Reaction Details Report a problem with these data
Target
Apelin receptor
Ligand
BDBM50393899
Substrate
n/a
Meas. Tech.
ChEMBL_855886 (CHEMBL2161530)
IC50
4700±n/a nM
Citation
Maloney, PR; Khan, P; Hedrick, M; Gosalia, P; Milewski, M; Li, L; Roth, GP; Sergienko, E; Suyama, E; Sugarman, E; Nguyen, K; Mehta, A; Vasile, S; Su, Y; Stonich, D; Nguyen, H; Zeng, FY; Novo, AM; Vicchiarelli, M; Diwan, J; Chung, TD; Smith, LH; Pinkerton, AB Discovery of 4-oxo-6-((pyrimidin-2-ylthio)methyl)-4H-pyran-3-yl 4-nitrobenzoate (ML221) as a functional antagonist of the apelin (APJ) receptor. Bioorg Med Chem Lett 22:6656-60 (2012) [PubMed] Article
More Info.:
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:
Human
Description:
P35414
Residue:
380
Sequence:
MEEGGDFDNYYGADNQSECEYTDWKSSGALIPAIYMLVFLLGTTGNGLVLWTVFRSSREKRRSADIFIASLAVADLTFVVTLPLWATYTYRDYDWPFGTFFCKLSSYLIFVNMYASVFCLTGLSFDRYLAIVRPVANARLRLRVSGAVATAVLWVLAALLAMPVMVLRTTGDLENTTKVQCYMDYSMVATVSSEWAWEVGLGVSSTTVGFVVPFTIMLTCYFFIAQTIAGHFRKERIEGLRKRRRLLSIIVVLVVTFALCWMPYHLVKTLYMLGSLLHWPCDFDLFLMNIFPYCTCISYVNSCLNPFLYAFFDPRFRQACTSMLCCGQSRCAGTSHSSSGEKSASYSSGHSQGPGPNMGKGGEQMHEKSIPYSQETLVVD