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Target
Rap guanine nucleotide exchange factor 3
Ligand
BDBM81292
Substrate
n/a
Meas. Tech.
ChEMBL_1900218 (CHEMBL4402333)
EC50
1090±n/a nM
Citation
 Lelle, M; Otte, M; Thon, S; Bertinetti, D; Herberg, FW; Benndorf, K Chemical synthesis and biological activity of novel brominated 7-deazaadenosine-3',5'-cyclic monophosphate derivatives. Bioorg Med Chem 27:1704-1713 (2019) [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:
BDBM81292
Synonyms:
8-Bromoadenosine 3',5'-cyclic monophosphate sodium salt | MLS002153216 | SMR000326869 | cid_23702958 | sodium;(4aR,6R,7R,7aS)-6-(6-amino-8-bromo-9-purinyl)-2-oxido-2-oxo-4a,6,7,7a-tetrahydro-4H-furo[3,2-d][1,3,2]dioxaphosphorin-7-ol | sodium;(4aR,6R,7R,7aS)-6-(6-amino-8-bromo-purin-9-yl)-2-keto-2-oxido-4a,6,7,7a-tetrahydro-4H-furo[3,2-d][1,3,2]dioxaphosphorin-7-ol | sodium;(4aR,6R,7R,7aS)-6-(6-amino-8-bromopurin-9-yl)-2-oxido-2-oxo-4a,6,7,7a-tetrahydro-4H-furo[3,2-d][1,3,2]dioxaphosphinin-7-ol | sodium;(4aR,6R,7R,7aS)-6-(6-azanyl-8-bromanyl-purin-9-yl)-2-oxidanidyl-2-oxidanylidene-4a,6,7,7a-tetrahydro-4H-furo[3,2-d][1,3,2]dioxaphosphinin-7-ol
Type:
Small organic molecule
Emp. Form.:
C10H10BrN5O6P
Mol. Mass.:
407.095
SMILES:
Nc1ncnc2n([C@@H]3O[C@@H]4COP([O-])(=O)O[C@H]4[C@H]3O)c(Br)nc12
Structure:
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