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Assay Detail

CHEMBL617845

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Binding
Affinity was evaluated as inhibition constant for serotonin 5-hydroxytryptamine 2C receptor
13
Total Activities
11
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 2C (CHEMBL324)
Type SINGLE PROTEIN
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 13 7.04 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL7430 1 8.52
CHEMBL42 CLOZAPINE 4.0 1 8.10
CHEMBL415300 ISOCLOZAPINE 1 7.96
CHEMBL327713 1 7.46
CHEMBL90654 1 7.16
CHEMBL266723 1 7.13
CHEMBL73538 1 7.08
CHEMBL91350 1 7.05
CHEMBL89719 1 6.60
CHEMBL94067 3 6.08
CHEMBL269396 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL7430 Ki = 3.0 nM 8.52
CHEMBL42 CLOZAPINE Ki = 8.0 nM 8.10
CHEMBL415300 ISOCLOZAPINE Ki = 11.0 nM 7.96
CHEMBL327713 Ki = 35.0 nM 7.46
CHEMBL90654 Ki = 70.0 nM 7.16
CHEMBL266723 Ki = 74.0 nM 7.13
CHEMBL73538 Ki = 84.0 nM 7.08
CHEMBL91350 Ki = 89.0 nM 7.05
CHEMBL89719 Ki = 250.0 nM 6.60
CHEMBL94067 Ki = 830.0 nM 6.08
CHEMBL94067 Ki = 1500.0 nM 5.82
CHEMBL94067 Ki = 3300.0 nM 5.48
CHEMBL269396 Ki > 1000.0 nM -