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Assay Detail

CHEMBL672339

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

Binding
Binding affinity towards Dopamine receptor D2
8
Total Activities
8
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

Pyrroloisoquinoline antidepressants. 2. In-depth exploration of structure-activity relationships.
Maryanoff BE, McComsey DF, Gardocki JF, Shank RP, Costanzo MJ, Nortey SO, Schneider CR, Setler PE.
J Med Chem (1987) 30 : 1433 -1454
PubMed 3039136 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 6.68 9.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL54 HALOPERIDOL 4.0 1 9.12
CHEMBL415 CLOMIPRAMINE 4.0 1 7.25
CHEMBL1743798 1 6.62
CHEMBL1743804 1 6.40
CHEMBL1743803 1 6.38
CHEMBL35184 1 6.06
CHEMBL34990 1 5.99
CHEMBL286849 1 5.65

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL54 HALOPERIDOL Ki = 0.75 nM 9.12
CHEMBL415 CLOMIPRAMINE Ki = 56.0 nM 7.25
CHEMBL1743798 Ki = 241.0 nM 6.62
CHEMBL1743804 Ki = 400.0 nM 6.40
CHEMBL1743803 Ki = 415.0 nM 6.38
CHEMBL35184 Ki = 875.0 nM 6.06
CHEMBL34990 Ki = 1030.0 nM 5.99
CHEMBL286849 Ki = 2220.0 nM 5.65