Target
Apelin receptor
Ligand
BDBM58188
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
1490±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:
BDBM58188
Synonyms:
1-benzyl-3-(tert-butyl)-N'-(4-methylphenyl)-1H-pyrazole-5-carbohydrazide | 2-benzyl-5-tert-butyl-N'-(4-methylphenyl)pyrazole-3-carbohydrazide | 2-benzyl-5-tert-butyl-N'-(p-tolyl)pyrazole-3-carbohydrazide | 5-tert-butyl-N'-(4-methylphenyl)-2-(phenylmethyl)-3-pyrazolecarbohydrazide | 5-tert-butyl-N'-(4-methylphenyl)-2-(phenylmethyl)pyrazole-3-carbohydrazide | MLS000834797 | SMR000458415 | cid_2812498
Type:
Small organic molecule
Emp. Form.:
C22H26N4O
Mol. Mass.:
362.468
SMILES:
Cc1ccc(NNC(=O)c2cc(nn2Cc2ccccc2)C(C)(C)C)cc1
Structure:
Search PDB for entries with ligand similarity: