Reaction Details Report a problem with these data
Target
Rap guanine nucleotide exchange factor 4
Ligand
BDBM50011360
Substrate
n/a
Meas. Tech.
ChEMBL_1746760 (CHEMBL4181270)
IC50
4400±n/a nM
Citation
 Liu, Z; Zhu, Y; Chen, H; Wang, P; Mei, FC; Ye, N; Cheng, X; Zhou, J Structure-activity relationships of 2-substituted phenyl-N-phenyl-2-oxoacetohydrazonoyl cyanides as novel antagonists of exchange proteins directly activated by cAMP (EPACs). Bioorg Med Chem Lett 27:5163-5166 (2017) [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:
BDBM50011360
Synonyms:
CHEMBL3260990
Type:
Small organic molecule
Emp. Form.:
C16H15ClN4O2
Mol. Mass.:
330.769
SMILES:
CC(C)(C)c1cc(no1)C(=O)C(=N\Nc1cccc(Cl)c1)\C#N
Structure:
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