Target
Vasopressin V2 receptor
Ligand
BDBM35703
Substrate
BDBM35667
Meas. Tech.
Binding Affinity Assay (Ki) and cAMP Accumulation Activity Assay (EC50)
pH
7.4±n/a
Temperature
296.15±n/a K
Ki
14±n/a nM
EC50
1.25±n/a nM
Comments
AMP accumulation max activity = 90.4 %.
Citation
 Tsukamoto, IKoshio, HAkamatsu, SKuramochi, TSaitoh, CYatsu, TYanai-Inamura, HKitada, CYamamoto, ESakamoto, STsukamoto, S Preparation of (4,4-difluoro-1,2,3,4-tetrahydro-5H-1-benzazepin-5-ylidene)acetamide derivatives as novel arginine vasopressin V(2) receptor agonists. Bioorg Med Chem 16:9524-35 (2008) [PubMed]  Article 
Target
Name:
Vasopressin V2 receptor
Synonyms:
ADHR | AVPR V2 | AVPR2 | Antidiuretic hormone receptor | DIR | DIR3 | Renal-type arginine vasopressin receptor | V2R | V2R_HUMAN | VASOPRESSIN V2 | Vasopressin V2 receptor | Vasopressin receptor
Type:
Receptor
Mol. Mass.:
40295.28
Organism:
Homo sapiens (Human)
Description:
P30518
Residue:
371
Sequence:
MLMASTTSAVPGHPSLPSLPSNSSQERPLDTRDPLLARAELALLSIVFVAVALSNGLVLAALARRGRRGHWAPIHVFIGHLCLADLAVALFQVLPQLAWKATDRFRGPDALCRAVKYLQMVGMYASSYMILAMTLDRHRAICRPMLAYRHGSGAHWNRPVLVAWAFSLLLSLPQLFIFAQRNVEGGSGVTDCWACFAEPWGRRTYVTWIALMVFVAPTLGIAACQVLIFREIHASLVPGPSERPGGRRRGRRTGSPGEGAHVSAAVAKTVRMTLVIVVVYVLCWAPFFLVQLWAAWDPEAPLEGAPFVLLMLLASLNSCTNPWIYASFSSSVSSELRSLLCCARGRTPPSLGPQDESCTTASSSLAKDTSS
  
Inhibitor
Name:
BDBM35703
Synonyms:
5H-1-benzazepin-5-ylidene acetamide, 10j | racemate
Type:
Small organic molecule
Emp. Form.:
C30H29ClF2N4O2
Mol. Mass.:
551.027
SMILES:
CC1CCN(C1)c1ccc(C(=O)N2CCC(F)(F)\C(=C/C(=O)NCc3ccccn3)c3ccccc23)c(Cl)c1
Structure:
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Substrate
Name:
BDBM35667
Synonyms:
AVP | CHEMBL373742 | US10131692, 44 (AVP) | [3H]Arginine vasopressin | [3H]Argipressin tannate | [3H]vasopressin
Type:
radiolabeled ligand
Emp. Form.:
C46H65N15O12S2
Mol. Mass.:
1084.232
SMILES:
[#7]-[#6@H]-1-[#6]-[#16]-[#16]-[#6]-[#6@H](-[#7]-[#6](=O)-[#6@H](-[#6]-[#6](-[#7])=O)-[#7]-[#6](=O)-[#6@H](-[#6]-[#6]-[#6](-[#7])=O)-[#7]-[#6](=O)-[#6@H](-[#6]-c2ccccc2)-[#7]-[#6](=O)-[#6@H](-[#6]-c2ccc(-[#8])cc2)-[#7]-[#6]-1=O)-[#6](=O)-[#7]-1-[#6]-[#6]-[#6]-[#6@H]-1-[#6](=O)-[#7]-[#6@@H](-[#6]-[#6]-[#6]\[#7]=[#6](\[#7])-[#7])-[#6](=O)-[#7]-[#6]-[#6](-[#7])=O
Structure:
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