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Assay Detail

CHEMBL648726

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

Binding
Binding affinity towards alpha-2 adrenergic receptor in rat cortex membrane using [3H]rauwolscine radioligand
ChEMBL ↗
50
Total Activities
50
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, biological evaluation, and pharmacophore generation of new pyridazinone derivatives with affinity toward alpha(1)- and alpha(2)-adrenoceptors.
Barbaro R, Betti L, Botta M, Corelli F, Giannaccini G, Maccari L, Manetti F, Strappaghetti G, Corsano S.
J Med Chem (2001) 44 : 2118 -2132
PubMed 11405649 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 50 7.07 8.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL66172 — — 1 8.46
CHEMBL10347 RAUWOLSCINE — 1 8.40
CHEMBL49152 — — 1 8.34
CHEMBL67132 — — 1 8.13
CHEMBL304783 — — 1 7.82
CHEMBL65963 — — 1 7.75
CHEMBL302832 — — 1 7.64
CHEMBL304325 — — 1 7.64
CHEMBL302857 — — 1 7.63
CHEMBL67201 — — 1 7.63
CHEMBL66965 — — 1 7.62
CHEMBL417745 — — 1 7.62
CHEMBL302268 — — 1 7.61
CHEMBL303347 — — 1 7.60
CHEMBL303894 — — 1 7.54
CHEMBL67114 — — 1 7.44
CHEMBL303895 — — 1 7.41
CHEMBL302554 — — 1 7.34
CHEMBL65887 — — 1 7.28
CHEMBL66450 — — 1 7.21
CHEMBL68447 — — 1 7.18
CHEMBL68052 — — 1 7.16
CHEMBL66748 — — 1 7.16
CHEMBL67773 — — 1 7.14
CHEMBL66272 — — 1 7.07
CHEMBL304943 — — 1 7.02
CHEMBL70173 — — 1 7.00
CHEMBL417565 — — 1 6.98
CHEMBL306440 — — 1 6.86
CHEMBL67081 — — 1 6.86

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL66172 — Ki = 3.5 nM 8.46
CHEMBL10347 RAUWOLSCINE Ki = 4.0 nM 8.40
CHEMBL49152 — Ki = 4.6 nM 8.34
CHEMBL67132 — Ki = 7.4 nM 8.13
CHEMBL304783 — Ki = 15.0 nM 7.82
CHEMBL65963 — Ki = 18.0 nM 7.75
CHEMBL302832 — Ki = 22.7 nM 7.64
CHEMBL304325 — Ki = 22.8 nM 7.64
CHEMBL302857 — Ki = 23.5 nM 7.63
CHEMBL67201 — Ki = 23.3 nM 7.63
CHEMBL66965 — Ki = 23.7 nM 7.62
CHEMBL417745 — Ki = 24.0 nM 7.62
CHEMBL302268 — Ki = 24.5 nM 7.61
CHEMBL303347 — Ki = 25.2 nM 7.60
CHEMBL303894 — Ki = 29.0 nM 7.54
CHEMBL67114 — Ki = 36.2 nM 7.44
CHEMBL303895 — Ki = 39.3 nM 7.41
CHEMBL302554 — Ki = 45.8 nM 7.34
CHEMBL65887 — Ki = 52.6 nM 7.28
CHEMBL66450 — Ki = 62.0 nM 7.21
CHEMBL68447 — Ki = 66.0 nM 7.18
CHEMBL68052 — Ki = 69.4 nM 7.16
CHEMBL66748 — Ki = 69.8 nM 7.16
CHEMBL67773 — Ki = 71.8 nM 7.14
CHEMBL66272 — Ki = 85.0 nM 7.07
CHEMBL304943 — Ki = 96.0 nM 7.02
CHEMBL70173 — Ki = 100.0 nM 7.00
CHEMBL417565 — Ki = 105.0 nM 6.98
CHEMBL306440 — Ki = 138.8 nM 6.86
CHEMBL67081 — Ki = 138.0 nM 6.86
CHEMBL302051 — Ki = 139.0 nM 6.86
CHEMBL67379 — Ki = 150.0 nM 6.82
CHEMBL431721 — Ki = 219.0 nM 6.66
CHEMBL66747 — Ki = 230.0 nM 6.64
CHEMBL67639 — Ki = 245.0 nM 6.61
CHEMBL67856 — Ki = 255.0 nM 6.59
CHEMBL67882 — Ki = 254.0 nM 6.59
CHEMBL63876 — Ki = 260.0 nM 6.58
CHEMBL305173 — Ki = 280.0 nM 6.55
CHEMBL66850 — Ki = 292.3 nM 6.53
CHEMBL67681 — Ki = 316.0 nM 6.50
CHEMBL63781 — Ki = 370.0 nM 6.43
CHEMBL303130 — Ki = 409.0 nM 6.39
CHEMBL67478 — Ki = 440.0 nM 6.36
CHEMBL46172 — Ki = 520.0 nM 6.28
CHEMBL66607 — Ki = 631.0 nM 6.20
CHEMBL67218 — Ki = 680.0 nM 6.17
CHEMBL303017 — Ki = 790.0 nM 6.10
CHEMBL67162 — Ki = 870.0 nM 6.06
CHEMBL66118 — Ki = 1261.0 nM 5.90