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Assay Detail

CHEMBL643957

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

Binding
Binding affinity at Alpha-2 adrenergic receptor in calf cerebral cortex homogenates by [3H]clonidine displacement.
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Cerebral cortex
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Alpha-2A adrenergic receptor (CHEMBL4744)
Type SINGLE PROTEIN
Organism Bos taurus

Publication

Synthesis and hypoglycemic activity of substituted 8-(1-piperazinyl)imidazo[1,2-a]pyrazines.
Meurer LC, Tolman RL, Chapin EW, Saperstein R, Vicario PP, Zrada MM, MacCoss M.
J Med Chem (1992) 35 : 3845 -3857
PubMed 1359141 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 19 6.46 7.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL331036 1 7.82
CHEMBL544354 1 7.29
CHEMBL330994 1 7.09
CHEMBL541088 1 6.85
CHEMBL123566 1 6.74
CHEMBL545289 1 6.72
CHEMBL555637 1 6.62
CHEMBL538788 1 6.62
CHEMBL338704 1 6.57
CHEMBL543653 1 6.47
CHEMBL555391 1 6.43
CHEMBL545293 1 6.32
CHEMBL538537 1 6.28
CHEMBL554785 1 6.21
CHEMBL340358 1 6.06
CHEMBL127303 1 5.99
CHEMBL127318 1 5.87
CHEMBL126394 1 5.80
CHEMBL124926 1 4.93

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL331036 Ki = 15.0 nM 7.82
CHEMBL544354 Ki = 51.0 nM 7.29
CHEMBL330994 Ki = 81.0 nM 7.09
CHEMBL541088 Ki = 140.0 nM 6.85
CHEMBL123566 Ki = 182.0 nM 6.74
CHEMBL545289 Ki = 190.0 nM 6.72
CHEMBL555637 Ki = 240.0 nM 6.62
CHEMBL538788 Ki = 240.0 nM 6.62
CHEMBL338704 Ki = 270.0 nM 6.57
CHEMBL543653 Ki = 340.0 nM 6.47
CHEMBL555391 Ki = 370.0 nM 6.43
CHEMBL545293 Ki = 480.0 nM 6.32
CHEMBL538537 Ki = 530.0 nM 6.28
CHEMBL554785 Ki = 620.0 nM 6.21
CHEMBL340358 Ki = 870.0 nM 6.06
CHEMBL127303 Ki = 1020.0 nM 5.99
CHEMBL127318 Ki = 1350.0 nM 5.87
CHEMBL126394 Ki = 1600.0 nM 5.80
CHEMBL124926 Ki = 11860.0 nM 4.93