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Assay Detail

CHEMBL644954

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

Binding
In vitro binding affinity at Alpha-1 adrenergic receptor in rat cortical tissues
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

New pyridobenzodiazepine derivatives: modifications of the basic side chain differentially modulate binding to dopamine (D(4.2), D(2L)) and serotonin (5-HT(2A)) receptors.
Liégeois JF, Eyrolles L, Ellenbroek BA, Lejeune C, Carato P, Bruhwyler J, Géczy J, Damas J, Delarge J.
J Med Chem (2002) 45 : 5136 -5149
PubMed 12408724 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 23 7.17 7.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL54 HALOPERIDOL 4.0 1 7.89
CHEMBL42 CLOZAPINE 4.0 1 7.85
CHEMBL347959 1 7.75
CHEMBL357391 1 7.20
CHEMBL63576 1 7.10
CHEMBL358657 1 7.00
CHEMBL63329 1 6.97
CHEMBL342536 1 6.79
CHEMBL422310 1 6.76
CHEMBL436274 1 6.43
CHEMBL423760 1 -
CHEMBL146856 1 -
CHEMBL148042 1 -
CHEMBL148965 1 -
CHEMBL149949 1 -
CHEMBL357320 1 -
CHEMBL347292 1 -
CHEMBL345964 1 -
CHEMBL148836 1 -
CHEMBL424314 1 -
CHEMBL147473 1 -
CHEMBL149493 1 -
CHEMBL148952 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL54 HALOPERIDOL Ki = 13.0 nM 7.89
CHEMBL42 CLOZAPINE Ki = 14.0 nM 7.85
CHEMBL347959 Ki = 18.0 nM 7.75
CHEMBL357391 Ki = 63.0 nM 7.20
CHEMBL63576 Ki = 79.0 nM 7.10
CHEMBL358657 Ki = 100.0 nM 7.00
CHEMBL63329 Ki = 108.0 nM 6.97
CHEMBL342536 Ki = 163.0 nM 6.79
CHEMBL422310 Ki = 172.0 nM 6.76
CHEMBL436274 Ki = 367.0 nM 6.43
CHEMBL423760 Ki > 1000.0 nM -
CHEMBL146856 Ki > 1000.0 nM -
CHEMBL148042 Ki > 1000.0 nM -
CHEMBL148965 Ki > 1000.0 nM -
CHEMBL149949 Ki > 1000.0 nM -
CHEMBL357320 Ki > 1000.0 nM -
CHEMBL347292 Ki > 1000.0 nM -
CHEMBL345964 Ki > 1000.0 nM -
CHEMBL148836 Ki > 1000.0 nM -
CHEMBL424314 Ki > 1000.0 nM -
CHEMBL147473 Ki > 1000.0 nM -
CHEMBL149493 Ki > 1000.0 nM -
CHEMBL148952 Ki > 1000.0 nM -