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Assay Detail

CHEMBL647613

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

Binding
Binding affinity towards rat Alpha-1 adrenergic receptor was evaluated using [3H]- prazosin as radioligand
20
Total Activities
20
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

Structure-activity relationship studies on the 5-HT(1A) receptor affinity of 1-phenyl-4-[omega-(alpha- or beta-tetralinyl)alkyl]piperazines. 4.
Perrone R, Berardi F, Colabufo NA, Leopoldo M, Tortorella V, Fornaretto MG, Caccia C, McArthur RA.
J Med Chem (1996) 39 : 4928 -4934
PubMed 8960552 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 7.21 8.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2 PRAZOSIN 4.0 1 8.85
CHEMBL26929 1 8.19
CHEMBL322275 1 7.37
CHEMBL147678 1 7.35
CHEMBL148055 1 7.31
CHEMBL342518 1 7.24
CHEMBL444590 1 7.18
CHEMBL144445 1 7.10
CHEMBL143728 1 7.10
CHEMBL144417 1 7.08
CHEMBL357176 1 7.06
CHEMBL343432 1 7.00
CHEMBL147440 1 6.92
CHEMBL341893 1 6.89
CHEMBL145432 1 6.89
CHEMBL143110 1 6.76
CHEMBL172601 1 6.74
CHEMBL147387 1 6.71
CHEMBL49 BUSPIRONE 4.0 1 -
CHEMBL56 8-OH-DPAT 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2 PRAZOSIN IC50 = 1.4 nM 8.85
CHEMBL26929 IC50 = 6.5 nM 8.19
CHEMBL322275 IC50 = 43.0 nM 7.37
CHEMBL147678 IC50 = 45.0 nM 7.35
CHEMBL148055 IC50 = 49.0 nM 7.31
CHEMBL342518 IC50 = 58.0 nM 7.24
CHEMBL444590 IC50 = 66.0 nM 7.18
CHEMBL144445 IC50 = 80.0 nM 7.10
CHEMBL143728 IC50 = 79.0 nM 7.10
CHEMBL144417 IC50 = 84.0 nM 7.08
CHEMBL357176 IC50 = 88.0 nM 7.06
CHEMBL343432 IC50 = 100.0 nM 7.00
CHEMBL147440 IC50 = 120.0 nM 6.92
CHEMBL341893 IC50 = 130.0 nM 6.89
CHEMBL145432 IC50 = 130.0 nM 6.89
CHEMBL143110 IC50 = 173.0 nM 6.76
CHEMBL172601 IC50 = 184.0 nM 6.74
CHEMBL147387 IC50 = 194.0 nM 6.71
CHEMBL49 BUSPIRONE IC50 > 10000.0 nM -
CHEMBL56 8-OH-DPAT IC50 > 10000.0 nM -