Target
Rap guanine nucleotide exchange factor 3
Ligand
BDBM50098719
Substrate
n/a
Meas. Tech.
ChEMBL_1743822 (CHEMBL4178332)
IC50
2400±n/a nM
Citation
 Wang, PLiu, ZChen, HYe, NCheng, XZhou, J Exchange proteins directly activated by cAMP (EPACs): Emerging therapeutic targets. Bioorg Med Chem Lett 27:1633-1639 (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:
BDBM50098719
Synonyms:
CHEMBL3593329
Type:
Small organic molecule
Emp. Form.:
C16H14Cl2N4O2
Mol. Mass.:
365.214
SMILES:
CC(C)(C)c1cc(no1)C(=O)C(=N\Nc1cc(Cl)cc(Cl)c1)\C#N
Structure:
Search PDB for entries with ligand similarity: