Target
Apelin receptor
Ligand
BDBM43465
Substrate
n/a
Meas. Tech.
Dose Response confirmation of uHTS hits from a small molecule antagonists of the APJ receptor via a luminescent beta-arrestin assay
IC50
3980±n/a nM
Citation
 PubChem, PC Dose Response confirmation of uHTS hits from a small molecule antagonists of the APJ receptor via a luminescent beta-arrestin assay PubChem Bioassay (2010)[AID] 
Target
Name:
Apelin receptor
Synonyms:
AGTRL1 | APJ | APJ_HUMAN | APLNR | Angiotensin receptor-like 1 | Apelin receptor | Apelin receptor (APJ) | G-protein coupled receptor APJ | G-protein coupled receptor HG11
Type:
Enzyme Catalytic Domain
Mol. Mass.:
42664.06
Organism:
Homo sapiens (Human)
Description:
P35414
Residue:
380
Sequence:
MEEGGDFDNYYGADNQSECEYTDWKSSGALIPAIYMLVFLLGTTGNGLVLWTVFRSSREKRRSADIFIASLAVADLTFVVTLPLWATYTYRDYDWPFGTFFCKLSSYLIFVNMYASVFCLTGLSFDRYLAIVRPVANARLRLRVSGAVATAVLWVLAALLAMPVMVLRTTGDLENTTKVQCYMDYSMVATVSSEWAWEVGLGVSSTTVGFVVPFTIMLTCYFFIAQTIAGHFRKERIEGLRKRRRLLSIIVVLVVTFALCWMPYHLVKTLYMLGSLLHWPCDFDLFLMNIFPYCTCISYVNSCLNPFLYAFFDPRFRQACTSMLCCGQSRCAGTSHSSSGEKSASYSSGHSQGPGPNMGKGGEQMHEKSIPYSQETLVVD
  
Inhibitor
Name:
BDBM43465
Synonyms:
(Z)-2,3-bis(chloranyl)-3-[(4-chlorophenyl)methylsulfinyl]-N-(6-methoxypyridin-3-yl)prop-2-enamide | (Z)-2,3-dichloro-3-(4-chlorobenzyl)sulfinyl-N-(6-methoxy-3-pyridyl)acrylamide | (Z)-2,3-dichloro-3-[(4-chlorophenyl)methylsulfinyl]-N-(6-methoxy-3-pyridinyl)-2-propenamide | (Z)-2,3-dichloro-3-[(4-chlorophenyl)methylsulfinyl]-N-(6-methoxypyridin-3-yl)prop-2-enamide | 2,3-dichloro-3-[(4-chlorobenzyl)sulfinyl]-N-(6-methoxy-3-pyridinyl)acrylamide | MLS000706843 | SMR000334340 | cid_1472220
Type:
Small organic molecule
Emp. Form.:
C16H13Cl3N2O3S
Mol. Mass.:
419.71
SMILES:
COc1ccc(NC(=O)C(Cl)=C(Cl)S(=O)Cc2ccc(Cl)cc2)cn1 |w:11.11|
Structure:
Search PDB for entries with ligand similarity: