Ligand source activities (1 row/activity)





Ligands (move mouse cursor over ligand name to see structure) Receptor Activity Chemical information
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DOI

10952349 35131 None 0 Human Functional pEC50 = 9.2 9.2 3467 2
Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.
ChEMBL 564 15 0 10 6.8 CN1CCC=C(c2nsnc2SCCCCCCCCCCSc2nsnc2C2=CCCN(C)C2)C1 10.1021/jm0102405
CHEMBL143434 35131 None 0 Human Functional pEC50 = 9.2 9.2 3467 2
Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.
ChEMBL 564 15 0 10 6.8 CN1CCC=C(c2nsnc2SCCCCCCCCCCSc2nsnc2C2=CCCN(C)C2)C1 10.1021/jm0102405
11072401 30776 None 0 Human Functional pEC50 = 9 9.0 12882 2
Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.
ChEMBL 592 17 0 10 7.6 CN1CCC=C(c2nsnc2SCCCCCCCCCCCCSc2nsnc2C2=CCCN(C)C2)C1 10.1021/jm0102405
CHEMBL139603 30776 None 0 Human Functional pEC50 = 9 9.0 12882 2
Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.
ChEMBL 592 17 0 10 7.6 CN1CCC=C(c2nsnc2SCCCCCCCCCCCCSc2nsnc2C2=CCCN(C)C2)C1 10.1021/jm0102405
9937709 34095 None 0 Human Functional pEC50 = 8.9 8.9 239 2
Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.
ChEMBL 560 17 0 10 6.2 CN1CCC=C(c2nsnc2OCCCCCCCCCCCCOc2nsnc2C2=CCCN(C)C2)C1 10.1021/jm0102405
CHEMBL142538 34095 None 0 Human Functional pEC50 = 8.9 8.9 239 2
Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.
ChEMBL 560 17 0 10 6.2 CN1CCC=C(c2nsnc2OCCCCCCCCCCCCOc2nsnc2C2=CCCN(C)C2)C1 10.1021/jm0102405
187 255 None 39 Human Functional pEC50 = 8 8.0 1 8
Agonist activity at human muscarinic M4 receptor expressed in BHK-21 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in BHK-21 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm100697g
294 255 None 39 Human Functional pEC50 = 8 8.0 1 8
Agonist activity at human muscarinic M4 receptor expressed in BHK-21 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in BHK-21 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm100697g
65 255 None 39 Human Functional pEC50 = 8 8.0 1 8
Agonist activity at human muscarinic M4 receptor expressed in BHK-21 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in BHK-21 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm100697g
8593 255 None 39 Human Functional pEC50 = 8 8.0 1 8
Agonist activity at human muscarinic M4 receptor expressed in BHK-21 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in BHK-21 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm100697g
CHEMBL667 255 None 39 Human Functional pEC50 = 8 8.0 1 8
Agonist activity at human muscarinic M4 receptor expressed in BHK-21 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in BHK-21 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm100697g
DB03128 255 None 39 Human Functional pEC50 = 8 8.0 1 8
Agonist activity at human muscarinic M4 receptor expressed in BHK-21 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in BHK-21 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm100697g
187 255 None 39 Human Functional pEC50 = 8 8.0 1 8
Agonist activity at muscarinic human M4 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at muscarinic human M4 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2012.05.048
294 255 None 39 Human Functional pEC50 = 8 8.0 1 8
Agonist activity at muscarinic human M4 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at muscarinic human M4 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2012.05.048
65 255 None 39 Human Functional pEC50 = 8 8.0 1 8
Agonist activity at muscarinic human M4 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at muscarinic human M4 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2012.05.048
8593 255 None 39 Human Functional pEC50 = 8 8.0 1 8
Agonist activity at muscarinic human M4 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at muscarinic human M4 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2012.05.048
CHEMBL667 255 None 39 Human Functional pEC50 = 8 8.0 1 8
Agonist activity at muscarinic human M4 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at muscarinic human M4 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2012.05.048
DB03128 255 None 39 Human Functional pEC50 = 8 8.0 1 8
Agonist activity at muscarinic human M4 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at muscarinic human M4 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2012.05.048
162665337 182274 None 0 Human Functional pEC50 = 8 8.0 - 1
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 358 2 2 5 3.1 Cc1c(Cl)nnc2sc(C(=O)NC3Cc4ccccc4C3)c(N)c12 10.1016/j.bmcl.2019.05.026
CHEMBL4783881 182274 None 0 Human Functional pEC50 = 8 8.0 - 1
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 358 2 2 5 3.1 Cc1c(Cl)nnc2sc(C(=O)NC3Cc4ccccc4C3)c(N)c12 10.1016/j.bmcl.2019.05.026
162675795 183414 None 0 Human Functional pEC50 = 8 8.0 - 1
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 438 4 2 8 2.9 COc1cc(N2CC(NC(=O)c3sc4nnc(Cl)c(C)c4c3N)C2)c(Cl)cn1 10.1016/j.bmcl.2019.05.026
CHEMBL4798497 183414 None 0 Human Functional pEC50 = 8 8.0 - 1
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 438 4 2 8 2.9 COc1cc(N2CC(NC(=O)c3sc4nnc(Cl)c(C)c4c3N)C2)c(Cl)cn1 10.1016/j.bmcl.2019.05.026
137643460 158265 None 0 Human Functional pEC50 = 8.0 8.0 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 390 3 2 7 2.2 Cc1nnc2sc(C(=O)NC3CN(c4cc(F)nc(F)c4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4088704 158265 None 0 Human Functional pEC50 = 8.0 8.0 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 390 3 2 7 2.2 Cc1nnc2sc(C(=O)NC3CN(c4cc(F)nc(F)c4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
42598358 16100 None 0 Human Functional pEC50 = 7 7.0 -100 5
Agonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 390 4 0 5 4.4 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4cc(F)c(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223860 16100 None 0 Human Functional pEC50 = 7 7.0 -100 5
Agonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 390 4 0 5 4.4 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4cc(F)c(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
137656230 159044 None 0 Human Functional pEC50 = 7 7.0 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 390 4 2 7 3.3 Cc1nnc2sc(C(=O)NCc3ccc(-c4cnccn4)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
CHEMBL4096878 159044 None 0 Human Functional pEC50 = 7 7.0 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 390 4 2 7 3.3 Cc1nnc2sc(C(=O)NCc3ccc(-c4cnccn4)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
162651352 180307 None 0 Human Functional pEC50 = 7 7.0 - 1
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 437 3 2 8 2.9 Cc1nc(Cl)c(C)c(N2CC(NC(=O)c3sc4nnc(Cl)c(C)c4c3N)C2)n1 10.1016/j.bmcl.2019.05.026
CHEMBL4751034 180307 None 0 Human Functional pEC50 = 7 7.0 - 1
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 437 3 2 8 2.9 Cc1nc(Cl)c(C)c(N2CC(NC(=O)c3sc4nnc(Cl)c(C)c4c3N)C2)n1 10.1016/j.bmcl.2019.05.026
89445242 174656 None 0 Human Functional pEC50 = 6 6.0 - 1
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 308 3 2 4 4.4 Cc1cc(C)c2c(n1)sc1c(NCc3ccccc3)n[nH]c12 10.1016/j.bmcl.2018.12.039
CHEMBL4558571 174656 None 0 Human Functional pEC50 = 6 6.0 - 1
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 308 3 2 4 4.4 Cc1cc(C)c2c(n1)sc1c(NCc3ccccc3)n[nH]c12 10.1016/j.bmcl.2018.12.039
155518224 170269 None 0 Human Functional pEC50 = 5 5.0 - 1
Positive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as as increase in acteylcholine-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol/acetylcholine by Glosensor cAMP reagent/plate reader based luminescence assayPositive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as as increase in acteylcholine-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol/acetylcholine by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 366 4 0 5 3.7 COc1cccnc1C1CCN(C2CCCN(c3cccnc3)CC2)CC1 10.1021/acsmedchemlett.9b00106
CHEMBL4446144 170269 None 0 Human Functional pEC50 = 5 5.0 - 1
Positive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as as increase in acteylcholine-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol/acetylcholine by Glosensor cAMP reagent/plate reader based luminescence assayPositive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as as increase in acteylcholine-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol/acetylcholine by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 366 4 0 5 3.7 COc1cccnc1C1CCN(C2CCCN(c3cccnc3)CC2)CC1 10.1021/acsmedchemlett.9b00106
155510640 174032 None 0 Human Functional pEC50 = 7.0 7.0 1 2
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 283 2 1 5 3.1 Cc1nnc2sc(C(=O)c3ccccc3)c(N)c2c1C 10.1016/j.bmcl.2016.07.042
CHEMBL4543522 174032 None 0 Human Functional pEC50 = 7.0 7.0 1 2
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 283 2 1 5 3.1 Cc1nnc2sc(C(=O)c3ccccc3)c(N)c2c1C 10.1016/j.bmcl.2016.07.042
155510640 174032 None 0 Human Functional pEC50 = 7.0 7.0 1 2
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 283 2 1 5 3.1 Cc1nnc2sc(C(=O)c3ccccc3)c(N)c2c1C 10.1016/j.bmcl.2016.07.042
CHEMBL4543522 174032 None 0 Human Functional pEC50 = 7.0 7.0 1 2
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 283 2 1 5 3.1 Cc1nnc2sc(C(=O)c3ccccc3)c(N)c2c1C 10.1016/j.bmcl.2016.07.042
137641943 158476 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 354 3 2 7 1.9 Cc1nnc2sc(C(=O)NC3CN(c4ccccn4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4090871 158476 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 354 3 2 7 1.9 Cc1nnc2sc(C(=O)NC3CN(c4ccccn4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
89777104 159121 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 389 4 2 6 3.9 Cc1nnc2sc(C(=O)NCc3ccc(-c4cccnc4)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
CHEMBL4097819 159121 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 389 4 2 6 3.9 Cc1nnc2sc(C(=O)NCc3ccc(-c4cccnc4)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
53382504 86329 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 359 3 2 4 4.4 Cc1ccc(CNC(=O)c2sc3nc(C)c(Cl)c(C)c3c2N)cc1 10.1016/j.bmcl.2012.10.073
CHEMBL2313395 86329 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 359 3 2 4 4.4 Cc1ccc(CNC(=O)c2sc3nc(C)c(Cl)c(C)c3c2N)cc1 10.1016/j.bmcl.2012.10.073
155539719 172871 None 0 Human Functional pEC50 = 7.0 7.0 3 2
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 284 2 1 6 2.5 Cc1nnc2sc(C(=O)c3cccnc3)c(N)c2c1C 10.1016/j.bmcl.2016.07.042
CHEMBL4515326 172871 None 0 Human Functional pEC50 = 7.0 7.0 3 2
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 284 2 1 6 2.5 Cc1nnc2sc(C(=O)c3cccnc3)c(N)c2c1C 10.1016/j.bmcl.2016.07.042
155564640 175513 None 0 Human Functional pEC50 = 7.0 7.0 3 2
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 317 2 1 5 3.8 Cc1nc2sc(C(=O)c3cccnc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2016.07.042
CHEMBL4577985 175513 None 0 Human Functional pEC50 = 7.0 7.0 3 2
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 317 2 1 5 3.8 Cc1nc2sc(C(=O)c3cccnc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2016.07.042
53382504 86329 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 359 3 2 4 4.4 Cc1ccc(CNC(=O)c2sc3nc(C)c(Cl)c(C)c3c2N)cc1 10.1016/j.bmcl.2012.10.073
CHEMBL2313395 86329 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 359 3 2 4 4.4 Cc1ccc(CNC(=O)c2sc3nc(C)c(Cl)c(C)c3c2N)cc1 10.1016/j.bmcl.2012.10.073
89768734 164707 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 354 2 2 6 2.2 Cc1nnc2sc(C(=O)N3CC(O)(c4ccccc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
CHEMBL4217300 164707 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 354 2 2 6 2.2 Cc1nnc2sc(C(=O)N3CC(O)(c4ccccc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
137645408 157907 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 436 5 1 5 3.9 COc1ccc(CNC(=O)C2CCN(c3c(C#N)cnc4ccc(F)cc34)CC2)cc1F 10.1016/j.bmcl.2017.08.043
CHEMBL4084306 157907 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 436 5 1 5 3.9 COc1ccc(CNC(=O)C2CCN(c3c(C#N)cnc4ccc(F)cc34)CC2)cc1F 10.1016/j.bmcl.2017.08.043
89768734 164707 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 354 2 2 6 2.2 Cc1nnc2sc(C(=O)N3CC(O)(c4ccccc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
CHEMBL4217300 164707 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 354 2 2 6 2.2 Cc1nnc2sc(C(=O)N3CC(O)(c4ccccc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
127043639 140506 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 337 3 0 6 3.1 Cc1ccc(OC2CCN(c3nc(C)nn4ccc(C)c34)CC2)cn1 10.1016/j.bmcl.2016.05.010
CHEMBL3810071 140506 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 337 3 0 6 3.1 Cc1ccc(OC2CCN(c3nc(C)nn4ccc(C)c34)CC2)cn1 10.1016/j.bmcl.2016.05.010
155539719 172871 None 0 Human Functional pEC50 = 7.0 7.0 3 2
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 284 2 1 6 2.5 Cc1nnc2sc(C(=O)c3cccnc3)c(N)c2c1C 10.1016/j.bmcl.2016.07.042
CHEMBL4515326 172871 None 0 Human Functional pEC50 = 7.0 7.0 3 2
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 284 2 1 6 2.5 Cc1nnc2sc(C(=O)c3cccnc3)c(N)c2c1C 10.1016/j.bmcl.2016.07.042
155564640 175513 None 0 Human Functional pEC50 = 7.0 7.0 3 2
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 317 2 1 5 3.8 Cc1nc2sc(C(=O)c3cccnc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2016.07.042
CHEMBL4577985 175513 None 0 Human Functional pEC50 = 7.0 7.0 3 2
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 317 2 1 5 3.8 Cc1nc2sc(C(=O)c3cccnc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2016.07.042
137635723 156081 None 0 Human Functional pEC50 = 7.0 7.0 2 2
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 411 3 2 9 2.5 Cc1nnc2sc(C(=O)NC3CN(c4nc5cccnc5s4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4062934 156081 None 0 Human Functional pEC50 = 7.0 7.0 2 2
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 411 3 2 9 2.5 Cc1nnc2sc(C(=O)NC3CN(c4nc5cccnc5s4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
5441 2424 None 10 Human Functional pEC50 = 6.0 6.0 -46 3
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 507 6 2 3 6.1 O[C@@H]1Cc2c([C@H]1NC(=O)c1ccc(cc1)c1ccccc1)cc(cc2)N=C(N(Cc1ccc(cc1)F)C)C 10.1016/j.bmcl.2015.08.011
9893054 2424 None 10 Human Functional pEC50 = 6.0 6.0 -46 3
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 507 6 2 3 6.1 O[C@@H]1Cc2c([C@H]1NC(=O)c1ccc(cc1)c1ccccc1)cc(cc2)N=C(N(Cc1ccc(cc1)F)C)C 10.1016/j.bmcl.2015.08.011
CHEMBL3616501 2424 None 10 Human Functional pEC50 = 6.0 6.0 -46 3
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 507 6 2 3 6.1 O[C@@H]1Cc2c([C@H]1NC(=O)c1ccc(cc1)c1ccccc1)cc(cc2)N=C(N(Cc1ccc(cc1)F)C)C 10.1016/j.bmcl.2015.08.011
135126271 164183 None 0 Rat Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 412 5 1 5 3.8 Cc1cc(N2CC(NC(=O)c3ccc4nc(C)cc(C)c4c3)C2)cc(OC(F)F)n1 10.1016/j.bmcl.2017.10.016
CHEMBL4210668 164183 None 0 Rat Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 412 5 1 5 3.8 Cc1cc(N2CC(NC(=O)c3ccc4nc(C)cc(C)c4c3)C2)cc(OC(F)F)n1 10.1016/j.bmcl.2017.10.016
53382512 86309 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 375 4 2 5 4.1 COc1ccc(CNC(=O)c2sc3nc(C)c(Cl)c(C)c3c2N)cc1 10.1016/j.bmcl.2012.10.073
CHEMBL2313375 86309 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 375 4 2 5 4.1 COc1ccc(CNC(=O)c2sc3nc(C)c(Cl)c(C)c3c2N)cc1 10.1016/j.bmcl.2012.10.073
53382512 86309 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 375 4 2 5 4.1 COc1ccc(CNC(=O)c2sc3nc(C)c(Cl)c(C)c3c2N)cc1 10.1016/j.bmcl.2012.10.073
CHEMBL2313375 86309 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 375 4 2 5 4.1 COc1ccc(CNC(=O)c2sc3nc(C)c(Cl)c(C)c3c2N)cc1 10.1016/j.bmcl.2012.10.073
53382528 86326 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 345 3 2 4 4.1 Cc1nc2sc(C(=O)NCc3ccccc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313392 86326 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 345 3 2 4 4.1 Cc1nc2sc(C(=O)NCc3ccccc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
145977993 163566 None 0 Rat Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 373 4 1 5 3.1 Cc1cc(C)c2cc(C(=O)NC3CN(c4cnc(C5CC5)cn4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
CHEMBL4203172 163566 None 0 Rat Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 373 4 1 5 3.1 Cc1cc(C)c2cc(C(=O)NC3CN(c4cnc(C5CC5)cn4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
145977993 163566 None 0 Rat Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 373 4 1 5 3.1 Cc1cc(C)c2cc(C(=O)NC3CN(c4cnc(C5CC5)cn4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
CHEMBL4203172 163566 None 0 Rat Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 373 4 1 5 3.1 Cc1cc(C)c2cc(C(=O)NC3CN(c4cnc(C5CC5)cn4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
135126271 164183 None 0 Rat Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 412 5 1 5 3.8 Cc1cc(N2CC(NC(=O)c3ccc4nc(C)cc(C)c4c3)C2)cc(OC(F)F)n1 10.1016/j.bmcl.2017.10.016
CHEMBL4210668 164183 None 0 Rat Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 412 5 1 5 3.8 Cc1cc(N2CC(NC(=O)c3ccc4nc(C)cc(C)c4c3)C2)cc(OC(F)F)n1 10.1016/j.bmcl.2017.10.016
145966725 164332 None 0 Rat Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 400 3 1 4 3.9 Cc1cc(C)c2cc(C(=O)NC3CN(c4ccc(C(F)(F)F)cn4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
CHEMBL4212499 164332 None 0 Rat Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 400 3 1 4 3.9 Cc1cc(C)c2cc(C(=O)NC3CN(c4ccc(C(F)(F)F)cn4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
53382528 86326 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 345 3 2 4 4.1 Cc1nc2sc(C(=O)NCc3ccccc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313392 86326 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 345 3 2 4 4.1 Cc1nc2sc(C(=O)NCc3ccccc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
145966725 164332 None 0 Rat Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 400 3 1 4 3.9 Cc1cc(C)c2cc(C(=O)NC3CN(c4ccc(C(F)(F)F)cn4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
CHEMBL4212499 164332 None 0 Rat Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 400 3 1 4 3.9 Cc1cc(C)c2cc(C(=O)NC3CN(c4ccc(C(F)(F)F)cn4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
137645408 157907 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 436 5 1 5 3.9 COc1ccc(CNC(=O)C2CCN(c3c(C#N)cnc4ccc(F)cc34)CC2)cc1F 10.1016/j.bmcl.2017.08.043
CHEMBL4084306 157907 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 436 5 1 5 3.9 COc1ccc(CNC(=O)C2CCN(c3c(C#N)cnc4ccc(F)cc34)CC2)cc1F 10.1016/j.bmcl.2017.08.043
145970522 164802 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 352 2 1 5 3.4 Cc1ccc(C2CN(C(=O)c3sc4nnc(C)c(C)c4c3N)C2)cc1 10.1016/j.bmcl.2017.10.053
CHEMBL4218472 164802 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 352 2 1 5 3.4 Cc1ccc(C2CN(C(=O)c3sc4nnc(C)c(C)c4c3N)C2)cc1 10.1016/j.bmcl.2017.10.053
145970522 164802 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 352 2 1 5 3.4 Cc1ccc(C2CN(C(=O)c3sc4nnc(C)c(C)c4c3N)C2)cc1 10.1016/j.bmcl.2017.10.053
CHEMBL4218472 164802 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 352 2 1 5 3.4 Cc1ccc(C2CN(C(=O)c3sc4nnc(C)c(C)c4c3N)C2)cc1 10.1016/j.bmcl.2017.10.053
78319052 171339 None 0 Human Functional pEC50 = 8.0 8.0 229 2
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 361 4 0 5 3.3 CCOC(=O)N1CCCC(N2CCC(c3ncccc3OC)CC2)CC1 10.1021/acsmedchemlett.9b00106
CHEMBL4461438 171339 None 0 Human Functional pEC50 = 8.0 8.0 229 2
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 361 4 0 5 3.3 CCOC(=O)N1CCCC(N2CCC(c3ncccc3OC)CC2)CC1 10.1021/acsmedchemlett.9b00106
137643460 158265 None 0 Human Functional pEC50 = 8.0 8.0 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 390 3 2 7 2.2 Cc1nnc2sc(C(=O)NC3CN(c4cc(F)nc(F)c4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4088704 158265 None 0 Human Functional pEC50 = 8.0 8.0 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 390 3 2 7 2.2 Cc1nnc2sc(C(=O)NC3CN(c4cc(F)nc(F)c4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
89777143 153840 None 0 Rat Functional pEC50 = 8.0 8.0 5 2
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 358 4 2 6 3.5 CSc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1 10.1016/j.bmcl.2016.11.086
CHEMBL3982695 153840 None 0 Rat Functional pEC50 = 8.0 8.0 5 2
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 358 4 2 6 3.5 CSc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1 10.1016/j.bmcl.2016.11.086
89777143 153840 None 0 Rat Functional pEC50 = 8.0 8.0 5 2
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 358 4 2 6 3.5 CSc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1 10.1016/j.bmcl.2016.11.086
CHEMBL3982695 153840 None 0 Rat Functional pEC50 = 8.0 8.0 5 2
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 358 4 2 6 3.5 CSc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1 10.1016/j.bmcl.2016.11.086
89777151 158571 None 0 Rat Functional pEC50 = 7.9 7.9 7 2
Positive allosteric modulation of rat M4 receptor assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 407 4 2 6 4.0 Cc1nnc2sc(C(=O)NCc3ccc(-c4cccnc4F)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
CHEMBL4091821 158571 None 0 Rat Functional pEC50 = 7.9 7.9 7 2
Positive allosteric modulation of rat M4 receptor assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 407 4 2 6 4.0 Cc1nnc2sc(C(=O)NCc3ccc(-c4cccnc4F)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
134207697 174277 None 0 Human Functional pEC50 = 7.0 7.0 10 2
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 428 3 2 7 3.0 Cc1nc2cc(C)c3c(N)c(C(=O)NC4CN(c5ccc(F)c(F)c5)C4)sc3n2n1 10.1016/j.bmcl.2019.06.032
CHEMBL4549515 174277 None 0 Human Functional pEC50 = 7.0 7.0 10 2
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 428 3 2 7 3.0 Cc1nc2cc(C)c3c(N)c(C(=O)NC4CN(c5ccc(F)c(F)c5)C4)sc3n2n1 10.1016/j.bmcl.2019.06.032
134207701 174638 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 287 2 2 6 1.7 Cc1cc2nncn2c2sc(C(=O)NC3CC3)c(N)c12 10.1016/j.bmcl.2019.06.032
CHEMBL4558111 174638 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 287 2 2 6 1.7 Cc1cc2nncn2c2sc(C(=O)NC3CC3)c(N)c12 10.1016/j.bmcl.2019.06.032
9958728 35151 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.
ChEMBL 532 15 0 10 5.4 CN1CCC=C(c2nsnc2OCCCCCCCCCCOc2nsnc2C2=CCCN(C)C2)C1 10.1021/jm0102405
CHEMBL143468 35151 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.
ChEMBL 532 15 0 10 5.4 CN1CCC=C(c2nsnc2OCCCCCCCCCCOc2nsnc2C2=CCCN(C)C2)C1 10.1021/jm0102405
155552432 174166 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 373 4 0 7 3.2 COc1cccnc1C1CCN(C2CCCN(c3ncns3)CC2)CC1 10.1021/acsmedchemlett.9b00106
CHEMBL4547008 174166 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 373 4 0 7 3.2 COc1cccnc1C1CCN(C2CCCN(c3ncns3)CC2)CC1 10.1021/acsmedchemlett.9b00106
89445225 170933 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 326 3 2 4 4.5 Cc1cc(C)c2c(n1)sc1c(NCc3ccc(F)cc3)n[nH]c12 10.1016/j.bmcl.2018.12.039
CHEMBL4455343 170933 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 326 3 2 4 4.5 Cc1cc(C)c2c(n1)sc1c(NCc3ccc(F)cc3)n[nH]c12 10.1016/j.bmcl.2018.12.039
29262717 140476 None 6 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 344 2 0 5 3.1 Cc1sc2ncnc(N3CCC(C(=O)N4CCCC4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
CHEMBL3809603 140476 None 6 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 344 2 0 5 3.1 Cc1sc2ncnc(N3CCC(C(=O)N4CCCC4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
127043639 140506 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 337 3 0 6 3.1 Cc1ccc(OC2CCN(c3nc(C)nn4ccc(C)c34)CC2)cn1 10.1016/j.bmcl.2016.05.010
CHEMBL3810071 140506 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 337 3 0 6 3.1 Cc1ccc(OC2CCN(c3nc(C)nn4ccc(C)c34)CC2)cn1 10.1016/j.bmcl.2016.05.010
122190994 123602 None 0 Human Functional pEC50 = 6.0 6.0 -21 3
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 481 4 3 3 5.1 C/C(=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(Br)cc1)[C@H](O)C2)Nc1ccc(F)cc1 10.1016/j.bmcl.2015.08.011
CHEMBL3618436 123602 None 0 Human Functional pEC50 = 6.0 6.0 -21 3
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 481 4 3 3 5.1 C/C(=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(Br)cc1)[C@H](O)C2)Nc1ccc(F)cc1 10.1016/j.bmcl.2015.08.011
CHEMBL5080134 214663 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL None None None Cc1cc(C)c2c(n1)sc1c(NCc3ccc(CN4CCOCC4)cc3)ncnc12 10.1016/j.bmcl.2021.128416
43989253 76056 None 2 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 assessed as potentiation of acetylcholine-mediated calcium mobilization incubated for 144 secs prior to acetylcholine addition by Fluo-4-AM stainingPositive allosteric modulation of human M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 assessed as potentiation of acetylcholine-mediated calcium mobilization incubated for 144 secs prior to acetylcholine addition by Fluo-4-AM staining
ChEMBL 300 3 1 6 2.7 COc1ccc(C)c2sc(NC(=O)c3cnccn3)nc12 10.1016/j.bmcl.2012.05.109
CHEMBL2057394 76056 None 2 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 assessed as potentiation of acetylcholine-mediated calcium mobilization incubated for 144 secs prior to acetylcholine addition by Fluo-4-AM stainingPositive allosteric modulation of human M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 assessed as potentiation of acetylcholine-mediated calcium mobilization incubated for 144 secs prior to acetylcholine addition by Fluo-4-AM staining
ChEMBL 300 3 1 6 2.7 COc1ccc(C)c2sc(NC(=O)c3cnccn3)nc12 10.1016/j.bmcl.2012.05.109
135126568 164445 None 0 Rat Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 398 5 1 5 3.5 Cc1cc(C)c2cc(C(=O)NC3CN(c4ccnc(OC(F)F)c4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
CHEMBL4213855 164445 None 0 Rat Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 398 5 1 5 3.5 Cc1cc(C)c2cc(C(=O)NC3CN(c4ccnc(OC(F)F)c4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
122189499 123335 None 0 Human Functional pEC50 = 7.0 7.0 -4 3
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 441 3 2 3 4.0 CN1CCCC/C1=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(Br)cc1)[C@H](O)C2 10.1016/j.bmcl.2015.08.011
CHEMBL3616504 123335 None 0 Human Functional pEC50 = 7.0 7.0 -4 3
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 441 3 2 3 4.0 CN1CCCC/C1=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(Br)cc1)[C@H](O)C2 10.1016/j.bmcl.2015.08.011
135126568 164445 None 0 Rat Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 398 5 1 5 3.5 Cc1cc(C)c2cc(C(=O)NC3CN(c4ccnc(OC(F)F)c4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
CHEMBL4213855 164445 None 0 Rat Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 398 5 1 5 3.5 Cc1cc(C)c2cc(C(=O)NC3CN(c4ccnc(OC(F)F)c4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
CHEMBL5087350 215084 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL None None None Cc1cc(C)c2c(n1)sc1c(NCc3ccc4c(c3)COC4)ncnc12 10.1016/j.bmcl.2021.128416
29262717 140476 None 6 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 344 2 0 5 3.1 Cc1sc2ncnc(N3CCC(C(=O)N4CCCC4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
CHEMBL3809603 140476 None 6 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 344 2 0 5 3.1 Cc1sc2ncnc(N3CCC(C(=O)N4CCCC4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
145973325 164721 None 0 Rat Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 401 3 1 5 3.3 Cc1cc(C)c2cc(C(=O)NC3CN(c4cnc(C(F)(F)F)cn4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
CHEMBL4217458 164721 None 0 Rat Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 401 3 1 5 3.3 Cc1cc(C)c2cc(C(=O)NC3CN(c4cnc(C(F)(F)F)cn4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
59654579 123605 None 0 Human Functional pEC50 = 6.9 6.9 -5 3
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 495 5 3 3 4.8 C/C(=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(Br)cc1)[C@H](O)C2)NCc1ccc(F)cc1 10.1016/j.bmcl.2015.08.011
CHEMBL3618440 123605 None 0 Human Functional pEC50 = 6.9 6.9 -5 3
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 495 5 3 3 4.8 C/C(=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(Br)cc1)[C@H](O)C2)NCc1ccc(F)cc1 10.1016/j.bmcl.2015.08.011
156017590 177839 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 385 4 1 6 2.6 COc1cc(N2CC(NC(=O)c3ccc4nc(C)c(C)n4c3)C2)c(Cl)cn1 10.1016/j.bmcl.2019.126812
CHEMBL4644084 177839 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 385 4 1 6 2.6 COc1cc(N2CC(NC(=O)c3ccc4nc(C)c(C)n4c3)C2)c(Cl)cn1 10.1016/j.bmcl.2019.126812
145973325 164721 None 0 Rat Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 401 3 1 5 3.3 Cc1cc(C)c2cc(C(=O)NC3CN(c4cnc(C(F)(F)F)cn4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
CHEMBL4217458 164721 None 0 Rat Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 401 3 1 5 3.3 Cc1cc(C)c2cc(C(=O)NC3CN(c4cnc(C(F)(F)F)cn4)C3)ccc2n1 10.1016/j.bmcl.2017.10.016
162658616 181051 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 439 4 3 9 1.5 Cc1c(CO)nnc2sc(C(=O)NC3CN(c4ncc(C(F)(F)F)cn4)C3)c(N)c12 10.1016/j.bmcl.2019.05.026
CHEMBL4759565 181051 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 439 4 3 9 1.5 Cc1c(CO)nnc2sc(C(=O)NC3CN(c4ncc(C(F)(F)F)cn4)C3)c(N)c12 10.1016/j.bmcl.2019.05.026
127044706 140443 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 334 3 0 5 3.7 Cc1ccc2ncnc(N3CCC(Oc4ccc(C)nc4)CC3)c2c1 10.1016/j.bmcl.2016.05.010
CHEMBL3809292 140443 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 334 3 0 5 3.7 Cc1ccc2ncnc(N3CCC(Oc4ccc(C)nc4)CC3)c2c1 10.1016/j.bmcl.2016.05.010
134207678 171220 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 414 3 2 7 2.7 Cc1cc2nncn2c2sc(C(=O)NC3CN(c4ccc(F)c(F)c4)C3)c(N)c12 10.1016/j.bmcl.2019.06.032
CHEMBL4459622 171220 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 414 3 2 7 2.7 Cc1cc2nncn2c2sc(C(=O)NC3CN(c4ccc(F)c(F)c4)C3)c(N)c12 10.1016/j.bmcl.2019.06.032
134207707 172325 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 397 2 2 6 3.4 Cc1c(Cl)c2nncn2c2sc(C(=O)NC3Cc4ccccc4C3)c(N)c12 10.1016/j.bmcl.2019.06.032
CHEMBL4475459 172325 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 397 2 2 6 3.4 Cc1c(Cl)c2nncn2c2sc(C(=O)NC3Cc4ccccc4C3)c(N)c12 10.1016/j.bmcl.2019.06.032
24967746 16053 None 0 Human Functional pEC50 = 7.9 7.9 -31 5
Agonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 403 5 1 4 4.5 CCCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)[nH]c4cc(F)c(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223754 16053 None 0 Human Functional pEC50 = 7.9 7.9 -31 5
Agonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 403 5 1 4 4.5 CCCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)[nH]c4cc(F)c(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
682264 40208 None 15 Human Functional pEC50 = 6.9 6.9 -1 2
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 296 2 1 4 4.0 Cc1nc2sc(C(=O)c3ccccc3)c(N)c2c(C)c1C 10.1016/j.bmcl.2016.07.042
CHEMBL1480401 40208 None 15 Human Functional pEC50 = 6.9 6.9 -1 2
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 296 2 1 4 4.0 Cc1nc2sc(C(=O)c3ccccc3)c(N)c2c(C)c1C 10.1016/j.bmcl.2016.07.042
89452242 175435 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 346 3 1 6 4.7 Cc1nc2sc3c(NCc4ccco4)nn(C)c3c2c(C)c1Cl 10.1016/j.bmcl.2018.12.039
CHEMBL4576513 175435 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 346 3 1 6 4.7 Cc1nc2sc3c(NCc4ccco4)nn(C)c3c2c(C)c1Cl 10.1016/j.bmcl.2018.12.039
134207717 171292 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 363 2 2 6 3.3 Cc1cc2nncn2c2sc(C(=O)N[C@H]3CCc4ccccc43)c(N)c12 10.1016/j.bmcl.2019.06.032
CHEMBL4460701 171292 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 363 2 2 6 3.3 Cc1cc2nncn2c2sc(C(=O)N[C@H]3CCc4ccccc43)c(N)c12 10.1016/j.bmcl.2019.06.032
134207690 174643 None 0 Human Functional pEC50 = 6.9 6.9 5 2
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 434 4 2 9 2.4 Cc1nc2cc(C)c3c(N)c(C(=O)NC4CN(c5cnc(C6CC6)nc5)C4)sc3n2n1 10.1016/j.bmcl.2019.06.032
CHEMBL4558206 174643 None 0 Human Functional pEC50 = 6.9 6.9 5 2
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 434 4 2 9 2.4 Cc1nc2cc(C)c3c(N)c(C(=O)NC4CN(c5cnc(C6CC6)nc5)C4)sc3n2n1 10.1016/j.bmcl.2019.06.032
134207705 175906 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 377 2 2 6 3.6 Cc1nc2cc(C)c3c(N)c(C(=O)N[C@H]4CCc5ccccc54)sc3n2n1 10.1016/j.bmcl.2019.06.032
CHEMBL4587040 175906 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 377 2 2 6 3.6 Cc1nc2cc(C)c3c(N)c(C(=O)N[C@H]4CCc5ccccc54)sc3n2n1 10.1016/j.bmcl.2019.06.032
162647361 179679 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 415 4 2 8 2.5 Cc1c(Cl)nnc2sc(C(=O)NC3CN(c4ccc(C5CC5)nn4)C3)c(N)c12 10.1016/j.bmcl.2019.05.026
CHEMBL4743571 179679 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 415 4 2 8 2.5 Cc1c(Cl)nnc2sc(C(=O)NC3CN(c4ccc(C5CC5)nn4)C3)c(N)c12 10.1016/j.bmcl.2019.05.026
89452686 170670 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 298 3 2 5 4.0 Cc1cc(C)c2c(n1)sc1c(NCc3ccco3)n[nH]c12 10.1016/j.bmcl.2018.12.039
CHEMBL4451608 170670 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 298 3 2 5 4.0 Cc1cc(C)c2c(n1)sc1c(NCc3ccco3)n[nH]c12 10.1016/j.bmcl.2018.12.039
134207730 173064 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 376 2 2 5 3.6 Cc1cn2c(cc(C)c3c(N)c(C(=O)NC4Cc5ccccc5C4)sc32)n1 10.1016/j.bmcl.2019.06.032
CHEMBL4519541 173064 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 376 2 2 5 3.6 Cc1cn2c(cc(C)c3c(N)c(C(=O)NC4Cc5ccccc5C4)sc32)n1 10.1016/j.bmcl.2019.06.032
127044706 140443 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 334 3 0 5 3.7 Cc1ccc2ncnc(N3CCC(Oc4ccc(C)nc4)CC3)c2c1 10.1016/j.bmcl.2016.05.010
CHEMBL3809292 140443 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 334 3 0 5 3.7 Cc1ccc2ncnc(N3CCC(Oc4ccc(C)nc4)CC3)c2c1 10.1016/j.bmcl.2016.05.010
16309462 26186 None 4 Human Functional pEC50 = 5.9 5.9 -4 2
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 445 4 2 7 2.8 Cc1sc2ncnc(N3CCC(C(=O)Nc4ccc(S(N)(=O)=O)cc4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
CHEMBL1357034 26186 None 4 Human Functional pEC50 = 5.9 5.9 -4 2
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 445 4 2 7 2.8 Cc1sc2ncnc(N3CCC(C(=O)Nc4ccc(S(N)(=O)=O)cc4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
53382518 86310 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 381 3 2 4 4.4 Cc1nc2sc(C(=O)NCc3cccc(F)c3F)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313376 86310 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 381 3 2 4 4.4 Cc1nc2sc(C(=O)NCc3cccc(F)c3F)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
155543990 173319 None 0 Rat Functional pEC50 = 5.9 5.9 -4 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 402 5 1 7 4.0 Nc1c(C(=O)c2ccncc2)sc2nc(OCc3ccncc3)c3c(c12)CCC3 10.1016/j.bmcl.2016.07.042
CHEMBL4526419 173319 None 0 Rat Functional pEC50 = 5.9 5.9 -4 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 402 5 1 7 4.0 Nc1c(C(=O)c2ccncc2)sc2nc(OCc3ccncc3)c3c(c12)CCC3 10.1016/j.bmcl.2016.07.042
45501061 156773 None 12 Human Functional pEC50 = 5.9 5.9 2 2
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 388 4 1 4 3.8 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)NCc2ccccc2)CC1 10.1016/j.bmcl.2017.08.043
CHEMBL4070787 156773 None 12 Human Functional pEC50 = 5.9 5.9 2 2
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 388 4 1 4 3.8 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)NCc2ccccc2)CC1 10.1016/j.bmcl.2017.08.043
137641943 158476 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 354 3 2 7 1.9 Cc1nnc2sc(C(=O)NC3CN(c4ccccn4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4090871 158476 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 354 3 2 7 1.9 Cc1nnc2sc(C(=O)NC3CN(c4ccccn4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
53382518 86310 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 381 3 2 4 4.4 Cc1nc2sc(C(=O)NCc3cccc(F)c3F)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313376 86310 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 381 3 2 4 4.4 Cc1nc2sc(C(=O)NCc3cccc(F)c3F)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL5087948 215128 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL None None None Cc1cc(C)c2c(n1)sc1c(NC3CCCC3)nccc12 10.1016/j.bmcl.2021.128416
156011081 177067 None 0 Human Functional pEC50 = 6.9 6.9 -3 2
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 404 3 2 6 2.8 Cc1c2c(N)c(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)ccc2nn1C 10.1016/j.bmcl.2019.126811
CHEMBL4632962 177067 None 0 Human Functional pEC50 = 6.9 6.9 -3 2
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 404 3 2 6 2.8 Cc1c2c(N)c(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)ccc2nn1C 10.1016/j.bmcl.2019.126811
25199525 16079 None 0 Human Functional pEC50 = 6.9 6.9 -5 3
Agonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 358 4 0 5 4.0 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccccc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223807 16079 None 0 Human Functional pEC50 = 6.9 6.9 -5 3
Agonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 358 4 0 5 4.0 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccccc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
137659901 159543 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 383 4 2 7 2.5 COc1ccc(N2CC(NC(=O)c3sc4nnc(C)c(C)c4c3N)C2)cc1 10.1016/j.bmcl.2017.05.014
CHEMBL4102480 159543 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 383 4 2 7 2.5 COc1ccc(N2CC(NC(=O)c3sc4nnc(C)c(C)c4c3N)C2)cc1 10.1016/j.bmcl.2017.05.014
53382505 86318 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 360 4 2 5 3.5 Cc1nc2sc(C(=O)NCCc3ccncc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313384 86318 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 360 4 2 5 3.5 Cc1nc2sc(C(=O)NCCc3ccncc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
53382505 86318 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 360 4 2 5 3.5 Cc1nc2sc(C(=O)NCCc3ccncc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313384 86318 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 360 4 2 5 3.5 Cc1nc2sc(C(=O)NCCc3ccncc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
137654582 159002 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 348 3 0 5 3.7 N#Cc1cnc2ccc(F)cc2c1N1CCC(Oc2cccnc2)CC1 10.1016/j.bmcl.2017.08.043
CHEMBL4096463 159002 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 348 3 0 5 3.7 N#Cc1cnc2ccc(F)cc2c1N1CCC(Oc2cccnc2)CC1 10.1016/j.bmcl.2017.08.043
56592910 76055 None 1 Human Functional pEC50 = 5.9 5.9 -5 2
Positive allosteric modulation of human M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 assessed as potentiation of acetylcholine-mediated calcium mobilization incubated for 144 secs prior to acetylcholine addition by Fluo-4-AM stainingPositive allosteric modulation of human M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 assessed as potentiation of acetylcholine-mediated calcium mobilization incubated for 144 secs prior to acetylcholine addition by Fluo-4-AM staining
ChEMBL 299 3 1 5 3.3 COc1ccc(C)c2sc(NC(=O)c3ccncc3)nc12 10.1016/j.bmcl.2012.05.109
CHEMBL2057392 76055 None 1 Human Functional pEC50 = 5.9 5.9 -5 2
Positive allosteric modulation of human M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 assessed as potentiation of acetylcholine-mediated calcium mobilization incubated for 144 secs prior to acetylcholine addition by Fluo-4-AM stainingPositive allosteric modulation of human M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 assessed as potentiation of acetylcholine-mediated calcium mobilization incubated for 144 secs prior to acetylcholine addition by Fluo-4-AM staining
ChEMBL 299 3 1 5 3.3 COc1ccc(C)c2sc(NC(=O)c3ccncc3)nc12 10.1016/j.bmcl.2012.05.109
137659901 159543 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 383 4 2 7 2.5 COc1ccc(N2CC(NC(=O)c3sc4nnc(C)c(C)c4c3N)C2)cc1 10.1016/j.bmcl.2017.05.014
CHEMBL4102480 159543 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 383 4 2 7 2.5 COc1ccc(N2CC(NC(=O)c3sc4nnc(C)c(C)c4c3N)C2)cc1 10.1016/j.bmcl.2017.05.014
137654582 159002 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 348 3 0 5 3.7 N#Cc1cnc2ccc(F)cc2c1N1CCC(Oc2cccnc2)CC1 10.1016/j.bmcl.2017.08.043
CHEMBL4096463 159002 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 348 3 0 5 3.7 N#Cc1cnc2ccc(F)cc2c1N1CCC(Oc2cccnc2)CC1 10.1016/j.bmcl.2017.08.043
71533671 112023 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at human muscarinic acetylcholine receptor M4 expressed in CHO cells assessed as calcium mobilization by FLIPR assayAgonist activity at human muscarinic acetylcholine receptor M4 expressed in CHO cells assessed as calcium mobilization by FLIPR assay
ChEMBL 450 4 0 6 2.5 CCOC(=O)N1CCC(C)(CN2CCC3(CC2)CN(S(C)(=O)=O)c2ncccc23)CC1 10.1016/j.bmcl.2014.04.083
CHEMBL3289442 112023 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at human muscarinic acetylcholine receptor M4 expressed in CHO cells assessed as calcium mobilization by FLIPR assayAgonist activity at human muscarinic acetylcholine receptor M4 expressed in CHO cells assessed as calcium mobilization by FLIPR assay
ChEMBL 450 4 0 6 2.5 CCOC(=O)N1CCC(C)(CN2CCC3(CC2)CN(S(C)(=O)=O)c2ncccc23)CC1 10.1016/j.bmcl.2014.04.083
89777151 158571 None 0 Rat Functional pEC50 = 7.9 7.9 7 2
Positive allosteric modulation of rat M4 receptor assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 407 4 2 6 4.0 Cc1nnc2sc(C(=O)NCc3ccc(-c4cccnc4F)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
CHEMBL4091821 158571 None 0 Rat Functional pEC50 = 7.9 7.9 7 2
Positive allosteric modulation of rat M4 receptor assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of rat M4 receptor assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 407 4 2 6 4.0 Cc1nnc2sc(C(=O)NCc3ccc(-c4cccnc4F)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
134207699 175376 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 286 2 2 5 2.3 Cc1cc2nccn2c2sc(C(=O)NC3CC3)c(N)c12 10.1016/j.bmcl.2019.06.032
CHEMBL4574990 175376 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 286 2 2 5 2.3 Cc1cc2nccn2c2sc(C(=O)NC3CC3)c(N)c12 10.1016/j.bmcl.2019.06.032
734373 15277 None 23 Rat Functional pEC50 = 5.9 5.9 - 1
Allosteric activation of rat recombinant muscarinic M4 receptor expressed in CHO cells assessed as potentiation of 15 nM acetylcholine-induced calcium mobilization after 1 hr by fluorescence assayAllosteric activation of rat recombinant muscarinic M4 receptor expressed in CHO cells assessed as potentiation of 15 nM acetylcholine-induced calcium mobilization after 1 hr by fluorescence assay
ChEMBL 311 3 2 4 3.4 Cc1cc(C)c2c(N)c(C(=O)NCc3ccccc3)sc2n1 10.1038/nchembio.2007.55
CHEMBL1212983 15277 None 23 Rat Functional pEC50 = 5.9 5.9 - 1
Allosteric activation of rat recombinant muscarinic M4 receptor expressed in CHO cells assessed as potentiation of 15 nM acetylcholine-induced calcium mobilization after 1 hr by fluorescence assayAllosteric activation of rat recombinant muscarinic M4 receptor expressed in CHO cells assessed as potentiation of 15 nM acetylcholine-induced calcium mobilization after 1 hr by fluorescence assay
ChEMBL 311 3 2 4 3.4 Cc1cc(C)c2c(N)c(C(=O)NCc3ccccc3)sc2n1 10.1038/nchembio.2007.55
137650228 157265 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 383 4 2 7 2.5 COc1cccc(N2CC(NC(=O)c3sc4nnc(C)c(C)c4c3N)C2)c1 10.1016/j.bmcl.2017.05.014
CHEMBL4076732 157265 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 383 4 2 7 2.5 COc1cccc(N2CC(NC(=O)c3sc4nnc(C)c(C)c4c3N)C2)c1 10.1016/j.bmcl.2017.05.014
156022087 178194 None 0 Human Functional pEC50 = 6.9 6.9 1 2
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 390 3 1 6 2.7 Cc1nc2cnc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)cn2c1C 10.1016/j.bmcl.2019.126812
CHEMBL4649459 178194 None 0 Human Functional pEC50 = 6.9 6.9 1 2
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 390 3 1 6 2.7 Cc1nc2cnc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)cn2c1C 10.1016/j.bmcl.2019.126812
2159295 76053 None 11 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 assessed as potentiation of acetylcholine-mediated calcium mobilization incubated for 144 secs prior to acetylcholine addition by Fluo-4-AM stainingPositive allosteric modulation of human M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 assessed as potentiation of acetylcholine-mediated calcium mobilization incubated for 144 secs prior to acetylcholine addition by Fluo-4-AM staining
ChEMBL 288 3 1 5 3.5 COc1ccc(C)c2sc(NC(=O)c3ccco3)nc12 10.1016/j.bmcl.2012.05.109
CHEMBL2057376 76053 None 11 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 assessed as potentiation of acetylcholine-mediated calcium mobilization incubated for 144 secs prior to acetylcholine addition by Fluo-4-AM stainingPositive allosteric modulation of human M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 assessed as potentiation of acetylcholine-mediated calcium mobilization incubated for 144 secs prior to acetylcholine addition by Fluo-4-AM staining
ChEMBL 288 3 1 5 3.5 COc1ccc(C)c2sc(NC(=O)c3ccco3)nc12 10.1016/j.bmcl.2012.05.109
122191004 123331 None 0 Human Functional pEC50 = 5.9 5.9 -3 3
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 521 7 3 4 4.7 COc1ccc(CCN/C(C)=N/c2ccc3c(c2)[C@@H](NC(=O)c2ccc(Br)cc2)[C@H](O)C3)cc1 10.1016/j.bmcl.2015.08.011
CHEMBL3616497 123331 None 0 Human Functional pEC50 = 5.9 5.9 -3 3
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 521 7 3 4 4.7 COc1ccc(CCN/C(C)=N/c2ccc3c(c2)[C@@H](NC(=O)c2ccc(Br)cc2)[C@H](O)C3)cc1 10.1016/j.bmcl.2015.08.011
156016090 177682 None 0 Human Functional pEC50 = 6.9 6.9 -1 2
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 404 3 2 6 2.5 Cc1c2c(N)c(C(=O)NC3CN(c4ccc(C(F)(F)F)nc4)C3)ccc2nn1C 10.1016/j.bmcl.2019.126811
CHEMBL4641848 177682 None 0 Human Functional pEC50 = 6.9 6.9 -1 2
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 404 3 2 6 2.5 Cc1c2c(N)c(C(=O)NC3CN(c4ccc(C(F)(F)F)nc4)C3)ccc2nn1C 10.1016/j.bmcl.2019.126811
53382500 86317 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 360 3 2 5 4.0 Cc1nc2sc(C(=O)NC(C)c3ccccn3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313383 86317 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 360 3 2 5 4.0 Cc1nc2sc(C(=O)NC(C)c3ccccn3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
44448421 12335 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Antagonist activity at human muscarinic M4 receptor expressed in CHO cells assessed as blockade of carbachol-induced inhibition of forskolin-stimulated cAMP accumulationAntagonist activity at human muscarinic M4 receptor expressed in CHO cells assessed as blockade of carbachol-induced inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 616 13 2 4 7.8 OC(CCCN1CCC(C2CCN(CCCC(O)(c3ccccc3)c3ccccc3)CC2)CC1)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2008.03.061
CHEMBL1185269 12335 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Antagonist activity at human muscarinic M4 receptor expressed in CHO cells assessed as blockade of carbachol-induced inhibition of forskolin-stimulated cAMP accumulationAntagonist activity at human muscarinic M4 receptor expressed in CHO cells assessed as blockade of carbachol-induced inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 616 13 2 4 7.8 OC(CCCN1CCC(C2CCN(CCCC(O)(c3ccccc3)c3ccccc3)CC2)CC1)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2008.03.061
CHEMBL403773 12335 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Antagonist activity at human muscarinic M4 receptor expressed in CHO cells assessed as blockade of carbachol-induced inhibition of forskolin-stimulated cAMP accumulationAntagonist activity at human muscarinic M4 receptor expressed in CHO cells assessed as blockade of carbachol-induced inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 616 13 2 4 7.8 OC(CCCN1CCC(C2CCN(CCCC(O)(c3ccccc3)c3ccccc3)CC2)CC1)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2008.03.061
682264 40208 None 15 Human Functional pEC50 = 6.9 6.9 -1 2
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 296 2 1 4 4.0 Cc1nc2sc(C(=O)c3ccccc3)c(N)c2c(C)c1C 10.1016/j.bmcl.2016.07.042
CHEMBL1480401 40208 None 15 Human Functional pEC50 = 6.9 6.9 -1 2
Positive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at human M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 296 2 1 4 4.0 Cc1nc2sc(C(=O)c3ccccc3)c(N)c2c(C)c1C 10.1016/j.bmcl.2016.07.042
89777181 144131 None 0 Rat Functional pEC50 = 6.9 6.9 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 374 4 2 6 2.6 Cc1nnc2sc(C(=O)NCc3ccc([S+](C)[O-])cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
CHEMBL3903798 144131 None 0 Rat Functional pEC50 = 6.9 6.9 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 374 4 2 6 2.6 Cc1nnc2sc(C(=O)NCc3ccc([S+](C)[O-])cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
53382500 86317 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 360 3 2 5 4.0 Cc1nc2sc(C(=O)NC(C)c3ccccn3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313383 86317 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 360 3 2 5 4.0 Cc1nc2sc(C(=O)NC(C)c3ccccn3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
156019946 177980 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 385 4 1 6 2.6 COc1cc(N2CC(NC(=O)c3ccc4nc(C)n(C)c4c3)C2)c(Cl)cn1 10.1016/j.bmcl.2019.126812
CHEMBL4646110 177980 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 385 4 1 6 2.6 COc1cc(N2CC(NC(=O)c3ccc4nc(C)n(C)c4c3)C2)c(Cl)cn1 10.1016/j.bmcl.2019.126812
89777181 144131 None 0 Rat Functional pEC50 = 6.9 6.9 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 374 4 2 6 2.6 Cc1nnc2sc(C(=O)NCc3ccc([S+](C)[O-])cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
CHEMBL3903798 144131 None 0 Rat Functional pEC50 = 6.9 6.9 - 1
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 374 4 2 6 2.6 Cc1nnc2sc(C(=O)NCc3ccc([S+](C)[O-])cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
302 2975 None 25 Human Functional pEC50 = 7.9 7.9 1 8
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1 10.1021/acsmedchemlett.9b00106
4630 2975 None 25 Human Functional pEC50 = 7.9 7.9 1 8
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1 10.1021/acsmedchemlett.9b00106
CHEMBL7634 2975 None 25 Human Functional pEC50 = 7.9 7.9 1 8
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1 10.1021/acsmedchemlett.9b00106
129277684 163549 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Positive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assayPositive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assay
ChEMBL 363 3 2 5 2.6 Cc1cc2c(nc1N1CCC(Oc3ccc4[nH]ncc4c3)CC1)CNC2=O 10.1021/acsmedchemlett.8b00330
CHEMBL4202966 163549 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Positive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assayPositive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assay
ChEMBL 363 3 2 5 2.6 Cc1cc2c(nc1N1CCC(Oc3ccc4[nH]ncc4c3)CC1)CNC2=O 10.1021/acsmedchemlett.8b00330
135154616 164574 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Positive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assayPositive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assay
ChEMBL 349 3 0 6 3.0 Cc1cc2c(nc1N1CCC(Oc3cccc(C#N)c3)CC1)COC2=O 10.1021/acsmedchemlett.8b00330
CHEMBL4215436 164574 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Positive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assayPositive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assay
ChEMBL 349 3 0 6 3.0 Cc1cc2c(nc1N1CCC(Oc3cccc(C#N)c3)CC1)COC2=O 10.1021/acsmedchemlett.8b00330
134207682 173642 None 0 Human Functional pEC50 = 6.9 6.9 4 2
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 461 3 2 8 3.5 Cc1nc2cc(C)c3c(N)c(C(=O)NC4CN(c5cc(Cl)ncc5Cl)C4)sc3n2n1 10.1016/j.bmcl.2019.06.032
CHEMBL4534301 173642 None 0 Human Functional pEC50 = 6.9 6.9 4 2
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 461 3 2 8 3.5 Cc1nc2cc(C)c3c(N)c(C(=O)NC4CN(c5cc(Cl)ncc5Cl)C4)sc3n2n1 10.1016/j.bmcl.2019.06.032
134207728 174685 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 428 3 2 9 2.2 Cc1nc2cc(C)c3c(N)c(C(=O)NC4CN(c5cnc(Cl)cn5)C4)sc3n2n1 10.1016/j.bmcl.2019.06.032
CHEMBL4559283 174685 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 428 3 2 9 2.2 Cc1nc2cc(C)c3c(N)c(C(=O)NC4CN(c5cnc(Cl)cn5)C4)sc3n2n1 10.1016/j.bmcl.2019.06.032
162659751 181292 None 0 Human Functional pEC50 = 6.9 6.9 2 2
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 409 3 2 8 2.3 Cc1c(Cl)nnc2sc(C(=O)NC3CN(c4cnc(Cl)cn4)C3)c(N)c12 10.1016/j.bmcl.2019.05.026
CHEMBL4762280 181292 None 0 Human Functional pEC50 = 6.9 6.9 2 2
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 409 3 2 8 2.3 Cc1c(Cl)nnc2sc(C(=O)NC3CN(c4cnc(Cl)cn4)C3)c(N)c12 10.1016/j.bmcl.2019.05.026
CHEMBL5089790 215225 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL None None None Cc1cc(C)c2c(n1)sc1c(NCc3cnc(C)nc3)ncnc12 10.1016/j.bmcl.2021.128416
137650228 157265 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 383 4 2 7 2.5 COc1cccc(N2CC(NC(=O)c3sc4nnc(C)c(C)c4c3N)C2)c1 10.1016/j.bmcl.2017.05.014
CHEMBL4076732 157265 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 383 4 2 7 2.5 COc1cccc(N2CC(NC(=O)c3sc4nnc(C)c(C)c4c3N)C2)c1 10.1016/j.bmcl.2017.05.014
53382493 86308 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 351 3 2 4 4.5 Cc1nc2sc(C(=O)NCC3CCCCC3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313374 86308 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 351 3 2 4 4.5 Cc1nc2sc(C(=O)NCC3CCCCC3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
