Ligand source activities (1 row/activity)





Ligands Receptor Assay information Chemical information
Sel. page Common
name
GPCRdb ID #Vendors Reference
ligand
Fold selectivity
(Potency)
# tested GPCRs
(Potency)
Species p-value
(-log)
Type Activity
Relation
Activity
Value
Assay Type Assay Description Source Mol
weight
Rot
Bonds
H don H acc LogP Smiles DOI
10952349 34907 0 None 3467 2 Human 9.2 pEC50 = 9.2 Functional
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 34907 0 None 3467 2 Human 9.2 pEC50 = 9.2 Functional
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 30562 0 None 12882 2 Human 9.0 pEC50 = 9 Functional
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 30562 0 None 12882 2 Human 9.0 pEC50 = 9 Functional
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 33875 0 None 239 2 Human 8.9 pEC50 = 8.9 Functional
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 33875 0 None 239 2 Human 8.9 pEC50 = 8.9 Functional
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
187 253 34 None 1 6 Human 8.0 pEC50 = 8 Functional
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
294 253 34 None 1 6 Human 8.0 pEC50 = 8 Functional
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
65 253 34 None 1 6 Human 8.0 pEC50 = 8 Functional
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 253 34 None 1 6 Human 8.0 pEC50 = 8 Functional
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 253 34 None 1 6 Human 8.0 pEC50 = 8 Functional
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 253 34 None 1 6 Human 8.0 pEC50 = 8 Functional
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
187 253 34 None 1 6 Human 8.0 pEC50 = 8 Functional
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
294 253 34 None 1 6 Human 8.0 pEC50 = 8 Functional
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
65 253 34 None 1 6 Human 8.0 pEC50 = 8 Functional
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 253 34 None 1 6 Human 8.0 pEC50 = 8 Functional
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 253 34 None 1 6 Human 8.0 pEC50 = 8 Functional
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 253 34 None 1 6 Human 8.0 pEC50 = 8 Functional
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 181694 0 None - 1 Human 8.0 pEC50 = 8 Functional
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 181694 0 None - 1 Human 8.0 pEC50 = 8 Functional
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 182834 0 None - 1 Human 8.0 pEC50 = 8 Functional
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 182834 0 None - 1 Human 8.0 pEC50 = 8 Functional
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 157722 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
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 157722 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
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 15926 0 None -100 5 Human 7.0 pEC50 = 7 Functional
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 15926 0 None -100 5 Human 7.0 pEC50 = 7 Functional
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 158500 0 None - 1 Human 7.0 pEC50 = 7 Functional
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 158500 0 None - 1 Human 7.0 pEC50 = 7 Functional
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 179729 0 None - 1 Human 7.0 pEC50 = 7 Functional
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 179729 0 None - 1 Human 7.0 pEC50 = 7 Functional
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 174086 0 None - 1 Human 6.0 pEC50 = 6 Functional
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 174086 0 None - 1 Human 6.0 pEC50 = 6 Functional
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 169704 0 None - 1 Human 5.0 pEC50 = 5 Functional
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 169704 0 None - 1 Human 5.0 pEC50 = 5 Functional
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 173462 0 None 1 2 Human 7.0 pEC50 = 7.0 Functional
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 173462 0 None 1 2 Human 7.0 pEC50 = 7.0 Functional
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 173462 0 None 1 2 Human 7.0 pEC50 = 7.0 Functional
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 173462 0 None 1 2 Human 7.0 pEC50 = 7.0 Functional
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 157932 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
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 157932 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
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 158577 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
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 158577 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
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 85904 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
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 85904 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
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 172304 0 None 3 2 Human 7.0 pEC50 = 7.0 Functional
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 172304 0 None 3 2 Human 7.0 pEC50 = 7.0 Functional
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 174942 0 None 3 2 Human 7.0 pEC50 = 7.0 Functional
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 174942 0 None 3 2 Human 7.0 pEC50 = 7.0 Functional
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 85904 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
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 85904 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
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 164157 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
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 164157 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
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 157367 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
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 157367 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
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 164157 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
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 164157 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
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 139978 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
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 139978 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
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 172304 0 None 3 2 Human 7.0 pEC50 = 7.0 Functional
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 172304 0 None 3 2 Human 7.0 pEC50 = 7.0 Functional
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 174942 0 None 3 2 Human 7.0 pEC50 = 7.0 Functional
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 174942 0 None 3 2 Human 7.0 pEC50 = 7.0 Functional
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 155542 0 None 2 2 Human 7.0 pEC50 = 7.0 Functional
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 155542 0 None 2 2 Human 7.0 pEC50 = 7.0 Functional
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 2393 5 None -46 3 Human 6.0 pEC50 = 6.0 Functional
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 2393 5 None -46 3 Human 6.0 pEC50 = 6.0 Functional
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 2393 5 None -46 3 Human 6.0 pEC50 = 6.0 Functional
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 163633 0 None - 1 Rat 6.0 pEC50 = 6.0 Functional
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 163633 0 None - 1 Rat 6.0 pEC50 = 6.0 Functional
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 85884 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
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 85884 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
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 85884 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
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 85884 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
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 85901 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
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 85901 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
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 163016 0 None - 1 Rat 6.0 pEC50 = 6.0 Functional
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 163016 0 None - 1 Rat 6.0 pEC50 = 6.0 Functional
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 163016 0 None - 1 Rat 6.0 pEC50 = 6.0 Functional
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 163016 0 None - 1 Rat 6.0 pEC50 = 6.0 Functional
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 163633 0 None - 1 Rat 6.0 pEC50 = 6.0 Functional
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 163633 0 None - 1 Rat 6.0 pEC50 = 6.0 Functional
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 163782 0 None - 1 Rat 6.0 pEC50 = 6.0 Functional
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 163782 0 None - 1 Rat 6.0 pEC50 = 6.0 Functional
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 85901 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
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 85901 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
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 163782 0 None - 1 Rat 6.0 pEC50 = 6.0 Functional
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 163782 0 None - 1 Rat 6.0 pEC50 = 6.0 Functional
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 157367 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
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 157367 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
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 164252 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
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 164252 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
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 164252 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
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 164252 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
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 170775 0 None 229 2 Human 8.0 pEC50 = 8.0 Functional
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 170775 0 None 229 2 Human 8.0 pEC50 = 8.0 Functional
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 157722 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
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 157722 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
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 153308 0 None 5 2 Rat 8.0 pEC50 = 8.0 Functional
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 153308 0 None 5 2 Rat 8.0 pEC50 = 8.0 Functional
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 153308 0 None 5 2 Rat 8.0 pEC50 = 8.0 Functional
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 153308 0 None 5 2 Rat 8.0 pEC50 = 8.0 Functional
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 158027 0 None 7 2 Rat 7.9 pEC50 = 7.9 Functional
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 158027 0 None 7 2 Rat 7.9 pEC50 = 7.9 Functional
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 173707 0 None 10 2 Human 7.0 pEC50 = 7.0 Functional
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 173707 0 None 10 2 Human 7.0 pEC50 = 7.0 Functional
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 174068 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
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 174068 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
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 34927 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
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 34927 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
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 173596 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
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 173596 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
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 170368 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
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 170368 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
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 139948 7 None - 1 Human 6.0 pEC50 = 6.0 Functional
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 139948 7 None - 1 Human 6.0 pEC50 = 6.0 Functional
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 139978 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
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 139978 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
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 123087 0 None -21 3 Human 6.0 pEC50 = 6.0 Functional
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 123087 0 None -21 3 Human 6.0 pEC50 = 6.0 Functional
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 212893 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
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 75705 2 None - 1 Human 6.0 pEC50 = 6.0 Functional
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 75705 2 None - 1 Human 6.0 pEC50 = 6.0 Functional
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 163895 0 None - 1 Rat 6.0 pEC50 = 6.0 Functional
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 163895 0 None - 1 Rat 6.0 pEC50 = 6.0 Functional
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 122821 0 None -4 3 Human 7.0 pEC50 = 7.0 Functional
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 122821 0 None -4 3 Human 7.0 pEC50 = 7.0 Functional
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 163895 0 None - 1 Rat 6.0 pEC50 = 6.0 Functional
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 163895 0 None - 1 Rat 6.0 pEC50 = 6.0 Functional
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 213312 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 139948 7 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 139948 7 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 164171 0 None - 1 Rat 5.9 pEC50 = 5.9 Functional
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 164171 0 None - 1 Rat 5.9 pEC50 = 5.9 Functional
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 123090 0 None -5 3 Human 6.9 pEC50 = 6.9 Functional
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 123090 0 None -5 3 Human 6.9 pEC50 = 6.9 Functional
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 177267 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 177267 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 164171 0 None - 1 Rat 5.9 pEC50 = 5.9 Functional
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 164171 0 None - 1 Rat 5.9 pEC50 = 5.9 Functional
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 180471 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 180471 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 139915 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 139915 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 170656 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
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 170656 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
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 171761 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
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 171761 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
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 15879 0 None -31 5 Human 7.9 pEC50 = 7.9 Functional
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 15879 0 None -31 5 Human 7.9 pEC50 = 7.9 Functional
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 39970 15 None -1 2 Human 6.9 pEC50 = 6.9 Functional
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 39970 15 None -1 2 Human 6.9 pEC50 = 6.9 Functional
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 174864 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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 174864 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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 170728 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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 170728 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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 174073 0 None 5 2 Human 6.9 pEC50 = 6.9 Functional
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 174073 0 None 5 2 Human 6.9 pEC50 = 6.9 Functional
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 175335 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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 175335 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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 179101 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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 179101 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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 170105 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 170105 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 172497 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 172497 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 139915 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 139915 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 25983 5 None -4 2 Human 5.9 pEC50 = 5.9 Functional
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 25983 5 None -4 2 Human 5.9 pEC50 = 5.9 Functional
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 85885 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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 85885 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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 172749 0 None -4 2 Rat 5.9 pEC50 = 5.9 Functional
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 172749 0 None -4 2 Rat 5.9 pEC50 = 5.9 Functional
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 156234 11 None 2 2 Human 5.9 pEC50 = 5.9 Functional
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 156234 11 None 2 2 Human 5.9 pEC50 = 5.9 Functional
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 157932 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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 157932 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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 85885 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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 85885 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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 213356 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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 176495 0 None -3 2 Human 6.9 pEC50 = 6.9 Functional
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 176495 0 None -3 2 Human 6.9 pEC50 = 6.9 Functional
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 15905 0 None -5 3 Human 6.9 pEC50 = 6.9 Functional
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 15905 0 None -5 3 Human 6.9 pEC50 = 6.9 Functional
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 158998 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 158998 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 85893 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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 85893 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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 85893 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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 85893 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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 158458 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 158458 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 75704 1 None -5 2 Human 5.9 pEC50 = 5.9 Functional
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 75704 1 None -5 2 Human 5.9 pEC50 = 5.9 Functional
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 158998 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 158998 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 158458 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 158458 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 111533 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
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 111533 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
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 158027 0 None 7 2 Rat 7.9 pEC50 = 7.9 Functional
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 158027 0 None 7 2 Rat 7.9 pEC50 = 7.9 Functional
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 174806 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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 174806 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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 15110 20 None - 1 Rat 5.9 pEC50 = 5.9 Functional
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 15110 20 None - 1 Rat 5.9 pEC50 = 5.9 Functional
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 156725 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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 156725 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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 177622 0 None 1 2 Human 6.9 pEC50 = 6.9 Functional
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 177622 0 None 1 2 Human 6.9 pEC50 = 6.9 Functional
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 75702 10 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 75702 10 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 122817 0 None -3 3 Human 5.9 pEC50 = 5.9 Functional
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 122817 0 None -3 3 Human 5.9 pEC50 = 5.9 Functional
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 177110 0 None -1 2 Human 6.9 pEC50 = 6.9 Functional
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 177110 0 None -1 2 Human 6.9 pEC50 = 6.9 Functional
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 85892 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 85892 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 12231 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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 12231 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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 12231 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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 39970 15 None -1 2 Human 6.9 pEC50 = 6.9 Functional
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 39970 15 None -1 2 Human 6.9 pEC50 = 6.9 Functional
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 143601 0 None - 1 Rat 6.9 pEC50 = 6.9 Functional
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 143601 0 None - 1 Rat 6.9 pEC50 = 6.9 Functional
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 85892 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 85892 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 177408 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 177408 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 143601 0 None - 1 Rat 6.9 pEC50 = 6.9 Functional
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 143601 0 None - 1 Rat 6.9 pEC50 = 6.9 Functional
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 2929 23 None 1 8 Human 7.9 pEC50 = 7.9 Functional
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 2929 23 None 1 8 Human 7.9 pEC50 = 7.9 Functional
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 2929 23 None 1 8 Human 7.9 pEC50 = 7.9 Functional
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 162999 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
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 162999 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
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 164024 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
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 164024 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
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 173072 0 None 4 2 Human 6.9 pEC50 = 6.9 Functional
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 173072 0 None 4 2 Human 6.9 pEC50 = 6.9 Functional
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 174115 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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 174115 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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 180712 0 None 2 2 Human 6.9 pEC50 = 6.9 Functional
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 180712 0 None 2 2 Human 6.9 pEC50 = 6.9 Functional
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 213453 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 156725 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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 156725 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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 85883 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 85883 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 158866 5 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 158866 5 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 85883 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 85883 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 158866 5 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 158866 5 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 177052 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 177052 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 157343 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 157343 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 212755 1 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 39970 15 None 1 2 Rat 6.8 pEC50 = 6.8 Functional
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 39970 15 None 1 2 Rat 6.8 pEC50 = 6.8 Functional
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 157343 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 157343 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 172275 0 None -2 2 Rat 5.8 pEC50 = 5.8 Functional
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 172275 0 None -2 2 Rat 5.8 pEC50 = 5.8 Functional
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 164124 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 164124 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 172275 0 None -2 2 Rat 5.8 pEC50 = 5.8 Functional
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 172275 0 None -2 2 Rat 5.8 pEC50 = 5.8 Functional
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 176793 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 176793 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 164124 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 164124 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 158374 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 158374 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 85911 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 85911 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 158374 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 158374 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 85911 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 85911 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 176909 0 None -1 2 Human 6.8 pEC50 = 6.8 Functional
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 176909 0 None -1 2 Human 6.8 pEC50 = 6.8 Functional
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 176960 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 176960 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 213368 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 176668 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 176668 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 87157 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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 87157 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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 163716 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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 163716 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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 159137 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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 159137 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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 180581 0 None 5 2 Human 6.8 pEC50 = 6.8 Functional
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 180581 0 None 5 2 Human 6.8 pEC50 = 6.8 Functional
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 181386 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 181386 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 212877 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 51031 23 None -1 2 Rat 5.8 pEC50 = 5.8 Functional
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 51031 23 None -1 2 Rat 5.8 pEC50 = 5.8 Functional
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 169907 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 169907 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 173836 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 173836 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 163688 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 163688 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 163688 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 163688 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 163731 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 163731 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 51031 23 None -1 2 Rat 5.8 pEC50 = 5.8 Functional
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 51031 23 None -1 2 Rat 5.8 pEC50 = 5.8 Functional
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 163731 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 163731 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 213222 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 85902 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 85902 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 85903 12 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 85903 12 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 155897 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 155897 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 213472 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 176665 0 None -1 2 Human 6.8 pEC50 = 6.8 Functional
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 176665 0 None -1 2 Human 6.8 pEC50 = 6.8 Functional
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 15903 0 None -50 5 Human 6.8 pEC50 = 6.8 Functional
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 15903 0 None -50 5 Human 6.8 pEC50 = 6.8 Functional
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 15928 0 None -63 5 Human 6.8 pEC50 = 6.8 Functional
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 15928 0 None -63 5 Human 6.8 pEC50 = 6.8 Functional
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 156979 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 156979 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 15930 0 None -125 5 Human 5.8 pEC50 = 5.8 Functional
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 15930 0 None -125 5 Human 5.8 pEC50 = 5.8 Functional
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 15947 0 None -7 4 Human 5.8 pEC50 = 5.8 Functional
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 15947 0 None -7 4 Human 5.8 pEC50 = 5.8 Functional
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 156137 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 156137 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 53400 6 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 53400 6 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 158500 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 158500 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 213411 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 170350 0 None 12 2 Human 7.8 pEC50 = 7.8 Functional
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 170350 0 None 12 2 Human 7.8 pEC50 = 7.8 Functional
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 169752 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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 169752 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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 159137 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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 159137 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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 157275 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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 157275 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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 174090 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 174090 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 169732 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 169732 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 171794 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 171794 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 85902 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 85902 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 85903 12 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 85903 12 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 25983 5 None 4 2 Rat 6.8 pEC50 = 6.8 Functional
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 25983 5 None 4 2 Rat 6.8 pEC50 = 6.8 Functional
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 53400 6 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 53400 6 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 213018 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 173462 0 None -1 2 Rat 6.8 pEC50 = 6.8 Functional
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 173462 0 None -1 2 Rat 6.8 pEC50 = 6.8 Functional
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 157056 0 None 2 2 Human 6.8 pEC50 = 6.8 Functional
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 157056 0 None 2 2 Human 6.8 pEC50 = 6.8 Functional
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 156137 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 156137 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 157458 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 157458 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 173462 0 None -1 2 Rat 6.8 pEC50 = 6.8 Functional
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 173462 0 None -1 2 Rat 6.8 pEC50 = 6.8 Functional
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 156501 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 156501 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 139841 2 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 139841 2 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 174814 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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 174814 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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 157275 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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 157275 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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 163467 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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 163467 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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 3984 26 None 7 2 Rat 7.8 pEC50 = 7.8 Functional
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 3984 26 None 7 2 Rat 7.8 pEC50 = 7.8 Functional
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 3984 26 None 7 2 Rat 7.8 pEC50 = 7.8 Functional
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 151102 0 None 14 2 Rat 7.8 pEC50 = 7.8 Functional
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 151102 0 None 14 2 Rat 7.8 pEC50 = 7.8 Functional
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 3984 26 None 7 2 Rat 7.8 pEC50 = 7.8 Functional
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 3984 26 None 7 2 Rat 7.8 pEC50 = 7.8 Functional
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 3984 26 None 7 2 Rat 7.8 pEC50 = 7.8 Functional
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 151102 0 None 14 2 Rat 7.8 pEC50 = 7.8 Functional
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 151102 0 None 14 2 Rat 7.8 pEC50 = 7.8 Functional
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 178845 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 178845 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 139841 2 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 139841 2 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 155897 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 155897 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 177543 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 177543 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 213059 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 177482 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 177482 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 139956 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 139956 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 85907 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 85907 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 85907 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 85907 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 157458 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 157458 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 155838 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 155838 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 164070 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 164070 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 85905 12 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 85905 12 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 164070 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 164070 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 155838 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 155838 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 4034 72 None -8 9 Human 7.8 pEC50 = 7.8 Functional
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 4034 72 None -8 9 Human 7.8 pEC50 = 7.8 Functional
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 4034 72 None -8 9 Human 7.8 pEC50 = 7.8 Functional
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 4034 72 None -8 9 Human 7.8 pEC50 = 7.8 Functional
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 4034 72 None -8 9 Human 7.8 pEC50 = 7.8 Functional
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 163410 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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 163410 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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 163429 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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 163429 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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 163618 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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 163618 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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 158883 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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 158883 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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 155489 7 None - 1 Human 7.7 pEC50 = 7.7 Functional
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 155489 7 None - 1 Human 7.7 pEC50 = 7.7 Functional
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 170121 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 170121 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 179469 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 179469 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 85905 12 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 85905 12 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 139956 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 139956 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 172336 0 None -3 2 Rat 6.7 pEC50 = 6.7 Functional
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 172336 0 None -3 2 Rat 6.7 pEC50 = 6.7 Functional
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 158745 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
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 158745 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
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 33773 11 None - 1 Human 5.7 pEC50 = 5.7 Functional
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 33773 11 None - 1 Human 5.7 pEC50 = 5.7 Functional
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 172336 0 None -3 2 Rat 6.7 pEC50 = 6.7 Functional
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 172336 0 None -3 2 Rat 6.7 pEC50 = 6.7 Functional
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 25746 0 None - 1 Rat 6.7 pEC50 = 6.7 Functional
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 25746 0 None - 1 Rat 6.7 pEC50 = 6.7 Functional
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 177286 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
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 177286 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
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 156979 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
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 156979 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
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 156501 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
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 156501 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
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 139866 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
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 139866 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
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 158745 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
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 158745 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
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 155489 7 None - 1 Human 7.7 pEC50 = 7.7 Functional
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 155489 7 None - 1 Human 7.7 pEC50 = 7.7 Functional
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 80047 2 None -1 4 Human 7.7 pEC50 = 7.7 Functional
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 80047 2 None -1 4 Human 7.7 pEC50 = 7.7 Functional
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 175085 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
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 175085 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
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 139866 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
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 139866 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
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 52354 0 None - 1 Rat 6.7 pEC50 = 6.7 Functional
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 52354 0 None - 1 Rat 6.7 pEC50 = 6.7 Functional
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 174751 0 None 1 2 Rat 6.7 pEC50 = 6.7 Functional
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 174751 0 None 1 2 Rat 6.7 pEC50 = 6.7 Functional
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 174751 0 None 1 2 Rat 6.7 pEC50 = 6.7 Functional
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 174751 0 None 1 2 Rat 6.7 pEC50 = 6.7 Functional
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 157056 0 None 2 2 Human 6.7 pEC50 = 6.7 Functional
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 157056 0 None 2 2 Human 6.7 pEC50 = 6.7 Functional
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 15927 0 None -158 5 Human 6.7 pEC50 = 6.7 Functional
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 15927 0 None -158 5 Human 6.7 pEC50 = 6.7 Functional
