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Assay Detail

CHEMBL1034994

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

Binding
Displacement of [3H]spiroperidol from human cloned dopamine D2L receptor expressed in rat C6 cells
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type C6
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Structural modifications of N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinehexanamides: influence on lipophilicity and 5-HT7 receptor activity. Part III.
Leopoldo M, Lacivita E, De Giorgio P, Fracasso C, Guzzetti S, Caccia S, Contino M, Colabufo NA, Berardi F, Perrone R.
J Med Chem (2008) 51 : 5813 -5822
PubMed 18800769 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 25 7.23 8.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL492282 1 8.89
CHEMBL54 HALOPERIDOL 4.0 1 8.38
CHEMBL493909 1 8.28
CHEMBL494661 1 8.11
CHEMBL492872 1 8.04
CHEMBL494312 1 7.70
CHEMBL522343 1 7.68
CHEMBL492690 1 7.66
CHEMBL521687 1 7.52
CHEMBL492691 1 7.48
CHEMBL493305 1 7.40
CHEMBL495321 1 7.19
CHEMBL494119 1 7.19
CHEMBL522194 1 7.04
CHEMBL494118 1 7.03
CHEMBL523381 1 7.02
CHEMBL522691 1 6.85
CHEMBL494709 1 6.73
CHEMBL495120 1 6.65
CHEMBL494512 1 6.51
CHEMBL492480 1 6.44
CHEMBL492871 1 6.30
CHEMBL493709 1 6.30
CHEMBL494458 1 6.14
CHEMBL494316 1 6.14

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL492282 Ki = 1.3 nM 8.89
CHEMBL54 HALOPERIDOL Ki = 4.2 nM 8.38
CHEMBL493909 Ki = 5.3 nM 8.28
CHEMBL494661 Ki = 7.8 nM 8.11
CHEMBL492872 Ki = 9.2 nM 8.04
CHEMBL494312 Ki = 20.0 nM 7.70
CHEMBL522343 Ki = 21.0 nM 7.68
CHEMBL492690 Ki = 22.0 nM 7.66
CHEMBL521687 Ki = 30.0 nM 7.52
CHEMBL492691 Ki = 33.0 nM 7.48
CHEMBL493305 Ki = 40.0 nM 7.40
CHEMBL495321 Ki = 64.0 nM 7.19
CHEMBL494119 Ki = 65.0 nM 7.19
CHEMBL522194 Ki = 91.0 nM 7.04
CHEMBL494118 Ki = 93.0 nM 7.03
CHEMBL523381 Ki = 96.0 nM 7.02
CHEMBL522691 Ki = 142.0 nM 6.85
CHEMBL494709 Ki = 185.0 nM 6.73
CHEMBL495120 Ki = 226.0 nM 6.65
CHEMBL494512 Ki = 311.0 nM 6.51
CHEMBL492480 Ki = 362.0 nM 6.44
CHEMBL492871 Ki = 503.0 nM 6.30
CHEMBL493709 Ki = 501.0 nM 6.30
CHEMBL494458 Ki = 723.0 nM 6.14
CHEMBL494316 Ki = 730.0 nM 6.14