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Assay Detail

CHEMBL669953

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

Binding
Binding affinity against dopamine D2 receptor
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

D(2) dopamine receptor (CHEMBL339)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Pyridobenzoxazepine and pyridobenzothiazepine derivatives as potential central nervous system agents: synthesis and neurochemical study.
Liégeois JF, Rogister FA, Bruhwyler J, Damas J, Nguyen TP, Inarejos MO, Chleide EM, Mercier MG, Delarge JE.
J Med Chem (1994) 37 : 519 -525
PubMed 7907148 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 16 6.66 9.06

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL54 HALOPERIDOL 4.0 1 9.06
CHEMBL71 CHLORPROMAZINE 4.0 1 8.70
CHEMBL304902 CLOTHIAPINE 2.0 1 8.35
CHEMBL415300 ISOCLOZAPINE 1 7.90
CHEMBL67284 ISOCLOTHIAPINE 1 7.52
CHEMBL42 CLOZAPINE 4.0 1 7.34
CHEMBL63756 FLUPERLAPINE 2.0 1 6.88
CHEMBL433744 1 6.58
CHEMBL149240 1 6.44
CHEMBL147463 1 5.92
CHEMBL151809 1 5.91
CHEMBL151263 1 5.64
CHEMBL356076 1 5.39
CHEMBL435441 1 5.18
CHEMBL149108 1 4.96
CHEMBL146741 1 4.83

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL54 HALOPERIDOL Ki = 0.871 nM 9.06
CHEMBL71 CHLORPROMAZINE Ki = 1.995 nM 8.70
CHEMBL304902 CLOTHIAPINE Ki = 4.467 nM 8.35
CHEMBL415300 ISOCLOZAPINE Ki = 12.59 nM 7.90
CHEMBL67284 ISOCLOTHIAPINE Ki = 30.2 nM 7.52
CHEMBL42 CLOZAPINE Ki = 45.71 nM 7.34
CHEMBL63756 FLUPERLAPINE Ki = 131.83 nM 6.88
CHEMBL433744 Ki = 263.03 nM 6.58
CHEMBL149240 Ki = 363.08 nM 6.44
CHEMBL147463 Ki = 1202.26 nM 5.92
CHEMBL151809 Ki = 1230.27 nM 5.91
CHEMBL151263 Ki = 2290.87 nM 5.64
CHEMBL356076 Ki = 4073.8 nM 5.39
CHEMBL435441 Ki = 6606.93 nM 5.18
CHEMBL149108 Ki = 10964.78 nM 4.96
CHEMBL146741 Ki = 14791.08 nM 4.83