Get vendors


Ligand source activities (1 row/activity)

<
Ligand Receptor Assay information Chemical information
Sel. page Common
name
GPCRdb ID #Vendors UniProt IUPHAR Species p-value
(-log)
Activity
Type
Activity
Relation
Activity
Value
Assay Type Assay Description Source Mol
weight
Rot
Bonds
H don H acc LogP Smiles DOI
10104167 1928 0 ACM4 M4 receptor Human - = Unclassified
UnclassifiedUnclassified
Guide to Pharmacology 197 2 0 3 0.4 C[N+](CC#CCOC1=NOCC1)(C)C 24863257
6937 1928 0 ACM4 M4 receptor Human - = Unclassified
UnclassifiedUnclassified
Guide to Pharmacology 197 2 0 3 0.4 C[N+](CC#CCOC1=NOCC1)(C)C 24863257
CHEMBL3121473 1928 0 ACM4 M4 receptor Human - = Unclassified
UnclassifiedUnclassified
Guide to Pharmacology 197 2 0 3 0.4 C[N+](CC#CCOC1=NOCC1)(C)C 24863257
154733029 3770 45 ACM4 M4 receptor Human - = Unclassified
UnclassifiedUnclassified
Guide to Pharmacology 347 3 2 4 3.1 O=C(C1Sc2c(C1N)c(C)cc(n2)C)NCc1ccc(cc1)Cl 19201489
7633 3770 45 ACM4 M4 receptor Human - = Unclassified
UnclassifiedUnclassified
Guide to Pharmacology 347 3 2 4 3.1 O=C(C1Sc2c(C1N)c(C)cc(n2)C)NCc1ccc(cc1)Cl 19201489
CHEMBL1212994 3770 45 ACM4 M4 receptor Human - = Unclassified
UnclassifiedUnclassified
Guide to Pharmacology 347 3 2 4 3.1 O=C(C1Sc2c(C1N)c(C)cc(n2)C)NCc1ccc(cc1)Cl 19201489
10952349 34713 0 ACM4 M4 receptor 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 34713 0 ACM4 M4 receptor 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 30370 0 ACM4 M4 receptor 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 30370 0 ACM4 M4 receptor 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 33682 0 ACM4 M4 receptor 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 33682 0 ACM4 M4 receptor 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
187 245 23 ACM4 M4 receptor 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
294 245 23 ACM4 M4 receptor 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
65 245 23 ACM4 M4 receptor 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 245 23 ACM4 M4 receptor 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 245 23 ACM4 M4 receptor 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 245 23 ACM4 M4 receptor 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
187 245 23 ACM4 M4 receptor 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
294 245 23 ACM4 M4 receptor 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
65 245 23 ACM4 M4 receptor 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 245 23 ACM4 M4 receptor 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 245 23 ACM4 M4 receptor 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 245 23 ACM4 M4 receptor 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
CHEMBL4783881 181402 0 ACM4 M4 receptor 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
CHEMBL4798497 182539 0 ACM4 M4 receptor 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 157445 0 ACM4 M4 receptor 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 157445 0 ACM4 M4 receptor 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
CHEMBL1223860 15743 0 ACM4 M4 receptor 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 158222 0 ACM4 M4 receptor 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 158222 0 ACM4 M4 receptor 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
CHEMBL4751034 179443 0 ACM4 M4 receptor 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
72713421 101824 0 ACM4 M4 receptor Human 7.0 pEC50 = 7 Binding
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 359 4 2 5 3.6 COc1ccc(CNC(=O)c2sc3nc(C)cc(C)c3c2N)cc1F 10.1021/jm401032k
CHEMBL2435361 101824 0 ACM4 M4 receptor Human 7.0 pEC50 = 7 Binding
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 359 4 2 5 3.6 COc1ccc(CNC(=O)c2sc3nc(C)cc(C)c3c2N)cc1F 10.1021/jm401032k
CHEMBL3040619 101824 0 ACM4 M4 receptor Human 7.0 pEC50 = 7 Binding
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 359 4 2 5 3.6 COc1ccc(CNC(=O)c2sc3nc(C)cc(C)c3c2N)cc1F 10.1021/jm401032k
89445242 173813 0 ACM4 M4 receptor 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 173813 0 ACM4 M4 receptor 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 169432 0 ACM4 M4 receptor 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 169432 0 ACM4 M4 receptor 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 173188 0 ACM4 M4 receptor 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 173188 0 ACM4 M4 receptor 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 173188 0 ACM4 M4 receptor 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 173188 0 ACM4 M4 receptor 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 157655 0 ACM4 M4 receptor 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 157655 0 ACM4 M4 receptor 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 158299 0 ACM4 M4 receptor 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 158299 0 ACM4 M4 receptor 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 85664 0 ACM4 M4 receptor 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 85664 0 ACM4 M4 receptor 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 172029 0 ACM4 M4 receptor 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 172029 0 ACM4 M4 receptor 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 174668 0 ACM4 M4 receptor 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 174668 0 ACM4 M4 receptor 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
44176134 101823 0 ACM4 M4 receptor Human 7.0 pEC50 = 7.0 Binding
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 347 3 2 4 3.7 Cc1cc(C)c2c(N)c(C(=O)NCc3cccc(F)c3F)sc2n1 10.1021/jm401032k
CHEMBL2435357 101823 0 ACM4 M4 receptor Human 7.0 pEC50 = 7.0 Binding
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 347 3 2 4 3.7 Cc1cc(C)c2c(N)c(C(=O)NCc3cccc(F)c3F)sc2n1 10.1021/jm401032k
CHEMBL3040618 101823 0 ACM4 M4 receptor Human 7.0 pEC50 = 7.0 Binding
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 347 3 2 4 3.7 Cc1cc(C)c2c(N)c(C(=O)NCc3cccc(F)c3F)sc2n1 10.1021/jm401032k
53382504 85664 0 ACM4 M4 receptor 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 85664 0 ACM4 M4 receptor 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 163885 0 ACM4 M4 receptor 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 163885 0 ACM4 M4 receptor 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 157091 0 ACM4 M4 receptor 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 157091 0 ACM4 M4 receptor 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 163885 0 ACM4 M4 receptor 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 163885 0 ACM4 M4 receptor 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 139711 0 ACM4 M4 receptor 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 139711 0 ACM4 M4 receptor 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 172029 0 ACM4 M4 receptor 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 172029 0 ACM4 M4 receptor 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 174668 0 ACM4 M4 receptor 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 174668 0 ACM4 M4 receptor 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 155274 0 ACM4 M4 receptor 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 155274 0 ACM4 M4 receptor 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
CHEMBL3616501 122561 0 ACM4 M4 receptor 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 C/C(=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(-c3ccccc3)cc1)[C@H](O)C2)N(C)Cc1ccc(F)cc1 10.1016/j.bmcl.2015.08.011
135126271 163361 0 ACM4 M4 receptor 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 163361 0 ACM4 M4 receptor 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 85644 0 ACM4 M4 receptor 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 85644 0 ACM4 M4 receptor 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 85644 0 ACM4 M4 receptor 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 85644 0 ACM4 M4 receptor 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 85661 0 ACM4 M4 receptor 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 85661 0 ACM4 M4 receptor 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 162741 0 ACM4 M4 receptor 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 162741 0 ACM4 M4 receptor 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 162741 0 ACM4 M4 receptor 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 162741 0 ACM4 M4 receptor 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 163361 0 ACM4 M4 receptor 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 163361 0 ACM4 M4 receptor 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 163510 0 ACM4 M4 receptor 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 163510 0 ACM4 M4 receptor 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 85661 0 ACM4 M4 receptor 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 85661 0 ACM4 M4 receptor 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 163510 0 ACM4 M4 receptor 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 163510 0 ACM4 M4 receptor 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 157091 0 ACM4 M4 receptor 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 157091 0 ACM4 M4 receptor 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 163980 0 ACM4 M4 receptor 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 163980 0 ACM4 M4 receptor 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 163980 0 ACM4 M4 receptor 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 163980 0 ACM4 M4 receptor 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 170502 0 ACM4 M4 receptor 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 170502 0 ACM4 M4 receptor 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 157445 0 ACM4 M4 receptor 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 157445 0 ACM4 M4 receptor 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 153040 0 ACM4 M4 receptor 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 153040 0 ACM4 M4 receptor 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 153040 0 ACM4 M4 receptor 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 153040 0 ACM4 M4 receptor 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 157750 0 ACM4 M4 receptor 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 157750 0 ACM4 M4 receptor 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 173433 0 ACM4 M4 receptor 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 173433 0 ACM4 M4 receptor 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 173795 0 ACM4 M4 receptor 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 173795 0 ACM4 M4 receptor 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
44176134 101823 0 ACM4 M4 receptor Human 7.0 pEC50 = 7.0 Binding
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 347 3 2 4 3.7 Cc1cc(C)c2c(N)c(C(=O)NCc3cccc(F)c3F)sc2n1 10.1021/jm401032k
CHEMBL2435357 101823 0 ACM4 M4 receptor Human 7.0 pEC50 = 7.0 Binding
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 347 3 2 4 3.7 Cc1cc(C)c2c(N)c(C(=O)NCc3cccc(F)c3F)sc2n1 10.1021/jm401032k
CHEMBL3040618 101823 0 ACM4 M4 receptor Human 7.0 pEC50 = 7.0 Binding
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 347 3 2 4 3.7 Cc1cc(C)c2c(N)c(C(=O)NCc3cccc(F)c3F)sc2n1 10.1021/jm401032k
9958728 34733 0 ACM4 M4 receptor 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 34733 0 ACM4 M4 receptor 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 173322 0 ACM4 M4 receptor 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 173322 0 ACM4 M4 receptor 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 170096 0 ACM4 M4 receptor 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 170096 0 ACM4 M4 receptor 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 139681 7 ACM4 M4 receptor 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 139681 7 ACM4 M4 receptor 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 139711 0 ACM4 M4 receptor 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 139711 0 ACM4 M4 receptor 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 122828 0 ACM4 M4 receptor 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 122828 0 ACM4 M4 receptor 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
CHEMBL4641848 176833 0 ACM4 M4 receptor Rat 7.0 pEC50 = 7.0 Binding
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
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
43989253 75466 2 ACM4 M4 receptor 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 75466 2 ACM4 M4 receptor 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 163623 0 ACM4 M4 receptor 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 163623 0 ACM4 M4 receptor 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
CHEMBL3616504 122562 0 ACM4 M4 receptor 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 163623 0 ACM4 M4 receptor 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 163623 0 ACM4 M4 receptor 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
29262717 139681 7 ACM4 M4 receptor 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 139681 7 ACM4 M4 receptor 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 163899 0 ACM4 M4 receptor 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 163899 0 ACM4 M4 receptor 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 122831 0 ACM4 M4 receptor 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 122831 0 ACM4 M4 receptor 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
CHEMBL4644084 176990 0 ACM4 M4 receptor 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 163899 0 ACM4 M4 receptor 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 163899 0 ACM4 M4 receptor 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
CHEMBL4759565 180180 0 ACM4 M4 receptor 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 139648 0 ACM4 M4 receptor 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 139648 0 ACM4 M4 receptor 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 170383 0 ACM4 M4 receptor 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 170383 0 ACM4 M4 receptor 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 171486 0 ACM4 M4 receptor 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 171486 0 ACM4 M4 receptor 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
CHEMBL1223754 15696 0 ACM4 M4 receptor 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 39773 15 ACM4 M4 receptor 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 39773 15 ACM4 M4 receptor 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 174590 0 ACM4 M4 receptor 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 174590 0 ACM4 M4 receptor 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 170455 0 ACM4 M4 receptor 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 170455 0 ACM4 M4 receptor 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 173800 0 ACM4 M4 receptor 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 173800 0 ACM4 M4 receptor 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 175061 0 ACM4 M4 receptor 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 175061 0 ACM4 M4 receptor 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
CHEMBL4743571 178815 0 ACM4 M4 receptor 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 169834 0 ACM4 M4 receptor 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 169834 0 ACM4 M4 receptor 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 172223 0 ACM4 M4 receptor 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 172223 0 ACM4 M4 receptor 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 139648 0 ACM4 M4 receptor 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 139648 0 ACM4 M4 receptor 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 25794 5 ACM4 M4 receptor 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 25794 5 ACM4 M4 receptor 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 85645 0 ACM4 M4 receptor 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 85645 0 ACM4 M4 receptor 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 172476 0 ACM4 M4 receptor 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 172476 0 ACM4 M4 receptor 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 155962 8 ACM4 M4 receptor 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 155962 8 ACM4 M4 receptor 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 157655 0 ACM4 M4 receptor 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 157655 0 ACM4 M4 receptor 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 85645 0 ACM4 M4 receptor 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 85645 0 ACM4 M4 receptor 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
CHEMBL4632962 176218 0 ACM4 M4 receptor 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
CHEMBL1223807 15722 0 ACM4 M4 receptor 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
44176127 101810 0 ACM4 M4 receptor Human 6.9 pEC50 = 6.9 Binding
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 329 3 2 4 3.6 Cc1cc(C)c2c(N)c(C(=O)NCc3ccccc3F)sc2n1 10.1021/jm401032k
CHEMBL2435354 101810 0 ACM4 M4 receptor Human 6.9 pEC50 = 6.9 Binding
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 329 3 2 4 3.6 Cc1cc(C)c2c(N)c(C(=O)NCc3ccccc3F)sc2n1 10.1021/jm401032k
CHEMBL3040499 101810 0 ACM4 M4 receptor Human 6.9 pEC50 = 6.9 Binding
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 329 3 2 4 3.6 Cc1cc(C)c2c(N)c(C(=O)NCc3ccccc3F)sc2n1 10.1021/jm401032k
137659901 158719 0 ACM4 M4 receptor 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 158719 0 ACM4 M4 receptor 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 85653 0 ACM4 M4 receptor 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 85653 0 ACM4 M4 receptor 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
3263 3778 44 ACM4 M4 receptor Human 6.9 pEC50 = 6.9 Binding
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 341 4 2 5 3.4 COc1ccc(cc1)CNC(=O)c1sc2c(c1N)c(C)cc(n2)C 10.1021/jm401032k
864492 3778 44 ACM4 M4 receptor Human 6.9 pEC50 = 6.9 Binding
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 341 4 2 5 3.4 COc1ccc(cc1)CNC(=O)c1sc2c(c1N)c(C)cc(n2)C 10.1021/jm401032k
CHEMBL1978713 3778 44 ACM4 M4 receptor Human 6.9 pEC50 = 6.9 Binding
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 341 4 2 5 3.4 COc1ccc(cc1)CNC(=O)c1sc2c(c1N)c(C)cc(n2)C 10.1021/jm401032k
53382505 85653 0 ACM4 M4 receptor 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 85653 0 ACM4 M4 receptor 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 158180 0 ACM4 M4 receptor 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 158180 0 ACM4 M4 receptor 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 75465 1 ACM4 M4 receptor 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 75465 1 ACM4 M4 receptor 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 158719 0 ACM4 M4 receptor 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 158719 0 ACM4 M4 receptor 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
CHEMBL4635732 176388 0 ACM4 M4 receptor Rat 6.9 pEC50 = 6.9 Binding
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
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
137654582 158180 0 ACM4 M4 receptor 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 158180 0 ACM4 M4 receptor 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 111294 0 ACM4 M4 receptor 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 111294 0 ACM4 M4 receptor 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 157750 0 ACM4 M4 receptor 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 157750 0 ACM4 M4 receptor 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
2230 445 46 ACM4 M4 receptor Human 6.9 pEC50 = 6.9 Binding
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M4 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M4 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm00012a019
296 445 46 ACM4 M4 receptor Human 6.9 pEC50 = 6.9 Binding
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M4 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M4 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm00012a019
CHEMBL7303 445 46 ACM4 M4 receptor Human 6.9 pEC50 = 6.9 Binding
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M4 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M4 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm00012a019
DB04365 445 46 ACM4 M4 receptor Human 6.9 pEC50 = 6.9 Binding
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M4 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M4 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 10.1021/jm00012a019
134207699 174532 0 ACM4 M4 receptor 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 174532 0 ACM4 M4 receptor 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
3263 3778 44 ACM4 M4 receptor Human 6.9 pEC50 = 6.9 Binding
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 341 4 2 5 3.4 COc1ccc(cc1)CNC(=O)c1sc2c(c1N)c(C)cc(n2)C 10.1021/jm401032k
864492 3778 44 ACM4 M4 receptor Human 6.9 pEC50 = 6.9 Binding
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 341 4 2 5 3.4 COc1ccc(cc1)CNC(=O)c1sc2c(c1N)c(C)cc(n2)C 10.1021/jm401032k
CHEMBL1978713 3778 44 ACM4 M4 receptor Human 6.9 pEC50 = 6.9 Binding
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 341 4 2 5 3.4 COc1ccc(cc1)CNC(=O)c1sc2c(c1N)c(C)cc(n2)C 10.1021/jm401032k
44176127 101810 0 ACM4 M4 receptor Human 6.9 pEC50 = 6.9 Binding
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 329 3 2 4 3.6 Cc1cc(C)c2c(N)c(C(=O)NCc3ccccc3F)sc2n1 10.1021/jm401032k
CHEMBL2435354 101810 0 ACM4 M4 receptor Human 6.9 pEC50 = 6.9 Binding
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 329 3 2 4 3.6 Cc1cc(C)c2c(N)c(C(=O)NCc3ccccc3F)sc2n1 10.1021/jm401032k
CHEMBL3040499 101810 0 ACM4 M4 receptor Human 6.9 pEC50 = 6.9 Binding
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 329 3 2 4 3.6 Cc1cc(C)c2c(N)c(C(=O)NCc3ccccc3F)sc2n1 10.1021/jm401032k
44176132 101820 0 ACM4 M4 receptor Human 6.9 pEC50 = 6.9 Binding
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 347 3 2 4 3.7 Cc1cc(C)c2c(N)c(C(=O)NCc3cc(F)ccc3F)sc2n1 10.1021/jm401032k
CHEMBL2435358 101820 0 ACM4 M4 receptor Human 6.9 pEC50 = 6.9 Binding
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 347 3 2 4 3.7 Cc1cc(C)c2c(N)c(C(=O)NCc3cc(F)ccc3F)sc2n1 10.1021/jm401032k
CHEMBL3040593 101820 0 ACM4 M4 receptor Human 6.9 pEC50 = 6.9 Binding
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 347 3 2 4 3.7 Cc1cc(C)c2c(N)c(C(=O)NCc3cc(F)ccc3F)sc2n1 10.1021/jm401032k
734373 14926 18 ACM4 M4 receptor 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 14926 18 ACM4 M4 receptor 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 156451 0 ACM4 M4 receptor 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 156451 0 ACM4 M4 receptor 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
44176132 101820 0 ACM4 M4 receptor Human 6.9 pEC50 = 6.9 Binding
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 347 3 2 4 3.7 Cc1cc(C)c2c(N)c(C(=O)NCc3cc(F)ccc3F)sc2n1 10.1021/jm401032k
CHEMBL2435358 101820 0 ACM4 M4 receptor Human 6.9 pEC50 = 6.9 Binding
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 347 3 2 4 3.7 Cc1cc(C)c2c(N)c(C(=O)NCc3cc(F)ccc3F)sc2n1 10.1021/jm401032k
CHEMBL3040593 101820 0 ACM4 M4 receptor Human 6.9 pEC50 = 6.9 Binding
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 347 3 2 4 3.7 Cc1cc(C)c2c(N)c(C(=O)NCc3cc(F)ccc3F)sc2n1 10.1021/jm401032k
CHEMBL4649459 177345 0 ACM4 M4 receptor 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 75463 7 ACM4 M4 receptor 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 75463 7 ACM4 M4 receptor 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 122557 0 ACM4 M4 receptor 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 122557 0 ACM4 M4 receptor 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
CHEMBL4641848 176833 0 ACM4 M4 receptor 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 85652 0 ACM4 M4 receptor 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 85652 0 ACM4 M4 receptor 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 12049 0 ACM4 M4 receptor 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 12049 0 ACM4 M4 receptor 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 12049 0 ACM4 M4 receptor 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 39773 15 ACM4 M4 receptor 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 39773 15 ACM4 M4 receptor 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 143331 0 ACM4 M4 receptor 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 143331 0 ACM4 M4 receptor 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 85652 0 ACM4 M4 receptor 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 85652 0 ACM4 M4 receptor 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
CHEMBL4646110 177131 0 ACM4 M4 receptor 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 143331 0 ACM4 M4 receptor 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 143331 0 ACM4 M4 receptor 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 2796 20 ACM4 M4 receptor 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 2796 20 ACM4 M4 receptor 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 2796 20 ACM4 M4 receptor 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 162724 0 ACM4 M4 receptor 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 162724 0 ACM4 M4 receptor 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 163752 0 ACM4 M4 receptor 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 163752 0 ACM4 M4 receptor 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 172799 0 ACM4 M4 receptor 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 172799 0 ACM4 M4 receptor 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 173842 0 ACM4 M4 receptor 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 173842 0 ACM4 M4 receptor 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
CHEMBL4762280 180420 0 ACM4 M4 receptor 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
72713420 101806 0 ACM4 M4 receptor Human 6.9 pEC50 = 6.9 Binding
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 365 3 2 4 3.8 Cc1cc(C)c2c(N)c(C(=O)NCc3cc(F)cc(F)c3F)sc2n1 10.1021/jm401032k
CHEMBL2435360 101806 0 ACM4 M4 receptor Human 6.9 pEC50 = 6.9 Binding
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 365 3 2 4 3.8 Cc1cc(C)c2c(N)c(C(=O)NCc3cc(F)cc(F)c3F)sc2n1 10.1021/jm401032k
CHEMBL3040457 101806 0 ACM4 M4 receptor Human 6.9 pEC50 = 6.9 Binding
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 365 3 2 4 3.8 Cc1cc(C)c2c(N)c(C(=O)NCc3cc(F)cc(F)c3F)sc2n1 10.1021/jm401032k
137650228 156451 0 ACM4 M4 receptor 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 156451 0 ACM4 M4 receptor 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
72713420 101806 0 ACM4 M4 receptor Human 6.9 pEC50 = 6.9 Binding
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 365 3 2 4 3.8 Cc1cc(C)c2c(N)c(C(=O)NCc3cc(F)cc(F)c3F)sc2n1 10.1021/jm401032k
CHEMBL2435360 101806 0 ACM4 M4 receptor Human 6.9 pEC50 = 6.9 Binding
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 365 3 2 4 3.8 Cc1cc(C)c2c(N)c(C(=O)NCc3cc(F)cc(F)c3F)sc2n1 10.1021/jm401032k
CHEMBL3040457 101806 0 ACM4 M4 receptor Human 6.9 pEC50 = 6.9 Binding
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 365 3 2 4 3.8 Cc1cc(C)c2c(N)c(C(=O)NCc3cc(F)cc(F)c3F)sc2n1 10.1021/jm401032k
53382493 85643 0 ACM4 M4 receptor 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 85643 0 ACM4 M4 receptor 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 158588 5 ACM4 M4 receptor 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 158588 5 ACM4 M4 receptor 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 85643 0 ACM4 M4 receptor 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 85643 0 ACM4 M4 receptor 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 158588 5 ACM4 M4 receptor 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 158588 5 ACM4 M4 receptor 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
CHEMBL4641135 176775 0 ACM4 M4 receptor 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 157067 0 ACM4 M4 receptor 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 157067 0 ACM4 M4 receptor 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
682264 39773 15 ACM4 M4 receptor 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 39773 15 ACM4 M4 receptor 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 157067 0 ACM4 M4 receptor 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 157067 0 ACM4 M4 receptor 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 172000 0 ACM4 M4 receptor 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 172000 0 ACM4 M4 receptor 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 163852 0 ACM4 M4 receptor 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 163852 0 ACM4 M4 receptor 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 172000 0 ACM4 M4 receptor 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 172000 0 ACM4 M4 receptor 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
CHEMBL4637785 176516 0 ACM4 M4 receptor 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 163852 0 ACM4 M4 receptor 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 163852 0 ACM4 M4 receptor 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 158096 0 ACM4 M4 receptor 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 158096 0 ACM4 M4 receptor 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 85671 0 ACM4 M4 receptor 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 85671 0 ACM4 M4 receptor 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
53382542 85646 0 ACM4 M4 receptor Rat 6.8 pEC50 = 6.8 Binding
Positive allosteric modulation of rat muscarinic M4 receptor assessed as acetylcholine responsePositive allosteric modulation of rat muscarinic M4 receptor assessed as acetylcholine response
ChEMBL 295 2 2 4 3.0 Cc1nc2sc(C(=O)NC3CC3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313377 85646 0 ACM4 M4 receptor Rat 6.8 pEC50 = 6.8 Binding
Positive allosteric modulation of rat muscarinic M4 receptor assessed as acetylcholine responsePositive allosteric modulation of rat muscarinic M4 receptor assessed as acetylcholine response
ChEMBL 295 2 2 4 3.0 Cc1nc2sc(C(=O)NC3CC3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
137640201 156147 2 ACM4 M4 receptor Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphaq activation after 2 mins by BRET assayAgonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphaq activation after 2 mins by BRET assay
ChEMBL 362 6 0 2 4.3 O=C1CCc2ccccc2N1CCCN1CCC(Cc2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4072818 156147 2 ACM4 M4 receptor Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphaq activation after 2 mins by BRET assayAgonist activity at human SP/Myc epitope-tagged muscarinic M4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphaq activation after 2 mins by BRET assay
ChEMBL 362 6 0 2 4.3 O=C1CCc2ccccc2N1CCCN1CCC(Cc2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
137653138 158096 0 ACM4 M4 receptor 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 158096 0 ACM4 M4 receptor 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 85671 0 ACM4 M4 receptor 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 85671 0 ACM4 M4 receptor 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
53382542 85646 0 ACM4 M4 receptor Rat 6.8 pEC50 = 6.8 Binding
Positive allosteric modulation of rat muscarinic M4 receptor assessed as acetylcholine responsePositive allosteric modulation of rat muscarinic M4 receptor assessed as acetylcholine response
ChEMBL 295 2 2 4 3.0 Cc1nc2sc(C(=O)NC3CC3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2313377 85646 0 ACM4 M4 receptor Rat 6.8 pEC50 = 6.8 Binding
Positive allosteric modulation of rat muscarinic M4 receptor assessed as acetylcholine responsePositive allosteric modulation of rat muscarinic M4 receptor assessed as acetylcholine response
ChEMBL 295 2 2 4 3.0 Cc1nc2sc(C(=O)NC3CC3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL4639222 176632 0 ACM4 M4 receptor 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
CHEMBL4640254 176693 0 ACM4 M4 receptor Rat 6.8 pEC50 = 6.8 Binding
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 400 3 1 8 2.9 Cn1nnc2ccc3c(NC4CN(c5cc(Cl)ncc5Cl)C4)ncnc3c21 10.1016/j.bmcl.2019.126811
CHEMBL4640119 176683 0 ACM4 M4 receptor 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
CHEMBL4635779 176391 0 ACM4 M4 receptor 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 86917 0 ACM4 M4 receptor 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 86917 0 ACM4 M4 receptor 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 163444 0 ACM4 M4 receptor 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 163444 0 ACM4 M4 receptor 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 158858 0 ACM4 M4 receptor 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 158858 0 ACM4 M4 receptor 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
89777266 147106 0 ACM4 M4 receptor Human 6.8 pEC50 = 6.8 Binding
Positive allosteric modulation of human M4 receptorPositive allosteric modulation of human M4 receptor
ChEMBL 342 4 2 6 2.8 COc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1 10.1016/j.bmcl.2016.11.086
CHEMBL3933538 147106 0 ACM4 M4 receptor Human 6.8 pEC50 = 6.8 Binding
Positive allosteric modulation of human M4 receptorPositive allosteric modulation of human M4 receptor
ChEMBL 342 4 2 6 2.8 COc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1 10.1016/j.bmcl.2016.11.086
CHEMBL4760902 180290 0 ACM4 M4 receptor 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
CHEMBL4780059 181093 0 ACM4 M4 receptor 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
683024 50823 19 ACM4 M4 receptor 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 50823 19 ACM4 M4 receptor 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 169636 0 ACM4 M4 receptor 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 169636 0 ACM4 M4 receptor 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 173563 0 ACM4 M4 receptor 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 173563 0 ACM4 M4 receptor 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 163416 0 ACM4 M4 receptor 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 163416 0 ACM4 M4 receptor 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 163416 0 ACM4 M4 receptor 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 163416 0 ACM4 M4 receptor 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 163459 0 ACM4 M4 receptor 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 163459 0 ACM4 M4 receptor 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 50823 19 ACM4 M4 receptor 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 50823 19 ACM4 M4 receptor 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 163459 0 ACM4 M4 receptor 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 163459 0 ACM4 M4 receptor 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
2551 750 19 ACM4 M4 receptor Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm501173q
298 750 19 ACM4 M4 receptor Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm501173q
488 750 19 ACM4 M4 receptor Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm501173q
CHEMBL965 750 19 ACM4 M4 receptor Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm501173q
DB00411 750 19 ACM4 M4 receptor Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm501173q
53382480 85662 0 ACM4 M4 receptor 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 85662 0 ACM4 M4 receptor 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 85663 11 ACM4 M4 receptor 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 85663 11 ACM4 M4 receptor 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 155627 0 ACM4 M4 receptor 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 155627 0 ACM4 M4 receptor 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
CHEMBL4647876 177245 0 ACM4 M4 receptor Rat 6.8 pEC50 = 6.8 Binding
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 391 3 2 7 1.9 Cn1nnc2ccc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)c(N)c21 10.1016/j.bmcl.2019.126811
CHEMBL4635732 176388 0 ACM4 M4 receptor 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
CHEMBL1223805 15720 0 ACM4 M4 receptor 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
CHEMBL1223862 15745 0 ACM4 M4 receptor 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 156704 0 ACM4 M4 receptor 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 156704 0 ACM4 M4 receptor 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
CHEMBL1223864 15747 0 ACM4 M4 receptor 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
CHEMBL1223938 15764 0 ACM4 M4 receptor 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 155866 0 ACM4 M4 receptor 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 155866 0 ACM4 M4 receptor 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 53188 5 ACM4 M4 receptor 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 53188 5 ACM4 M4 receptor 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 158222 0 ACM4 M4 receptor 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 158222 0 ACM4 M4 receptor 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
155524827 170078 0 ACM4 M4 receptor 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 170078 0 ACM4 M4 receptor 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 169481 0 ACM4 M4 receptor 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 169481 0 ACM4 M4 receptor 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 158858 0 ACM4 M4 receptor 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 158858 0 ACM4 M4 receptor 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
3652 3848 63 ACM4 M4 receptor Human 7.8 pEC50 = 7.8 Binding
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm501173q
57 3848 63 ACM4 M4 receptor Human 7.8 pEC50 = 7.8 Binding
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm501173q
60809 3848 63 ACM4 M4 receptor Human 7.8 pEC50 = 7.8 Binding
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm501173q
CHEMBL21536 3848 63 ACM4 M4 receptor Human 7.8 pEC50 = 7.8 Binding
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm501173q
DB15357 3848 63 ACM4 M4 receptor Human 7.8 pEC50 = 7.8 Binding
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm501173q
137646286 156999 0 ACM4 M4 receptor 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 156999 0 ACM4 M4 receptor 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 173817 0 ACM4 M4 receptor 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 173817 0 ACM4 M4 receptor 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 169460 0 ACM4 M4 receptor 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 169460 0 ACM4 M4 receptor 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 171519 0 ACM4 M4 receptor 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 171519 0 ACM4 M4 receptor 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 85662 0 ACM4 M4 receptor 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 85662 0 ACM4 M4 receptor 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 85663 11 ACM4 M4 receptor 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 85663 11 ACM4 M4 receptor 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 25794 5 ACM4 M4 receptor 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 25794 5 ACM4 M4 receptor 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 53188 5 ACM4 M4 receptor 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 53188 5 ACM4 M4 receptor 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
155510640 173188 0 ACM4 M4 receptor 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 173188 0 ACM4 M4 receptor 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 156781 0 ACM4 M4 receptor 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 156781 0 ACM4 M4 receptor 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 155866 0 ACM4 M4 receptor 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 155866 0 ACM4 M4 receptor 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 157182 0 ACM4 M4 receptor 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 157182 0 ACM4 M4 receptor 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 173188 0 ACM4 M4 receptor 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 173188 0 ACM4 M4 receptor 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
CHEMBL4639387 176640 0 ACM4 M4 receptor Rat 6.8 pEC50 = 6.8 Binding
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 375 3 2 7 1.4 Cn1nnc2ccc(C(=O)NC3CN(c4ncc(Cl)cc4F)C3)c(N)c21 10.1016/j.bmcl.2019.126811
CHEMBL4642156 176856 0 ACM4 M4 receptor Rat 6.8 pEC50 = 6.8 Binding
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 414 5 2 6 4.1 Cc1c2c(ccc3c(NCc4ccc(C(=O)NC5CCCC5)cc4)ncnc32)nn1C 10.1016/j.bmcl.2019.126811
137640564 156229 0 ACM4 M4 receptor 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 156229 0 ACM4 M4 receptor 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 139574 2 ACM4 M4 receptor 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 139574 2 ACM4 M4 receptor 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 174540 0 ACM4 M4 receptor 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 174540 0 ACM4 M4 receptor 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 156999 0 ACM4 M4 receptor 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 156999 0 ACM4 M4 receptor 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 163194 0 ACM4 M4 receptor 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 163194 0 ACM4 M4 receptor 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
73774630 144819 19 ACM4 M4 receptor 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 Cc1nnc2sc(C(=O)NCc3ccc(S(=O)(=O)C(F)(F)F)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
CHEMBL3915634 144819 19 ACM4 M4 receptor 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 Cc1nnc2sc(C(=O)NCc3ccc(S(=O)(=O)C(F)(F)F)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
89768534 150832 0 ACM4 M4 receptor 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 150832 0 ACM4 M4 receptor 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
73774630 144819 19 ACM4 M4 receptor 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 Cc1nnc2sc(C(=O)NCc3ccc(S(=O)(=O)C(F)(F)F)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
CHEMBL3915634 144819 19 ACM4 M4 receptor 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 Cc1nnc2sc(C(=O)NCc3ccc(S(=O)(=O)C(F)(F)F)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
89768534 150832 0 ACM4 M4 receptor 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 150832 0 ACM4 M4 receptor 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
CHEMBL4740272 178560 0 ACM4 M4 receptor 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 139574 2 ACM4 M4 receptor 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 139574 2 ACM4 M4 receptor 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 155627 0 ACM4 M4 receptor 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 155627 0 ACM4 M4 receptor 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
CHEMBL4648135 177266 0 ACM4 M4 receptor 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
CHEMBL4647288 177205 0 ACM4 M4 receptor 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
53382523 75470 0 ACM4 M4 receptor Rat 6.8 pEC50 = 6.8 Binding
Positive allosteric modulation of rat muscarinic M4 receptor assessed as acetylcholine responsePositive allosteric modulation of rat muscarinic M4 receptor assessed as acetylcholine response
ChEMBL 346 3 2 5 3.5 Cc1nc2sc(C(=O)NCc3ccncc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2057417 75470 0 ACM4 M4 receptor Rat 6.8 pEC50 = 6.8 Binding
Positive allosteric modulation of rat muscarinic M4 receptor assessed as acetylcholine responsePositive allosteric modulation of rat muscarinic M4 receptor assessed as acetylcholine response
ChEMBL 346 3 2 5 3.5 Cc1nc2sc(C(=O)NCc3ccncc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
127043636 139689 0 ACM4 M4 receptor 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 139689 0 ACM4 M4 receptor 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 85667 0 ACM4 M4 receptor 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 85667 0 ACM4 M4 receptor 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 85667 0 ACM4 M4 receptor 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 85667 0 ACM4 M4 receptor 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 157182 0 ACM4 M4 receptor 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 157182 0 ACM4 M4 receptor 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
53382523 75470 0 ACM4 M4 receptor Rat 6.8 pEC50 = 6.8 Binding
Positive allosteric modulation of rat muscarinic M4 receptor assessed as acetylcholine responsePositive allosteric modulation of rat muscarinic M4 receptor assessed as acetylcholine response
ChEMBL 346 3 2 5 3.5 Cc1nc2sc(C(=O)NCc3ccncc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
CHEMBL2057417 75470 0 ACM4 M4 receptor Rat 6.8 pEC50 = 6.8 Binding
Positive allosteric modulation of rat muscarinic M4 receptor assessed as acetylcholine responsePositive allosteric modulation of rat muscarinic M4 receptor assessed as acetylcholine response
ChEMBL 346 3 2 5 3.5 Cc1nc2sc(C(=O)NCc3ccncc3)c(N)c2c(C)c1Cl 10.1016/j.bmcl.2012.10.073
89777147 155569 0 ACM4 M4 receptor 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 155569 0 ACM4 M4 receptor 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 163798 0 ACM4 M4 receptor 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 163798 0 ACM4 M4 receptor 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 85665 11 ACM4 M4 receptor 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 85665 11 ACM4 M4 receptor 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 163798 0 ACM4 M4 receptor 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 163798 0 ACM4 M4 receptor 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 155569 0 ACM4 M4 receptor 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 155569 0 ACM4 M4 receptor 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 3848 63 ACM4 M4 receptor 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 3848 63 ACM4 M4 receptor 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 3848 63 ACM4 M4 receptor 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 3848 63 ACM4 M4 receptor 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 3848 63 ACM4 M4 receptor 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 163137 0 ACM4 M4 receptor 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 163137 0 ACM4 M4 receptor 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 163156 0 ACM4 M4 receptor 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 163156 0 ACM4 M4 receptor 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 163346 0 ACM4 M4 receptor 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 163346 0 ACM4 M4 receptor 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 158605 0 ACM4 M4 receptor 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 158605 0 ACM4 M4 receptor 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
118719922 115032 0 ACM4 M4 receptor Human 7.7 pEC50 = 7.7 Binding
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein engagement assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein engagement assay
ChEMBL 565 14 0 7 6.1 CN1CCC=C(c2nsnc2OCCCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
CHEMBL3354068 115032 0 ACM4 M4 receptor Human 7.7 pEC50 = 7.7 Binding
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein engagement assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein engagement assay
ChEMBL 565 14 0 7 6.1 CN1CCC=C(c2nsnc2OCCCCCCCC2CCN(CCCN3C(=O)CCc4ccccc43)CC2)C1 10.1021/jm501173q
137635043 155221 1 ACM4 M4 receptor 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 155221 1 ACM4 M4 receptor 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 169850 0 ACM4 M4 receptor 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 169850 0 ACM4 M4 receptor 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
CHEMBL4747706 179182 0 ACM4 M4 receptor 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 85665 11 ACM4 M4 receptor 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 85665 11 ACM4 M4 receptor 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 139689 0 ACM4 M4 receptor 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 139689 0 ACM4 M4 receptor 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
CHEMBL4635909 176396 0 ACM4 M4 receptor Rat 6.7 pEC50 = 6.7 Binding
Positive allosteric modulation of rat muscarinic M4 receptorPositive allosteric modulation of rat muscarinic M4 receptor
ChEMBL 351 4 1 6 3.6 COc1ccc(CNc2ncnc3c2ccc2nn(C)c(C)c23)cc1F 10.1016/j.bmcl.2019.126811
155540233 172061 0 ACM4 M4 receptor 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 172061 0 ACM4 M4 receptor 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 158467 0 ACM4 M4 receptor 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 158467 0 ACM4 M4 receptor 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 33580 8 ACM4 M4 receptor 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 33580 8 ACM4 M4 receptor 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 172061 0 ACM4 M4 receptor 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 172061 0 ACM4 M4 receptor 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 25557 0 ACM4 M4 receptor 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 25557 0 ACM4 M4 receptor 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
CHEMBL4644300 177009 0 ACM4 M4 receptor 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 156704 0 ACM4 M4 receptor 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 156704 0 ACM4 M4 receptor 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 156229 0 ACM4 M4 receptor 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 156229 0 ACM4 M4 receptor 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
3652 3848 63 ACM4 M4 receptor Human 6.7 pEC50 = 6.7 Binding
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based beta-arrestin engagement assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based beta-arrestin engagement assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm501173q
57 3848 63 ACM4 M4 receptor Human 6.7 pEC50 = 6.7 Binding
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based beta-arrestin engagement assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based beta-arrestin engagement assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm501173q
60809 3848 63 ACM4 M4 receptor Human 6.7 pEC50 = 6.7 Binding
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based beta-arrestin engagement assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based beta-arrestin engagement assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm501173q
CHEMBL21536 3848 63 ACM4 M4 receptor Human 6.7 pEC50 = 6.7 Binding
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based beta-arrestin engagement assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based beta-arrestin engagement assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm501173q
DB15357 3848 63 ACM4 M4 receptor Human 6.7 pEC50 = 6.7 Binding
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based beta-arrestin engagement assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based beta-arrestin engagement assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm501173q
127043450 139599 0 ACM4 M4 receptor 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 139599 0 ACM4 M4 receptor 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 158467 0 ACM4 M4 receptor 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 158467 0 ACM4 M4 receptor 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 155221 1 ACM4 M4 receptor 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 155221 1 ACM4 M4 receptor 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 79811 1 ACM4 M4 receptor 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 79811 1 ACM4 M4 receptor 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 174811 0 ACM4 M4 receptor 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 174811 0 ACM4 M4 receptor 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 139599 0 ACM4 M4 receptor 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 139599 0 ACM4 M4 receptor 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 52142 0 ACM4 M4 receptor 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 52142 0 ACM4 M4 receptor 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 174477 0 ACM4 M4 receptor 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 174477 0 ACM4 M4 receptor 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 174477 0 ACM4 M4 receptor 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 174477 0 ACM4 M4 receptor 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 156781 0 ACM4 M4 receptor 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 156781 0 ACM4 M4 receptor 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
CHEMBL1223861 15744 0 ACM4 M4 receptor 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
CHEMBL1223940 15766 0 ACM4 M4 receptor 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 79812 0 ACM4 M4 receptor 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 79812 0 ACM4 M4 receptor 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 163134 0 ACM4 M4 receptor 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 163134 0 ACM4 M4 receptor 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
118719926 115037 0 ACM4 M4 receptor Human 5.7 pEC50 = 5.7 Binding
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assay
ChEMBL 358 9 1 3 3.6 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCO)CC1 10.1021/jm501173q
CHEMBL3354073 115037 0 ACM4 M4 receptor Human 5.7 pEC50 = 5.7 Binding
Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assayAgonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assay
ChEMBL 358 9 1 3 3.6 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCO)CC1 10.1021/jm501173q
53382534 85670 0 ACM4 M4 receptor 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 85670 0 ACM4 M4 receptor 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 169532 0 ACM4 M4 receptor 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 169532 0 ACM4 M4 receptor 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 168969 0 ACM4 M4 receptor 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 168969 0 ACM4 M4 receptor 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
CHEMBL4776981 180841 0 ACM4 M4 receptor 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
CHEMBL4778766 180989 0 ACM4 M4 receptor 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
CHEMBL4782416 181282 0 ACM4 M4 receptor 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
CHEMBL4785432 181521 0 ACM4 M4 receptor 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 162783 0 ACM4 M4 receptor 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 162783 0 ACM4 M4 receptor 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 163092 0 ACM4 M4 receptor 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 163092 0 ACM4 M4 receptor 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 163480 0 ACM4 M4 receptor 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 163480 0 ACM4 M4 receptor 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 163134 0 ACM4 M4 receptor 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 163134 0 ACM4 M4 receptor 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 173862 0 ACM4 M4 receptor 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 173862 0 ACM4 M4 receptor 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 169226 0 ACM4 M4 receptor 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 169226 0 ACM4 M4 receptor 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 34735 0 ACM4 M4 receptor 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 34735 0 ACM4 M4 receptor 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 85670 0 ACM4 M4 receptor 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 85670 0 ACM4 M4 receptor 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
137642025 157311 0 ACM4 M4 receptor 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 157311 0 ACM4 M4 receptor 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 157311 0 ACM4 M4 receptor 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 157311 0 ACM4 M4 receptor 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 85649 0 ACM4 M4 receptor 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 85649 0 ACM4 M4 receptor 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 155515 0 ACM4 M4 receptor 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 155515 0 ACM4 M4 receptor 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 143487 0 ACM4 M4 receptor 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 143487 0 ACM4 M4 receptor 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 85649 0 ACM4 M4 receptor 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 85649 0 ACM4 M4 receptor 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 143487 0 ACM4 M4 receptor 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 143487 0 ACM4 M4 receptor 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 143487 0 ACM4 M4 receptor 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 143487 0 ACM4 M4 receptor 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 169953 0 ACM4 M4 receptor 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 169953 0 ACM4 M4 receptor 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 170952 0 ACM4 M4 receptor 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 170952 0 ACM4 M4 receptor 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 173593 0 ACM4 M4 receptor 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 173593 0 ACM4 M4 receptor 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 156820 0 ACM4 M4 receptor 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 156820 0 ACM4 M4 receptor 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 157496 0 ACM4 M4 receptor 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 157496 0 ACM4 M4 receptor 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 158784 0 ACM4 M4 receptor 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 158784 0 ACM4 M4 receptor 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 3243 12 ACM4 M4 receptor 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 3243 12 ACM4 M4 receptor 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 3243 12 ACM4 M4 receptor 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 3243 12 ACM4 M4 receptor 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 3243 12 ACM4 M4 receptor 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 53914 9 ACM4 M4 receptor 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 53914 9 ACM4 M4 receptor 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 53914 9 ACM4 M4 receptor 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 155505 0 ACM4 M4 receptor 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 155505 0 ACM4 M4 receptor 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 155505 0 ACM4 M4 receptor 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 155505 0 ACM4 M4 receptor 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
16757565 14927 0 ACM4 M4 receptor Human 6.7 pEC50 = 6.7 Binding
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 329 3 2 4 3.6 Cc1cc(C)c2c(N)c(C(=O)NCc3ccc(F)cc3)sc2n1 10.1021/jm401032k
CHEMBL1212989 14927 0 ACM4 M4 receptor Human 6.7 pEC50 = 6.7 Binding
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 329 3 2 4 3.6 Cc1cc(C)c2c(N)c(C(=O)NCc3ccc(F)cc3)sc2n1 10.1021/jm401032k
CHEMBL2435356 14927 0 ACM4 M4 receptor Human 6.7 pEC50 = 6.7 Binding
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 329 3 2 4 3.6 Cc1cc(C)c2c(N)c(C(=O)NCc3ccc(F)cc3)sc2n1 10.1021/jm401032k
134207726 174229 0 ACM4 M4 receptor 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 174229 0 ACM4 M4 receptor 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 163550 0 ACM4 M4 receptor 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 163550 0 ACM4 M4 receptor 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 156307 0 ACM4 M4 receptor 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 156307 0 ACM4 M4 receptor 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 153162 0 ACM4 M4 receptor 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 416 5 2 7 2.8 Cc1nnc2sc(C(=O)NCc3ccc(S(=O)(=O)C4CC4)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
CHEMBL3983700 153162 0 ACM4 M4 receptor 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 416 5 2 7 2.8 Cc1nnc2sc(C(=O)NCc3ccc(S(=O)(=O)C4CC4)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
89777160 153162 0 ACM4 M4 receptor 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 416 5 2 7 2.8 Cc1nnc2sc(C(=O)NCc3ccc(S(=O)(=O)C4CC4)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
CHEMBL3983700 153162 0 ACM4 M4 receptor 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 416 5 2 7 2.8 Cc1nnc2sc(C(=O)NCc3ccc(S(=O)(=O)C4CC4)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
155562860 174341 0 ACM4 M4 receptor Human 6.7 pEC50 = 6.7 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 364 2 2 7 2.1 Cc1cc2nncn2c2sc(C(=O)NC3Cc4cccnc4C3)c(N)c12 10.1016/j.bmcl.2019.06.032
CHEMBL4570659 174341 0 ACM4 M4 receptor Human 6.7 pEC50 = 6.7 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 364 2 2 7 2.1 Cc1cc2nncn2c2sc(C(=O)NC3Cc4cccnc4C3)c(N)c12 10.1016/j.bmcl.2019.06.032
CHEMBL4748261 179228 0 ACM4 M4 receptor Human 6.7 pEC50 = 6.7 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 400 3 2 9 1.5 Cc1c(Cl)nnc2sc(C(=O)NC3CN(c4ncncc4C#N)C3)c(N)c12 10.1016/j.bmcl.2019.05.026
16757565 14927 0 ACM4 M4 receptor Human 6.7 pEC50 = 6.7 Binding
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 329 3 2 4 3.6 Cc1cc(C)c2c(N)c(C(=O)NCc3ccc(F)cc3)sc2n1 10.1021/jm401032k
CHEMBL1212989 14927 0 ACM4 M4 receptor Human 6.7 pEC50 = 6.7 Binding
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 329 3 2 4 3.6 Cc1cc(C)c2c(N)c(C(=O)NCc3ccc(F)cc3)sc2n1 10.1021/jm401032k
CHEMBL2435356 14927 0 ACM4 M4 receptor Human 6.7 pEC50 = 6.7 Binding
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assayPositive allosteric modulation of human muscarinic M4 receptor expressed in CHO Flp-In cells assessed as stimulation of acetylcholine-induced ERK1/2 phosphorylation incubated under green light condition by fluorescence assay
ChEMBL 329 3 2 4 3.6 Cc1cc(C)c2c(N)c(C(=O)NCc3ccc(F)cc3)sc2n1 10.1021/jm401032k
89445250 170328 0 ACM4 M4 receptor 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 338 4 2 5 4.4 COc1ccc(CNc2n[nH]c3c2sc2nc(C)cc(C)c23)cc1 10.1016/j.bmcl.2018.12.039
CHEMBL4458842 170328 0 ACM4 M4 receptor 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 338 4 2 5 4.4 COc1ccc(CNc2n[nH]c3c2sc2nc(C)cc(C)c23)cc1 10.1016/j.bmcl.2018.12.039
155540893 172118 0 ACM4 M4 receptor 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 373 5 1 5 3.9 CCc1c(C(=O)NCc2ccc(OC)c(F)c2)sc2nnc(C)c(C)c12 10.1016/j.bmcl.2018.12.039
CHEMBL4517529 172118 0 ACM4 M4 receptor 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 373 5 1 5 3.9 CCc1c(C(=O)NCc2ccc(OC)c(F)c2)sc2nnc(C)c(C)c12 10.1016/j.bmcl.2018.12.039