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Assay Detail

CHEMBL616070

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

Binding
Binding was determined on 5-hydroxytryptamine 1A receptor in rat hippocampal membranes
31
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Hippocampus
Confidence 8 — Homologous single protein target
Curated By Expert

Target

5-hydroxytryptamine receptor 1A (CHEMBL273)
Type SINGLE PROTEIN
Organism Rattus norvegicus

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 31 8.25 10.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2112779 2 10.70
CHEMBL2112780 2 10.59
CHEMBL2112778 2 10.55
CHEMBL2112771 2 10.34
CHEMBL423181 1 9.80
CHEMBL138109 1 9.72
CHEMBL2112773 2 9.70
CHEMBL2112776 2 9.66
CHEMBL140406 1 9.51
CHEMBL139505 1 9.42
CHEMBL444590 1 9.32
CHEMBL344432 1 9.27
CHEMBL136563 1 9.15
CHEMBL56 8-OH-DPAT 1 8.68
CHEMBL138892 1 8.15
CHEMBL138289 1 7.82
CHEMBL2112774 2 7.77
CHEMBL344146 1 7.64
CHEMBL49 BUSPIRONE 4.0 1 7.50
CHEMBL139146 1 7.41
CHEMBL138899 1 7.23
CHEMBL139848 1 6.59
CHEMBL140287 1 6.27
CHEMBL138900 1 6.17

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2112779 Ki = 0.02 nM 10.70
CHEMBL2112780 Ki = 0.026 nM 10.59
CHEMBL2112778 Ki = 0.028 nM 10.55
CHEMBL2112771 Ki = 0.046 nM 10.34
CHEMBL423181 Ki = 0.16 nM 9.80
CHEMBL138109 Ki = 0.19 nM 9.72
CHEMBL2112773 Ki = 0.2 nM 9.70
CHEMBL2112776 Ki = 0.22 nM 9.66
CHEMBL140406 Ki = 0.31 nM 9.51
CHEMBL139505 Ki = 0.38 nM 9.42
CHEMBL444590 Ki = 0.48 nM 9.32
CHEMBL344432 Ki = 0.54 nM 9.27
CHEMBL136563 Ki = 0.71 nM 9.15
CHEMBL56 8-OH-DPAT Ki = 2.1 nM 8.68
CHEMBL138892 Ki = 7.1 nM 8.15
CHEMBL138289 Ki = 15.0 nM 7.82
CHEMBL2112774 Ki = 17.0 nM 7.77
CHEMBL344146 Ki = 23.0 nM 7.64
CHEMBL49 BUSPIRONE Ki = 32.0 nM 7.50
CHEMBL139146 Ki = 39.0 nM 7.41
CHEMBL138899 Ki = 59.0 nM 7.23
CHEMBL2112776 Ki = 74.0 nM 7.13
CHEMBL2112779 Ki = 79.6 nM 7.10
CHEMBL2112771 Ki = 94.0 nM 7.03
CHEMBL2112780 Ki = 183.0 nM 6.74
CHEMBL139848 Ki = 257.0 nM 6.59
CHEMBL2112774 Ki = 373.0 nM 6.43
CHEMBL2112773 Ki = 480.0 nM 6.32
CHEMBL140287 Ki = 536.0 nM 6.27
CHEMBL138900 Ki = 676.0 nM 6.17
CHEMBL2112778 Ki = 815.0 nM 6.09