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Assay Detail

CHEMBL617416

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

Binding
Binding affinity towards 5-hydroxytryptamine 2 receptor
17
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Serotonin 2 (5-HT2) receptor (CHEMBL2093870)
Type PROTEIN FAMILY
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 17 7.40 8.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL54 HALOPERIDOL 4.0 1 8.38
CHEMBL1743803 3 8.19
CHEMBL1743798 1 8.13
CHEMBL415 CLOMIPRAMINE 4.0 1 8.08
CHEMBL62 SCH-23390 1 7.89
CHEMBL11 IMIPRAMINE 4.0 1 7.64
CHEMBL287620 1 7.54
CHEMBL1743811 1 7.54
CHEMBL287257 DICLOFENSINE 2.0 1 7.43
CHEMBL1743790 1 7.31
CHEMBL34990 3 6.85
CHEMBL286849 1 6.22
CHEMBL41 FLUOXETINE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL54 HALOPERIDOL Ki = 4.2 nM 8.38
CHEMBL1743803 Ki = 6.4 nM 8.19
CHEMBL1743798 Ki = 7.4 nM 8.13
CHEMBL415 CLOMIPRAMINE Ki = 8.3 nM 8.08
CHEMBL1743803 Ki = 8.6 nM 8.07
CHEMBL62 SCH-23390 Ki = 13.0 nM 7.89
CHEMBL11 IMIPRAMINE Ki = 23.0 nM 7.64
CHEMBL1743811 Ki = 29.0 nM 7.54
CHEMBL287620 Ki = 29.0 nM 7.54
CHEMBL287257 DICLOFENSINE Ki = 37.0 nM 7.43
CHEMBL1743790 Ki = 49.0 nM 7.31
CHEMBL34990 Ki = 142.0 nM 6.85
CHEMBL34990 Ki = 208.0 nM 6.68
CHEMBL1743803 Ki = 406.0 nM 6.39
CHEMBL286849 Ki = 602.0 nM 6.22
CHEMBL34990 Ki = 939.0 nM 6.03
CHEMBL41 FLUOXETINE Ki > 1000.0 nM -