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Assay Detail

CHEMBL749203

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Binding
Binding affinity towards muscarinic receptor M2
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Muscarinic acetylcholine receptor M2 (CHEMBL211)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Piperazine-based CCR5 antagonists as HIV-1 inhibitors. III: synthesis, antiviral and pharmacokinetic profiles of symmetrical heteroaryl carboxamides.
McCombie SW, Tagat JR, Vice SF, Lin SI, Steensma R, Palani A, Neustadt BR, Baroudy BM, Strizki JM, Endres M, Cox K, Dan N, Chou CC.
Bioorg Med Chem Lett (2003) 13 : 567 -571
PubMed 12565973 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 6.30 7.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL357557 1 7.17
CHEMBL348667 1 6.79
CHEMBL422326 1 6.77
CHEMBL140706 1 6.70
CHEMBL322251 1 6.60
CHEMBL141699 1 6.59
CHEMBL334470 1 6.46
CHEMBL311795 1 6.24
CHEMBL337820 1 6.21
CHEMBL342137 1 6.01
CHEMBL140490 1 5.96
CHEMBL344607 1 5.91
CHEMBL138502 1 5.78
CHEMBL140827 1 5.69
CHEMBL113436 1 5.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL357557 Ki = 68.0 nM 7.17
CHEMBL348667 Ki = 164.0 nM 6.79
CHEMBL422326 Ki = 169.0 nM 6.77
CHEMBL140706 Ki = 202.0 nM 6.70
CHEMBL322251 Ki = 250.0 nM 6.60
CHEMBL141699 Ki = 255.0 nM 6.59
CHEMBL334470 Ki = 348.0 nM 6.46
CHEMBL311795 Ki = 575.0 nM 6.24
CHEMBL337820 Ki = 613.0 nM 6.21
CHEMBL342137 Ki = 985.0 nM 6.01
CHEMBL140490 Ki = 1100.0 nM 5.96
CHEMBL344607 Ki = 1225.0 nM 5.91
CHEMBL138502 Ki = 1678.0 nM 5.78
CHEMBL140827 Ki = 2031.0 nM 5.69
CHEMBL113436 Ki = 2500.0 nM 5.60