Reaction Details Report a problem with these data
Target
Rap guanine nucleotide exchange factor 4
Ligand
BDBM517684
Substrate
n/a
Meas. Tech.
In Vitro Evaluation of EPAC2 Inhibition
IC50
2200±300 nM
Citation
 Zhou, J; Liu, Z; Ye, N; Mei, F; Cheng, X EPAC antagonists US Patent  US11124489 Publication Date 9/21/2021 
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:
BDBM517684
Synonyms:
NY0725 | US11124489, Compound 26
Type:
Small organic molecule
Emp. Form.:
C17H10ClF3N4O3
Mol. Mass.:
410.735
SMILES:
FC(F)(F)c1cc(Cl)cc(NNC(C#N)C(=O)c2cc(on2)-c2ccco2)c1
Structure:
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