSFGVLLWEIFSLGASPYPGVQINEEFCQRLRDGTRMRAPELATPAIRRIMLNCWSGDPKARPAFSELVEILGDLLQGRGLQEEEEVCMAPRSSQSSEEGSFSQVSTMALHIAQADAEDSPPSLQRHSLAARYYNWVSFPGCLARGAETRGSSRMKTFEEFPMTPTTYKGSVDNQTDSGMVLASEEFEQIESRHRQESGFSCKGPGQNVAVTRAHPDSQGRRRRPERGARGGQVFYNSEYGELSEPSEEDHCSPSARVTFFTDNSY
Inhibitor
Name:
BDBM50318958
Synonyms:
CHEMBL1082829 | rac-9-butyl-5-methyl-12-(tetrahydro-2H-pyran-2-yl)-5,7,8,9-tetrahydro-1H-indazolo[5,4-a]pyrrolo[3,4-c]carbazol-3(2H)-one
Type:
Small organic molecule
Emp. Form.:
C29H32N4O2
Mol. Mass.:
468.59
SMILES:
CCCCn1c2ccc(cc2c2c3CNC(=O)c3c3-c4cn(C)nc4CCc3c12)C1CCCCO1