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Assay Detail

CHEMBL870200

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

Binding
Binding affinity to D2 receptor by radioligand binding assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

D(2) dopamine receptor (CHEMBL217)
Type SINGLE PROTEIN
Organism Homo sapiens

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 6 7.36 7.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL49 BUSPIRONE 4.0 1 7.89
CHEMBL284092 GEPIRONE 4.0 1 7.24
CHEMBL8412 IPSAPIRONE 2.0 1 6.96
CHEMBL209821 NALUZOTAN 3.0 1 -
CHEMBL379984 1 -
CHEMBL411941 CYCLORGDFV 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL49 BUSPIRONE Ki = 13.0 nM 7.89
CHEMBL284092 GEPIRONE Ki = 58.0 nM 7.24
CHEMBL8412 IPSAPIRONE Ki = 110.0 nM 6.96
CHEMBL209821 NALUZOTAN Ki > 2000.0 nM -
CHEMBL379984 Ki > 5000.0 nM -
CHEMBL411941 CYCLORGDFV Ki - -