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 15949 0 None -79 5 Human 6.7 pEC50 = 6.7 Functional
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 15949 0 None -79 5 Human 6.7 pEC50 = 6.7 Functional
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 80048 0 None -3 3 Human 6.7 pEC50 = 6.7 Functional
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 80048 0 None -3 3 Human 6.7 pEC50 = 6.7 Functional
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 163407 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
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 163407 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
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 85910 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
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 85910 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
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 169804 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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 169804 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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 169243 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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 169243 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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 181134 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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 181134 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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 181282 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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 181282 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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 181574 0 None 54 2 Human 7.7 pEC50 = 7.7 Functional
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 181574 0 None 54 2 Human 7.7 pEC50 = 7.7 Functional
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 181813 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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 181813 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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 163057 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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 163057 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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 163365 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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 163365 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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 163752 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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 163752 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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 163407 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
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 163407 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
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
89445258 174135 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
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 272 3 2 4 3.6 Cc1cc(C)c2c(n1)sc1c(NCC3CC3)n[nH]c12 10.1016/j.bmcl.2018.12.039
CHEMBL4559841 174135 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
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 272 3 2 4 3.6 Cc1cc(C)c2c(n1)sc1c(NCC3CC3)n[nH]c12 10.1016/j.bmcl.2018.12.039
134207685 169499 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
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 4.2 Cc1cn2c(cc(C)c3c(N)c(C(=O)N[C@H]4CCc5ccccc54)sc32)n1 10.1016/j.bmcl.2019.06.032
CHEMBL4443127 169499 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
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 4.2 Cc1cn2c(cc(C)c3c(N)c(C(=O)N[C@H]4CCc5ccccc54)sc32)n1 10.1016/j.bmcl.2019.06.032
9936450 34929 0 None -27 2 Human 4.7 pEC50 = 4.7 Functional
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 518 14 0 10 5.0 CN1CCC=C(c2nsnc2OCCCCCCCCCOc2nsnc2C2=CCCN(C)C2)C1 10.1021/jm0102405
CHEMBL143469 34929 0 None -27 2 Human 4.7 pEC50 = 4.7 Functional
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 518 14 0 10 5.0 CN1CCC=C(c2nsnc2OCCCCCCCCCOc2nsnc2C2=CCCN(C)C2)C1 10.1021/jm0102405
53382534 85910 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
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 85910 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
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
CHEMBL5078186 212769 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
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(N(C)C)nccc12 10.1016/j.bmcl.2021.128416
137642025 157588 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
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 376 3 0 5 4.3 Cc1ccc(OC2CCN(c3c(C#N)cnc4c(C)cc(F)cc34)CC2)cn1 10.1016/j.bmcl.2017.08.043
CHEMBL4087127 157588 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
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 376 3 0 5 4.3 Cc1ccc(OC2CCN(c3c(C#N)cnc4c(C)cc(F)cc34)CC2)cn1 10.1016/j.bmcl.2017.08.043
137642025 157588 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
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 376 3 0 5 4.3 Cc1ccc(OC2CCN(c3c(C#N)cnc4c(C)cc(F)cc34)CC2)cn1 10.1016/j.bmcl.2017.08.043
CHEMBL4087127 157588 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
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 376 3 0 5 4.3 Cc1ccc(OC2CCN(c3c(C#N)cnc4c(C)cc(F)cc34)CC2)cn1 10.1016/j.bmcl.2017.08.043
53382508 85889 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
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 346 3 2 5 3.5 Cc1nc2sc(C(=O)NCc3cccnc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313380 85889 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
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 346 3 2 5 3.5 Cc1nc2sc(C(=O)NCc3cccnc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
137632597 155784 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
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 380 3 0 5 4.1 Cc1ccc(OC2CCN(c3c(C#N)cnc4c(F)cc(F)cc34)CC2)cn1 10.1016/j.bmcl.2017.08.043
CHEMBL4065706 155784 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
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 380 3 0 5 4.1 Cc1ccc(OC2CCN(c3c(C#N)cnc4c(F)cc(F)cc34)CC2)cn1 10.1016/j.bmcl.2017.08.043
89768736 143757 0 None -11 2 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 408 5 2 7 2.5 Cc1nnc2sc(C(=O)NCc3ccc(S(=O)(=O)CF)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
CHEMBL3905112 143757 0 None -11 2 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
ChEMBL 408 5 2 7 2.5 Cc1nnc2sc(C(=O)NCc3ccc(S(=O)(=O)CF)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
53382508 85889 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
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 346 3 2 5 3.5 Cc1nc2sc(C(=O)NCc3cccnc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313380 85889 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
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 346 3 2 5 3.5 Cc1nc2sc(C(=O)NCc3cccnc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
89768736 143757 0 None 11 2 Rat 7.7 pEC50 = 7.7 Functional
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 408 5 2 7 2.5 Cc1nnc2sc(C(=O)NCc3ccc(S(=O)(=O)CF)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
