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Assay Detail

CHEMBL616344

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

Binding
Binding affinity of a compound to rat brain 5-hydroxytryptamine 1A (serotonin) receptor assayed by radiolabeled [3H]-8-OH-DPAT ligand displacement
ChEMBL ↗
281
Total Activities
268
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Binding of arylpiperazines, (aryloxy)propanolamines, and tetrahydropyridylindoles to the 5-HT1A receptor: contribution of the molecular lipophilicity potential to three-dimensional quantitative structure-affinity relationship models.
Gaillard P, Carrupt PA, Testa B, Schambel P.
J Med Chem (1996) 39 : 126 -134
PubMed 8568799 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 281 7.37 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL11592 — — 1 10.00
CHEMBL27991 — — 1 9.70
CHEMBL28143 — — 1 9.60
CHEMBL18840 — — 1 9.53
CHEMBL26533 — — 1 9.40
CHEMBL282798 — — 1 9.40
CHEMBL26926 — — 1 9.30
CHEMBL26304 — — 2 9.30
CHEMBL28287 — — 1 9.30
CHEMBL27763 — — 2 9.30
CHEMBL27457 — — 1 9.30
CHEMBL28312 — — 1 9.30
CHEMBL27060 — — 1 9.30
CHEMBL27650 — — 1 9.30
CHEMBL27558 — — 1 9.27
CHEMBL28000 — — 1 9.25
CHEMBL26962 — — 1 9.22
CHEMBL8618 NAN-190 — 1 9.22
CHEMBL285158 — — 2 9.21
CHEMBL286250 — — 1 9.15
CHEMBL410826 — — 1 9.15
CHEMBL26834 — — 1 9.09
CHEMBL26018 — — 1 9.00
CHEMBL26783 — — 1 9.00
CHEMBL283846 — — 1 9.00
CHEMBL21008 — — 1 9.00
CHEMBL26587 — — 1 9.00
CHEMBL280608 — — 1 9.00
CHEMBL416747 — — 1 9.00
CHEMBL280586 — — 1 8.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL11592 — Ki = 0.1 nM 10.00
CHEMBL27991 — Ki = 0.1995 nM 9.70
CHEMBL28143 — Ki = 0.2512 nM 9.60
CHEMBL18840 — Ki = 0.2951 nM 9.53
CHEMBL282798 — Ki = 0.3981 nM 9.40
CHEMBL26533 — Ki = 0.3981 nM 9.40
CHEMBL28287 — Ki = 0.5012 nM 9.30
CHEMBL26926 — Ki = 0.5012 nM 9.30
CHEMBL27650 — Ki = 0.5012 nM 9.30
CHEMBL27763 — Ki = 0.5012 nM 9.30
CHEMBL28312 — Ki = 0.5012 nM 9.30
CHEMBL26304 — Ki = 0.5012 nM 9.30
CHEMBL27457 — Ki = 0.5012 nM 9.30
CHEMBL27060 — Ki = 0.5012 nM 9.30
CHEMBL27558 — Ki = 0.537 nM 9.27
CHEMBL28000 — Ki = 0.5623 nM 9.25
CHEMBL26962 — Ki = 0.6026 nM 9.22
CHEMBL8618 NAN-190 Ki = 0.6026 nM 9.22
CHEMBL285158 — Ki = 0.6166 nM 9.21
CHEMBL286250 — Ki = 0.7079 nM 9.15
CHEMBL410826 — Ki = 0.7079 nM 9.15
CHEMBL26834 — Ki = 0.8128 nM 9.09
CHEMBL285158 — Ki = 1.0 nM 9.00
CHEMBL21008 — Ki = 1.0 nM 9.00
CHEMBL26304 — Ki = 1.0 nM 9.00
CHEMBL280608 — Ki = 1.0 nM 9.00
CHEMBL26587 — Ki = 1.0 nM 9.00
CHEMBL26018 — Ki = 1.0 nM 9.00
CHEMBL283846 — Ki = 1.0 nM 9.00
CHEMBL416747 — Ki = 1.0 nM 9.00
CHEMBL26783 — Ki = 1.0 nM 9.00
CHEMBL280586 — Ki = 1.514 nM 8.82
CHEMBL26835 — Ki = 1.698 nM 8.77
CHEMBL26988 — Ki = 1.698 nM 8.77
CHEMBL27021 — Ki = 1.82 nM 8.74
CHEMBL283174 — Ki = 1.82 nM 8.74
CHEMBL56 8-OH-DPAT Ki = 1.862 nM 8.73
CHEMBL285351 — Ki = 1.905 nM 8.72
CHEMBL27429 — Ki = 1.995 nM 8.70
CHEMBL27995 — Ki = 1.995 nM 8.70
CHEMBL26975 — Ki = 1.995 nM 8.70
CHEMBL26188 — Ki = 1.995 nM 8.70
CHEMBL27937 — Ki = 1.995 nM 8.70
CHEMBL27996 — Ki = 1.995 nM 8.70
CHEMBL28111 — Ki = 2.089 nM 8.68
CHEMBL26781 — Ki = 2.138 nM 8.67
CHEMBL26601 — Ki = 2.188 nM 8.66
CHEMBL13647 BMY-7378 Ki = 2.399 nM 8.62
CHEMBL1290 PENBUTOLOL Ki = 2.399 nM 8.62
CHEMBL283207 — Ki = 2.512 nM 8.60