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Assay Detail

CHEMBL616101

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

Binding
Ability to displace [3H]-8-OH-DPAT from serotonergic 5-hydroxytryptamine 1A receptor
26
Total Activities
26
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

N-(2-pyrrolidinylmethyl)benzoxazine-8-carboxamides exhibiting high affinities for All of D2, 5-HT1 A, and 5-HT2 receptors
Kuroita T, Ikebe T, Murakami S, Takehara S, Kawakita T
Bioorg Med Chem Lett (1995) 5 : 1245 -1250
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 26 7.05 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL281363 1 8.00
CHEMBL21940 1 7.80
CHEMBL278151 1 7.77
CHEMBL22772 1 7.75
CHEMBL21971 1 7.72
CHEMBL22468 1 7.68
CHEMBL279937 1 7.46
CHEMBL280912 1 7.09
CHEMBL21318 1 6.92
CHEMBL85 RISPERIDONE 4.0 1 6.89
CHEMBL21386 1 6.66
CHEMBL278838 1 6.48
CHEMBL22306 1 6.48
CHEMBL22154 1 6.24
CHEMBL22835 1 6.06
CHEMBL54 HALOPERIDOL 4.0 1 5.75
CHEMBL21802 1 -
CHEMBL418560 1 -
CHEMBL22469 1 -
CHEMBL279292 1 -
CHEMBL21403 1 -
CHEMBL418374 1 -
CHEMBL21680 1 -
CHEMBL21819 1 -
CHEMBL282935 1 -
CHEMBL279698 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL281363 Ki = 10.0 nM 8.00
CHEMBL21940 Ki = 16.0 nM 7.80
CHEMBL278151 Ki = 17.0 nM 7.77
CHEMBL22772 Ki = 18.0 nM 7.75
CHEMBL21971 Ki = 19.0 nM 7.72
CHEMBL22468 Ki = 21.0 nM 7.68
CHEMBL279937 Ki = 35.0 nM 7.46
CHEMBL280912 Ki = 81.0 nM 7.09
CHEMBL21318 Ki = 120.0 nM 6.92
CHEMBL85 RISPERIDONE Ki = 130.0 nM 6.89
CHEMBL21386 Ki = 220.0 nM 6.66
CHEMBL278838 Ki = 330.0 nM 6.48
CHEMBL22306 Ki = 330.0 nM 6.48
CHEMBL22154 Ki = 570.0 nM 6.24
CHEMBL22835 Ki = 880.0 nM 6.06
CHEMBL54 HALOPERIDOL Ki = 1800.0 nM 5.75
CHEMBL21802 Ki > 1000.0 nM -
CHEMBL418560 Ki > 1000.0 nM -
CHEMBL22469 Ki > 1000.0 nM -
CHEMBL279292 Ki > 1000.0 nM -
CHEMBL21403 Ki > 1000.0 nM -
CHEMBL418374 Ki > 1000.0 nM -
CHEMBL21680 Ki > 1000.0 nM -
CHEMBL21819 Ki > 1000.0 nM -
CHEMBL282935 Ki > 1000.0 nM -
CHEMBL279698 Ki > 1000.0 nM -