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Assay Detail

CHEMBL615963

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

Binding
Evaluated for the binding affinity to hippocampus striatal membranes at 5-hydroxytryptamine 1A receptor binding site by using [3H]-8-OH- DPAT as a radioligand.
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Striatum
Subcellular Membrane
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Central serotonin receptors as targets for drug research.
Glennon RA.
J Med Chem (1987) 30 : 1 -12
PubMed 3543362 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 23 7.16 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL18840 1 9.70
CHEMBL56 8-OH-DPAT 1 8.70
CHEMBL39 SEROTONIN 3.0 1 8.52
CHEMBL18785 RU-24969 1 8.30
CHEMBL277362 1 8.30
CHEMBL19215 METERGOLINE 2.0 1 8.22
CHEMBL8165 5-METHOXYTRYPTAMINE 1 8.05
CHEMBL7257 MEBUFOTENIN 2.0 1 7.70
CHEMBL500 PINDOLOL 4.0 1 7.70
CHEMBL267930 SPIPERONE 2.0 1 7.40
CHEMBL275854 1 7.07
CHEMBL18855 1 7.02
CHEMBL452861 LEVOPROPRANOLOL 2.0 1 6.94
CHEMBL6640 TRYPTAMINE 1 6.77
CHEMBL416526 BUFOTENINE 1 6.59
CHEMBL12314 MESULERGINE 2.0 1 6.52
CHEMBL19264 1 5.80
CHEMBL18331 PIRENPERONE 2.0 1 5.77
CHEMBL51 KETANSERIN 3.0 1 5.72
CHEMBL274866 1 5.71
CHEMBL478 CHLOROPHENYLPIPERAZINE 2.0 1 5.62
CHEMBL18772 QUIPAZINE 2.0 1 5.48
CHEMBL134519 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL18840 Ki = 0.2 nM 9.70
CHEMBL56 8-OH-DPAT Ki = 2.0 nM 8.70
CHEMBL39 SEROTONIN Ki = 3.0 nM 8.52
CHEMBL18785 RU-24969 Ki = 5.0 nM 8.30
CHEMBL277362 Ki = 5.0 nM 8.30
CHEMBL19215 METERGOLINE Ki = 6.0 nM 8.22
CHEMBL8165 5-METHOXYTRYPTAMINE Ki = 9.0 nM 8.05
CHEMBL7257 MEBUFOTENIN Ki = 20.0 nM 7.70
CHEMBL500 PINDOLOL Ki = 20.0 nM 7.70
CHEMBL267930 SPIPERONE Ki = 40.0 nM 7.40
CHEMBL275854 Ki = 85.0 nM 7.07
CHEMBL18855 Ki = 95.0 nM 7.02
CHEMBL452861 LEVOPROPRANOLOL Ki = 115.0 nM 6.94
CHEMBL6640 TRYPTAMINE Ki = 170.0 nM 6.77
CHEMBL416526 BUFOTENINE Ki = 259.0 nM 6.59
CHEMBL12314 MESULERGINE Ki = 300.0 nM 6.52
CHEMBL19264 Ki = 1590.0 nM 5.80
CHEMBL18331 PIRENPERONE Ki = 1700.0 nM 5.77
CHEMBL51 KETANSERIN Ki = 1900.0 nM 5.72
CHEMBL274866 Ki = 1950.0 nM 5.71
CHEMBL478 CHLOROPHENYLPIPERAZINE Ki = 2400.0 nM 5.62
CHEMBL18772 QUIPAZINE Ki = 3300.0 nM 5.48
CHEMBL134519 Ki - nM -