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Ligand source activities (1 row/activity)

Ligand Receptor Assay information Chemical information
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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
2230 445 46 ACM5 M5 receptor Human - = Unclassified
UnclassifiedUnclassified
Guide to Pharmacology 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 32717485
2230 445 46 ACM5 M5 receptor Human - = Unclassified
UnclassifiedUnclassified
Guide to Pharmacology 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 7620715
296 445 46 ACM5 M5 receptor Human - = Unclassified
UnclassifiedUnclassified
Guide to Pharmacology 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 32717485
296 445 46 ACM5 M5 receptor Human - = Unclassified
UnclassifiedUnclassified
Guide to Pharmacology 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 7620715
CHEMBL7303 445 46 ACM5 M5 receptor Human - = Unclassified
UnclassifiedUnclassified
Guide to Pharmacology 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 32717485
CHEMBL7303 445 46 ACM5 M5 receptor Human - = Unclassified
UnclassifiedUnclassified
Guide to Pharmacology 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 7620715
DB04365 445 46 ACM5 M5 receptor Human - = Unclassified
UnclassifiedUnclassified
Guide to Pharmacology 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 32717485
DB04365 445 46 ACM5 M5 receptor Human - = Unclassified
UnclassifiedUnclassified
Guide to Pharmacology 155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C 7620715
2370 592 25 ACM5 M5 receptor Human - = Unclassified
UnclassifiedUnclassified
Guide to Pharmacology 161 3 1 2 0.2 CC(C[N+](C)(C)C)OC(=O)N 7620715
297 592 25 ACM5 M5 receptor Human - = Unclassified
UnclassifiedUnclassified
Guide to Pharmacology 161 3 1 2 0.2 CC(C[N+](C)(C)C)OC(=O)N 7620715
358 592 25 ACM5 M5 receptor Human - = Unclassified
UnclassifiedUnclassified
Guide to Pharmacology 161 3 1 2 0.2 CC(C[N+](C)(C)C)OC(=O)N 7620715
CHEMBL1482 592 25 ACM5 M5 receptor Human - = Unclassified
UnclassifiedUnclassified
Guide to Pharmacology 161 3 1 2 0.2 CC(C[N+](C)(C)C)OC(=O)N 7620715
DB01019 592 25 ACM5 M5 receptor Human - = Unclassified
UnclassifiedUnclassified
Guide to Pharmacology 161 3 1 2 0.2 CC(C[N+](C)(C)C)OC(=O)N 7620715
10104167 1928 0 ACM5 M5 receptor Human - = Unclassified
UnclassifiedUnclassified
Guide to Pharmacology 197 2 0 3 0.4 C[N+](CC#CCOC1=NOCC1)(C)C 24863257
6937 1928 0 ACM5 M5 receptor Human - = Unclassified
UnclassifiedUnclassified
Guide to Pharmacology 197 2 0 3 0.4 C[N+](CC#CCOC1=NOCC1)(C)C 24863257
CHEMBL3121473 1928 0 ACM5 M5 receptor Human - = Unclassified
UnclassifiedUnclassified
Guide to Pharmacology 197 2 0 3 0.4 C[N+](CC#CCOC1=NOCC1)(C)C 24863257
1726 2346 8 ACM5 M5 receptor Human - = Unclassified
UnclassifiedUnclassified
Guide to Pharmacology 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 7620715
1993 2346 8 ACM5 M5 receptor Human - = Unclassified
UnclassifiedUnclassified
Guide to Pharmacology 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 7620715
7438 2346 8 ACM5 M5 receptor Human - = Unclassified
UnclassifiedUnclassified
Guide to Pharmacology 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 7620715
CHEMBL978 2346 8 ACM5 M5 receptor Human - = Unclassified
UnclassifiedUnclassified
Guide to Pharmacology 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 7620715
DB06709 2346 8 ACM5 M5 receptor Human - = Unclassified
UnclassifiedUnclassified
Guide to Pharmacology 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 7620715
57525860 89400 0 ACM5 M5 receptor Rat 9.7 pEC50 = 9.7 Binding
Positive allosteric modulation of rat muscarinic M5 receptor assessed as effect on acetylcholine-induced responsePositive allosteric modulation of rat muscarinic M5 receptor assessed as effect on acetylcholine-induced response
ChEMBL 351 5 0 4 3.2 O=C1C(=O)N(CCOc2ccccc2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2013.03.032
CHEMBL2381694 89400 0 ACM5 M5 receptor Rat 9.7 pEC50 = 9.7 Binding
Positive allosteric modulation of rat muscarinic M5 receptor assessed as effect on acetylcholine-induced responsePositive allosteric modulation of rat muscarinic M5 receptor assessed as effect on acetylcholine-induced response
ChEMBL 351 5 0 4 3.2 O=C1C(=O)N(CCOc2ccccc2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2013.03.032
57525860 89400 0 ACM5 M5 receptor Rat 9.7 pEC50 = 9.7 Binding
Positive allosteric modulation of rat muscarinic M5 receptor assessed as effect on acetylcholine-induced responsePositive allosteric modulation of rat muscarinic M5 receptor assessed as effect on acetylcholine-induced response
ChEMBL 351 5 0 4 3.2 O=C1C(=O)N(CCOc2ccccc2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2013.03.032
CHEMBL2381694 89400 0 ACM5 M5 receptor Rat 9.7 pEC50 = 9.7 Binding
Positive allosteric modulation of rat muscarinic M5 receptor assessed as effect on acetylcholine-induced responsePositive allosteric modulation of rat muscarinic M5 receptor assessed as effect on acetylcholine-induced response
ChEMBL 351 5 0 4 3.2 O=C1C(=O)N(CCOc2ccccc2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2013.03.032
3257 3781 49 ACM5 M5 receptor Rat 9.6 pEC50 = 9.6 Binding
Positive allosteric modulation of rat muscarinic M5 receptor assessed as effect on acetylcholine-induced responsePositive allosteric modulation of rat muscarinic M5 receptor assessed as effect on acetylcholine-induced response
ChEMBL 351 4 0 4 3.3 COc1ccc(cc1)CN1c2ccc(cc2C(=O)C1=O)OC(F)(F)F 10.1016/j.bmcl.2013.03.032
42633508 3781 49 ACM5 M5 receptor Rat 9.6 pEC50 = 9.6 Binding
Positive allosteric modulation of rat muscarinic M5 receptor assessed as effect on acetylcholine-induced responsePositive allosteric modulation of rat muscarinic M5 receptor assessed as effect on acetylcholine-induced response
ChEMBL 351 4 0 4 3.3 COc1ccc(cc1)CN1c2ccc(cc2C(=O)C1=O)OC(F)(F)F 10.1016/j.bmcl.2013.03.032
CHEMBL466253 3781 49 ACM5 M5 receptor Rat 9.6 pEC50 = 9.6 Binding
Positive allosteric modulation of rat muscarinic M5 receptor assessed as effect on acetylcholine-induced responsePositive allosteric modulation of rat muscarinic M5 receptor assessed as effect on acetylcholine-induced response
ChEMBL 351 4 0 4 3.3 COc1ccc(cc1)CN1c2ccc(cc2C(=O)C1=O)OC(F)(F)F 10.1016/j.bmcl.2013.03.032
3257 3781 49 ACM5 M5 receptor Rat 9.6 pEC50 = 9.6 Binding
Positive allosteric modulation of rat muscarinic M5 receptor assessed as effect on acetylcholine-induced responsePositive allosteric modulation of rat muscarinic M5 receptor assessed as effect on acetylcholine-induced response
ChEMBL 351 4 0 4 3.3 COc1ccc(cc1)CN1c2ccc(cc2C(=O)C1=O)OC(F)(F)F 10.1016/j.bmcl.2013.03.032
42633508 3781 49 ACM5 M5 receptor Rat 9.6 pEC50 = 9.6 Binding
Positive allosteric modulation of rat muscarinic M5 receptor assessed as effect on acetylcholine-induced responsePositive allosteric modulation of rat muscarinic M5 receptor assessed as effect on acetylcholine-induced response
ChEMBL 351 4 0 4 3.3 COc1ccc(cc1)CN1c2ccc(cc2C(=O)C1=O)OC(F)(F)F 10.1016/j.bmcl.2013.03.032
CHEMBL466253 3781 49 ACM5 M5 receptor Rat 9.6 pEC50 = 9.6 Binding
Positive allosteric modulation of rat muscarinic M5 receptor assessed as effect on acetylcholine-induced responsePositive allosteric modulation of rat muscarinic M5 receptor assessed as effect on acetylcholine-induced response
ChEMBL 351 4 0 4 3.3 COc1ccc(cc1)CN1c2ccc(cc2C(=O)C1=O)OC(F)(F)F 10.1016/j.bmcl.2013.03.032
187 245 23 ACM5 M5 receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human muscarinic M5 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human muscarinic M5 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 ACM5 M5 receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human muscarinic M5 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human muscarinic M5 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 ACM5 M5 receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human muscarinic M5 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human muscarinic M5 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 ACM5 M5 receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human muscarinic M5 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human muscarinic M5 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 ACM5 M5 receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human muscarinic M5 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human muscarinic M5 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 ACM5 M5 receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human muscarinic M5 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human muscarinic M5 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
187 245 23 ACM5 M5 receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human muscarinic M5 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in BHK-21 cells 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 ACM5 M5 receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human muscarinic M5 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in BHK-21 cells 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 ACM5 M5 receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human muscarinic M5 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in BHK-21 cells 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 ACM5 M5 receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human muscarinic M5 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in BHK-21 cells 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 ACM5 M5 receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human muscarinic M5 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in BHK-21 cells 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 ACM5 M5 receptor Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human muscarinic M5 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in BHK-21 cells 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
2551 750 19 ACM5 M5 receptor Human 6.0 pEC50 = 6 Functional
Agonist activity at human M5 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M5 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0606995
298 750 19 ACM5 M5 receptor Human 6.0 pEC50 = 6 Functional
Agonist activity at human M5 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M5 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0606995
488 750 19 ACM5 M5 receptor Human 6.0 pEC50 = 6 Functional
Agonist activity at human M5 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M5 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0606995
CHEMBL965 750 19 ACM5 M5 receptor Human 6.0 pEC50 = 6 Functional
Agonist activity at human M5 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M5 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0606995
DB00411 750 19 ACM5 M5 receptor Human 6.0 pEC50 = 6 Functional
Agonist activity at human M5 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M5 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0606995
334 227 15 ACM5 M5 receptor Human 6.0 pEC50 = 6 Functional
Agonist activity at human muscarinic M5 receptor by calcium mobilization assayAgonist activity at human muscarinic M5 receptor by calcium mobilization assay
ChEMBL 348 7 0 3 3.8 CCCCC1CCN(CC1)CCCN1C(=O)COc2c1ccc(c2)F 10.1016/j.bmcl.2012.03.088
9928284 227 15 ACM5 M5 receptor Human 6.0 pEC50 = 6 Functional
Agonist activity at human muscarinic M5 receptor by calcium mobilization assayAgonist activity at human muscarinic M5 receptor by calcium mobilization assay
ChEMBL 348 7 0 3 3.8 CCCCC1CCN(CC1)CCCN1C(=O)COc2c1ccc(c2)F 10.1016/j.bmcl.2012.03.088
CHEMBL2022960 227 15 ACM5 M5 receptor Human 6.0 pEC50 = 6 Functional
Agonist activity at human muscarinic M5 receptor by calcium mobilization assayAgonist activity at human muscarinic M5 receptor by calcium mobilization assay
ChEMBL 348 7 0 3 3.8 CCCCC1CCN(CC1)CCCN1C(=O)COc2c1ccc(c2)F 10.1016/j.bmcl.2012.03.088
CHEMBL1223807 15722 0 ACM5 M5 receptor Human 6.0 pEC50 = 6 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells 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
CHEMBL1223941 15767 0 ACM5 M5 receptor Human 6.0 pEC50 = 6 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 413 6 0 7 3.5 COCCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(C#N)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
17516658 53128 5 ACM5 M5 receptor Human 5.0 pEC50 = 5 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 444 6 0 5 2.9 CCN(Cc1ccccc1)C(=O)C1CCN(S(=O)(=O)c2ccc3c(c2)OCCO3)CC1 10.1021/jm500995y
CHEMBL1602658 53128 5 ACM5 M5 receptor Human 5.0 pEC50 = 5 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 444 6 0 5 2.9 CCN(Cc1ccccc1)C(=O)C1CCN(S(=O)(=O)c2ccc3c(c2)OCCO3)CC1 10.1021/jm500995y
57525872 89401 0 ACM5 M5 receptor Human 6.0 pEC50 = 6.0 Binding
Positive allosteric modulation of human muscarinic M5 receptorPositive allosteric modulation of human muscarinic M5 receptor
ChEMBL 443 7 0 5 5.0 O=C1C(=O)N(CCOc2ccc(Oc3ccccc3)cc2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2013.03.032
CHEMBL2381695 89401 0 ACM5 M5 receptor Human 6.0 pEC50 = 6.0 Binding
Positive allosteric modulation of human muscarinic M5 receptorPositive allosteric modulation of human muscarinic M5 receptor
ChEMBL 443 7 0 5 5.0 O=C1C(=O)N(CCOc2ccc(Oc3ccccc3)cc2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2013.03.032
57525872 89401 0 ACM5 M5 receptor Human 6.0 pEC50 = 6.0 Binding
Positive allosteric modulation of human muscarinic M5 receptorPositive allosteric modulation of human muscarinic M5 receptor
ChEMBL 443 7 0 5 5.0 O=C1C(=O)N(CCOc2ccc(Oc3ccccc3)cc2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2013.03.032
CHEMBL2381695 89401 0 ACM5 M5 receptor Human 6.0 pEC50 = 6.0 Binding
Positive allosteric modulation of human muscarinic M5 receptorPositive allosteric modulation of human muscarinic M5 receptor
ChEMBL 443 7 0 5 5.0 O=C1C(=O)N(CCOc2ccc(Oc3ccccc3)cc2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2013.03.032
10465280 102073 1 ACM5 M5 receptor Human 7.0 pEC50 = 7.0 Binding
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M5 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M5 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 196 2 1 4 1.5 CC(C)Oc1noc2c1CNCCC2 10.1021/jm00012a019
CHEMBL305264 102073 1 ACM5 M5 receptor Human 7.0 pEC50 = 7.0 Binding
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M5 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M5 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 196 2 1 4 1.5 CC(C)Oc1noc2c1CNCCC2 10.1021/jm00012a019
3257 3781 49 ACM5 M5 receptor Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilizationAgonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilization
ChEMBL 351 4 0 4 3.3 COc1ccc(cc1)CN1c2ccc(cc2C(=O)C1=O)OC(F)(F)F 10.1016/j.bmcl.2009.11.089
42633508 3781 49 ACM5 M5 receptor Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilizationAgonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilization
ChEMBL 351 4 0 4 3.3 COc1ccc(cc1)CN1c2ccc(cc2C(=O)C1=O)OC(F)(F)F 10.1016/j.bmcl.2009.11.089
CHEMBL466253 3781 49 ACM5 M5 receptor Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilizationAgonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilization
ChEMBL 351 4 0 4 3.3 COc1ccc(cc1)CN1c2ccc(cc2C(=O)C1=O)OC(F)(F)F 10.1016/j.bmcl.2009.11.089
3257 3781 49 ACM5 M5 receptor Human 6.0 pEC50 = 6.0 Binding
Positive allosteric modulation of human muscarinic M5 receptorPositive allosteric modulation of human muscarinic M5 receptor
ChEMBL 351 4 0 4 3.3 COc1ccc(cc1)CN1c2ccc(cc2C(=O)C1=O)OC(F)(F)F 10.1016/j.bmcl.2013.03.032
42633508 3781 49 ACM5 M5 receptor Human 6.0 pEC50 = 6.0 Binding
Positive allosteric modulation of human muscarinic M5 receptorPositive allosteric modulation of human muscarinic M5 receptor
ChEMBL 351 4 0 4 3.3 COc1ccc(cc1)CN1c2ccc(cc2C(=O)C1=O)OC(F)(F)F 10.1016/j.bmcl.2013.03.032
CHEMBL466253 3781 49 ACM5 M5 receptor Human 6.0 pEC50 = 6.0 Binding
Positive allosteric modulation of human muscarinic M5 receptorPositive allosteric modulation of human muscarinic M5 receptor
ChEMBL 351 4 0 4 3.3 COc1ccc(cc1)CN1c2ccc(cc2C(=O)C1=O)OC(F)(F)F 10.1016/j.bmcl.2013.03.032
71737628 113467 0 ACM5 M5 receptor Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 442 6 0 4 3.6 CCN(C(=O)C1CCN(S(=O)(=O)c2ccc3c(c2)CCO3)CC1)[C@H](C)c1ccccc1 10.1021/jm500995y
CHEMBL3329738 113467 0 ACM5 M5 receptor Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 442 6 0 4 3.6 CCN(C(=O)C1CCN(S(=O)(=O)c2ccc3c(c2)CCO3)CC1)[C@H](C)c1ccccc1 10.1021/jm500995y
71737628 113467 0 ACM5 M5 receptor Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 442 6 0 4 3.6 CCN(C(=O)C1CCN(S(=O)(=O)c2ccc3c(c2)CCO3)CC1)[C@H](C)c1ccccc1 10.1021/jm500995y
CHEMBL3329738 113467 0 ACM5 M5 receptor Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 442 6 0 4 3.6 CCN(C(=O)C1CCN(S(=O)(=O)c2ccc3c(c2)CCO3)CC1)[C@H](C)c1ccccc1 10.1021/jm500995y
3257 3781 49 ACM5 M5 receptor Human 5.9 pEC50 = 5.9 Functional
Activation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 351 4 0 4 3.3 COc1ccc(cc1)CN1c2ccc(cc2C(=O)C1=O)OC(F)(F)F 10.1021/jm900286j
42633508 3781 49 ACM5 M5 receptor Human 5.9 pEC50 = 5.9 Functional
Activation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 351 4 0 4 3.3 COc1ccc(cc1)CN1c2ccc(cc2C(=O)C1=O)OC(F)(F)F 10.1021/jm900286j
CHEMBL466253 3781 49 ACM5 M5 receptor Human 5.9 pEC50 = 5.9 Functional
Activation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 351 4 0 4 3.3 COc1ccc(cc1)CN1c2ccc(cc2C(=O)C1=O)OC(F)(F)F 10.1021/jm900286j
CHEMBL1223754 15696 0 ACM5 M5 receptor Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells 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
118712536 113487 0 ACM5 M5 receptor Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 536 6 1 4 5.1 CC(C)(C)CN(Cc1ccccc1C(F)(F)F)C(=O)C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1 10.1021/jm500995y
CHEMBL3329764 113487 0 ACM5 M5 receptor Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 536 6 1 4 5.1 CC(C)(C)CN(Cc1ccccc1C(F)(F)F)C(=O)C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1 10.1021/jm500995y
118712537 113488 0 ACM5 M5 receptor Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 520 7 1 4 4.4 O=C(C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1)N(Cc1ccccc1C(F)(F)F)CC1CC1 10.1021/jm500995y
CHEMBL3329765 113488 0 ACM5 M5 receptor Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 520 7 1 4 4.4 O=C(C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1)N(Cc1ccccc1C(F)(F)F)CC1CC1 10.1021/jm500995y
118712537 113488 0 ACM5 M5 receptor Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 520 7 1 4 4.4 O=C(C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1)N(Cc1ccccc1C(F)(F)F)CC1CC1 10.1021/jm500995y
CHEMBL3329765 113488 0 ACM5 M5 receptor Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 520 7 1 4 4.4 O=C(C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1)N(Cc1ccccc1C(F)(F)F)CC1CC1 10.1021/jm500995y
44208359 16340 0 ACM5 M5 receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human muscarinic M5 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 501 9 1 5 3.5 COc1ccc(CC(=O)NC2CCN(CCCN3C(=O)CCc4cc(F)c(F)cc43)CC2)cc1OC 10.1021/jm100697g
CHEMBL1242979 16340 0 ACM5 M5 receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human muscarinic M5 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 501 9 1 5 3.5 COc1ccc(CC(=O)NC2CCN(CCCN3C(=O)CCc4cc(F)c(F)cc43)CC2)cc1OC 10.1021/jm100697g
3257 3781 49 ACM5 M5 receptor Human 5.9 pEC50 = 5.9 Binding
Positive allosteric modulation activity at muscarinic M5 receptorPositive allosteric modulation activity at muscarinic M5 receptor
ChEMBL 351 4 0 4 3.3 COc1ccc(cc1)CN1c2ccc(cc2C(=O)C1=O)OC(F)(F)F 10.1021/jm201139r
42633508 3781 49 ACM5 M5 receptor Human 5.9 pEC50 = 5.9 Binding
Positive allosteric modulation activity at muscarinic M5 receptorPositive allosteric modulation activity at muscarinic M5 receptor
ChEMBL 351 4 0 4 3.3 COc1ccc(cc1)CN1c2ccc(cc2C(=O)C1=O)OC(F)(F)F 10.1021/jm201139r
CHEMBL466253 3781 49 ACM5 M5 receptor Human 5.9 pEC50 = 5.9 Binding
Positive allosteric modulation activity at muscarinic M5 receptorPositive allosteric modulation activity at muscarinic M5 receptor
ChEMBL 351 4 0 4 3.3 COc1ccc(cc1)CN1c2ccc(cc2C(=O)C1=O)OC(F)(F)F 10.1021/jm201139r
306 3243 12 ACM5 M5 receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M5 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 ACM5 M5 receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M5 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 ACM5 M5 receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M5 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 ACM5 M5 receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M5 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 ACM5 M5 receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M5 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
118712536 113487 0 ACM5 M5 receptor Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 536 6 1 4 5.1 CC(C)(C)CN(Cc1ccccc1C(F)(F)F)C(=O)C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1 10.1021/jm500995y
CHEMBL3329764 113487 0 ACM5 M5 receptor Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 536 6 1 4 5.1 CC(C)(C)CN(Cc1ccccc1C(F)(F)F)C(=O)C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1 10.1021/jm500995y
CHEMBL1223805 15720 0 ACM5 M5 receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells 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
CHEMBL1223864 15747 0 ACM5 M5 receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells 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
16123945 79813 8 ACM5 M5 receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assay
ChEMBL 315 2 1 4 2.5 Cc1ccc2[nH]c(=O)n(C3CCN(C4CCOCC4)CC3)c2c1 10.1021/ml100105x
CHEMBL2146599 79813 8 ACM5 M5 receptor Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assay
ChEMBL 315 2 1 4 2.5 Cc1ccc2[nH]c(=O)n(C3CCN(C4CCOCC4)CC3)c2c1 10.1021/ml100105x
10182490 13591 0 ACM5 M5 receptor Human 5.9 pEC50 = 5.9 Binding
Effective concentration was evaluated against Muscarinic acetylcholine receptor M5 expressed in A9 L cellsEffective concentration was evaluated against Muscarinic acetylcholine receptor M5 expressed in A9 L cells
ChEMBL 415 14 0 10 1.2 CC(=O)OCCOCCOCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0301235
CHEMBL1196131 13591 0 ACM5 M5 receptor Human 5.9 pEC50 = 5.9 Binding
Effective concentration was evaluated against Muscarinic acetylcholine receptor M5 expressed in A9 L cellsEffective concentration was evaluated against Muscarinic acetylcholine receptor M5 expressed in A9 L cells
ChEMBL 415 14 0 10 1.2 CC(=O)OCCOCCOCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0301235
CHEMBL555992 13591 0 ACM5 M5 receptor Human 5.9 pEC50 = 5.9 Binding
Effective concentration was evaluated against Muscarinic acetylcholine receptor M5 expressed in A9 L cellsEffective concentration was evaluated against Muscarinic acetylcholine receptor M5 expressed in A9 L cells
ChEMBL 415 14 0 10 1.2 CC(=O)OCCOCCOCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0301235
71771056 113485 0 ACM5 M5 receptor Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 512 7 1 4 4.0 O=C(C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1)N(CCF)Cc1ccccc1C(F)(F)F 10.1021/jm500995y
CHEMBL3329762 113485 0 ACM5 M5 receptor Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 512 7 1 4 4.0 O=C(C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1)N(CCF)Cc1ccccc1C(F)(F)F 10.1021/jm500995y
3652 3848 63 ACM5 M5 receptor Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human M5 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M5 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
57 3848 63 ACM5 M5 receptor Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human M5 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M5 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
60809 3848 63 ACM5 M5 receptor Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human M5 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M5 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
CHEMBL21536 3848 63 ACM5 M5 receptor Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human M5 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M5 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
DB15357 3848 63 ACM5 M5 receptor Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human M5 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M5 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
118712538 113489 0 ACM5 M5 receptor Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 534 7 1 4 4.8 O=C(C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1)N(Cc1ccccc1C(F)(F)F)CC1CCC1 10.1021/jm500995y
CHEMBL3329766 113489 0 ACM5 M5 receptor Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 534 7 1 4 4.8 O=C(C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1)N(Cc1ccccc1C(F)(F)F)CC1CCC1 10.1021/jm500995y
118712538 113489 0 ACM5 M5 receptor Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 534 7 1 4 4.8 O=C(C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1)N(Cc1ccccc1C(F)(F)F)CC1CCC1 10.1021/jm500995y
CHEMBL3329766 113489 0 ACM5 M5 receptor Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 534 7 1 4 4.8 O=C(C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1)N(Cc1ccccc1C(F)(F)F)CC1CCC1 10.1021/jm500995y
9308 17386 10 ACM5 M5 receptor Human 5.9 pEC50 = 5.9 Binding
Activation of M5-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M5-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
ChEMBL 174 2 1 2 0.2 C[C@@H]1O[C@H](C[N+](C)(C)C)C[C@H]1O 10.1016/j.bmc.2010.07.060
CHEMBL1255785 17386 10 ACM5 M5 receptor Human 5.9 pEC50 = 5.9 Binding
Activation of M5-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M5-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
ChEMBL 174 2 1 2 0.2 C[C@@H]1O[C@H](C[N+](C)(C)C)C[C@H]1O 10.1016/j.bmc.2010.07.060
CHEMBL12587 17386 10 ACM5 M5 receptor Human 5.9 pEC50 = 5.9 Binding
Activation of M5-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M5-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
ChEMBL 174 2 1 2 0.2 C[C@@H]1O[C@H](C[N+](C)(C)C)C[C@H]1O 10.1016/j.bmc.2010.07.060
CHEMBL292911 17386 10 ACM5 M5 receptor Human 5.9 pEC50 = 5.9 Binding
Activation of M5-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M5-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
ChEMBL 174 2 1 2 0.2 C[C@@H]1O[C@H](C[N+](C)(C)C)C[C@H]1O 10.1016/j.bmc.2010.07.060
139414008 163537 0 ACM5 M5 receptor Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of M5 receptor (unknown origin)Positive allosteric modulation of M5 receptor (unknown origin)
ChEMBL 346 2 1 2 5.1 CC(C)[C@@H]1N=C(c2ccccc2F)c2cc(Cl)ccc2NC1=S 10.1016/j.bmcl.2017.11.008
CHEMBL4212760 163537 0 ACM5 M5 receptor Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of M5 receptor (unknown origin)Positive allosteric modulation of M5 receptor (unknown origin)
ChEMBL 346 2 1 2 5.1 CC(C)[C@@H]1N=C(c2ccccc2F)c2cc(Cl)ccc2NC1=S 10.1016/j.bmcl.2017.11.008
71771056 113485 0 ACM5 M5 receptor Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 512 7 1 4 4.0 O=C(C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1)N(CCF)Cc1ccccc1C(F)(F)F 10.1021/jm500995y
CHEMBL3329762 113485 0 ACM5 M5 receptor Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 512 7 1 4 4.0 O=C(C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1)N(CCF)Cc1ccccc1C(F)(F)F 10.1021/jm500995y
3652 3848 63 ACM5 M5 receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human muscarinic M5 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm100697g
57 3848 63 ACM5 M5 receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human muscarinic M5 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm100697g
60809 3848 63 ACM5 M5 receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human muscarinic M5 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm100697g
CHEMBL21536 3848 63 ACM5 M5 receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human muscarinic M5 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm100697g
DB15357 3848 63 ACM5 M5 receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human muscarinic M5 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm100697g
57525867 89398 0 ACM5 M5 receptor Human 5.9 pEC50 = 5.9 Binding
Positive allosteric modulation of human muscarinic M5 receptorPositive allosteric modulation of human muscarinic M5 receptor
ChEMBL 412 6 1 6 2.6 COc1ccc(CN2C(=O)C(O)(C[N+](=O)[O-])c3cc(OC(F)(F)F)ccc32)cc1 10.1016/j.bmcl.2013.03.032
CHEMBL2381692 89398 0 ACM5 M5 receptor Human 5.9 pEC50 = 5.9 Binding
Positive allosteric modulation of human muscarinic M5 receptorPositive allosteric modulation of human muscarinic M5 receptor
ChEMBL 412 6 1 6 2.6 COc1ccc(CN2C(=O)C(O)(C[N+](=O)[O-])c3cc(OC(F)(F)F)ccc32)cc1 10.1016/j.bmcl.2013.03.032
3652 3848 63 ACM5 M5 receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1016/j.bmcl.2015.08.011
57 3848 63 ACM5 M5 receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1016/j.bmcl.2015.08.011
60809 3848 63 ACM5 M5 receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1016/j.bmcl.2015.08.011
CHEMBL21536 3848 63 ACM5 M5 receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1016/j.bmcl.2015.08.011
DB15357 3848 63 ACM5 M5 receptor Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1016/j.bmcl.2015.08.011
118712535 113486 0 ACM5 M5 receptor Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 522 7 1 4 4.8 CCC(C)N(Cc1ccccc1C(F)(F)F)C(=O)C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1 10.1021/jm500995y
CHEMBL3329763 113486 0 ACM5 M5 receptor Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 522 7 1 4 4.8 CCC(C)N(Cc1ccccc1C(F)(F)F)C(=O)C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1 10.1021/jm500995y
46945663 17174 0 ACM5 M5 receptor Human 5.8 pEC50 = 5.8 Binding
Positive allosteric modulation of human muscarinic M5 receptorPositive allosteric modulation of human muscarinic M5 receptor
ChEMBL 432 5 0 5 4.6 O=C1C(=O)N(Cc2ccc(Oc3cccc(F)n3)cc2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2013.03.032
CHEMBL1257975 17174 0 ACM5 M5 receptor Human 5.8 pEC50 = 5.8 Binding
Positive allosteric modulation of human muscarinic M5 receptorPositive allosteric modulation of human muscarinic M5 receptor
ChEMBL 432 5 0 5 4.6 O=C1C(=O)N(Cc2ccc(Oc3cccc(F)n3)cc2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2013.03.032
46945663 17174 0 ACM5 M5 receptor Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assayPositive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 432 5 0 5 4.6 O=C1C(=O)N(Cc2ccc(Oc3cccc(F)n3)cc2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2010.08.042
CHEMBL1257975 17174 0 ACM5 M5 receptor Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assayPositive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 432 5 0 5 4.6 O=C1C(=O)N(Cc2ccc(Oc3cccc(F)n3)cc2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2010.08.042
71737627 113471 0 ACM5 M5 receptor Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 444 6 1 4 3.2 CCN(Cc1cccc(F)c1)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1 10.1021/jm500995y
CHEMBL3329743 113471 0 ACM5 M5 receptor Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 444 6 1 4 3.2 CCN(Cc1cccc(F)c1)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1 10.1021/jm500995y
118712535 113486 0 ACM5 M5 receptor Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 522 7 1 4 4.8 CCC(C)N(Cc1ccccc1C(F)(F)F)C(=O)C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1 10.1021/jm500995y
CHEMBL3329763 113486 0 ACM5 M5 receptor Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 522 7 1 4 4.8 CCC(C)N(Cc1ccccc1C(F)(F)F)C(=O)C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1 10.1021/jm500995y
71737627 113471 0 ACM5 M5 receptor Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 444 6 1 4 3.2 CCN(Cc1cccc(F)c1)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1 10.1021/jm500995y
CHEMBL3329743 113471 0 ACM5 M5 receptor Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 444 6 1 4 3.2 CCN(Cc1cccc(F)c1)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1 10.1021/jm500995y
71771058 113482 0 ACM5 M5 receptor Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 508 7 1 4 4.4 CCCN(Cc1ccccc1C(F)(F)F)C(=O)C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1 10.1021/jm500995y
CHEMBL3329756 113482 0 ACM5 M5 receptor Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 508 7 1 4 4.4 CCCN(Cc1ccccc1C(F)(F)F)C(=O)C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1 10.1021/jm500995y
71737578 113461 0 ACM5 M5 receptor Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 426 6 1 4 3.0 CCN(Cc1ccccc1)C(=O)C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1 10.1021/jm500995y
CHEMBL3329730 113461 0 ACM5 M5 receptor Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 426 6 1 4 3.0 CCN(Cc1ccccc1)C(=O)C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1 10.1021/jm500995y
CHEMBL1223861 15744 0 ACM5 M5 receptor Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells 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
CHEMBL1223862 15745 0 ACM5 M5 receptor Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells 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
CHEMBL1223940 15766 0 ACM5 M5 receptor Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells 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
44204999 63261 5 ACM5 M5 receptor Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assay
ChEMBL 369 6 1 4 3.6 O=c1[nH]c2ccccc2n1C1CCN(CCCOc2ccc(F)cc2)CC1 10.1021/ml100105x
CHEMBL1802360 63261 5 ACM5 M5 receptor Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assay
ChEMBL 369 6 1 4 3.6 O=c1[nH]c2ccccc2n1C1CCN(CCCOc2ccc(F)cc2)CC1 10.1021/ml100105x
71771058 113482 0 ACM5 M5 receptor Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 508 7 1 4 4.4 CCCN(Cc1ccccc1C(F)(F)F)C(=O)C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1 10.1021/jm500995y
CHEMBL3329756 113482 0 ACM5 M5 receptor Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 508 7 1 4 4.4 CCCN(Cc1ccccc1C(F)(F)F)C(=O)C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1 10.1021/jm500995y
52947398 16990 0 ACM5 M5 receptor Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assayPositive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 398 4 0 4 4.4 O=C1C(=O)N(Cc2ccc(-c3cccnc3)cc2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2010.08.042
CHEMBL1257388 16990 0 ACM5 M5 receptor Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assayPositive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 398 4 0 4 4.4 O=C1C(=O)N(Cc2ccc(-c3cccnc3)cc2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2010.08.042
45281794 193318 37 ACM5 M5 receptor Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assayPositive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 397 4 0 3 5.0 O=C1C(=O)N(Cc2ccc(-c3ccccc3)cc2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2010.08.042
CHEMBL593506 193318 37 ACM5 M5 receptor Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assayPositive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 397 4 0 3 5.0 O=C1C(=O)N(Cc2ccc(-c3ccccc3)cc2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2010.08.042
71737578 113461 0 ACM5 M5 receptor Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 426 6 1 4 3.0 CCN(Cc1ccccc1)C(=O)C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1 10.1021/jm500995y
CHEMBL3329730 113461 0 ACM5 M5 receptor Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 426 6 1 4 3.0 CCN(Cc1ccccc1)C(=O)C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1 10.1021/jm500995y
71737646 113473 0 ACM5 M5 receptor Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 460 6 1 4 3.7 CCN(Cc1cccc(Cl)c1)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1 10.1021/jm500995y
CHEMBL3329745 113473 0 ACM5 M5 receptor Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 460 6 1 4 3.7 CCN(Cc1cccc(Cl)c1)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1 10.1021/jm500995y
71737646 113473 0 ACM5 M5 receptor Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 460 6 1 4 3.7 CCN(Cc1cccc(Cl)c1)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1 10.1021/jm500995y
CHEMBL3329745 113473 0 ACM5 M5 receptor Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 460 6 1 4 3.7 CCN(Cc1cccc(Cl)c1)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1 10.1021/jm500995y
71737611 113462 0 ACM5 M5 receptor Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 426 6 1 4 3.0 CCN(Cc1ccccc1)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1 10.1021/jm500995y
CHEMBL3329731 113462 0 ACM5 M5 receptor Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 426 6 1 4 3.0 CCN(Cc1ccccc1)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1 10.1021/jm500995y
135409468 199515 54 ACM5 M5 receptor Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human muscarinic M5 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 312 0 2 4 3.4 Clc1ccc2c(c1)N=C(N1CCNCC1)c1ccccc1N2 10.1021/jm100697g
CHEMBL845 199515 54 ACM5 M5 receptor Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human muscarinic M5 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 312 0 2 4 3.4 Clc1ccc2c(c1)N=C(N1CCNCC1)c1ccccc1N2 10.1021/jm100697g
44158075 177948 0 ACM5 M5 receptor Human 5.8 pEC50 = 5.8 Functional
Activation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 351 4 0 4 3.3 COc1cccc(CN2C(=O)C(=O)c3cc(OC(F)(F)F)ccc32)c1 10.1021/jm900286j
CHEMBL469144 177948 0 ACM5 M5 receptor Human 5.8 pEC50 = 5.8 Functional
Activation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 351 4 0 4 3.3 COc1cccc(CN2C(=O)C(=O)c3cc(OC(F)(F)F)ccc32)c1 10.1021/jm900286j
71737611 113462 0 ACM5 M5 receptor Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 426 6 1 4 3.0 CCN(Cc1ccccc1)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1 10.1021/jm500995y
CHEMBL3329731 113462 0 ACM5 M5 receptor Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 426 6 1 4 3.0 CCN(Cc1ccccc1)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1 10.1021/jm500995y
71771053 113483 0 ACM5 M5 receptor Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 506 7 1 4 4.2 C=CCN(Cc1ccccc1C(F)(F)F)C(=O)C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1 10.1021/jm500995y
CHEMBL3329757 113483 0 ACM5 M5 receptor Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 506 7 1 4 4.2 C=CCN(Cc1ccccc1C(F)(F)F)C(=O)C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1 10.1021/jm500995y
118712534 113484 0 ACM5 M5 receptor Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 520 6 1 4 4.6 O=C(C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1)N(Cc1ccccc1C(F)(F)F)C1CCC1 10.1021/jm500995y
CHEMBL3329760 113484 0 ACM5 M5 receptor Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 520 6 1 4 4.6 O=C(C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1)N(Cc1ccccc1C(F)(F)F)C1CCC1 10.1021/jm500995y
71771053 113483 0 ACM5 M5 receptor Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 506 7 1 4 4.2 C=CCN(Cc1ccccc1C(F)(F)F)C(=O)C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1 10.1021/jm500995y
CHEMBL3329757 113483 0 ACM5 M5 receptor Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 506 7 1 4 4.2 C=CCN(Cc1ccccc1C(F)(F)F)C(=O)C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1 10.1021/jm500995y
118712534 113484 0 ACM5 M5 receptor Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 520 6 1 4 4.6 O=C(C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1)N(Cc1ccccc1C(F)(F)F)C1CCC1 10.1021/jm500995y
CHEMBL3329760 113484 0 ACM5 M5 receptor Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 520 6 1 4 4.6 O=C(C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1)N(Cc1ccccc1C(F)(F)F)C1CCC1 10.1021/jm500995y
44158221 171268 0 ACM5 M5 receptor Human 5.7 pEC50 = 5.7 Functional
Activation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 389 3 0 3 4.3 O=C1C(=O)N(Cc2ccc(C(F)(F)F)cc2)c2ccc(OC(F)(F)F)cc21 10.1021/jm900286j
CHEMBL447265 171268 0 ACM5 M5 receptor Human 5.7 pEC50 = 5.7 Functional
Activation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 389 3 0 3 4.3 O=C1C(=O)N(Cc2ccc(C(F)(F)F)cc2)c2ccc(OC(F)(F)F)cc21 10.1021/jm900286j
44157243 184817 0 ACM5 M5 receptor Human 5.7 pEC50 = 5.7 Functional
Activation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 405 4 0 4 4.2 O=C1C(=O)N(Cc2ccc(OC(F)(F)F)cc2)c2ccc(OC(F)(F)F)cc21 10.1021/jm900286j
CHEMBL494190 184817 0 ACM5 M5 receptor Human 5.7 pEC50 = 5.7 Functional
Activation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 405 4 0 4 4.2 O=C1C(=O)N(Cc2ccc(OC(F)(F)F)cc2)c2ccc(OC(F)(F)F)cc21 10.1021/jm900286j
187 245 23 ACM5 M5 receptor Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2015.08.011
294 245 23 ACM5 M5 receptor Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2015.08.011
65 245 23 ACM5 M5 receptor Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2015.08.011
8593 245 23 ACM5 M5 receptor Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2015.08.011
CHEMBL667 245 23 ACM5 M5 receptor Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2015.08.011
DB03128 245 23 ACM5 M5 receptor Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2015.08.011
CHEMBL1223803 15718 0 ACM5 M5 receptor Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 384 5 0 3 4.5 CCCO[C@H]1CC[C@](C)(N2CCC(N3C(=O)Cc4ccc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223804 15719 0 ACM5 M5 receptor Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 370 4 0 3 4.1 CCO[C@H]1CC[C@](C)(N2CCC(N3C(=O)Cc4ccc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
71737672 2419 4 ACM5 M5 receptor Human 6.7 pEC50 = 6.7 Binding
Positive allosteric modulation of M5 AchR (unknown origin) assessed as increase in acetylcholine-induced responsePositive allosteric modulation of M5 AchR (unknown origin) assessed as increase in acetylcholine-induced response
ChEMBL 494 6 1 4 4.0 CCN(C(=O)C1CCN(CC1)S(=O)(=O)c1ccc2c(c1)cn[nH]2)Cc1ccccc1C(F)(F)F 10.1021/acs.jmedchem.8b00875
8687 2419 4 ACM5 M5 receptor Human 6.7 pEC50 = 6.7 Binding
Positive allosteric modulation of M5 AchR (unknown origin) assessed as increase in acetylcholine-induced responsePositive allosteric modulation of M5 AchR (unknown origin) assessed as increase in acetylcholine-induced response
ChEMBL 494 6 1 4 4.0 CCN(C(=O)C1CCN(CC1)S(=O)(=O)c1ccc2c(c1)cn[nH]2)Cc1ccccc1C(F)(F)F 10.1021/acs.jmedchem.8b00875
CHEMBL3329755 2419 4 ACM5 M5 receptor Human 6.7 pEC50 = 6.7 Binding
Positive allosteric modulation of M5 AchR (unknown origin) assessed as increase in acetylcholine-induced responsePositive allosteric modulation of M5 AchR (unknown origin) assessed as increase in acetylcholine-induced response
ChEMBL 494 6 1 4 4.0 CCN(C(=O)C1CCN(CC1)S(=O)(=O)c1ccc2c(c1)cn[nH]2)Cc1ccccc1C(F)(F)F 10.1021/acs.jmedchem.8b00875
71737672 2419 4 ACM5 M5 receptor Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 494 6 1 4 4.0 CCN(C(=O)C1CCN(CC1)S(=O)(=O)c1ccc2c(c1)cn[nH]2)Cc1ccccc1C(F)(F)F 10.1021/jm500995y
8687 2419 4 ACM5 M5 receptor Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 494 6 1 4 4.0 CCN(C(=O)C1CCN(CC1)S(=O)(=O)c1ccc2c(c1)cn[nH]2)Cc1ccccc1C(F)(F)F 10.1021/jm500995y
CHEMBL3329755 2419 4 ACM5 M5 receptor Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 494 6 1 4 4.0 CCN(C(=O)C1CCN(CC1)S(=O)(=O)c1ccc2c(c1)cn[nH]2)Cc1ccccc1C(F)(F)F 10.1021/jm500995y
44602489 194952 0 ACM5 M5 receptor Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilizationAgonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilization
ChEMBL 413 5 0 4 5.1 O=C1C(=O)N(Cc2ccc(Oc3ccccc3)cc2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2009.11.089
CHEMBL604482 194952 0 ACM5 M5 receptor Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilizationAgonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilization
ChEMBL 413 5 0 4 5.1 O=C1C(=O)N(Cc2ccc(Oc3ccccc3)cc2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2009.11.089
44602489 194952 0 ACM5 M5 receptor Human 5.7 pEC50 = 5.7 Binding
Positive allosteric modulation activity at muscarinic M5 receptorPositive allosteric modulation activity at muscarinic M5 receptor
ChEMBL 413 5 0 4 5.1 O=C1C(=O)N(Cc2ccc(Oc3ccccc3)cc2)c2ccc(OC(F)(F)F)cc21 10.1021/jm201139r
CHEMBL604482 194952 0 ACM5 M5 receptor Human 5.7 pEC50 = 5.7 Binding
Positive allosteric modulation activity at muscarinic M5 receptorPositive allosteric modulation activity at muscarinic M5 receptor
ChEMBL 413 5 0 4 5.1 O=C1C(=O)N(Cc2ccc(Oc3ccccc3)cc2)c2ccc(OC(F)(F)F)cc21 10.1021/jm201139r
44602489 194952 0 ACM5 M5 receptor Human 5.7 pEC50 = 5.7 Binding
Positive allosteric modulation of human muscarinic M5 receptorPositive allosteric modulation of human muscarinic M5 receptor
ChEMBL 413 5 0 4 5.1 O=C1C(=O)N(Cc2ccc(Oc3ccccc3)cc2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2013.03.032
CHEMBL604482 194952 0 ACM5 M5 receptor Human 5.7 pEC50 = 5.7 Binding
Positive allosteric modulation of human muscarinic M5 receptorPositive allosteric modulation of human muscarinic M5 receptor
ChEMBL 413 5 0 4 5.1 O=C1C(=O)N(Cc2ccc(Oc3ccccc3)cc2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2013.03.032
44157160 177921 2 ACM5 M5 receptor Human 5.7 pEC50 = 5.7 Functional
Activation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 333 2 0 2 3.3 O=C1C(=O)N(Cc2ccc(Br)cc2)c2c(F)cccc21 10.1021/jm900286j
CHEMBL468925 177921 2 ACM5 M5 receptor Human 5.7 pEC50 = 5.7 Functional
Activation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 333 2 0 2 3.3 O=C1C(=O)N(Cc2ccc(Br)cc2)c2c(F)cccc21 10.1021/jm900286j
71737672 2419 4 ACM5 M5 receptor Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 494 6 1 4 4.0 CCN(C(=O)C1CCN(CC1)S(=O)(=O)c1ccc2c(c1)cn[nH]2)Cc1ccccc1C(F)(F)F 10.1021/jm500995y
8687 2419 4 ACM5 M5 receptor Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 494 6 1 4 4.0 CCN(C(=O)C1CCN(CC1)S(=O)(=O)c1ccc2c(c1)cn[nH]2)Cc1ccccc1C(F)(F)F 10.1021/jm500995y
CHEMBL3329755 2419 4 ACM5 M5 receptor Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 494 6 1 4 4.0 CCN(C(=O)C1CCN(CC1)S(=O)(=O)c1ccc2c(c1)cn[nH]2)Cc1ccccc1C(F)(F)F 10.1021/jm500995y
44158142 185836 28 ACM5 M5 receptor Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilizationAgonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilization
ChEMBL 339 2 0 2 4.1 O=C1C(=O)N(Cc2ccc(C(F)(F)F)cc2)c2c(Cl)cccc21 10.1016/j.bmcl.2009.11.089
CHEMBL503735 185836 28 ACM5 M5 receptor Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilizationAgonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilization
ChEMBL 339 2 0 2 4.1 O=C1C(=O)N(Cc2ccc(C(F)(F)F)cc2)c2c(Cl)cccc21 10.1016/j.bmcl.2009.11.089
10442337 197521 2 ACM5 M5 receptor Human 5.7 pEC50 = 5.7 Binding
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M5 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M5 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 182 2 1 4 1.1 CCOc1noc2c1CNCCC2 10.1021/jm00012a019
CHEMBL69305 197521 2 ACM5 M5 receptor Human 5.7 pEC50 = 5.7 Binding
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M5 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M5 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 182 2 1 4 1.1 CCOc1noc2c1CNCCC2 10.1021/jm00012a019
52947457 17030 0 ACM5 M5 receptor Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assayPositive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 399 4 0 5 3.8 O=C1C(=O)N(Cc2ccc(-c3cncnc3)cc2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2010.08.042
CHEMBL1257498 17030 0 ACM5 M5 receptor Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assayPositive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 399 4 0 5 3.8 O=C1C(=O)N(Cc2ccc(-c3cncnc3)cc2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2010.08.042
71737647 113472 0 ACM5 M5 receptor Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 444 6 1 4 3.2 CCN(Cc1ccccc1F)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1 10.1021/jm500995y
CHEMBL3329744 113472 0 ACM5 M5 receptor Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 444 6 1 4 3.2 CCN(Cc1ccccc1F)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1 10.1021/jm500995y
44158142 185836 28 ACM5 M5 receptor Human 5.7 pEC50 = 5.7 Functional
Activation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 339 2 0 2 4.1 O=C1C(=O)N(Cc2ccc(C(F)(F)F)cc2)c2c(Cl)cccc21 10.1021/jm900286j
CHEMBL503735 185836 28 ACM5 M5 receptor Human 5.7 pEC50 = 5.7 Functional
Activation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 339 2 0 2 4.1 O=C1C(=O)N(Cc2ccc(C(F)(F)F)cc2)c2c(Cl)cccc21 10.1021/jm900286j
71737647 113472 0 ACM5 M5 receptor Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 444 6 1 4 3.2 CCN(Cc1ccccc1F)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1 10.1021/jm500995y
CHEMBL3329744 113472 0 ACM5 M5 receptor Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 444 6 1 4 3.2 CCN(Cc1ccccc1F)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1 10.1021/jm500995y
57525851 89399 0 ACM5 M5 receptor Human 5.7 pEC50 = 5.7 Binding
Positive allosteric modulation of human muscarinic M5 receptorPositive allosteric modulation of human muscarinic M5 receptor
ChEMBL 448 5 1 5 3.9 COc1ccc(CN2C(=O)C(O)(c3ccc(F)nc3)c3cc(OC(F)(F)F)ccc32)cc1 10.1016/j.bmcl.2013.03.032
CHEMBL2381693 89399 0 ACM5 M5 receptor Human 5.7 pEC50 = 5.7 Binding
Positive allosteric modulation of human muscarinic M5 receptorPositive allosteric modulation of human muscarinic M5 receptor
ChEMBL 448 5 1 5 3.9 COc1ccc(CN2C(=O)C(O)(c3ccc(F)nc3)c3cc(OC(F)(F)F)ccc32)cc1 10.1016/j.bmcl.2013.03.032
46945864 17207 0 ACM5 M5 receptor Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assayPositive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 444 6 0 6 4.5 COc1cccc(Oc2ccc(CN3C(=O)C(=O)c4cc(OC(F)(F)F)ccc43)cc2)n1 10.1016/j.bmcl.2010.08.042
CHEMBL1258090 17207 0 ACM5 M5 receptor Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assayPositive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 444 6 0 6 4.5 COc1cccc(Oc2ccc(CN3C(=O)C(=O)c4cc(OC(F)(F)F)ccc43)cc2)n1 10.1016/j.bmcl.2010.08.042
303 2797 10 ACM5 M5 receptor Human 5.6 pEC50 = 5.6 Binding
Activation of M5-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M5-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
ChEMBL 195 2 0 1 0.3 O=C1CCCN1CC#CC[N+](C)(C)C 10.1016/j.bmc.2010.07.060
4629 2797 10 ACM5 M5 receptor Human 5.6 pEC50 = 5.6 Binding
Activation of M5-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M5-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
ChEMBL 195 2 0 1 0.3 O=C1CCCN1CC#CC[N+](C)(C)C 10.1016/j.bmc.2010.07.060
8595 2797 10 ACM5 M5 receptor Human 5.6 pEC50 = 5.6 Binding
Activation of M5-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M5-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
ChEMBL 195 2 0 1 0.3 O=C1CCCN1CC#CC[N+](C)(C)C 10.1016/j.bmc.2010.07.060
CHEMBL44674 2797 10 ACM5 M5 receptor Human 5.6 pEC50 = 5.6 Binding
Activation of M5-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M5-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
ChEMBL 195 2 0 1 0.3 O=C1CCCN1CC#CC[N+](C)(C)C 10.1016/j.bmc.2010.07.060
71737606 113460 0 ACM5 M5 receptor Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 426 6 0 4 3.9 CCN(Cc1ccccc1)C(=O)C1CCN(S(=O)(=O)c2ccc3occc3c2)CC1 10.1021/jm500995y
CHEMBL3329729 113460 0 ACM5 M5 receptor Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 426 6 0 4 3.9 CCN(Cc1ccccc1)C(=O)C1CCN(S(=O)(=O)c2ccc3occc3c2)CC1 10.1021/jm500995y
52950176 17031 0 ACM5 M5 receptor Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assayPositive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 356 3 0 4 3.4 O=C1C(=O)N(Cc2ccc(Cl)nc2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2010.08.042
CHEMBL1257499 17031 0 ACM5 M5 receptor Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assayPositive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 356 3 0 4 3.4 O=C1C(=O)N(Cc2ccc(Cl)nc2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2010.08.042
71737606 113460 0 ACM5 M5 receptor Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 426 6 0 4 3.9 CCN(Cc1ccccc1)C(=O)C1CCN(S(=O)(=O)c2ccc3occc3c2)CC1 10.1021/jm500995y
CHEMBL3329729 113460 0 ACM5 M5 receptor Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 426 6 0 4 3.9 CCN(Cc1ccccc1)C(=O)C1CCN(S(=O)(=O)c2ccc3occc3c2)CC1 10.1021/jm500995y
25010776 55445 1 ACM5 M5 receptor Human 4.6 pEC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M5. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M5. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]
ChEMBL 333 6 2 4 1.9 CCOC(=O)N1CCC(NCCNC(=O)c2ccccc2C)CC1 nan
CHEMBL1559151 55445 1 ACM5 M5 receptor Human 4.6 pEC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M5. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M5. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]
ChEMBL 333 6 2 4 1.9 CCOC(=O)N1CCC(NCCNC(=O)c2ccccc2C)CC1 nan
CHEMBL1624037 55445 1 ACM5 M5 receptor Human 4.6 pEC50 = 4.6 Functional
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M5. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M5. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]
ChEMBL 333 6 2 4 1.9 CCOC(=O)N1CCC(NCCNC(=O)c2ccccc2C)CC1 nan
3652 3848 63 ACM5 M5 receptor Human 5.6 pEC50 = 5.6 Binding
Effective concentration was evaluated against Muscarinic acetylcholine receptor M5 expressed in A9 L cellsEffective concentration was evaluated against Muscarinic acetylcholine receptor M5 expressed in A9 L cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0301235
57 3848 63 ACM5 M5 receptor Human 5.6 pEC50 = 5.6 Binding
Effective concentration was evaluated against Muscarinic acetylcholine receptor M5 expressed in A9 L cellsEffective concentration was evaluated against Muscarinic acetylcholine receptor M5 expressed in A9 L cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0301235
60809 3848 63 ACM5 M5 receptor Human 5.6 pEC50 = 5.6 Binding
Effective concentration was evaluated against Muscarinic acetylcholine receptor M5 expressed in A9 L cellsEffective concentration was evaluated against Muscarinic acetylcholine receptor M5 expressed in A9 L cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0301235
CHEMBL21536 3848 63 ACM5 M5 receptor Human 5.6 pEC50 = 5.6 Binding
Effective concentration was evaluated against Muscarinic acetylcholine receptor M5 expressed in A9 L cellsEffective concentration was evaluated against Muscarinic acetylcholine receptor M5 expressed in A9 L cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0301235
DB15357 3848 63 ACM5 M5 receptor Human 5.6 pEC50 = 5.6 Binding
Effective concentration was evaluated against Muscarinic acetylcholine receptor M5 expressed in A9 L cellsEffective concentration was evaluated against Muscarinic acetylcholine receptor M5 expressed in A9 L cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0301235
1424 89 27 ACM5 M5 receptor Human 5.6 pEC50 = 5.6 Binding
Positive allosteric modulator activity at human muscarinic acetylcholine receptor M5 expressed in CHO cells by fluorometric imaging plate readerPositive allosteric modulator activity at human muscarinic acetylcholine receptor M5 expressed in CHO cells by fluorometric imaging plate reader
ChEMBL 244 3 0 2 3.4 Fc1cccc(c1)/C=N/N=C/c1cccc(c1)F 10.1021/jm5011786
6604893 89 27 ACM5 M5 receptor Human 5.6 pEC50 = 5.6 Binding
Positive allosteric modulator activity at human muscarinic acetylcholine receptor M5 expressed in CHO cells by fluorometric imaging plate readerPositive allosteric modulator activity at human muscarinic acetylcholine receptor M5 expressed in CHO cells by fluorometric imaging plate reader
ChEMBL 244 3 0 2 3.4 Fc1cccc(c1)/C=N/N=C/c1cccc(c1)F 10.1021/jm5011786
CHEMBL371811 89 27 ACM5 M5 receptor Human 5.6 pEC50 = 5.6 Binding
Positive allosteric modulator activity at human muscarinic acetylcholine receptor M5 expressed in CHO cells by fluorometric imaging plate readerPositive allosteric modulator activity at human muscarinic acetylcholine receptor M5 expressed in CHO cells by fluorometric imaging plate reader
ChEMBL 244 3 0 2 3.4 Fc1cccc(c1)/C=N/N=C/c1cccc(c1)F 10.1021/jm5011786
71737645 113474 0 ACM5 M5 receptor Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 456 7 1 5 3.0 CCN(Cc1cccc(OC)c1)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1 10.1021/jm500995y
CHEMBL3329746 113474 0 ACM5 M5 receptor Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 456 7 1 5 3.0 CCN(Cc1cccc(OC)c1)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1 10.1021/jm500995y
71737645 113474 0 ACM5 M5 receptor Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 456 7 1 5 3.0 CCN(Cc1cccc(OC)c1)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1 10.1021/jm500995y
CHEMBL3329746 113474 0 ACM5 M5 receptor Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 456 7 1 5 3.0 CCN(Cc1cccc(OC)c1)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1 10.1021/jm500995y
45281794 193318 37 ACM5 M5 receptor Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilizationAgonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilization
ChEMBL 397 4 0 3 5.0 O=C1C(=O)N(Cc2ccc(-c3ccccc3)cc2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2009.11.089
CHEMBL593506 193318 37 ACM5 M5 receptor Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilizationAgonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilization
ChEMBL 397 4 0 3 5.0 O=C1C(=O)N(Cc2ccc(-c3ccccc3)cc2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2009.11.089
45281808 193638 0 ACM5 M5 receptor Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilizationAgonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilization
ChEMBL 397 4 0 3 5.0 O=C1C(=O)N(Cc2ccc(-c3ccccc3)cc2)c2cc(OC(F)(F)F)ccc21 10.1016/j.bmcl.2009.11.089
CHEMBL595628 193638 0 ACM5 M5 receptor Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilizationAgonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilization
ChEMBL 397 4 0 3 5.0 O=C1C(=O)N(Cc2ccc(-c3ccccc3)cc2)c2cc(OC(F)(F)F)ccc21 10.1016/j.bmcl.2009.11.089
2551 750 19 ACM5 M5 receptor Human 5.6 pEC50 = 5.6 Binding
Activation of M5-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M5-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmc.2010.07.060
298 750 19 ACM5 M5 receptor Human 5.6 pEC50 = 5.6 Binding
Activation of M5-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M5-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmc.2010.07.060
488 750 19 ACM5 M5 receptor Human 5.6 pEC50 = 5.6 Binding
Activation of M5-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M5-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmc.2010.07.060
CHEMBL965 750 19 ACM5 M5 receptor Human 5.6 pEC50 = 5.6 Binding
Activation of M5-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M5-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmc.2010.07.060
DB00411 750 19 ACM5 M5 receptor Human 5.6 pEC50 = 5.6 Binding
Activation of M5-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M5-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/j.bmc.2010.07.060
45281797 194768 0 ACM5 M5 receptor Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilizationAgonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilization
ChEMBL 403 4 0 4 5.0 O=C1C(=O)N(Cc2ccc(-c3ccsc3)cc2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2009.11.089
CHEMBL603445 194768 0 ACM5 M5 receptor Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilizationAgonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilization
ChEMBL 403 4 0 4 5.0 O=C1C(=O)N(Cc2ccc(-c3ccsc3)cc2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2009.11.089
CHEMBL3084447 102551 0 ACM5 M5 receptor Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human muscarinic M5 receptor by calcium mobilization assayAgonist activity at human muscarinic M5 receptor by calcium mobilization assay
ChEMBL 345 6 2 4 1.9 CCOC(=O)N1C[C@@H]2CC[C@H](C1)[C@@H]2NCCNC(=O)c1ccccc1 10.1016/j.bmcl.2012.03.088
52949833 16991 0 ACM5 M5 receptor Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assayPositive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 398 4 0 4 4.4 O=C1C(=O)N(Cc2ccc(-c3ccncc3)cc2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2010.08.042
CHEMBL1257389 16991 0 ACM5 M5 receptor Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assayPositive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 398 4 0 4 4.4 O=C1C(=O)N(Cc2ccc(-c3ccncc3)cc2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2010.08.042
46945865 17208 0 ACM5 M5 receptor Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assayPositive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 420 5 0 6 4.6 O=C1C(=O)N(Cc2ccc(Oc3nccs3)cc2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2010.08.042
CHEMBL1258091 17208 0 ACM5 M5 receptor Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assayPositive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 420 5 0 6 4.6 O=C1C(=O)N(Cc2ccc(Oc3nccs3)cc2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2010.08.042
71771054 113463 0 ACM5 M5 receptor Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 444 6 0 6 3.1 CCN(Cc1ccccc1)C(=O)C1CCN(S(=O)(=O)c2ccc3nsnc3c2)CC1 10.1021/jm500995y
CHEMBL3329732 113463 0 ACM5 M5 receptor Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 444 6 0 6 3.1 CCN(Cc1ccccc1)C(=O)C1CCN(S(=O)(=O)c2ccc3nsnc3c2)CC1 10.1021/jm500995y
6891506 113752 19 ACM5 M5 receptor Human 5.5 pEC50 = 5.5 Binding
Negative allosteric modulator activity at human muscarinic acetylcholine receptor M5 expressed in CHO cells by fluorometric imaging plate readerNegative allosteric modulator activity at human muscarinic acetylcholine receptor M5 expressed in CHO cells by fluorometric imaging plate reader
ChEMBL 268 5 0 4 3.2 COc1cccc(/C=N/N=C/c2cccc(OC)c2)c1 10.1021/jm5011786
CHEMBL3334989 113752 19 ACM5 M5 receptor Human 5.5 pEC50 = 5.5 Binding
Negative allosteric modulator activity at human muscarinic acetylcholine receptor M5 expressed in CHO cells by fluorometric imaging plate readerNegative allosteric modulator activity at human muscarinic acetylcholine receptor M5 expressed in CHO cells by fluorometric imaging plate reader
ChEMBL 268 5 0 4 3.2 COc1cccc(/C=N/N=C/c2cccc(OC)c2)c1 10.1021/jm5011786
71771054 113463 0 ACM5 M5 receptor Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 444 6 0 6 3.1 CCN(Cc1ccccc1)C(=O)C1CCN(S(=O)(=O)c2ccc3nsnc3c2)CC1 10.1021/jm500995y
CHEMBL3329732 113463 0 ACM5 M5 receptor Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 444 6 0 6 3.1 CCN(Cc1ccccc1)C(=O)C1CCN(S(=O)(=O)c2ccc3nsnc3c2)CC1 10.1021/jm500995y
71737574 113459 0 ACM5 M5 receptor Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 416 7 0 4 3.1 CCN(Cc1ccccc1)C(=O)C1CCN(S(=O)(=O)c2cccc(OC)c2)CC1 10.1021/jm500995y
CHEMBL3329717 113459 0 ACM5 M5 receptor Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 416 7 0 4 3.1 CCN(Cc1ccccc1)C(=O)C1CCN(S(=O)(=O)c2cccc(OC)c2)CC1 10.1021/jm500995y
52941424 17071 0 ACM5 M5 receptor Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assayPositive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 398 4 0 4 4.4 O=C1C(=O)N(Cc2ccc(-c3ccccc3)cn2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2010.08.042
CHEMBL1257619 17071 0 ACM5 M5 receptor Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assayPositive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 398 4 0 4 4.4 O=C1C(=O)N(Cc2ccc(-c3ccccc3)cn2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2010.08.042
71737574 113459 0 ACM5 M5 receptor Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 416 7 0 4 3.1 CCN(Cc1ccccc1)C(=O)C1CCN(S(=O)(=O)c2cccc(OC)c2)CC1 10.1021/jm500995y
CHEMBL3329717 113459 0 ACM5 M5 receptor Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 416 7 0 4 3.1 CCN(Cc1ccccc1)C(=O)C1CCN(S(=O)(=O)c2cccc(OC)c2)CC1 10.1021/jm500995y
CHEMBL1223939 15765 0 ACM5 M5 receptor Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 450 6 0 7 3.8 CCCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(S(C)(=O)=O)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
10946670 186335 2 ACM5 M5 receptor Human 5.5 pEC50 = 5.5 Functional
Activation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 305 2 0 2 3.4 O=C1C(=O)N(Cc2ccc(C(F)(F)F)cc2)c2ccccc21 10.1021/jm900286j
CHEMBL511206 186335 2 ACM5 M5 receptor Human 5.5 pEC50 = 5.5 Functional
Activation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 305 2 0 2 3.4 O=C1C(=O)N(Cc2ccc(C(F)(F)F)cc2)c2ccccc21 10.1021/jm900286j
52943684 16925 0 ACM5 M5 receptor Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assayPositive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 365 3 0 5 3.0 O=C1C(=O)N(Cc2ccc3c(c2)OCO3)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2010.08.042
CHEMBL1257151 16925 0 ACM5 M5 receptor Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assayPositive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 365 3 0 5 3.0 O=C1C(=O)N(Cc2ccc3c(c2)OCO3)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2010.08.042
46945664 17173 0 ACM5 M5 receptor Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assayPositive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 414 5 0 5 4.5 O=C1C(=O)N(Cc2ccc(Oc3ccccn3)cc2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2010.08.042
CHEMBL1257974 17173 0 ACM5 M5 receptor Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assayPositive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 414 5 0 5 4.5 O=C1C(=O)N(Cc2ccc(Oc3ccccn3)cc2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2010.08.042
44158139 177845 0 ACM5 M5 receptor Human 5.5 pEC50 = 5.5 Functional
Activation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 323 2 0 2 3.6 O=C1C(=O)N(Cc2ccc(C(F)(F)F)cc2)c2c(F)cccc21 10.1021/jm900286j
CHEMBL468290 177845 0 ACM5 M5 receptor Human 5.5 pEC50 = 5.5 Functional
Activation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 323 2 0 2 3.6 O=C1C(=O)N(Cc2ccc(C(F)(F)F)cc2)c2c(F)cccc21 10.1021/jm900286j
44158003 185971 0 ACM5 M5 receptor Human 5.5 pEC50 = 5.5 Functional
Activation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 335 3 0 3 3.6 Cc1ccccc1CN1C(=O)C(=O)c2cc(OC(F)(F)F)ccc21 10.1021/jm900286j
CHEMBL506043 185971 0 ACM5 M5 receptor Human 5.5 pEC50 = 5.5 Functional
Activation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 335 3 0 3 3.6 Cc1ccccc1CN1C(=O)C(=O)c2cc(OC(F)(F)F)ccc21 10.1021/jm900286j
CHEMBL3334991 113754 0 ACM5 M5 receptor Human 7.5 pEC50 = 7.5 Binding
Positive allosteric modulator activity at human muscarinic acetylcholine receptor M5 expressed in CHO cells by fluorometric imaging plate readerPositive allosteric modulator activity at human muscarinic acetylcholine receptor M5 expressed in CHO cells by fluorometric imaging plate reader
ChEMBL 310 2 2 3 1.9 O=C(N[C@H]1C[C@@H](O)C1)c1ccc(C#Cc2cccc(F)c2)cn1 10.1021/jm5011786
45281803 193755 0 ACM5 M5 receptor Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilizationAgonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilization
ChEMBL 401 4 0 5 3.7 Cn1cc(-c2ccc(CN3C(=O)C(=O)c4cc(OC(F)(F)F)ccc43)cc2)cn1 10.1016/j.bmcl.2009.11.089
CHEMBL596510 193755 0 ACM5 M5 receptor Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilizationAgonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilization
ChEMBL 401 4 0 5 3.7 Cn1cc(-c2ccc(CN3C(=O)C(=O)c4cc(OC(F)(F)F)ccc43)cc2)cn1 10.1016/j.bmcl.2009.11.089
26415265 113458 1 ACM5 M5 receptor Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 416 7 0 4 3.1 CCN(Cc1ccccc1)C(=O)C1CCN(S(=O)(=O)c2ccc(OC)cc2)CC1 10.1021/jm500995y
CHEMBL3329716 113458 1 ACM5 M5 receptor Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 416 7 0 4 3.1 CCN(Cc1ccccc1)C(=O)C1CCN(S(=O)(=O)c2ccc(OC)cc2)CC1 10.1021/jm500995y
26415265 113458 1 ACM5 M5 receptor Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 416 7 0 4 3.1 CCN(Cc1ccccc1)C(=O)C1CCN(S(=O)(=O)c2ccc(OC)cc2)CC1 10.1021/jm500995y
CHEMBL3329716 113458 1 ACM5 M5 receptor Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 416 7 0 4 3.1 CCN(Cc1ccccc1)C(=O)C1CCN(S(=O)(=O)c2ccc(OC)cc2)CC1 10.1021/jm500995y
44589681 183695 0 ACM5 M5 receptor Human 7.5 pEC50 = 7.5 Functional
Agonist activity at muscarinic M5 receptorAgonist activity at muscarinic M5 receptor
ChEMBL 387 5 2 6 1.5 NC(=O)OCCN1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1 10.1016/j.bmcl.2008.09.032
CHEMBL485913 183695 0 ACM5 M5 receptor Human 7.5 pEC50 = 7.5 Functional
Agonist activity at muscarinic M5 receptorAgonist activity at muscarinic M5 receptor
ChEMBL 387 5 2 6 1.5 NC(=O)OCCN1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1 10.1016/j.bmcl.2008.09.032
22745278 184386 1 ACM5 M5 receptor Human 7.5 pEC50 = 7.5 Functional
Agonist activity at muscarinic M5 receptorAgonist activity at muscarinic M5 receptor
ChEMBL 372 3 1 5 2.6 CCOC(=O)N1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1 10.1016/j.bmcl.2008.09.023
CHEMBL491209 184386 1 ACM5 M5 receptor Human 7.5 pEC50 = 7.5 Functional
Agonist activity at muscarinic M5 receptorAgonist activity at muscarinic M5 receptor
ChEMBL 372 3 1 5 2.6 CCOC(=O)N1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1 10.1016/j.bmcl.2008.09.023
71737709 113481 0 ACM5 M5 receptor Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 460 6 1 4 3.7 CCN(Cc1ccccc1Cl)C(=O)C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1 10.1021/jm500995y
CHEMBL3329754 113481 0 ACM5 M5 receptor Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 460 6 1 4 3.7 CCN(Cc1ccccc1Cl)C(=O)C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1 10.1021/jm500995y
71737709 113481 0 ACM5 M5 receptor Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 460 6 1 4 3.7 CCN(Cc1ccccc1Cl)C(=O)C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1 10.1021/jm500995y
CHEMBL3329754 113481 0 ACM5 M5 receptor Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 460 6 1 4 3.7 CCN(Cc1ccccc1Cl)C(=O)C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1 10.1021/jm500995y
2551 750 19 ACM5 M5 receptor Human 6.4 pEC50 = 6.4 Binding
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M5 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M5 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm00012a019
298 750 19 ACM5 M5 receptor Human 6.4 pEC50 = 6.4 Binding
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M5 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M5 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm00012a019
488 750 19 ACM5 M5 receptor Human 6.4 pEC50 = 6.4 Binding
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M5 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M5 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm00012a019
CHEMBL965 750 19 ACM5 M5 receptor Human 6.4 pEC50 = 6.4 Binding
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M5 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M5 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm00012a019
DB00411 750 19 ACM5 M5 receptor Human 6.4 pEC50 = 6.4 Binding
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M5 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M5 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm00012a019
45281801 193754 0 ACM5 M5 receptor Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilizationAgonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilization
ChEMBL 416 4 0 4 4.5 O=C1C(=O)N(Cc2ccc(-c3ccc(F)nc3)cc2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2009.11.089
CHEMBL596509 193754 0 ACM5 M5 receptor Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilizationAgonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilization
ChEMBL 416 4 0 4 4.5 O=C1C(=O)N(Cc2ccc(-c3ccc(F)nc3)cc2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2009.11.089
53385782 73729 0 ACM5 M5 receptor Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human muscarinic M5 receptor by calcium mobilization assayAgonist activity at human muscarinic M5 receptor by calcium mobilization assay
ChEMBL 399 4 1 4 3.3 CCOC(=O)N1C2CCC1CC(N1CCC[C@@H](NC(=O)c3ccccc3C)C1)C2 10.1016/j.bmcl.2012.03.088
CHEMBL2024331 73729 0 ACM5 M5 receptor Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human muscarinic M5 receptor by calcium mobilization assayAgonist activity at human muscarinic M5 receptor by calcium mobilization assay
ChEMBL 399 4 1 4 3.3 CCOC(=O)N1C2CCC1CC(N1CCC[C@@H](NC(=O)c3ccccc3C)C1)C2 10.1016/j.bmcl.2012.03.088
46945662 17109 0 ACM5 M5 receptor Human 5.4 pEC50 = 5.4 Functional
Positive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assayPositive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 398 4 0 4 4.4 O=C1C(=O)N(Cc2ccc(-c3ccccc3)nc2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2010.08.042
CHEMBL1257741 17109 0 ACM5 M5 receptor Human 5.4 pEC50 = 5.4 Functional
Positive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assayPositive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 398 4 0 4 4.4 O=C1C(=O)N(Cc2ccc(-c3ccccc3)nc2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2010.08.042
45281796 193599 0 ACM5 M5 receptor Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilizationAgonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilization
ChEMBL 427 5 0 4 5.0 COc1ccccc1-c1ccc(CN2C(=O)C(=O)c3cc(OC(F)(F)F)ccc32)cc1 10.1016/j.bmcl.2009.11.089
CHEMBL595403 193599 0 ACM5 M5 receptor Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilizationAgonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilization
ChEMBL 427 5 0 4 5.0 COc1ccccc1-c1ccc(CN2C(=O)C(=O)c3cc(OC(F)(F)F)ccc32)cc1 10.1016/j.bmcl.2009.11.089
44157241 186346 2 ACM5 M5 receptor Human 5.4 pEC50 = 5.4 Functional
Activation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 301 3 0 3 3.1 COc1ccc(CN2C(=O)C(=O)c3cccc(Cl)c32)cc1 10.1021/jm900286j
CHEMBL511254 186346 2 ACM5 M5 receptor Human 5.4 pEC50 = 5.4 Functional
Activation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 301 3 0 3 3.1 COc1ccc(CN2C(=O)C(=O)c3cccc(Cl)c32)cc1 10.1021/jm900286j
CHEMBL1223806 15721 0 ACM5 M5 receptor Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 358 3 0 5 3.9 CO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223863 15746 0 ACM5 M5 receptor Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 383 4 0 6 3.8 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(C#N)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
3257 3781 49 ACM5 M5 receptor Rat 8.3 pEC50 = 8.3 Binding
Positive allosteric modulation of rat muscarinic M5 receptorPositive allosteric modulation of rat muscarinic M5 receptor
ChEMBL 351 4 0 4 3.3 COc1ccc(cc1)CN1c2ccc(cc2C(=O)C1=O)OC(F)(F)F 10.1016/j.bmcl.2013.03.032
42633508 3781 49 ACM5 M5 receptor Rat 8.3 pEC50 = 8.3 Binding
Positive allosteric modulation of rat muscarinic M5 receptorPositive allosteric modulation of rat muscarinic M5 receptor
ChEMBL 351 4 0 4 3.3 COc1ccc(cc1)CN1c2ccc(cc2C(=O)C1=O)OC(F)(F)F 10.1016/j.bmcl.2013.03.032
CHEMBL466253 3781 49 ACM5 M5 receptor Rat 8.3 pEC50 = 8.3 Binding
Positive allosteric modulation of rat muscarinic M5 receptorPositive allosteric modulation of rat muscarinic M5 receptor
ChEMBL 351 4 0 4 3.3 COc1ccc(cc1)CN1c2ccc(cc2C(=O)C1=O)OC(F)(F)F 10.1016/j.bmcl.2013.03.032
57525860 89400 0 ACM5 M5 receptor Rat 8.3 pEC50 = 8.3 Binding
Positive allosteric modulation of rat muscarinic M5 receptorPositive allosteric modulation of rat muscarinic M5 receptor
ChEMBL 351 5 0 4 3.2 O=C1C(=O)N(CCOc2ccccc2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2013.03.032
CHEMBL2381694 89400 0 ACM5 M5 receptor Rat 8.3 pEC50 = 8.3 Binding
Positive allosteric modulation of rat muscarinic M5 receptorPositive allosteric modulation of rat muscarinic M5 receptor
ChEMBL 351 5 0 4 3.2 O=C1C(=O)N(CCOc2ccccc2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2013.03.032
3257 3781 49 ACM5 M5 receptor Rat 8.3 pEC50 = 8.3 Binding
Positive allosteric modulation of rat muscarinic M5 receptorPositive allosteric modulation of rat muscarinic M5 receptor
ChEMBL 351 4 0 4 3.3 COc1ccc(cc1)CN1c2ccc(cc2C(=O)C1=O)OC(F)(F)F 10.1016/j.bmcl.2013.03.032
42633508 3781 49 ACM5 M5 receptor Rat 8.3 pEC50 = 8.3 Binding
Positive allosteric modulation of rat muscarinic M5 receptorPositive allosteric modulation of rat muscarinic M5 receptor
ChEMBL 351 4 0 4 3.3 COc1ccc(cc1)CN1c2ccc(cc2C(=O)C1=O)OC(F)(F)F 10.1016/j.bmcl.2013.03.032
CHEMBL466253 3781 49 ACM5 M5 receptor Rat 8.3 pEC50 = 8.3 Binding
Positive allosteric modulation of rat muscarinic M5 receptorPositive allosteric modulation of rat muscarinic M5 receptor
ChEMBL 351 4 0 4 3.3 COc1ccc(cc1)CN1c2ccc(cc2C(=O)C1=O)OC(F)(F)F 10.1016/j.bmcl.2013.03.032
57525860 89400 0 ACM5 M5 receptor Rat 8.3 pEC50 = 8.3 Binding
Positive allosteric modulation of rat muscarinic M5 receptorPositive allosteric modulation of rat muscarinic M5 receptor
ChEMBL 351 5 0 4 3.2 O=C1C(=O)N(CCOc2ccccc2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2013.03.032
CHEMBL2381694 89400 0 ACM5 M5 receptor Rat 8.3 pEC50 = 8.3 Binding
Positive allosteric modulation of rat muscarinic M5 receptorPositive allosteric modulation of rat muscarinic M5 receptor
ChEMBL 351 5 0 4 3.2 O=C1C(=O)N(CCOc2ccccc2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2013.03.032
CHEMBL2431187 91775 0 ACM5 M5 receptor Human 6.4 pEC50 = 6.4 Binding
Allosteric agonist activity at human muscarinic acetylcholine receptor M5Allosteric agonist activity at human muscarinic acetylcholine receptor M5
ChEMBL 310 2 2 3 1.9 O=C(N[C@H]1C[C@H](O)C1)c1ccc(C#Cc2cccc(F)c2)cn1 10.1021/jm5011786
52949292 17144 0 ACM5 M5 receptor Human 5.4 pEC50 = 5.4 Functional
Positive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assayPositive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 399 4 0 5 3.8 O=C1C(=O)N(Cc2ccc(-c3cccnc3)nc2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2010.08.042
CHEMBL1257862 17144 0 ACM5 M5 receptor Human 5.4 pEC50 = 5.4 Functional
Positive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assayPositive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 399 4 0 5 3.8 O=C1C(=O)N(Cc2ccc(-c3cccnc3)nc2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2010.08.042
57525860 89400 0 ACM5 M5 receptor Human 6.4 pEC50 = 6.4 Binding
Positive allosteric modulation of human muscarinic M5 receptorPositive allosteric modulation of human muscarinic M5 receptor
ChEMBL 351 5 0 4 3.2 O=C1C(=O)N(CCOc2ccccc2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2013.03.032
CHEMBL2381694 89400 0 ACM5 M5 receptor Human 6.4 pEC50 = 6.4 Binding
Positive allosteric modulation of human muscarinic M5 receptorPositive allosteric modulation of human muscarinic M5 receptor
ChEMBL 351 5 0 4 3.2 O=C1C(=O)N(CCOc2ccccc2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2013.03.032
44157714 186576 0 ACM5 M5 receptor Human 5.4 pEC50 = 5.4 Functional
Activation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 355 3 0 3 4.0 O=C1C(=O)N(Cc2ccccc2Cl)c2ccc(OC(F)(F)F)cc21 10.1021/jm900286j
CHEMBL513299 186576 0 ACM5 M5 receptor Human 5.4 pEC50 = 5.4 Functional
Activation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 355 3 0 3 4.0 O=C1C(=O)N(Cc2ccccc2Cl)c2ccc(OC(F)(F)F)cc21 10.1021/jm900286j
3008304 3776 40 ACM5 M5 receptor Human 5.4 pEC50 = 5.4 Functional
Activation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 315 2 0 2 3.2 Brc1ccc(cc1)CN1c2ccccc2C(=O)C1=O 10.1021/jm900286j
7632 3776 40 ACM5 M5 receptor Human 5.4 pEC50 = 5.4 Functional
Activation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 315 2 0 2 3.2 Brc1ccc(cc1)CN1c2ccccc2C(=O)C1=O 10.1021/jm900286j
CHEMBL523685 3776 40 ACM5 M5 receptor Human 5.4 pEC50 = 5.4 Functional
Activation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 315 2 0 2 3.2 Brc1ccc(cc1)CN1c2ccccc2C(=O)C1=O 10.1021/jm900286j
44158077 177741 0 ACM5 M5 receptor Human 5.4 pEC50 = 5.4 Functional
Activation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 323 2 0 2 3.6 O=C1C(=O)N(Cc2ccccc2C(F)(F)F)c2ccc(F)cc21 10.1021/jm900286j
CHEMBL467281 177741 0 ACM5 M5 receptor Human 5.4 pEC50 = 5.4 Functional
Activation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 323 2 0 2 3.6 O=C1C(=O)N(Cc2ccccc2C(F)(F)F)c2ccc(F)cc21 10.1021/jm900286j
57525860 89400 0 ACM5 M5 receptor Human 6.4 pEC50 = 6.4 Binding
Positive allosteric modulation of human muscarinic M5 receptorPositive allosteric modulation of human muscarinic M5 receptor
ChEMBL 351 5 0 4 3.2 O=C1C(=O)N(CCOc2ccccc2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2013.03.032
CHEMBL2381694 89400 0 ACM5 M5 receptor Human 6.4 pEC50 = 6.4 Binding
Positive allosteric modulation of human muscarinic M5 receptorPositive allosteric modulation of human muscarinic M5 receptor
ChEMBL 351 5 0 4 3.2 O=C1C(=O)N(CCOc2ccccc2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2013.03.032
3008304 3776 40 ACM5 M5 receptor Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilizationAgonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilization
ChEMBL 315 2 0 2 3.2 Brc1ccc(cc1)CN1c2ccccc2C(=O)C1=O 10.1016/j.bmcl.2009.11.089
7632 3776 40 ACM5 M5 receptor Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilizationAgonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilization
ChEMBL 315 2 0 2 3.2 Brc1ccc(cc1)CN1c2ccccc2C(=O)C1=O 10.1016/j.bmcl.2009.11.089
CHEMBL523685 3776 40 ACM5 M5 receptor Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilizationAgonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilization
ChEMBL 315 2 0 2 3.2 Brc1ccc(cc1)CN1c2ccccc2C(=O)C1=O 10.1016/j.bmcl.2009.11.089
3008304 3776 40 ACM5 M5 receptor Human 5.4 pEC50 = 5.4 Binding
Positive allosteric modulation activity at muscarinic M5 receptorPositive allosteric modulation activity at muscarinic M5 receptor
ChEMBL 315 2 0 2 3.2 Brc1ccc(cc1)CN1c2ccccc2C(=O)C1=O 10.1021/jm201139r
7632 3776 40 ACM5 M5 receptor Human 5.4 pEC50 = 5.4 Binding
Positive allosteric modulation activity at muscarinic M5 receptorPositive allosteric modulation activity at muscarinic M5 receptor
ChEMBL 315 2 0 2 3.2 Brc1ccc(cc1)CN1c2ccccc2C(=O)C1=O 10.1021/jm201139r
CHEMBL523685 3776 40 ACM5 M5 receptor Human 5.4 pEC50 = 5.4 Binding
Positive allosteric modulation activity at muscarinic M5 receptorPositive allosteric modulation activity at muscarinic M5 receptor
ChEMBL 315 2 0 2 3.2 Brc1ccc(cc1)CN1c2ccccc2C(=O)C1=O 10.1021/jm201139r
CHEMBL3084449 102553 0 ACM5 M5 receptor Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human muscarinic M5 receptor by calcium mobilization assayAgonist activity at human muscarinic M5 receptor by calcium mobilization assay
ChEMBL 379 6 2 4 2.5 CCOC(=O)N1C[C@@H]2CC[C@H](C1)[C@@H]2NCCNC(=O)c1cccc(Cl)c1 10.1016/j.bmcl.2012.03.088
71792 77759 25 ACM5 M5 receptor Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 165 2 0 2 0.7 C#CCO[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2015.08.011
CHEMBL2111051 77759 25 ACM5 M5 receptor Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 165 2 0 2 0.7 C#CCO[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2015.08.011
52941977 17145 0 ACM5 M5 receptor Human 5.4 pEC50 = 5.4 Functional
Positive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assayPositive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 399 4 0 5 3.8 O=C1C(=O)N(Cc2ccc(-c3ccncc3)nc2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2010.08.042
CHEMBL1257863 17145 0 ACM5 M5 receptor Human 5.4 pEC50 = 5.4 Functional
Positive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assayPositive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 399 4 0 5 3.8 O=C1C(=O)N(Cc2ccc(-c3ccncc3)nc2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2010.08.042
57525833 89402 0 ACM5 M5 receptor Human 6.4 pEC50 = 6.4 Binding
Positive allosteric modulation of human muscarinic M5 receptorPositive allosteric modulation of human muscarinic M5 receptor
ChEMBL 385 5 0 4 3.8 O=C1C(=O)N(CCOc2ccc(Cl)cc2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2013.03.032
CHEMBL2381696 89402 0 ACM5 M5 receptor Human 6.4 pEC50 = 6.4 Binding
Positive allosteric modulation of human muscarinic M5 receptorPositive allosteric modulation of human muscarinic M5 receptor
ChEMBL 385 5 0 4 3.8 O=C1C(=O)N(CCOc2ccc(Cl)cc2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2013.03.032
57525833 89402 0 ACM5 M5 receptor Human 6.4 pEC50 = 6.4 Binding
Positive allosteric modulation of human muscarinic M5 receptorPositive allosteric modulation of human muscarinic M5 receptor
ChEMBL 385 5 0 4 3.8 O=C1C(=O)N(CCOc2ccc(Cl)cc2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2013.03.032
CHEMBL2381696 89402 0 ACM5 M5 receptor Human 6.4 pEC50 = 6.4 Binding
Positive allosteric modulation of human muscarinic M5 receptorPositive allosteric modulation of human muscarinic M5 receptor
ChEMBL 385 5 0 4 3.8 O=C1C(=O)N(CCOc2ccc(Cl)cc2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2013.03.032
3008304 3776 40 ACM5 M5 receptor Human 5.3 pEC50 = 5.3 Functional
Positive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assayPositive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 315 2 0 2 3.2 Brc1ccc(cc1)CN1c2ccccc2C(=O)C1=O 10.1016/j.bmcl.2010.08.042
7632 3776 40 ACM5 M5 receptor Human 5.3 pEC50 = 5.3 Functional
Positive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assayPositive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 315 2 0 2 3.2 Brc1ccc(cc1)CN1c2ccccc2C(=O)C1=O 10.1016/j.bmcl.2010.08.042
CHEMBL523685 3776 40 ACM5 M5 receptor Human 5.3 pEC50 = 5.3 Functional
Positive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assayPositive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 315 2 0 2 3.2 Brc1ccc(cc1)CN1c2ccccc2C(=O)C1=O 10.1016/j.bmcl.2010.08.042
13248082 184943 4 ACM5 M5 receptor Human 5.3 pEC50 = 5.3 Functional
Activation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 367 2 0 2 4.0 O=C1C(=O)N(Cc2ccc(Br)cc2F)c2c(Cl)cccc21 10.1021/jm900286j
CHEMBL494846 184943 4 ACM5 M5 receptor Human 5.3 pEC50 = 5.3 Functional
Activation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 367 2 0 2 4.0 O=C1C(=O)N(Cc2ccc(Br)cc2F)c2c(Cl)cccc21 10.1021/jm900286j
10442081 101896 8 ACM5 M5 receptor Human 5.3 pEC50 = 5.3 Binding
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M5 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M5 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 168 1 1 4 0.7 COc1noc2c1CNCCC2 10.1021/jm00012a019
CHEMBL304142 101896 8 ACM5 M5 receptor Human 5.3 pEC50 = 5.3 Binding
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M5 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M5 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 168 1 1 4 0.7 COc1noc2c1CNCCC2 10.1021/jm00012a019
644390 39974 6 ACM5 M5 receptor Human 4.3 pEC50 = 4.3 Functional
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M5. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M5. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]
ChEMBL 353 6 2 4 2.3 CCOC(=O)N1CCC(NCCNC(=O)c2ccccc2Cl)CC1 nan
CHEMBL1482157 39974 6 ACM5 M5 receptor Human 4.3 pEC50 = 4.3 Functional
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M5. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M5. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]
ChEMBL 353 6 2 4 2.3 CCOC(=O)N1CCC(NCCNC(=O)c2ccccc2Cl)CC1 nan
71737648 113479 0 ACM5 M5 receptor Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 494 6 1 4 4.0 CCN(Cc1ccccc1C(F)(F)F)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1 10.1021/jm500995y
CHEMBL3329751 113479 0 ACM5 M5 receptor Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 494 6 1 4 4.0 CCN(Cc1ccccc1C(F)(F)F)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1 10.1021/jm500995y
71737648 113479 0 ACM5 M5 receptor Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 494 6 1 4 4.0 CCN(Cc1ccccc1C(F)(F)F)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1 10.1021/jm500995y
CHEMBL3329751 113479 0 ACM5 M5 receptor Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 494 6 1 4 4.0 CCN(Cc1ccccc1C(F)(F)F)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1 10.1021/jm500995y
45281798 193723 0 ACM5 M5 receptor Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilizationAgonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilization
ChEMBL 432 4 0 4 5.0 O=C1C(=O)N(Cc2ccc(-c3ccc(Cl)nc3)cc2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2009.11.089
CHEMBL596289 193723 0 ACM5 M5 receptor Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilizationAgonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilization
ChEMBL 432 4 0 4 5.0 O=C1C(=O)N(Cc2ccc(-c3ccc(Cl)nc3)cc2)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2009.11.089
CHEMBL1223860 15743 0 ACM5 M5 receptor Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells 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
CHEMBL1223938 15764 0 ACM5 M5 receptor Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells 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
57525835 89404 0 ACM5 M5 receptor Human 6.3 pEC50 = 6.3 Binding
Positive allosteric modulation of human muscarinic M5 receptorPositive allosteric modulation of human muscarinic M5 receptor
ChEMBL 365 5 0 4 3.5 Cc1cccc(OCCN2C(=O)C(=O)c3cc(OC(F)(F)F)ccc32)c1 10.1016/j.bmcl.2013.03.032
CHEMBL2381698 89404 0 ACM5 M5 receptor Human 6.3 pEC50 = 6.3 Binding
Positive allosteric modulation of human muscarinic M5 receptorPositive allosteric modulation of human muscarinic M5 receptor
ChEMBL 365 5 0 4 3.5 Cc1cccc(OCCN2C(=O)C(=O)c3cc(OC(F)(F)F)ccc32)c1 10.1016/j.bmcl.2013.03.032
57525835 89404 0 ACM5 M5 receptor Human 6.3 pEC50 = 6.3 Binding
Positive allosteric modulation of human muscarinic M5 receptorPositive allosteric modulation of human muscarinic M5 receptor
ChEMBL 365 5 0 4 3.5 Cc1cccc(OCCN2C(=O)C(=O)c3cc(OC(F)(F)F)ccc32)c1 10.1016/j.bmcl.2013.03.032
CHEMBL2381698 89404 0 ACM5 M5 receptor Human 6.3 pEC50 = 6.3 Binding
Positive allosteric modulation of human muscarinic M5 receptorPositive allosteric modulation of human muscarinic M5 receptor
ChEMBL 365 5 0 4 3.5 Cc1cccc(OCCN2C(=O)C(=O)c3cc(OC(F)(F)F)ccc32)c1 10.1016/j.bmcl.2013.03.032
71737683 113480 0 ACM5 M5 receptor Human 5.3 pEC50 = 5.3 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 494 6 1 4 4.0 CCN(Cc1cccc(C(F)(F)F)c1)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1 10.1021/jm500995y
CHEMBL3329752 113480 0 ACM5 M5 receptor Human 5.3 pEC50 = 5.3 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 494 6 1 4 4.0 CCN(Cc1cccc(C(F)(F)F)c1)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1 10.1021/jm500995y
302 2796 20 ACM5 M5 receptor Human 7.3 pEC50 = 7.3 Binding
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M5 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M5 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1 10.1021/jm00012a019
4630 2796 20 ACM5 M5 receptor Human 7.3 pEC50 = 7.3 Binding
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M5 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M5 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1 10.1021/jm00012a019
CHEMBL7634 2796 20 ACM5 M5 receptor Human 7.3 pEC50 = 7.3 Binding
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M5 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M5 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1 10.1021/jm00012a019
71737683 113480 0 ACM5 M5 receptor Human 5.3 pEC50 = 5.3 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 494 6 1 4 4.0 CCN(Cc1cccc(C(F)(F)F)c1)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1 10.1021/jm500995y
CHEMBL3329752 113480 0 ACM5 M5 receptor Human 5.3 pEC50 = 5.3 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 494 6 1 4 4.0 CCN(Cc1cccc(C(F)(F)F)c1)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1 10.1021/jm500995y
45281807 193600 0 ACM5 M5 receptor Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilizationAgonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilization
ChEMBL 351 4 0 4 3.3 COc1ccc(CN2C(=O)C(=O)c3ccc(OC(F)(F)F)cc32)cc1 10.1016/j.bmcl.2009.11.089
CHEMBL595404 193600 0 ACM5 M5 receptor Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilizationAgonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilization
ChEMBL 351 4 0 4 3.3 COc1ccc(CN2C(=O)C(=O)c3ccc(OC(F)(F)F)cc32)cc1 10.1016/j.bmcl.2009.11.089
57525858 89403 0 ACM5 M5 receptor Human 6.2 pEC50 = 6.2 Binding
Positive allosteric modulation of human muscarinic M5 receptorPositive allosteric modulation of human muscarinic M5 receptor
ChEMBL 381 6 0 5 3.2 COc1ccc(OCCN2C(=O)C(=O)c3cc(OC(F)(F)F)ccc32)cc1 10.1016/j.bmcl.2013.03.032
CHEMBL2381697 89403 0 ACM5 M5 receptor Human 6.2 pEC50 = 6.2 Binding
Positive allosteric modulation of human muscarinic M5 receptorPositive allosteric modulation of human muscarinic M5 receptor
ChEMBL 381 6 0 5 3.2 COc1ccc(OCCN2C(=O)C(=O)c3cc(OC(F)(F)F)ccc32)cc1 10.1016/j.bmcl.2013.03.032
57525858 89403 0 ACM5 M5 receptor Human 6.2 pEC50 = 6.2 Binding
Positive allosteric modulation of human muscarinic M5 receptorPositive allosteric modulation of human muscarinic M5 receptor
ChEMBL 381 6 0 5 3.2 COc1ccc(OCCN2C(=O)C(=O)c3cc(OC(F)(F)F)ccc32)cc1 10.1016/j.bmcl.2013.03.032
CHEMBL2381697 89403 0 ACM5 M5 receptor Human 6.2 pEC50 = 6.2 Binding
Positive allosteric modulation of human muscarinic M5 receptorPositive allosteric modulation of human muscarinic M5 receptor
ChEMBL 381 6 0 5 3.2 COc1ccc(OCCN2C(=O)C(=O)c3cc(OC(F)(F)F)ccc32)cc1 10.1016/j.bmcl.2013.03.032
52940924 16774 0 ACM5 M5 receptor Human 5.2 pEC50 = 5.2 Functional
Positive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assayPositive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 415 4 0 3 5.1 O=C1C(=O)N(Cc2ccc(-c3ccccc3)cc2F)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2010.08.042
CHEMBL1255607 16774 0 ACM5 M5 receptor Human 5.2 pEC50 = 5.2 Functional
Positive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assayPositive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 415 4 0 3 5.1 O=C1C(=O)N(Cc2ccc(-c3ccccc3)cc2F)c2ccc(OC(F)(F)F)cc21 10.1016/j.bmcl.2010.08.042
2230 445 46 ACM5 M5 receptor Human 6.2 pEC50 = 6.2 Binding
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M5 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M5 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 ACM5 M5 receptor Human 6.2 pEC50 = 6.2 Binding
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M5 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M5 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 ACM5 M5 receptor Human 6.2 pEC50 = 6.2 Binding
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M5 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M5 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 ACM5 M5 receptor Human 6.2 pEC50 = 6.2 Binding
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M5 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M5 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
44251556 6350 3 ACM5 M5 receptor Human 6.2 pEC50 = 6.2 Binding
Positive allosteric modulation of human muscarinic M5 receptorPositive allosteric modulation of human muscarinic M5 receptor
ChEMBL 335 3 0 4 3.0 Cn1cc(-c2ccc(CN3C(=O)C(=O)c4ccccc43)c(F)c2)cn1 10.1016/j.bmcl.2013.03.032
CHEMBL1083203 6350 3 ACM5 M5 receptor Human 6.2 pEC50 = 6.2 Binding
Positive allosteric modulation of human muscarinic M5 receptorPositive allosteric modulation of human muscarinic M5 receptor
ChEMBL 335 3 0 4 3.0 Cn1cc(-c2ccc(CN3C(=O)C(=O)c4ccccc43)c(F)c2)cn1 10.1016/j.bmcl.2013.03.032
71737672 2419 4 ACM5 M5 receptor Rat 6.2 pEC50 = 6.2 Functional
Activity at rat muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayActivity at rat muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 494 6 1 4 4.0 CCN(C(=O)C1CCN(CC1)S(=O)(=O)c1ccc2c(c1)cn[nH]2)Cc1ccccc1C(F)(F)F 10.1021/jm500995y
8687 2419 4 ACM5 M5 receptor Rat 6.2 pEC50 = 6.2 Functional
Activity at rat muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayActivity at rat muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 494 6 1 4 4.0 CCN(C(=O)C1CCN(CC1)S(=O)(=O)c1ccc2c(c1)cn[nH]2)Cc1ccccc1C(F)(F)F 10.1021/jm500995y
CHEMBL3329755 2419 4 ACM5 M5 receptor Rat 6.2 pEC50 = 6.2 Functional
Activity at rat muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayActivity at rat muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 494 6 1 4 4.0 CCN(C(=O)C1CCN(CC1)S(=O)(=O)c1ccc2c(c1)cn[nH]2)Cc1ccccc1C(F)(F)F 10.1021/jm500995y
26415263 113457 3 ACM5 M5 receptor Human 5.2 pEC50 = 5.2 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 386 6 0 3 3.1 CCN(Cc1ccccc1)C(=O)C1CCN(S(=O)(=O)c2ccccc2)CC1 10.1021/jm500995y
CHEMBL3329715 113457 3 ACM5 M5 receptor Human 5.2 pEC50 = 5.2 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 386 6 0 3 3.1 CCN(Cc1ccccc1)C(=O)C1CCN(S(=O)(=O)c2ccccc2)CC1 10.1021/jm500995y
26415263 113457 3 ACM5 M5 receptor Human 5.2 pEC50 = 5.2 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 386 6 0 3 3.1 CCN(Cc1ccccc1)C(=O)C1CCN(S(=O)(=O)c2ccccc2)CC1 10.1021/jm500995y
CHEMBL3329715 113457 3 ACM5 M5 receptor Human 5.2 pEC50 = 5.2 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 386 6 0 3 3.1 CCN(Cc1ccccc1)C(=O)C1CCN(S(=O)(=O)c2ccccc2)CC1 10.1021/jm500995y
187 245 23 ACM5 M5 receptor Human 6.2 pEC50 = 6.2 Functional
Agonistic activity against muscarinic acetylcholine receptor M5 expressed in NIH 3T3 cells.Agonistic activity against muscarinic acetylcholine receptor M5 expressed in NIH 3T3 cells.
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm0102405
294 245 23 ACM5 M5 receptor Human 6.2 pEC50 = 6.2 Functional
Agonistic activity against muscarinic acetylcholine receptor M5 expressed in NIH 3T3 cells.Agonistic activity against muscarinic acetylcholine receptor M5 expressed in NIH 3T3 cells.
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm0102405
65 245 23 ACM5 M5 receptor Human 6.2 pEC50 = 6.2 Functional
Agonistic activity against muscarinic acetylcholine receptor M5 expressed in NIH 3T3 cells.Agonistic activity against muscarinic acetylcholine receptor M5 expressed in NIH 3T3 cells.
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm0102405
8593 245 23 ACM5 M5 receptor Human 6.2 pEC50 = 6.2 Functional
Agonistic activity against muscarinic acetylcholine receptor M5 expressed in NIH 3T3 cells.Agonistic activity against muscarinic acetylcholine receptor M5 expressed in NIH 3T3 cells.
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm0102405
CHEMBL667 245 23 ACM5 M5 receptor Human 6.2 pEC50 = 6.2 Functional
Agonistic activity against muscarinic acetylcholine receptor M5 expressed in NIH 3T3 cells.Agonistic activity against muscarinic acetylcholine receptor M5 expressed in NIH 3T3 cells.
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm0102405
DB03128 245 23 ACM5 M5 receptor Human 6.2 pEC50 = 6.2 Functional
Agonistic activity against muscarinic acetylcholine receptor M5 expressed in NIH 3T3 cells.Agonistic activity against muscarinic acetylcholine receptor M5 expressed in NIH 3T3 cells.
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm0102405
44418764 81511 0 ACM5 M5 receptor Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human M5 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M5 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 487 16 0 13 1.8 COc1nsc(OCCOCCOCCOCCOc2nsnc2C2C=CCCN2C)n1 10.1021/jm0606995
CHEMBL216928 81511 0 ACM5 M5 receptor Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human M5 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M5 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 487 16 0 13 1.8 COc1nsc(OCCOCCOCCOCCOc2nsnc2C2C=CCCN2C)n1 10.1021/jm0606995
2551 750 19 ACM5 M5 receptor Human 5.2 pEC50 = 5.2 Binding
Effective concentration was evaluated against Muscarinic acetylcholine receptor M5 expressed in A9 L cellsEffective concentration was evaluated against Muscarinic acetylcholine receptor M5 expressed in A9 L cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0301235
298 750 19 ACM5 M5 receptor Human 5.2 pEC50 = 5.2 Binding
Effective concentration was evaluated against Muscarinic acetylcholine receptor M5 expressed in A9 L cellsEffective concentration was evaluated against Muscarinic acetylcholine receptor M5 expressed in A9 L cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0301235
488 750 19 ACM5 M5 receptor Human 5.2 pEC50 = 5.2 Binding
Effective concentration was evaluated against Muscarinic acetylcholine receptor M5 expressed in A9 L cellsEffective concentration was evaluated against Muscarinic acetylcholine receptor M5 expressed in A9 L cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0301235
CHEMBL965 750 19 ACM5 M5 receptor Human 5.2 pEC50 = 5.2 Binding
Effective concentration was evaluated against Muscarinic acetylcholine receptor M5 expressed in A9 L cellsEffective concentration was evaluated against Muscarinic acetylcholine receptor M5 expressed in A9 L cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0301235
DB00411 750 19 ACM5 M5 receptor Human 5.2 pEC50 = 5.2 Binding
Effective concentration was evaluated against Muscarinic acetylcholine receptor M5 expressed in A9 L cellsEffective concentration was evaluated against Muscarinic acetylcholine receptor M5 expressed in A9 L cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0301235
71737675 113478 0 ACM5 M5 receptor Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 460 6 1 4 3.7 CCN(Cc1ccccc1Cl)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1 10.1021/jm500995y
CHEMBL3329750 113478 0 ACM5 M5 receptor Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 460 6 1 4 3.7 CCN(Cc1ccccc1Cl)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1 10.1021/jm500995y
71737675 113478 0 ACM5 M5 receptor Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 460 6 1 4 3.7 CCN(Cc1ccccc1Cl)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1 10.1021/jm500995y
CHEMBL3329750 113478 0 ACM5 M5 receptor Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 460 6 1 4 3.7 CCN(Cc1ccccc1Cl)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1 10.1021/jm500995y
650899 53914 9 ACM5 M5 receptor Human 4.2 pEC50 = 4.2 Functional
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M5. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M5. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]
ChEMBL 319 6 2 4 1.6 CCOC(=O)N1CCC(NCCNC(=O)c2ccccc2)CC1 nan
CHEMBL1535797 53914 9 ACM5 M5 receptor Human 4.2 pEC50 = 4.2 Functional
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M5. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M5. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]
ChEMBL 319 6 2 4 1.6 CCOC(=O)N1CCC(NCCNC(=O)c2ccccc2)CC1 nan
CHEMBL1609153 53914 9 ACM5 M5 receptor Human 4.2 pEC50 = 4.2 Functional
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M5. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M5. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]
ChEMBL 319 6 2 4 1.6 CCOC(=O)N1CCC(NCCNC(=O)c2ccccc2)CC1 nan
11056389 186543 0 ACM5 M5 receptor Human 5.2 pEC50 = 5.2 Functional
Activation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 323 2 0 2 3.6 O=C1C(=O)N(Cc2ccc(C(F)(F)F)cc2)c2ccc(F)cc21 10.1021/jm900286j
CHEMBL512977 186543 0 ACM5 M5 receptor Human 5.2 pEC50 = 5.2 Functional
Activation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 323 2 0 2 3.6 O=C1C(=O)N(Cc2ccc(C(F)(F)F)cc2)c2ccc(F)cc21 10.1021/jm900286j
44158005 186579 0 ACM5 M5 receptor Human 5.2 pEC50 = 5.2 Functional
Activation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 335 3 0 3 3.7 COc1cccc(CN2C(=O)C(=O)c3c(Cl)ccc(Cl)c32)c1 10.1021/jm900286j
CHEMBL513311 186579 0 ACM5 M5 receptor Human 5.2 pEC50 = 5.2 Functional
Activation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 335 3 0 3 3.7 COc1cccc(CN2C(=O)C(=O)c3c(Cl)ccc(Cl)c32)c1 10.1021/jm900286j
71737624 113468 0 ACM5 M5 receptor Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 440 6 0 3 4.2 CCN(C(=O)C1CCN(S(=O)(=O)c2ccc3c(c2)CCC3)CC1)[C@H](C)c1ccccc1 10.1021/jm500995y
CHEMBL3329739 113468 0 ACM5 M5 receptor Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 440 6 0 3 4.2 CCN(C(=O)C1CCN(S(=O)(=O)c2ccc3c(c2)CCC3)CC1)[C@H](C)c1ccccc1 10.1021/jm500995y
71737624 113468 0 ACM5 M5 receptor Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 440 6 0 3 4.2 CCN(C(=O)C1CCN(S(=O)(=O)c2ccc3c(c2)CCC3)CC1)[C@H](C)c1ccccc1 10.1021/jm500995y
CHEMBL3329739 113468 0 ACM5 M5 receptor Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 440 6 0 3 4.2 CCN(C(=O)C1CCN(S(=O)(=O)c2ccc3c(c2)CCC3)CC1)[C@H](C)c1ccccc1 10.1021/jm500995y
71737617 113470 0 ACM5 M5 receptor Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 440 6 1 4 3.6 CCN(C(=O)C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1)[C@H](C)c1ccccc1 10.1021/jm500995y
CHEMBL3329741 113470 0 ACM5 M5 receptor Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 440 6 1 4 3.6 CCN(C(=O)C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1)[C@H](C)c1ccccc1 10.1021/jm500995y
71737760 113464 0 ACM5 M5 receptor Human 5.1 pEC50 = 5.1 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 430 6 0 5 2.9 CCN(Cc1ccccc1)C(=O)C1CCN(S(=O)(=O)c2ccc3c(c2)OCO3)CC1 10.1021/jm500995y
CHEMBL3329734 113464 0 ACM5 M5 receptor Human 5.1 pEC50 = 5.1 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 430 6 0 5 2.9 CCN(Cc1ccccc1)C(=O)C1CCN(S(=O)(=O)c2ccc3c(c2)OCO3)CC1 10.1021/jm500995y
71737617 113470 0 ACM5 M5 receptor Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 440 6 1 4 3.6 CCN(C(=O)C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1)[C@H](C)c1ccccc1 10.1021/jm500995y
CHEMBL3329741 113470 0 ACM5 M5 receptor Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 440 6 1 4 3.6 CCN(C(=O)C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1)[C@H](C)c1ccccc1 10.1021/jm500995y
71737760 113464 0 ACM5 M5 receptor Human 5.1 pEC50 = 5.1 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 430 6 0 5 2.9 CCN(Cc1ccccc1)C(=O)C1CCN(S(=O)(=O)c2ccc3c(c2)OCO3)CC1 10.1021/jm500995y
CHEMBL3329734 113464 0 ACM5 M5 receptor Human 5.1 pEC50 = 5.1 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 430 6 0 5 2.9 CCN(Cc1ccccc1)C(=O)C1CCN(S(=O)(=O)c2ccc3c(c2)OCO3)CC1 10.1021/jm500995y
71737763 113477 0 ACM5 M5 receptor Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 456 7 1 5 3.0 CCN(Cc1ccccc1OC)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1 10.1021/jm500995y
CHEMBL3329749 113477 0 ACM5 M5 receptor Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 456 7 1 5 3.0 CCN(Cc1ccccc1OC)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1 10.1021/jm500995y
71737618 113469 0 ACM5 M5 receptor Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 440 6 1 4 3.6 CCN(C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1)[C@H](C)c1ccccc1 10.1021/jm500995y
CHEMBL3329740 113469 0 ACM5 M5 receptor Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 440 6 1 4 3.6 CCN(C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1)[C@H](C)c1ccccc1 10.1021/jm500995y
71737763 113477 0 ACM5 M5 receptor Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 456 7 1 5 3.0 CCN(Cc1ccccc1OC)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1 10.1021/jm500995y
CHEMBL3329749 113477 0 ACM5 M5 receptor Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 456 7 1 5 3.0 CCN(Cc1ccccc1OC)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1 10.1021/jm500995y
71737618 113469 0 ACM5 M5 receptor Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 440 6 1 4 3.6 CCN(C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1)[C@H](C)c1ccccc1 10.1021/jm500995y
CHEMBL3329740 113469 0 ACM5 M5 receptor Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 440 6 1 4 3.6 CCN(C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1)[C@H](C)c1ccccc1 10.1021/jm500995y
6861557 113753 20 ACM5 M5 receptor Human 5.1 pEC50 = 5.1 Binding
Silent allosteric modulator activity at human muscarinic acetylcholine receptor M5 expressed in CHO cells by fluorometric imaging plate readerSilent allosteric modulator activity at human muscarinic acetylcholine receptor M5 expressed in CHO cells by fluorometric imaging plate reader
ChEMBL 276 3 0 2 4.4 Clc1cccc(/C=N/N=C/c2cccc(Cl)c2)c1 10.1021/jm5011786
CHEMBL3334990 113753 20 ACM5 M5 receptor Human 5.1 pEC50 = 5.1 Binding
Silent allosteric modulator activity at human muscarinic acetylcholine receptor M5 expressed in CHO cells by fluorometric imaging plate readerSilent allosteric modulator activity at human muscarinic acetylcholine receptor M5 expressed in CHO cells by fluorometric imaging plate reader
ChEMBL 276 3 0 2 4.4 Clc1cccc(/C=N/N=C/c2cccc(Cl)c2)c1 10.1021/jm5011786
187 245 23 ACM5 M5 receptor Human 6.1 pEC50 = 6.1 Binding
Activation of M5-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M5-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmc.2010.07.060
294 245 23 ACM5 M5 receptor Human 6.1 pEC50 = 6.1 Binding
Activation of M5-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M5-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmc.2010.07.060
65 245 23 ACM5 M5 receptor Human 6.1 pEC50 = 6.1 Binding
Activation of M5-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M5-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmc.2010.07.060
8593 245 23 ACM5 M5 receptor Human 6.1 pEC50 = 6.1 Binding
Activation of M5-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M5-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmc.2010.07.060
CHEMBL667 245 23 ACM5 M5 receptor Human 6.1 pEC50 = 6.1 Binding
Activation of M5-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M5-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmc.2010.07.060
DB03128 245 23 ACM5 M5 receptor Human 6.1 pEC50 = 6.1 Binding
Activation of M5-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signalActivation of M5-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmc.2010.07.060
16071018 15695 13 ACM5 M5 receptor Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 333 2 1 4 2.6 Cc1cc2c(cc1F)[nH]c(=O)n2C1CCN(C2CCOCC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223753 15695 13 ACM5 M5 receptor Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 333 2 1 4 2.6 Cc1cc2c(cc1F)[nH]c(=O)n2C1CCN(C2CCOCC2)CC1 10.1016/j.bmcl.2010.07.097
16071018 15695 13 ACM5 M5 receptor Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assay
ChEMBL 333 2 1 4 2.6 Cc1cc2c(cc1F)[nH]c(=O)n2C1CCN(C2CCOCC2)CC1 10.1021/ml100105x
CHEMBL1223753 15695 13 ACM5 M5 receptor Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assayAgonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assay
ChEMBL 333 2 1 4 2.6 Cc1cc2c(cc1F)[nH]c(=O)n2C1CCN(C2CCOCC2)CC1 10.1021/ml100105x
71737681 113475 0 ACM5 M5 receptor Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 440 6 1 4 3.3 CCN(Cc1cccc(C)c1)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1 10.1021/jm500995y
CHEMBL3329747 113475 0 ACM5 M5 receptor Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 440 6 1 4 3.3 CCN(Cc1cccc(C)c1)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1 10.1021/jm500995y
71737677 113476 0 ACM5 M5 receptor Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 440 6 1 4 3.3 CCN(Cc1ccccc1C)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1 10.1021/jm500995y
CHEMBL3329748 113476 0 ACM5 M5 receptor Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 440 6 1 4 3.3 CCN(Cc1ccccc1C)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1 10.1021/jm500995y
71737681 113475 0 ACM5 M5 receptor Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 440 6 1 4 3.3 CCN(Cc1cccc(C)c1)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1 10.1021/jm500995y
CHEMBL3329747 113475 0 ACM5 M5 receptor Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 440 6 1 4 3.3 CCN(Cc1cccc(C)c1)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1 10.1021/jm500995y
71737677 113476 0 ACM5 M5 receptor Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 440 6 1 4 3.3 CCN(Cc1ccccc1C)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1 10.1021/jm500995y
CHEMBL3329748 113476 0 ACM5 M5 receptor Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 440 6 1 4 3.3 CCN(Cc1ccccc1C)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1 10.1021/jm500995y
647412 26922 9 ACM5 M5 receptor Human 4.1 pEC50 = 4.1 Functional
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M5. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M5. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]
ChEMBL 325 6 2 5 1.7 CCOC(=O)N1CCC(NCCNC(=O)c2cccs2)CC1 nan
CHEMBL1367424 26922 9 ACM5 M5 receptor Human 4.1 pEC50 = 4.1 Functional
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M5. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist NMS competition at M5. (Class of assay: confirmatory) [Related pubchem assays: 1488 (Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Confirmation Assay), 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen)]
ChEMBL 325 6 2 5 1.7 CCOC(=O)N1CCC(NCCNC(=O)c2cccs2)CC1 nan
2551 750 19 ACM5 M5 receptor Human 5.1 pEC50 = 5.1 Functional
Agonistic activity against muscarinic acetylcholine receptor M5 expressed in NIH 3T3 cellsAgonistic activity against muscarinic acetylcholine receptor M5 expressed in NIH 3T3 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0102405
298 750 19 ACM5 M5 receptor Human 5.1 pEC50 = 5.1 Functional
Agonistic activity against muscarinic acetylcholine receptor M5 expressed in NIH 3T3 cellsAgonistic activity against muscarinic acetylcholine receptor M5 expressed in NIH 3T3 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0102405
488 750 19 ACM5 M5 receptor Human 5.1 pEC50 = 5.1 Functional
Agonistic activity against muscarinic acetylcholine receptor M5 expressed in NIH 3T3 cellsAgonistic activity against muscarinic acetylcholine receptor M5 expressed in NIH 3T3 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0102405
CHEMBL965 750 19 ACM5 M5 receptor Human 5.1 pEC50 = 5.1 Functional
Agonistic activity against muscarinic acetylcholine receptor M5 expressed in NIH 3T3 cellsAgonistic activity against muscarinic acetylcholine receptor M5 expressed in NIH 3T3 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0102405
DB00411 750 19 ACM5 M5 receptor Human 5.1 pEC50 = 5.1 Functional
Agonistic activity against muscarinic acetylcholine receptor M5 expressed in NIH 3T3 cellsAgonistic activity against muscarinic acetylcholine receptor M5 expressed in NIH 3T3 cells
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0102405
71737619 113466 0 ACM5 M5 receptor Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 440 6 0 4 4.4 CCN(C(=O)C1CCN(S(=O)(=O)c2ccc3occc3c2)CC1)[C@H](C)c1ccccc1 10.1021/jm500995y
CHEMBL3329737 113466 0 ACM5 M5 receptor Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 440 6 0 4 4.4 CCN(C(=O)C1CCN(S(=O)(=O)c2ccc3occc3c2)CC1)[C@H](C)c1ccccc1 10.1021/jm500995y
71737619 113466 0 ACM5 M5 receptor Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 440 6 0 4 4.4 CCN(C(=O)C1CCN(S(=O)(=O)c2ccc3occc3c2)CC1)[C@H](C)c1ccccc1 10.1021/jm500995y
CHEMBL3329737 113466 0 ACM5 M5 receptor Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 440 6 0 4 4.4 CCN(C(=O)C1CCN(S(=O)(=O)c2ccc3occc3c2)CC1)[C@H](C)c1ccccc1 10.1021/jm500995y
10261985 197522 0 ACM5 M5 receptor Human 6.0 pEC50 = 6.0 Binding
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M5 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M5 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 192 2 1 4 0.7 C#CCOc1noc2c1CNCCC2 10.1021/jm00012a019
CHEMBL69306 197522 0 ACM5 M5 receptor Human 6.0 pEC50 = 6.0 Binding
In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M5 determined by receptor selection and amplification technology (R-SAT)In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M5 determined by receptor selection and amplification technology (R-SAT)
ChEMBL 192 2 1 4 0.7 C#CCOc1noc2c1CNCCC2 10.1021/jm00012a019
71737602 113465 0 ACM5 M5 receptor Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 430 7 0 4 3.7 CCN(C(=O)C1CCN(S(=O)(=O)c2ccc(OC)cc2)CC1)[C@H](C)c1ccccc1 10.1021/jm500995y
CHEMBL3329736 113465 0 ACM5 M5 receptor Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 430 7 0 4 3.7 CCN(C(=O)C1CCN(S(=O)(=O)c2ccc(OC)cc2)CC1)[C@H](C)c1ccccc1 10.1021/jm500995y
71737602 113465 0 ACM5 M5 receptor Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 430 7 0 4 3.7 CCN(C(=O)C1CCN(S(=O)(=O)c2ccc(OC)cc2)CC1)[C@H](C)c1ccccc1 10.1021/jm500995y
CHEMBL3329736 113465 0 ACM5 M5 receptor Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
ChEMBL 430 7 0 4 3.7 CCN(C(=O)C1CCN(S(=O)(=O)c2ccc(OC)cc2)CC1)[C@H](C)c1ccccc1 10.1021/jm500995y
CHEMBL1900528 67012 0 ACM5 M5 receptor Human 10.0 pIC50 = 10 Binding
Displacement of [3H]NMS from human muscarinic M5 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M5 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 392 4 1 6 2.3 C[N+]1(C)[C@H]2C[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)C[C@@H]1[C@H]1O[C@@H]21 10.1016/j.bmcl.2010.10.016
CHEMBL3545181 67012 0 ACM5 M5 receptor Human 10.0 pIC50 = 10 Binding
Displacement of [3H]NMS from human muscarinic M5 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M5 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 392 4 1 6 2.3 C[N+]1(C)[C@H]2C[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)C[C@@H]1[C@H]1O[C@@H]21 10.1016/j.bmcl.2010.10.016
CHEMBL4440620 67012 0 ACM5 M5 receptor Human 10.0 pIC50 = 10 Binding
Displacement of [3H]NMS from human muscarinic M5 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M5 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 392 4 1 6 2.3 C[N+]1(C)[C@H]2C[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)C[C@@H]1[C@H]1O[C@@H]21 10.1016/j.bmcl.2010.10.016
11434515 251 2 ACM5 M5 receptor Human 9.8 pIC50 = 9.8 Binding
Displacement of [3H]NMS from human muscarinic M5 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M5 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1016/j.bmcl.2010.10.016
11519741 251 2 ACM5 M5 receptor Human 9.8 pIC50 = 9.8 Binding
Displacement of [3H]NMS from human muscarinic M5 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M5 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1016/j.bmcl.2010.10.016
4484 251 2 ACM5 M5 receptor Human 9.8 pIC50 = 9.8 Binding
Displacement of [3H]NMS from human muscarinic M5 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M5 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1016/j.bmcl.2010.10.016
7449 251 2 ACM5 M5 receptor Human 9.8 pIC50 = 9.8 Binding
Displacement of [3H]NMS from human muscarinic M5 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M5 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1016/j.bmcl.2010.10.016
CHEMBL1194325 251 2 ACM5 M5 receptor Human 9.8 pIC50 = 9.8 Binding
Displacement of [3H]NMS from human muscarinic M5 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M5 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1016/j.bmcl.2010.10.016
DB08897 251 2 ACM5 M5 receptor Human 9.8 pIC50 = 9.8 Binding
Displacement of [3H]NMS from human muscarinic M5 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M5 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1016/j.bmcl.2010.10.016
11693 1707 10 ACM5 M5 receptor Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]NMS from human muscarinic M5 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M5 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1016/j.bmcl.2010.10.016
3494 1707 10 ACM5 M5 receptor Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]NMS from human muscarinic M5 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M5 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1016/j.bmcl.2010.10.016
4302 1707 10 ACM5 M5 receptor Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]NMS from human muscarinic M5 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M5 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1016/j.bmcl.2010.10.016
7459 1707 10 ACM5 M5 receptor Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]NMS from human muscarinic M5 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M5 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1016/j.bmcl.2010.10.016
CHEMBL1201335 1707 10 ACM5 M5 receptor Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]NMS from human muscarinic M5 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M5 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1016/j.bmcl.2010.10.016
DB00986 1707 10 ACM5 M5 receptor Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]NMS from human muscarinic M5 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assayDisplacement of [3H]NMS from human muscarinic M5 receptor expressed in CHO-K1 cells after 16 hrs by scintillation proximity assay
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1016/j.bmcl.2010.10.016
1734 112 5 ACM5 M5 receptor Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]4-DAMP from human recombinant M5 receptor expressed in CHO cells measured after 60 mins by scintillation counting methodDisplacement of [3H]4-DAMP from human recombinant M5 receptor expressed in CHO cells measured after 60 mins by scintillation counting method
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.bmc.2016.11.014
307 112 5 ACM5 M5 receptor Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]4-DAMP from human recombinant M5 receptor expressed in CHO cells measured after 60 mins by scintillation counting methodDisplacement of [3H]4-DAMP from human recombinant M5 receptor expressed in CHO cells measured after 60 mins by scintillation counting method
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.bmc.2016.11.014
CHEMBL168067 112 5 ACM5 M5 receptor Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]4-DAMP from human recombinant M5 receptor expressed in CHO cells measured after 60 mins by scintillation counting methodDisplacement of [3H]4-DAMP from human recombinant M5 receptor expressed in CHO cells measured after 60 mins by scintillation counting method
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.bmc.2016.11.014
1734 112 5 ACM5 M5 receptor Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]4-DAMP from human recombinant muscarinic M5 receptor expressed in CHO cellsDisplacement of [3H]4-DAMP from human recombinant muscarinic M5 receptor expressed in CHO cells
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.bmc.2016.03.006
307 112 5 ACM5 M5 receptor Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]4-DAMP from human recombinant muscarinic M5 receptor expressed in CHO cellsDisplacement of [3H]4-DAMP from human recombinant muscarinic M5 receptor expressed in CHO cells
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.bmc.2016.03.006
CHEMBL168067 112 5 ACM5 M5 receptor Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]4-DAMP from human recombinant muscarinic M5 receptor expressed in CHO cellsDisplacement of [3H]4-DAMP from human recombinant muscarinic M5 receptor expressed in CHO cells
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.bmc.2016.03.006
CHEMBL1201024 14152 0 ACM5 M5 receptor Human 9.4 pIC50 = 9.4 Binding
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 318 4 1 4 1.1 C[N+]1(C)[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@H]1[C@H]1O[C@@H]21 nan
CHEMBL1201268 14152 0 ACM5 M5 receptor Human 9.4 pIC50 = 9.4 Binding
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 318 4 1 4 1.1 C[N+]1(C)[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@H]1[C@H]1O[C@@H]21 nan
1734 112 5 ACM5 M5 receptor Human 9.4 pIC50 = 9.4 Binding
Binding affinity to human muscarinic M5 receptor by radioligand displacement assayBinding affinity to human muscarinic M5 receptor by radioligand displacement assay
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.ejmech.2013.01.044
307 112 5 ACM5 M5 receptor Human 9.4 pIC50 = 9.4 Binding
Binding affinity to human muscarinic M5 receptor by radioligand displacement assayBinding affinity to human muscarinic M5 receptor by radioligand displacement assay
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.ejmech.2013.01.044
CHEMBL168067 112 5 ACM5 M5 receptor Human 9.4 pIC50 = 9.4 Binding
Binding affinity to human muscarinic M5 receptor by radioligand displacement assayBinding affinity to human muscarinic M5 receptor by radioligand displacement assay
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.ejmech.2013.01.044
71575552 85527 0 ACM5 M5 receptor Rat 9.4 pIC50 = 9.4 Binding
Orthosteric antagonist activity at M5 muscarinic receptor in rat striatal slices assessed as inhibition of 100 uM oxotremorine-evoked [3H]DA releaseOrthosteric antagonist activity at M5 muscarinic receptor in rat striatal slices assessed as inhibition of 100 uM oxotremorine-evoked [3H]DA release
ChEMBL 381 7 0 5 3.6 COc1ccc(CCOC(=O)C2=C(c3ccccc3)CCN(C)C2)cc1OC 10.1021/jm301774u
CHEMBL2312346 85527 0 ACM5 M5 receptor Rat 9.4 pIC50 = 9.4 Binding
Orthosteric antagonist activity at M5 muscarinic receptor in rat striatal slices assessed as inhibition of 100 uM oxotremorine-evoked [3H]DA releaseOrthosteric antagonist activity at M5 muscarinic receptor in rat striatal slices assessed as inhibition of 100 uM oxotremorine-evoked [3H]DA release
ChEMBL 381 7 0 5 3.6 COc1ccc(CCOC(=O)C2=C(c3ccccc3)CCN(C)C2)cc1OC 10.1021/jm301774u
1734 112 5 ACM5 M5 receptor Human 9.1 pIC50 = 9.1 Binding
Binding affinity to human muscarinic M5 receptor by radioligand displacement assayBinding affinity to human muscarinic M5 receptor by radioligand displacement assay
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.bmc.2013.03.016
307 112 5 ACM5 M5 receptor Human 9.1 pIC50 = 9.1 Binding
Binding affinity to human muscarinic M5 receptor by radioligand displacement assayBinding affinity to human muscarinic M5 receptor by radioligand displacement assay
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.bmc.2013.03.016
CHEMBL168067 112 5 ACM5 M5 receptor Human 9.1 pIC50 = 9.1 Binding
Binding affinity to human muscarinic M5 receptor by radioligand displacement assayBinding affinity to human muscarinic M5 receptor by radioligand displacement assay
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1016/j.bmc.2013.03.016
1734 112 5 ACM5 M5 receptor Human 9.1 pIC50 = 9.1 Binding
Displacement of radiolabeled 4DAMP from human muscarinic M5 receptorDisplacement of radiolabeled 4DAMP from human muscarinic M5 receptor
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1021/jm8007618
307 112 5 ACM5 M5 receptor Human 9.1 pIC50 = 9.1 Binding
Displacement of radiolabeled 4DAMP from human muscarinic M5 receptorDisplacement of radiolabeled 4DAMP from human muscarinic M5 receptor
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1021/jm8007618
CHEMBL168067 112 5 ACM5 M5 receptor Human 9.1 pIC50 = 9.1 Binding
Displacement of radiolabeled 4DAMP from human muscarinic M5 receptorDisplacement of radiolabeled 4DAMP from human muscarinic M5 receptor
ChEMBL 324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C 10.1021/jm8007618
174174 501 0 ACM5 M5 receptor Human 9.0 pIC50 = 9.0 Binding
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C nan
260 501 0 ACM5 M5 receptor Human 9.0 pIC50 = 9.0 Binding
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C nan
320 501 0 ACM5 M5 receptor Human 9.0 pIC50 = 9.0 Binding
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C nan
CHEMBL517712 501 0 ACM5 M5 receptor Human 9.0 pIC50 = 9.0 Binding
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C nan
DB00572 501 0 ACM5 M5 receptor Human 9.0 pIC50 = 9.0 Binding
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C nan
2683 102176 19 ACM5 M5 receptor Human 8.0 pIC50 = 8 Binding
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 304 15 0 0 6.5 CCCCCCCCCCCCCCCC[n+]1ccccc1 nan
CHEMBL305906 102176 19 ACM5 M5 receptor Human 8.0 pIC50 = 8 Binding
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 304 15 0 0 6.5 CCCCCCCCCCCCCCCC[n+]1ccccc1 nan
CHEMBL334255 102176 19 ACM5 M5 receptor Human 8.0 pIC50 = 8 Binding
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 304 15 0 0 6.5 CCCCCCCCCCCCCCCC[n+]1ccccc1 nan
2745 3621 32 ACM5 M5 receptor Human 8.0 pIC50 = 8.0 Binding
Evaluated for its binding affinity at human muscarinic receptor m5 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m5 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 10.1016/s0960-894x(98)00351-5
5572 3621 32 ACM5 M5 receptor Human 8.0 pIC50 = 8.0 Binding
Evaluated for its binding affinity at human muscarinic receptor m5 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m5 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 10.1016/s0960-894x(98)00351-5
66007 3621 32 ACM5 M5 receptor Human 8.0 pIC50 = 8.0 Binding
Evaluated for its binding affinity at human muscarinic receptor m5 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m5 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 10.1016/s0960-894x(98)00351-5
7315 3621 32 ACM5 M5 receptor Human 8.0 pIC50 = 8.0 Binding
Evaluated for its binding affinity at human muscarinic receptor m5 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m5 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 10.1016/s0960-894x(98)00351-5
CHEMBL1490 3621 32 ACM5 M5 receptor Human 8.0 pIC50 = 8.0 Binding
Evaluated for its binding affinity at human muscarinic receptor m5 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m5 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 10.1016/s0960-894x(98)00351-5
DB00376 3621 32 ACM5 M5 receptor Human 8.0 pIC50 = 8.0 Binding
Evaluated for its binding affinity at human muscarinic receptor m5 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m5 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 10.1016/s0960-894x(98)00351-5
71607130 103963 0 ACM5 M5 receptor Human 6.0 pIC50 = 6 Functional
Negative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assayNegative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assay
ChEMBL 424 2 0 2 4.4 O=C(c1cc(F)cc(F)c1)N1CCN2C(=O)c3ccccc3C12c1ccc(Cl)cc1 10.1021/jm4013246
CHEMBL3105212 103963 0 ACM5 M5 receptor Human 6.0 pIC50 = 6 Functional
Negative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assayNegative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assay
ChEMBL 424 2 0 2 4.4 O=C(c1cc(F)cc(F)c1)N1CCN2C(=O)c3ccccc3C12c1ccc(Cl)cc1 10.1021/jm4013246
118719486 114804 0 ACM5 M5 receptor Human 6.0 pIC50 = 6 Functional
Negative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assayNegative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assay
ChEMBL 452 2 0 4 3.6 O=C(c1cc(F)c(F)c(F)c1)N1CCN2C(=O)c3ccccc3C12c1ccc2c(c1)OCO2 10.1016/j.bmcl.2014.11.082
CHEMBL3353274 114804 0 ACM5 M5 receptor Human 6.0 pIC50 = 6 Functional
Negative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assayNegative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assay
ChEMBL 452 2 0 4 3.6 O=C(c1cc(F)c(F)c(F)c1)N1CCN2C(=O)c3ccccc3C12c1ccc2c(c1)OCO2 10.1016/j.bmcl.2014.11.082
14660293 52161 3 ACM5 M5 receptor Human 4.0 pIC50 = 4 Binding
Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M5Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M5
ChEMBL 191 0 1 4 1.3 c1cc2nsnc2c2c1CCNC2 10.1021/jm9705216
CHEMBL15936 52161 3 ACM5 M5 receptor Human 4.0 pIC50 = 4 Binding
Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M5Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M5
ChEMBL 191 0 1 4 1.3 c1cc2nsnc2c2c1CCNC2 10.1021/jm9705216
10354348 98182 0 ACM5 M5 receptor Human 4.0 pIC50 = 4 Binding
Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M5Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M5
ChEMBL 241 2 0 5 2.4 CSc1nsnc1C1=C(C)CCN(C)C1 10.1021/jm9705216
CHEMBL279105 98182 0 ACM5 M5 receptor Human 4.0 pIC50 = 4 Binding
Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M5Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M5
ChEMBL 241 2 0 5 2.4 CSc1nsnc1C1=C(C)CCN(C)C1 10.1021/jm9705216
324 1800 6 ACM5 M5 receptor Human 6.0 pIC50 = 6.0 Binding
Evaluated for its binding affinity at human muscarinic receptor m5 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m5 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@@H]2[C@H]1[C@H](/C=C/[C@H]1CCC[C@@H](N1C)C)[C@H]1CCCC[C@@H]1C2 10.1016/s0960-894x(98)00351-5
6436265 1800 6 ACM5 M5 receptor Human 6.0 pIC50 = 6.0 Binding
Evaluated for its binding affinity at human muscarinic receptor m5 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m5 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@@H]2[C@H]1[C@H](/C=C/[C@H]1CCC[C@@H](N1C)C)[C@H]1CCCC[C@@H]1C2 10.1016/s0960-894x(98)00351-5
CHEMBL277642 1800 6 ACM5 M5 receptor Human 6.0 pIC50 = 6.0 Binding
Evaluated for its binding affinity at human muscarinic receptor m5 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cellEvaluated for its binding affinity at human muscarinic receptor m5 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
ChEMBL 345 2 0 3 4.4 C[C@@H]1OC(=O)[C@@H]2[C@H]1[C@H](/C=C/[C@H]1CCC[C@@H](N1C)C)[C@H]1CCCC[C@@H]1C2 10.1016/s0960-894x(98)00351-5
137638270 156063 0 ACM5 M5 receptor Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant muscarinic M5 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M5 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 434 4 0 8 2.2 Cc1noc(C)c1S(=O)(=O)N1CCN(c2ccc(N3CCCC(C)(C)C3)nn2)CC1 10.1016/j.bmcl.2017.05.042
CHEMBL4071900 156063 0 ACM5 M5 receptor Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant muscarinic M5 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assayAntagonist activity at human recombinant muscarinic M5 receptor expressed in CHO cells co-transfected with Gqi5 in presence of EC80 acetylcholine by calcium mobilization assay
ChEMBL 434 4 0 8 2.2 Cc1noc(C)c1S(=O)(=O)N1CCN(c2ccc(N3CCCC(C)(C)C3)nn2)CC1 10.1016/j.bmcl.2017.05.042
1210 870 35 ACM5 M5 receptor Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
1213 870 35 ACM5 M5 receptor Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
2725 870 35 ACM5 M5 receptor Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
33036 870 35 ACM5 M5 receptor Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
4411 870 35 ACM5 M5 receptor Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
616 870 35 ACM5 M5 receptor Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
6976 870 35 ACM5 M5 receptor Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
716121 870 35 ACM5 M5 receptor Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
90475904 870 35 ACM5 M5 receptor Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
CHEMBL1201353 870 35 ACM5 M5 receptor Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
CHEMBL1554789 870 35 ACM5 M5 receptor Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
CHEMBL505 870 35 ACM5 M5 receptor Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
DB01114 870 35 ACM5 M5 receptor Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
DB13679 870 35 ACM5 M5 receptor Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 274 5 0 2 3.8 CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C nan
71598521 2418 4 ACM5 M5 receptor Human 6.0 pIC50 = 6.0 Functional
Negative allosteric modulation of human M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of human M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 424 2 0 2 4.4 Clc1ccc(cc1)[C@]12N(CCN1C(=O)c1c2cccc1)C(=O)c1ccc(c(c1)F)F 10.1016/j.bmcl.2017.02.020
7631 2418 4 ACM5 M5 receptor Human 6.0 pIC50 = 6.0 Functional
Negative allosteric modulation of human M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of human M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 424 2 0 2 4.4 Clc1ccc(cc1)[C@]12N(CCN1C(=O)c1c2cccc1)C(=O)c1ccc(c(c1)F)F 10.1016/j.bmcl.2017.02.020
CHEMBL3105228 2418 4 ACM5 M5 receptor Human 6.0 pIC50 = 6.0 Functional
Negative allosteric modulation of human M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of human M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 424 2 0 2 4.4 Clc1ccc(cc1)[C@]12N(CCN1C(=O)c1c2cccc1)C(=O)c1ccc(c(c1)F)F 10.1016/j.bmcl.2017.02.020
71607097 103958 0 ACM5 M5 receptor Human 6.0 pIC50 = 6.0 Functional
Negative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assayNegative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assay
ChEMBL 390 2 0 2 3.8 O=C(c1ccc(F)c(F)c1)N1CCN2C(=O)c3ccccc3C12c1ccccc1 10.1021/jm4013246
CHEMBL3105208 103958 0 ACM5 M5 receptor Human 6.0 pIC50 = 6.0 Functional
Negative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assayNegative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assay
ChEMBL 390 2 0 2 3.8 O=C(c1ccc(F)c(F)c1)N1CCN2C(=O)c3ccccc3C12c1ccccc1 10.1021/jm4013246
71607097 103958 0 ACM5 M5 receptor Human 6.0 pIC50 = 6.0 Functional
Negative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assayNegative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assay
ChEMBL 390 2 0 2 3.8 O=C(c1ccc(F)c(F)c1)N1CCN2C(=O)c3ccccc3C12c1ccccc1 10.1021/jm4013246
CHEMBL3105208 103958 0 ACM5 M5 receptor Human 6.0 pIC50 = 6.0 Functional
Negative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assayNegative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assay
ChEMBL 390 2 0 2 3.8 O=C(c1ccc(F)c(F)c1)N1CCN2C(=O)c3ccccc3C12c1ccccc1 10.1021/jm4013246
4841 66860 3 ACM5 M5 receptor Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 368 7 1 3 3.5 CC[N+]1(CCOC(=O)C(O)(c2ccccc2)c2ccccc2)CCCCC1 nan
CHEMBL1889399 66860 3 ACM5 M5 receptor Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 368 7 1 3 3.5 CC[N+]1(CCOC(=O)C(O)(c2ccccc2)c2ccccc2)CCCCC1 nan
CHEMBL1909073 66860 3 ACM5 M5 receptor Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 368 7 1 3 3.5 CC[N+]1(CCOC(=O)C(O)(c2ccccc2)c2ccccc2)CCCCC1 nan
4746 198453 19 ACM5 M5 receptor Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 4 1 1 5.3 C1CCC(C(CC2CCCCN2)C2CCCCC2)CC1 nan
CHEMBL1334033 198453 19 ACM5 M5 receptor Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 4 1 1 5.3 C1CCC(C(CC2CCCCN2)C2CCCCC2)CC1 nan
CHEMBL75880 198453 19 ACM5 M5 receptor Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 277 4 1 1 5.3 C1CCC(C(CC2CCCCN2)C2CCCCC2)CC1 nan
10594386 11133 0 ACM5 M5 receptor Human 5.0 pIC50 = 5.0 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M5 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M5 using membranes from transfected CHO cells
ChEMBL 355 7 0 3 4.9 CCN1CC=C(c2ccccc2)C(C(=O)OCCCC2CCCCC2)C1 10.1021/jm980067l
CHEMBL1180249 11133 0 ACM5 M5 receptor Human 5.0 pIC50 = 5.0 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M5 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M5 using membranes from transfected CHO cells
ChEMBL 355 7 0 3 4.9 CCN1CC=C(c2ccccc2)C(C(=O)OCCCC2CCCCC2)C1 10.1021/jm980067l
CHEMBL118553 11133 0 ACM5 M5 receptor Human 5.0 pIC50 = 5.0 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M5 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M5 using membranes from transfected CHO cells
ChEMBL 355 7 0 3 4.9 CCN1CC=C(c2ccccc2)C(C(=O)OCCCC2CCCCC2)C1 10.1021/jm980067l
24882532 94433 0 ACM5 M5 receptor Rat 6.0 pIC50 = 6.0 Functional
Antagonist activity at rat muscarinic M5 receptor expressed in CHO cells by calcium mobilization assayAntagonist activity at rat muscarinic M5 receptor expressed in CHO cells by calcium mobilization assay
ChEMBL 363 6 1 3 4.4 CCN1CCN(c2ccc(NC(=O)CCC3CCCC3)cc2Cl)CC1 10.1016/j.bmcl.2007.12.051
CHEMBL255523 94433 0 ACM5 M5 receptor Rat 6.0 pIC50 = 6.0 Functional
Antagonist activity at rat muscarinic M5 receptor expressed in CHO cells by calcium mobilization assayAntagonist activity at rat muscarinic M5 receptor expressed in CHO cells by calcium mobilization assay
ChEMBL 363 6 1 3 4.4 CCN1CCN(c2ccc(NC(=O)CCC3CCCC3)cc2Cl)CC1 10.1016/j.bmcl.2007.12.051
118719495 114812 0 ACM5 M5 receptor Human 6.0 pIC50 = 6.0 Functional
Negative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assayNegative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assay
ChEMBL 456 4 0 5 4.0 CC(C)Oc1ccc(C(=O)N2CCN3C(=O)c4ccccc4C23c2ccc3c(c2)OCO3)cc1 10.1016/j.bmcl.2014.11.082
CHEMBL3353283 114812 0 ACM5 M5 receptor Human 6.0 pIC50 = 6.0 Functional
Negative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assayNegative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assay
ChEMBL 456 4 0 5 4.0 CC(C)Oc1ccc(C(=O)N2CCN3C(=O)c4ccccc4C23c2ccc3c(c2)OCO3)cc1 10.1016/j.bmcl.2014.11.082
71598549 103964 0 ACM5 M5 receptor Rat 6.0 pIC50 = 6.0 Functional
Negative allosteric modulation of rat muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assayNegative allosteric modulation of rat muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assay
ChEMBL 424 2 0 2 4.4 O=C(c1ccc(F)c(F)c1)N1CCN2C(=O)c3ccccc3C12c1ccc(Cl)cc1 10.1021/jm4013246
CHEMBL3105213 103964 0 ACM5 M5 receptor Rat 6.0 pIC50 = 6.0 Functional
Negative allosteric modulation of rat muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assayNegative allosteric modulation of rat muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assay
ChEMBL 424 2 0 2 4.4 O=C(c1ccc(F)c(F)c1)N1CCN2C(=O)c3ccccc3C12c1ccc(Cl)cc1 10.1021/jm4013246
941361 101085 42 ACM5 M5 receptor Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 404 6 0 2 5.4 Fc1ccc(C(c2ccc(F)cc2)N2CCN(C/C=C/c3ccccc3)CC2)cc1 nan
CHEMBL30008 101085 42 ACM5 M5 receptor Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 404 6 0 2 5.4 Fc1ccc(C(c2ccc(F)cc2)N2CCN(C/C=C/c3ccccc3)CC2)cc1 nan
CHEMBL539027 101085 42 ACM5 M5 receptor Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 404 6 0 2 5.4 Fc1ccc(C(c2ccc(F)cc2)N2CCN(C/C=C/c3ccccc3)CC2)cc1 nan
CHEMBL552659 101085 42 ACM5 M5 receptor Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 404 6 0 2 5.4 Fc1ccc(C(c2ccc(F)cc2)N2CCN(C/C=C/c3ccccc3)CC2)cc1 nan
71598521 2418 4 ACM5 M5 receptor Human 6.0 pIC50 = 6.0 Functional
Negative allosteric modulation of human M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of human M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 424 2 0 2 4.4 Clc1ccc(cc1)[C@]12N(CCN1C(=O)c1c2cccc1)C(=O)c1ccc(c(c1)F)F 10.1016/j.bmcl.2017.02.020
7631 2418 4 ACM5 M5 receptor Human 6.0 pIC50 = 6.0 Functional
Negative allosteric modulation of human M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of human M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 424 2 0 2 4.4 Clc1ccc(cc1)[C@]12N(CCN1C(=O)c1c2cccc1)C(=O)c1ccc(c(c1)F)F 10.1016/j.bmcl.2017.02.020
CHEMBL3105228 2418 4 ACM5 M5 receptor Human 6.0 pIC50 = 6.0 Functional
Negative allosteric modulation of human M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of human M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 424 2 0 2 4.4 Clc1ccc(cc1)[C@]12N(CCN1C(=O)c1c2cccc1)C(=O)c1ccc(c(c1)F)F 10.1016/j.bmcl.2017.02.020
10547222 114046 0 ACM5 M5 receptor Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M5 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M5 using membranes from transfected CHO cells
ChEMBL 371 12 0 3 5.7 CCCCCCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL333940 114046 0 ACM5 M5 receptor Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M5 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M5 using membranes from transfected CHO cells
ChEMBL 371 12 0 3 5.7 CCCCCCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
10516408 11156 0 ACM5 M5 receptor Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M5 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M5 using membranes from transfected CHO cells
ChEMBL 273 5 0 3 3.0 CCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL1180330 11156 0 ACM5 M5 receptor Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M5 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M5 using membranes from transfected CHO cells
ChEMBL 273 5 0 3 3.0 CCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
CHEMBL122353 11156 0 ACM5 M5 receptor Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M5 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M5 using membranes from transfected CHO cells
ChEMBL 273 5 0 3 3.0 CCCOC(=O)C1CN(CC)CC=C1c1ccccc1 10.1021/jm980067l
137654353 158192 0 ACM5 M5 receptor Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at recombinant human M5 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M5 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 436 4 0 5 4.3 O=C(C1CCN(c2cc(Oc3ccc(F)cc3F)ncn2)CC1)N1Cc2ccccc2C1 10.1016/j.bmcl.2017.04.009
CHEMBL4096589 158192 0 ACM5 M5 receptor Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at recombinant human M5 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assayAntagonist activity at recombinant human M5 receptor expressed in CHO cells co-expressing Gqi5 by calcium mobilization assay
ChEMBL 436 4 0 5 4.3 O=C(C1CCN(c2cc(Oc3ccc(F)cc3F)ncn2)CC1)N1Cc2ccccc2C1 10.1016/j.bmcl.2017.04.009
9905467 11151 0 ACM5 M5 receptor Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M5 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M5 using membranes from transfected CHO cells
ChEMBL 327 5 0 3 4.3 CCN1CCC(c2ccccc2)=C(C(=O)OCC2CCCCC2)C1 10.1021/jm980067l
CHEMBL1180316 11151 0 ACM5 M5 receptor Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M5 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M5 using membranes from transfected CHO cells
ChEMBL 327 5 0 3 4.3 CCN1CCC(c2ccccc2)=C(C(=O)OCC2CCCCC2)C1 10.1021/jm980067l
CHEMBL121520 11151 0 ACM5 M5 receptor Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M5 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M5 using membranes from transfected CHO cells
ChEMBL 327 5 0 3 4.3 CCN1CCC(c2ccccc2)=C(C(=O)OCC2CCCCC2)C1 10.1021/jm980067l
134824563 155237 7 ACM5 M5 receptor Human 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of human M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of human M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 438 2 0 2 4.7 Cc1cc([C@@]23c4ccccc4C(=O)N2CCN3C(=O)c2ccc(F)c(F)c2)ccc1Cl 10.1016/j.bmcl.2017.02.020
CHEMBL4062497 155237 7 ACM5 M5 receptor Human 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of human M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of human M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 438 2 0 2 4.7 Cc1cc([C@@]23c4ccccc4C(=O)N2CCN3C(=O)c2ccc(F)c(F)c2)ccc1Cl 10.1016/j.bmcl.2017.02.020
3055 200881 36 ACM5 M5 receptor Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 6 1 2 4.2 OC(CCCN1CCCCC1)(c1ccccc1)c1ccccc1 nan
CHEMBL1529 200881 36 ACM5 M5 receptor Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 6 1 2 4.2 OC(CCCN1CCCCC1)(c1ccccc1)c1ccccc1 nan
CHEMBL936 200881 36 ACM5 M5 receptor Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 309 6 1 2 4.2 OC(CCCN1CCCCC1)(c1ccccc1)c1ccccc1 nan
2745 3621 32 ACM5 M5 receptor Human 7.9 pIC50 = 7.9 Binding
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 nan
5572 3621 32 ACM5 M5 receptor Human 7.9 pIC50 = 7.9 Binding
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 nan
66007 3621 32 ACM5 M5 receptor Human 7.9 pIC50 = 7.9 Binding
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 nan
7315 3621 32 ACM5 M5 receptor Human 7.9 pIC50 = 7.9 Binding
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 nan
CHEMBL1490 3621 32 ACM5 M5 receptor Human 7.9 pIC50 = 7.9 Binding
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 nan
DB00376 3621 32 ACM5 M5 receptor Human 7.9 pIC50 = 7.9 Binding
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 nan
13457440 196956 0 ACM5 M5 receptor Rat 5.9 pIC50 = 5.9 Binding
Binding affinity towards muscarinic acetylcholine receptor by inhibiting specific binding of [3H]quinuclidinyl benzilate (0.8 nM) in vitro to membranes of rat brain without cerebellumBinding affinity towards muscarinic acetylcholine receptor by inhibiting specific binding of [3H]quinuclidinyl benzilate (0.8 nM) in vitro to membranes of rat brain without cerebellum
ChEMBL 280 3 0 2 3.4 CN(C)CC1c2ccccc2C(c2ccccc2)CN1C 10.1021/jm00374a011
CHEMBL6528 196956 0 ACM5 M5 receptor Rat 5.9 pIC50 = 5.9 Binding
Binding affinity towards muscarinic acetylcholine receptor by inhibiting specific binding of [3H]quinuclidinyl benzilate (0.8 nM) in vitro to membranes of rat brain without cerebellumBinding affinity towards muscarinic acetylcholine receptor by inhibiting specific binding of [3H]quinuclidinyl benzilate (0.8 nM) in vitro to membranes of rat brain without cerebellum
ChEMBL 280 3 0 2 3.4 CN(C)CC1c2ccccc2C(c2ccccc2)CN1C 10.1021/jm00374a011
134824563 155237 7 ACM5 M5 receptor Human 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of human M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of human M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 438 2 0 2 4.7 Cc1cc([C@@]23c4ccccc4C(=O)N2CCN3C(=O)c2ccc(F)c(F)c2)ccc1Cl 10.1016/j.bmcl.2017.02.020
CHEMBL4062497 155237 7 ACM5 M5 receptor Human 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of human M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of human M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 438 2 0 2 4.7 Cc1cc([C@@]23c4ccccc4C(=O)N2CCN3C(=O)c2ccc(F)c(F)c2)ccc1Cl 10.1016/j.bmcl.2017.02.020
118719480 114798 0 ACM5 M5 receptor Human 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assayNegative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assay
ChEMBL 434 3 0 3 4.1 COc1ccc(C23c4ccccc4C(=O)N2CCN3C(=O)c2ccc(F)c(F)c2)cc1C 10.1016/j.bmcl.2014.11.082
CHEMBL3353268 114798 0 ACM5 M5 receptor Human 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assayNegative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assay
ChEMBL 434 3 0 3 4.1 COc1ccc(C23c4ccccc4C(=O)N2CCN3C(=O)c2ccc(F)c(F)c2)cc1C 10.1016/j.bmcl.2014.11.082
656392 182923 1 ACM5 M5 receptor Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]NMS from human cloned muscarinic M5 receptor expressed in insect Sf9 cellsDisplacement of [3H]NMS from human cloned muscarinic M5 receptor expressed in insect Sf9 cells
ChEMBL 255 5 1 4 1.4 CC[C@@H](C)[C@@H](O)C(=O)OC[C@H]1CCN2CCC[C@@H]12 10.1021/np049650x
CHEMBL480464 182923 1 ACM5 M5 receptor Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]NMS from human cloned muscarinic M5 receptor expressed in insect Sf9 cellsDisplacement of [3H]NMS from human cloned muscarinic M5 receptor expressed in insect Sf9 cells
ChEMBL 255 5 1 4 1.4 CC[C@@H](C)[C@@H](O)C(=O)OC[C@H]1CCN2CCC[C@@H]12 10.1021/np049650x
43815 184242 50 ACM5 M5 receptor Human 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 nan
CHEMBL1708 184242 50 ACM5 M5 receptor Human 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 nan
CHEMBL490 184242 50 ACM5 M5 receptor Human 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 nan
10522202 11149 0 ACM5 M5 receptor Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M5 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M5 using membranes from transfected CHO cells
ChEMBL 355 7 0 3 5.1 CCN1CCC(c2ccccc2)=C(C(=O)OCCCC2CCCCC2)C1 10.1021/jm980067l
CHEMBL1180312 11149 0 ACM5 M5 receptor Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M5 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M5 using membranes from transfected CHO cells
ChEMBL 355 7 0 3 5.1 CCN1CCC(c2ccccc2)=C(C(=O)OCCCC2CCCCC2)C1 10.1021/jm980067l
CHEMBL121385 11149 0 ACM5 M5 receptor Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M5 using membranes from transfected CHO cellsDisplacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M5 using membranes from transfected CHO cells
ChEMBL 355 7 0 3 5.1 CCN1CCC(c2ccccc2)=C(C(=O)OCCCC2CCCCC2)C1 10.1021/jm980067l
137658629 158546 0 ACM5 M5 receptor Human 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of human M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of human M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 473 4 0 3 4.8 CN(c1ccc([C@@]23c4ccccc4C(=O)N2CCN3C(=O)c2ccc(F)c(F)c2)cc1)C1CCC1 10.1016/j.bmcl.2017.02.020
CHEMBL4100518 158546 0 ACM5 M5 receptor Human 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of human M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of human M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 473 4 0 3 4.8 CN(c1ccc([C@@]23c4ccccc4C(=O)N2CCN3C(=O)c2ccc(F)c(F)c2)cc1)C1CCC1 10.1016/j.bmcl.2017.02.020
71607117 103965 0 ACM5 M5 receptor Human 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assayNegative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assay
ChEMBL 472 3 0 3 5.3 O=C(c1ccc(SC(F)(F)F)cc1)N1CCN2C(=O)c3ccccc3C12c1ccc(F)cc1 10.1021/jm4013246
CHEMBL3105215 103965 0 ACM5 M5 receptor Human 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assayNegative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assay
ChEMBL 472 3 0 3 5.3 O=C(c1ccc(SC(F)(F)F)cc1)N1CCN2C(=O)c3ccccc3C12c1ccc(F)cc1 10.1021/jm4013246
135398737 904 82 ACM5 M5 receptor Human 7.9 pIC50 = 7.9 Binding
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
38 904 82 ACM5 M5 receptor Human 7.9 pIC50 = 7.9 Binding
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
722 904 82 ACM5 M5 receptor Human 7.9 pIC50 = 7.9 Binding
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
CHEMBL42 904 82 ACM5 M5 receptor Human 7.9 pIC50 = 7.9 Binding
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
DB00363 904 82 ACM5 M5 receptor Human 7.9 pIC50 = 7.9 Binding
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
10468793 197088 0 ACM5 M5 receptor Rat 6.9 pIC50 = 6.9 Binding
Binding affinity towards muscarinic acetylcholine receptor by inhibiting specific binding of [3H]quinuclidinyl benzilate (0.8 nM) in vitro to membranes of rat brain without cerebellumBinding affinity towards muscarinic acetylcholine receptor by inhibiting specific binding of [3H]quinuclidinyl benzilate (0.8 nM) in vitro to membranes of rat brain without cerebellum
ChEMBL 278 1 0 2 3.1 CN1CCN2CC(c3ccccc3)c3ccccc3C2C1 10.1021/jm00374a011
CHEMBL6627 197088 0 ACM5 M5 receptor Rat 6.9 pIC50 = 6.9 Binding
Binding affinity towards muscarinic acetylcholine receptor by inhibiting specific binding of [3H]quinuclidinyl benzilate (0.8 nM) in vitro to membranes of rat brain without cerebellumBinding affinity towards muscarinic acetylcholine receptor by inhibiting specific binding of [3H]quinuclidinyl benzilate (0.8 nM) in vitro to membranes of rat brain without cerebellum
ChEMBL 278 1 0 2 3.1 CN1CCN2CC(c3ccccc3)c3ccccc3C2C1 10.1021/jm00374a011
3156646 7999 9 ACM5 M5 receptor Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human muscarinic M5 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic M5 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 373 5 1 4 3.7 CCN1CCN(c2ccc(NC(=O)c3ccccc3OC)cc2Cl)CC1 10.1016/j.bmcl.2010.02.041
CHEMBL1092460 7999 9 ACM5 M5 receptor Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human muscarinic M5 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine-induced calcium mobilizationAntagonist activity at human muscarinic M5 receptor expressed in CHO-K1 cells assessed as inhibition of acetylcholine-induced calcium mobilization
ChEMBL 373 5 1 4 3.7 CCN1CCN(c2ccc(NC(=O)c3ccccc3OC)cc2Cl)CC1 10.1016/j.bmcl.2010.02.041
13457895 197260 0 ACM5 M5 receptor Rat 5.9 pIC50 = 5.9 Binding
Binding affinity towards muscarinic acetylcholine receptor by inhibiting specific binding of [3H]quinuclidinyl benzilate (0.8 nM) in vitro to membranes of rat brain without cerebellumBinding affinity towards muscarinic acetylcholine receptor by inhibiting specific binding of [3H]quinuclidinyl benzilate (0.8 nM) in vitro to membranes of rat brain without cerebellum
ChEMBL 292 2 0 2 3.5 CCN1CCN2CC(c3ccccc3)c3ccccc3C2C1 10.1021/jm00374a011
CHEMBL6747 197260 0 ACM5 M5 receptor Rat 5.9 pIC50 = 5.9 Binding
Binding affinity towards muscarinic acetylcholine receptor by inhibiting specific binding of [3H]quinuclidinyl benzilate (0.8 nM) in vitro to membranes of rat brain without cerebellumBinding affinity towards muscarinic acetylcholine receptor by inhibiting specific binding of [3H]quinuclidinyl benzilate (0.8 nM) in vitro to membranes of rat brain without cerebellum
ChEMBL 292 2 0 2 3.5 CCN1CCN2CC(c3ccccc3)c3ccccc3C2C1 10.1021/jm00374a011
71607117 103965 0 ACM5 M5 receptor Human 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assayNegative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assay
ChEMBL 472 3 0 3 5.3 O=C(c1ccc(SC(F)(F)F)cc1)N1CCN2C(=O)c3ccccc3C12c1ccc(F)cc1 10.1021/jm4013246
CHEMBL3105215 103965 0 ACM5 M5 receptor Human 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assayNegative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assay
ChEMBL 472 3 0 3 5.3 O=C(c1ccc(SC(F)(F)F)cc1)N1CCN2C(=O)c3ccccc3C12c1ccc(F)cc1 10.1021/jm4013246
118719477 114795 0 ACM5 M5 receptor Human 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assayNegative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assay
ChEMBL 434 2 0 4 3.5 O=C(c1ccc(F)c(F)c1)N1CCN2C(=O)c3ccccc3C12c1ccc2c(c1)OCO2 10.1016/j.bmcl.2014.11.082
CHEMBL3353265 114795 0 ACM5 M5 receptor Human 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assayNegative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assay
ChEMBL 434 2 0 4 3.5 O=C(c1ccc(F)c(F)c1)N1CCN2C(=O)c3ccccc3C12c1ccc2c(c1)OCO2 10.1016/j.bmcl.2014.11.082
118719483 114802 0 ACM5 M5 receptor Human 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assayNegative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assay
ChEMBL 434 3 0 3 4.1 COc1cc(C23c4ccccc4C(=O)N2CCN3C(=O)c2ccc(F)c(F)c2)ccc1C 10.1016/j.bmcl.2014.11.082
CHEMBL3353271 114802 0 ACM5 M5 receptor Human 5.9 pIC50 = 5.9 Functio