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Target
Rap guanine nucleotide exchange factor 3
Ligand
BDBM50511913
Substrate
n/a
Meas. Tech.
ChEMBL_1846040 (CHEMBL4346467)
IC50
4600±n/a nM
Citation
 Wang, P; Luchowska-Sta?ska, U; van Basten, B; Chen, H; Liu, Z; Wiejak, J; Whelan, P; Morgan, D; Lochhead, E; Barker, G; Rehmann, H; Yarwood, SJ; Zhou, J Synthesis and Biochemical Evaluation of Noncyclic Nucleotide Exchange Proteins Directly Activated by cAMP 1 (EPAC1) Regulators. J Med Chem 63:5159-5184 (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:
BDBM50511913
Synonyms:
CHEMBL4459738
Type:
Small organic molecule
Emp. Form.:
C25H20F3N3O4S
Mol. Mass.:
515.504
SMILES:
Cc1cc(Nc2ncccc2C(F)(F)F)cc(c1)S(=O)(=O)NC(=O)COc1ccc2ccccc2c1
Structure:
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