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Assay Detail

CHEMBL676299

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Binding
Tested for binding affinity against dopamine receptor D3 expressed in Sf9 cells.
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type Sf9
Confidence 8 — Homologous single protein target
Curated By Expert

Target

D(3) dopamine receptor (CHEMBL3138)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis of (R,S)-2'-trans-7-hydroxy-2-[N-n-propyl-N-(3'-iodo-2'- propenyl)-amino]tetralin (trans-7-OH-PIPAT): a new D3 dopamine receptor ligand.
Foulon C, Kung MP, Kung HF.
J Med Chem (1993) 36 : 1499 -1500
PubMed 8098771 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 7.27 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL110239 1 9.00
CHEMBL285755 1 8.93
CHEMBL6066838 1 8.41
CHEMBL240773 QUINPIROLE 2.0 1 8.25
CHEMBL8809 RACLOPRIDE 2.0 1 8.03
CHEMBL54 HALOPERIDOL 4.0 1 7.84
CHEMBL59 DOPAMINE 4.0 1 7.31
CHEMBL25554 1 6.97
CHEMBL56 8-OH-DPAT 1 6.61
CHEMBL62 SCH-23390 1 6.12
CHEMBL6437 MIANSERIN 4.0 1 5.82
CHEMBL39 SEROTONIN 3.0 1 5.63
CHEMBL15245 YOHIMBINE 3.0 1 5.61
CHEMBL80 NALOXONE 4.0 1 -
CHEMBL27 PROPRANOLOL 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL110239 Ki = 0.99 nM 9.00
CHEMBL285755 Ki = 1.18 nM 8.93
CHEMBL6066838 Ki = 3.91 nM 8.41
CHEMBL240773 QUINPIROLE Ki = 5.65 nM 8.25
CHEMBL8809 RACLOPRIDE Ki = 9.25 nM 8.03
CHEMBL54 HALOPERIDOL Ki = 14.3 nM 7.84
CHEMBL59 DOPAMINE Ki = 49.3 nM 7.31
CHEMBL25554 Ki = 107.0 nM 6.97
CHEMBL56 8-OH-DPAT Ki = 248.0 nM 6.61
CHEMBL62 SCH-23390 Ki = 768.0 nM 6.12
CHEMBL6437 MIANSERIN Ki = 1524.0 nM 5.82
CHEMBL39 SEROTONIN Ki = 2338.0 nM 5.63
CHEMBL15245 YOHIMBINE Ki = 2430.0 nM 5.61
CHEMBL80 NALOXONE Ki > 20000.0 nM -
CHEMBL27 PROPRANOLOL Ki > 5000.0 nM -