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Assay Detail

CHEMBL645519

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

Binding
Binding affinity towards rat Alpha-2 adrenergic receptor was evaluated using [3H]- yohimbine as radioligand
17
Total Activities
17
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-2 (CHEMBL2093864)
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 17 6.82 7.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL26929 1 7.77
CHEMBL144417 1 7.66
CHEMBL15245 YOHIMBINE 3.0 1 7.52
CHEMBL444590 1 7.32
CHEMBL342518 1 6.91
CHEMBL357176 1 6.89
CHEMBL145432 1 6.85
CHEMBL143728 1 6.80
CHEMBL147678 1 6.77
CHEMBL322275 1 6.58
CHEMBL144445 1 6.58
CHEMBL147440 1 6.54
CHEMBL147387 1 6.45
CHEMBL343432 1 6.22
CHEMBL341893 1 6.11
CHEMBL56 8-OH-DPAT 1 6.09
CHEMBL49 BUSPIRONE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL26929 IC50 = 17.0 nM 7.77
CHEMBL144417 IC50 = 22.0 nM 7.66
CHEMBL15245 YOHIMBINE IC50 = 30.0 nM 7.52
CHEMBL444590 IC50 = 48.0 nM 7.32
CHEMBL342518 IC50 = 122.0 nM 6.91
CHEMBL357176 IC50 = 130.0 nM 6.89
CHEMBL145432 IC50 = 140.0 nM 6.85
CHEMBL143728 IC50 = 160.0 nM 6.80
CHEMBL147678 IC50 = 170.0 nM 6.77
CHEMBL322275 IC50 = 260.0 nM 6.58
CHEMBL144445 IC50 = 260.0 nM 6.58
CHEMBL147440 IC50 = 290.0 nM 6.54
CHEMBL147387 IC50 = 357.0 nM 6.45
CHEMBL343432 IC50 = 600.0 nM 6.22
CHEMBL341893 IC50 = 770.0 nM 6.11
CHEMBL56 8-OH-DPAT IC50 = 810.0 nM 6.09
CHEMBL49 BUSPIRONE IC50 > 10000.0 nM -