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Assay Detail

CHEMBL671731

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

Binding
In vitro binding affinity at human cloned dopamine receptor D2 (long) stably expressed in CHO cells by [3H]-Spiperone displacement.
17
Total Activities
17
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 (CHEMBL217)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Di- and trisubstituted pyrazolo[1,5-a]pyridine derivatives: synthesis, dopamine receptor binding and ligand efficacy.
Löber S, Aboul-Fadl T, Hübner H, Gmeiner P.
Bioorg Med Chem Lett (2002) 12 : 633 -636
PubMed 11844688 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 5.24 7.39

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL42 CLOZAPINE 4.0 1 7.39
CHEMBL160536 1 6.52
CHEMBL160266 1 6.19
CHEMBL160454 1 5.51
CHEMBL7927 FAUC 113 1 5.50
CHEMBL160952 1 5.43
CHEMBL423247 1 5.31
CHEMBL155913 1 5.27
CHEMBL346805 1 5.02
CHEMBL156369 1 4.89
CHEMBL160749 1 4.85
CHEMBL156198 1 4.82
CHEMBL156851 1 4.68
CHEMBL351550 1 4.55
CHEMBL345357 1 4.55
CHEMBL267014 L-745870 1 4.27
CHEMBL160396 1 4.25

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL42 CLOZAPINE Ki = 41.0 nM 7.39
CHEMBL160536 Ki = 300.0 nM 6.52
CHEMBL160266 Ki = 640.0 nM 6.19
CHEMBL160454 Ki = 3100.0 nM 5.51
CHEMBL7927 FAUC 113 Ki = 3200.0 nM 5.50
CHEMBL160952 Ki = 3700.0 nM 5.43
CHEMBL423247 Ki = 4900.0 nM 5.31
CHEMBL155913 Ki = 5400.0 nM 5.27
CHEMBL346805 Ki = 9500.0 nM 5.02
CHEMBL156369 Ki = 13000.0 nM 4.89
CHEMBL160749 Ki = 14000.0 nM 4.85
CHEMBL156198 Ki = 15000.0 nM 4.82
CHEMBL156851 Ki = 21000.0 nM 4.68
CHEMBL351550 Ki = 28000.0 nM 4.55
CHEMBL345357 Ki = 28000.0 nM 4.55
CHEMBL267014 L-745870 Ki = 54000.0 nM 4.27
CHEMBL160396 Ki = 56000.0 nM 4.25