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Assay Detail

CHEMBL641150

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Binding
Binding affinity to alpha-2 adrenergic receptor determined by measurement of [3H]yohimbine displacement from rat cortical membrane
ChEMBL ↗
62
Total Activities
62
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-affinity relationships of 12-sulfonyl derivatives of 5,8,8a,9,10,11,12,12a,13,13a-decahydro-6H-isoquino[2,1-g][1 ,6] naphthyridines at alpha-adrenoceptors.
Clark RD, Repke DB, Berger J, Nelson JT, Kilpatrick AT, Brown CM, MacKinnon AC, Clague RU, Spedding M.
J Med Chem (1991) 34 : 705 -717
PubMed 1671705 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 62 8.00 9.45

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL279807 — — 1 9.45
CHEMBL349665 — — 1 9.34
CHEMBL349747 — — 1 9.22
CHEMBL348793 — — 1 9.19
CHEMBL163911 DELEQUAMINE 2.0 1 9.18
CHEMBL162971 — — 1 9.18
CHEMBL349004 — — 1 9.15
CHEMBL164420 — — 1 8.97
CHEMBL163570 — — 1 8.95
CHEMBL411954 — — 1 8.90
CHEMBL161278 — — 1 8.83
CHEMBL348831 — — 1 8.82
CHEMBL162965 — — 1 8.82
CHEMBL163290 — — 1 8.82
CHEMBL159919 — — 1 8.81
CHEMBL348726 — — 1 8.80
CHEMBL162841 — — 1 8.77
CHEMBL350388 — — 1 8.77
CHEMBL352278 — — 1 8.77
CHEMBL262446 — — 1 8.74
CHEMBL355140 — — 1 8.73
CHEMBL350168 — — 1 8.69
CHEMBL162024 — — 1 8.66
CHEMBL350393 — — 1 8.66
CHEMBL162109 — — 1 8.65
CHEMBL349777 — — 1 8.63
CHEMBL443554 — — 1 8.43
CHEMBL346462 — — 1 8.30
CHEMBL161070 — — 1 8.30
CHEMBL350144 — — 1 8.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL279807 — Ki = 0.3548 nM 9.45
CHEMBL349665 — Ki = 0.4571 nM 9.34
CHEMBL349747 — Ki = 0.6026 nM 9.22
CHEMBL348793 — Ki = 0.6457 nM 9.19
CHEMBL163911 DELEQUAMINE Ki = 0.6607 nM 9.18
CHEMBL162971 — Ki = 0.6607 nM 9.18
CHEMBL349004 — Ki = 0.7079 nM 9.15
CHEMBL164420 — Ki = 1.072 nM 8.97
CHEMBL163570 — Ki = 1.122 nM 8.95
CHEMBL411954 — Ki = 1.259 nM 8.90
CHEMBL161278 — Ki = 1.479 nM 8.83
CHEMBL348831 — Ki = 1.514 nM 8.82
CHEMBL162965 — Ki = 1.514 nM 8.82
CHEMBL163290 — Ki = 1.514 nM 8.82
CHEMBL159919 — Ki = 1.549 nM 8.81
CHEMBL348726 — Ki = 1.585 nM 8.80
CHEMBL162841 — Ki = 1.698 nM 8.77
CHEMBL350388 — Ki = 1.698 nM 8.77
CHEMBL352278 — Ki = 1.698 nM 8.77
CHEMBL262446 — Ki = 1.82 nM 8.74
CHEMBL355140 — Ki = 1.862 nM 8.73
CHEMBL350168 — Ki = 2.042 nM 8.69
CHEMBL162024 — Ki = 2.188 nM 8.66
CHEMBL350393 — Ki = 2.188 nM 8.66
CHEMBL162109 — Ki = 2.239 nM 8.65
CHEMBL349777 — Ki = 2.344 nM 8.63
CHEMBL443554 — Ki = 3.715 nM 8.43
CHEMBL346462 — Ki = 5.012 nM 8.30
CHEMBL161070 — Ki = 5.012 nM 8.30
CHEMBL350144 — Ki = 5.012 nM 8.30
CHEMBL350105 — Ki = 6.31 nM 8.20
CHEMBL159802 — Ki = 6.761 nM 8.17
CHEMBL435057 — Ki = 6.918 nM 8.16
CHEMBL10347 RAUWOLSCINE Ki = 7.079 nM 8.15
CHEMBL161531 — Ki = 7.943 nM 8.10
CHEMBL354693 — Ki = 9.12 nM 8.04
CHEMBL30477 — Ki = 9.12 nM 8.04
CHEMBL350312 — Ki = 9.772 nM 8.01
CHEMBL10316 IDAZOXAN Ki = 10.96 nM 7.96
CHEMBL162686 — Ki = 11.48 nM 7.94
CHEMBL15245 YOHIMBINE Ki = 12.59 nM 7.90
CHEMBL160028 — Ki = 14.45 nM 7.84
CHEMBL160023 — Ki = 16.6 nM 7.78
CHEMBL351929 — Ki = 16.6 nM 7.78
CHEMBL354698 — Ki = 27.54 nM 7.56
CHEMBL161775 — Ki = 28.84 nM 7.54
CHEMBL350863 — Ki = 38.02 nM 7.42
CHEMBL350528 — Ki = 42.66 nM 7.37
CHEMBL163400 — Ki = 56.23 nM 7.25
CHEMBL163802 — Ki = 57.54 nM 7.24