Target
Apelin receptor
Ligand
BDBM76127
Substrate
n/a
Meas. Tech.
Dose Response confirmation of uHTS hits from a small molecule agonists of the APJ receptor via a luminescent beta-arrestin assay
EC50
>100000±n/a nM
Citation
 PubChem, PC Dose Response confirmation of uHTS hits from a small molecule agonists 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:
BDBM76127
Synonyms:
2-thiophenecarboxylic acid [2-cyclohexyl-3-(4-methoxy-4-oxobutyl)-7-methyl-6,8-dioxo-7-isoquinolinyl] ester | CMLD004048 | MLS000438638 | SMR000452689 | [2-cyclohexyl-3-(4-methoxy-4-oxidanylidene-butyl)-7-methyl-6,8-bis(oxidanylidene)isoquinolin-7-yl] thiophene-2-carboxylate | [2-cyclohexyl-3-(4-methoxy-4-oxobutyl)-7-methyl-6,8-dioxoisoquinolin-7-yl] thiophene-2-carboxylate | cid_16745587 | thiophene-2-carboxylic acid [2-cyclohexyl-6,8-diketo-3-(4-keto-4-methoxy-butyl)-7-methyl-7-isoquinolyl] ester
Type:
Small organic molecule
Emp. Form.:
C26H29NO6S
Mol. Mass.:
483.577
SMILES:
COC(=O)CCCC1=CC2=CC(=O)C(C)(OC(=O)c3cccs3)C(=O)C2=CN1C1CCCCC1 |c:27,t:7,9|
Structure:
Search PDB for entries with ligand similarity: