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Assay Detail

CHEMBL643613

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

Binding
Binding affinity for rat cortex alpha-1 adrenergic receptor by inhibition of [3H]prazosin binding
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Expert

Target

Alpha-1A adrenergic receptor (CHEMBL319)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis and pharmacological evaluation of potent and highly selective D3 receptor ligands: inhibition of cocaine-seeking behavior and the role of dopamine D3/D2 receptors.
Campiani G, Butini S, Trotta F, Fattorusso C, Catalanotti B, Aiello F, Gemma S, Nacci V, Novellino E, Stark JA, Cagnotto A, Fumagalli E, Carnovali F, Cervo L, Mennini T.
J Med Chem (2003) 46 : 3822 -3839
PubMed 12930145 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 6.69 8.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL127400 1 8.24
CHEMBL420510 1 7.48
CHEMBL124444 1 7.44
CHEMBL25236 BP-897 1 7.22
CHEMBL339960 1 6.26
CHEMBL340641 1 6.20
CHEMBL125916 1 6.18
CHEMBL435218 1 6.11
CHEMBL126889 1 5.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL127400 Ki = 5.8 nM 8.24
CHEMBL420510 Ki = 33.0 nM 7.48
CHEMBL124444 Ki = 36.0 nM 7.44
CHEMBL25236 BP-897 Ki = 60.0 nM 7.22
CHEMBL339960 Ki = 547.0 nM 6.26
CHEMBL340641 Ki = 629.0 nM 6.20
CHEMBL125916 Ki = 666.0 nM 6.18
CHEMBL435218 Ki = 779.0 nM 6.11
CHEMBL126889 Ki = 8100.0 nM 5.09