Target
RAS guanyl-releasing protein 1
Ligand
BDBM50241855
Substrate
n/a
Meas. Tech.
ChEMBL_1670921 (CHEMBL4020950)
Ki
31±n/a nM
Citation
 Elhalem, EDonadío, LGZhou, XLewin, NEGarcia, LCLai, CCKelley, JAPeach, MLBlumberg, PMComin, 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:
BDBM50241855
Synonyms:
CHEMBL4075373
Type:
Small organic molecule
Emp. Form.:
C25H33NO5
Mol. Mass.:
427.5332
SMILES:
CC(C)C(C\C=C1/CC(CO)(COC(=O)c2cn(C)c3ccccc23)OC1=O)C(C)C
Structure:
Search PDB for entries with ligand similarity: