Target
Apelin receptor
Ligand
BDBM76148
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:
BDBM76148
Synonyms:
2-[2-oxidanylidene-2-(4-phenylpiperazin-1-yl)ethyl]sulfanyl-3-prop-2-enyl-5H-pyrimido[5,4-b]indol-4-one | 2-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]sulfanyl-3-prop-2-enyl-5H-pyrimido[5,4-b]indol-4-one | 2-[[2-oxo-2-(4-phenyl-1-piperazinyl)ethyl]thio]-3-prop-2-enyl-5H-pyrimido[5,4-b]indol-4-one | 3-allyl-2-[[2-keto-2-(4-phenylpiperazino)ethyl]thio]-5H-pyrimid[5,4-b]indol-4-one | MLS001236003 | SMR000807080 | cid_22583638
Type:
Small organic molecule
Emp. Form.:
C25H25N5O2S
Mol. Mass.:
459.563
SMILES:
C=CCn1c(SCC(=O)N2CCN(CC2)c2ccccc2)nc2c3ccccc3[nH]c2c1=O
Structure:
Search PDB for entries with ligand similarity: