Purchasability


Ligand source activities (1 row/activity)

Select all ChEMBL ID Receptor Species Purchasable p-value
(-log)		 Activity
Type		 Activity
Relation		 Activity
Value		 Unit Assay Type Assay Description Mol
weight		 Rot
Bonds		 H don H acc LogP Smiles
CHEMBL2381694 acm5_rat Rat No 9.7 EC50 = 0.2 nM Bind
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
351 5 0 4 3.2 O=C1C(=O)N(CCOc2ccccc2)c2ccc(OC(F)(F)F)cc21
CHEMBL2381694 acm5_rat Rat No 9.7 EC50 = 0.2 nM Bind
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
351 5 0 4 3.2 O=C1C(=O)N(CCOc2ccccc2)c2ccc(OC(F)(F)F)cc21
CHEMBL466253 acm5_rat Rat Yes 9.6 EC50 = 0.3 nM Bind
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
351 4 0 4 3.3 COc1ccc(cc1)CN1c2ccc(cc2C(=O)C1=O)OC(F)(F)F
CHEMBL466253 acm5_rat Rat Yes 9.6 EC50 = 0.3 nM Bind
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
351 4 0 4 3.3 COc1ccc(cc1)CN1c2ccc(cc2C(=O)C1=O)OC(F)(F)F
CHEMBL667 acm5_human Human Yes 8.9 EC50 = 1.2 nM Funct
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
146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C
CHEMBL667 acm5_human Human Yes 8.9 EC50 = 1.2 nM Funct
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
146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C
CHEMBL965 acm5_human Human Yes 6.0 EC50 = 1000 nM Funct
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
147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C
CHEMBL2022960 acm5_human Human Yes 6.0 EC50 = 1000 nM Funct
Agonist activity at human muscarinic M5 receptor by calcium mobilization assayAgonist activity at human muscarinic M5 receptor by calcium mobilization assay
348 7 0 3 3.8 CCCCC1CCN(CC1)CCCN1C(=O)COc2c1ccc(c2)F
CHEMBL1223807 acm5_human Human No 6.0 EC50 = 1000 nM Funct
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
358 4 0 5 4.0 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccccc43)CC2)CC1
CHEMBL1223941 acm5_human Human No 6.0 EC50 = 1000 nM Funct
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
413 6 0 7 3.5 COCCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(C#N)cc43)CC2)CC1
CHEMBL1602658 acm5_human Human Yes 5.0 EC50 = 10000 nM Funct
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
444 6 0 5 2.9 CCN(Cc1ccccc1)C(=O)C1CCN(S(=O)(=O)c2ccc3c(c2)OCCO3)CC1
CHEMBL2381695 acm5_human Human No 6.0 EC50 = 1047.1 nM Bind
Positive allosteric modulation of human muscarinic M5 receptorPositive allosteric modulation of human muscarinic M5 receptor
443 7 0 5 5.0 O=C1C(=O)N(CCOc2ccc(Oc3ccccc3)cc2)c2ccc(OC(F)(F)F)cc21
CHEMBL2381695 acm5_human Human No 6.0 EC50 = 1050 nM Bind
Positive allosteric modulation of human muscarinic M5 receptorPositive allosteric modulation of human muscarinic M5 receptor
443 7 0 5 5.0 O=C1C(=O)N(CCOc2ccc(Oc3ccccc3)cc2)c2ccc(OC(F)(F)F)cc21
CHEMBL305264 acm5_human Human Yes 7.0 EC50 = 110 nM Bind
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)
196 2 1 4 1.5 CC(C)Oc1noc2c1CNCCC2
CHEMBL466253 acm5_human Human Yes 6.0 EC50 = 1100 nM Funct
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
351 4 0 4 3.3 COc1ccc(cc1)CN1c2ccc(cc2C(=O)C1=O)OC(F)(F)F
CHEMBL466253 acm5_human Human Yes 6.0 EC50 = 1100 nM Bind
Positive allosteric modulation of human muscarinic M5 receptorPositive allosteric modulation of human muscarinic M5 receptor
351 4 0 4 3.3 COc1ccc(cc1)CN1c2ccc(cc2C(=O)C1=O)OC(F)(F)F
CHEMBL3329738 acm5_human Human No 6.0 EC50 = 1110 nM Funct
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
442 6 0 4 3.6 CCN(C(=O)C1CCN(S(=O)(=O)c2ccc3c(c2)CCO3)CC1)[C@H](C)c1ccccc1
CHEMBL3329738 acm5_human Human No 6.0 EC50 = 1122.0 nM Funct
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
442 6 0 4 3.6 CCN(C(=O)C1CCN(S(=O)(=O)c2ccc3c(c2)CCO3)CC1)[C@H](C)c1ccccc1
CHEMBL466253 acm5_human Human Yes 5.9 EC50 = 1160 nM Funct
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
351 4 0 4 3.3 COc1ccc(cc1)CN1c2ccc(cc2C(=O)C1=O)OC(F)(F)F
CHEMBL1223754 acm5_human Human No 7.9 EC50 = 12.6 nM Funct
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
403 5 1 4 4.5 CCCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)[nH]c4cc(F)c(C)cc43)CC2)CC1
CHEMBL3329764 acm5_human Human No 6.9 EC50 = 120 nM Funct
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
536 6 1 4 5.1 CC(C)(C)CN(Cc1ccccc1C(F)(F)F)C(=O)C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1
CHEMBL3329765 acm5_human Human No 6.9 EC50 = 120 nM Funct
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
520 7 1 4 4.4 O=C(C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1)N(Cc1ccccc1C(F)(F)F)CC1CC1
CHEMBL3329765 acm5_human Human No 6.9 EC50 = 120.2 nM Funct
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
520 7 1 4 4.4 O=C(C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1)N(Cc1ccccc1C(F)(F)F)CC1CC1
CHEMBL1242979 acm5_human Human No 5.9 EC50 = 1200 nM Funct
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
501 9 1 5 3.5 COc1ccc(CC(=O)NC2CCN(CCCN3C(=O)CCc4cc(F)c(F)cc43)CC2)cc1OC
CHEMBL466253 acm5_human Human Yes 5.9 EC50 = 1200 nM Bind
Positive allosteric modulation activity at muscarinic M5 receptorPositive allosteric modulation activity at muscarinic M5 receptor
351 4 0 4 3.3 COc1ccc(cc1)CN1c2ccc(cc2C(=O)C1=O)OC(F)(F)F
CHEMBL134641 acm5_human Human Yes 6.9 EC50 = 123 nM Funct
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
193 2 0 4 0.9 CO/N=C(/[C@H]1CN2CCC1CC2)\C#N
CHEMBL3329764 acm5_human Human No 6.9 EC50 = 123.0 nM Funct
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
536 6 1 4 5.1 CC(C)(C)CN(Cc1ccccc1C(F)(F)F)C(=O)C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1
CHEMBL1223805 acm5_human Human No 6.9 EC50 = 125.9 nM Funct
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
356 3 0 3 3.7 CO[C@H]1CC[C@](C)(N2CCC(N3C(=O)Cc4ccc(C)cc43)CC2)CC1
CHEMBL1223864 acm5_human Human No 5.9 EC50 = 1258.9 nM Funct
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
436 5 0 7 3.4 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(S(C)(=O)=O)cc43)CC2)CC1
CHEMBL2146599 acm5_human Human Yes 5.9 EC50 = 1258.9 nM Funct
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
315 2 1 4 2.5 Cc1ccc2[nH]c(=O)n(C3CCN(C4CCOCC4)CC3)c2c1
CHEMBL1196131 acm5_human Human No 5.9 EC50 = 1258.9 nM Bind
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
415 14 0 10 1.2 CC(=O)OCCOCCOCCOCCOc1nsnc1C1=CCCN(C)C1
CHEMBL555992 acm5_human Human No 5.9 EC50 = 1258.9 nM Bind
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
415 14 0 10 1.2 CC(=O)OCCOCCOCCOCCOc1nsnc1C1=CCCN(C)C1
CHEMBL3329762 acm5_human Human No 5.9 EC50 = 1258.9 nM Funct
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
512 7 1 4 4.0 O=C(C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1)N(CCF)Cc1ccccc1C(F)(F)F
CHEMBL21536 acm5_human Human Yes 4.9 EC50 = 12589.3 nM Funct
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
281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C
CHEMBL3329766 acm5_human Human No 6.9 EC50 = 128.8 nM Funct
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
534 7 1 4 4.8 O=C(C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1)N(Cc1ccccc1C(F)(F)F)CC1CCC1
CHEMBL3329766 acm5_human Human No 6.9 EC50 = 130 nM Funct
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
534 7 1 4 4.8 O=C(C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1)N(Cc1ccccc1C(F)(F)F)CC1CCC1
CHEMBL1255785 acm5_human Human Yes 5.9 EC50 = 1300 nM Bind
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
174 2 1 2 0.2 C[C@@H]1O[C@H](C[N+](C)(C)C)C[C@H]1O
CHEMBL12587 acm5_human Human Yes 5.9 EC50 = 1300 nM Bind
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
174 2 1 2 0.2 C[C@@H]1O[C@H](C[N+](C)(C)C)C[C@H]1O
CHEMBL292911 acm5_human Human Yes 5.9 EC50 = 1300 nM Bind
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
174 2 1 2 0.2 C[C@@H]1O[C@H](C[N+](C)(C)C)C[C@H]1O
CHEMBL4212760 acm5_human Human No 5.9 EC50 = 1300 nM Funct
Positive allosteric modulation of M5 receptor (unknown origin)Positive allosteric modulation of M5 receptor (unknown origin)
346 2 1 2 5.1 CC(C)[C@@H]1N=C(c2ccccc2F)c2cc(Cl)ccc2NC1=S
CHEMBL3329762 acm5_human Human No 5.9 EC50 = 1300 nM Funct
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
512 7 1 4 4.0 O=C(C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1)N(CCF)Cc1ccccc1C(F)(F)F
CHEMBL21536 acm5_human Human Yes 6.9 EC50 = 140 nM Funct
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
281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C
CHEMBL2381692 acm5_human Human No 5.9 EC50 = 1400 nM Bind
Positive allosteric modulation of human muscarinic M5 receptorPositive allosteric modulation of human muscarinic M5 receptor
412 6 1 6 2.6 COc1ccc(CN2C(=O)C(O)(C[N+](=O)[O-])c3cc(OC(F)(F)F)ccc32)cc1
CHEMBL21536 acm5_human Human Yes 6.9 EC50 = 142 nM Funct
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
281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C
CHEMBL3329763 acm5_human Human No 6.8 EC50 = 150 nM Funct
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
522 7 1 4 4.8 CCC(C)N(Cc1ccccc1C(F)(F)F)C(=O)C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1
CHEMBL1257975 acm5_human Human No 5.8 EC50 = 1500 nM Bind
Positive allosteric modulation of human muscarinic M5 receptorPositive allosteric modulation of human muscarinic M5 receptor
432 5 0 5 4.6 O=C1C(=O)N(Cc2ccc(Oc3cccc(F)n3)cc2)c2ccc(OC(F)(F)F)cc21
CHEMBL1257975 acm5_human Human No 5.8 EC50 = 1500 nM Funct
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
432 5 0 5 4.6 O=C1C(=O)N(Cc2ccc(Oc3cccc(F)n3)cc2)c2ccc(OC(F)(F)F)cc21
CHEMBL3329743 acm5_human Human No 5.8 EC50 = 1500 nM Funct
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
444 6 1 4 3.2 CCN(Cc1cccc(F)c1)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1
CHEMBL3329763 acm5_human Human No 6.8 EC50 = 151.4 nM Funct
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
522 7 1 4 4.8 CCC(C)N(Cc1ccccc1C(F)(F)F)C(=O)C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1
CHEMBL3329743 acm5_human Human No 5.8 EC50 = 1513.6 nM Funct
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
444 6 1 4 3.2 CCN(Cc1cccc(F)c1)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1
CHEMBL3329756 acm5_human Human No 6.8 EC50 = 154.9 nM Funct
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
508 7 1 4 4.4 CCCN(Cc1ccccc1C(F)(F)F)C(=O)C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1
CHEMBL3329730 acm5_human Human No 5.8 EC50 = 1548.8 nM Funct
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
426 6 1 4 3.0 CCN(Cc1ccccc1)C(=O)C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1
CHEMBL1223861 acm5_human Human No 6.8 EC50 = 158.5 nM Funct
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
390 4 0 5 4.4 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4c(F)cc(C)cc43)CC2)CC1
CHEMBL1223862 acm5_human Human No 6.8 EC50 = 158.5 nM Funct
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
388 5 0 6 4.0 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(OC)cc43)CC2)CC1
CHEMBL1223940 acm5_human Human No 6.8 EC50 = 158.5 nM Funct
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
402 6 0 6 3.9 COCCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(C)cc43)CC2)CC1
CHEMBL1802360 acm5_human Human Yes 5.8 EC50 = 1584.9 nM Funct
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
369 6 1 4 3.6 O=c1[nH]c2ccccc2n1C1CCN(CCCOc2ccc(F)cc2)CC1
CHEMBL3329756 acm5_human Human No 6.8 EC50 = 160 nM Funct
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
508 7 1 4 4.4 CCCN(Cc1ccccc1C(F)(F)F)C(=O)C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1
CHEMBL1257388 acm5_human Human No 5.8 EC50 = 1600 nM Funct
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
398 4 0 4 4.4 O=C1C(=O)N(Cc2ccc(-c3cccnc3)cc2)c2ccc(OC(F)(F)F)cc21
CHEMBL593506 acm5_human Human Yes 5.8 EC50 = 1600 nM Funct
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
397 4 0 3 5.0 O=C1C(=O)N(Cc2ccc(-c3ccccc3)cc2)c2ccc(OC(F)(F)F)cc21
CHEMBL3329730 acm5_human Human No 5.8 EC50 = 1600 nM Funct
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
426 6 1 4 3.0 CCN(Cc1ccccc1)C(=O)C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1
CHEMBL3329745 acm5_human Human No 5.8 EC50 = 1600 nM Funct
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
460 6 1 4 3.7 CCN(Cc1cccc(Cl)c1)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1
CHEMBL3329745 acm5_human Human No 5.8 EC50 = 1621.8 nM Funct
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
460 6 1 4 3.7 CCN(Cc1cccc(Cl)c1)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1
CHEMBL3329731 acm5_human Human No 5.8 EC50 = 1698.2 nM Funct
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
426 6 1 4 3.0 CCN(Cc1ccccc1)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1
CHEMBL845 acm5_human Human Yes 6.8 EC50 = 170 nM Funct
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
312 0 2 4 3.4 C1CN(CCN1)C2=NC3=C(C=CC(=C3)Cl)NC4=CC=CC=C42
CHEMBL469144 acm5_human Human No 5.8 EC50 = 1700 nM Funct
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
351 4 0 4 3.3 COc1cccc(CN2C(=O)C(=O)c3cc(OC(F)(F)F)ccc32)c1
CHEMBL3329731 acm5_human Human No 5.8 EC50 = 1700 nM Funct
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
426 6 1 4 3.0 CCN(Cc1ccccc1)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1
CHEMBL3329757 acm5_human Human No 5.8 EC50 = 1800 nM Funct
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
506 7 1 4 4.2 C=CCN(Cc1ccccc1C(F)(F)F)C(=O)C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1
CHEMBL3329760 acm5_human Human No 5.8 EC50 = 1800 nM Funct
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
520 6 1 4 4.6 O=C(C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1)N(Cc1ccccc1C(F)(F)F)C1CCC1
CHEMBL3329757 acm5_human Human No 5.7 EC50 = 1819.7 nM Funct
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
506 7 1 4 4.2 C=CCN(Cc1ccccc1C(F)(F)F)C(=O)C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1
CHEMBL3329760 acm5_human Human No 5.7 EC50 = 1819.7 nM Funct
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
520 6 1 4 4.6 O=C(C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1)N(Cc1ccccc1C(F)(F)F)C1CCC1
CHEMBL447265 acm5_human Human No 5.7 EC50 = 1850 nM Funct
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
389 3 0 3 4.3 O=C1C(=O)N(Cc2ccc(C(F)(F)F)cc2)c2ccc(OC(F)(F)F)cc21
CHEMBL494190 acm5_human Human No 5.7 EC50 = 1860 nM Funct
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
405 4 0 4 4.2 O=C1C(=O)N(Cc2ccc(OC(F)(F)F)cc2)c2ccc(OC(F)(F)F)cc21
CHEMBL667 acm5_human Human Yes 7.7 EC50 = 19.1 nM Funct
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
146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C
CHEMBL1223803 acm5_human Human No 7.7 EC50 = 20.0 nM Funct
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
384 5 0 3 4.5 CCCO[C@H]1CC[C@](C)(N2CCC(N3C(=O)Cc4ccc(C)cc43)CC2)CC1
CHEMBL1223804 acm5_human Human No 7.7 EC50 = 20.0 nM Funct
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
370 4 0 3 4.1 CCO[C@H]1CC[C@](C)(N2CCC(N3C(=O)Cc4ccc(C)cc43)CC2)CC1
CHEMBL3329755 acm5_human Human Yes 6.7 EC50 = 190 nM Bind
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
494 6 1 4 4.0 CCN(C(=O)C1CCN(CC1)S(=O)(=O)c1ccc2c(c1)cn[nH]2)Cc1ccccc1C(F)(F)F
CHEMBL3329755 acm5_human Human Yes 6.7 EC50 = 190 nM Funct
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
494 6 1 4 4.0 CCN(C(=O)C1CCN(CC1)S(=O)(=O)c1ccc2c(c1)cn[nH]2)Cc1ccccc1C(F)(F)F
CHEMBL604482 acm5_human Human No 5.7 EC50 = 1900 nM Funct
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
413 5 0 4 5.1 O=C1C(=O)N(Cc2ccc(Oc3ccccc3)cc2)c2ccc(OC(F)(F)F)cc21
CHEMBL604482 acm5_human Human No 5.7 EC50 = 1900 nM Bind
Positive allosteric modulation activity at muscarinic M5 receptorPositive allosteric modulation activity at muscarinic M5 receptor
413 5 0 4 5.1 O=C1C(=O)N(Cc2ccc(Oc3ccccc3)cc2)c2ccc(OC(F)(F)F)cc21
CHEMBL604482 acm5_human Human No 5.7 EC50 = 1900 nM Bind
Positive allosteric modulation of human muscarinic M5 receptorPositive allosteric modulation of human muscarinic M5 receptor
413 5 0 4 5.1 O=C1C(=O)N(Cc2ccc(Oc3ccccc3)cc2)c2ccc(OC(F)(F)F)cc21
CHEMBL468925 acm5_human Human Yes 5.7 EC50 = 1930 nM Funct
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
333 2 0 2 3.3 O=C1C(=O)N(Cc2ccc(Br)cc2)c2c(F)cccc21
CHEMBL3329755 acm5_human Human Yes 6.7 EC50 = 195.0 nM Funct
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
494 6 1 4 4.0 CCN(C(=O)C1CCN(CC1)S(=O)(=O)c1ccc2c(c1)cn[nH]2)Cc1ccccc1C(F)(F)F
CHEMBL503735 acm5_human Human Yes 5.7 EC50 = 2100 nM Funct
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
339 2 0 2 4.1 O=C1C(=O)N(Cc2ccc(C(F)(F)F)cc2)c2c(Cl)cccc21
CHEMBL69305 acm5_human Human Yes 5.7 EC50 = 2100 nM Bind
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)
182 2 1 4 1.1 CCOc1noc2c1CNCCC2
CHEMBL1257498 acm5_human Human No 5.7 EC50 = 2100 nM Funct
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
399 4 0 5 3.8 O=C1C(=O)N(Cc2ccc(-c3cncnc3)cc2)c2ccc(OC(F)(F)F)cc21
CHEMBL3329744 acm5_human Human No 5.7 EC50 = 2100 nM Funct
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
444 6 1 4 3.2 CCN(Cc1ccccc1F)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1
CHEMBL503735 acm5_human Human Yes 5.7 EC50 = 2110 nM Funct
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
339 2 0 2 4.1 O=C1C(=O)N(Cc2ccc(C(F)(F)F)cc2)c2c(Cl)cccc21
CHEMBL3329744 acm5_human Human No 5.7 EC50 = 2138.0 nM Funct
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
444 6 1 4 3.2 CCN(Cc1ccccc1F)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1
CHEMBL2381693 acm5_human Human No 5.7 EC50 = 2200 nM Bind
Positive allosteric modulation of human muscarinic M5 receptorPositive allosteric modulation of human muscarinic M5 receptor
448 5 1 5 3.9 COc1ccc(CN2C(=O)C(O)(c3ccc(F)nc3)c3cc(OC(F)(F)F)ccc32)cc1
CHEMBL1258090 acm5_human Human No 5.7 EC50 = 2200 nM Funct
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
444 6 0 6 4.5 COc1cccc(Oc2ccc(CN3C(=O)C(=O)c4cc(OC(F)(F)F)ccc43)cc2)n1
CHEMBL44674 acm5_human Human Yes 5.6 EC50 = 2300 nM Bind
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
195 2 0 1 0.3 O=C1CCCN1CC#CC[N+](C)(C)C
CHEMBL3329729 acm5_human Human No 5.6 EC50 = 2344.2 nM Funct
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
426 6 0 4 3.9 CCN(Cc1ccccc1)C(=O)C1CCN(S(=O)(=O)c2ccc3occc3c2)CC1
CHEMBL1257499 acm5_human Human No 5.6 EC50 = 2400 nM Funct
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
356 3 0 4 3.4 O=C1C(=O)N(Cc2ccc(Cl)nc2)c2ccc(OC(F)(F)F)cc21
CHEMBL3329729 acm5_human Human No 5.6 EC50 = 2400 nM Funct
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
426 6 0 4 3.9 CCN(Cc1ccccc1)C(=O)C1CCN(S(=O)(=O)c2ccc3occc3c2)CC1
CHEMBL1624037 acm5_human Human No 4.6 EC50 = 24070 nM Funct
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)]
333 6 2 4 1.9 CCOC(=O)N1CCC(CC1)NCCNC(=O)C2=CC=CC=C2C
CHEMBL21536 acm5_human Human Yes 5.6 EC50 = 2511.9 nM Bind
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
281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C
CHEMBL371811 acm5_human Human Yes 5.6 EC50 = 2600 nM Bind
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
244 3 0 2 3.4 Fc1cccc(c1)/C=N/N=C/c1cccc(c1)F
CHEMBL3329746 acm5_human Human No 5.6 EC50 = 2600 nM Funct
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
456 7 1 5 3.0 CCN(Cc1cccc(OC)c1)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1
CHEMBL3329746 acm5_human Human No 5.6 EC50 = 2630.3 nM Funct
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
456 7 1 5 3.0 CCN(Cc1cccc(OC)c1)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1
CHEMBL593506 acm5_human Human Yes 5.6 EC50 = 2700 nM Funct
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
397 4 0 3 5.0 O=C1C(=O)N(Cc2ccc(-c3ccccc3)cc2)c2ccc(OC(F)(F)F)cc21
CHEMBL595628 acm5_human Human No 5.6 EC50 = 2700 nM Funct
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
397 4 0 3 5.0 O=C1C(=O)N(Cc2ccc(-c3ccccc3)cc2)c2cc(OC(F)(F)F)ccc21
CHEMBL965 acm5_human Human Yes 5.6 EC50 = 2800 nM Bind
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
147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C
CHEMBL603445 acm5_human Human No 5.6 EC50 = 2800 nM Funct
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
403 4 0 4 5.0 O=C1C(=O)N(Cc2ccc(-c3ccsc3)cc2)c2ccc(OC(F)(F)F)cc21
CHEMBL3084447 acm5_human Human No 5.6 EC50 = 2800 nM Funct
Agonist activity at human muscarinic M5 receptor by calcium mobilization assayAgonist activity at human muscarinic M5 receptor by calcium mobilization assay
345 6 2 4 1.9 CCOC(=O)N1C[C@@H]2CC[C@H](C1)[C@@H]2NCCNC(=O)c1ccccc1
CHEMBL1257389 acm5_human Human No 5.6 EC50 = 2800 nM Funct
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
398 4 0 4 4.4 O=C1C(=O)N(Cc2ccc(-c3ccncc3)cc2)c2ccc(OC(F)(F)F)cc21
CHEMBL1258091 acm5_human Human No 5.6 EC50 = 2800 nM Funct
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
420 5 0 6 4.6 O=C1C(=O)N(Cc2ccc(Oc3nccs3)cc2)c2ccc(OC(F)(F)F)cc21
CHEMBL3329732 acm5_human Human No 5.5 EC50 = 2951.2 nM Funct
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
444 6 0 6 3.1 CCN(Cc1ccccc1)C(=O)C1CCN(S(=O)(=O)c2ccc3nsnc3c2)CC1
CHEMBL3334989 acm5_human Human Yes 5.5 EC50 = 3000 nM Bind
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
268 5 0 4 3.2 COc1cccc(/C=N/N=C/c2cccc(OC)c2)c1
CHEMBL3329732 acm5_human Human No 5.5 EC50 = 3000 nM Funct
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
444 6 0 6 3.1 CCN(Cc1ccccc1)C(=O)C1CCN(S(=O)(=O)c2ccc3nsnc3c2)CC1
CHEMBL3329717 acm5_human Human No 5.5 EC50 = 3090.3 nM Funct
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
416 7 0 4 3.1 CCN(Cc1ccccc1)C(=O)C1CCN(S(=O)(=O)c2cccc(OC)c2)CC1
CHEMBL1257619 acm5_human Human No 5.5 EC50 = 3100 nM Funct
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
398 4 0 4 4.4 O=C1C(=O)N(Cc2ccc(-c3ccccc3)cn2)c2ccc(OC(F)(F)F)cc21
CHEMBL3329717 acm5_human Human No 5.5 EC50 = 3100 nM Funct
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
416 7 0 4 3.1 CCN(Cc1ccccc1)C(=O)C1CCN(S(=O)(=O)c2cccc(OC)c2)CC1
CHEMBL1223939 acm5_human Human No 6.5 EC50 = 316.2 nM Funct
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
450 6 0 7 3.8 CCCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(S(C)(=O)=O)cc43)CC2)CC1
CHEMBL511206 acm5_human Human Yes 5.5 EC50 = 3190 nM Funct
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
305 2 0 2 3.4 O=C1C(=O)N(Cc2ccc(C(F)(F)F)cc2)c2ccccc21
CHEMBL1257151 acm5_human Human No 5.5 EC50 = 3200 nM Funct
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
365 3 0 5 3.0 O=C1C(=O)N(Cc2ccc3c(c2)OCO3)c2ccc(OC(F)(F)F)cc21
CHEMBL1257974 acm5_human Human No 5.5 EC50 = 3200 nM Funct
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
414 5 0 5 4.5 O=C1C(=O)N(Cc2ccc(Oc3ccccn3)cc2)c2ccc(OC(F)(F)F)cc21
CHEMBL468290 acm5_human Human No 5.5 EC50 = 3260 nM Funct
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
323 2 0 2 3.6 O=C1C(=O)N(Cc2ccc(C(F)(F)F)cc2)c2c(F)cccc21
CHEMBL506043 acm5_human Human No 5.5 EC50 = 3280 nM Funct
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
335 3 0 3 3.6 Cc1ccccc1CN1C(=O)C(=O)c2cc(OC(F)(F)F)ccc21
CHEMBL3334991 acm5_human Human No 7.5 EC50 = 33 nM Bind
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
310 2 2 3 1.9 O=C(N[C@H]1C[C@@H](O)C1)c1ccc(C#Cc2cccc(F)c2)cn1
CHEMBL596510 acm5_human Human No 5.5 EC50 = 3300 nM Funct
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
401 4 0 5 3.7 Cn1cc(-c2ccc(CN3C(=O)C(=O)c4cc(OC(F)(F)F)ccc43)cc2)cn1
CHEMBL3329716 acm5_human Human No 5.5 EC50 = 3300 nM Funct
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
416 7 0 4 3.1 CCN(Cc1ccccc1)C(=O)C1CCN(S(=O)(=O)c2ccc(OC)cc2)CC1
CHEMBL3329716 acm5_human Human No 5.5 EC50 = 3311.3 nM Funct
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
416 7 0 4 3.1 CCN(Cc1ccccc1)C(=O)C1CCN(S(=O)(=O)c2ccc(OC)cc2)CC1
CHEMBL485913 acm5_human Human No 7.5 EC50 = 34.3 nM Funct
Agonist activity at muscarinic M5 receptorAgonist activity at muscarinic M5 receptor
387 5 2 6 1.5 NC(=O)OCCN1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1
CHEMBL491209 acm5_human Human Yes 7.5 EC50 = 34.3 nM Funct
Agonist activity at muscarinic M5 receptorAgonist activity at muscarinic M5 receptor
372 3 1 5 2.6 CCOC(=O)N1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1
CHEMBL3329754 acm5_human Human No 6.5 EC50 = 346.7 nM Funct
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
460 6 1 4 3.7 CCN(Cc1ccccc1Cl)C(=O)C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1
CHEMBL3329754 acm5_human Human No 6.5 EC50 = 350 nM Funct
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
460 6 1 4 3.7 CCN(Cc1ccccc1Cl)C(=O)C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1
CHEMBL965 acm5_human Human Yes 6.4 EC50 = 360 nM Bind
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)
147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C
CHEMBL596509 acm5_human Human No 5.4 EC50 = 3600 nM Funct
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
416 4 0 4 4.5 O=C1C(=O)N(Cc2ccc(-c3ccc(F)nc3)cc2)c2ccc(OC(F)(F)F)cc21
CHEMBL2024331 acm5_human Human No 5.4 EC50 = 3700 nM Funct
Agonist activity at human muscarinic M5 receptor by calcium mobilization assayAgonist activity at human muscarinic M5 receptor by calcium mobilization assay
399 4 1 4 3.3 CCOC(=O)N1C2CCC1CC(N1CCC[C@@H](NC(=O)c3ccccc3C)C1)C2
CHEMBL1257741 acm5_human Human No 5.4 EC50 = 3800 nM Funct
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
398 4 0 4 4.4 O=C1C(=O)N(Cc2ccc(-c3ccccc3)nc2)c2ccc(OC(F)(F)F)cc21
CHEMBL595403 acm5_human Human No 5.4 EC50 = 3900 nM Funct
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
427 5 0 4 5.0 COc1ccccc1-c1ccc(CN2C(=O)C(=O)c3cc(OC(F)(F)F)ccc32)cc1
CHEMBL511254 acm5_human Human Yes 5.4 EC50 = 3960 nM Funct
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
301 3 0 3 3.1 COc1ccc(CN2C(=O)C(=O)c3cccc(Cl)c32)cc1
CHEMBL1223806 acm5_human Human No 6.4 EC50 = 398.1 nM Funct
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
358 3 0 5 3.9 CO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(C)cc43)CC2)CC1
CHEMBL1223863 acm5_human Human No 6.4 EC50 = 398.1 nM Funct
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
383 4 0 6 3.8 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(C#N)cc43)CC2)CC1
CHEMBL466253 acm5_rat Rat Yes 8.3 EC50 = 4.6 nM Bind
Positive allosteric modulation of rat muscarinic M5 receptorPositive allosteric modulation of rat muscarinic M5 receptor
351 4 0 4 3.3 COc1ccc(cc1)CN1c2ccc(cc2C(=O)C1=O)OC(F)(F)F
CHEMBL2381694 acm5_rat Rat No 8.3 EC50 = 4.6 nM Bind
Positive allosteric modulation of rat muscarinic M5 receptorPositive allosteric modulation of rat muscarinic M5 receptor
351 5 0 4 3.2 O=C1C(=O)N(CCOc2ccccc2)c2ccc(OC(F)(F)F)cc21
CHEMBL466253 acm5_rat Rat Yes 8.3 EC50 = 4.6 nM Bind
Positive allosteric modulation of rat muscarinic M5 receptorPositive allosteric modulation of rat muscarinic M5 receptor
351 4 0 4 3.3 COc1ccc(cc1)CN1c2ccc(cc2C(=O)C1=O)OC(F)(F)F
CHEMBL2381694 acm5_rat Rat No 8.3 EC50 = 4.6 nM Bind
Positive allosteric modulation of rat muscarinic M5 receptorPositive allosteric modulation of rat muscarinic M5 receptor
351 5 0 4 3.2 O=C1C(=O)N(CCOc2ccccc2)c2ccc(OC(F)(F)F)cc21
CHEMBL2431187 acm5_human Human No 6.4 EC50 = 400 nM Bind
Allosteric agonist activity at human muscarinic acetylcholine receptor M5Allosteric agonist activity at human muscarinic acetylcholine receptor M5
310 2 2 3 1.9 O=C(N[C@H]1C[C@H](O)C1)c1ccc(C#Cc2cccc(F)c2)cn1
CHEMBL1257862 acm5_human Human No 5.4 EC50 = 4000 nM Funct
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
399 4 0 5 3.8 O=C1C(=O)N(Cc2ccc(-c3cccnc3)nc2)c2ccc(OC(F)(F)F)cc21
CHEMBL2381694 acm5_human Human No 6.4 EC50 = 407.4 nM Bind
Positive allosteric modulation of human muscarinic M5 receptorPositive allosteric modulation of human muscarinic M5 receptor
351 5 0 4 3.2 O=C1C(=O)N(CCOc2ccccc2)c2ccc(OC(F)(F)F)cc21
CHEMBL513299 acm5_human Human No 5.4 EC50 = 4070 nM Funct
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
355 3 0 3 4.0 O=C1C(=O)N(Cc2ccccc2Cl)c2ccc(OC(F)(F)F)cc21
CHEMBL523685 acm5_human Human Yes 5.4 EC50 = 4080 nM Funct
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
315 2 0 2 3.2 Brc1ccc(cc1)CN1c2ccccc2C(=O)C1=O
CHEMBL467281 acm5_human Human No 5.4 EC50 = 4090 nM Funct
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
323 2 0 2 3.6 O=C1C(=O)N(Cc2ccccc2C(F)(F)F)c2ccc(F)cc21
CHEMBL2381694 acm5_human Human No 6.4 EC50 = 410 nM Bind
Positive allosteric modulation of human muscarinic M5 receptorPositive allosteric modulation of human muscarinic M5 receptor
351 5 0 4 3.2 O=C1C(=O)N(CCOc2ccccc2)c2ccc(OC(F)(F)F)cc21
CHEMBL523685 acm5_human Human Yes 5.4 EC50 = 4100 nM Funct
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
315 2 0 2 3.2 Brc1ccc(cc1)CN1c2ccccc2C(=O)C1=O
CHEMBL523685 acm5_human Human Yes 5.4 EC50 = 4100 nM Bind
Positive allosteric modulation activity at muscarinic M5 receptorPositive allosteric modulation activity at muscarinic M5 receptor
315 2 0 2 3.2 Brc1ccc(cc1)CN1c2ccccc2C(=O)C1=O
CHEMBL3084449 acm5_human Human No 5.4 EC50 = 4200 nM Funct
Agonist activity at human muscarinic M5 receptor by calcium mobilization assayAgonist activity at human muscarinic M5 receptor by calcium mobilization assay
379 6 2 4 2.5 CCOC(=O)N1C[C@@H]2CC[C@H](C1)[C@@H]2NCCNC(=O)c1cccc(Cl)c1
CHEMBL2111051 acm5_human Human Yes 6.4 EC50 = 422 nM Funct
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
165 2 0 2 0.7 C#CCO[C@H]1CN2CCC1CC2
CHEMBL1257863 acm5_human Human No 5.4 EC50 = 4400 nM Funct
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
399 4 0 5 3.8 O=C1C(=O)N(Cc2ccc(-c3ccncc3)nc2)c2ccc(OC(F)(F)F)cc21
CHEMBL2381696 acm5_human Human No 6.4 EC50 = 446.7 nM Bind
Positive allosteric modulation of human muscarinic M5 receptorPositive allosteric modulation of human muscarinic M5 receptor
385 5 0 4 3.8 O=C1C(=O)N(CCOc2ccc(Cl)cc2)c2ccc(OC(F)(F)F)cc21
CHEMBL2381696 acm5_human Human No 6.4 EC50 = 450 nM Bind
Positive allosteric modulation of human muscarinic M5 receptorPositive allosteric modulation of human muscarinic M5 receptor
385 5 0 4 3.8 O=C1C(=O)N(CCOc2ccc(Cl)cc2)c2ccc(OC(F)(F)F)cc21
CHEMBL523685 acm5_human Human Yes 5.3 EC50 = 4600 nM Funct
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
315 2 0 2 3.2 Brc1ccc(cc1)CN1c2ccccc2C(=O)C1=O
CHEMBL494846 acm5_human Human Yes 5.3 EC50 = 4660 nM Funct
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
367 2 0 2 4.0 O=C1C(=O)N(Cc2ccc(Br)cc2F)c2c(Cl)cccc21
CHEMBL304142 acm5_human Human Yes 5.3 EC50 = 4700 nM Bind
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)
168 1 1 4 0.7 COc1noc2c1CNCCC2
CHEMBL1482157 acm5_human Human Yes 4.3 EC50 = 47620 nM Funct
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)]
353 6 2 4 2.3 CCOC(=O)N1CCC(NCCNC(=O)c2ccccc2Cl)CC1
CHEMBL3329751 acm5_human Human No 6.3 EC50 = 478.6 nM Funct
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
494 6 1 4 4.0 CCN(Cc1ccccc1C(F)(F)F)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1
CHEMBL3329751 acm5_human Human No 6.3 EC50 = 480 nM Funct
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
494 6 1 4 4.0 CCN(Cc1ccccc1C(F)(F)F)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1
CHEMBL596289 acm5_human Human No 5.3 EC50 = 4800 nM Funct
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
432 4 0 4 5.0 O=C1C(=O)N(Cc2ccc(-c3ccc(Cl)nc3)cc2)c2ccc(OC(F)(F)F)cc21
CHEMBL1223860 acm5_human Human No 7.3 EC50 = 50.1 nM Funct
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
390 4 0 5 4.4 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4cc(F)c(C)cc43)CC2)CC1
CHEMBL1223938 acm5_human Human No 5.3 EC50 = 5011.9 nM Funct
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
450 6 0 7 3.8 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(S(=O)(=O)CC)cc43)CC2)CC1
CHEMBL2381698 acm5_human Human No 6.3 EC50 = 524.8 nM Bind
Positive allosteric modulation of human muscarinic M5 receptorPositive allosteric modulation of human muscarinic M5 receptor
365 5 0 4 3.5 Cc1cccc(OCCN2C(=O)C(=O)c3cc(OC(F)(F)F)ccc32)c1
CHEMBL2381698 acm5_human Human No 6.3 EC50 = 530 nM Bind
Positive allosteric modulation of human muscarinic M5 receptorPositive allosteric modulation of human muscarinic M5 receptor
365 5 0 4 3.5 Cc1cccc(OCCN2C(=O)C(=O)c3cc(OC(F)(F)F)ccc32)c1
CHEMBL3329752 acm5_human Human No 5.3 EC50 = 5495.4 nM Funct
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
494 6 1 4 4.0 CCN(Cc1cccc(C(F)(F)F)c1)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1
CHEMBL7634 acm5_human Human Yes 7.3 EC50 = 55 nM Bind
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)
206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1
CHEMBL3329752 acm5_human Human No 5.3 EC50 = 5600 nM Funct
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
494 6 1 4 4.0 CCN(Cc1cccc(C(F)(F)F)c1)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1
CHEMBL595404 acm5_human Human No 5.2 EC50 = 5700 nM Funct
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
351 4 0 4 3.3 COc1ccc(CN2C(=O)C(=O)c3ccc(OC(F)(F)F)cc32)cc1
CHEMBL2381697 acm5_human Human No 6.2 EC50 = 588.8 nM Bind
Positive allosteric modulation of human muscarinic M5 receptorPositive allosteric modulation of human muscarinic M5 receptor
381 6 0 5 3.2 COc1ccc(OCCN2C(=O)C(=O)c3cc(OC(F)(F)F)ccc32)cc1
CHEMBL2381697 acm5_human Human No 6.2 EC50 = 590 nM Bind
Positive allosteric modulation of human muscarinic M5 receptorPositive allosteric modulation of human muscarinic M5 receptor
381 6 0 5 3.2 COc1ccc(OCCN2C(=O)C(=O)c3cc(OC(F)(F)F)ccc32)cc1
CHEMBL1255607 acm5_human Human No 5.2 EC50 = 5900 nM Funct
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
415 4 0 3 5.1 O=C1C(=O)N(Cc2ccc(-c3ccccc3)cc2F)c2ccc(OC(F)(F)F)cc21
CHEMBL7303 acm5_human Human Yes 6.2 EC50 = 600 nM Bind
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)
155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C
CHEMBL1083203 acm5_human Human Yes 6.2 EC50 = 600 nM Bind
Positive allosteric modulation of human muscarinic M5 receptorPositive allosteric modulation of human muscarinic M5 receptor
335 3 0 4 3.0 Cn1cc(-c2ccc(CN3C(=O)C(=O)c4ccccc43)c(F)c2)cn1
CHEMBL3329755 acm5_rat Rat Yes 6.2 EC50 = 610 nM Funct
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
494 6 1 4 4.0 CCN(C(=O)C1CCN(CC1)S(=O)(=O)c1ccc2c(c1)cn[nH]2)Cc1ccccc1C(F)(F)F
CHEMBL3329715 acm5_human Human Yes 5.2 EC50 = 6166.0 nM Funct
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
386 6 0 3 3.1 CCN(Cc1ccccc1)C(=O)C1CCN(S(=O)(=O)c2ccccc2)CC1
CHEMBL3329715 acm5_human Human Yes 5.2 EC50 = 6200 nM Funct
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
386 6 0 3 3.1 CCN(Cc1ccccc1)C(=O)C1CCN(S(=O)(=O)c2ccccc2)CC1
CHEMBL667 acm5_human Human Yes 6.2 EC50 = 630 nM Funct
Agonistic activity against muscarinic acetylcholine receptor M5 expressed in NIH 3T3 cells.Agonistic activity against muscarinic acetylcholine receptor M5 expressed in NIH 3T3 cells.
146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C
CHEMBL216928 acm5_human Human No 6.2 EC50 = 631.0 nM Funct
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
487 16 0 13 1.8 COc1nsc(OCCOCCOCCOCCOc2nsnc2C2C=CCCN2C)n1
CHEMBL965 acm5_human Human Yes 5.2 EC50 = 6309.6 nM Bind
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
147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C
CHEMBL3329750 acm5_human Human No 6.2 EC50 = 640 nM Funct
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
460 6 1 4 3.7 CCN(Cc1ccccc1Cl)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1
CHEMBL3329750 acm5_human Human No 6.2 EC50 = 645.7 nM Funct
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
460 6 1 4 3.7 CCN(Cc1ccccc1Cl)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1
CHEMBL1535797 acm5_human Human Yes 4.2 EC50 = 64580 nM Funct
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)]
319 6 2 4 1.6 CCOC(=O)N1CCC(NCCNC(=O)c2ccccc2)CC1
CHEMBL1609153 acm5_human Human Yes 4.2 EC50 = 64580 nM Funct
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)]
319 6 2 4 1.6 CCOC(=O)N1CCC(NCCNC(=O)c2ccccc2)CC1
CHEMBL512977 acm5_human Human No 5.2 EC50 = 7130 nM Funct
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
323 2 0 2 3.6 O=C1C(=O)N(Cc2ccc(C(F)(F)F)cc2)c2ccc(F)cc21
CHEMBL513311 acm5_human Human No 5.2 EC50 = 7150 nM Funct
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
335 3 0 3 3.7 COc1cccc(CN2C(=O)C(=O)c3c(Cl)ccc(Cl)c32)c1
CHEMBL3329739 acm5_human Human No 6.1 EC50 = 724.4 nM Funct
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
440 6 0 3 4.2 CCN(C(=O)C1CCN(S(=O)(=O)c2ccc3c(c2)CCC3)CC1)[C@H](C)c1ccccc1
CHEMBL3329739 acm5_human Human No 6.1 EC50 = 730 nM Funct
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
440 6 0 3 4.2 CCN(C(=O)C1CCN(S(=O)(=O)c2ccc3c(c2)CCC3)CC1)[C@H](C)c1ccccc1
CHEMBL3329741 acm5_human Human No 6.1 EC50 = 740 nM Funct
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
440 6 1 4 3.6 CCN(C(=O)C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1)[C@H](C)c1ccccc1
CHEMBL3329734 acm5_human Human No 5.1 EC50 = 7400 nM Funct
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
430 6 0 5 2.9 CCN(Cc1ccccc1)C(=O)C1CCN(S(=O)(=O)c2ccc3c(c2)OCO3)CC1
CHEMBL3329741 acm5_human Human No 6.1 EC50 = 741.3 nM Funct
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
440 6 1 4 3.6 CCN(C(=O)C1CCN(S(=O)(=O)c2ccc3[nH]ncc3c2)CC1)[C@H](C)c1ccccc1
CHEMBL3329734 acm5_human Human No 5.1 EC50 = 7413.1 nM Funct
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
430 6 0 5 2.9 CCN(Cc1ccccc1)C(=O)C1CCN(S(=O)(=O)c2ccc3c(c2)OCO3)CC1
CHEMBL3329749 acm5_human Human No 6.1 EC50 = 750 nM Funct
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
456 7 1 5 3.0 CCN(Cc1ccccc1OC)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1
CHEMBL3329740 acm5_human Human No 6.1 EC50 = 758.6 nM Funct
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
440 6 1 4 3.6 CCN(C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1)[C@H](C)c1ccccc1
CHEMBL3329749 acm5_human Human No 6.1 EC50 = 758.6 nM Funct
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
456 7 1 5 3.0 CCN(Cc1ccccc1OC)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1
CHEMBL3329740 acm5_human Human No 6.1 EC50 = 760 nM Funct
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
440 6 1 4 3.6 CCN(C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1)[C@H](C)c1ccccc1
CHEMBL3334990 acm5_human Human Yes 5.1 EC50 = 7600 nM Bind
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
276 3 0 2 4.4 Clc1cccc(/C=N/N=C/c2cccc(Cl)c2)c1
CHEMBL667 acm5_human Human Yes 6.1 EC50 = 790 nM Bind
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
146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C
CHEMBL1223753 acm5_human Human Yes 6.1 EC50 = 794.3 nM Funct
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
333 2 1 4 2.6 Cc1cc2c(cc1F)[nH]c(=O)n2C1CCN(C2CCOCC2)CC1
CHEMBL1223753 acm5_human Human Yes 6.1 EC50 = 794.3 nM Funct
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
333 2 1 4 2.6 Cc1cc2c(cc1F)[nH]c(=O)n2C1CCN(C2CCOCC2)CC1
CHEMBL3329747 acm5_human Human No 6.1 EC50 = 870 nM Funct
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
440 6 1 4 3.3 CCN(Cc1cccc(C)c1)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1
CHEMBL3329748 acm5_human Human No 6.1 EC50 = 870 nM Funct
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
440 6 1 4 3.3 CCN(Cc1ccccc1C)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1
CHEMBL3329747 acm5_human Human No 6.1 EC50 = 871.0 nM Funct
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
440 6 1 4 3.3 CCN(Cc1cccc(C)c1)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1
CHEMBL3329748 acm5_human Human No 6.1 EC50 = 871.0 nM Funct
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
440 6 1 4 3.3 CCN(Cc1ccccc1C)C(=O)C1CCN(S(=O)(=O)c2ccc3cn[nH]c3c2)CC1
CHEMBL1367424 acm5_human Human Yes 4.1 EC50 = 88380 nM Funct
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)]
325 6 2 5 1.7 CCOC(=O)N1CCC(NCCNC(=O)c2cccs2)CC1
CHEMBL965 acm5_human Human Yes 5.1 EC50 = 8900 nM Funct
Agonistic activity against muscarinic acetylcholine receptor M5 expressed in NIH 3T3 cellsAgonistic activity against muscarinic acetylcholine receptor M5 expressed in NIH 3T3 cells
147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C
CHEMBL3329737 acm5_human Human No 6.0 EC50 = 930 nM Funct
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
440 6 0 4 4.4 CCN(C(=O)C1CCN(S(=O)(=O)c2ccc3occc3c2)CC1)[C@H](C)c1ccccc1
CHEMBL3329737 acm5_human Human No 6.0 EC50 = 933.3 nM Funct
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
440 6 0 4 4.4 CCN(C(=O)C1CCN(S(=O)(=O)c2ccc3occc3c2)CC1)[C@H](C)c1ccccc1
CHEMBL69306 acm5_human Human No 6.0 EC50 = 950 nM Bind
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)
192 2 1 4 0.7 C#CCOc1noc2c1CNCCC2
CHEMBL3329736 acm5_human Human No 6.0 EC50 = 970 nM Funct
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
430 7 0 4 3.7 CCN(C(=O)C1CCN(S(=O)(=O)c2ccc(OC)cc2)CC1)[C@H](C)c1ccccc1
CHEMBL3329736 acm5_human Human No 6.0 EC50 = 977.2 nM Funct
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
430 7 0 4 3.7 CCN(C(=O)C1CCN(S(=O)(=O)c2ccc(OC)cc2)CC1)[C@H](C)c1ccccc1
CHEMBL1900528 acm5_human Human No 10.0 IC50 = 0.1 nM Bind
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
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
CHEMBL3545181 acm5_human Human No 10.0 IC50 = 0.1 nM Bind
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
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
CHEMBL4440620 acm5_human Human No 10.0 IC50 = 0.1 nM Bind
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
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
CHEMBL1194325 acm5_human Human Yes 9.8 IC50 = 0.2 nM Bind
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
484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2
CHEMBL1201335 acm5_human Human Yes 9.7 IC50 = 0.2 nM Bind
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
318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C
CHEMBL168067 acm5_human Human Yes 9.5 IC50 = 0.3 nM Bind
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
324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C
CHEMBL168067 acm5_human Human Yes 9.5 IC50 = 0.3 nM Bind
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
324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C
CHEMBL1201024 acm5_human Human No 9.4 IC50 = 0.4 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
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
CHEMBL1201268 acm5_human Human No 9.4 IC50 = 0.4 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
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
CHEMBL168067 acm5_human Human Yes 9.4 IC50 = 0.5 nM Bind
Binding affinity to human muscarinic M5 receptor by radioligand displacement assayBinding affinity to human muscarinic M5 receptor by radioligand displacement assay
324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C
CHEMBL2312346 acm5_rat Rat No 9.4 IC50 = 0.5 nM Bind
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
381 7 0 5 3.6 COc1ccc(CCOC(=O)C2=C(c3ccccc3)CCN(C)C2)cc1OC
CHEMBL168067 acm5_human Human Yes 9.1 IC50 = 0.8 nM Bind
Binding affinity to human muscarinic M5 receptor by radioligand displacement assayBinding affinity to human muscarinic M5 receptor by radioligand displacement assay
324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C
CHEMBL168067 acm5_human Human Yes 9.1 IC50 = 0.8 nM Bind
Displacement of radiolabeled 4DAMP from human muscarinic M5 receptorDisplacement of radiolabeled 4DAMP from human muscarinic M5 receptor
324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C
CHEMBL517712 acm5_human Human No 9.0 IC50 = 0.9 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C
CHEMBL305906 acm5_human Human Yes 8.0 IC50 = 10 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
304 15 0 0 6.5 CCCCCCCCCCCCCCCC[n+]1ccccc1
CHEMBL334255 acm5_human Human Yes 8.0 IC50 = 10 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
304 15 0 0 6.5 CCCCCCCCCCCCCCCC[n+]1ccccc1
CHEMBL1490 acm5_human Human Yes 8.0 IC50 = 10.3 nM Bind
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
301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1
CHEMBL3105212 acm5_human Human No 6.0 IC50 = 1000 nM Funct
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
424 2 0 2 4.4 O=C(c1cc(F)cc(F)c1)N1CCN2C(=O)c3ccccc3C12c1ccc(Cl)cc1
CHEMBL3353274 acm5_human Human No 6.0 IC50 = 1000 nM Funct
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
452 2 0 4 3.6 O=C(c1cc(F)c(F)c(F)c1)N1CCN2C(=O)c3ccccc3C12c1ccc2c(c1)OCO2
CHEMBL15936 acm5_human Human Yes 4.0 IC50 = 100000 nM Bind
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
191 0 1 4 1.3 c1cc2nsnc2c2c1CCNC2
CHEMBL279105 acm5_human Human No 4.0 IC50 = 100000 nM Bind
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
241 2 0 5 2.4 CSc1nsnc1C1=C(C)CCN(C)C1
CHEMBL277642 acm5_human Human Yes 6.0 IC50 = 1016 nM Bind
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
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
CHEMBL4071900 acm5_human Human No 6.0 IC50 = 1030 nM Funct
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
434 4 0 8 2.2 Cc1noc(C)c1S(=O)(=O)N1CCN(c2ccc(N3CCCC(C)(C)C3)nn2)CC1
CHEMBL1201353 acm5_human Human Yes 6.0 IC50 = 1043 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C
CHEMBL3105228 acm5_human Human Yes 6.0 IC50 = 1047.1 nM Funct
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
424 2 0 2 4.4 Clc1ccc(cc1)[C@]12N(CCN1C(=O)c1c2cccc1)C(=O)c1ccc(c(c1)F)F
CHEMBL3105208 acm5_human Human No 6.0 IC50 = 1047.1 nM Funct
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
390 2 0 2 3.8 O=C(c1ccc(F)c(F)c1)N1CCN2C(=O)c3ccccc3C12c1ccccc1
CHEMBL3105208 acm5_human Human No 6.0 IC50 = 1050 nM Funct
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
390 2 0 2 3.8 O=C(c1ccc(F)c(F)c1)N1CCN2C(=O)c3ccccc3C12c1ccccc1
CHEMBL1889399 acm5_human Human Yes 7.0 IC50 = 107 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
368 7 1 3 3.5 CC[N+]1(CCOC(=O)C(O)(c2ccccc2)c2ccccc2)CCCCC1
CHEMBL1909073 acm5_human Human Yes 7.0 IC50 = 107 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
368 7 1 3 3.5 CC[N+]1(CCOC(=O)C(O)(c2ccccc2)c2ccccc2)CCCCC1
CHEMBL1334033 acm5_human Human Yes 6.0 IC50 = 1093.2 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
277 4 1 1 5.3 C1CCC(C(CC2CCCCN2)C2CCCCC2)CC1
CHEMBL75880 acm5_human Human Yes 6.0 IC50 = 1093.2 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
277 4 1 1 5.3 C1CCC(C(CC2CCCCN2)C2CCCCC2)CC1
CHEMBL1180249 acm5_human Human No 5.0 IC50 = 10969.8 nM Bind
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
355 7 0 3 4.9 CCN1CC=C(c2ccccc2)C(C(=O)OCCCC2CCCCC2)C1
CHEMBL118553 acm5_human Human No 5.0 IC50 = 10969.8 nM Bind
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
355 7 0 3 4.9 CCN1CC=C(c2ccccc2)C(C(=O)OCCCC2CCCCC2)C1
CHEMBL255523 acm5_rat Rat No 6.0 IC50 = 1100 nM Funct
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
363 6 1 3 4.4 CCN1CCN(c2ccc(NC(=O)CCC3CCCC3)cc2Cl)CC1
CHEMBL3353283 acm5_human Human No 6.0 IC50 = 1100 nM Funct
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
456 4 0 5 4.0 CC(C)Oc1ccc(C(=O)N2CCN3C(=O)c4ccccc4C23c2ccc3c(c2)OCO3)cc1
CHEMBL3105213 acm5_rat Rat No 6.0 IC50 = 1100 nM Funct
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
424 2 0 2 4.4 O=C(c1ccc(F)c(F)c1)N1CCN2C(=O)c3ccccc3C12c1ccc(Cl)cc1
CHEMBL30008 acm5_human Human Yes 6.0 IC50 = 1107 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
404 6 0 2 5.4 Fc1ccc(C(c2ccc(F)cc2)N2CCN(C/C=C/c3ccccc3)CC2)cc1
CHEMBL539027 acm5_human Human Yes 6.0 IC50 = 1107 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
404 6 0 2 5.4 Fc1ccc(C(c2ccc(F)cc2)N2CCN(C/C=C/c3ccccc3)CC2)cc1
CHEMBL552659 acm5_human Human Yes 6.0 IC50 = 1107 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
404 6 0 2 5.4 Fc1ccc(C(c2ccc(F)cc2)N2CCN(C/C=C/c3ccccc3)CC2)cc1
CHEMBL3105228 acm5_human Human Yes 6.0 IC50 = 1110 nM Funct
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
424 2 0 2 4.4 Clc1ccc(cc1)[C@]12N(CCN1C(=O)c1c2cccc1)C(=O)c1ccc(c(c1)F)F
CHEMBL333940 acm5_human Human No 6.0 IC50 = 1114.8 nM Bind
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
371 12 0 3 5.7 CCCCCCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1
CHEMBL1180330 acm5_human Human No 6.0 IC50 = 1127.9 nM Bind
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
273 5 0 3 3.0 CCCOC(=O)C1CN(CC)CC=C1c1ccccc1
CHEMBL122353 acm5_human Human No 6.0 IC50 = 1127.9 nM Bind
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
273 5 0 3 3.0 CCCOC(=O)C1CN(CC)CC=C1c1ccccc1
CHEMBL4096589 acm5_human Human No 6.0 IC50 = 1130 nM Funct
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
436 4 0 5 4.3 O=C(C1CCN(c2cc(Oc3ccc(F)cc3F)ncn2)CC1)N1Cc2ccccc2C1
CHEMBL1180316 acm5_human Human No 6.9 IC50 = 115.4 nM Bind
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
327 5 0 3 4.3 CCN1CCC(c2ccccc2)=C(C(=O)OCC2CCCCC2)C1
CHEMBL121520 acm5_human Human No 6.9 IC50 = 115.4 nM Bind
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
327 5 0 3 4.3 CCN1CCC(c2ccccc2)=C(C(=O)OCC2CCCCC2)C1
CHEMBL4062497 acm5_human Human Yes 5.9 IC50 = 1174.9 nM Funct
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
438 2 0 2 4.7 Cc1cc([C@@]23c4ccccc4C(=O)N2CCN3C(=O)c2ccc(F)c(F)c2)ccc1Cl
CHEMBL1529 acm5_human Human Yes 5.9 IC50 = 1191 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
309 6 1 2 4.2 OC(CCCN1CCCCC1)(c1ccccc1)c1ccccc1
CHEMBL936 acm5_human Human Yes 5.9 IC50 = 1191 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
309 6 1 2 4.2 OC(CCCN1CCCCC1)(c1ccccc1)c1ccccc1
CHEMBL1490 acm5_human Human Yes 7.9 IC50 = 12 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1
CHEMBL6528 acm5_rat Rat No 5.9 IC50 = 1200 nM Bind
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
280 3 0 2 3.4 CN(C)CC1c2ccccc2C(c2ccccc2)CN1C
CHEMBL4062497 acm5_human Human Yes 5.9 IC50 = 1200 nM Funct
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
438 2 0 2 4.7 Cc1cc([C@@]23c4ccccc4C(=O)N2CCN3C(=O)c2ccc(F)c(F)c2)ccc1Cl
CHEMBL3353268 acm5_human Human No 5.9 IC50 = 1200 nM Funct
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
434 3 0 3 4.1 COc1ccc(C23c4ccccc4C(=O)N2CCN3C(=O)c2ccc(F)c(F)c2)cc1C
CHEMBL480464 acm5_human Human Yes 5.9 IC50 = 1220 nM Bind
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
255 5 1 4 1.4 CC[C@@H](C)[C@@H](O)C(=O)OC[C@H]1CCN2CCC[C@@H]12
CHEMBL1708 acm5_human Human Yes 6.9 IC50 = 123 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1
CHEMBL490 acm5_human Human Yes 6.9 IC50 = 123 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1
CHEMBL1180312 acm5_human Human No 5.9 IC50 = 1260.5 nM Bind
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
355 7 0 3 5.1 CCN1CCC(c2ccccc2)=C(C(=O)OCCCC2CCCCC2)C1
CHEMBL121385 acm5_human Human No 5.9 IC50 = 1260.5 nM Bind
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
355 7 0 3 5.1 CCN1CCC(c2ccccc2)=C(C(=O)OCCCC2CCCCC2)C1
CHEMBL4100518 acm5_human Human No 5.9 IC50 = 1288.3 nM Funct
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
473 4 0 3 4.8 CN(c1ccc([C@@]23c4ccccc4C(=O)N2CCN3C(=O)c2ccc(F)c(F)c2)cc1)C1CCC1
CHEMBL3105215 acm5_human Human No 5.9 IC50 = 1288.3 nM Funct
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
472 3 0 3 5.3 O=C(c1ccc(SC(F)(F)F)cc1)N1CCN2C(=O)c3ccccc3C12c1ccc(F)cc1
CHEMBL42 acm5_human Human Yes 7.9 IC50 = 13 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2
CHEMBL6627 acm5_rat Rat No 6.9 IC50 = 130 nM Bind
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
278 1 0 2 3.1 CN1CCN2CC(c3ccccc3)c3ccccc3C2C1
CHEMBL1092460 acm5_human Human Yes 5.9 IC50 = 1300 nM Funct
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
373 5 1 4 3.7 CCN1CCN(c2ccc(NC(=O)c3ccccc3OC)cc2Cl)CC1
CHEMBL6747 acm5_rat Rat No 5.9 IC50 = 1300 nM Bind
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
292 2 0 2 3.5 CCN1CCN2CC(c3ccccc3)c3ccccc3C2C1
CHEMBL3105215 acm5_human Human No 5.9 IC50 = 1300 nM Funct
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
472 3 0 3 5.3 O=C(c1ccc(SC(F)(F)F)cc1)N1CCN2C(=O)c3ccccc3C12c1ccc(F)cc1
CHEMBL3353265 acm5_human Human No 5.9 IC50 = 1300 nM Funct
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
434 2 0 4 3.5 O=C(c1ccc(F)c(F)c1)N1CCN2C(=O)c3ccccc3C12c1ccc2c(c1)OCO2
CHEMBL3353271 acm5_human Human No 5.9 IC50 = 1300 nM Funct
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
434 3 0 3 4.1 COc1cc(C23c4ccccc4C(=O)N2CCN3C(=O)c2ccc(F)c(F)c2)ccc1C
CHEMBL3353286 acm5_human Human No 5.9 IC50 = 1300 nM Funct
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
456 5 0 4 4.6 COc1ccc(C23c4ccccc4C(=O)N2CCN3C(=O)c2ccc(OC(C)C)cc2)cc1C
CHEMBL3353287 acm5_human Human No 5.9 IC50 = 1300 nM Funct
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
460 5 0 4 4.4 COc1cc(C23c4ccccc4C(=O)N2CCN3C(=O)c2ccc(OC(C)C)cc2)ccc1F
CHEMBL3361328 acm5_human Human No 5.9 IC50 = 1300 nM Funct
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
420 3 0 3 3.8 COc1ccc(C23c4ccccc4C(=O)N2CCN3C(=O)c2ccc(F)c(F)c2)cc1
CHEMBL271704 acm5_rat Rat No 4.9 IC50 = 13000 nM Funct
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
383 5 1 3 4.2 CCN1CCN(c2ccc(NC(=O)[C@H]3C[C@@H]3c3ccccc3)cc2Cl)CC1
CHEMBL3361328 acm5_human Human No 5.9 IC50 = 1318.3 nM Funct
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
420 3 0 3 3.8 COc1ccc(C23c4ccccc4C(=O)N2CCN3C(=O)c2ccc(F)c(F)c2)cc1
CHEMBL4100518 acm5_human Human No 5.9 IC50 = 1320 nM Funct
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
473 4 0 3 4.8 CN(c1ccc([C@@]23c4ccccc4C(=O)N2CCN3C(=O)c2ccc(F)c(F)c2)cc1)C1CCC1
CHEMBL1184096 acm5_human Human No 5.9 IC50 = 1331.2 nM Bind
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
259 4 0 3 2.7 CCOC(=O)C1=C(c2ccccc2)CCN(CC)C1
CHEMBL332335 acm5_human Human No 5.9 IC50 = 1331.2 nM Bind
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
259 4 0 3 2.7 CCOC(=O)C1=C(c2ccccc2)CCN(CC)C1
CHEMBL762 acm5_human Human Yes 5.9 IC50 = 1332 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C
CHEMBL1182210 acm5_human Human Yes 6.9 IC50 = 134 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1
CHEMBL221753 acm5_human Human Yes 6.9 IC50 = 134 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1
CHEMBL346389 acm5_human Human Yes 5.9 IC50 = 1340 nM Bind
Inhibition of [3H]- NMS binding against human recombinant Muscarinic acetylcholine receptor M5Inhibition of [3H]- NMS binding against human recombinant Muscarinic acetylcholine receptor M5
357 3 1 4 3.0 O=C1COc2cc(CN3CCN(c4ccc(Cl)cc4)CC3)ccc2N1
CHEMBL41 acm5_human Human Yes 5.9 IC50 = 1358 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F
CHEMBL1180331 acm5_human Human No 6.9 IC50 = 138.9 nM Bind
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
315 8 0 3 4.3 CCCCCCOC(=O)C1=C(c2ccccc2)CCN(CC)C1
CHEMBL122354 acm5_human Human No 6.9 IC50 = 138.9 nM Bind
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
315 8 0 3 4.3 CCCCCCOC(=O)C1=C(c2ccccc2)CCN(CC)C1
CHEMBL3105203 acm5_human Human No 5.9 IC50 = 1380 nM Funct
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
454 3 0 3 5.1 O=C(c1ccc(SC(F)(F)F)cc1)N1CCN2C(=O)c3ccccc3C12c1ccccc1
CHEMBL3105203 acm5_human Human No 5.9 IC50 = 1380.4 nM Funct
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
454 3 0 3 5.1 O=C(c1ccc(SC(F)(F)F)cc1)N1CCN2C(=O)c3ccccc3C12c1ccccc1
CHEMBL3353276 acm5_human Human No 5.9 IC50 = 1400 nM Funct
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
472 3 0 3 4.6 COc1ccc(C23c4ccccc4C(=O)N2CCN3C(=O)c2cc(F)c(F)c(F)c2)cc1Cl
CHEMBL4065335 acm5_human Human No 5.8 IC50 = 1445.4 nM Funct
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
509 3 0 3 5.0 O=C(c1ccc(F)c(F)c1)N1CCN2C(=O)c3ccccc3[C@@]12c1ccc(N2CCCC(F)(F)C2)cc1
CHEMBL4086766 acm5_human Human No 5.8 IC50 = 1445.4 nM Funct
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
541 3 0 3 5.7 O=C(c1ccc(F)c(F)c1)N1CCN2C(=O)c3ccccc3[C@@]12c1ccc(N2CCCCC2C(F)(F)F)cc1
CHEMBL4065335 acm5_human Human No 5.8 IC50 = 1460 nM Funct
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
509 3 0 3 5.0 O=C(c1ccc(F)c(F)c1)N1CCN2C(=O)c3ccccc3[C@@]12c1ccc(N2CCCC(F)(F)C2)cc1
CHEMBL1185758 acm5_human Human No 5.8 IC50 = 1467.3 nM Bind
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
325 7 0 4 4.4 CCCCCc1noc(C2=C(c3ccccc3)CCN(CC)C2)n1
CHEMBL431688 acm5_human Human No 5.8 IC50 = 1467.3 nM Bind
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
325 7 0 4 4.4 CCCCCc1noc(C2=C(c3ccccc3)CCN(CC)C2)n1
CHEMBL633 acm5_human Human Yes 5.8 IC50 = 1499 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2
CHEMBL1184134 acm5_human Human No 5.8 IC50 = 1567.9 nM Bind
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
377 9 0 3 5.0 CCN1CC=C(c2ccccc2)C(C(=O)OCCCCCc2ccccc2)C1
CHEMBL334093 acm5_human Human No 5.8 IC50 = 1567.9 nM Bind
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
377 9 0 3 5.0 CCN1CC=C(c2ccccc2)C(C(=O)OCCCCCc2ccccc2)C1
CHEMBL1184188 acm5_human Human No 5.8 IC50 = 1568.6 nM Bind
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
307 4 0 3 3.8 CCN1CCC(c2ccccc2)=C(C(=O)Oc2ccccc2)C1
CHEMBL338280 acm5_human Human No 5.8 IC50 = 1568.6 nM Bind
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
307 4 0 3 3.8 CCN1CCC(c2ccccc2)=C(C(=O)Oc2ccccc2)C1
CHEMBL1083618 acm5_human Human No 5.8 IC50 = 1584.9 nM Bind
Inhibition of human muscarinic M5 receptor expressed in CHO cellsInhibition of human muscarinic M5 receptor expressed in CHO cells
344 4 2 2 3.8 O=C(NCC1=CCNCC1)c1c(F)cccc1-c1cccc(Cl)c1
CHEMBL1180298 acm5_human Human No 6.8 IC50 = 159.2 nM Bind
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
341 6 0 3 4.5 CCN1CC=C(c2ccccc2)C(C(=O)OCCC2CCCCC2)C1
CHEMBL120599 acm5_human Human No 6.8 IC50 = 159.2 nM Bind
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
341 6 0 3 4.5 CCN1CC=C(c2ccccc2)C(C(=O)OCCC2CCCCC2)C1
CHEMBL21731 acm5_human Human Yes 6.8 IC50 = 160 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12
CHEMBL3353279 acm5_human Human No 5.8 IC50 = 1600 nM Funct
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
472 3 0 3 4.6 COc1cc(C23c4ccccc4C(=O)N2CCN3C(=O)c2cc(F)c(F)c(F)c2)ccc1Cl
CHEMBL3361327 acm5_human Human No 5.8 IC50 = 1600 nM Funct
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
420 3 0 3 3.8 COc1cccc(C23c4ccccc4C(=O)N2CCN3C(=O)c2ccc(F)c(F)c2)c1
CHEMBL4062497 acm5_rat Rat Yes 5.8 IC50 = 1600 nM Funct
Negative allosteric modulation of rat 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 rat 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
438 2 0 2 4.7 Cc1cc([C@@]23c4ccccc4C(=O)N2CCN3C(=O)c2ccc(F)c(F)c2)ccc1Cl
CHEMBL657 acm5_human Human Yes 6.8 IC50 = 162 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C
CHEMBL1160977 acm5_human Human No 6.8 IC50 = 162.5 nM Bind
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
315 8 0 3 4.1 CCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1
CHEMBL1184119 acm5_human Human No 6.8 IC50 = 162.5 nM Bind
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
315 8 0 3 4.1 CCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1
CHEMBL333065 acm5_human Human No 6.8 IC50 = 162.5 nM Bind
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
315 8 0 3 4.1 CCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1
CHEMBL3361327 acm5_human Human No 5.8 IC50 = 1621.8 nM Funct
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
420 3 0 3 3.8 COc1cccc(C23c4ccccc4C(=O)N2CCN3C(=O)c2ccc(F)c(F)c2)c1
CHEMBL499519 acm5_human Human Yes 5.8 IC50 = 1640 nM Bind
Binding affinity to human muscarinic M5 receptor expressed in insect Sf9 cellsBinding affinity to human muscarinic M5 receptor expressed in insect Sf9 cells
757 23 5 11 5.9 CCCCCCCCCCCC(OC(=O)C(CCCCN(O)C(C)=O)NC(=O)c1coc(-c2ccccc2O)n1)C(C)C(=O)NC1CCCCN(O)C1=O
CHEMBL4062497 acm5_rat Rat Yes 5.8 IC50 = 1659.6 nM Funct
Negative allosteric modulation of rat 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 rat 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
438 2 0 2 4.7 Cc1cc([C@@]23c4ccccc4C(=O)N2CCN3C(=O)c2ccc(F)c(F)c2)ccc1Cl
CHEMBL1160977 acm5_human Human No 6.8 IC50 = 167 nM Bind
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
315 8 0 3 4.1 CCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1
CHEMBL1184119 acm5_human Human No 6.8 IC50 = 167 nM Bind
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
315 8 0 3 4.1 CCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1
CHEMBL333065 acm5_human Human No 6.8 IC50 = 167 nM Bind
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
315 8 0 3 4.1 CCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1
CHEMBL1184062 acm5_human Human No 4.8 IC50 = 16901.9 nM Bind
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
245 3 0 3 2.2 CCN1CC=C(c2ccccc2)C(C(=O)OC)C1
CHEMBL330885 acm5_human Human No 4.8 IC50 = 16901.9 nM Bind
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
245 3 0 3 2.2 CCN1CC=C(c2ccccc2)C(C(=O)OC)C1
CHEMBL304036 acm5_human Human No 5.8 IC50 = 1731.8 nM Bind
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
376 2 1 4 4.4 CCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cccc(C)c2C1O3
CHEMBL954 acm5_human Human Yes 5.8 IC50 = 1771 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
405 9 0 2 6.6 CCN(CC)CCOc1ccc(/C(=C(/Cl)c2ccccc2)c2ccccc2)cc1
CHEMBL4071136 acm5_human Human Yes 5.8 IC50 = 1778.3 nM Funct
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
438 2 0 2 4.7 Cc1cc(C23c4ccccc4C(=O)N2CCN3C(=O)c2ccc(F)c(F)c2)ccc1Cl
CHEMBL294726 acm5_human Human No 4.8 IC50 = 17980.7 nM Bind
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
320 1 1 3 3.9 COc1ccc2c(c1)CCN1Cc3c(ccc4[nH]c(C)cc34)OC21
CHEMBL4071136 acm5_human Human Yes 5.8 IC50 = 1800 nM Funct
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
438 2 0 2 4.7 Cc1cc(C23c4ccccc4C(=O)N2CCN3C(=O)c2ccc(F)c(F)c2)ccc1Cl
CHEMBL3361317 acm5_human Human No 5.8 IC50 = 1800 nM Funct
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
418 3 0 3 4.2 COc1ccc(C(=O)N2CCN3C(=O)c4ccccc4C23c2ccc(Cl)cc2)cc1
CHEMBL6482 acm5_rat Rat No 4.8 IC50 = 18000 nM Bind
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
320 4 0 2 4.3 CCCCN1CCN2CC(c3ccccc3)c3ccccc3C2C1
CHEMBL4092786 acm5_human Human No 5.7 IC50 = 1819.7 nM Funct
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
509 3 0 3 5.0 O=C(c1ccc(F)c(F)c1)N1CCN2C(=O)c3ccccc3[C@@]12c1ccc(N2CCC(F)(F)CC2)cc1
CHEMBL3361317 acm5_human Human No 5.7 IC50 = 1819.7 nM Funct
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
418 3 0 3 4.2 COc1ccc(C(=O)N2CCN3C(=O)c4ccccc4C23c2ccc(Cl)cc2)cc1
CHEMBL4092786 acm5_human Human No 5.7 IC50 = 1820 nM Funct
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
509 3 0 3 5.0 O=C(c1ccc(F)c(F)c1)N1CCN2C(=O)c3ccccc3[C@@]12c1ccc(N2CCC(F)(F)CC2)cc1
CHEMBL1160977 acm5_human Human No 6.7 IC50 = 186.9 nM Bind
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
315 8 0 3 4.1 CCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1
CHEMBL1184119 acm5_human Human No 6.7 IC50 = 186.9 nM Bind
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
315 8 0 3 4.1 CCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1
CHEMBL333065 acm5_human Human No 6.7 IC50 = 186.9 nM Bind
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
315 8 0 3 4.1 CCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1
CHEMBL120135 acm5_human Human No 5.7 IC50 = 1889.3 nM Bind
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
315 4 0 3 4.0 CCN1CC[C@@H](c2ccccc2)[C@@H](C(=O)OC2CCCCC2)C1
CHEMBL1180367 acm5_human Human No 6.7 IC50 = 190.3 nM Bind
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
349 6 0 3 4.1 CCN1CC=C(c2ccccc2)C(C(=O)OCCc2ccc(C)cc2)C1
CHEMBL124173 acm5_human Human No 6.7 IC50 = 190.3 nM Bind
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
349 6 0 3 4.1 CCN1CC=C(c2ccccc2)C(C(=O)OCCc2ccc(C)cc2)C1
CHEMBL6437 acm5_rat Rat Yes 5.7 IC50 = 1900 nM Bind
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
264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1
CHEMBL3353282 acm5_human Human No 5.7 IC50 = 1900 nM Funct
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
470 6 0 4 5.1 CC(C)Oc1ccc(C(=O)N2CCN3C(=O)c4ccccc4C23c2ccc(OC(C)C)cc2)cc1
CHEMBL114379 acm5_human Human No 5.7 IC50 = 1910 nM Bind
Binding affinity against muscarinic acetylcholine receptor M5Binding affinity against muscarinic acetylcholine receptor M5
385 3 1 6 4.0 Oc1nc2ccccc2n1C1CCN(Cc2cc3c(cc2Cl)OCO3)CC1
CHEMBL1184139 acm5_human Human No 6.7 IC50 = 194.2 nM Bind
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
329 9 0 3 4.7 CCCCCCCOC(=O)C1=C(c2ccccc2)CCN(CC)C1
CHEMBL334245 acm5_human Human No 6.7 IC50 = 194.2 nM Bind
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
329 9 0 3 4.7 CCCCCCCOC(=O)C1=C(c2ccccc2)CCN(CC)C1
CHEMBL3105204 acm5_human Human No 5.7 IC50 = 1949.8 nM Funct
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
422 2 0 2 4.5 O=C(c1ccc(C(F)(F)F)cc1)N1CCN2C(=O)c3ccccc3C12c1ccccc1
CHEMBL3105204 acm5_human Human No 5.7 IC50 = 1950 nM Funct
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
422 2 0 2 4.5 O=C(c1ccc(C(F)(F)F)cc1)N1CCN2C(=O)c3ccccc3C12c1ccccc1
CHEMBL284237 acm5_human Human Yes 8.7 IC50 = 2 nM Bind
Percent inhibition against Muscarinic acetylcholine receptor M5 at 1 uMPercent inhibition against Muscarinic acetylcholine receptor M5 at 1 uM
221 0 1 1 3.2 C[C@]12N[C@H](Cc3ccccc31)c1ccccc12
CHEMBL1201203 acm5_human Human Yes 8.7 IC50 = 2.0 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1
CHEMBL438151 acm5_human Human Yes 8.7 IC50 = 2.0 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1
CHEMBL1506225 acm5_human Human No 8.6 IC50 = 2.3 nM Bind
Compound was evaluated for its binding affinity at human muscarinic receptor m5 by the displacement of [3H]-NMS radioligand using membranes from transfected chinese hamster ovarian cellCompound was evaluated for its binding affinity at human muscarinic receptor m5 by the displacement of [3H]-NMS radioligand using membranes from transfected chinese hamster ovarian cell
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
CHEMBL376897 acm5_human Human No 8.6 IC50 = 2.3 nM Bind
Compound was evaluated for its binding affinity at human muscarinic receptor m5 by the displacement of [3H]-NMS radioligand using membranes from transfected chinese hamster ovarian cellCompound was evaluated for its binding affinity at human muscarinic receptor m5 by the displacement of [3H]-NMS radioligand using membranes from transfected chinese hamster ovarian cell
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
CHEMBL1123 acm5_human Human Yes 8.6 IC50 = 2.4 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC
CHEMBL3102882 acm5_human Human No 5.7 IC50 = 2000 nM Funct
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
456 2 0 2 5.2 O=C(c1ccc(C(F)(F)F)cc1)N1CCN2C(=O)c3ccccc3C12c1ccc(Cl)cc1
CHEMBL3353270 acm5_human Human No 5.7 IC50 = 2000 nM Funct
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
454 3 0 3 4.4 COc1cc(C23c4ccccc4C(=O)N2CCN3C(=O)c2ccc(F)c(F)c2)ccc1Cl
CHEMBL6638 acm5_rat Rat No 4.7 IC50 = 20000 nM Bind
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
348 6 0 2 5.1 CCCCCCN1CCN2CC(c3ccccc3)c3ccccc3C2C1
CHEMBL61700 acm5_human Human No 5.7 IC50 = 2033.9 nM Bind
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
454 4 1 5 5.9 CCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cc(Oc4ccccc4)ccc2C1O3
CHEMBL3102882 acm5_human Human No 5.7 IC50 = 2041.7 nM Funct
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
456 2 0 2 5.2 O=C(c1ccc(C(F)(F)F)cc1)N1CCN2C(=O)c3ccccc3C12c1ccc(Cl)cc1
CHEMBL1184098 acm5_human Human No 5.7 IC50 = 2075.4 nM Bind
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
325 7 0 4 4.3 CCCCCc1noc(C2CN(CC)CC=C2c2ccccc2)n1
CHEMBL332405 acm5_human Human No 5.7 IC50 = 2075.4 nM Bind
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
325 7 0 4 4.3 CCCCCc1noc(C2CN(CC)CC=C2c2ccccc2)n1
CHEMBL3105217 acm5_human Human No 5.7 IC50 = 2089.3 nM Funct
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
440 2 0 2 4.7 O=C(c1cccc(C(F)(F)F)c1)N1CCN2C(=O)c3ccccc3C12c1ccc(F)cc1
CHEMBL540195 acm5_rat Rat No 5.7 IC50 = 2100 nM Bind
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
294 1 1 3 2.8 CN1CCN2CC(c3ccc(O)cc3)c3ccccc3C2C1
CHEMBL15944 acm5_human Human No 5.7 IC50 = 2100 nM Bind
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
227 2 0 5 2.0 CSc1nsnc1C1=CCCN(C)C1
CHEMBL308608 acm5_human Human No 5.7 IC50 = 2100 nM Bind
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
227 2 0 5 2.0 CSc1nsnc1C1=CCCN(C)C1
CHEMBL3105217 acm5_human Human No 5.7 IC50 = 2100 nM Funct
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
440 2 0 2 4.7 O=C(c1cccc(C(F)(F)F)c1)N1CCN2C(=O)c3ccccc3C12c1ccc(F)cc1
CHEMBL3361330 acm5_human Human No 5.7 IC50 = 2100 nM Funct
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
396 2 0 2 4.3 O=C(c1ccc(F)c(F)c1)N1CCN2C(=O)c3ccccc3C12C1CCCCC1
CHEMBL3105208 acm5_rat Rat No 5.7 IC50 = 2100 nM Funct
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
390 2 0 2 3.8 O=C(c1ccc(F)c(F)c1)N1CCN2C(=O)c3ccccc3C12c1ccccc1
CHEMBL3361330 acm5_human Human No 5.7 IC50 = 2138.0 nM Funct
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
396 2 0 2 4.3 O=C(c1ccc(F)c(F)c1)N1CCN2C(=O)c3ccccc3C12C1CCCCC1
CHEMBL1184068 acm5_human Human No 6.7 IC50 = 214.5 nM Bind
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
327 5 0 3 4.1 CCN1CC=C(c2ccccc2)C(C(=O)OCC2CCCCC2)C1
CHEMBL330999 acm5_human Human No 6.7 IC50 = 214.5 nM Bind
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
327 5 0 3 4.1 CCN1CC=C(c2ccccc2)C(C(=O)OCC2CCCCC2)C1
CHEMBL728 acm5_human Human Yes 6.7 IC50 = 220 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2
CHEMBL3353289 acm5_human Human No 5.7 IC50 = 2200 nM Funct
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
456 5 0 4 4.6 COc1cc(C23c4ccccc4C(=O)N2CCN3C(=O)c2ccc(OC(C)C)cc2)ccc1C
CHEMBL1184244 acm5_human Human No 6.7 IC50 = 222.1 nM Bind
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
317 8 0 3 4.2 CCCCCCOC(=O)[C@H]1CN(CC)CC[C@H]1c1ccccc1
CHEMBL340780 acm5_human Human No 6.7 IC50 = 222.1 nM Bind
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
317 8 0 3 4.2 CCCCCCOC(=O)[C@H]1CN(CC)CC[C@H]1c1ccccc1
CHEMBL1108 acm5_human Human Yes 5.6 IC50 = 2298 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1
CHEMBL1094003 acm5_human Human Yes 5.6 IC50 = 2300 nM Funct
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
377 4 1 3 4.4 CCN1CCN(c2ccc(NC(=O)c3ccccc3Cl)cc2Cl)CC1
CHEMBL3105209 acm5_human Human No 5.6 IC50 = 2300 nM Funct
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
472 3 0 3 5.1 O=C(c1ccc(OC(F)(F)F)cc1)N1CCN2C(=O)c3ccccc3C12c1ccc(Cl)cc1
CHEMBL3105226 acm5_human Human No 5.6 IC50 = 2300 nM Funct
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
404 2 0 2 4.1 Cc1ccc(C23c4ccccc4C(=O)N2CCN3C(=O)c2cc(F)cc(F)c2)cc1
CHEMBL15675 acm5_human Human No 4.6 IC50 = 23000 nM Bind
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
225 0 0 5 1.7 CN1CCC2=C(C1)c1nsnc1SC2
CHEMBL3105209 acm5_human Human No 5.6 IC50 = 2344.2 nM Funct
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
472 3 0 3 5.1 O=C(c1ccc(OC(F)(F)F)cc1)N1CCN2C(=O)c3ccccc3C12c1ccc(Cl)cc1
CHEMBL3105226 acm5_human Human No 5.6 IC50 = 2344.2 nM Funct
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
404 2 0 2 4.1 Cc1ccc(C23c4ccccc4C(=O)N2CCN3C(=O)c2cc(F)cc(F)c2)cc1
CHEMBL332320 acm5_human Human No 6.6 IC50 = 235.6 nM Bind
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
371 12 0 3 5.9 CCCCCCCCCCOC(=O)C1=C(c2ccccc2)CCN(CC)C1
CHEMBL1180285 acm5_human Human No 7.6 IC50 = 24.8 nM Bind
Binding affinity to human M5 muscarinic receptor expressed in cell membranes by radioligand binding assayBinding affinity to human M5 muscarinic receptor expressed in cell membranes by radioligand binding assay
349 6 0 3 4.3 CCN1CCC(c2ccccc2)=C(C(=O)OCCc2ccc(C)cc2)C1
CHEMBL120119 acm5_human Human No 7.6 IC50 = 24.8 nM Bind
Binding affinity to human M5 muscarinic receptor expressed in cell membranes by radioligand binding assayBinding affinity to human M5 muscarinic receptor expressed in cell membranes by radioligand binding assay
349 6 0 3 4.3 CCN1CCC(c2ccccc2)=C(C(=O)OCCc2ccc(C)cc2)C1
CHEMBL1180285 acm5_human Human No 7.6 IC50 = 24.8 nM Bind
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
349 6 0 3 4.3 CCN1CCC(c2ccccc2)=C(C(=O)OCCc2ccc(C)cc2)C1
CHEMBL120119 acm5_human Human No 7.6 IC50 = 24.8 nM Bind
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
349 6 0 3 4.3 CCN1CCC(c2ccccc2)=C(C(=O)OCCc2ccc(C)cc2)C1
CHEMBL3353273 acm5_human Human No 5.6 IC50 = 2400 nM Funct
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
466 4 0 3 4.7 CC(C)Oc1ccc(C23c4ccccc4C(=O)N2CCN3C(=O)c2cc(F)c(F)c(F)c2)cc1
CHEMBL3361331 acm5_human Human No 5.6 IC50 = 2400 nM Funct
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
382 2 0 2 3.9 O=C(c1ccc(F)c(F)c1)N1CCN2C(=O)c3ccccc3C12C1CCCC1
CHEMBL3361331 acm5_human Human No 5.6 IC50 = 2454.7 nM Funct
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
382 2 0 2 3.9 O=C(c1ccc(F)c(F)c1)N1CCN2C(=O)c3ccccc3C12C1CCCC1
CHEMBL3353290 acm5_human Human No 6.6 IC50 = 246 nM Funct
Antagonist activity at human muscarinic M5 receptor assessed as inhibition of acetylcholine-induced calcium responseAntagonist activity at human muscarinic M5 receptor assessed as inhibition of acetylcholine-induced calcium response
452 3 0 3 4.2 COc1ccc([C@@]23c4ccccc4C(=O)N2CCN3C(=O)c2cc(F)c(F)c(F)c2)cc1C
CHEMBL71 acm5_human Human Yes 7.6 IC50 = 25 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C
CHEMBL965 acm5_human Human Yes 4.6 IC50 = 25200 nM Bind
Compound was evaluated for its binding affinity at human muscarinic receptor m5 by the displacement of [3H]-NMS radioligand using membranes from transfected chinese hamster ovarian cellCompound was evaluated for its binding affinity at human muscarinic receptor m5 by the displacement of [3H]-NMS radioligand using membranes from transfected chinese hamster ovarian cell
147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C
CHEMBL1183926 acm5_human Human No 6.6 IC50 = 254.9 nM Bind
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
287 6 0 3 3.5 CCCCOC(=O)C1=C(c2ccccc2)CCN(CC)C1
CHEMBL324712 acm5_human Human No 6.6 IC50 = 254.9 nM Bind
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
287 6 0 3 3.5 CCCCOC(=O)C1=C(c2ccccc2)CCN(CC)C1
CHEMBL1190178 acm5_human Human No 6.6 IC50 = 255.8 nM Bind
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
349 7 0 3 4.2 CCN1CC=C(c2ccccc2)C(C(=O)OCCCc2ccccc2)C1
CHEMBL540316 acm5_human Human No 6.6 IC50 = 255.8 nM Bind
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
349 7 0 3 4.2 CCN1CC=C(c2ccccc2)C(C(=O)OCCCc2ccccc2)C1
CHEMBL83 acm5_human Human Yes 5.6 IC50 = 2585 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1
CHEMBL1628227 acm5_human Human Yes 7.6 IC50 = 26 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21
CHEMBL6649 acm5_rat Rat No 5.6 IC50 = 2600 nM Bind
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
252 3 2 2 2.7 CNCC1NCC(c2ccccc2)c2ccccc21
CHEMBL1507034 acm5_human Human Yes 5.6 IC50 = 2600 nM Funct
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
402 2 0 2 4.5 Cc1ccc(C(=O)N2CCN3C(=O)c4ccccc4C23c2ccc(Cl)cc2)cc1
CHEMBL3105227 acm5_human Human No 5.6 IC50 = 2600 nM Funct
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
404 2 0 2 4.1 Cc1ccc(C23c4ccccc4C(=O)N2CCN3C(=O)c2ccc(F)c(F)c2)cc1
CHEMBL2391353 acm5_human Human No 4.6 IC50 = 26000 nM Bind
Binding affinity to M5 receptor (unknown origin) by radioligand displacement assayBinding affinity to M5 receptor (unknown origin) by radioligand displacement assay
265 3 1 3 1.2 O=C(CN1CCN2CCC[C@H]2C1)NC1CCCCC1
CHEMBL1200348 acm5_human Human Yes 5.6 IC50 = 2607 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
396 6 0 3 6.5 Clc1ccc(CSC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1
CHEMBL1221 acm5_human Human Yes 5.6 IC50 = 2607 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
396 6 0 3 6.5 Clc1ccc(CSC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1
CHEMBL3353290 acm5_human Human No 6.6 IC50 = 263.0 nM Funct
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
452 3 0 3 4.2 COc1ccc([C@@]23c4ccccc4C(=O)N2CCN3C(=O)c2cc(F)c(F)c(F)c2)cc1C
CHEMBL1507034 acm5_human Human Yes 5.6 IC50 = 2630.3 nM Funct
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
402 2 0 2 4.5 Cc1ccc(C(=O)N2CCN3C(=O)c4ccccc4C23c2ccc(Cl)cc2)cc1
CHEMBL3105227 acm5_human Human No 5.6 IC50 = 2630.3 nM Funct
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
404 2 0 2 4.1 Cc1ccc(C23c4ccccc4C(=O)N2CCN3C(=O)c2ccc(F)c(F)c2)cc1
CHEMBL3353290 acm5_human Human No 6.6 IC50 = 264 nM Funct
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
452 3 0 3 4.2 COc1ccc([C@@]23c4ccccc4C(=O)N2CCN3C(=O)c2cc(F)c(F)c(F)c2)cc1C
CHEMBL1184092 acm5_human Human No 6.6 IC50 = 264.7 nM Bind
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
287 6 0 3 3.4 CCCCOC(=O)C1CN(CC)CC=C1c1ccccc1
CHEMBL332181 acm5_human Human No 6.6 IC50 = 264.7 nM Bind
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
287 6 0 3 3.4 CCCCOC(=O)C1CN(CC)CC=C1c1ccccc1
CHEMBL58228 acm5_human Human No 4.6 IC50 = 26644.8 nM Bind
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
422 4 1 6 4.1 CCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cc(OC)c(OC)cc2C1O3
CHEMBL1201156 acm5_human Human Yes 7.6 IC50 = 27 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2ccccc21
CHEMBL445 acm5_human Human Yes 7.6 IC50 = 27 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2ccccc21
CHEMBL3353269 acm5_human Human No 5.6 IC50 = 2700 nM Funct
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
438 3 0 3 3.9 COc1cc(C23c4ccccc4C(=O)N2CCN3C(=O)c2ccc(F)c(F)c2)ccc1F
CHEMBL1192001 acm5_human Human No 6.6 IC50 = 272.8 nM Bind
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
321 5 0 3 3.9 CCN1CCC(c2ccccc2)=C(C(=O)OCc2ccccc2)C1
CHEMBL543177 acm5_human Human No 6.6 IC50 = 272.8 nM Bind
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
321 5 0 3 3.9 CCN1CCC(c2ccccc2)=C(C(=O)OCc2ccccc2)C1
CHEMBL1201023 acm5_human Human Yes 7.6 IC50 = 28 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1
CHEMBL900 acm5_human Human Yes 7.6 IC50 = 28 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1
CHEMBL361506 acm5_human Human Yes 5.5 IC50 = 2885 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
340 10 4 4 2.9 N=C(N)c1ccc(OCCCCCOc2ccc(C(=N)N)cc2)cc1
CHEMBL55 acm5_human Human Yes 5.5 IC50 = 2885 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
340 10 4 4 2.9 N=C(N)c1ccc(OCCCCCOc2ccc(C(=N)N)cc2)cc1
CHEMBL1172 acm5_human Human Yes 6.5 IC50 = 292 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1
CHEMBL1182713 acm5_human Human No 5.5 IC50 = 2971.4 nM Bind
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
315 4 0 3 4.0 CCN1CC[C@@H](c2ccccc2)[C@H](C(=O)OC2CCCCC2)C1
CHEMBL262303 acm5_human Human No 5.5 IC50 = 2971.4 nM Bind
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
315 4 0 3 4.0 CCN1CC[C@@H](c2ccccc2)[C@H](C(=O)OC2CCCCC2)C1
CHEMBL1231 acm5_human Human Yes 8.5 IC50 = 3.2 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC
CHEMBL516 acm5_human Human Yes 8.4 IC50 = 3.8 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1
CHEMBL3105228 acm5_human Human Yes 6.5 IC50 = 300 nM Funct
Antagonist activity at human muscarinic M5 receptor assessed as inhibition of acetylcholine-induced calcium responseAntagonist activity at human muscarinic M5 receptor assessed as inhibition of acetylcholine-induced calcium response
424 2 0 2 4.4 Clc1ccc(cc1)[C@]12N(CCN1C(=O)c1c2cccc1)C(=O)c1ccc(c(c1)F)F
CHEMBL1770373 acm5_human Human Yes 6.5 IC50 = 300 nM Bind
Binding affinity to muscarinic M5 receptorBinding affinity to muscarinic M5 receptor
239 2 1 3 1.8 c1ccc(Cc2ncc3c(n2)CCNCC3)cc1
CHEMBL11 acm5_rat Rat Yes 6.5 IC50 = 300 nM Bind
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
280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C
CHEMBL3105228 acm5_human Human Yes 6.5 IC50 = 300 nM Funct
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
424 2 0 2 4.4 Clc1ccc(cc1)[C@]12N(CCN1C(=O)c1c2cccc1)C(=O)c1ccc(c(c1)F)F
CHEMBL3105210 acm5_human Human No 5.5 IC50 = 3000 nM Funct
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
488 3 0 3 5.8 O=C(c1ccc(SC(F)(F)F)cc1)N1CCN2C(=O)c3ccccc3C12c1ccc(Cl)cc1
CHEMBL716 acm5_human Human Yes 5.5 IC50 = 3000.7 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2
CHEMBL4081565 acm5_human Human No 5.5 IC50 = 3020.0 nM Funct
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
477 3 0 3 4.3 O=C(c1ccc(F)c(F)c1)N1CCN2C(=O)c3ccccc3[C@@]12c1ccc(N2CC[C@@H](F)C2)cc1
CHEMBL3105205 acm5_human Human No 5.5 IC50 = 3020.0 nM Funct
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
422 2 0 2 4.5 O=C(c1cccc(C(F)(F)F)c1)N1CCN2C(=O)c3ccccc3C12c1ccccc1
CHEMBL3105210 acm5_human Human No 5.5 IC50 = 3020.0 nM Funct
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
488 3 0 3 5.8 O=C(c1ccc(SC(F)(F)F)cc1)N1CCN2C(=O)c3ccccc3C12c1ccc(Cl)cc1
CHEMBL3105205 acm5_human Human No 5.5 IC50 = 3020 nM Funct
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
422 2 0 2 4.5 O=C(c1cccc(C(F)(F)F)c1)N1CCN2C(=O)c3ccccc3C12c1ccccc1
CHEMBL195437 acm5_human Human Yes 4.5 IC50 = 30764 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
206 7 1 1 4.3 CCCCCCCCc1ccc(O)cc1
CHEMBL4081565 acm5_human Human No 5.5 IC50 = 3090 nM Funct
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
477 3 0 3 4.3 O=C(c1ccc(F)c(F)c1)N1CCN2C(=O)c3ccccc3[C@@]12c1ccc(N2CC[C@@H](F)C2)cc1
CHEMBL1184108 acm5_human Human No 4.5 IC50 = 31057 nM Bind
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
307 4 0 3 3.6 CCN1CC=C(c2ccccc2)C(C(=O)Oc2ccccc2)C1
CHEMBL332645 acm5_human Human No 4.5 IC50 = 31057 nM Bind
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
307 4 0 3 3.6 CCN1CC=C(c2ccccc2)C(C(=O)Oc2ccccc2)C1
CHEMBL1180305 acm5_human Human No 5.5 IC50 = 3108.6 nM Bind
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
411 7 0 3 5.5 CCN1CCC(c2ccccc2)=C(C(=O)OCC(c2ccccc2)c2ccccc2)C1
CHEMBL120963 acm5_human Human No 5.5 IC50 = 3108.6 nM Bind
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
411 7 0 3 5.5 CCN1CCC(c2ccccc2)=C(C(=O)OCC(c2ccccc2)c2ccccc2)C1
CHEMBL1909072 acm5_human Human Yes 5.5 IC50 = 3144 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
401 5 1 4 4.5 NC(=O)C1CCN(CCCN2c3ccccc3Sc3ccc(Cl)cc32)CC1
CHEMBL1200406 acm5_human Human Yes 6.5 IC50 = 316 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
469 6 1 7 3.0 CN(C)CCOC(c1ccccc1)c1ccccc1.Cn1c(=O)c2[nH]c(Cl)nc2n(C)c1=O
CHEMBL6437 acm5_human Human Yes 6.5 IC50 = 320 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1
CHEMBL3353284 acm5_human Human No 5.5 IC50 = 3200 nM Funct
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
460 5 0 4 4.4 COc1ccc(C23c4ccccc4C(=O)N2CCN3C(=O)c2ccc(OC(C)C)cc2)cc1F
CHEMBL3361338 acm5_human Human No 5.5 IC50 = 3200 nM Funct
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
434 4 0 3 4.2 CCOc1ccc(C23c4ccccc4C(=O)N2CCN3C(=O)c2ccc(F)c(F)c2)cc1
CHEMBL1255739 acm5_human Human Yes 5.5 IC50 = 3265 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
261 6 0 4 2.7 CN(C)CCN(Cc1cccs1)c1ccccn1
CHEMBL1411979 acm5_human Human Yes 5.5 IC50 = 3265 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
261 6 0 4 2.7 CN(C)CCN(Cc1cccs1)c1ccccn1
CHEMBL120972 acm5_human Human No 6.5 IC50 = 328.6 nM Bind
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
357 11 0 3 5.3 CCCCCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1
CHEMBL1184064 acm5_human Human No 6.5 IC50 = 330.9 nM Bind
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
335 6 0 3 3.8 CCN1CC=C(c2ccccc2)C(C(=O)OCCc2ccccc2)C1
CHEMBL330892 acm5_human Human No 6.5 IC50 = 330.9 nM Bind
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
335 6 0 3 3.8 CCN1CC=C(c2ccccc2)C(C(=O)OCCc2ccccc2)C1
CHEMBL3353266 acm5_human Human No 5.5 IC50 = 3300 nM Funct
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
438 3 0 3 3.9 COc1ccc(C23c4ccccc4C(=O)N2CCN3C(=O)c2ccc(F)c(F)c2)cc1F
CHEMBL3353285 acm5_human Human No 5.5 IC50 = 3300 nM Funct
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
476 5 0 4 4.9 COc1ccc(C23c4ccccc4C(=O)N2CCN3C(=O)c2ccc(OC(C)C)cc2)cc1Cl
CHEMBL305660 acm5_human Human Yes 6.5 IC50 = 337.8 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1
CHEMBL4072027 acm5_human Human No 5.5 IC50 = 3388.4 nM Funct
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
541 3 0 3 5.6 O=C(c1ccc(F)c(F)c1)N1CCN2C(=O)c3ccccc3[C@@]12c1ccc(N2CCC(C(F)(F)F)CC2)cc1
CHEMBL2107687 acm5_human Human Yes 7.5 IC50 = 34 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
306 9 0 2 3.8 CCC(C)C(C(=O)OCC[N+](C)(CC)CC)c1ccccc1
CHEMBL2111176 acm5_human Human Yes 7.5 IC50 = 34 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
306 9 0 2 3.8 CCC(C)C(C(=O)OCC[N+](C)(CC)CC)c1ccccc1
CHEMBL9967 acm5_human Human Yes 6.5 IC50 = 340.6 nM Bind
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
351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2
CHEMBL1184242 acm5_human Human No 6.5 IC50 = 341.9 nM Bind
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
301 7 0 3 3.9 CCCCCOC(=O)C1=C(c2ccccc2)CCN(CC)C1
CHEMBL340561 acm5_human Human No 6.5 IC50 = 341.9 nM Bind
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
301 7 0 3 3.9 CCCCCOC(=O)C1=C(c2ccccc2)CCN(CC)C1
CHEMBL4072027 acm5_human Human No 5.5 IC50 = 3420 nM Funct
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
541 3 0 3 5.6 O=C(c1ccc(F)c(F)c1)N1CCN2C(=O)c3ccccc3[C@@]12c1ccc(N2CCC(C(F)(F)F)CC2)cc1
CHEMBL56564 acm5_human Human No 5.5 IC50 = 3450 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
284 2 1 3 3.0 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(=O)c1c[nH]c2c1cccc2
CHEMBL4100810 acm5_human Human No 5.5 IC50 = 3467.4 nM Funct
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
536 4 0 4 5.5 O=C(c1ccc(F)c(F)c1)N1CCN2C(=O)c3ccccc3[C@@]12c1ccc(N2CCC[C@H]2c2cccnc2)cc1
CHEMBL3105221 acm5_human Human No 5.5 IC50 = 3467.4 nM Funct
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
452 3 0 3 4.7 Cc1ccc(C23c4ccccc4C(=O)N2CCN3C(=O)c2ccc(OC(F)(F)F)cc2)cc1
CHEMBL1459098 acm5_human Human Yes 5.5 IC50 = 3490 nM Funct
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
372 2 0 2 3.6 O=C(c1ccc(F)cc1)N1CCN2C(=O)c3ccccc3C12c1ccccc1
CHEMBL1093775 acm5_human Human Yes 5.5 IC50 = 3500 nM Funct
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
357 4 1 3 4.0 CCN1CCN(c2ccc(NC(=O)c3cccc(C)c3)cc2Cl)CC1
CHEMBL266801 acm5_rat Rat No 5.5 IC50 = 3500 nM Bind
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
323 2 0 4 3.0 CN1CCN2CC(c3ccc([N+](=O)[O-])cc3)c3ccccc3C2C1
CHEMBL4100810 acm5_human Human No 5.5 IC50 = 3500 nM Funct
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
536 4 0 4 5.5 O=C(c1ccc(F)c(F)c1)N1CCN2C(=O)c3ccccc3[C@@]12c1ccc(N2CCC[C@H]2c2cccnc2)cc1
CHEMBL3105221 acm5_human Human No 5.5 IC50 = 3500 nM Funct
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
452 3 0 3 4.7 Cc1ccc(C23c4ccccc4C(=O)N2CCN3C(=O)c2ccc(OC(F)(F)F)cc2)cc1
CHEMBL1180349 acm5_human Human No 5.5 IC50 = 3565.8 nM Bind
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
411 7 0 3 5.4 CCN1CC=C(c2ccccc2)C(C(=O)OCC(c2ccccc2)c2ccccc2)C1
CHEMBL123198 acm5_human Human No 5.5 IC50 = 3565.8 nM Bind
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
411 7 0 3 5.4 CCN1CC=C(c2ccccc2)C(C(=O)OCC(c2ccccc2)c2ccccc2)C1
CHEMBL1200633 acm5_human Human Yes 5.4 IC50 = 3608 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
None None None CC[C@H](C)[C@H]1O[C@]2(CC[C@@H]1C)C[C@@H]1C[C@@H](C/C=C(\C)[C@@H](O[C@H]3C[C@H](OC)[C@@H](O[C@H]4C[C@H](OC)[C@@H](O)[C@H](C)O4)[C@H](C)O3)[C@@H](C)/C=C/C=C3\CO[C@@H]4[C@H](O)C(C)=C[C@@H](C(=O)O1)[C@]34O)O2.CO[C@H]1C[C@H](O[C@H]2[C@H](C)O[C@@H](O[C@@H]3/C(C)=C/C[C@@H]4C[C@@H](C[C@]5(CC[C@H](C)[C@@H](C(C)C)O5)O4)OC(=O)[C@@H]4C=C(C)[C@@H](O)[C@H]5OC/C(=C\C=C\[C@@H]3C)[C@@]45O)C[C@@H]2OC)O[C@@H](C)[C@@H]1O
CHEMBL546257 acm5_human Human Yes 5.4 IC50 = 3736 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12
CHEMBL554190 acm5_human Human Yes 5.4 IC50 = 3736 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12
CHEMBL7568 acm5_human Human Yes 5.4 IC50 = 3736 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
399 9 1 4 6.0 CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12
CHEMBL534 acm5_human Human Yes 6.4 IC50 = 374 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1
CHEMBL116601 acm5_human Human No 6.4 IC50 = 374 nM Bind
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
301 7 0 3 3.8 CCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1
CHEMBL1180202 acm5_human Human No 6.4 IC50 = 374 nM Bind
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
301 7 0 3 3.8 CCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1
CHEMBL3105207 acm5_human Human No 5.4 IC50 = 3800 nM Funct
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
390 2 0 2 3.8 O=C(c1cc(F)cc(F)c1)N1CCN2C(=O)c3ccccc3C12c1ccccc1
CHEMBL3105207 acm5_human Human No 5.4 IC50 = 3801.9 nM Funct
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
390 2 0 2 3.8 O=C(c1cc(F)cc(F)c1)N1CCN2C(=O)c3ccccc3C12c1ccccc1
CHEMBL61412 acm5_human Human No 5.4 IC50 = 3807.6 nM Bind
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
406 4 1 5 4.5 CCCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cc(OC)ccc2C1O3
CHEMBL4542697 acm5_human Human Yes 5.4 IC50 = 3860 nM Funct
Antagonist activity at human muscarinic M5 receptor assessed as inhibition of acetylcholine-induced calcium responseAntagonist activity at human muscarinic M5 receptor assessed as inhibition of acetylcholine-induced calcium response
331 2 0 6 1.3 Cc1nn(C)c(C)c1S(=O)(=O)N1CCC2(CC1)OCCS2
CHEMBL303758 acm5_human Human No 5.4 IC50 = 3884.2 nM Bind
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
376 2 1 4 4.4 CCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cc(C)ccc2C1O3
CHEMBL54 acm5_human Human Yes 5.4 IC50 = 3890 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl
CHEMBL522460 acm5_rat Rat Yes 5.4 IC50 = 3970 nM Funct
Antagonist activity at rat muscarinic M5 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium responseAntagonist activity at rat muscarinic M5 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium response
404 4 1 4 3.9 Cc1ccccc1CN1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1
CHEMBL4085038 acm5_human Human No 5.4 IC50 = 3981.1 nM Funct
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
487 3 0 3 5.0 CC1CCCN(c2ccc([C@@]34c5ccccc5C(=O)N3CCN4C(=O)c3ccc(F)c(F)c3)cc2)C1
CHEMBL643 acm5_human Human Yes 8.3 IC50 = 4.6 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C
CHEMBL715 acm5_human Human Yes 7.4 IC50 = 40 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C
CHEMBL395110 acm5_human Human Yes 7.4 IC50 = 40 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
310 2 0 3 4.6 CN1CCCC(CN2c3ccccc3Sc3ccccc32)C1
CHEMBL1180239 acm5_human Human No 6.4 IC50 = 400.6 nM Bind
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
343 10 0 3 4.9 CCCCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1
CHEMBL118241 acm5_human Human No 6.4 IC50 = 400.6 nM Bind
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
343 10 0 3 4.9 CCCCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1
CHEMBL414182 acm5_rat Rat No 5.4 IC50 = 4000 nM Bind
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
266 3 1 2 3.0 CN(C)CC1NCC(c2ccccc2)c2ccccc21
CHEMBL6455 acm5_rat Rat No 5.4 IC50 = 4000 nM Bind
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
293 1 1 3 2.7 CN1CCN2CC(c3ccc(N)cc3)c3ccccc3C2C1
CHEMBL4085038 acm5_human Human No 5.4 IC50 = 4010 nM Funct
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
487 3 0 3 5.0 CC1CCCN(c2ccc([C@@]34c5ccccc5C(=O)N3CCN4C(=O)c3ccc(F)c(F)c3)cc2)C1
CHEMBL1180297 acm5_human Human No 6.4 IC50 = 407.3 nM Bind
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
287 5 0 3 3.4 CCN1CCC(c2ccccc2)=C(C(=O)OCC(C)C)C1
CHEMBL120581 acm5_human Human No 6.4 IC50 = 407.3 nM Bind
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
287 5 0 3 3.4 CCN1CCC(c2ccccc2)=C(C(=O)OCC(C)C)C1
CHEMBL3105222 acm5_human Human No 5.4 IC50 = 4073.8 nM Funct
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
468 3 0 3 5.4 Cc1ccc(C23c4ccccc4C(=O)N2CCN3C(=O)c2ccc(SC(F)(F)F)cc2)cc1
CHEMBL59939 acm5_human Human No 5.4 IC50 = 4093 nM Bind
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
378 2 1 5 3.7 COC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cc(OC)ccc2C1O3
CHEMBL1090096 acm5_human Human No 5.4 IC50 = 4100 nM Funct
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
411 4 1 3 4.8 CCN1CCN(c2ccc(NC(=O)c3cccc(C(F)(F)F)c3)cc2Cl)CC1
CHEMBL1090097 acm5_human Human No 5.4 IC50 = 4100 nM Funct
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
479 4 1 3 5.8 CCN1CCN(c2ccc(NC(=O)c3cc(C(F)(F)F)ccc3C(F)(F)F)cc2Cl)CC1
CHEMBL3105222 acm5_human Human No 5.4 IC50 = 4100 nM Funct
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
468 3 0 3 5.4 Cc1ccc(C23c4ccccc4C(=O)N2CCN3C(=O)c2ccc(SC(F)(F)F)cc2)cc1
CHEMBL3353281 acm5_human Human No 5.4 IC50 = 4100 nM Funct
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
456 6 0 4 4.7 CCOc1ccc(C23c4ccccc4C(=O)N2CCN3C(=O)c2ccc(OC(C)C)cc2)cc1
CHEMBL1180296 acm5_human Human No 5.4 IC50 = 4169.5 nM Bind
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
259 4 0 3 2.6 CCOC(=O)C1CN(CC)CC=C1c1ccccc1
CHEMBL120539 acm5_human Human No 5.4 IC50 = 4169.5 nM Bind
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
259 4 0 3 2.6 CCOC(=O)C1CN(CC)CC=C1c1ccccc1
CHEMBL301041 acm5_human Human No 5.4 IC50 = 4187.1 nM Bind
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
362 2 1 4 4.1 CCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2ccccc2C1O3
CHEMBL1190784 acm5_human Human No 7.4 IC50 = 42.5 nM Bind
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
321 5 0 3 3.8 CCN1CC=C(c2ccccc2)C(C(=O)OCc2ccccc2)C1
CHEMBL541584 acm5_human Human No 7.4 IC50 = 42.5 nM Bind
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
321 5 0 3 3.8 CCN1CC=C(c2ccccc2)C(C(=O)OCc2ccccc2)C1
CHEMBL1184138 acm5_human Human No 5.4 IC50 = 4264 nM Bind
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
337 6 0 3 3.9 CCN1CC[C@@H](c2ccccc2)[C@@H](C(=O)OCCc2ccccc2)C1
CHEMBL334194 acm5_human Human No 5.4 IC50 = 4264 nM Bind
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
337 6 0 3 3.9 CCN1CC[C@@H](c2ccccc2)[C@@H](C(=O)OCCc2ccccc2)C1
CHEMBL4103187 acm5_human Human No 5.4 IC50 = 4265.8 nM Funct
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
491 3 0 3 4.7 O=C(c1ccc(F)c(F)c1)N1CCN2C(=O)c3ccccc3[C@@]12c1ccc(N2CCC(F)CC2)cc1
CHEMBL4103187 acm5_human Human No 5.4 IC50 = 4280 nM Funct
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
491 3 0 3 4.7 O=C(c1ccc(F)c(F)c1)N1CCN2C(=O)c3ccccc3[C@@]12c1ccc(N2CCC(F)CC2)cc1
CHEMBL6627 acm5_rat Rat No 6.4 IC50 = 430 nM Bind
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
278 1 0 2 3.1 CN1CCN2CC(c3ccccc3)c3ccccc3C2C1
CHEMBL59347 acm5_human Human No 4.4 IC50 = 43462.7 nM Bind
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
350 2 1 4 3.9 COc1cc2c(cc1OC)C1Oc3ccc4[nH]c(C)cc4c3CN1CC2
CHEMBL1306 acm5_human Human Yes 5.4 IC50 = 4362 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
531 8 0 8 4.5 CC(C)N1CCN(c2ccc(OC[C@H]3CO[C@](Cn4cncn4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1
CHEMBL4090346 acm5_human Human No 5.4 IC50 = 4466.8 nM Funct
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
521 3 0 3 5.9 CC1Cc2ccccc2N1c1ccc([C@@]23c4ccccc4C(=O)N2CCN3C(=O)c2ccc(F)c(F)c2)cc1
CHEMBL3105202 acm5_human Human No 5.4 IC50 = 4466.8 nM Funct
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
438 3 0 3 4.4 O=C(c1ccc(OC(F)(F)F)cc1)N1CCN2C(=O)c3ccccc3C12c1ccccc1
CHEMBL3105202 acm5_human Human No 5.4 IC50 = 4470 nM Funct
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
438 3 0 3 4.4 O=C(c1ccc(OC(F)(F)F)cc1)N1CCN2C(=O)c3ccccc3C12c1ccccc1
CHEMBL588119 acm5_human Human Yes 5.4 IC50 = 4486.8 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
337 12 2 3 5.6 CCCCCCCCN[C@H](C)[C@@H](O)c1ccc(SC(C)C)cc1
CHEMBL6575 acm5_rat Rat No 4.4 IC50 = 45000 nM Bind
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
368 3 0 6 2.9 CN1CCN2CC(c3ccc([N+](=O)[O-])cc3)c3ccc([N+](=O)[O-])cc3C2C1
CHEMBL4090346 acm5_human Human No 5.3 IC50 = 4550 nM Funct
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
521 3 0 3 5.9 CC1Cc2ccccc2N1c1ccc([C@@]23c4ccccc4C(=O)N2CCN3C(=O)c2ccc(F)c(F)c2)cc1
CHEMBL6627 acm5_rat Rat No 4.3 IC50 = 46000 nM Bind
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
278 1 0 2 3.1 CN1CCN2CC(c3ccccc3)c3ccccc3C2C1
CHEMBL1184074 acm5_human Human No 6.3 IC50 = 472.2 nM Bind
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
377 9 0 3 5.1 CCN1CCC(c2ccccc2)=C(C(=O)OCCCCCc2ccccc2)C1
CHEMBL331516 acm5_human Human No 6.3 IC50 = 472.2 nM Bind
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
377 9 0 3 5.1 CCN1CCC(c2ccccc2)=C(C(=O)OCCCCCc2ccccc2)C1
CHEMBL61494 acm5_human Human No 4.3 IC50 = 47361.5 nM Bind
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
408 4 1 6 3.8 CCOC(=O)c1c[nH]c2ccc3c(c12)CN1CCc2cc(OC)c(OC)cc2C1O3
CHEMBL62251 acm5_human Human No 5.3 IC50 = 4737 nM Bind
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
406 3 1 5 4.5 COc1ccc2c(c1)CCN1Cc3c(ccc4[nH]c(C)c(C(=O)OC(C)C)c34)OC21
CHEMBL3105213 acm5_human Human No 6.3 IC50 = 478.6 nM Funct
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
424 2 0 2 4.4 O=C(c1ccc(F)c(F)c1)N1CCN2C(=O)c3ccccc3C12c1ccc(Cl)cc1
CHEMBL3105213 acm5_human Human No 6.3 IC50 = 478.6 nM Funct
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
424 2 0 2 4.4 O=C(c1ccc(F)c(F)c1)N1CCN2C(=O)c3ccccc3C12c1ccc(Cl)cc1
CHEMBL1192621 acm5_human Human No 6.3 IC50 = 479.4 nM Bind
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
349 7 0 3 4.3 CCN1CCC(c2ccccc2)=C(C(=O)OCCCc2ccccc2)C1
CHEMBL543890 acm5_human Human No 6.3 IC50 = 479.4 nM Bind
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
349 7 0 3 4.3 CCN1CCC(c2ccccc2)=C(C(=O)OCCCc2ccccc2)C1
CHEMBL3105213 acm5_human Human No 6.3 IC50 = 480 nM Funct
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
424 2 0 2 4.4 O=C(c1ccc(F)c(F)c1)N1CCN2C(=O)c3ccccc3C12c1ccc(Cl)cc1
CHEMBL3105213 acm5_human Human No 6.3 IC50 = 480 nM Funct
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
424 2 0 2 4.4 O=C(c1ccc(F)c(F)c1)N1CCN2C(=O)c3ccccc3C12c1ccc(Cl)cc1
CHEMBL522460 acm5_human Human Yes 5.3 IC50 = 4897.8 nM Funct
Antagonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium responseAntagonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium response
404 4 1 4 3.9 Cc1ccccc1CN1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1
CHEMBL3105211 acm5_human Human No 5.3 IC50 = 4897.8 nM Funct
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
456 2 0 2 5.2 O=C(c1cccc(C(F)(F)F)c1)N1CCN2C(=O)c3ccccc3C12c1ccc(Cl)cc1
CHEMBL2024407 acm5_human Human No 5.3 IC50 = 4900 nM Funct
Antagonist activity at human muscarinic M5 receptor by calcium mobilization assayAntagonist activity at human muscarinic M5 receptor by calcium mobilization assay
345 6 2 4 2.2 CCOC(=O)N1[C@H]2CC[C@@H]1C[C@H](NCCNC(=O)c1ccccc1)C2
CHEMBL522460 acm5_human Human Yes 5.3 IC50 = 4900 nM Funct
Antagonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium responseAntagonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium response
404 4 1 4 3.9 Cc1ccccc1CN1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1
CHEMBL3105211 acm5_human Human No 5.3 IC50 = 4900 nM Funct
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
456 2 0 2 5.2 O=C(c1cccc(C(F)(F)F)c1)N1CCN2C(=O)c3ccccc3C12c1ccc(Cl)cc1
CHEMBL1180310 acm5_human Human No 6.3 IC50 = 499.7 nM Bind
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
365 7 0 4 3.8 CCN1CC=C(c2ccccc2)C(C(=O)OCCc2ccc(OC)cc2)C1
CHEMBL121299 acm5_human Human No 6.3 IC50 = 499.7 nM Bind
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
365 7 0 4 3.8 CCN1CC=C(c2ccccc2)C(C(=O)OCCc2ccc(OC)cc2)C1
CHEMBL1180309 acm5_human Human No 5.3 IC50 = 5000 nM Bind
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
363 8 0 3 4.6 CCN1CC=C(c2ccccc2)C(C(=O)OCCCCc2ccccc2)C1
CHEMBL121298 acm5_human Human No 5.3 IC50 = 5000 nM Bind
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
363 8 0 3 4.6 CCN1CC=C(c2ccccc2)C(C(=O)OCCCCc2ccccc2)C1
CHEMBL1083925 acm5_human Human No 6.3 IC50 = 501.2 nM Bind
Inhibition of human muscarinic M5 receptor expressed in CHO cellsInhibition of human muscarinic M5 receptor expressed in CHO cells
360 4 2 2 4.1 C[C@H]1CNCC[C@@H]1CNC(=O)c1c(F)cccc1-c1cccc(Cl)c1
CHEMBL1083108 acm5_human Human No 5.3 IC50 = 5011.9 nM Bind
Inhibition of human muscarinic M5 receptor expressed in CHO cellsInhibition of human muscarinic M5 receptor expressed in CHO cells
346 4 2 2 3.9 O=C(NCC1CCNCC1)c1ccccc1-c1cc(Cl)ccc1F
CHEMBL1709 acm5_human Human Yes 6.3 IC50 = 507.3 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21
CHEMBL809 acm5_human Human Yes 6.3 IC50 = 507.3 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21
CHEMBL1160977 acm5_human Human No 6.3 IC50 = 508.2 nM Bind
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
315 8 0 3 4.1 CCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1
CHEMBL1184119 acm5_human Human No 6.3 IC50 = 508.2 nM Bind
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
315 8 0 3 4.1 CCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1
CHEMBL333065 acm5_human Human No 6.3 IC50 = 508.2 nM Bind
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
315 8 0 3 4.1 CCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1
CHEMBL4059829 acm5_human Human No 6.3 IC50 = 510 nM Funct
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
450 4 0 5 4.3 O=C(C1CCN(c2cc(Oc3ccc(F)cc3F)ncn2)CC1)N1CCc2ccccc2C1
CHEMBL3353277 acm5_human Human No 6.3 IC50 = 510 nM Funct
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
452 3 0 3 4.2 COc1ccc(C23c4ccccc4C(=O)N2CCN3C(=O)c2cc(F)c(F)c(F)c2)cc1C
CHEMBL3353277 acm5_human Human No 6.3 IC50 = 512.9 nM Funct
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
452 3 0 3 4.2 COc1ccc(C23c4ccccc4C(=O)N2CCN3C(=O)c2cc(F)c(F)c(F)c2)cc1C
CHEMBL3353290 acm5_rat Rat No 6.3 IC50 = 516 nM Funct
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 Fluo4AM 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 Fluo4AM staining-based fluorescence assay
452 3 0 3 4.2 COc1ccc([C@@]23c4ccccc4C(=O)N2CCN3C(=O)c2cc(F)c(F)c(F)c2)cc1C
CHEMBL4448840 acm5_human Human Yes 5.3 IC50 = 5160 nM Funct
Antagonist activity at human muscarinic M5 receptor assessed as inhibition of acetylcholine-induced calcium responseAntagonist activity at human muscarinic M5 receptor assessed as inhibition of acetylcholine-induced calcium response
384 4 0 8 3.4 Fc1cc(F)cc(-c2nnc(Cc3nc(-c4ccc5c(c4)OCO5)no3)o2)c1
CHEMBL1200710 acm5_human Human Yes 7.3 IC50 = 53 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
314 4 0 2 4.5 CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21
CHEMBL415 acm5_human Human Yes 7.3 IC50 = 53 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
314 4 0 2 4.5 CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21
CHEMBL459265 acm5_human Human Yes 6.3 IC50 = 535 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1
CHEMBL64894 acm5_human Human Yes 6.3 IC50 = 535 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1
CHEMBL1180314 acm5_human Human No 6.3 IC50 = 537.3 nM Bind
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
329 9 0 3 4.5 CCCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1
CHEMBL121476 acm5_human Human No 6.3 IC50 = 537.3 nM Bind
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
329 9 0 3 4.5 CCCCCCCOC(=O)C1CN(CC)CC=C1c1ccccc1
CHEMBL1184116 acm5_human Human No 7.3 IC50 = 54.1 nM Bind
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
313 4 0 3 4.0 CCN1CCC(c2ccccc2)=C(C(=O)OC2CCCCC2)C1
CHEMBL332980 acm5_human Human No 7.3 IC50 = 54.1 nM Bind
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
313 4 0 3 4.0 CCN1CCC(c2ccccc2)=C(C(=O)OC2CCCCC2)C1
CHEMBL1319362 acm5_human Human No 7.3 IC50 = 55 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
275 3 1 4 1.9 CN1[C@H]2CC[C@@H]1C[C@H](OC(=O)C(O)c1ccccc1)C2
CHEMBL1618018 acm5_human Human No 7.3 IC50 = 55 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
275 3 1 4 1.9 CN1[C@H]2CC[C@@H]1C[C@H](OC(=O)C(O)c1ccccc1)C2
CHEMBL3353267 acm5_human Human No 5.3 IC50 = 5500 nM Funct
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
454 3 0 3 4.4 COc1ccc(C23c4ccccc4C(=O)N2CCN3C(=O)c2ccc(F)c(F)c2)cc1Cl
CHEMBL3361326 acm5_human Human No 5.3 IC50 = 5500 nM Funct
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
420 3 0 3 3.8 COc1ccccc1C12c3ccccc3C(=O)N1CCN2C(=O)c1ccc(F)c(F)c1
CHEMBL1180317 acm5_human Human No 6.3 IC50 = 558.9 nM Bind
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
287 5 0 3 3.2 CCN1CC=C(c2ccccc2)C(C(=O)OCC(C)C)C1
CHEMBL121552 acm5_human Human No 6.3 IC50 = 558.9 nM Bind
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
287 5 0 3 3.2 CCN1CC=C(c2ccccc2)C(C(=O)OCC(C)C)C1
CHEMBL1180292 acm5_human Human No 7.3 IC50 = 56.2 nM Bind
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
341 6 0 3 4.7 CCN1CCC(c2ccccc2)=C(C(=O)OCCC2CCCCC2)C1
CHEMBL120472 acm5_human Human No 7.3 IC50 = 56.2 nM Bind
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
341 6 0 3 4.7 CCN1CCC(c2ccccc2)=C(C(=O)OCCC2CCCCC2)C1
CHEMBL6446 acm5_rat Rat No 5.3 IC50 = 5600 nM Bind
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
308 2 0 3 3.1 COc1ccc(C2CN3CCN(C)CC3c3ccccc32)cc1
CHEMBL3361326 acm5_human Human No 5.3 IC50 = 5623.4 nM Funct
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
420 3 0 3 3.8 COc1ccccc1C12c3ccccc3C(=O)N1CCN2C(=O)c1ccc(F)c(F)c1
CHEMBL1459098 acm5_rat Rat Yes 5.3 IC50 = 5670 nM Funct
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
372 2 0 2 3.6 O=C(c1ccc(F)cc1)N1CCN2C(=O)c3ccccc3C12c1ccccc1
CHEMBL1180282 acm5_human Human No 7.2 IC50 = 57.9 nM Bind
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
343 10 0 3 5.1 CCCCCCCCOC(=O)C1=C(c2ccccc2)CCN(CC)C1
CHEMBL120080 acm5_human Human No 7.2 IC50 = 57.9 nM Bind
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
343 10 0 3 5.1 CCCCCCCCOC(=O)C1=C(c2ccccc2)CCN(CC)C1
CHEMBL4086766 acm5_human Human No 5.2 IC50 = 5700 nM Funct
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
541 3 0 3 5.7 O=C(c1ccc(F)c(F)c1)N1CCN2C(=O)c3ccccc3[C@@]12c1ccc(N2CCCCC2C(F)(F)F)cc1
CHEMBL3105206 acm5_human Human No 5.2 IC50 = 5750 nM Funct
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
422 2 0 2 4.8 O=C(c1cc(Cl)cc(Cl)c1)N1CCN2C(=O)c3ccccc3C12c1ccccc1
CHEMBL3105206 acm5_human Human No 5.2 IC50 = 5754.4 nM Funct
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
422 2 0 2 4.8 O=C(c1cc(Cl)cc(Cl)c1)N1CCN2C(=O)c3ccccc3C12c1ccccc1
CHEMBL61774 acm5_human Human No 5.2 IC50 = 5760.1 nM Bind
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
348 1 1 4 3.7 COC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2ccccc2C1O3
CHEMBL3361323 acm5_human Human No 5.2 IC50 = 5800 nM Funct
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
407 2 0 3 3.7 O=C(c1ccnc(F)c1)N1CCN2C(=O)c3ccccc3C12c1ccc(Cl)cc1
CHEMBL3361323 acm5_human Human No 5.2 IC50 = 5888.4 nM Funct
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
407 2 0 3 3.7 O=C(c1ccnc(F)c1)N1CCN2C(=O)c3ccccc3C12c1ccc(Cl)cc1
CHEMBL1386 acm5_human Human No 5.2 IC50 = 5925.4 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
None None None None
CHEMBL60142 acm5_human Human No 5.2 IC50 = 5999.2 nM Bind
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
378 3 1 5 3.8 CCOC(=O)c1c[nH]c2ccc3c(c12)CN1CCc2cc(OC)ccc2C1O3
CHEMBL1180290 acm5_human Human No 6.2 IC50 = 602.9 nM Bind
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
273 5 0 3 3.1 CCCOC(=O)C1=C(c2ccccc2)CCN(CC)C1
CHEMBL120329 acm5_human Human No 6.2 IC50 = 602.9 nM Bind
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
273 5 0 3 3.1 CCCOC(=O)C1=C(c2ccccc2)CCN(CC)C1
CHEMBL4068043 acm5_human Human No 5.2 IC50 = 6025.6 nM Funct
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
473 3 0 3 4.8 O=C(c1ccc(F)c(F)c1)N1CCN2C(=O)c3ccccc3[C@@]12c1ccc(N2CCCCC2)cc1
CHEMBL4068043 acm5_human Human No 5.2 IC50 = 6040 nM Funct
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
473 3 0 3 4.8 O=C(c1ccc(F)c(F)c1)N1CCN2C(=O)c3ccccc3[C@@]12c1ccc(N2CCCCC2)cc1
CHEMBL3361320 acm5_human Human No 6.2 IC50 = 610 nM Funct
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
442 2 0 2 4.6 O=C(c1cc(F)c(F)c(F)c1)N1CCN2C(=O)c3ccccc3C12c1ccc(Cl)cc1
CHEMBL3361320 acm5_human Human No 6.2 IC50 = 616.6 nM Funct
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
442 2 0 2 4.6 O=C(c1cc(F)c(F)c(F)c1)N1CCN2C(=O)c3ccccc3C12c1ccc(Cl)cc1
CHEMBL7303 acm5_human Human Yes 4.2 IC50 = 62500 nM Bind
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
155 1 0 3 0.4 COC(=O)C1=CCCN(C1)C
CHEMBL1183934 acm5_human Human No 7.2 IC50 = 63 nM Bind
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
313 4 0 3 3.9 CCN1CC=C(c2ccccc2)C(C(=O)OC2CCCCC2)C1
CHEMBL324936 acm5_human Human No 7.2 IC50 = 63 nM Bind
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
313 4 0 3 3.9 CCN1CC=C(c2ccccc2)C(C(=O)OC2CCCCC2)C1
CHEMBL244946 acm5_human Human Yes 6.2 IC50 = 631.0 nM Funct
Antagonist activity at human muscarinic receptor M5Antagonist activity at human muscarinic receptor M5
537 7 0 8 5.6 Cc1ccc2c(-c3nnc(SCCCN4CCc5ccc(-c6cc(C)nn6C)cc5CC4)n3C)cccc2n1
CHEMBL6649 acm5_rat Rat No 5.2 IC50 = 6300 nM Bind
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
252 3 2 2 2.7 CNCC1NCC(c2ccccc2)c2ccccc21
CHEMBL2391356 acm5_human Human Yes 4.2 IC50 = 63000 nM Bind
Binding affinity to M5 receptor (unknown origin) by radioligand displacement assayBinding affinity to M5 receptor (unknown origin) by radioligand displacement assay
185 3 2 3 -0.6 CC(C)NC(=O)CN1CCNCC1
CHEMBL1082365 acm5_human Human No 5.2 IC50 = 6309.6 nM Bind
Inhibition of human muscarinic M5 receptor expressed in CHO cellsInhibition of human muscarinic M5 receptor expressed in CHO cells
378 4 2 2 4.2 C[C@H]1CNCC[C@]1(F)CNC(=O)c1c(F)cccc1-c1cccc(Cl)c1
CHEMBL4078908 acm5_human Human No 5.2 IC50 = 6309.6 nM Funct
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
491 3 0 3 4.7 O=C(c1ccc(F)c(F)c1)N1CCN2C(=O)c3ccccc3[C@@]12c1ccc(N2CCCC(F)C2)cc1
CHEMBL648 acm5_human Human Yes 6.2 IC50 = 633 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1
CHEMBL4078908 acm5_human Human No 5.2 IC50 = 6360 nM Funct
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
491 3 0 3 4.7 O=C(c1ccc(F)c(F)c1)N1CCN2C(=O)c3ccccc3[C@@]12c1ccc(N2CCCC(F)C2)cc1
CHEMBL564 acm5_human Human Yes 7.2 IC50 = 64 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C
CHEMBL3353288 acm5_human Human No 5.2 IC50 = 6400 nM Funct
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
476 5 0 4 4.9 COc1cc(C23c4ccccc4C(=O)N2CCN3C(=O)c2ccc(OC(C)C)cc2)ccc1Cl
CHEMBL4096727 acm5_human Human No 5.2 IC50 = 6500 nM Funct
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
435 4 0 6 3.0 C[C@H]1CCCCN1c1ccc(N2CCN(S(=O)(=O)c3ccccc3Cl)CC2)nn1
CHEMBL4542697 acm5_human Human Yes 6.2 IC50 = 660.7 nM Funct
Antagonist activity at human muscarinic M5 receptor assessed as inhibition of acetylcholine-induced calcium responseAntagonist activity at human muscarinic M5 receptor assessed as inhibition of acetylcholine-induced calcium response
331 2 0 6 1.3 Cc1nn(C)c(C)c1S(=O)(=O)N1CCC2(CC1)OCCS2
CHEMBL404992 acm5_rat Rat No 5.2 IC50 = 6600 nM Bind
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
306 3 0 2 3.9 CCCN1CCN2CC(c3ccccc3)c3ccccc3C2C1
CHEMBL3361316 acm5_human Human Yes 5.2 IC50 = 6600 nM Funct
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
418 3 0 3 4.2 COc1cccc(C(=O)N2CCN3C(=O)c4ccccc4C23c2ccc(Cl)cc2)c1
CHEMBL3361316 acm5_human Human Yes 5.2 IC50 = 6606.9 nM Funct
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
418 3 0 3 4.2 COc1cccc(C(=O)N2CCN3C(=O)c4ccccc4C23c2ccc(Cl)cc2)c1
CHEMBL4082503 acm5_human Human No 5.2 IC50 = 6760.8 nM Funct
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
459 4 1 3 4.7 O=C(c1ccc(F)c(F)c1)N1CCN2C(=O)c3ccccc3[C@@]12c1ccc(NC2CCC2)cc1
CHEMBL4082503 acm5_human Human No 5.2 IC50 = 6920 nM Funct
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
459 4 1 3 4.7 O=C(c1ccc(F)c(F)c1)N1CCN2C(=O)c3ccccc3[C@@]12c1ccc(NC2CCC2)cc1
CHEMBL4083681 acm5_human Human No 6.2 IC50 = 695 nM Funct
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
448 4 0 5 4.7 O=C(C1CCN(c2cc(Oc3ccc(Cl)cc3)ncn2)CC1)N1CCc2ccccc2C1
CHEMBL3353278 acm5_human Human No 6.2 IC50 = 700 nM Funct
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
456 3 0 3 4.1 COc1cc(C23c4ccccc4C(=O)N2CCN3C(=O)c2cc(F)c(F)c(F)c2)ccc1F
CHEMBL6603 acm5_rat Rat No 5.2 IC50 = 7000 nM Bind
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
266 4 2 2 3.1 CCNCC1NCC(c2ccccc2)c2ccccc21
CHEMBL296419 acm5_human Human Yes 6.2 IC50 = 703 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2
CHEMBL1983100 acm5_human Human Yes 4.2 IC50 = 71000 nM Bind
Binding affinity to M5 receptor (unknown origin) by radioligand displacement assayBinding affinity to M5 receptor (unknown origin) by radioligand displacement assay
225 3 2 3 0.3 O=C(CN1CCNCC1)NC1CCCCC1
CHEMBL6627 acm5_rat Rat No 5.1 IC50 = 7200 nM Bind
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
278 1 0 2 3.1 CN1CCN2CC(c3ccccc3)c3ccccc3C2C1
CHEMBL4063401 acm5_human Human No 5.1 IC50 = 7244.4 nM Funct
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
498 3 0 4 4.5 N#CC1CCCN(c2ccc([C@@]34c5ccccc5C(=O)N3CCN4C(=O)c3ccc(F)c(F)c3)cc2)C1
CHEMBL4063401 acm5_human Human No 5.1 IC50 = 7290 nM Funct
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
498 3 0 4 4.5 N#CC1CCCN(c2ccc([C@@]34c5ccccc5C(=O)N3CCN4C(=O)c3ccc(F)c(F)c3)cc2)C1
CHEMBL4096143 acm5_human Human No 6.1 IC50 = 732 nM Funct
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
432 4 0 5 4.2 O=C(C1CCN(c2cc(Oc3ccccc3F)ncn2)CC1)N1CCc2ccccc2C1
CHEMBL2391352 acm5_human Human No 4.1 IC50 = 74000 nM Bind
Binding affinity to M5 receptor (unknown origin) by radioligand displacement assayBinding affinity to M5 receptor (unknown origin) by radioligand displacement assay
265 3 1 3 1.2 O=C(CN1CCN2CCC[C@@H]2C1)NC1CCCCC1
CHEMBL59898 acm5_human Human Yes 5.1 IC50 = 7411.7 nM Bind
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
392 3 1 5 4.1 CCOC(=O)c1c(C)[nH]c2c1c1CN3CCc4c(C3Oc1cc2)ccc(c4)OC
CHEMBL43064 acm5_human Human Yes 6.1 IC50 = 759 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
368 6 0 2 5.1 C(=C/c1ccccc1)\CN1CCN(C(c2ccccc2)c2ccccc2)CC1
CHEMBL255169 acm5_rat Rat Yes 5.1 IC50 = 7600 nM Funct
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
371 6 1 3 4.1 CCN1CCN(c2ccc(NC(=O)CCc3ccccc3)cc2Cl)CC1
CHEMBL4062351 acm5_human Human No 5.1 IC50 = 7762.5 nM Funct
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
521 3 0 3 5.3 O=C(c1ccc(F)c(F)c1)N1CCN2C(=O)c3ccccc3[C@@]12c1ccc(N2CCc3ccccc3C2)cc1
CHEMBL1182709 acm5_human Human No 7.1 IC50 = 78.1 nM Bind
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
335 6 0 3 4.0 CCN1CCC(c2ccccc2)=C(C(=O)OCCc2ccccc2)C1
CHEMBL262198 acm5_human Human No 7.1 IC50 = 78.1 nM Bind
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
335 6 0 3 4.0 CCN1CCC(c2ccccc2)=C(C(=O)OCCc2ccccc2)C1
CHEMBL1201207 acm5_human Human Yes 5.1 IC50 = 7861 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
472 4 4 6 2.0 C[C@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)[C@@]3(F)[C@@H](O)C[C@]2(C)[C@@]1(O)C(=O)COP(=O)(O)O
CHEMBL3361319 acm5_human Human No 6.1 IC50 = 790 nM Funct
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
446 4 0 3 4.9 CC(C)Oc1ccc(C(=O)N2CCN3C(=O)c4ccccc4C23c2ccc(Cl)cc2)cc1
CHEMBL3105228 acm5_rat Rat Yes 6.1 IC50 = 790 nM Funct
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
424 2 0 2 4.4 Clc1ccc(cc1)[C@]12N(CCN1C(=O)c1c2cccc1)C(=O)c1ccc(c(c1)F)F
CHEMBL1083723 acm5_human Human No 6.1 IC50 = 794.3 nM Bind
Inhibition of human muscarinic M5 receptor expressed in CHO cellsInhibition of human muscarinic M5 receptor expressed in CHO cells
342 4 2 2 4.0 Cc1ccc(-c2ccccc2C(=O)NCC2CCNCC2)cc1Cl
CHEMBL3361319 acm5_human Human No 6.1 IC50 = 794.3 nM Funct
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
446 4 0 3 4.9 CC(C)Oc1ccc(C(=O)N2CCN3C(=O)c4ccccc4C23c2ccc(Cl)cc2)cc1
CHEMBL629 acm5_human Human Yes 8.1 IC50 = 8.0 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C
CHEMBL1626 acm5_human Human Yes 8.1 IC50 = 8.4 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C
CHEMBL7634 acm5_human Human Yes 5.1 IC50 = 8000 nM Bind
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
206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1
CHEMBL2164905 acm5_human Human No 7.1 IC50 = 82 nM Funct
Antagonist activity at human muscarinic M5 receptor by calcium mobilization assayAntagonist activity at human muscarinic M5 receptor by calcium mobilization assay
326 4 0 2 2.9 CN1CCN(C(=O)[C@@](F)(Cc2ccccc2)c2ccccc2)CC1
CHEMBL4062351 acm5_human Human No 5.1 IC50 = 8210 nM Funct
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
521 3 0 3 5.3 O=C(c1ccc(F)c(F)c1)N1CCN2C(=O)c3ccccc3[C@@]12c1ccc(N2CCc3ccccc3C2)cc1
CHEMBL300987 acm5_human Human No 5.1 IC50 = 8211.3 nM Bind
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
392 3 1 5 4.1 CCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2ccc(OC)cc2C1O3
CHEMBL1090094 acm5_human Human No 6.1 IC50 = 830 nM Funct
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
433 4 1 3 4.4 CCN1CCN(c2ccc(NC(=O)c3c(F)c(F)c(F)c(F)c3F)cc2Cl)CC1
CHEMBL1184120 acm5_human Human No 6.1 IC50 = 842 nM Bind
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
363 8 0 3 4.7 CCN1CCC(c2ccccc2)=C(C(=O)OCCCCc2ccccc2)C1
CHEMBL333125 acm5_human Human No 6.1 IC50 = 842 nM Bind
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
363 8 0 3 4.7 CCN1CCC(c2ccccc2)=C(C(=O)OCCCCc2ccccc2)C1
CHEMBL121059 acm5_human Human No 7.1 IC50 = 85.4 nM Bind
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
357 11 0 3 5.5 CCCCCCCCCOC(=O)C1=C(c2ccccc2)CCN(CC)C1
CHEMBL3361318 acm5_human Human No 6.1 IC50 = 850 nM Funct
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
432 4 0 3 4.6 CCOc1ccc(C(=O)N2CCN3C(=O)c4ccccc4C23c2ccc(Cl)cc2)cc1
CHEMBL3361318 acm5_human Human No 6.1 IC50 = 851.1 nM Funct
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
432 4 0 3 4.6 CCOc1ccc(C(=O)N2CCN3C(=O)c4ccccc4C23c2ccc(Cl)cc2)cc1
CHEMBL1113 acm5_human Human Yes 6.1 IC50 = 856 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1
CHEMBL6445 acm5_rat Rat No 6.1 IC50 = 860 nM Bind
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
264 1 1 2 2.8 c1ccc(C2CN3CCNCC3c3ccccc32)cc1
CHEMBL584 acm5_human Human Yes 4.1 IC50 = 86074 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
567 9 4 6 4.7 Cc1c(O)cccc1C(=O)N[C@@H](CSc1ccccc1)[C@H](O)CN1C[C@H]2CCCC[C@H]2C[C@H]1C(=O)NC(C)(C)C
CHEMBL62247 acm5_human Human No 5.1 IC50 = 8624 nM Bind
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
406 4 1 5 4.5 CCOC(=O)c1c(C)[nH]c2ccc3c(c12)CN1CCc2cc(OCC)ccc2C1O3
CHEMBL1180343 acm5_human Human No 6.1 IC50 = 865.9 nM Bind
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
365 7 0 4 4.0 CCN1CCC(c2ccccc2)=C(C(=O)OCCc2ccc(OC)cc2)C1
CHEMBL123099 acm5_human Human No 6.1 IC50 = 865.9 nM Bind
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
365 7 0 4 4.0 CCN1CCC(c2ccccc2)=C(C(=O)OCCc2ccc(OC)cc2)C1
CHEMBL1180343 acm5_human Human No 6.1 IC50 = 866 nM Bind
Binding affinity to human M5 muscarinic receptor expressed in cell membranes by radioligand binding assayBinding affinity to human M5 muscarinic receptor expressed in cell membranes by radioligand binding assay
365 7 0 4 4.0 CCN1CCC(c2ccccc2)=C(C(=O)OCCc2ccc(OC)cc2)C1
CHEMBL123099 acm5_human Human No 6.1 IC50 = 866 nM Bind
Binding affinity to human M5 muscarinic receptor expressed in cell membranes by radioligand binding assayBinding affinity to human M5 muscarinic receptor expressed in cell membranes by radioligand binding assay
365 7 0 4 4.0 CCN1CCC(c2ccccc2)=C(C(=O)OCCc2ccc(OC)cc2)C1
CHEMBL4059751 acm5_human Human No 5.1 IC50 = 8709.6 nM Funct
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
546 4 0 5 4.1 CCOC(=O)N1CCN(c2ccc([C@@]34c5ccccc5C(=O)N3CCN4C(=O)c3ccc(F)c(F)c3)cc2)CC1
CHEMBL1200604 acm5_human Human Yes 7.1 IC50 = 89 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1
CHEMBL479 acm5_human Human Yes 8.0 IC50 = 9.2 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1
CHEMBL6459 acm5_rat Rat No 6.1 IC50 = 900 nM Bind
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
312 1 0 2 3.8 CN1CCN2CC(c3ccc(Cl)cc3)c3ccccc3C2C1
CHEMBL3353280 acm5_human Human No 6.1 IC50 = 900 nM Funct
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
452 3 0 3 4.2 COc1cc(C23c4ccccc4C(=O)N2CCN3C(=O)c2cc(F)c(F)c(F)c2)ccc1C
CHEMBL4059751 acm5_human Human No 5.0 IC50 = 9490 nM Funct
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
546 4 0 5 4.1 CCOC(=O)N1CCN(c2ccc([C@@]34c5ccccc5C(=O)N3CCN4C(=O)c3ccc(F)c(F)c3)cc2)CC1
CHEMBL2112589 acm5_human Human No 7.0 IC50 = 96.8 nM Bind
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
337 6 0 3 3.9 CCN1CC[C@@H](c2ccccc2)[C@H](C(=O)OCCc2ccccc2)C1
CHEMBL2219563 acm5_human Human No 7.0 IC50 = 96.8 nM Bind
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
337 6 0 3 3.9 CCN1CC[C@@H](c2ccccc2)[C@H](C(=O)OCCc2ccccc2)C1
CHEMBL3353277 acm5_rat Rat No 6.0 IC50 = 963 nM Funct
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 Fluo4AM 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 Fluo4AM staining-based fluorescence assay
452 3 0 3 4.2 COc1ccc(C23c4ccccc4C(=O)N2CCN3C(=O)c2cc(F)c(F)c(F)c2)cc1C
CHEMBL1180284 acm5_human Human No 6.0 IC50 = 977 nM Bind
Binding affinity to human M5 muscarinic receptor expressed in cell membranes by radioligand binding assayBinding affinity to human M5 muscarinic receptor expressed in cell membranes by radioligand binding assay
245 3 0 3 2.3 CCN1CCC(c2ccccc2)=C(C(=O)OC)C1
CHEMBL120109 acm5_human Human No 6.0 IC50 = 977 nM Bind
Binding affinity to human M5 muscarinic receptor expressed in cell membranes by radioligand binding assayBinding affinity to human M5 muscarinic receptor expressed in cell membranes by radioligand binding assay
245 3 0 3 2.3 CCN1CCC(c2ccccc2)=C(C(=O)OC)C1
CHEMBL1180284 acm5_human Human No 6.0 IC50 = 977.3 nM Bind
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
245 3 0 3 2.3 CCN1CCC(c2ccccc2)=C(C(=O)OC)C1
CHEMBL120109 acm5_human Human No 6.0 IC50 = 977.3 nM Bind
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
245 3 0 3 2.3 CCN1CCC(c2ccccc2)=C(C(=O)OC)C1
CHEMBL1900528 acm5_human Human No 10.6 Ki = 0.0 nM Bind
Displacement of [3H]-NMS from human recombinant M5 receptor expressed in CHO cells after 24 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M5 receptor expressed in CHO cells after 24 hrs by filter binding assay
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
CHEMBL3545181 acm5_human Human No 10.6 Ki = 0.0 nM Bind
Displacement of [3H]-NMS from human recombinant M5 receptor expressed in CHO cells after 24 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M5 receptor expressed in CHO cells after 24 hrs by filter binding assay
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
CHEMBL4440620 acm5_human Human No 10.6 Ki = 0.0 nM Bind
Displacement of [3H]-NMS from human recombinant M5 receptor expressed in CHO cells after 24 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M5 receptor expressed in CHO cells after 24 hrs by filter binding assay
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
CHEMBL1182201 acm5_human Human No 10.0 Ki = 0.1 nM Bind
Binding affinity to human cloned muscarinic receptor M5 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M5 expressed in CHO cells
346 3 0 2 4.8 C[N+]1(C)CCC[C@H]1[C@H]1CS[C@@](c2ccccc2)(C2CCCCC2)O1
CHEMBL219786 acm5_human Human No 10.0 Ki = 0.1 nM Bind
Binding affinity to human cloned muscarinic receptor M5 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M5 expressed in CHO cells
346 3 0 2 4.8 C[N+]1(C)CCC[C@H]1[C@H]1CS[C@@](c2ccccc2)(C2CCCCC2)O1
CHEMBL2449003 acm5_human Human Yes 9.9 Ki = 0.1 nM Bind
Antagonist activity at muscarinic M5 receptor (unknown origin) by PDSP assayAntagonist activity at muscarinic M5 receptor (unknown origin) by PDSP assay
289 4 1 4 1.9 CN1[C@H]2CC[C@@H]1CC(OC(=O)[C@H](CO)c1ccccc1)C2
CHEMBL1910856 acm5_human Human Yes 9.8 Ki = 0.2 nM Bind
Displacement of [3H]-NMS from human recombinant M5 receptor expressed in CHO cells after 24 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M5 receptor expressed in CHO cells after 24 hrs by filter binding assay
444 9 2 4 4.5 CC(C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)N1CC(Oc2cccc(O)c2)C1
CHEMBL1184886 acm5_human Human No 9.7 Ki = 0.2 nM Bind
Binding affinity to human cloned muscarinic receptor M5 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M5 expressed in CHO cells
346 3 0 2 4.8 C[N+]1(C)CCC[C@H]1[C@H]1CS[C@](c2ccccc2)(C2CCCCC2)O1
CHEMBL376057 acm5_human Human No 9.7 Ki = 0.2 nM Bind
Binding affinity to human cloned muscarinic receptor M5 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M5 expressed in CHO cells
346 3 0 2 4.8 C[N+]1(C)CCC[C@H]1[C@H]1CS[C@](c2ccccc2)(C2CCCCC2)O1
CHEMBL1506225 acm5_human Human No 9.7 Ki = 0.2 nM Bind
Binding affinity to human cloned muscarinic receptor M5 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M5 expressed in CHO cells
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
CHEMBL376897 acm5_human Human No 9.7 Ki = 0.2 nM Bind
Binding affinity to human cloned muscarinic receptor M5 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M5 expressed in CHO cells
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
CHEMBL1506225 acm5_human Human No 9.7 Ki = 0.2 nM Bind
Displacement of [3H]N-methylscopolamine from human muscarinic M5 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M5 receptor expressed in CHO cells after 120 mins by scintillation counting
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
CHEMBL376897 acm5_human Human No 9.7 Ki = 0.2 nM Bind
Displacement of [3H]N-methylscopolamine from human muscarinic M5 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M5 receptor expressed in CHO cells after 120 mins by scintillation counting
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
CHEMBL1506225 acm5_human Human No 9.7 Ki = 0.2 nM Bind
Displacement of [3H]NMS from human cloned muscarinic M5 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M5 receptor expressed in CHO cells by scintillation counting
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
CHEMBL376897 acm5_human Human No 9.7 Ki = 0.2 nM Bind
Displacement of [3H]NMS from human cloned muscarinic M5 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M5 receptor expressed in CHO cells by scintillation counting
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
CHEMBL517712 acm5_human Human No 9.7 Ki = 0.2 nM Funct
Activation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as increase in acetylcholine potency at 30 uM by calcium mobilization-based ACh concentration-response curve assay relative to controlActivation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as increase in acetylcholine potency at 30 uM by calcium mobilization-based ACh concentration-response curve assay relative to control
289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C
CHEMBL168067 acm5_human Human Yes 9.7 Ki = 0.2 nM Bind
Binding affinity to human muscarinic M5 receptor by radioligand displacement assayBinding affinity to human muscarinic M5 receptor by radioligand displacement assay
324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C
CHEMBL1201024 acm5_human Human No 9.5 Ki = 0.3 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
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
CHEMBL1201268 acm5_human Human No 9.5 Ki = 0.3 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
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
CHEMBL2449003 acm5_human Human Yes 9.5 Ki = 0.3 nM Bind
Displacement of [3H]QNB from muscarinic M5 receptor (unknown origin)Displacement of [3H]QNB from muscarinic M5 receptor (unknown origin)
289 4 1 4 1.9 CN1[C@H]2CC[C@@H]1CC(OC(=O)[C@H](CO)c1ccccc1)C2
CHEMBL2449003 acm5_human Human Yes 9.5 Ki = 0.3 nM Bind
Displacement of [3H]QNB from muscarinic M5 receptor (unknown origin)Displacement of [3H]QNB from muscarinic M5 receptor (unknown origin)
289 4 1 4 1.9 CN1[C@H]2CC[C@@H]1CC(OC(=O)[C@H](CO)c1ccccc1)C2
CHEMBL517712 acm5_human Human No 9.4 Ki = 0.4 nM Bind
Displacement of [3H]QNB from muscarinic acetylcholine M5 receptor after 1.5 hrs by scintillation countingDisplacement of [3H]QNB from muscarinic acetylcholine M5 receptor after 1.5 hrs by scintillation counting
289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C
CHEMBL1184884 acm5_human Human No 9.4 Ki = 0.4 nM Bind
Binding affinity to human cloned muscarinic receptor M5 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M5 expressed in CHO cells
340 3 0 2 4.3 C[N+]1(C)CCC[C@H]1[C@H]1CSC(c2ccccc2)(c2ccccc2)O1
CHEMBL375969 acm5_human Human No 9.4 Ki = 0.4 nM Bind
Binding affinity to human cloned muscarinic receptor M5 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M5 expressed in CHO cells
340 3 0 2 4.3 C[N+]1(C)CCC[C@H]1[C@H]1CSC(c2ccccc2)(c2ccccc2)O1
CHEMBL168067 acm5_human Human Yes 9.4 Ki = 0.4 nM Bind
Displacement of radiolabeled 4DAMP from human muscarinic M5 receptorDisplacement of radiolabeled 4DAMP from human muscarinic M5 receptor
324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C
CHEMBL168067 acm5_human Human Yes 9.3 Ki = 0.5 nM Bind
Displacement of [3H]4-DAMP from human recombinant M5 receptor expressed in CHO cellsDisplacement of [3H]4-DAMP from human recombinant M5 receptor expressed in CHO cells
324 4 0 2 3.6 O=C(C(c1ccccc1)c1ccccc1)OC1CC[N+](CC1)(C)C
CHEMBL517712 acm5_human Human No 9.3 Ki = 0.5 nM Bind
Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M5Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M5
289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C
CHEMBL517712 acm5_human Human No 9.2 Ki = 0.6 nM Bind
Displacement of [3H]NMS from human M5 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M5 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C
CHEMBL4645580 acm5_human Human No 9.2 Ki = 0.7 nM Bind
Displacement of [3H]NMS from human recombinant muscarinic receptor M5 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M5 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
318 4 0 2 3.6 C[N+](C)(C)C[C@H]1COC[C@@](c2ccccc2)(C2CCCCC2)O1
CHEMBL4651099 acm5_human Human No 9.2 Ki = 0.7 nM Bind
Displacement of [3H]NMS from human recombinant muscarinic receptor M5 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M5 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
318 4 0 2 3.6 C[N+](C)(C)C[C@H]1COC[C@@](c2ccccc2)(C2CCCCC2)O1
CHEMBL517712 acm5_human Human No 9.2 Ki = 0.7 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C
CHEMBL1182214 acm5_human Human No 9.1 Ki = 0.8 nM Bind
Binding affinity to human cloned muscarinic receptor M5 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M5 expressed in CHO cells
346 3 0 2 4.8 C[N+]1(C)CCC[C@@H]1[C@@H]1CS[C@@](c2ccccc2)(C2CCCCC2)O1
CHEMBL222259 acm5_human Human No 9.1 Ki = 0.8 nM Bind
Binding affinity to human cloned muscarinic receptor M5 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M5 expressed in CHO cells
346 3 0 2 4.8 C[N+]1(C)CCC[C@@H]1[C@@H]1CS[C@@](c2ccccc2)(C2CCCCC2)O1
CHEMBL517712 acm5_rat Rat No 9.1 Ki = 0.9 nM Bind
Displacement of [3H]NMS from rat recombinant muscarinic M5 receptor expressed in CHO cells after 2 hrs by microplate scintillation countingDisplacement of [3H]NMS from rat recombinant muscarinic M5 receptor expressed in CHO cells after 2 hrs by microplate scintillation counting
289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C
CHEMBL517712 acm5_human Human No 9.0 Ki = 1 nM Bind
Displacement of [3H]-4-DAMP from human muscarinic M5 receptor expressed in BHK-21 cellsDisplacement of [3H]-4-DAMP from human muscarinic M5 receptor expressed in BHK-21 cells
289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C
CHEMBL1464005 acm5_human Human No 9.0 Ki = 1.0 nM Bind
Displacement of [3H]-NMS from human recombinant M5 receptor expressed in CHO cells after 24 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M5 receptor expressed in CHO cells after 24 hrs by filter binding assay
332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2
CHEMBL1621597 acm5_human Human No 9.0 Ki = 1.0 nM Bind
Displacement of [3H]-NMS from human recombinant M5 receptor expressed in CHO cells after 24 hrs by filter binding assayDisplacement of [3H]-NMS from human recombinant M5 receptor expressed in CHO cells after 24 hrs by filter binding assay
332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2
CHEMBL3629360 acm5_human Human No 9.0 Ki = 1.1 nM Bind
Antagonist activity at muscarinic M5 receptor (unknown origin)Antagonist activity at muscarinic M5 receptor (unknown origin)
704 14 5 9 5.5 O=c1ccc2c([C@@H](O)CNCCc3ccc(CCN4CCC(Cn5cnc([C@](O)(c6ccccc6)C6CCCCC6)n5)CC4)cc3)ccc(O)c2[nH]1
CHEMBL1506225 acm5_human Human No 9.0 Ki = 1.1 nM Bind
Displacement of [3H]-NMS from wild-type human muscarinic M5 receptor expressed in CHO-K1 cells by liquid scintillation countingDisplacement of [3H]-NMS from wild-type human muscarinic M5 receptor expressed in CHO-K1 cells by liquid scintillation counting
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
CHEMBL376897 acm5_human Human No 9.0 Ki = 1.1 nM Bind
Displacement of [3H]-NMS from wild-type human muscarinic M5 receptor expressed in CHO-K1 cells by liquid scintillation countingDisplacement of [3H]-NMS from wild-type human muscarinic M5 receptor expressed in CHO-K1 cells by liquid scintillation counting
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
CHEMBL219825 acm5_human Human No 8.9 Ki = 1.2 nM Bind
Binding affinity to human cloned muscarinic receptor M5 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M5 expressed in CHO cells
331 3 0 3 4.6 CN1CCC[C@@H]1[C@@H]1CS[C@@](c2ccccc2)(C2CCCCC2)O1
CHEMBL1187846 acm5_human Human No 8.9 Ki = 1.3 nM Bind
Displacement of [3H]-NMS from wild-type human muscarinic M5 receptor expressed in CHO-K1 cells by liquid scintillation countingDisplacement of [3H]-NMS from wild-type human muscarinic M5 receptor expressed in CHO-K1 cells by liquid scintillation counting
303 4 1 5 0.9 CN1[C@H]2C[C@H](OC(=O)[C@H](CO)c3ccccc3)C[C@@H]1[C@@H]1O[C@H]12
CHEMBL385328 acm5_human Human No 8.9 Ki = 1.3 nM Bind
Binding affinity to human cloned muscarinic receptor M5 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M5 expressed in CHO cells
331 3 0 3 4.6 CN1CCC[C@H]1[C@H]1CS[C@@](c2ccccc2)(C2CCCCC2)O1
CHEMBL1201203 acm5_human Human Yes 8.8 Ki = 1.5 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1
CHEMBL438151 acm5_human Human Yes 8.8 Ki = 1.5 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1
CHEMBL517712 acm5_human Human No 8.8 Ki = 1.5 nM Bind
Displacement of [3H]NMS from human muscarinic acetylcholine receptor subtype 5 expressed in CHO cell membranes by scintillation counting methodDisplacement of [3H]NMS from human muscarinic acetylcholine receptor subtype 5 expressed in CHO cell membranes by scintillation counting method
289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C
CHEMBL4635500 acm5_human Human No 8.8 Ki = 1.5 nM Bind
Displacement of [3H]NMS from human recombinant muscarinic receptor M5 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M5 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
303 4 0 3 3.4 CN(C)C[C@H]1COC[C@@](c2ccccc2)(C2CCCCC2)O1
CHEMBL1197382 acm5_human Human No 8.8 Ki = 1.5 nM Bind
Displacement of [3H]NMS from human cloned muscarinic M5 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M5 receptor expressed in CHO cells by scintillation counting
354 4 1 2 5.0 C[N+]1(C)CCC[C@@H]1c1ccc([C@](O)(c2ccccc2)C2CCCCC2)o1
CHEMBL569307 acm5_human Human No 8.8 Ki = 1.5 nM Bind
Displacement of [3H]NMS from human cloned muscarinic M5 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]NMS from human cloned muscarinic M5 receptor expressed in CHO cells by scintillation counting
354 4 1 2 5.0 C[N+]1(C)CCC[C@@H]1c1ccc([C@](O)(c2ccccc2)C2CCCCC2)o1
CHEMBL71124 acm5_human Human No 8.8 Ki = 1.7 nM Bind
The compound was tested for the binding affinity against Muscarinic acetylcholine receptor M5The compound was tested for the binding affinity against Muscarinic acetylcholine receptor M5
425 6 0 3 6.0 COc1ccc([S+]([O-])c2ccc(C(C)C3CCN(C4CCCCC4)CC3)cc2)cc1
CHEMBL2042405 acm5_human Human No 8.8 Ki = 1.7 nM Bind
Displacement of [3H]N-methylscopolamine from human muscarinic M5 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M5 receptor expressed in CHO cells after 120 mins by scintillation counting
312 4 0 2 3.1 C[N+](C)(C)C[C@H]1COCC(c2ccccc2)(c2ccccc2)O1
CHEMBL2079009 acm5_human Human No 8.8 Ki = 1.7 nM Bind
Displacement of [3H]N-methylscopolamine from human muscarinic M5 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M5 receptor expressed in CHO cells after 120 mins by scintillation counting
312 4 0 2 3.1 C[N+](C)(C)C[C@H]1COCC(c2ccccc2)(c2ccccc2)O1
CHEMBL1123 acm5_human Human Yes 8.8 Ki = 1.7 nM Bind
DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC
CHEMBL4519301 acm5_human Human No 8.7 Ki = 1.8 nM Bind
Displacement of [3H]NMS from human M5 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M5 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
368 5 0 3 4.1 O=C(OC1CN2CCC1CC2)N(CCc1ccc(F)cc1)c1ccccc1
CHEMBL2449003 acm5_rat Rat Yes 8.7 Ki = 1.8 nM Bind
Displacement of [3H]NMS from rat muscarinic M5 receptor expressed in CHO cellsDisplacement of [3H]NMS from rat muscarinic M5 receptor expressed in CHO cells
289 4 1 4 1.9 CN1[C@H]2CC[C@@H]1CC(OC(=O)[C@H](CO)c1ccccc1)C2
CHEMBL2042553 acm5_human Human No 8.7 Ki = 1.8 nM Bind
Displacement of [3H]N-methylscopolamine from human muscarinic M5 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M5 receptor expressed in CHO cells after 120 mins by scintillation counting
297 4 0 3 2.9 CN(C)C[C@H]1COCC(c2ccccc2)(c2ccccc2)O1
CHEMBL2078942 acm5_human Human No 8.7 Ki = 1.8 nM Bind
Displacement of [3H]N-methylscopolamine from human muscarinic M5 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]N-methylscopolamine from human muscarinic M5 receptor expressed in CHO cells after 120 mins by scintillation counting
297 4 0 3 2.9 CN(C)C[C@H]1COCC(c2ccccc2)(c2ccccc2)O1
CHEMBL2042553 acm5_human Human No 8.7 Ki = 1.8 nM Bind
Displacement of [3H]NMS from recombinant human muscarinic M5 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M5 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
297 4 0 3 2.9 CN(C)C[C@H]1COCC(c2ccccc2)(c2ccccc2)O1
CHEMBL2078942 acm5_human Human No 8.7 Ki = 1.8 nM Bind
Displacement of [3H]NMS from recombinant human muscarinic M5 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting methodDisplacement of [3H]NMS from recombinant human muscarinic M5 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
297 4 0 3 2.9 CN(C)C[C@H]1COCC(c2ccccc2)(c2ccccc2)O1
CHEMBL376255 acm5_human Human No 8.7 Ki = 2.0 nM Bind
Binding affinity to human cloned muscarinic receptor M5 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M5 expressed in CHO cells
331 3 0 3 4.6 CN1CCC[C@H]1[C@H]1CS[C@](c2ccccc2)(C2CCCCC2)O1
CHEMBL376870 acm5_human Human No 8.7 Ki = 2.0 nM Bind
Binding affinity to human cloned muscarinic receptor M5 expressed in CHO cellsBinding affinity to human cloned muscarinic receptor M5 expressed in CHO cells
331 3 0 3 4.6 CN1CCC[C@@H]1[C@@H]1CS[C@](c2ccccc2)(C2CCCCC2)O1
CHEMBL715 acm5_human Human Yes 8.0 Ki = 10 nM Bind
Binding affinity to M5 receptor (unknown origin) by PDSP assayBinding affinity to M5 receptor (unknown origin) by PDSP assay
312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C
CHEMBL4585326 acm5_human Human No 8.0 Ki = 10 nM Bind
Displacement of [3H]NMS from human M5 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M5 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
380 6 0 4 4.0 COc1ccc(CCN(C(=O)OC2CN3CCC2CC3)c2ccccc2)cc1
CHEMBL4742721 acm5_human Human No 8.0 Ki = 10 nM Bind
Displacement of [3H]NMS from human recombinant muscarinic receptor M5 expressed in CHO-K1 cell membranes measured after 3 hrs by radioligand competition binding assayDisplacement of [3H]NMS from human recombinant muscarinic receptor M5 expressed in CHO-K1 cell membranes measured after 3 hrs by radioligand competition binding assay
1117 25 4 11 9.5 O=C(CCCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1)NCCNC(=O)CCc1cn(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)cn1
CHEMBL4802414 acm5_human Human No 8.0 Ki = 10 nM Bind
Displacement of [3H]NMS from human recombinant muscarinic receptor M5 expressed in CHO-K1 cell membranes measured after 3 hrs by radioligand competition binding assayDisplacement of [3H]NMS from human recombinant muscarinic receptor M5 expressed in CHO-K1 cell membranes measured after 3 hrs by radioligand competition binding assay
1117 25 4 11 9.5 O=C(CCCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1)NCCNC(=O)CCc1cn(CCCCC2CCN(CC(=O)N3c4ccccc4NC(=O)c4ccccc43)CC2)cn1
CHEMBL42 acm5_human Human Yes 7.0 Ki = 100 nM Bind
Binding affinity to M5 receptor (unknown origin) by PDSP assayBinding affinity to M5 receptor (unknown origin) by PDSP assay
326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2
CHEMBL4577453 acm5_human Human No 7.0 Ki = 100 nM Bind
Displacement of [3H]NMS from human M5 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry methodDisplacement of [3H]NMS from human M5 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method
400 6 0 3 4.6 O=C(OCCCc1ccc(F)c(F)c1)N(c1ccccc1)C1CN2CCC1CC2
CHEMBL376295 acm5_human Human No 7.0 Ki = 100 nM Bind
Inhibition of [3H](R)-QNB binding to human M5 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M5 receptor expressed in A9 L cells
467 16 0 12 3.1 COc1nsnc1OCCCOCCCOCCCOc1nsnc1-c1cccnc1
CHEMBL386983 acm5_human Human No 7.0 Ki = 100 nM Bind
Inhibition of [3H](R)-QNB binding to human M5 receptor expressed in A9 L cellsInhibition of [3H](R)-QNB binding to human M5 receptor expressed in A9 L cells
531 19 0 14 1.6 COc1nsnc1OCCOCCOCCOCCOCCOc1nsnc1C1=CCCN(C)C1
CHEMBL608151 acm5_human Human No 7.0 Ki = 100 nM Bind
Inhibition of muscarinic M5 receptorInhibition of muscarinic M5 receptor
285 4 1 2 3.1 CCOC[C@H]1[C@@H]2CNC[C@@]21c1ccc(Cl)c(Cl)c1
CHEMBL4633679 acm5_human Human No 6.0 Ki = 1000 nM Bind
Displacement of [3H]NMS from human recombinant muscarinic receptor M5 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M5 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
344 5 0 3 4.0 C[N+](C)(C)C[C@@H]1CO[C@H](c2ccc(Sc3ccccc3)cc2)CO1
CHEMBL4650842 acm5_human Human No 6.0 Ki = 1000 nM Bind
Displacement of [3H]NMS from human recombinant muscarinic receptor M5 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]NMS from human recombinant muscarinic receptor M5 expressed in CHO-K1 cell membranes incubated for 2 hrs by scintillation counting method
344 5 0 3 4.0 C[N+](C)(C)C[C@@H]1CO[C@H](c2ccc(Sc3ccccc3)cc2)CO1
CHEMBL1834350 acm5_human Human No 5.0 Ki = 10000 nM Bind
Inhibition of human muscarinic M5 receptorInhibition of human muscarinic M5 receptor
383 3 2 4 1.7 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC2(C=N1)CCNCC2
CHEMBL3354066 acm5_human