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Assay Detail

CHEMBL925953

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

Binding
Displacement of [N-methyl-3H]scopolamine from human recombinant muscarinic receptor M1 expressed in CHO cell membrane
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

3,5-Dihydro-imidazo[4,5-d]pyridazin-4-ones: a class of potent DPP-4 inhibitors.
Eckhardt M, Hauel N, Himmelsbach F, Langkopf E, Nar H, Mark M, Tadayyon M, Thomas L, Guth B, Lotz R.
Bioorg Med Chem Lett (2008) 18 : 3158 -3162
PubMed 18485703 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 5.97 7.03

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL256121 1 7.03
CHEMBL404220 1 6.06
CHEMBL257999 1 6.02
CHEMBL403553 1 5.92
CHEMBL401971 1 5.55
CHEMBL256729 1 5.25
CHEMBL403408 1 -
CHEMBL257376 1 -
CHEMBL401502 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL256121 IC50 = 93.0 nM 7.03
CHEMBL404220 IC50 = 862.0 nM 6.06
CHEMBL257999 IC50 = 954.0 nM 6.02
CHEMBL403553 IC50 = 1190.0 nM 5.92
CHEMBL401971 IC50 = 2804.0 nM 5.55
CHEMBL256729 IC50 = 5607.0 nM 5.25
CHEMBL403408 IC50 > 5000.0 nM -
CHEMBL257376 IC50 > 5000.0 nM -
CHEMBL401502 IC50 > 5000.0 nM -