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Target
Rap guanine nucleotide exchange factor 4
Ligand
BDBM50011368
Substrate
n/a
Meas. Tech.
ChEMBL_1352339 (CHEMBL3269756)
IC50
600±n/a nM
Citation
 Chen, H; Wild, C; Zhou, X; Ye, N; Cheng, X; Zhou, J Recent advances in the discovery of small molecules targeting exchange proteins directly activated by cAMP (EPAC). J Med Chem 57:3651-65 (2014) [PubMed]  Article 
Target
Name:
Rap guanine nucleotide exchange factor 4
Synonyms:
CGEF2 | EPAC 2 | EPAC2 | Exchange factor directly activated by cAMP 2 | Exchange protein directly activated by cAMP 2 | RAPGEF4 | RPGF4_HUMAN | cAMP-GEFII | cAMP-regulated guanine nucleotide exchange factor II
Type:
PROTEIN
Mol. Mass.:
115526.83
Organism:
Homo sapiens (Human)
Description:
ChEMBL_1504794
Residue:
1011
Sequence:
MVAAHAAHSSSSAEWIACLDKRPLERSSEDVDIIFTRLKEVKAFEKFHPNLLHQICLCGYYENLEKGITLFRQGDIGTNWYAVLAGSLDVKVSETSSHQDAVTICTLGIGTAFGESILDNTPRHATIVTRESSELLRIEQKDFKALWEKYRQYMAGLLAPPYGVMETGSNNDRIPDKENTPLIEPHVPLRPANTITKVPSEKILRAGKILRNAILSRAPHMIRDRKYHLKTYRQCCVGTELVDWMMQQTPCVHSRTQAVGMWQVLLEDGVLNHVDQEHHFQDKYLFYRFLDDEHEDAPLPTEEEKKECDEELQDTMLLLSQMGPDAHMRMILRKPPGQRTVDDLEIIYEELLHIKALSHLSTTVKRELAGVLIFESHAKGGTVLFNQGEEGTSWYIILKGSVNVVIYGKGVVCTLHEGDDFGKLALVNDAPRAASIVLREDNCHFLRVDKEDFNRILRDVEANTVRLKEHDQDVLVLEKVPAGNRASNQGNSQPQQKYTVMSGTPEKILEHFLETIRLEATLNEATDSVLNDFIMMHCVFMPNTQLCPALVAHYHAQPSQGTEQEKMDYALNNKRRVIRLVLQWAAMYGDLLQEDDVSMAFLEEFYVSVSDDARMIAALKEQLPELEKIVKQISEDAKAPQKKHKVLLQQFNTGDERAQKRQPIRGSDEVLFKVYCMDHTYTTIRVPVATSVKEVISAVADKLGSGEGLIIVKMSSGGEKVVLKPNDVSVFTTLTINGRLFACPREQFDSLTPLPEQEGPTVGTVGTFELMSSKDLAYQMTIYDWELFNCVHELELIYHTFGRHNFKKTTANLDLFLRRFNEIQFWVVTEICLCSQLSKRVQLLKKFIKIAAHCKEYKNLNSFFAIVMGLSNVAVSRLALTWEKLPSKFKKFYAEFESLMDPSRNHRAYRLTVAKLEPPLIPFMPLLIKDMTFTHEGNKTFIDNLVNFEKMRMIANTARTVRYYRSQPFNPDAAQANKNHQDVRSYVRQLNVIDNQRTLSQMSHRLEPRRP
  
Inhibitor
Name:
BDBM50011368
Synonyms:
CHEMBL3260989
Type:
Small organic molecule
Emp. Form.:
C17H25IN2OS
Mol. Mass.:
432.363
SMILES:
[I-].COCCC[n+]1c(C)csc1Nc1c(C)cc(C)cc1C
Structure:
Search PDB for entries with ligand similarity: