Ki Summary

Reaction Details

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Target

Apelin receptor

Ligand

BDBM456581

Substrate/Competitor

n/a

Meas. Tech.

GTPγS Binding

EC50

0.280±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

BDBM456581

n/a

Name

BDBM456581

Synonyms:

US10736883, Example 18.0

Type

Small organic molecule

Emp. Form.

C22H21BrClN5O5S

Mol. Mass.

582.855

SMILES

COc1cccc(OC)c1-n1c(NS(=O)(=O)[C@H](C)Cc2ncc(Cl)cc2Br)nnc1-c1ccco1 |r,wD:16.17,(-6.96,-2.72,;-5.63,-3.49,;-4.3,-2.72,;-4.3,-1.18,;-2.96,-.41,;-1.63,-1.18,;-1.63,-2.72,;-.3,-3.49,;1.04,-2.72,;-2.96,-3.49,;-2.96,-5.17,;-1.72,-6.08,;-.38,-5.31,;.95,-6.08,;.18,-7.41,;1.72,-7.41,;2.28,-5.31,;2.28,-3.77,;3.62,-6.08,;4.95,-5.31,;4.95,-3.77,;6.28,-3,;7.62,-3.77,;8.95,-3,;7.62,-5.31,;6.28,-6.08,;6.28,-7.62,;-2.19,-7.54,;-3.73,-7.54,;-4.21,-6.08,;-5.58,-5.49,;-6.06,-4.03,;-7.6,-4.03,;-8.07,-5.49,;-6.83,-6.4,)|

Structure