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Target
Ras guanyl-releasing protein 3
Ligand
BDBM50244974
Substrate
n/a
Meas. Tech.
ChEMBL_1722136 (CHEMBL4137136)
Ki
18±n/a nM
Citation
Ann, J; Czikora, A; Saini, AS; Zhou, X; Mitchell, GA; Lewin, NE; Peach, ML; Blumberg, PM; Lee, J ?-Arylidene Diacylglycerol-Lactones (DAG-Lactones) as Selective Ras Guanine-Releasing Protein 3 (RasGRP3) Ligands. J Med Chem 61:6261-6276 (2018) [PubMed] Article
More Info.:
Target
Name:
Ras guanyl-releasing protein 3
Synonyms:
GRP3 | GRP3_HUMAN | KIAA0846 | RAS guanyl releasing protein 3 | RASGRP3
Type:
PROTEIN
Mol. Mass.:
78335.20
Organism:
Homo sapiens (Human)
Description:
ChEMBL_1364407
Residue:
690
Sequence:
MGSSGLGKAATLDELLCTCIEMFDDNGELDNSYLPRIVLLMHRWYLSSTELAEKLLCMYRNATGESCNEFRLKICYFMRYWILKFPAEFNLDLGLIRMTEEFREVASQLGYEKHVSLIDISSIPSYDWMRRVTQRKKVSKKGKACLLFDHLEPIELAEHLTFLEHKSFRRISFTDYQSYVIHGCLENNPTLERSIALFNGISKWVQLMVLSKPTPQQRAEVITKFINVAKKLLQLKNFNTLMAVVGGLSHSSISRLKETHSHLSSEVTKNWNEMTELVSSNGNYCNYRKAFADCDGFKIPILGVHLKDLIAVHVIFPDWTEENKVNIVKMHQLSVTLSELVSLQNASHHLEPNMDLINLLTLSLDLYHTEDDIYKLSLVLEPRNSKSQPTSPTTPNKPVVPLEWALGVMPKPDPTVINKHIRKLVESVFRNYDHDHDGYISQEDFESIAANFPFLDSFCVLDKDQDGLISKDEMMAYFLRAKSQLHCKMGPGFIHNFQEMTYLKPTFCEHCAGFLWGIIKQGYKCKDCGANCHKQCKDLLVLACRRFARAPSLSSGHGSLPGSPSLPPAQDEVFEFPGVTAGHRDLDSRAITLVTGSSRKISVRLQRATTSQATQTEPVWSEAGWGDSGSHTFPKMKSKFHDKAAKDKGFAKWENEKPRVHAGVDVVDRGTEFELDQDEGEETRQDGEDG
Inhibitor
Name:
BDBM50244974
Synonyms:
(E)-(2-(hydroxymethyl)-4-((1-methyl-1H-indol-3-yl)methylene)-5-oxo-tetrahydrofuran-2-yl)methyl 4-(dimethylamino)benzoate | CHEMBL472521
Type:
Small organic molecule
Emp. Form.:
C25H26N2O5
Mol. Mass.:
434.4843
SMILES:
CN(C)c1ccc(cc1)C(=O)OCC1(CO)C\C(=C/c2cn(C)c3ccccc23)C(=O)O1