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Assay Detail

CHEMBL2026138

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

Binding
Displacement of [3H]-prazosin from adrenergic alpha-1 receptor in rat cerebral cortical membranes
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Subcellular Membrane
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

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

Publication

Discovery of cariprazine (RGH-188): a novel antipsychotic acting on dopamine D3/D2 receptors.
Agai-Csongor E, Domány G, Nógrádi K, Galambos J, Vágó I, Keserű GM, Greiner I, Laszlovszky I, Gere A, Schmidt E, Kiss B, Vastag M, Tihanyi K, Sághy K, Laszy J, Gyertyán I, Zájer-Balázs M, Gémesi L, Kapás M, Szombathelyi Z.
Bioorg Med Chem Lett (2012) 22 : 3437 -3440
PubMed 22537450 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 6.98 7.53

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2024676 1 7.53
CHEMBL2024675 1 7.46
CHEMBL2024522 1 7.34
CHEMBL2024523 1 7.14
CHEMBL2024524 1 6.97
CHEMBL2024525 1 6.81
CHEMBL2024521 1 6.69
CHEMBL2024517 CARIPRAZINE HYDROCHLORIDE 4.0 1 6.67
CHEMBL2024677 1 6.18

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2024676 Ki = 29.6 nM 7.53
CHEMBL2024675 Ki = 34.9 nM 7.46
CHEMBL2024522 Ki = 45.9 nM 7.34
CHEMBL2024523 Ki = 72.9 nM 7.14
CHEMBL2024524 Ki = 106.4 nM 6.97
CHEMBL2024525 Ki = 156.0 nM 6.81
CHEMBL2024521 Ki = 204.0 nM 6.69
CHEMBL2024517 CARIPRAZINE HYDROCHLORIDE Ki = 214.0 nM 6.67
CHEMBL2024677 Ki = 667.0 nM 6.18