Reaction Details Report a problem with these data
Target
Apelin receptor
Ligand
BDBM269513
Substrate
n/a
Meas. Tech.
[35S]GTPgammaS Binding Assay
pH
7.5±n/a
EC50
830±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 
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:
BDBM269513
Synonyms:
N-(4-(2,6-dimethoxyphenyl)-5-(6-methyl-2-pyridinyl)-4H-1,2,4-triazol-3-yl)ethanesulfonamide | US10058550, Example 30.0 | US10221162, Example 30.0 | US9845310, Example 30.0
Type:
Small organic molecule
Emp. Form.:
C18H21N5O4S
Mol. Mass.:
403.455
SMILES:
CCS(=O)(=O)Nc1nnc(-c2cccc(C)n2)n1-c1c(OC)cccc1OC |(5.82,.28,;5.82,-1.26,;4.49,-2.03,;3.72,-3.36,;5.26,-3.36,;3.16,-1.26,;1.82,-2.03,;1.35,-3.49,;-.19,-3.49,;-.67,-2.03,;-2.16,-1.63,;-2.56,-.14,;-4.04,.25,;-5.13,-.83,;-4.73,-2.32,;-5.82,-3.41,;-3.25,-2.72,;.58,-1.13,;.58,.41,;1.91,1.18,;3.24,.41,;4.58,1.18,;1.91,2.72,;.58,3.49,;-.76,2.72,;-.76,1.18,;-2.09,.41,;-3.43,1.18,)|
Structure:
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