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Assay Detail

CHEMBL2166090

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

Binding
Displacement of [3H]LSD from rat kidney proximal convoluted tubule 5HT7R expressed in COS7 cells
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type COS-7
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

5-hydroxytryptamine receptor 7 (CHEMBL3223)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Investigations on the 1-(2-biphenyl)piperazine motif: identification of new potent and selective ligands for the serotonin(7) (5-HT(7)) receptor with agonist or antagonist action in vitro or ex vivo.
Lacivita E, Patarnello D, Stroth N, Caroli A, Niso M, Contino M, De Giorgio P, Di Pilato P, Colabufo NA, Berardi F, Perrone R, Svenningsson P, Hedlund PB, Leopoldo M.
J Med Chem (2012) 55 : 6375 -6380
PubMed 22738316 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 6.71 7.08

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL277120 1 7.08
CHEMBL9666 1 6.61
CHEMBL478 CHLOROPHENYLPIPERAZINE 2.0 1 6.45

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL277120 Ki = 83.0 nM 7.08
CHEMBL9666 Ki = 243.0 nM 6.61
CHEMBL478 CHLOROPHENYLPIPERAZINE Ki = 352.0 nM 6.45