Target
Rap guanine nucleotide exchange factor 3
Ligand
BDBM50280395
Substrate
n/a
Meas. Tech.
ChEMBL_1721963 (CHEMBL4136963)
IC50
3300±n/a nM
Citation
 Sonawane, YAZhu, YGarrison, JCEzell, ELZahid, MCheng, XNatarajan, A Structure-Activity Relationship Studies with Tetrahydroquinoline Analogs as EPAC Inhibitors. ACS Med Chem Lett 8:1183-1187 (2017) [PubMed]  Article 
Target
Name:
Rap guanine nucleotide exchange factor 3
Synonyms:
CGEF1 | EPAC | EPAC 1 | EPAC1 | Exchange factor directly activated by cAMP 1 | Exchange protein directly activated by cAMP 1 | RAPGEF3 | RPGF3_HUMAN | Rap1 guanine-nucleotide-exchange factor directly activated by cAMP | cAMP-GEFI | cAMP-regulated guanine nucleotide exchange factor I
Type:
PROTEIN
Mol. Mass.:
103769.52
Organism:
Homo sapiens (Human)
Description:
ChEMBL_104531
Residue:
923
Sequence:
MKVGWPGESCWQVGLAVEDSPALGAPRVGALPDVVPEGTLLNMVLRRMHRPRSCSYQLLLEHQRPSCIQGLRWTPLTNSEESLDFSESLEQASTERVLRAGRQLHRHLLATCPNLIRDRKYHLRLYRQCCSGRELVDGILALGLGVHSRSQVVGICQVLLDEGALCHVKHDWAFQDRDAQFYRFPGPEPEPVRTHEMEEELAEAVALLSQRGPDALLTVALRKPPGQRTDEELDLIFEELLHIKAVAHLSNSVKRELAAVLLFEPHSKAGTVLFSQGDKGTSWYIIWKGSVNVVTHGKGLVTTLHEGDDFGQLALVNDAPRAATIILREDNCHFLRVDKQDFNRIIKDVEAKTMRLEEHGKVVLVLERASQGAGPSRPPTPGRNRYTVMSGTPEKILELLLEAMGPDSSAHDPTETFLSDFLLTHRVFMPSAQLCAALLHHFHVEPAGGSEQERSTYVCNKRQQILRLVSQWVALYGSMLHTDPVATSFLQKLSDLVGRDTRLSNLLREQWPERRRCHRLENGCGNASPQMKARNLPVWLPNQDEPLPGSSCAIQVGDKVPYDICRPDHSVLTLQLPVTASVREVMAALAQEDGWTKGQVLVKVNSAGDAIGLQPDARGVATSLGLNERLFVVNPQEVHELIPHPDQLGPTVGSAEGLDLVSAKDLAGQLTDHDWSLFNSIHQVELIHYVLGPQHLRDVTTANLERFMRRFNELQYWVATELCLCPVPGPRAQLLRKFIKLAAHLKEQKNLNSFFAVMFGLSNSAISRLAHTWERLPHKVRKLYSALERLLDPSWNHRVYRLALAKLSPPVIPFMPLLLKDMTFIHEGNHTLVENLINFEKMRMMARAARMLHHCRSHNPVPLSPLRSRVSHLHEDSQVARISTCSEQSLSTRSPASTWAYVQQLKVIDNQRELSRLSRELEP
  
Inhibitor
Name:
BDBM50280395
Synonyms:
CHEMBL4171480
Type:
Small organic molecule
Emp. Form.:
C11H10Br2FNO
Mol. Mass.:
351.01
SMILES:
C[C@@H]1CCc2c(Br)c(F)c(Br)cc2N1C=O |r|
Structure:
Search PDB for entries with ligand similarity: