Reaction Details Report a problem with these data
Target
RAS guanyl-releasing protein 1
Ligand
BDBM50244449
Substrate
n/a
Meas. Tech.
ChEMBL_1670921 (CHEMBL4020950)
Ki
0.580000±n/a nM
Citation
 Elhalem, E; Donadío, LG; Zhou, X; Lewin, NE; Garcia, LC; Lai, CC; Kelley, JA; Peach, ML; Blumberg, PM; Comin, MJ Exploring the influence of indololactone structure on selectivity for binding to the C1 domains of PKC?, PKC?, and RasGRP. Bioorg Med Chem 25:2971-2980 (2017) [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:
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