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Assay Detail

CHEMBL4396178

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

Binding
Displacement of [3H]OH-DPAT from human recombinant 5-HT1A receptor measured after 60 mins by scintillation counter method
6
Total Activities
3
Compounds Tested
2
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

Multi-targeting protein-protein interaction inhibitors: Evolution of macrocyclic ligands with embedded carbohydrates (MECs) to improve selectivity.
Negi A, Reilly CO, Jarikote DV, Zhou J, Murphy PV.
Eur J Med Chem (2019) 176 : 292 -309
PubMed 31112891 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 7.54 9.74
IC50 3 7.34 9.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL56 8-OH-DPAT 2 9.74
CHEMBL4579120 2 6.51
CHEMBL4562303 2 6.38

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL56 8-OH-DPAT Ki = 0.18 nM 9.74
CHEMBL56 8-OH-DPAT IC50 = 0.28 nM 9.55
CHEMBL4579120 Ki = 310.0 nM 6.51
CHEMBL4562303 Ki = 420.0 nM 6.38
CHEMBL4579120 IC50 = 490.0 nM 6.31
CHEMBL4562303 IC50 = 680.0 nM 6.17