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Assay Detail

CHEMBL671444

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

Binding
In vitro ability to displace [3H]pramipexole from high affinity binding sites of bovine cloned D2 receptors stably expressed in CHO cells.
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

D(2) dopamine receptor (CHEMBL3998)
Type SINGLE PROTEIN
Organism Bos taurus

Publication

Dopaminergic 7-aminotetrahydroindolizines: ex-chiral pool synthesis and preferential D3 receptor binding.
Lehmann T, Hübner H, Gmeiner P.
Bioorg Med Chem Lett (2001) 11 : 2863 -2866
PubMed 11597417 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 18 6.32 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL301559 1 8.30
CHEMBL316983 1 7.68
CHEMBL95230 1 7.06
CHEMBL318924 1 6.82
CHEMBL96958 1 6.82
CHEMBL95618 1 6.70
CHEMBL97283 1 6.42
CHEMBL97319 1 6.42
CHEMBL440143 1 6.37
CHEMBL98072 1 6.19
CHEMBL323557 1 6.10
CHEMBL97750 1 6.00
CHEMBL98071 1 6.00
CHEMBL98563 1 5.80
CHEMBL97436 1 5.77
CHEMBL99291 1 5.33
CHEMBL96998 1 5.10
CHEMBL97348 1 4.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL301559 Ki = 5.0 nM 8.30
CHEMBL316983 Ki = 21.0 nM 7.68
CHEMBL95230 Ki = 87.0 nM 7.06
CHEMBL318924 Ki = 150.0 nM 6.82
CHEMBL96958 Ki = 150.0 nM 6.82
CHEMBL95618 Ki = 200.0 nM 6.70
CHEMBL97283 Ki = 380.0 nM 6.42
CHEMBL97319 Ki = 380.0 nM 6.42
CHEMBL440143 Ki = 430.0 nM 6.37
CHEMBL98072 Ki = 640.0 nM 6.19
CHEMBL323557 Ki = 800.0 nM 6.10
CHEMBL97750 Ki = 1000.0 nM 6.00
CHEMBL98071 Ki = 1000.0 nM 6.00
CHEMBL98563 Ki = 1600.0 nM 5.80
CHEMBL97436 Ki = 1700.0 nM 5.77
CHEMBL99291 Ki = 4700.0 nM 5.33
CHEMBL96998 Ki = 8000.0 nM 5.10
CHEMBL97348 Ki = 13000.0 nM 4.89