CHEMBL3905112 143757 0 None 11 2 Rat 7.7 pEC50 = 7.7 Functional
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 408 5 2 7 2.5 Cc1nnc2sc(C(=O)NCc3ccc(S(=O)(=O)CF)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
89768736 143757 0 None 11 2 Rat 7.7 pEC50 = 7.7 Functional
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 408 5 2 7 2.5 Cc1nnc2sc(C(=O)NCc3ccc(S(=O)(=O)CF)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
CHEMBL3905112 143757 0 None 11 2 Rat 7.7 pEC50 = 7.7 Functional
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 408 5 2 7 2.5 Cc1nnc2sc(C(=O)NCc3ccc(S(=O)(=O)CF)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
117917124 170225 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
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 359 4 1 5 3.7 COc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2C)cc1F 10.1016/j.bmcl.2018.12.039
CHEMBL4453085 170225 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
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 359 4 1 5 3.7 COc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2C)cc1F 10.1016/j.bmcl.2018.12.039
41358726 171225 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
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 368 3 1 5 3.9 Cc1cc(C)c2c(C)c(C(=O)NCc3ccc4c(c3)OCCO4)sc2n1 10.1016/j.bmcl.2018.12.039
CHEMBL4467950 171225 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
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 368 3 1 5 3.9 Cc1cc(C)c2c(C)c(C(=O)NCc3ccc4c(c3)OCCO4)sc2n1 10.1016/j.bmcl.2018.12.039
134207706 173866 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
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 362 2 2 5 3.9 Cc1cc2nccn2c2sc(C(=O)N[C@H]3CCc4ccccc43)c(N)c12 10.1016/j.bmcl.2019.06.032
CHEMBL4553231 173866 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
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 362 2 2 5 3.9 Cc1cc2nccn2c2sc(C(=O)N[C@H]3CCc4ccccc43)c(N)c12 10.1016/j.bmcl.2019.06.032
137646437 157095 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
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(-c4ccccn4)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
CHEMBL4081305 157095 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
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(-c4ccccn4)cc3)c(N)c2c1C 10.1016/j.bmcl.2017.04.043
137641641 157773 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
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 404 4 2 7 3.6 Cc1ncc(-c2ccc(CNC(=O)c3sc4nnc(C)c(C)c4c3N)cc2)cn1 10.1016/j.bmcl.2017.04.043
CHEMBL4089170 157773 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
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 404 4 2 7 3.6 Cc1ncc(-c2ccc(CNC(=O)c3sc4nnc(C)c(C)c4c3N)cc2)cn1 10.1016/j.bmcl.2017.04.043
137656749 159063 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
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 337 3 0 4 4.1 Cc1ccc(OC2CCN(c3ccnc4ccc(F)cc34)CC2)cn1 10.1016/j.bmcl.2017.08.043
CHEMBL4103287 159063 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
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 337 3 0 4 4.1 Cc1ccc(OC2CCN(c3ccnc4ccc(F)cc34)CC2)cn1 10.1016/j.bmcl.2017.08.043
306 3400 18 None 1 5 Human 6.7 pEC50 = 6.7 Functional
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 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N 10.1016/j.bmcl.2015.08.011
3536 3400 18 None 1 5 Human 6.7 pEC50 = 6.7 Functional
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 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N 10.1016/j.bmcl.2015.08.011
53930639 3400 18 None 1 5 Human 6.7 pEC50 = 6.7 Functional
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 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N 10.1016/j.bmcl.2015.08.011
9577995 3400 18 None 1 5 Human 6.7 pEC50 = 6.7 Functional
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 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N 10.1016/j.bmcl.2015.08.011
CHEMBL134641 3400 18 None 1 5 Human 6.7 pEC50 = 6.7 Functional
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 193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N 10.1016/j.bmcl.2015.08.011
650899 54129 10 None -7 5 Rat 4.7 pEC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M4. (Class of assay: confirmatory) [Related pubchem assays: 626, 1488, 1741 ]PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M4. (Class of assay: confirmatory) [Related pubchem assays: 626, 1488, 1741 ]
ChEMBL 319 6 2 4 1.6 CCOC(=O)N1CCC(NCCNC(=O)c2ccccc2)CC1 nan
CHEMBL1535797 54129 10 None -7 5 Rat 4.7 pEC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M4. (Class of assay: confirmatory) [Related pubchem assays: 626, 1488, 1741 ]PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M4. (Class of assay: confirmatory) [Related pubchem assays: 626, 1488, 1741 ]
ChEMBL 319 6 2 4 1.6 CCOC(=O)N1CCC(NCCNC(=O)c2ccccc2)CC1 nan
CHEMBL1609153 54129 10 None -7 5 Rat 4.7 pEC50 = 4.7 Functional
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M4. (Class of assay: confirmatory) [Related pubchem assays: 626, 1488, 1741 ]PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M4. (Class of assay: confirmatory) [Related pubchem assays: 626, 1488, 1741 ]
ChEMBL 319 6 2 4 1.6 CCOC(=O)N1CCC(NCCNC(=O)c2ccccc2)CC1 nan
89777237 155774 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
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 396 3 3 6 2.5 Cc1nnc2sc(C(=O)NC3CN(C(=O)Nc4ccccc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4065565 155774 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
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 396 3 3 6 2.5 Cc1nnc2sc(C(=O)NC3CN(C(=O)Nc4ccccc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
89777237 155774 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
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 396 3 3 6 2.5 Cc1nnc2sc(C(=O)NC3CN(C(=O)Nc4ccccc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4065565 155774 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
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 396 3 3 6 2.5 Cc1nnc2sc(C(=O)NC3CN(C(=O)Nc4ccccc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
134207726 174502 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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 335 2 2 6 2.7 Cc1c(Cl)c2nnc(C)n2c2sc(C(=O)NC3CC3)c(N)c12 10.1016/j.bmcl.2019.06.032
CHEMBL4568327 174502 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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 335 2 2 6 2.7 Cc1c(Cl)c2nnc(C)n2c2sc(C(=O)NC3CC3)c(N)c12 10.1016/j.bmcl.2019.06.032
135153778 163822 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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 4 1 7 2.1 COc1ccc(OC2CCN(c3nc4cn[nH]c(=O)c4cc3C)CC2)cn1 10.1021/acsmedchemlett.8b00330
CHEMBL4212929 163822 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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 4 1 7 2.1 COc1ccc(OC2CCN(c3nc4cn[nH]c(=O)c4cc3C)CC2)cn1 10.1021/acsmedchemlett.8b00330
89777060 156579 0 None 114 2 Human 7.7 pEC50 = 7.7 Functional
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 397 3 2 7 2.5 Cc1nnc2sc(C(=O)NC3CN(C(=O)Oc4ccccc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
CHEMBL4074908 156579 0 None 114 2 Human 7.7 pEC50 = 7.7 Functional
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 397 3 2 7 2.5 Cc1nnc2sc(C(=O)NC3CN(C(=O)Oc4ccccc4)C3)c(N)c2c1C 10.1016/j.bmcl.2017.05.014
89777160 153430 0 None - 1 Rat 7.7 pEC50 = 7.7 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assayPositive allosteri