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Assay Detail

CHEMBL4775347

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Displacement of [125I] [NIe75, Tyr77]Pyr-apelin-13 from YFP-tagged human APJ receptor expressed in HEK293 cell membranes incubated for 1 hr by gamma counting based Cheng-Prusoff equation analysis
71
Total Activities
71
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Apelin receptor (CHEMBL1628481)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-Activity Relationship and Bioactivity of Short Analogues of ELABELA as Agonists of the Apelin Receptor.
Trân K,Murza A,Sainsily X,Delile E,Couvineau P,Côté J,Coquerel D,Peloquin M,Auger-Messier M,Bouvier M,Lesur O,Sarret P,Marsault É
J Med Chem (2021) 64 : 602 -615
PubMed 33350824 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 71 7.43 9.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4796315 1 9.72
CHEMBL3184840 1 9.15
CHEMBL4780368 1 9.03
CHEMBL4791583 1 8.96
CHEMBL4797921 1 8.62
CHEMBL4781348 1 8.41
CHEMBL4794333 1 8.40
CHEMBL4790636 1 8.40
CHEMBL4777690 1 8.40
CHEMBL4788436 1 8.34
CHEMBL4797169 1 8.29
CHEMBL4791398 1 8.05
CHEMBL4791473 1 8.03
CHEMBL4793361 1 7.89
CHEMBL4779171 1 7.80
CHEMBL4787249 1 7.80
CHEMBL4785339 1 7.80
CHEMBL4795334 1 7.75
CHEMBL4795339 1 7.72
CHEMBL4780010 1 7.72
CHEMBL4788480 1 7.70
CHEMBL4789289 1 7.68
CHEMBL4778604 1 7.68
CHEMBL4792840 1 7.60
CHEMBL4795922 1 7.54
CHEMBL4784932 1 7.42
CHEMBL4776332 1 7.35
CHEMBL4779853 1 7.32
CHEMBL4797849 1 7.27
CHEMBL4782415 1 7.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4796315 Ki = 0.19 nM 9.72
CHEMBL3184840 Ki = 0.7 nM 9.15
CHEMBL4780368 Ki = 0.93 nM 9.03
CHEMBL4791583 Ki = 1.1 nM 8.96
CHEMBL4797921 Ki = 2.4 nM 8.62
CHEMBL4781348 Ki = 3.9 nM 8.41
CHEMBL4794333 Ki = 4.0 nM 8.40
CHEMBL4790636 Ki = 4.0 nM 8.40
CHEMBL4777690 Ki = 4.0 nM 8.40
CHEMBL4788436 Ki = 4.6 nM 8.34
CHEMBL4797169 Ki = 5.1 nM 8.29
CHEMBL4791398 Ki = 8.9 nM 8.05
CHEMBL4791473 Ki = 9.3 nM 8.03
CHEMBL4793361 Ki = 13.0 nM 7.89
CHEMBL4785339 Ki = 16.0 nM 7.80
CHEMBL4787249 Ki = 16.0 nM 7.80
CHEMBL4779171 Ki = 16.0 nM 7.80
CHEMBL4795334 Ki = 18.0 nM 7.75
CHEMBL4795339 Ki = 19.0 nM 7.72
CHEMBL4780010 Ki = 19.0 nM 7.72
CHEMBL4788480 Ki = 20.0 nM 7.70
CHEMBL4789289 Ki = 21.0 nM 7.68
CHEMBL4778604 Ki = 21.0 nM 7.68
CHEMBL4792840 Ki = 25.0 nM 7.60
CHEMBL4795922 Ki = 29.0 nM 7.54
CHEMBL4784932 Ki = 38.0 nM 7.42
CHEMBL4776332 Ki = 45.0 nM 7.35
CHEMBL4779853 Ki = 48.0 nM 7.32
CHEMBL4797849 Ki = 54.0 nM 7.27
CHEMBL4782415 Ki = 57.0 nM 7.24
CHEMBL4799819 Ki = 62.0 nM 7.21
CHEMBL4785901 Ki = 69.0 nM 7.16
CHEMBL4798898 Ki = 71.0 nM 7.15
CHEMBL4798345 Ki = 72.0 nM 7.14
CHEMBL4792261 Ki = 73.0 nM 7.14
CHEMBL4786248 Ki = 76.0 nM 7.12
CHEMBL4776966 Ki = 92.0 nM 7.04
CHEMBL4787473 Ki = 94.0 nM 7.03
CHEMBL4792342 Ki = 120.0 nM 6.92
CHEMBL4780831 Ki = 128.0 nM 6.89
CHEMBL4789073 Ki = 152.0 nM 6.82
CHEMBL4785505 Ki = 159.0 nM 6.80
CHEMBL4781727 Ki = 174.0 nM 6.76
CHEMBL4799725 Ki = 186.0 nM 6.73
CHEMBL4787012 Ki = 212.0 nM 6.67
CHEMBL4791432 Ki = 228.0 nM 6.64
CHEMBL4791619 Ki = 278.0 nM 6.56
CHEMBL4795676 Ki = 419.0 nM 6.38
CHEMBL4784523 Ki = 438.0 nM 6.36
CHEMBL4777893 Ki = 463.0 nM 6.33