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Assay Detail

CHEMBL615782

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Binding
Tested for 5-hydroxytryptamine 1 receptor binding ability by displacement of [3H]5-HT from rat brain synaptosomes
ChEMBL ↗
60
Total Activities
60
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Brain
Subcellular Synaptosomes
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Serotonin 1 (5-HT1) receptor (CHEMBL2095159) ↗
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Synthesis and 5-hydroxytryptamine antagonist activity of 2-[[2-(dimethylamino)ethyl]thio]-3-phenylquinoline and its analogues.
Blackburn TP, Cox B, Guildford AJ, Le Count DJ, Middlemiss DN, Pearce RJ, Thornber CW.
J Med Chem (1987) 30 : 2252 -2259
PubMed 3681895 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 60 5.92 7.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1065 METHYSERGIDE 4.0 1 7.50
CHEMBL307590 — — 1 6.70
CHEMBL73081 — — 1 6.60
CHEMBL544293 — — 1 6.60
CHEMBL553289 — — 1 6.60
CHEMBL76109 — — 1 6.50
CHEMBL310155 — — 1 6.40
CHEMBL75931 — — 1 6.40
CHEMBL75999 — — 1 6.40
CHEMBL544060 — — 1 6.40
CHEMBL305663 — — 1 6.30
CHEMBL72656 — — 1 6.30
CHEMBL541554 — — 1 6.20
CHEMBL543350 — — 1 6.20
CHEMBL543114 — — 1 6.20
CHEMBL544062 — — 1 6.20
CHEMBL543112 — — 1 6.20
CHEMBL542401 — — 1 6.20
CHEMBL543824 — — 1 6.20
CHEMBL544531 — — 1 6.20
CHEMBL543346 — — 1 6.10
CHEMBL543347 — — 1 6.10
CHEMBL73124 — — 1 6.10
CHEMBL544061 — — 1 6.10
CHEMBL553501 — — 1 6.00
CHEMBL419444 — — 1 6.00
CHEMBL74995 — — 1 6.00
CHEMBL72420 — — 1 6.00
CHEMBL306411 — — 1 6.00
CHEMBL76227 — — 1 6.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1065 METHYSERGIDE IC50 = 31.62 nM 7.50
CHEMBL307590 — IC50 = 199.53 nM 6.70
CHEMBL73081 — IC50 = 251.19 nM 6.60
CHEMBL544293 — IC50 = 251.19 nM 6.60
CHEMBL553289 — IC50 = 251.19 nM 6.60
CHEMBL76109 — IC50 = 316.23 nM 6.50
CHEMBL310155 — IC50 = 398.11 nM 6.40
CHEMBL75931 — IC50 = 398.11 nM 6.40
CHEMBL75999 — IC50 = 398.11 nM 6.40
CHEMBL544060 — IC50 = 398.11 nM 6.40
CHEMBL305663 — IC50 = 501.19 nM 6.30
CHEMBL72656 — IC50 = 501.19 nM 6.30
CHEMBL542401 — IC50 = 630.96 nM 6.20
CHEMBL543350 — IC50 = 630.96 nM 6.20
CHEMBL543114 — IC50 = 630.96 nM 6.20
CHEMBL544062 — IC50 = 630.96 nM 6.20
CHEMBL543112 — IC50 = 630.96 nM 6.20
CHEMBL541554 — IC50 = 630.96 nM 6.20
CHEMBL543824 — IC50 = 630.96 nM 6.20
CHEMBL544531 — IC50 = 630.96 nM 6.20
CHEMBL543346 — IC50 = 794.33 nM 6.10
CHEMBL543347 — IC50 = 794.33 nM 6.10
CHEMBL73124 — IC50 = 794.33 nM 6.10
CHEMBL544061 — IC50 = 794.33 nM 6.10
CHEMBL419444 — IC50 = 1000.0 nM 6.00
CHEMBL544998 — IC50 = 1000.0 nM 6.00
CHEMBL76227 — IC50 = 1000.0 nM 6.00
CHEMBL306411 — IC50 = 1000.0 nM 6.00
CHEMBL74995 — IC50 = 1000.0 nM 6.00
CHEMBL553501 — IC50 = 1000.0 nM 6.00
CHEMBL72420 — IC50 = 1000.0 nM 6.00
CHEMBL544999 — IC50 = 1258.93 nM 5.90
CHEMBL545701 — IC50 = 1258.93 nM 5.90
CHEMBL419628 — IC50 = 1584.89 nM 5.80
CHEMBL73230 — IC50 = 1584.89 nM 5.80
CHEMBL555008 — IC50 = 1584.89 nM 5.80
CHEMBL544294 — IC50 = 1584.89 nM 5.80
CHEMBL540801 — IC50 = 1584.89 nM 5.80
CHEMBL305907 — IC50 = 1584.89 nM 5.80
CHEMBL545696 — IC50 = 1584.89 nM 5.80
CHEMBL73166 — IC50 = 1995.26 nM 5.70
CHEMBL73422 — IC50 = 1995.26 nM 5.70
CHEMBL542644 — IC50 = 1995.26 nM 5.70
CHEMBL556134 — IC50 = 1995.26 nM 5.70
CHEMBL543831 — IC50 = 2511.89 nM 5.60
CHEMBL539014 — IC50 = 2511.89 nM 5.60
CHEMBL311130 — IC50 = 2511.89 nM 5.60
CHEMBL542151 — IC50 = 2511.89 nM 5.60
CHEMBL552901 — IC50 = 3162.28 nM 5.50
CHEMBL542882 — IC50 = 3981.07 nM 5.40