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Assay Detail

CHEMBL870198

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 cortex cells
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Cerebral cortex
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

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

Publication

An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression.
Becker OM, Dhanoa DS, Marantz Y, Chen D, Shacham S, Cheruku S, Heifetz A, Mohanty P, Fichman M, Sharadendu A, Nudelman R, Kauffman M, Noiman S.
J Med Chem (2006) 49 : 3116 -3135
PubMed 16722631 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 6.70 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL209324 1 8.22
CHEMBL2111058 SUNEPITRON 2.0 1 7.46
CHEMBL8412 IPSAPIRONE 2.0 1 6.64
CHEMBL49 BUSPIRONE 4.0 1 6.43
CHEMBL209821 NALUZOTAN 3.0 1 5.80
CHEMBL284092 GEPIRONE 4.0 1 5.62
CHEMBL210537 1 -
CHEMBL379984 1 -
CHEMBL411941 CYCLORGDFV 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL209324 Ki = 6.0 nM 8.22
CHEMBL2111058 SUNEPITRON Ki = 35.0 nM 7.46
CHEMBL8412 IPSAPIRONE Ki = 229.0 nM 6.64
CHEMBL49 BUSPIRONE Ki = 367.0 nM 6.43
CHEMBL209821 NALUZOTAN Ki = 1600.0 nM 5.80
CHEMBL284092 GEPIRONE Ki = 2400.0 nM 5.62
CHEMBL210537 Ki > 3500.0 nM -
CHEMBL379984 Ki > 5000.0 nM -
CHEMBL411941 CYCLORGDFV Ki - -