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Assay Detail

CHEMBL1006686

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

Binding
Displacement of [3H]LY278584 from 5HT3 receptor in rat cortical homogenate
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

5-hydroxytryptamine receptor 3A (CHEMBL2411)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Specific targeting of peripheral serotonin 5-HT(3) receptors. Synthesis, biological investigation, and structure-activity relationships.
Morelli E, Gemma S, Budriesi R, Campiani G, Novellino E, Fattorusso C, Catalanotti B, Coccone SS, Ros S, Borrelli G, Persico M, Fiorini I, Nacci V, Ioan P, Chiarini A, Hamon M, Cagnotto A, Mennini T, Fracasso C, Colovic M, Caccia S, Butini S.
J Med Chem (2009) 52 : 3548 -3562
PubMed 19425598 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 19 8.03 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL523716 1 9.10
CHEMBL341474 1 9.10
CHEMBL18772 QUIPAZINE 2.0 1 9.02
CHEMBL466462 1 8.92
CHEMBL445505 1 8.68
CHEMBL492395 1 8.66
CHEMBL511555 1 8.55
CHEMBL523042 1 8.52
CHEMBL503987 1 8.47
CHEMBL493183 1 8.14
CHEMBL468498 1 7.95
CHEMBL523497 1 7.93
CHEMBL512418 1 7.77
CHEMBL494999 1 7.36
CHEMBL466456 1 7.19
CHEMBL495000 1 7.10
CHEMBL466655 1 6.90
CHEMBL466662 1 6.62
CHEMBL466446 1 6.61

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL523716 Ki = 0.8 nM 9.10
CHEMBL341474 Ki = 0.8 nM 9.10
CHEMBL18772 QUIPAZINE Ki = 0.96 nM 9.02
CHEMBL466462 Ki = 1.2 nM 8.92
CHEMBL445505 Ki = 2.1 nM 8.68
CHEMBL492395 Ki = 2.2 nM 8.66
CHEMBL511555 Ki = 2.8 nM 8.55
CHEMBL523042 Ki = 3.0 nM 8.52
CHEMBL503987 Ki = 3.4 nM 8.47
CHEMBL493183 Ki = 7.3 nM 8.14
CHEMBL468498 Ki = 11.2 nM 7.95
CHEMBL523497 Ki = 11.7 nM 7.93
CHEMBL512418 Ki = 17.0 nM 7.77
CHEMBL494999 Ki = 44.0 nM 7.36
CHEMBL466456 Ki = 65.0 nM 7.19
CHEMBL495000 Ki = 79.0 nM 7.10
CHEMBL466655 Ki = 127.0 nM 6.90
CHEMBL466662 Ki = 237.0 nM 6.62
CHEMBL466446 Ki = 246.0 nM 6.61