Target
RAS guanyl-releasing protein 1
Ligand
BDBM50244449
Substrate
n/a
Meas. Tech.
ChEMBL_1364410 (CHEMBL3294522)
Ki
0.250000±n/a nM
Citation
 Garcia, LCDonadío, LGMann, EKolusheva, SKedei, NLewin, NEHill, CSKelsey, JSYang, JEsch, TESantos, MPeach, MLKelley, JABlumberg, PMJelinek, RMarquez, VEComin, MJ Synthesis, biological, and biophysical studies of DAG-indololactones designed as selective activators of RasGRP. Bioorg Med Chem 22:3123-40 (2014) [PubMed]  Article 
Target
Name:
RAS guanyl-releasing protein 1
Synonyms:
CalDAG-GEFII | Calcium and DAG-regulated guanine nucleotide exchange factor II | GRP1_HUMAN | RASGRP | RASGRP1 | Ras guanyl-releasing protein
Type:
PROTEIN
Mol. Mass.:
90418.98
Organism:
Homo sapiens (Human)
Description:
ChEMBL_102739
Residue:
797
Sequence:
MGTLGKAREAPRKPSHGCRAASKARLEAKPANSPFPSHPSLAHITQFRMMVSLGHLAKGASLDDLIDSCIQSFDADGNLCRSNQLLQVMLTMHRIVISSAELLQKVITLYKDALAKNSPGLCLKICYFVRYWITEFWVMFKMDASLTDTMEEFQELVKAKGEELHCRLIDTTQINARDWSRKLTQRIKSNTSKKRKVSLLFDHLEPEELSEHLTYLEFKSFRRISFSDYQNYLVNSCVKENPTMERSIALCNGISQWVQLMVLSRPTPQLRAEVFIKFIQVAQKLHQLQNFNTLMAVIGGLCHSSISRLKETSSHVPHEINKVLGEMTELLSSSRNYDNYRRAYGECTDFKIPILGVHLKDLISLYEAMPDYLEDGKVNVHKLLALYNHISELVQLQEVAPPLEANKDLVHLLTLSLDLYYTEDEIYELSYAREPRNHRAPPLTPSKPPVVVDWASGVSPKPDPKTISKHVQRMVDSVFKNYDHDQDGYISQEEFEKIAASFPFSFCVMDKDREGLISRDEITAYFMRASSIYSKLGLGFPHNFQETTYLKPTFCDNCAGFLWGVIKQGYRCKDCGMNCHKQCKDLVVFECKKRAKNPVAPTENNTSVGPVSNLCSLGAKDLLHAPEEGPFTFPNGEAVEHGEESKDRTIMLMGVSSQKISLRLKRAVAHKATQTESQPWIGSEGPSGPFVLSSPRKTAQDTLYVLPSPTSPCPSPVLVRKRAFVKWENKDSLIKSKEELRHLRLPTYQELEQEINTLKADNDALKIQLKYAQKKIESLQLEKSNHVLAQMEQGDCS
  
Inhibitor
Name:
BDBM50244449
Synonyms:
(E)-(2-(hydroxymethyl)-4-((1-methyl-1H-indol-3-yl)methylene)-5-oxo-tetrahydrofuran-2-yl)methyl 2-propylpentanoate | CHEMBL519741
Type:
Small organic molecule
Emp. Form.:
C24H31NO5
Mol. Mass.:
413.5066
SMILES:
CCCC(CCC)C(=O)OCC1(CO)C\C(=C/c2cn(C)c3ccccc23)C(=O)O1
Structure:
Search PDB for entries with ligand similarity: