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Assay Detail

CHEMBL618921

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Binding
Affinity was evaluated as inhibition constant for serotonin 5-hydroxytryptamine 3 receptor
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 6 — Multiple protein complex / RNA
Curated By Autocuration

Target

Serotonin 3 (5-HT3) receptor (CHEMBL2094116)
Type PROTEIN COMPLEX
Organism Rattus norvegicus

Publication

Binding of 5H-dibenzo[b,e][1,4]diazepine and chiral 5H-dibenzo[a,d]cycloheptene analogues of clozapine to dopamine and serotonin receptors.
Phillips ST, de Paulis T, Baron BM, Siegel BW, Seeman P, Van Tol HH, Guan HC, Smith HE.
J Med Chem (1994) 37 : 2686 -2696
PubMed 8064797 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 7.43 7.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL415300 ISOCLOZAPINE 1 7.66
CHEMBL73538 1 7.40
CHEMBL266723 1 7.40
CHEMBL7430 1 7.39
CHEMBL42 CLOZAPINE 4.0 1 7.28
CHEMBL269396 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL415300 ISOCLOZAPINE Ki = 22.0 nM 7.66
CHEMBL73538 Ki = 40.0 nM 7.40
CHEMBL266723 Ki = 40.0 nM 7.40
CHEMBL7430 Ki = 41.0 nM 7.39
CHEMBL42 CLOZAPINE Ki = 53.0 nM 7.28
CHEMBL269396 Ki > 1000.0 nM -