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Assay Detail

CHEMBL646572

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

Binding
In vitro binding affinity towards alpha-1 adrenergic receptor by using [3H]prazosin in rat brain cortex membranes.
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Brain
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Adrenergic receptor alpha-1 (CHEMBL1907610)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

A structure-affinity relationship study on derivatives of N-[2-[4-(4-Chlorophenyl)piperazin-1-yl]ethyl]-3-methoxybenzamide, a high-affinity and selective D(4) receptor ligand.
Perrone R, Berardi F, Colabufo NA, Leopoldo M, Tortorella V.
J Med Chem (2000) 43 : 270 -277
PubMed 10649982 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 6.39 6.84

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL92121 1 6.84
CHEMBL93403 1 6.61
CHEMBL329228 1 6.52
CHEMBL315879 1 6.39
CHEMBL94265 1 6.33
CHEMBL96799 1 6.20
CHEMBL96322 1 6.17
CHEMBL327245 1 6.04
CHEMBL328283 1 -
CHEMBL330470 1 -
CHEMBL318747 1 -
CHEMBL92411 1 -
CHEMBL321557 1 -
CHEMBL2112375 1 -
CHEMBL420067 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL92121 Ki = 146.0 nM 6.84
CHEMBL93403 Ki = 245.0 nM 6.61
CHEMBL329228 Ki = 303.0 nM 6.52
CHEMBL315879 Ki = 406.0 nM 6.39
CHEMBL94265 Ki = 470.0 nM 6.33
CHEMBL96799 Ki = 631.0 nM 6.20
CHEMBL96322 Ki = 678.0 nM 6.17
CHEMBL327245 Ki = 908.0 nM 6.04
CHEMBL328283 Ki > 850.0 nM -
CHEMBL330470 Ki > 850.0 nM -
CHEMBL318747 Ki > 850.0 nM -
CHEMBL92411 Ki > 850.0 nM -
CHEMBL321557 Ki > 850.0 nM -
CHEMBL2112375 Ki > 850.0 nM -
CHEMBL420067 Ki > 850.0 nM -