Reaction Details
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Report a problem with these dataTarget
Apelin receptor
Ligand
BDBM360120
Substrate
n/a
Meas. Tech.
[35S]GTPgammaS Binding Assay
EC50
1.30±n/a nM
Citation
Chen, N; Chen, X; Chen, Y; Cheng, AC; Connors, RV; Deignan, J; Dransfield, PJ; Du, X; Fu, Z; Heath, JA; Horne, DB; Houze, J; Kaller, MR; Khakoo, AY; Kopecky, DJ; Lai, S; Ma, Z; McGee, LR; Medina, JC; Mihalic, JT; Nishimura, N; Olson, SH; Pattaropong, V; Swaminath, G; Wang, X; Yang, K; Yeh, W; Debenedetto, MV; Farrell, RP; Hedley, SJ; Judd, TC; Kayser, F Triazole agonists of the APJ receptor US Patent US10221162 Publication Date 3/5/2019 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:
BDBM360120
Synonyms:
(1R,2S)-N-(4-(2,6-dimethoxyphenyl)-5-(6-methoxy-2-pyridinyl)-4H-1,2,4-triazol-3- | US10221162, Example 422.0
Type:
Small organic molecule
Emp. Form.:
C25H30N8O5S
Mol. Mass.:
554.621
SMILES:
CN[C@@H]([C@H](C)S(=O)(=O)Nc1nnc(-c2cccc(OC)n2)n1-c1c(OC)cccc1OC)c1ncc(C)cn1 |r,wU:2.1,3.3,(2.97,13.76,;4.3,14.53,;4.3,16.07,;2.97,16.84,;2.97,18.38,;1.63,16.07,;.86,14.73,;2.4,14.73,;.3,16.84,;-1.04,16.07,;-1.2,14.53,;-2.7,14.21,;-3.47,15.55,;-5.01,15.55,;-5.78,16.88,;-7.32,16.88,;-8.09,15.55,;-7.32,14.21,;-8.09,12.88,;-9.63,12.88,;-5.78,14.21,;-2.44,16.69,;-2.76,18.2,;-4.23,18.67,;-5.72,18.28,;-6.49,19.61,;-4.55,20.18,;-3.4,21.21,;-1.94,20.73,;-1.62,19.23,;-.15,18.75,;1.33,19.15,;5.63,16.84,;6.97,16.07,;8.3,16.84,;8.3,18.38,;9.63,19.15,;6.97,19.15,;5.63,18.38,)|
Structure:
