Reaction Details Report a problem with these data
Target
Apelin receptor
Ligand
BDBM270128
Substrate
n/a
Meas. Tech.
[35S]GTPgammaS Binding Assay
pH
7.5±n/a
EC50
0.120±n/a nM
Comments
extracted
Citation
Chen, N; Chen, X; Chen, Y; Fu, Z; Heath, JA; Horne, DB; Kaller, MR; Khakoo, AY; Kopecky, DJ; Ma, Z; Mihalic, JT; Swaminath, G; Wang, X; Yeh, W Methods of treating heart failure US Patent US10058550 Publication Date 8/28/2018
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:
Homo sapiens (Human)
Description:
P35414
Residue:
380
Sequence:
MEEGGDFDNYYGADNQSECEYTDWKSSGALIPAIYMLVFLLGTTGNGLVLWTVFRSSREKRRSADIFIASLAVADLTFVVTLPLWATYTYRDYDWPFGTFFCKLSSYLIFVNMYASVFCLTGLSFDRYLAIVRPVANARLRLRVSGAVATAVLWVLAALLAMPVMVLRTTGDLENTTKVQCYMDYSMVATVSSEWAWEVGLGVSSTTVGFVVPFTIMLTCYFFIAQTIAGHFRKERIEGLRKRRRLLSIIVVLVVTFALCWMPYHLVKTLYMLGSLLHWPCDFDLFLMNIFPYCTCISYVNSCLNPFLYAFFDPRFRQACTSMLCCGQSRCAGTSHSSSGEKSASYSSGHSQGPGPNMGKGGEQMHEKSIPYSQETLVVD
Inhibitor
Name:
BDBM270128
Synonyms:
(1R,2S)N-(4-(2,6-dimethoxyphenyl)-5-(6-methoxypyridin-2-yl)-4H-1,2,4-triazol-3-yl)-1-(2-methoxyethoxy)-1-(5-methylpyrimidin-2-yl)propane-2-sulfonamide | US10058550, Example 695.0 | US10221162, Example 695.0 | US9845310, Example 695.0
Type:
Small organic molecule
Emp. Form.:
C30H43N3O5SSi
Mol. Mass.:
585.83
SMILES:
COc1ccc(CN(Cc2ccc(OC)cc2)S(=O)(=O)[C@@H](C)[C@H](O[Si](C)(C)C(C)(C)C)c2ncc(C)cn2)cc1 |r|