53002540 159411 None 6 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 384 2 0 5 3.0 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)N2CCSCC2)CC1 10.1016/j.bmcl.2017.08.043
CHEMBL4100855 159411 None 6 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 384 2 0 5 3.0 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)N2CCSCC2)CC1 10.1016/j.bmcl.2017.08.043
53382493 86308 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 351 3 2 4 4.5 Cc1nc2sc(C(=O)NCC3CCCCC3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313374 86308 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 351 3 2 4 4.5 Cc1nc2sc(C(=O)NCC3CCCCC3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
53002540 159411 None 6 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 384 2 0 5 3.0 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)N2CCSCC2)CC1 10.1016/j.bmcl.2017.08.043
CHEMBL4100855 159411 None 6 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 384 2 0 5 3.0 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)N2CCSCC2)CC1 10.1016/j.bmcl.2017.08.043
156016031 177624 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 386 4 1 7 2.0 COc1cc(N2CC(NC(=O)c3cc4c(C)nn(C)c4cn3)C2)c(Cl)cn1 10.1016/j.bmcl.2019.126812
CHEMBL4641135 177624 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 386 4 1 7 2.0 COc1cc(N2CC(NC(=O)c3cc4c(C)nn(C)c4cn3)C2)c(Cl)cn1 10.1016/j.bmcl.2019.126812
89777316 157883 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 407 4 2 6 4.0 Cc1nnc2sc(C(=O)NCc3ccc(-c4cncc(F)c4)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
CHEMBL4084063 157883 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 407 4 2 6 4.0 Cc1nnc2sc(C(=O)NCc3ccc(-c4cncc(F)c4)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
CHEMBL5077997 214524 None 1 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL None None None Cc1cc(C)c2c(n1)sc1c(N3CC4(COC4)C3)ncnc12 10.1016/j.bmcl.2021.128416
682264 40208 None 15 Rat Functional pEC50 = 6.8 6.8 1 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 296 2 1 4 4.0 Cc1nc2sc(C(=O)c3ccccc3)c(N)c2c(C)c1C 10.1016/j.bmcl.2016.07.042
CHEMBL1480401 40208 None 15 Rat Functional pEC50 = 6.8 6.8 1 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 296 2 1 4 4.0 Cc1nc2sc(C(=O)c3ccccc3)c(N)c2c(C)c1C 10.1016/j.bmcl.2016.07.042
89777316 157883 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 407 4 2 6 4.0 Cc1nnc2sc(C(=O)NCc3ccc(-c4cncc(F)c4)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
CHEMBL4084063 157883 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 407 4 2 6 4.0 Cc1nnc2sc(C(=O)NCc3ccc(-c4cncc(F)c4)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
155539604 172842 None 0 Rat Functional pEC50 = 5.8 5.8 -2 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 313 3 1 6 3.1 COc1ccc(C(=O)c2sc3nnc(C)c(C)c3c2N)cc1 10.1016/j.bmcl.2016.07.042
CHEMBL4514671 172842 None 0 Rat Functional pEC50 = 5.8 5.8 -2 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 313 3 1 6 3.1 COc1ccc(C(=O)c2sc3nnc(C)c(C)c3c2N)cc1 10.1016/j.bmcl.2016.07.042
145972844 164674 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 370 2 1 5 3.7 Cc1nnc2sc(C(=O)N3CC(c4cccc(F)c4)C3C)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
CHEMBL4216874 164674 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 370 2 1 5 3.7 Cc1nnc2sc(C(=O)N3CC(c4cccc(F)c4)C3C)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
155539604 172842 None 0 Rat Functional pEC50 = 5.8 5.8 -2 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 313 3 1 6 3.1 COc1ccc(C(=O)c2sc3nnc(C)c(C)c3c2N)cc1 10.1016/j.bmcl.2016.07.042
CHEMBL4514671 172842 None 0 Rat Functional pEC50 = 5.8 5.8 -2 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 313 3 1 6 3.1 COc1ccc(C(=O)c2sc3nnc(C)c(C)c3c2N)cc1 10.1016/j.bmcl.2016.07.042
156012013 177365 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 370 3 2 6 2.1 Cc1c2c(N)c(C(=O)NC3CN(c4cccc(Cl)n4)C3)ccc2nn1C 10.1016/j.bmcl.2019.126811
CHEMBL4637785 177365 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 370 3 2 6 2.1 Cc1c2c(N)c(C(=O)NC3CN(c4cccc(Cl)n4)C3)ccc2nn1C 10.1016/j.bmcl.2019.126811
145972844 164674 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 370 2 1 5 3.7 Cc1nnc2sc(C(=O)N3CC(c4cccc(F)c4)C3C)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
CHEMBL4216874 164674 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 370 2 1 5 3.7 Cc1nnc2sc(C(=O)N3CC(c4cccc(F)c4)C3C)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
137653138 158918 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 375 3 1 5 3.5 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)Nc2ccncc2)CC1 10.1016/j.bmcl.2017.08.043
CHEMBL4095560 158918 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 375 3 1 5 3.5 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)Nc2ccncc2)CC1 10.1016/j.bmcl.2017.08.043
53382529 86336 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 297 2 2 4 3.3 Cc1nc2sc(C(=O)NC(C)C)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313404 86336 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 297 2 2 4 3.3 Cc1nc2sc(C(=O)NC(C)C)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
137653138 158918 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 375 3 1 5 3.5 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)Nc2ccncc2)CC1 10.1016/j.bmcl.2017.08.043
CHEMBL4095560 158918 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 375 3 1 5 3.5 N#Cc1cnc2ccc(F)cc2c1N1CCC(C(=O)Nc2ccncc2)CC1 10.1016/j.bmcl.2017.08.043
53382529 86336 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 297 2 2 4 3.3 Cc1nc2sc(C(=O)NC(C)C)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313404 86336 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 297 2 2 4 3.3 Cc1nc2sc(C(=O)NC(C)C)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
156013272 177481 None 0 Human Functional pEC50 = 6.8 6.8 -1 2
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 400 4 2 7 2.1 COc1cc(N2CC(NC(=O)c3ccc4nn(C)c(C)c4c3N)C2)c(Cl)cn1 10.1016/j.bmcl.2019.126811
CHEMBL4639222 177481 None 0 Human Functional pEC50 = 6.8 6.8 -1 2
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 400 4 2 7 2.1 COc1cc(N2CC(NC(=O)c3ccc4nn(C)c(C)c4c3N)C2)c(Cl)cn1 10.1016/j.bmcl.2019.126811
156014779 177532 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 339 3 1 5 3.7 Cc1c2c(ccc3c(NCc4ccc(F)c(F)c4)ncnc32)nn1C 10.1016/j.bmcl.2019.126811
CHEMBL4640119 177532 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 339 3 1 5 3.7 Cc1c2c(ccc3c(NCc4ccc(F)c(F)c4)ncnc32)nn1C 10.1016/j.bmcl.2019.126811
CHEMBL5088165 215140 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL None None None Cc1cc(C)c2c(n1)oc1c(NC3CN(c4cc(Cl)ncc4Cl)C3)ncnc12 10.1016/j.bmcl.2021.128416
156014138 177240 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 396 4 1 9 2.3 COc1cc(N2CC(Nc3ncnc4c3ccc3nnn(C)c34)C2)c(Cl)cn1 10.1016/j.bmcl.2019.126811
CHEMBL4635779 177240 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 396 4 1 9 2.3 COc1cc(N2CC(Nc3ncnc4c3ccc3nnn(C)c34)C2)c(Cl)cn1 10.1016/j.bmcl.2019.126811
71528087 87583 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Partial agonist activity at human M4 receptor co-expressed with Galpha16 in CHO cells assessed as calcium mobilization after 60 mins by FLIPR assayPartial agonist activity at human M4 receptor co-expressed with Galpha16 in CHO cells assessed as calcium mobilization after 60 mins by FLIPR assay
ChEMBL 385 4 0 4 2.9 CCOC(=O)N1CCC(C)(CN2CC[C@H](N3C(=O)Cc4ccccc43)C2)CC1 10.1021/ml300372f
CHEMBL2336056 87583 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Partial agonist activity at human M4 receptor co-expressed with Galpha16 in CHO cells assessed as calcium mobilization after 60 mins by FLIPR assayPartial agonist activity at human M4 receptor co-expressed with Galpha16 in CHO cells assessed as calcium mobilization after 60 mins by FLIPR assay
ChEMBL 385 4 0 4 2.9 CCOC(=O)N1CCC(C)(CN2CC[C@H](N3C(=O)Cc4ccccc43)C2)CC1 10.1021/ml300372f
145966439 164266 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Positive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assayPositive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assay
ChEMBL 418 4 1 8 2.3 COc1ccc(OC2CCN(c3nc4oc(=O)[nH]c(=O)c4c(Cl)c3C)CC2)cn1 10.1021/acsmedchemlett.8b00330
CHEMBL4211671 164266 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Positive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assayPositive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assay
ChEMBL 418 4 1 8 2.3 COc1ccc(OC2CCN(c3nc4oc(=O)[nH]c(=O)c4c(Cl)c3C)CC2)cn1 10.1021/acsmedchemlett.8b00330
137656783 159682 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 372 3 2 7 2.0 Cc1nnc2sc(C(=O)NC3CN(c4cncc(F)c4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4104144 159682 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 372 3 2 7 2.0 Cc1nnc2sc(C(=O)NC3CN(c4cncc(F)c4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
162657433 181161 None 0 Human Functional pEC50 = 6.8 6.8 5 2
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 428 4 2 7 3.4 Cc1cc(C2CC2)ncc1N1CC(NC(=O)c2sc3nnc(Cl)c(C)c3c2N)C1 10.1016/j.bmcl.2019.05.026
CHEMBL4760902 181161 None 0 Human Functional pEC50 = 6.8 6.8 5 2
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 428 4 2 7 3.4 Cc1cc(C2CC2)ncc1N1CC(NC(=O)c2sc3nnc(Cl)c(C)c3c2N)C1 10.1016/j.bmcl.2019.05.026
162663713 181966 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 459 4 2 8 2.9 Cc1c(C(F)F)nnc2sc(C(=O)NC3CN(c4ncc(C(F)(F)F)cn4)C3)c(N)c12 10.1016/j.bmcl.2019.05.026
CHEMBL4780059 181966 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 459 4 2 8 2.9 Cc1c(C(F)F)nnc2sc(C(=O)NC3CN(c4ncc(C(F)(F)F)cn4)C3)c(N)c12 10.1016/j.bmcl.2019.05.026
CHEMBL5079861 214647 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL None None None Cc1cc(C)c2c(n1)sc1c(NC3CN(c4ncc(C(F)(F)F)cn4)C3)nccc12 10.1016/j.bmcl.2021.128416
683024 51304 None 24 Rat Functional pEC50 = 5.8 5.8 -1 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 282 2 1 4 3.7 Cc1cc(C)c2c(N)c(C(=O)c3ccccc3)sc2n1 10.1016/j.bmcl.2016.07.042
CHEMBL1581020 51304 None 24 Rat Functional pEC50 = 5.8 5.8 -1 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 282 2 1 4 3.7 Cc1cc(C)c2c(N)c(C(=O)c3ccccc3)sc2n1 10.1016/j.bmcl.2016.07.042
117916889 170473 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 356 4 1 4 4.9 CSc1ccc(CNC(=O)c2sc3nc(C)cc(C)c3c2C)cc1 10.1016/j.bmcl.2018.12.039
CHEMBL4448985 170473 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 356 4 1 4 4.9 CSc1ccc(CNC(=O)c2sc3nc(C)cc(C)c3c2C)cc1 10.1016/j.bmcl.2018.12.039
117910878 174406 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 345 4 1 5 3.4 COc1ccc(CNC(=O)c2cc3c(C)c(C)nnc3s2)cc1F 10.1016/j.bmcl.2018.12.039
CHEMBL4552552 174406 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 345 4 1 5 3.4 COc1ccc(CNC(=O)c2cc3c(C)c(C)nnc3s2)cc1F 10.1016/j.bmcl.2018.12.039
145966183 164238 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 356 2 1 5 3.3 Cc1nnc2sc(C(=O)N3CC(c4ccc(F)cc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
CHEMBL4211252 164238 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 356 2 1 5 3.3 Cc1nnc2sc(C(=O)N3CC(c4ccc(F)cc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
145966183 164238 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 356 2 1 5 3.3 Cc1nnc2sc(C(=O)N3CC(c4ccc(F)cc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
CHEMBL4211252 164238 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 356 2 1 5 3.3 Cc1nnc2sc(C(=O)N3CC(c4ccc(F)cc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
145964807 164281 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 352 2 1 5 3.5 Cc1nnc2sc(C(=O)N3CC(c4ccccc4)C3C)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
CHEMBL4211897 164281 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 352 2 1 5 3.5 Cc1nnc2sc(C(=O)N3CC(c4ccccc4)C3C)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
683024 51304 None 24 Rat Functional pEC50 = 5.8 5.8 -1 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 282 2 1 4 3.7 Cc1cc(C)c2c(N)c(C(=O)c3ccccc3)sc2n1 10.1016/j.bmcl.2016.07.042
CHEMBL1581020 51304 None 24 Rat Functional pEC50 = 5.8 5.8 -1 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 282 2 1 4 3.7 Cc1cc(C)c2c(N)c(C(=O)c3ccccc3)sc2n1 10.1016/j.bmcl.2016.07.042
145964807 164281 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 352 2 1 5 3.5 Cc1nnc2sc(C(=O)N3CC(c4ccccc4)C3C)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
CHEMBL4211897 164281 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 352 2 1 5 3.5 Cc1nnc2sc(C(=O)N3CC(c4ccccc4)C3C)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
CHEMBL5085861 214993 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL None None None Cc1cc(C)c2c(n1)sc1c(C3CCOCC3)ncnc12 10.1016/j.bmcl.2021.128416
53382480 86327 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 381 3 2 4 4.4 Cc1nc2sc(C(=O)NCc3ccc(F)c(F)c3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313393 86327 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 381 3 2 4 4.4 Cc1nc2sc(C(=O)NCc3ccc(F)c(F)c3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
1505737 86328 None 12 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 379 3 2 4 4.7 Cc1nc2sc(C(=O)NCc3ccccc3Cl)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313394 86328 None 12 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 379 3 2 4 4.7 Cc1nc2sc(C(=O)NCc3ccccc3Cl)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
137632847 156436 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 407 4 2 6 4.0 Cc1nnc2sc(C(=O)NCc3ccc(-c4ccncc4F)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
CHEMBL4066953 156436 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 407 4 2 6 4.0 Cc1nnc2sc(C(=O)NCc3ccc(-c4ccncc4F)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
CHEMBL5090162 215244 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL None None None Cc1cc(C)c2c(n1)sc1c(NCc3ccc(-n4ccnc4)nc3)ncnc12 10.1016/j.bmcl.2021.128416
156013904 177237 None 0 Human Functional pEC50 = 6.8 6.8 -1 2
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 395 3 2 7 2.0 Cc1c2c(N)c(C(=O)NC3CN(c4ncc(C#N)cc4Cl)C3)ccc2nn1C 10.1016/j.bmcl.2019.126811
CHEMBL4635732 177237 None 0 Human Functional pEC50 = 6.8 6.8 -1 2
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 395 3 2 7 2.0 Cc1c2c(N)c(C(=O)NC3CN(c4ncc(C#N)cc4Cl)C3)ccc2nn1C 10.1016/j.bmcl.2019.126811
42599068 16077 None 0 Human Functional pEC50 = 6.8 6.8 -50 5
Agonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 356 3 0 3 3.7 CO[C@H]1CC[C@](C)(N2CCC(N3C(=O)Cc4ccc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223805 16077 None 0 Human Functional pEC50 = 6.8 6.8 -50 5
Agonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 356 3 0 3 3.7 CO[C@H]1CC[C@](C)(N2CCC(N3C(=O)Cc4ccc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
42598360 16102 None 0 Human Functional pEC50 = 6.8 6.8 -63 5
Agonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 388 5 0 6 4.0 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(OC)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223862 16102 None 0 Human Functional pEC50 = 6.8 6.8 -63 5
Agonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 388 5 0 6 4.0 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(OC)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
137649420 157519 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 388 3 2 7 2.6 Cc1nnc2sc(C(=O)NC3CN(c4ccnc(Cl)c4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4079904 157519 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 388 3 2 7 2.6 Cc1nnc2sc(C(=O)NC3CN(c4ccnc(Cl)c4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
42598359 16104 None 0 Human Functional pEC50 = 5.8 5.8 -125 5
Agonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 436 5 0 7 3.4 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(S(C)(=O)=O)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223864 16104 None 0 Human Functional pEC50 = 5.8 5.8 -125 5
Agonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 436 5 0 7 3.4 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(S(C)(=O)=O)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
42598586 16121 None 0 Human Functional pEC50 = 5.8 5.8 -7 4
Agonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 450 6 0 7 3.8 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(S(=O)(=O)CC)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223938 16121 None 0 Human Functional pEC50 = 5.8 5.8 -7 4
Agonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 450 6 0 7 3.8 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(S(=O)(=O)CC)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
89777262 156676 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 388 4 2 5 4.5 Cc1nnc2sc(C(=O)NCc3cccc(-c4ccccc4)c3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
CHEMBL4069641 156676 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 388 4 2 5 4.5 Cc1nnc2sc(C(=O)NCc3cccc(-c4ccccc4)c3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
25162692 53680 None 5 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 418 3 1 5 5.0 Cc1sc2ncnc(N3CCC(C(=O)Nc4ccc(F)cc4Cl)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
CHEMBL1603219 53680 None 5 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 418 3 1 5 5.0 Cc1sc2ncnc(N3CCC(C(=O)Nc4ccc(F)cc4Cl)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
137656230 159044 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 390 4 2 7 3.3 Cc1nnc2sc(C(=O)NCc3ccc(-c4cnccn4)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
CHEMBL4096878 159044 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 390 4 2 7 3.3 Cc1nnc2sc(C(=O)NCc3ccc(-c4cnccn4)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
CHEMBL5088899 215183 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL None None None Cc1cc(C)c2c(n1)oc1c(NC3CCC3)ncnc12 10.1016/j.bmcl.2021.128416
155524827 170915 None 0 Human Functional pEC50 = 7.8 7.8 12 2
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 367 4 0 6 3.1 COc1cccnc1C1CCN(C2CCCN(c3cnccn3)CC2)CC1 10.1021/acsmedchemlett.9b00106
CHEMBL4455058 170915 None 0 Human Functional pEC50 = 7.8 7.8 12 2
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 367 4 0 6 3.1 COc1cccnc1C1CCN(C2CCCN(c3cnccn3)CC2)CC1 10.1021/acsmedchemlett.9b00106
134207713 170318 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 321 2 2 6 2.4 Cc1c(Cl)c2nncn2c2sc(C(=O)NC3CC3)c(N)c12 10.1016/j.bmcl.2019.06.032
CHEMBL4446894 170318 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 321 2 2 6 2.4 Cc1c(Cl)c2nncn2c2sc(C(=O)NC3CC3)c(N)c12 10.1016/j.bmcl.2019.06.032
137656783 159682 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 372 3 2 7 2.0 Cc1nnc2sc(C(=O)NC3CN(c4cncc(F)c4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4104144 159682 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 372 3 2 7 2.0 Cc1nnc2sc(C(=O)NC3CN(c4cncc(F)c4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
137646286 157815 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 384 4 2 8 1.9 COc1cncc(N2CC(NC(=O)c3sc4nnc(C)c(C)c4c3N)C2)c1 10.1016/j.bmcl.2017.05.014
CHEMBL4083327 157815 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 384 4 2 8 1.9 COc1cncc(N2CC(NC(=O)c3sc4nnc(C)c(C)c4c3N)C2)c1 10.1016/j.bmcl.2017.05.014
155557669 174660 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 419 4 1 8 3.4 Cc1nnc2sc3c(NCc4ccc(S(C)(=O)=O)c(F)c4)nn(C)c3c2c1C 10.1016/j.bmcl.2018.12.039
CHEMBL4558665 174660 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 419 4 1 8 3.4 Cc1nnc2sc3c(NCc4ccc(S(C)(=O)=O)c(F)c4)nn(C)c3c2c1C 10.1016/j.bmcl.2018.12.039
134207694 170298 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 399 4 2 7 3.2 COc1ccc(CNC(=O)c2sc3c(c(C)cc4nc(C)nn43)c2N)cc1F 10.1016/j.bmcl.2019.06.032
CHEMBL4446559 170298 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 399 4 2 7 3.2 COc1ccc(CNC(=O)c2sc3c(c(C)cc4nc(C)nn43)c2N)cc1F 10.1016/j.bmcl.2019.06.032
134207702 172358 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 442 3 2 9 2.5 Cc1nc(Cl)cc(N2CC(NC(=O)c3sc4c(c(C)cc5nc(C)nn54)c3N)C2)n1 10.1016/j.bmcl.2019.06.032
CHEMBL4475984 172358 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 442 3 2 9 2.5 Cc1nc(Cl)cc(N2CC(NC(=O)c3sc4c(c(C)cc5nc(C)nn54)c3N)C2)n1 10.1016/j.bmcl.2019.06.032
53382480 86327 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 381 3 2 4 4.4 Cc1nc2sc(C(=O)NCc3ccc(F)c(F)c3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313393 86327 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 381 3 2 4 4.4 Cc1nc2sc(C(=O)NCc3ccc(F)c(F)c3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
1505737 86328 None 12 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 379 3 2 4 4.7 Cc1nc2sc(C(=O)NCc3ccccc3Cl)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313394 86328 None 12 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 379 3 2 4 4.7 Cc1nc2sc(C(=O)NCc3ccccc3Cl)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
16309462 26186 None 4 Rat Functional pEC50 = 6.8 6.8 4 2
Positive allosteric modulation of rat M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 445 4 2 7 2.8 Cc1sc2ncnc(N3CCC(C(=O)Nc4ccc(S(N)(=O)=O)cc4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
CHEMBL1357034 26186 None 4 Rat Functional pEC50 = 6.8 6.8 4 2
Positive allosteric modulation of rat M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 445 4 2 7 2.8 Cc1sc2ncnc(N3CCC(C(=O)Nc4ccc(S(N)(=O)=O)cc4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
25162692 53680 None 5 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 418 3 1 5 5.0 Cc1sc2ncnc(N3CCC(C(=O)Nc4ccc(F)cc4Cl)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
CHEMBL1603219 53680 None 5 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 418 3 1 5 5.0 Cc1sc2ncnc(N3CCC(C(=O)Nc4ccc(F)cc4Cl)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
CHEMBL5082166 214788 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL None None None COc1ccc(C2CC2Nc2ncnc3c2sc2nc(C)cc(C)c23)cc1 10.1016/j.bmcl.2021.128416
155510640 174032 None 0 Rat Functional pEC50 = 6.8 6.8 -1 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 283 2 1 5 3.1 Cc1nnc2sc(C(=O)c3ccccc3)c(N)c2c1C 10.1016/j.bmcl.2016.07.042
CHEMBL4543522 174032 None 0 Rat Functional pEC50 = 6.8 6.8 -1 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 283 2 1 5 3.1 Cc1nnc2sc(C(=O)c3ccccc3)c(N)c2c1C 10.1016/j.bmcl.2016.07.042
137647620 157596 None 0 Human Functional pEC50 = 6.8 6.8 2 2
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 362 3 0 5 4.0 Cc1ccc(OC2CCN(c3c(C#N)cnc4ccc(F)cc34)CC2)cn1 10.1016/j.bmcl.2017.08.043
CHEMBL4080878 157596 None 0 Human Functional pEC50 = 6.8 6.8 2 2
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 362 3 0 5 4.0 Cc1ccc(OC2CCN(c3c(C#N)cnc4ccc(F)cc34)CC2)cn1 10.1016/j.bmcl.2017.08.043
89777262 156676 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 388 4 2 5 4.5 Cc1nnc2sc(C(=O)NCc3cccc(-c4ccccc4)c3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
CHEMBL4069641 156676 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 388 4 2 5 4.5 Cc1nnc2sc(C(=O)NCc3cccc(-c4ccccc4)c3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
137646601 158000 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 378 3 1 6 2.8 Cn1nccc1NC(=O)C1CCN(c2c(C#N)cnc3ccc(F)cc23)CC1 10.1016/j.bmcl.2017.08.043
CHEMBL4085378 158000 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 378 3 1 6 2.8 Cn1nccc1NC(=O)C1CCN(c2c(C#N)cnc3ccc(F)cc23)CC1 10.1016/j.bmcl.2017.08.043
155510640 174032 None 0 Rat Functional pEC50 = 6.8 6.8 -1 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 283 2 1 5 3.1 Cc1nnc2sc(C(=O)c3ccccc3)c(N)c2c1C 10.1016/j.bmcl.2016.07.042
CHEMBL4543522 174032 None 0 Rat Functional pEC50 = 6.8 6.8 -1 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 283 2 1 5 3.1 Cc1nnc2sc(C(=O)c3ccccc3)c(N)c2c1C 10.1016/j.bmcl.2016.07.042
137640564 157041 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 390 3 2 5 3.6 Cc1nnc2sc(C(=O)NCc3cccc(Br)c3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
CHEMBL4073827 157041 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 390 3 2 5 3.6 Cc1nnc2sc(C(=O)NCc3cccc(Br)c3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
26441386 140369 None 2 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 360 2 0 6 2.4 Cc1sc2ncnc(N3CCC(C(=O)N4CCOCC4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
CHEMBL3808425 140369 None 2 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 360 2 0 6 2.4 Cc1sc2ncnc(N3CCC(C(=O)N4CCOCC4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
134207723 175384 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 363 2 2 6 2.7 Cc1cc2nncn2c2sc(C(=O)NC3Cc4ccccc4C3)c(N)c12 10.1016/j.bmcl.2019.06.032
CHEMBL4575270 175384 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 363 2 2 6 2.7 Cc1cc2nncn2c2sc(C(=O)NC3Cc4ccccc4C3)c(N)c12 10.1016/j.bmcl.2019.06.032
137646286 157815 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 384 4 2 8 1.9 COc1cncc(N2CC(NC(=O)c3sc4nnc(C)c(C)c4c3N)C2)c1 10.1016/j.bmcl.2017.05.014
CHEMBL4083327 157815 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 384 4 2 8 1.9 COc1cncc(N2CC(NC(=O)c3sc4nnc(C)c(C)c4c3N)C2)c1 10.1016/j.bmcl.2017.05.014
129277689 164017 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Positive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assayPositive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assay
ChEMBL 395 3 1 6 2.5 Cc1cc2c(nc1N1CC[C@@H](Oc3ccc4c(cnn4C)c3)[C@@H](F)C1)CNC2=O 10.1021/acsmedchemlett.8b00330
CHEMBL4208543 164017 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Positive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assayPositive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assay
ChEMBL 395 3 1 6 2.5 Cc1cc2c(nc1N1CC[C@@H](Oc3ccc4c(cnn4C)c3)[C@@H](F)C1)CNC2=O 10.1021/acsmedchemlett.8b00330
12301 4045 None 30 Rat Functional pEC50 = 7.8 7.8 7 2
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 444 4 2 7 3.1 Cc1c(nnc2c1c(c(s2)C(=O)NCc1ccc(cc1)S(=O)(=O)C(F)(F)F)N)C 10.1016/j.bmcl.2016.11.086
73774630 4045 None 30 Rat Functional pEC50 = 7.8 7.8 7 2
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 444 4 2 7 3.1 Cc1c(nnc2c1c(c(s2)C(=O)NCc1ccc(cc1)S(=O)(=O)C(F)(F)F)N)C 10.1016/j.bmcl.2016.11.086
CHEMBL3915634 4045 None 30 Rat Functional pEC50 = 7.8 7.8 7 2
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 444 4 2 7 3.1 Cc1c(nnc2c1c(c(s2)C(=O)NCc1ccc(cc1)S(=O)(=O)C(F)(F)F)N)C 10.1016/j.bmcl.2016.11.086
89768534 151632 None 0 Rat Functional pEC50 = 7.8 7.8 14 2
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 426 5 2 7 2.8 Cc1nnc2sc(C(=O)NCc3ccc(S(=O)(=O)C(F)F)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
CHEMBL3963788 151632 None 0 Rat Functional pEC50 = 7.8 7.8 14 2
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 426 5 2 7 2.8 Cc1nnc2sc(C(=O)NCc3ccc(S(=O)(=O)C(F)F)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
12301 4045 None 30 Rat Functional pEC50 = 7.8 7.8 7 2
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 444 4 2 7 3.1 Cc1c(nnc2c1c(c(s2)C(=O)NCc1ccc(cc1)S(=O)(=O)C(F)(F)F)N)C 10.1016/j.bmcl.2016.11.086
73774630 4045 None 30 Rat Functional pEC50 = 7.8 7.8 7 2
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 444 4 2 7 3.1 Cc1c(nnc2c1c(c(s2)C(=O)NCc1ccc(cc1)S(=O)(=O)C(F)(F)F)N)C 10.1016/j.bmcl.2016.11.086
CHEMBL3915634 4045 None 30 Rat Functional pEC50 = 7.8 7.8 7 2
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 444 4 2 7 3.1 Cc1c(nnc2c1c(c(s2)C(=O)NCc1ccc(cc1)S(=O)(=O)C(F)(F)F)N)C 10.1016/j.bmcl.2016.11.086
89768534 151632 None 0 Rat Functional pEC50 = 7.8 7.8 14 2
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 426 5 2 7 2.8 Cc1nnc2sc(C(=O)NCc3ccc(S(=O)(=O)C(F)F)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
CHEMBL3963788 151632 None 0 Rat Functional pEC50 = 7.8 7.8 14 2
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 426 5 2 7 2.8 Cc1nnc2sc(C(=O)NCc3ccc(S(=O)(=O)C(F)F)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
162644740 179423 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 441 4 2 8 2.5 Cc1c(CF)nnc2sc(C(=O)NC3CN(c4ncc(C(F)(F)F)cn4)C3)c(N)c12 10.1016/j.bmcl.2019.05.026
CHEMBL4740272 179423 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 441 4 2 8 2.5 Cc1c(CF)nnc2sc(C(=O)NC3CN(c4ncc(C(F)(F)F)cn4)C3)c(N)c12 10.1016/j.bmcl.2019.05.026
26441386 140369 None 2 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 360 2 0 6 2.4 Cc1sc2ncnc(N3CCC(C(=O)N4CCOCC4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
CHEMBL3808425 140369 None 2 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 360 2 0 6 2.4 Cc1sc2ncnc(N3CCC(C(=O)N4CCOCC4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
137632847 156436 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 407 4 2 6 4.0 Cc1nnc2sc(C(=O)NCc3ccc(-c4ccncc4F)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
CHEMBL4066953 156436 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 407 4 2 6 4.0 Cc1nnc2sc(C(=O)NCc3ccc(-c4ccncc4F)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
156020948 178115 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 348 4 2 7 2.8 Cn1nnc2ccc3c(NCc4ccc(C(C)(C)O)cc4)ncnc3c21 10.1016/j.bmcl.2019.126811
CHEMBL4648135 178115 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 348 4 2 7 2.8 Cn1nnc2ccc3c(NCc4ccc(C(C)(C)O)cc4)ncnc3c21 10.1016/j.bmcl.2019.126811
CHEMBL5082904 214829 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL None None None Cc1cc(C)c2c(n1)sc1c(N3CCC3)ncnc12 10.1016/j.bmcl.2021.128416
156020141 178054 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 348 3 2 8 0.4 Cn1nnc2ccc(C(=O)NC3CN(c4ccc(C#N)cn4)C3)c(N)c21 10.1016/j.bmcl.2019.126811
CHEMBL4647288 178054 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 348 3 2 8 0.4 Cn1nnc2ccc(C(=O)NC3CN(c4ccc(C#N)cn4)C3)c(N)c21 10.1016/j.bmcl.2019.126811
127043636 140484 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 358 3 0 6 3.9 Cc1sc2ncnc(N3CCC(Oc4ccc(F)nc4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
CHEMBL3809693 140484 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 358 3 0 6 3.9 Cc1sc2ncnc(N3CCC(Oc4ccc(F)nc4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
53382478 86332 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 413 3 2 4 5.1 Cc1nc2sc(C(=O)NCc3ccc(C(F)(F)F)cc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313398 86332 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 413 3 2 4 5.1 Cc1nc2sc(C(=O)NCc3ccc(C(F)(F)F)cc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
53382478 86332 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 413 3 2 4 5.1 Cc1nc2sc(C(=O)NCc3ccc(C(F)(F)F)cc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313398 86332 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 413 3 2 4 5.1 Cc1nc2sc(C(=O)NCc3ccc(C(F)(F)F)cc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
137646601 158000 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 378 3 1 6 2.8 Cn1nccc1NC(=O)C1CCN(c2c(C#N)cnc3ccc(F)cc23)CC1 10.1016/j.bmcl.2017.08.043
CHEMBL4085378 158000 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 378 3 1 6 2.8 Cn1nccc1NC(=O)C1CCN(c2c(C#N)cnc3ccc(F)cc23)CC1 10.1016/j.bmcl.2017.08.043
89777147 156377 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 382 3 2 7 1.5 Cc1nnc2sc(C(=O)NC3CN(C(=O)c4ccncc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4066301 156377 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 382 3 2 7 1.5 Cc1nnc2sc(C(=O)NC3CN(C(=O)c4ccncc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
89777355 164620 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 344 2 1 5 3.5 Cc1nnc2sc(C(=O)N3CC(C4CCCCC4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
CHEMBL4216038 164620 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 344 2 1 5 3.5 Cc1nnc2sc(C(=O)N3CC(C4CCCCC4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
1506223 86330 None 12 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 379 3 2 4 4.7 Cc1nc2sc(C(=O)NCc3ccc(Cl)cc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313396 86330 None 12 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 379 3 2 4 4.7 Cc1nc2sc(C(=O)NCc3ccc(Cl)cc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
89777355 164620 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 344 2 1 5 3.5 Cc1nnc2sc(C(=O)N3CC(C4CCCCC4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
CHEMBL4216038 164620 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 344 2 1 5 3.5 Cc1nnc2sc(C(=O)N3CC(C4CCCCC4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
89777147 156377 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 382 3 2 7 1.5 Cc1nnc2sc(C(=O)NC3CN(C(=O)c4ccncc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4066301 156377 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 382 3 2 7 1.5 Cc1nnc2sc(C(=O)NC3CN(C(=O)c4ccncc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
3652 4095 None 79 Human Functional pEC50 = 7.8 7.8 -8 15
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/acsmedchemlett.9b00106
57 4095 None 79 Human Functional pEC50 = 7.8 7.8 -8 15
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/acsmedchemlett.9b00106
60809 4095 None 79 Human Functional pEC50 = 7.8 7.8 -8 15
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/acsmedchemlett.9b00106
CHEMBL21536 4095 None 79 Human Functional pEC50 = 7.8 7.8 -8 15
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/acsmedchemlett.9b00106
DB15357 4095 None 79 Human Functional pEC50 = 7.8 7.8 -8 15
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/acsmedchemlett.9b00106
135154300 163960 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Positive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assayPositive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assay
ChEMBL 461 6 1 8 2.9 Cc1cc(C(=O)NCc2ccncc2)nnc1N1CCC(Oc2ccc3c(c2)OCCO3)CC1 10.1021/acsmedchemlett.8b00330
CHEMBL4207853 163960 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Positive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assayPositive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assay
ChEMBL 461 6 1 8 2.9 Cc1cc(C(=O)NCc2ccncc2)nnc1N1CCC(Oc2ccc3c(c2)OCCO3)CC1 10.1021/acsmedchemlett.8b00330
135171475 163979 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Positive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assayPositive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assay
ChEMBL 383 4 2 7 1.4 COc1ccc(OC2CCN(c3nc4[nH]c(=O)[nH]c(=O)c4cc3C)CC2)cn1 10.1021/acsmedchemlett.8b00330
CHEMBL4208024 163979 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Positive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assayPositive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assay
ChEMBL 383 4 2 7 1.4 COc1ccc(OC2CCN(c3nc4[nH]c(=O)[nH]c(=O)c4cc3C)CC2)cn1 10.1021/acsmedchemlett.8b00330
135171550 164168 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Positive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assayPositive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assay
ChEMBL 328 4 1 5 2.4 Cc1cc2c(=O)[nH]ncc2nc1N1CCC(OCC2(C)CC2)CC1 10.1021/acsmedchemlett.8b00330
CHEMBL4210497 164168 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Positive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assayPositive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assay
ChEMBL 328 4 1 5 2.4 Cc1cc2c(=O)[nH]ncc2nc1N1CCC(OCC2(C)CC2)CC1 10.1021/acsmedchemlett.8b00330
137658662 159428 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 372 3 2 7 2.0 Cc1nnc2sc(C(=O)NC3CN(c4cccnc4F)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4101054 159428 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 372 3 2 7 2.0 Cc1nnc2sc(C(=O)NC3CN(c4cccnc4F)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
137635043 156028 None 13 Human Functional pEC50 = 7.7 7.7 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 389 3 2 6 2.8 Cc1nnc2sc(C(=O)NC3CN(c4cccc(F)c4F)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4062319 156028 None 13 Human Functional pEC50 = 7.7 7.7 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 389 3 2 6 2.8 Cc1nnc2sc(C(=O)NC3CN(c4cccc(F)c4F)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
155522181 170686 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 317 3 1 7 2.8 Cc1nnc2sc3c(NCC4CCCO4)nn(C)c3c2c1C 10.1016/j.bmcl.2018.12.039
CHEMBL4451787 170686 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 317 3 1 7 2.8 Cc1nnc2sc3c(NCC4CCCO4)nn(C)c3c2c1C 10.1016/j.bmcl.2018.12.039
162650513 180047 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 483 7 2 10 2.0 COCCOc1nnc2sc(C(=O)NC3CN(c4ncc(C(F)(F)F)cn4)C3)c(N)c2c1C 10.1016/j.bmcl.2019.05.026
CHEMBL4747706 180047 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 483 7 2 10 2.0 COCCOc1nnc2sc(C(=O)NC3CN(c4ncc(C(F)(F)F)cn4)C3)c(N)c2c1C 10.1016/j.bmcl.2019.05.026
1506223 86330 None 12 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 379 3 2 4 4.7 Cc1nc2sc(C(=O)NCc3ccc(Cl)cc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313396 86330 None 12 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 379 3 2 4 4.7 Cc1nc2sc(C(=O)NCc3ccc(Cl)cc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
127043636 140484 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 358 3 0 6 3.9 Cc1sc2ncnc(N3CCC(Oc4ccc(F)nc4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
CHEMBL3809693 140484 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 358 3 0 6 3.9 Cc1sc2ncnc(N3CCC(Oc4ccc(F)nc4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
155540233 172903 None 0 Rat Functional pEC50 = 6.7 6.7 -3 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 325 2 2 6 3.1 Nc1c(C(=O)c2ccncc2)sc2nc(O)c3c(c12)CCCC3 10.1016/j.bmcl.2016.07.042
CHEMBL4516136 172903 None 0 Rat Functional pEC50 = 6.7 6.7 -3 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 325 2 2 6 3.1 Nc1c(C(=O)c2ccncc2)sc2nc(O)c3c(c12)CCCC3 10.1016/j.bmcl.2016.07.042
89768749 159290 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 390 3 2 5 3.6 Cc1nnc2sc(C(=O)NCc3ccc(Br)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
CHEMBL4099560 159290 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 390 3 2 5 3.6 Cc1nnc2sc(C(=O)NCc3ccc(Br)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
5204148 33993 None 12 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 assessed as potentiation of acetylcholine-mediated calcium mobilization incubated for 144 secs prior to acetylcholine addition by Fluo-4-AM stainingPositive allosteric modulation of human M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 assessed as potentiation of acetylcholine-mediated calcium mobilization incubated for 144 secs prior to acetylcholine addition by Fluo-4-AM staining
ChEMBL 306 3 1 6 2.4 COc1ccc(C)c2sc(NC(=O)C3=COCCO3)nc12 10.1016/j.bmcl.2012.05.109
CHEMBL1424504 33993 None 12 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 assessed as potentiation of acetylcholine-mediated calcium mobilization incubated for 144 secs prior to acetylcholine addition by Fluo-4-AM stainingPositive allosteric modulation of human M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 assessed as potentiation of acetylcholine-mediated calcium mobilization incubated for 144 secs prior to acetylcholine addition by Fluo-4-AM staining
ChEMBL 306 3 1 6 2.4 COc1ccc(C)c2sc(NC(=O)C3=COCCO3)nc12 10.1016/j.bmcl.2012.05.109
155540233 172903 None 0 Rat Functional pEC50 = 6.7 6.7 -3 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 325 2 2 6 3.1 Nc1c(C(=O)c2ccncc2)sc2nc(O)c3c(c12)CCCC3 10.1016/j.bmcl.2016.07.042
CHEMBL4516136 172903 None 0 Rat Functional pEC50 = 6.7 6.7 -3 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 325 2 2 6 3.1 Nc1c(C(=O)c2ccncc2)sc2nc(O)c3c(c12)CCCC3 10.1016/j.bmcl.2016.07.042
45142487 25949 None 0 Rat Functional pEC50 = 6.7 6.7 - 1
PUBCHEM_BIOASSAY: Discovery of a Highly Selective in vitro and in vivo M4 Positive Allosteric Modulator(PAM): Activity with human M4. (Class of assay: confirmatory) PUBCHEM_BIOASSAY: Discovery of a Highly Selective in vitro and in vivo M4 Positive Allosteric Modulator(PAM): Activity with human M4. (Class of assay: confirmatory)
ChEMBL 440 6 2 6 4.4 Cc1cc(OCc2ccncc2)nc2sc(C(=O)NCc3cc(F)ccc3F)c(N)c12 nan
CHEMBL1354105 25949 None 0 Rat Functional pEC50 = 6.7 6.7 - 1
PUBCHEM_BIOASSAY: Discovery of a Highly Selective in vitro and in vivo M4 Positive Allosteric Modulator(PAM): Activity with human M4. (Class of assay: confirmatory) PUBCHEM_BIOASSAY: Discovery of a Highly Selective in vitro and in vivo M4 Positive Allosteric Modulator(PAM): Activity with human M4. (Class of assay: confirmatory)
ChEMBL 440 6 2 6 4.4 Cc1cc(OCc2ccncc2)nc2sc(C(=O)NCc3cc(F)ccc3F)c(N)c12 nan
156017839 177858 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 386 4 1 7 2.0 COc1cc(N2CC(NC(=O)c3cnc4nc(C)c(C)n4c3)C2)c(Cl)cn1 10.1016/j.bmcl.2019.126812
CHEMBL4644300 177858 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 386 4 1 7 2.0 COc1cc(N2CC(NC(=O)c3cnc4nc(C)c(C)n4c3)C2)c(Cl)cn1 10.1016/j.bmcl.2019.126812
137649420 157519 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 388 3 2 7 2.6 Cc1nnc2sc(C(=O)NC3CN(c4ccnc(Cl)c4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4079904 157519 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 388 3 2 7 2.6 Cc1nnc2sc(C(=O)NC3CN(c4ccnc(Cl)c4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
137640564 157041 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 390 3 2 5 3.6 Cc1nnc2sc(C(=O)NCc3cccc(Br)c3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
CHEMBL4073827 157041 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 390 3 2 5 3.6 Cc1nnc2sc(C(=O)NCc3cccc(Br)c3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
127043450 140394 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 394 2 0 5 3.8 Cc1sc2ncnc(N3CCC(C(=O)N4CCCC(F)(F)C4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
CHEMBL3808696 140394 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 394 2 0 5 3.8 Cc1sc2ncnc(N3CCC(C(=O)N4CCCC(F)(F)C4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
89768749 159290 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 390 3 2 5 3.6 Cc1nnc2sc(C(=O)NCc3ccc(Br)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
CHEMBL4099560 159290 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 390 3 2 5 3.6 Cc1nnc2sc(C(=O)NCc3ccc(Br)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
137635043 156028 None 13 Human Functional pEC50 = 7.7 7.7 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 389 3 2 6 2.8 Cc1nnc2sc(C(=O)NC3CN(c4cccc(F)c4F)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4062319 156028 None 13 Human Functional pEC50 = 7.7 7.7 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 389 3 2 6 2.8 Cc1nnc2sc(C(=O)NC3CN(c4cccc(F)c4F)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
44253016 80455 None 2 Human Functional pEC50 = 7.7 7.7 -1 4
Agonist activity at human muscarinic M4 receptor expressed in CHO cells coexpressing Galpha16 subunit assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells coexpressing Galpha16 subunit assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assay
ChEMBL 299 2 1 3 3.3 O=c1[nH]c2ccccc2n1C1CCN(C2CCCCC2)CC1 10.1021/ml100105x
CHEMBL2146597 80455 None 2 Human Functional pEC50 = 7.7 7.7 -1 4
Agonist activity at human muscarinic M4 receptor expressed in CHO cells coexpressing Galpha16 subunit assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells coexpressing Galpha16 subunit assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assay
ChEMBL 299 2 1 3 3.3 O=c1[nH]c2ccccc2n1C1CCN(C2CCCCC2)CC1 10.1021/ml100105x
134207681 175656 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 483 4 2 8 3.4 Cc1nc2cc(C)c3c(N)c(C(=O)NCc4ccc(S(=O)(=O)C(F)(F)F)cc4)sc3n2n1 10.1016/j.bmcl.2019.06.032
CHEMBL4581412 175656 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 483 4 2 8 3.4 Cc1nc2cc(C)c3c(N)c(C(=O)NCc4ccc(S(=O)(=O)C(F)(F)F)cc4)sc3n2n1 10.1016/j.bmcl.2019.06.032
127043450 140394 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 394 2 0 5 3.8 Cc1sc2ncnc(N3CCC(C(=O)N4CCCC(F)(F)C4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
CHEMBL3808696 140394 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells coexpressing Gqi5 by calcium mobilization assay
ChEMBL 394 2 0 5 3.8 Cc1sc2ncnc(N3CCC(C(=O)N4CCCC(F)(F)C4)CC3)c2c1C 10.1016/j.bmcl.2016.05.010
45142483 52632 None 0 Rat Functional pEC50 = 6.7 6.7 - 1
PUBCHEM_BIOASSAY: Discovery of a Highly Selective in vitro and in vivo M4 Positive Allosteric Modulator(PAM): Activity with human M4. (Class of assay: confirmatory) PUBCHEM_BIOASSAY: Discovery of a Highly Selective in vitro and in vivo M4 Positive Allosteric Modulator(PAM): Activity with human M4. (Class of assay: confirmatory)
ChEMBL 392 5 2 7 2.4 Cc1cc(OCCN2CCOCC2)nc2sc(C(=O)NC(C)(C)C)c(N)c12 nan
CHEMBL1593296 52632 None 0 Rat Functional pEC50 = 6.7 6.7 - 1
PUBCHEM_BIOASSAY: Discovery of a Highly Selective in vitro and in vivo M4 Positive Allosteric Modulator(PAM): Activity with human M4. (Class of assay: confirmatory) PUBCHEM_BIOASSAY: Discovery of a Highly Selective in vitro and in vivo M4 Positive Allosteric Modulator(PAM): Activity with human M4. (Class of assay: confirmatory)
ChEMBL 392 5 2 7 2.4 Cc1cc(OCCN2CCOCC2)nc2sc(C(=O)NC(C)(C)C)c(N)c12 nan
155563393 175321 None 0 Rat Functional pEC50 = 6.7 6.7 1 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 334 2 1 4 4.5 Cc1cc(C)c2c(N)c(C(=O)c3ccc(F)c(Cl)c3)sc2n1 10.1016/j.bmcl.2016.07.042
CHEMBL4573723 175321 None 0 Rat Functional pEC50 = 6.7 6.7 1 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 334 2 1 4 4.5 Cc1cc(C)c2c(N)c(C(=O)c3ccc(F)c(Cl)c3)sc2n1 10.1016/j.bmcl.2016.07.042
155563393 175321 None 0 Rat Functional pEC50 = 6.7 6.7 1 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 334 2 1 4 4.5 Cc1cc(C)c2c(N)c(C(=O)c3ccc(F)c(Cl)c3)sc2n1 10.1016/j.bmcl.2016.07.042
CHEMBL4573723 175321 None 0 Rat Functional pEC50 = 6.7 6.7 1 2
Positive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assayPositive allosteric modulation activity at rat M4 receptor expressed in CHO cells co-expressing Gqi5 protein assessed as potentiation of EC20 acetyl choline-induced response by calcium mobilization assay
ChEMBL 334 2 1 4 4.5 Cc1cc(C)c2c(N)c(C(=O)c3ccc(F)c(Cl)c3)sc2n1 10.1016/j.bmcl.2016.07.042
137647620 157596 None 0 Human Functional pEC50 = 6.7 6.7 2 2
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 362 3 0 5 4.0 Cc1ccc(OC2CCN(c3c(C#N)cnc4ccc(F)cc34)CC2)cn1 10.1016/j.bmcl.2017.08.043
CHEMBL4080878 157596 None 0 Human Functional pEC50 = 6.7 6.7 2 2
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 362 3 0 5 4.0 Cc1ccc(OC2CCN(c3c(C#N)cnc4ccc(F)cc34)CC2)cn1 10.1016/j.bmcl.2017.08.043
42598828 16101 None 0 Human Functional pEC50 = 6.7 6.7 -158 5
Agonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 390 4 0 5 4.4 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4c(F)cc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223861 16101 None 0 Human Functional pEC50 = 6.7 6.7 -158 5
Agonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 390 4 0 5 4.4 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4c(F)cc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
25230693 16123 None 0 Human Functional pEC50 = 6.7 6.7 -79 5
Agonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 402 6 0 6 3.9 COCCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223940 16123 None 0 Human Functional pEC50 = 6.7 6.7 -79 5
Agonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 chimeric G-protein assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 402 6 0 6 3.9 COCCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
16038385 80456 None 0 Human Functional pEC50 = 6.7 6.7 -3 3
Agonist activity at human muscarinic M4 receptor expressed in CHO cells coexpressing Galpha16 subunit assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells coexpressing Galpha16 subunit assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assay
ChEMBL 301 2 1 4 2.1 O=c1[nH]c2ccccc2n1C1CCN(C2CCOCC2)CC1 10.1021/ml100105x
CHEMBL2146598 80456 None 0 Human Functional pEC50 = 6.7 6.7 -3 3
Agonist activity at human muscarinic M4 receptor expressed in CHO cells coexpressing Galpha16 subunit assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assayAgonist activity at human muscarinic M4 receptor expressed in CHO cells coexpressing Galpha16 subunit assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assay
ChEMBL 301 2 1 4 2.1 O=c1[nH]c2ccccc2n1C1CCN(C2CCOCC2)CC1 10.1021/ml100105x
145978398 163957 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 344 2 1 6 3.2 Cc1nnc2sc(C(=O)N3CC(c4cccs4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
CHEMBL4207811 163957 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 344 2 1 6 3.2 Cc1nnc2sc(C(=O)N3CC(c4cccs4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
53382534 86335 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 311 2 2 5 2.3 Cc1nc2sc(C(=O)NC3COC3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313403 86335 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
ChEMBL 311 2 2 5 2.3 Cc1nc2sc(C(=O)NC3COC3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
155519300 170370 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 373 4 0 7 3.2 COc1cccnc1C1CCN(C2CCCN(c3cnsn3)CC2)CC1 10.1021/acsmedchemlett.9b00106
CHEMBL4447724 170370 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assayAgonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay
ChEMBL 373 4 0 7 3.2 COc1cccnc1C1CCN(C2CCCN(c3cnsn3)CC2)CC1 10.1021/acsmedchemlett.9b00106
134207721 169808 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 397 2 2 6 3.9 Cc1c(Cl)c2nncn2c2sc(C(=O)N[C@H]3CCc4ccccc43)c(N)c12 10.1016/j.bmcl.2019.06.032
CHEMBL4439440 169808 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Positive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 AchR expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 397 2 2 6 3.9 Cc1c(Cl)c2nncn2c2sc(C(=O)N[C@H]3CCc4ccccc43)c(N)c12 10.1016/j.bmcl.2019.06.032
162643836 181714 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 476 3 2 7 3.9 Cc1c(Cl)nnc2sc(C(=O)NC3CN(c4cc(C(F)(F)F)ncc4Cl)C3)c(N)c12 10.1016/j.bmcl.2019.05.026
CHEMBL4776981 181714 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 476 3 2 7 3.9 Cc1c(Cl)nnc2sc(C(=O)NC3CN(c4cc(C(F)(F)F)ncc4Cl)C3)c(N)c12 10.1016/j.bmcl.2019.05.026
162661731 181862 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 354 3 2 6 2.5 COc1nnc2sc(C(=O)NC3Cc4ccccc4C3)c(N)c2c1C 10.1016/j.bmcl.2019.05.026
CHEMBL4778766 181862 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 354 3 2 6 2.5 COc1nnc2sc(C(=O)NC3Cc4ccccc4C3)c(N)c2c1C 10.1016/j.bmcl.2019.05.026
162664667 182154 None 0 Human Functional pEC50 = 7.7 7.7 54 2
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 374 3 2 7 2.2 Cc1c(Cl)nnc2sc(C(=O)NC3CN(c4cccnc4)C3)c(N)c12 10.1016/j.bmcl.2019.05.026
CHEMBL4782416 182154 None 0 Human Functional pEC50 = 7.7 7.7 54 2
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 374 3 2 7 2.2 Cc1c(Cl)nnc2sc(C(=O)NC3CN(c4cccnc4)C3)c(N)c12 10.1016/j.bmcl.2019.05.026
162665586 182393 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 338 2 2 5 2.8 Cc1nnc2sc(C(=O)NC3Cc4ccccc4C3)c(N)c2c1C 10.1016/j.bmcl.2019.05.026
CHEMBL4785432 182393 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Positive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulation of human M4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 338 2 2 5 2.8 Cc1nnc2sc(C(=O)NC3Cc4ccccc4C3)c(N)c2c1C 10.1016/j.bmcl.2019.05.026
135154593 163607 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Positive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assayPositive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assay
ChEMBL 367 3 1 7 1.8 Cc1cn2c(=O)[nH]nc2nc1N1CCC(Oc2ccc3c(c2)COC3)CC1 10.1021/acsmedchemlett.8b00330
CHEMBL4203670 163607 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Positive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assayPositive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assay
ChEMBL 367 3 1 7 1.8 Cc1cn2c(=O)[nH]nc2nc1N1CCC(Oc2ccc3c(c2)COC3)CC1 10.1021/acsmedchemlett.8b00330
135150478 163915 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Positive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assayPositive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assay
ChEMBL 391 4 2 6 2.8 Cc1c(Cl)nc(CO)nc1N1CC[C@@H](Oc2ccc3[nH]ncc3c2)[C@@H](F)C1 10.1021/acsmedchemlett.8b00330
CHEMBL4207315 163915 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Positive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assayPositive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assay
ChEMBL 391 4 2 6 2.8 Cc1c(Cl)nc(CO)nc1N1CC[C@@H](Oc2ccc3[nH]ncc3c2)[C@@H](F)C1 10.1021/acsmedchemlett.8b00330
135150406 164302 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Positive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assayPositive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assay
ChEMBL 387 4 0 5 2.7 Cc1cc2c(nc1N1CCC(Oc3ccccc3)CC1)CN(S(C)(=O)=O)C2 10.1021/acsmedchemlett.8b00330
CHEMBL4212205 164302 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Positive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assayPositive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assay
ChEMBL 387 4 0 5 2.7 Cc1cc2c(nc1N1CCC(Oc3ccccc3)CC1)CN(S(C)(=O)=O)C2 10.1021/acsmedchemlett.8b00330
145978398 163957 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization
ChEMBL 344 2 1 6 3.2 Cc1nnc2sc(C(=O)N3CC(c4cccs4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.10.053
CHEMBL4207811 163957 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilizationPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization