Ki Summary

Reaction Details

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Target

Apelin receptor

Ligand

BDBM456577

Substrate/Competitor

n/a

Meas. Tech.

GTPγS Binding

EC50

0.200±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

BDBM456577

n/a

Name

BDBM456577

Synonyms:

US10736883, Example 14.0

Type

Small organic molecule

Emp. Form.

C22H22ClN5O5S

Mol. Mass.

503.959

SMILES

COc1cccc(OC)c1-n1c(NS(=O)(=O)[C@H](C)Cc2ccc(Cl)cn2)nnc1-c1ccco1 |r,wD:16.17,(1.69,-3.6,;.6,-4.69,;-.88,-4.29,;-1.28,-2.8,;-2.77,-2.41,;-3.86,-3.49,;-3.46,-4.98,;-4.55,-6.07,;-6.04,-5.67,;-1.97,-5.38,;-1.57,-6.87,;-.11,-7.34,;1.22,-6.57,;2.56,-7.34,;3.89,-8.11,;1.79,-8.68,;3.33,-6.01,;2.56,-4.68,;4.87,-6.01,;5.64,-4.68,;7.18,-4.68,;7.95,-3.34,;7.18,-2.01,;7.95,-.68,;5.64,-2.01,;4.87,-3.34,;-.11,-8.88,;-1.57,-9.36,;-2.48,-8.11,;-3.97,-7.72,;-4.87,-6.47,;-6.34,-6.95,;-6.34,-8.49,;-4.87,-8.96,)|

Structure