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Assay Detail

CHEMBL790107

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

Functional
Inhibition constant of compound on R-(+)-125[I]-8 radioligand binding to rat striatal membranes
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Tissue Striatum
Subcellular Membrane
Confidence 1 — Organism
Curated By Intermediate

Target

Rattus norvegicus (CHEMBL376)
Type ORGANISM
Organism Rattus norvegicus

Publication

Synthesis and resolution of (+-)-7-chloro-8-hydroxy-1-(3'-iodophenyl)-3-methyl-2,3,4,5-tetrahydro- 1H-3- benzazepine (TISCH): a high affinity and selective iodinated ligand for CNS D1 dopamine receptor.
Chumpradit S, Kung MP, Billings JJ, Kung HF.
J Med Chem (1991) 34 : 877 -883
PubMed 1825848 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 7.81 9.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL62 SCH-23390 1 9.55
CHEMBL172352 1 8.97
CHEMBL1255588 1 8.28
CHEMBL25554 1 6.20
CHEMBL267930 SPIPERONE 2.0 1 6.07
CHEMBL39 SEROTONIN 3.0 1 -
CHEMBL59 DOPAMINE 4.0 1 -
CHEMBL80 NALOXONE 4.0 1 -
CHEMBL27 PROPRANOLOL 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL62 SCH-23390 Ki = 0.28 nM 9.55
CHEMBL172352 Ki = 1.07 nM 8.97
CHEMBL1255588 Ki = 5.26 nM 8.28
CHEMBL25554 Ki = 634.0 nM 6.20
CHEMBL267930 SPIPERONE Ki = 849.0 nM 6.07
CHEMBL39 SEROTONIN Ki > 5000.0 nM -
CHEMBL59 DOPAMINE Ki > 3000.0 nM -
CHEMBL80 NALOXONE Ki > 6000.0 nM -
CHEMBL27 PROPRANOLOL Ki > 5000.0 nM -