Ki Summary

Reaction Details

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Target

Apelin receptor

Ligand

BDBM456580

Substrate/Competitor

n/a

Meas. Tech.

GTPγS Binding

EC50

0.260±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

BDBM456580

n/a

Name

BDBM456580

Synonyms:

US10736883, Example 17.0

Type

Small organic molecule

Emp. Form.

C23H23ClN6O6S

Mol. Mass.

546.983

SMILES

COc1cccc(OC)c1-n1c(NS(=O)(=O)[C@H](C)Cc2ncc(Cl)cc2C(N)=O)nnc1-c1ccco1 |r,wD:16.17,(-6.97,-2.85,;-5.64,-3.62,;-4.3,-2.85,;-4.3,-1.31,;-2.97,-.54,;-1.64,-1.31,;-1.64,-2.85,;-.3,-3.62,;1.03,-2.85,;-2.97,-3.62,;-2.97,-5.3,;-1.72,-6.21,;-.39,-5.44,;.94,-6.21,;.17,-7.54,;1.71,-7.54,;2.28,-5.44,;2.28,-3.9,;3.61,-6.21,;4.94,-5.44,;4.94,-3.9,;6.28,-3.13,;7.61,-3.9,;8.94,-3.13,;7.61,-5.44,;6.28,-6.21,;6.28,-7.75,;4.94,-8.52,;7.61,-8.52,;-2.2,-7.67,;-3.74,-7.67,;-4.22,-6.21,;-5.59,-5.62,;-6.06,-4.16,;-7.6,-4.16,;-8.08,-5.62,;-6.83,-6.53,)|

Structure