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Assay Detail

CHEMBL3376443

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Functional
Positive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assay
ChEMBL ↗
68
Total Activities
40
Compounds Tested
3
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Discovery and SAR of muscarinic receptor subtype 1 (M1) allosteric activators from a molecular libraries high throughput screen. Part 1: 2,5-dibenzyl-2H-pyrazolo[4,3-c]quinolin-3(5H)-ones as positive allosteric modulators.
Han C, Chatterjee A, Noetzel MJ, Panarese JD, Smith E, Chase P, Hodder P, Niswender C, Conn PJ, Lindsley CW, Stauffer SR.
Bioorg Med Chem Lett (2015) 25 : 384 -388
PubMed 25435150 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 54 6.16 9.22
pEC50 13 - -
IP 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3360954 — — 1 9.22
CHEMBL3360955 — — 1 8.92
CHEMBL3360956 — — 1 8.00
CHEMBL115581 — — 1 8.00
CHEMBL1556989 — — 1 6.33
CHEMBL3360938 — — 2 6.18
CHEMBL3360931 — — 2 6.11
CHEMBL3360947 — — 2 6.09
CHEMBL1083203 — — 1 6.08
CHEMBL3360927 — — 1 6.07
CHEMBL3360928 — — 2 6.00
CHEMBL3360950 — — 2 5.94
CHEMBL3360939 — — 2 5.85
CHEMBL3360946 — — 2 5.81
CHEMBL3360949 — — 2 5.71
CHEMBL3360940 — — 2 5.70
CHEMBL3360958 — — 1 5.61
CHEMBL3360945 — — 2 5.44
CHEMBL3360944 — — 2 5.42
CHEMBL3360935 — — 2 5.20
CHEMBL608112 — — 1 -
CHEMBL3360930 — — 2 -
CHEMBL3360929 — — 2 -
CHEMBL3360959 — — 1 -
CHEMBL86888 — — 2 -
CHEMBL89202 — — 2 -
CHEMBL3360957 — — 1 -
CHEMBL3360932 — — 2 -
CHEMBL3360933 — — 2 -
CHEMBL3360934 — — 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3360954 — EC50 = 0.6 nM 9.22
CHEMBL3360955 — EC50 = 1.2 nM 8.92
CHEMBL3360956 — EC50 = 10.0 nM 8.00
CHEMBL115581 — EC50 = 10.0 nM 8.00
CHEMBL1556989 — EC50 = 473.0 nM 6.33
CHEMBL3360938 — EC50 = 660.69 nM 6.18
CHEMBL3360938 — EC50 = 656.0 nM 6.18
CHEMBL3360931 — EC50 = 776.25 nM 6.11
CHEMBL3360931 — EC50 = 783.0 nM 6.11
CHEMBL3360947 — EC50 = 812.83 nM 6.09
CHEMBL3360947 — EC50 = 821.0 nM 6.09
CHEMBL1083203 — EC50 = 830.0 nM 6.08
CHEMBL3360927 — EC50 = 845.0 nM 6.07
CHEMBL3360928 — EC50 = 1010.0 nM 6.00
CHEMBL3360928 — EC50 = 1000.0 nM 6.00
CHEMBL3360950 — EC50 = 1148.15 nM 5.94
CHEMBL3360950 — EC50 = 1150.0 nM 5.94
CHEMBL3360939 — EC50 = 1412.54 nM 5.85
CHEMBL3360939 — EC50 = 1420.0 nM 5.85
CHEMBL3360946 — EC50 = 1550.0 nM 5.81
CHEMBL3360946 — EC50 = 1548.82 nM 5.81
CHEMBL3360949 — EC50 = 1949.84 nM 5.71
CHEMBL3360949 — EC50 = 1940.0 nM 5.71
CHEMBL3360940 — EC50 = 2020.0 nM 5.70
CHEMBL3360940 — EC50 = 2041.74 nM 5.69
CHEMBL3360958 — EC50 = 2430.0 nM 5.61
CHEMBL3360945 — EC50 = 3660.0 nM 5.44
CHEMBL3360945 — EC50 = 3630.78 nM 5.44
CHEMBL3360944 — EC50 = 3801.89 nM 5.42
CHEMBL3360944 — EC50 = 3790.0 nM 5.42
CHEMBL3360935 — EC50 = 6310.0 nM 5.20
CHEMBL3360935 — EC50 = 6309.57 nM 5.20
CHEMBL3360951 — EC50 - — -
CHEMBL3360952 — EC50 - — -
CHEMBL3360953 — EC50 - — -
CHEMBL1705277 — EC50 - — -
CHEMBL3360933 — EC50 - — -
CHEMBL3360929 — pEC50 - — -
CHEMBL3360932 — pEC50 - — -
CHEMBL3360933 — pEC50 - — -
CHEMBL86888 — pEC50 - — -
CHEMBL3360934 — EC50 > 10000.0 nM -
CHEMBL3360936 — EC50 > 10000.0 nM -
CHEMBL89202 — EC50 > 10000.0 nM -
CHEMBL3360930 — pEC50 - — -
CHEMBL608112 — IP = 845.0 nM -
CHEMBL3360957 — EC50 > 30000.0 nM -
CHEMBL3360959 — EC50 > 10.0 nM -
CHEMBL3360952 — pEC50 - — -
CHEMBL3360937 — pEC50 - — -