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Assay Detail

CHEMBL4047798

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

Binding
Displacement of [3H]AF-DX 384 from recombinant human M1 receptor expressed in CHO cells
2
Total Activities
2
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

Muscarinic acetylcholine receptor M1 (CHEMBL216)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of selective 8-(piperidin-4-yloxy)quinoline sulfone and sulfonamide histamine H1 receptor antagonists for use in allergic rhinitis.
Procopiou PA, Ford AJ, Gore PM, Hancock AP, Hodgson ST, Holmes DS, Looker BE, Vile S, Clark KL, Saunders KA, Slack RJ, Watts CJ.
Bioorg Med Chem Lett (2017) 27 : 4914 -4919
PubMed 28958623 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 5.70 6.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4088036 1 6.20
CHEMBL639 AZELASTINE 4.0 1 5.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4088036 IC50 = 630.96 nM 6.20
CHEMBL639 AZELASTINE IC50 = 6309.57 nM 5.20