Target
Apelin receptor
Ligand
BDBM59072
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
3150±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:
BDBM59072
Synonyms:
5-chloranyl-2-ethylsulfonyl-N-[4-(3-methylpiperidin-1-yl)sulfonylphenyl]pyrimidine-4-carboxamide | 5-chloro-2-esyl-N-[4-(3-methylpiperidino)sulfonylphenyl]pyrimidine-4-carboxamide | 5-chloro-2-ethylsulfonyl-N-[4-(3-methylpiperidin-1-yl)sulfonylphenyl]pyrimidine-4-carboxamide | 5-chloro-2-ethylsulfonyl-N-[4-[(3-methyl-1-piperidinyl)sulfonyl]phenyl]-4-pyrimidinecarboxamide | MLS001116387 | SMR000625583 | cid_16436605
Type:
Small organic molecule
Emp. Form.:
C19H23ClN4O5S2
Mol. Mass.:
486.993
SMILES:
CCS(=O)(=O)c1ncc(Cl)c(n1)C(=O)Nc1ccc(cc1)S(=O)(=O)N1CCCC(C)C1
Structure:
Search PDB for entries with ligand similarity: