Reaction Details Report a problem with these data
Target
Apelin receptor
Ligand
BDBM507163
Substrate
n/a
Meas. Tech.
[35S]GTPgammaS Binding
EC50
27.0±n/a nM
Citation
Chen, N; Chen, X; Chen, Y; Cheng, AC; Connors, RV; Deignan, J; Dransfield, PJ; Du, X; Fu, Z; Harvey, JS; Heath, JA; Heumann, LV; Horne, DB; Houze, J; Kaller, MR; Kayser, F; Khakoo, AY; Kopecky, DJ; Lai, S; Ma, Z; Medina, JC; Mihalic, JT; Nishimura, N; Olson, SH; Pattaropong, V; Swaminath, G; Wang, X; Wanska, M; Yang, K; Yeh, W Heteroaryl-substituted triazoles as APJ receptor agonists US Patent US11046680 Publication Date 6/29/2021
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:
BDBM507163
Synonyms:
US11046680, Example 34.0 | US11046680, Example 35.0
Type:
Small organic molecule
Emp. Form.:
C22H24FN7O4S
Mol. Mass.:
501.534
SMILES:
COc1cccc(OC)c1-n1c(NS(=O)(=O)[C@@H](C)Cc2ncc(F)cn2)nnc1-c1ccn(C)c1 |r,wU:16.17,(-6.12,6.09,;-4.66,5.62,;-3.51,6.65,;-3.83,8.15,;-2.69,9.19,;-1.22,8.71,;-.9,7.2,;.56,6.73,;1.69,7.77,;-2.05,6.17,;-1.57,4.18,;-.16,3.55,;1.17,4.32,;2.51,3.55,;1.74,2.22,;3.84,2.78,;3.28,4.89,;2.51,6.22,;4.82,4.89,;5.59,6.22,;4.82,7.55,;5.59,8.89,;7.13,8.89,;7.9,10.22,;7.9,7.55,;7.13,6.22,;-.32,2.02,;-1.83,1.7,;-2.6,3.04,;-4.13,3.2,;-4.9,4.53,;-6.4,4.21,;-6.56,2.68,;-7.9,1.91,;-5.16,2.05,)|