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Assay Detail

CHEMBL4678991

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

Binding
Displacement of [125I]Sar-Ile-angiotensin 2 from human AT2 receptor expressed in HEK293 cells incubated for 240 mins by radiometric scintillation analysis
12
Total Activities
12
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

Type-2 angiotensin II receptor (CHEMBL4607)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

N-(Methyloxycarbonyl)thiophene sulfonamides as high affinity AT2 receptor ligands.
Wannberg J,Gising J,Lindman J,Salander J,Gutiérrez-de-Terán H,Ablahad H,Hamid S,Grönbladh A,Spizzo I,Gaspari TA,Widdop RE,Hallberg A,Backlund M,Leśniak A,Hallberg M,Larhed M
Bioorg Med Chem (2021) 29 : 115859 -115859
PubMed 33309749 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 7.38 8.18

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4779819 1 8.18
CHEMBL4779945 1 8.12
CHEMBL4788892 1 8.03
CHEMBL4759641 1 7.77
CHEMBL4751226 1 7.58
CHEMBL4784233 1 7.41
CHEMBL2086911 1 7.32
CHEMBL4747530 1 7.28
CHEMBL4762752 1 6.96
CHEMBL4797684 1 6.77
CHEMBL2086892 1 6.57
CHEMBL2086910 1 6.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4779819 Ki = 6.6 nM 8.18
CHEMBL4779945 Ki = 7.6 nM 8.12
CHEMBL4788892 Ki = 9.3 nM 8.03
CHEMBL4759641 Ki = 17.0 nM 7.77
CHEMBL4751226 Ki = 26.0 nM 7.58
CHEMBL4784233 Ki = 39.0 nM 7.41
CHEMBL2086911 Ki = 48.0 nM 7.32
CHEMBL4747530 Ki = 53.0 nM 7.28
CHEMBL4762752 Ki = 110.0 nM 6.96
CHEMBL4797684 Ki = 170.0 nM 6.77
CHEMBL2086892 Ki = 270.0 nM 6.57
CHEMBL2086910 Ki = 280.0 nM 6.55