Ki Summary

Reaction Details

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Target

Apelin receptor

Ligand

BDBM456578

Substrate/Competitor

n/a

Meas. Tech.

GTPγS Binding

EC50

0.210±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

BDBM456578

n/a

Name

BDBM456578

Synonyms:

US10736883, Example 15.0

Type

Small organic molecule

Emp. Form.

C24H25FN6O6S

Mol. Mass.

544.555

SMILES

COc1cccc(OC)c1-n1c(NS(=O)(=O)[C@H](C)Cc2ncc(F)cc2NC(C)=O)nnc1-c1ccco1 |r,wD:16.17,(-.77,6.35,;-1.86,5.26,;-3.34,5.66,;-3.74,7.15,;-5.23,7.55,;-6.32,6.46,;-5.92,4.97,;-7.01,3.88,;-8.5,4.28,;-4.43,4.57,;-4.03,3.09,;-2.57,2.61,;-1.23,3.38,;.1,2.61,;1.43,1.84,;-.67,1.28,;.87,3.94,;.1,5.28,;2.41,3.94,;3.18,5.28,;2.41,6.61,;3.18,7.94,;4.72,7.94,;5.49,9.28,;5.49,6.61,;4.72,5.28,;5.49,3.94,;7.03,3.94,;7.8,2.61,;7.8,5.28,;-2.57,1.07,;-4.03,.59,;-4.94,1.84,;-6.43,2.24,;-7.33,3.48,;-8.8,3.01,;-8.8,1.47,;-7.33,.99,)|

Structure