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Assay Detail

CHEMBL4032443

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

Binding
Displacement of [3H]8-OH-DPAT from human 5-HT1A receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting method
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

5-hydroxytryptamine receptor 1A (CHEMBL214)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Highly Selective Dopamine D3 Receptor Antagonists with Arylated Diazaspiro Alkane Cores.
Reilly SW, Griffin S, Taylor M, Sahlholm K, Weng CC, Xu K, Jacome DA, Luedtke RR, Mach RH.
J Med Chem (2017) 60 : 9905 -9910
PubMed 29125762 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 7.02 9.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4083252 1 9.66
CHEMBL4073927 1 6.23
CHEMBL4062553 1 6.14
CHEMBL4084262 1 6.03

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4083252 Ki = 0.22 nM 9.66
CHEMBL4073927 Ki = 587.0 nM 6.23
CHEMBL4062553 Ki = 724.0 nM 6.14
CHEMBL4084262 Ki = 931.0 nM 6.03