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Assay Detail

CHEMBL867413

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

Binding
Displacement of [3H]clonidine from Sprague-Dawley rat cortex adrenergic alpha 2 receptor
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Adrenergic receptor alpha-2 (CHEMBL2093864)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Comparison of the binding of 3-fluoromethyl-7-sulfonyl-1,2,3,4-tetrahydroisoquinolines with their isosteric sulfonamides to the active site of phenylethanolamine N-methyltransferase.
Grunewald GL, Seim MR, Regier RC, Martin JL, Gee CL, Drinkwater N, Criscione KR.
J Med Chem (2006) 49 : 5424 -5433
PubMed 16942016 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 27 5.08 7.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL287837 1 7.68
CHEMBL14346 1,2,3,4-TETRAHYDROISOQUINOLINE 1 6.46
CHEMBL28431 1 4.68
CHEMBL27599 1 4.47
CHEMBL176112 1 4.28
CHEMBL280592 1 4.02
CHEMBL26717 1 4.00
CHEMBL41647 1 -
CHEMBL290890 1 -
CHEMBL184931 1 -
CHEMBL435536 1 -
CHEMBL177861 1 -
CHEMBL120975 1 -
CHEMBL177621 1 -
CHEMBL366785 1 -
CHEMBL178695 1 -
CHEMBL95873 1 -
CHEMBL213339 1 -
CHEMBL214064 1 -
CHEMBL213579 1 -
CHEMBL212790 1 -
CHEMBL215871 1 -
CHEMBL212026 1 -
CHEMBL213031 1 -
CHEMBL333578 1 -
CHEMBL27664 1 -
CHEMBL439320 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL287837 Ki = 21.0 nM 7.68
CHEMBL14346 1,2,3,4-TETRAHYDROISOQUINOLINE Ki = 350.0 nM 6.46
CHEMBL28431 Ki = 21000.0 nM 4.68
CHEMBL27599 Ki = 34000.0 nM 4.47
CHEMBL176112 Ki = 53000.0 nM 4.28
CHEMBL280592 Ki = 95000.0 nM 4.02
CHEMBL26717 Ki = 100000.0 nM 4.00
CHEMBL41647 Ki = 1400000.0 nM -
CHEMBL290890 Ki = 140000.0 nM -
CHEMBL184931 Ki = 430000.0 nM -
CHEMBL435536 Ki = 610000.0 nM -
CHEMBL177861 Ki = 550000.0 nM -
CHEMBL120975 Ki = 310000.0 nM -
CHEMBL177621 Ki = 660000.0 nM -
CHEMBL366785 Ki = 340000.0 nM -
CHEMBL178695 Ki = 1200000.0 nM -
CHEMBL95873 Ki = 680000.0 nM -
CHEMBL213339 Ki > 1000000.0 nM -
CHEMBL214064 Ki > 1000000.0 nM -
CHEMBL213579 Ki = 1100000.0 nM -
CHEMBL212790 Ki = 690000.0 nM -
CHEMBL215871 Ki = 540000.0 nM -
CHEMBL212026 Ki = 1200000.0 nM -
CHEMBL213031 Ki = 740000.0 nM -
CHEMBL333578 Ki = 230000.0 nM -
CHEMBL27664 Ki = 160000.0 nM -
CHEMBL439320 Ki > 1000000.0 nM -