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Assay Detail

CHEMBL951050

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

Functional
Agonist activity at rat dopamine D4.2 receptor expressed in CHO10001A cells assessed as incorporation of [3H]thymidine
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Synthesis, radiofluorination, and in vitro evaluation of pyrazolo[1,5-a]pyridine-based dopamine D4 receptor ligands: discovery of an inverse agonist radioligand for PET.
Prante O, Tietze R, Hocke C, Löber S, Hübner H, Kuwert T, Gmeiner P.
J Med Chem (2008) 51 : 1800 -1810
PubMed 18307287 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 7 8.33 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL405260 1 9.10
CHEMBL411437 1 9.00
CHEMBL240773 QUINPIROLE 2.0 1 8.15
CHEMBL272853 1 8.04
CHEMBL7927 FAUC 113 1 7.92
CHEMBL272873 1 7.75
CHEMBL310843 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL405260 EC50 = 0.8 nM 9.10
CHEMBL411437 EC50 = 1.0 nM 9.00
CHEMBL240773 QUINPIROLE EC50 = 7.1 nM 8.15
CHEMBL272853 EC50 = 9.1 nM 8.04
CHEMBL7927 FAUC 113 EC50 = 12.0 nM 7.92
CHEMBL272873 EC50 = 18.0 nM 7.75
CHEMBL310843 EC50 - -