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Target
Apelin receptor
Ligand
BDBM269567
Substrate
n/a
Meas. Tech.
[35S]GTPgammaS Binding Assay
pH
7.5±n/a
EC50
1.10±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:
BDBM269567
Synonyms:
US10058550, Example 244.0 | fluoro-2-pyrimidinyl)-1-methoxy-2-propanesulfonamide
Type:
Small organic molecule
Emp. Form.:
C23H24FN7O5S
Mol. Mass.:
529.544
SMILES:
CO[C@@H]([C@H](C)S(=O)(=O)Nc1nnc(-c2cccnc2)n1-c1c(OC)cccc1OC)c1ncc(F)cn1 |r,wD:3.3,2.1,(3.42,-2.85,;1.89,-2.69,;.98,-3.93,;-.55,-3.77,;-1.46,-5.02,;-1.18,-2.36,;-2.58,-2.99,;.23,-1.74,;-1.8,-.96,;-.9,.29,;.64,.29,;1.12,1.75,;-.13,2.66,;-.13,4.2,;1.21,4.97,;1.21,6.51,;-.13,7.28,;-1.46,6.51,;-1.46,4.97,;-1.37,1.75,;-2.84,2.23,;-3.98,1.2,;-3.66,-.31,;-4.81,-1.34,;-5.45,1.67,;-5.77,3.18,;-4.62,4.21,;-3.16,3.74,;-2.01,4.77,;-2.33,6.27,;1.61,-5.34,;3.14,-5.5,;3.77,-6.91,;2.86,-8.15,;3.49,-9.56,;1.33,-7.99,;.7,-6.59,)|
Structure:
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