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Assay Detail

CHEMBL617433

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

Binding
Ability to displace [3H]ketanserin from serotonergic 5-hydroxytryptamine 2 receptor
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Serotonin 2 (5-HT2) receptor (CHEMBL2093870)
Type PROTEIN FAMILY
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 6.65 9.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL85 RISPERIDONE 4.0 1 9.85
CHEMBL21318 1 7.66
CHEMBL278151 1 7.57
CHEMBL54 HALOPERIDOL 4.0 1 7.37
CHEMBL22468 1 7.00
CHEMBL281363 1 6.55
CHEMBL22306 1 6.40
CHEMBL21386 1 6.38
CHEMBL22835 1 6.26
CHEMBL279937 1 5.77
CHEMBL21971 1 5.68
CHEMBL280912 1 5.64
CHEMBL22772 1 5.48
CHEMBL21940 1 5.43
CHEMBL21819 1 -
CHEMBL22469 1 -
CHEMBL21802 1 -
CHEMBL278838 1 -
CHEMBL21403 1 -
CHEMBL21680 1 -
CHEMBL418374 1 -
CHEMBL22154 1 -
CHEMBL282935 1 -
CHEMBL279698 1 -
CHEMBL279292 1 -
CHEMBL418560 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL85 RISPERIDONE Ki = 0.14 nM 9.85
CHEMBL21318 Ki = 22.0 nM 7.66
CHEMBL278151 Ki = 27.0 nM 7.57
CHEMBL54 HALOPERIDOL Ki = 43.0 nM 7.37
CHEMBL22468 Ki = 99.0 nM 7.00
CHEMBL281363 Ki = 280.0 nM 6.55
CHEMBL22306 Ki = 400.0 nM 6.40
CHEMBL21386 Ki = 420.0 nM 6.38
CHEMBL22835 Ki = 550.0 nM 6.26
CHEMBL279937 Ki = 1700.0 nM 5.77
CHEMBL21971 Ki = 2100.0 nM 5.68
CHEMBL280912 Ki = 2300.0 nM 5.64
CHEMBL22772 Ki = 3300.0 nM 5.48
CHEMBL21940 Ki = 3700.0 nM 5.43
CHEMBL21819 Ki > 1000.0 nM -
CHEMBL22469 Ki > 1000.0 nM -
CHEMBL21802 Ki > 1000.0 nM -
CHEMBL278838 Ki > 1000.0 nM -
CHEMBL21403 Ki > 1000.0 nM -
CHEMBL21680 Ki > 1000.0 nM -
CHEMBL418374 Ki > 1000.0 nM -
CHEMBL22154 Ki > 1000.0 nM -
CHEMBL282935 Ki > 1000.0 nM -
CHEMBL279698 Ki > 1000.0 nM -
CHEMBL279292 Ki > 1000.0 nM -
CHEMBL418560 Ki > 1000.0 nM -