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Assay Detail

CHEMBL647207

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Binding
Compound was tested in vitro for its affinity towards rat Alpha-2 adrenergic receptor
25
Total Activities
25
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

Synthesis and biochemical evaluation of 3-fluoromethyl-1,2,3, 4-tetrahydroisoquinolines as selective inhibitors of phenylethanolamine N-methyltransferase versus the alpha(2)-adrenoceptor.
Grunewald GL, Caldwell TM, Li Q, Slavica M, Criscione KR, Borchardt RT, Wang W.
J Med Chem (1999) 42 : 3588 -3601
PubMed 10479290 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 25 5.22 7.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL287837 1 7.68
CHEMBL59994 1 6.17
CHEMBL60434 1 6.12
CHEMBL294562 1 5.55
CHEMBL121531 1 5.42
CHEMBL38681 1 5.35
CHEMBL39928 1 5.19
CHEMBL60068 1 5.18
CHEMBL275595 1 5.15
CHEMBL6409 CGS-19281A 1 4.92
CHEMBL121570 1 4.66
CHEMBL121252 1 4.39
CHEMBL287360 1 4.33
CHEMBL97282 1 4.12
CHEMBL26717 1 4.00
CHEMBL290890 1 -
CHEMBL43021 1 -
CHEMBL40081 1 -
CHEMBL41647 1 -
CHEMBL36909 1 -
CHEMBL333578 1 -
CHEMBL112964 1 -
CHEMBL95873 1 -
CHEMBL120975 1 -
CHEMBL112357 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL287837 Ki = 21.0 nM 7.68
CHEMBL59994 Ki = 670.0 nM 6.17
CHEMBL60434 Ki = 760.0 nM 6.12
CHEMBL294562 Ki = 2800.0 nM 5.55
CHEMBL121531 Ki = 3800.0 nM 5.42
CHEMBL38681 Ki = 4500.0 nM 5.35
CHEMBL39928 Ki = 6400.0 nM 5.19
CHEMBL60068 Ki = 6600.0 nM 5.18
CHEMBL275595 Ki = 7100.0 nM 5.15
CHEMBL6409 CGS-19281A Ki = 12000.0 nM 4.92
CHEMBL121570 Ki = 22000.0 nM 4.66
CHEMBL121252 Ki = 41000.0 nM 4.39
CHEMBL287360 Ki = 47000.0 nM 4.33
CHEMBL97282 Ki = 76000.0 nM 4.12
CHEMBL26717 Ki = 100000.0 nM 4.00
CHEMBL290890 Ki = 160000.0 nM -
CHEMBL43021 Ki = 660000.0 nM -
CHEMBL40081 Ki = 460000.0 nM -
CHEMBL41647 Ki = 1400000.0 nM -
CHEMBL36909 Ki = 110000.0 nM -
CHEMBL333578 Ki = 230000.0 nM -
CHEMBL112964 Ki > 1000000.0 nM -
CHEMBL95873 Ki = 680000.0 nM -
CHEMBL120975 Ki = 310000.0 nM -
CHEMBL112357 Ki = 3900000.0 nM -