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Assay Detail

CHEMBL875016

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

Binding
Ability to displace [3H]rauwolscine from Alpha-2 adrenergic receptor in rat cortical membranes
61
Total Activities
61
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-activity studies for a novel series of N-(arylethyl)-N-(1,2,3,4-tetrahydronaphthalen-1-ylmethyl)-N-methylamine s possessing dual 5-HT uptake inhibiting and alpha2-antagonistic activities.
Meyer MD, Hancock AA, Tietje K, Sippy KB, Prasad R, Stout DM, Arendsen DL, Donner BG, Carroll WA.
J Med Chem (1997) 40 : 1049 -1062
PubMed 9089327 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 61 8.02 8.91

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL10425 1 8.91
CHEMBL9783 1 8.77
CHEMBL9925 1 8.75
CHEMBL9912 1 8.75
CHEMBL9970 1 8.75
CHEMBL9924 1 8.74
CHEMBL274391 1 8.73
CHEMBL9894 1 8.73
CHEMBL268258 1 8.70
CHEMBL10304 1 8.67
CHEMBL10369 1 8.58
CHEMBL269171 1 8.58
CHEMBL10102 1 8.56
CHEMBL274867 1 8.56
CHEMBL10347 RAUWOLSCINE 1 8.54
CHEMBL10067 1 8.54
CHEMBL276236 1 8.47
CHEMBL10411 1 8.41
CHEMBL167493 NAPAMEZOLE 2.0 1 8.38
CHEMBL10115 1 8.35
CHEMBL10170 1 8.34
CHEMBL10066 1 8.33
CHEMBL10152 1 8.32
CHEMBL9869 1 8.31
CHEMBL10068 1 8.31
CHEMBL9896 1 8.28
CHEMBL10410 1 8.27
CHEMBL269402 1 8.27
CHEMBL418337 1 8.26
CHEMBL10052 1 8.25

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL10425 Ki = 1.22 nM 8.91
CHEMBL9783 Ki = 1.7 nM 8.77
CHEMBL9912 Ki = 1.76 nM 8.75
CHEMBL9970 Ki = 1.78 nM 8.75
CHEMBL9925 Ki = 1.77 nM 8.75
CHEMBL9924 Ki = 1.81 nM 8.74
CHEMBL274391 Ki = 1.88 nM 8.73
CHEMBL9894 Ki = 1.86 nM 8.73
CHEMBL268258 Ki = 2.01 nM 8.70
CHEMBL10304 Ki = 2.12 nM 8.67
CHEMBL10369 Ki = 2.65 nM 8.58
CHEMBL269171 Ki = 2.64 nM 8.58
CHEMBL10102 Ki = 2.78 nM 8.56
CHEMBL274867 Ki = 2.73 nM 8.56
CHEMBL10067 Ki = 2.88 nM 8.54
CHEMBL10347 RAUWOLSCINE Ki = 2.89 nM 8.54
CHEMBL276236 Ki = 3.42 nM 8.47
CHEMBL10411 Ki = 3.91 nM 8.41
CHEMBL167493 NAPAMEZOLE Ki = 4.17 nM 8.38
CHEMBL10115 Ki = 4.51 nM 8.35
CHEMBL10170 Ki = 4.62 nM 8.34
CHEMBL10066 Ki = 4.67 nM 8.33
CHEMBL10152 Ki = 4.82 nM 8.32
CHEMBL9869 Ki = 4.91 nM 8.31
CHEMBL10068 Ki = 4.88 nM 8.31
CHEMBL9896 Ki = 5.21 nM 8.28
CHEMBL269402 Ki = 5.35 nM 8.27
CHEMBL10410 Ki = 5.33 nM 8.27
CHEMBL418337 Ki = 5.45 nM 8.26
CHEMBL10052 Ki = 5.57 nM 8.25
CHEMBL273874 Ki = 5.67 nM 8.25
CHEMBL10187 Ki = 5.73 nM 8.24
CHEMBL268463 Ki = 6.07 nM 8.22
CHEMBL430314 Ki = 5.99 nM 8.22
CHEMBL9831 Ki = 6.71 nM 8.17
CHEMBL9938 Ki = 6.79 nM 8.17
CHEMBL9844 Ki = 7.54 nM 8.12
CHEMBL269452 Ki = 7.5 nM 8.12
CHEMBL10451 Ki = 8.19 nM 8.09
CHEMBL10409 Ki = 8.99 nM 8.05
CHEMBL10385 Ki = 9.27 nM 8.03
CHEMBL9886 Ki = 10.8 nM 7.97
CHEMBL276667 Ki = 11.0 nM 7.96
CHEMBL274055 Ki = 11.7 nM 7.93
CHEMBL276826 Ki = 15.5 nM 7.81
CHEMBL400421 Ki = 17.9 nM 7.75
CHEMBL10216 Ki = 19.0 nM 7.72
CHEMBL9860 Ki = 21.0 nM 7.68
CHEMBL268749 Ki = 23.5 nM 7.63
CHEMBL269208 Ki = 54.3 nM 7.26