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Target
Rap guanine nucleotide exchange factor 4
Ligand
BDBM50384274
Substrate
n/a
Meas. Tech.
ChEMBL_820257 (CHEMBL2033344)
IC50
5900±n/a nM
Citation
 Chen, H; Tsalkova, T; Mei, FC; Hu, Y; Cheng, X; Zhou, J 5-Cyano-6-oxo-1,6-dihydro-pyrimidines as potent antagonists targeting exchange proteins directly activated by cAMP. Bioorg Med Chem Lett 22:4038-43 (2012) [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:
BDBM50384274
Synonyms:
CHEMBL2030613
Type:
Small organic molecule
Emp. Form.:
C19H21N3OS
Mol. Mass.:
339.455
SMILES:
Cc1ccc(C)c(CSc2nc(C3CCCC3)c(C#N)c(=O)[nH]2)c1
Structure:
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