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Assay Detail

CHEMBL615766

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

Binding
Binding affinity on human cloned 5-hydroxytryptamine 1A receptor transfected in human cell lines(He La)
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

5-hydroxytryptamine receptor 1A (CHEMBL214)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

trans-4-[4-(Methoxyphenyl)cyclohexyl]-1-arylpiperazines: a new class of potent and selective 5-HT(1A) receptor ligands as conformationally constrained analogues of 4-[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl]-1-arylpiperazines.
Perrone R, Berardi F, Colabufo NA, Leopoldo M, Lacivita E, Tortorella V, Leonardi A, Poggesi E, Testa R.
J Med Chem (2001) 44 : 4431 -4442
PubMed 11728188 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 9.07 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2112778 1 9.70
CHEMBL2112779 1 9.68
CHEMBL344432 1 9.64
CHEMBL138109 1 9.07
CHEMBL139505 1 8.52
CHEMBL56 8-OH-DPAT 1 8.46
CHEMBL2112774 1 8.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2112778 Ki = 0.2 nM 9.70
CHEMBL2112779 Ki = 0.21 nM 9.68
CHEMBL344432 Ki = 0.23 nM 9.64
CHEMBL138109 Ki = 0.86 nM 9.07
CHEMBL139505 Ki = 3.0 nM 8.52
CHEMBL56 8-OH-DPAT Ki = 3.44 nM 8.46
CHEMBL2112774 Ki = 3.77 nM 8.42