Ki Summary

Reaction Details

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Target

Apelin receptor

Ligand

BDBM456603

Substrate/Competitor

n/a

Meas. Tech.

GTPγS Binding

EC50

11.0±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

BDBM456603

n/a

Name

BDBM456603

Synonyms:

US10736883, Example 40.0

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:18.19,16.17,(-7.96,-5.02,;-6.47,-5.42,;-5.38,-4.33,;-5.78,-2.84,;-4.69,-1.75,;-3.2,-2.15,;-2.81,-3.64,;-1.32,-4.04,;-.23,-2.95,;-3.89,-4.73,;-3.26,-6.46,;-1.82,-7.01,;-.48,-6.24,;.85,-7.01,;1.62,-5.67,;.08,-8.34,;2.18,-7.78,;2.18,-9.32,;3.52,-7.01,;3.52,-5.47,;4.85,-7.78,;4.85,-9.32,;6.18,-10.09,;7.57,-9.34,;7.52,-7.78,;6.18,-7.01,;8.9,-10.11,;10.23,-10.88,;-1.9,-8.55,;-3.39,-8.94,;-4.22,-7.65,;-5.71,-7.25,;-6.55,-5.96,;-8.04,-6.36,;-8.12,-7.9,;-9.45,-8.67,;-6.68,-8.45,)|

Structure