Ki Summary

Reaction Details

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Target

Apelin receptor

Ligand

BDBM456573

Substrate/Competitor

n/a

Meas. Tech.

GTPγS Binding

EC50

0.110±n/a nM

Citation

Brown, M; Chen, N; Chen, X; Chen, Y; Cheng, AC; Connors, RV; Deignan, J; Dransfield, PJ; Du, X; Fu, Z; Harvey, JS; Heath, JA; Heumann, LV; Houze, J; Kayser, F; Khakoo, AY; Kopecky, D; Lai, S; Ma, Z; Medina, JC; Mihalic, JT; Olson, SH; Pattaropong, V; Swaminath, G; Wang, X; Wanska, M; Yeh, W Triazole furan compounds as agonists of the APJ receptor US Patent US10736883 Publication Date 8/11/2020

More Info.:

Get all data from this article, Assay Method

Apelin receptor

Name:

Apelin receptor

Synonyms:

Type:

Enzyme Catalytic Domain

Mol. Mass.:

42664.06

Organism:

Homo sapiens (Human)

Description:

P35414

Residue:

380

Sequence:

MEEGGDFDNYYGADNQSECEYTDWKSSGALIPAIYMLVFLLGTTGNGLVLWTVFRSSREK
RRSADIFIASLAVADLTFVVTLPLWATYTYRDYDWPFGTFFCKLSSYLIFVNMYASVFCL
TGLSFDRYLAIVRPVANARLRLRVSGAVATAVLWVLAALLAMPVMVLRTTGDLENTTKVQ
CYMDYSMVATVSSEWAWEVGLGVSSTTVGFVVPFTIMLTCYFFIAQTIAGHFRKERIEGL
RKRRRLLSIIVVLVVTFALCWMPYHLVKTLYMLGSLLHWPCDFDLFLMNIFPYCTCISYV
NSCLNPFLYAFFDPRFRQACTSMLCCGQSRCAGTSHSSSGEKSASYSSGHSQGPGPNMGK
GGEQMHEKSIPYSQETLVVD

BDBM456573

n/a

Name

BDBM456573

Synonyms:

US10736883, Example 10.0

Type

Small organic molecule

Emp. Form.

C24H24N6O6S

Mol. Mass.

524.549

SMILES

COc1cccc(OC)c1-n1c(NS(=O)(=O)[C@H](C)[C@H](O)c2ccc(cn2)C#N)nnc1-c1ccc(C)o1 |r,wU:16.17,wD:18.19,(-.07,-1.2,;-1.16,-2.29,;-2.65,-1.9,;-3.05,-.41,;-4.54,-.01,;-5.62,-1.1,;-5.23,-2.59,;-6.31,-3.67,;-7.8,-3.28,;-3.74,-2.98,;-3.34,-4.47,;-1.87,-4.95,;-.54,-4.18,;.79,-4.95,;1.56,-3.61,;.02,-6.28,;2.13,-5.72,;2.13,-7.26,;3.46,-4.95,;3.46,-3.41,;4.79,-5.72,;4.79,-7.26,;6.13,-8.03,;7.51,-7.29,;7.46,-5.72,;6.13,-4.95,;8.84,-8.06,;10.18,-8.83,;-1.87,-6.49,;-3.34,-6.96,;-4.24,-5.72,;-5.73,-5.32,;-6.79,-4.23,;-8.1,-4.55,;-8.1,-6.09,;-9.35,-6.99,;-6.64,-6.56,)|

Structure