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Assay Detail

CHEMBL649152

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Binding
Binding affinity was determined on human cloned alpha-1B adrenergic receptor
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Alpha-1B adrenergic receptor (CHEMBL232)
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 8 7.12 8.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL139505 1 8.38
CHEMBL444590 1 8.10
CHEMBL344432 1 7.58
CHEMBL2112779 1 7.36
CHEMBL2112778 1 7.28
CHEMBL138109 1 6.57
CHEMBL2112774 1 6.48
CHEMBL56 8-OH-DPAT 1 5.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL139505 Ki = 4.21 nM 8.38
CHEMBL444590 Ki = 7.88 nM 8.10
CHEMBL344432 Ki = 26.4 nM 7.58
CHEMBL2112779 Ki = 43.3 nM 7.36
CHEMBL2112778 Ki = 53.1 nM 7.28
CHEMBL138109 Ki = 270.0 nM 6.57
CHEMBL2112774 Ki = 332.0 nM 6.48
CHEMBL56 8-OH-DPAT Ki = 5975.0 nM 5.22