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Assay Detail

CHEMBL830303

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

Binding
Binding affinity against human Dopamine receptor D2
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

D(2) dopamine receptor (CHEMBL217)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

4-Fluorosulfonylpiperidines: selective 5-HT2A ligands for the treatment of insomnia.
Fish LR, Gilligan MT, Humphries AC, Ivarsson M, Ladduwahetty T, Merchant KJ, O'Connor D, Patel S, Philipps E, Vargas HM, Hutson PH, MacLeod AM.
Bioorg Med Chem Lett (2005) 15 : 3665 -3669
PubMed 15993598 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 6.14 6.58

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL177416 1 6.58
CHEMBL175832 1 6.50
CHEMBL177401 1 6.10
CHEMBL368816 1 6.06
CHEMBL74355 VOLINANSERIN 3.0 1 5.89
CHEMBL176109 1 5.70
CHEMBL175586 1 -
CHEMBL145939 1 -
CHEMBL358075 1 -
CHEMBL177807 1 -
CHEMBL178055 1 -
CHEMBL174049 1 -
CHEMBL175544 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL177416 Ki = 266.0 nM 6.58
CHEMBL175832 Ki = 313.0 nM 6.50
CHEMBL177401 Ki = 791.0 nM 6.10
CHEMBL368816 Ki = 863.0 nM 6.06
CHEMBL74355 VOLINANSERIN Ki = 1300.0 nM 5.89
CHEMBL176109 Ki = 2000.0 nM 5.70
CHEMBL175586 Ki > 1000.0 nM -
CHEMBL145939 Ki > 1500.0 nM -
CHEMBL358075 Ki > 1500.0 nM -
CHEMBL177807 Ki > 1500.0 nM -
CHEMBL178055 Ki > 2000.0 nM -
CHEMBL174049 Ki > 2000.0 nM -
CHEMBL175544 Ki > 1000.0 nM -