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Assay Detail

CHEMBL615844

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

Binding
Binding affinity for 5-hydroxytryptamine 1A receptor in rat brain tissue using [3H]8-OH-DPAT as radioligand
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Brain
Confidence 8 — Homologous single protein target
Curated By Expert

Target

5-hydroxytryptamine receptor 1A (CHEMBL273)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Derivatives of cis-2-amino-8-hydroxy-1-methyltetralin: mixed 5-HT1A-receptor agonists and dopamine D2-receptor antagonists.
Liu Y, Yu H, Mohell N, Nordvall G, Lewander T, Hacksell U.
J Med Chem (1995) 38 : 150 -160
PubMed 7530773 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 23 7.31 9.25

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL290091 1 9.25
CHEMBL41187 1 8.59
CHEMBL43475 1 8.54
CHEMBL26998 1 8.39
CHEMBL290446 1 8.22
CHEMBL290546 1 8.17
CHEMBL289106 1 8.12
CHEMBL40634 1 7.75
CHEMBL288284 1 7.42
CHEMBL297143 1 7.36
CHEMBL41802 1 7.31
CHEMBL288721 1 7.09
CHEMBL38192 1 6.94
CHEMBL38748 1 6.86
CHEMBL288540 1 6.63
CHEMBL287770 1 6.54
CHEMBL40603 1 6.38
CHEMBL38916 1 5.85
CHEMBL40264 1 5.54
CHEMBL288583 1 5.18
CHEMBL44569 1 -
CHEMBL41801 1 -
CHEMBL41261 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL290091 Ki = 0.56 nM 9.25
CHEMBL41187 Ki = 2.6 nM 8.59
CHEMBL43475 Ki = 2.9 nM 8.54
CHEMBL26998 Ki = 4.1 nM 8.39
CHEMBL290446 Ki = 6.0 nM 8.22
CHEMBL290546 Ki = 6.7 nM 8.17
CHEMBL289106 Ki = 7.6 nM 8.12
CHEMBL40634 Ki = 18.0 nM 7.75
CHEMBL288284 Ki = 38.0 nM 7.42
CHEMBL297143 Ki = 44.0 nM 7.36
CHEMBL41802 Ki = 49.0 nM 7.31
CHEMBL288721 Ki = 81.0 nM 7.09
CHEMBL38192 Ki = 116.0 nM 6.94
CHEMBL38748 Ki = 138.0 nM 6.86
CHEMBL288540 Ki = 236.0 nM 6.63
CHEMBL287770 Ki = 285.0 nM 6.54
CHEMBL40603 Ki = 417.0 nM 6.38
CHEMBL38916 Ki = 1420.0 nM 5.85
CHEMBL40264 Ki = 2920.0 nM 5.54
CHEMBL288583 Ki = 6650.0 nM 5.18
CHEMBL44569 Ki > 1000.0 nM -
CHEMBL41801 Ki > 1000.0 nM -
CHEMBL41261 Ki > 1000.0 nM -