Reaction Details Report a problem with these data
Target
Rap guanine nucleotide exchange factor 3
Ligand
BDBM50384264
Substrate
n/a
Meas. Tech.
ChEMBL_1973121 (CHEMBL4605939)
Kd
4500±n/a nM
Citation
 Shao, H; Mohamed, H; Boulton, S; Huang, J; Wang, P; Chen, H; Zhou, J; Luchowska-Sta?ska, U; Jentsch, NG; Armstrong, AL; Magolan, J; Yarwood, S; Melacini, G Mechanism of Action of an EPAC1-Selective Competitive Partial Agonist. J Med Chem 63:4762-4775 (2020) [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:
BDBM50384264
Synonyms:
CHEMBL316966
Type:
Small organic molecule
Emp. Form.:
C10H12N5O6P
Mol. Mass.:
329.2059
SMILES:
Nc1ncnc2n(cnc12)[C@@H]1O[C@@H]2CO[P@](O)(=O)O[C@H]2[C@H]1O |r|
Structure:
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