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Assay Detail

CHEMBL616062

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

Binding
Binding affinity towards 5-hydroxytryptamine 1A receptor of rat hippocampus using [3H]-8-hydroxy-2-(di-n-propylamine) tetralin (8-OH-DPAT) as a radioligand
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Analogues of the 5-HT1A serotonin antagonist 1-(2-methoxyphenyl)-4-[4-(2-phthalimido)butyl]piperazine with reduced alpha 1-adrenergic affinity.
Raghupathi RK, Rydelek-Fitzgerald L, Teitler M, Glennon RA.
J Med Chem (1991) 34 : 2633 -2638
PubMed 1652026 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 18 8.31 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL26533 1 9.40
CHEMBL8618 NAN-190 1 9.22
CHEMBL410826 1 9.15
CHEMBL21008 1 9.00
CHEMBL26587 1 9.00
CHEMBL27996 1 8.70
CHEMBL26188 1 8.70
CHEMBL24515 1 8.44
CHEMBL26189 1 8.40
CHEMBL27254 1 8.40
CHEMBL282902 1 8.36
CHEMBL27377 1 8.27
CHEMBL287186 1 8.20
CHEMBL27098 1 8.12
CHEMBL26539 1 7.92
CHEMBL26306 1 7.66
CHEMBL316090 1 6.67
CHEMBL26030 1 6.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL26533 Ki = 0.4 nM 9.40
CHEMBL8618 NAN-190 Ki = 0.6 nM 9.22
CHEMBL410826 Ki = 0.7 nM 9.15
CHEMBL21008 Ki = 1.0 nM 9.00
CHEMBL26587 Ki = 1.0 nM 9.00
CHEMBL27996 Ki = 2.0 nM 8.70
CHEMBL26188 Ki = 2.0 nM 8.70
CHEMBL24515 Ki = 3.6 nM 8.44
CHEMBL26189 Ki = 4.0 nM 8.40
CHEMBL27254 Ki = 4.0 nM 8.40
CHEMBL282902 Ki = 4.4 nM 8.36
CHEMBL27377 Ki = 5.4 nM 8.27
CHEMBL287186 Ki = 6.3 nM 8.20
CHEMBL27098 Ki = 7.5 nM 8.12
CHEMBL26539 Ki = 12.0 nM 7.92
CHEMBL26306 Ki = 22.0 nM 7.66
CHEMBL316090 Ki = 213.0 nM 6.67
CHEMBL26030 Ki = 1000.0 nM 6.00