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Ligand source activities (1 row/activity)
Ligands | Receptor | Activity | Chemical information | ||||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Common name | GPCRdb ID | Reference ligand | Vendors | Species | Assay Type | Activity Type | Activity Relation | Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description | Source | Mol weight | Rot Bonds | H don | H acc | LogP | Smiles | DOI | |
Ligands | Receptor | Activity | Chemical information | ||||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Common name | GPCRdb ID | Reference ligand | Vendors | Species | Assay Type | Activity Type | Activity Relation | Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description | Source | Mol weight | Rot Bonds | H don | H acc | LogP | Smiles | DOI | |
(+)-chlorpheniramine | 918 | None | 42 | Human | Binding | Ki | = | 276.00 | 6.56 | -91 | 27 | DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine) | ChEMBL | 274.1 | 5 | 0 | 2 | 3.82 | CN(C)CC[C@@H](c1ccc(Cl)cc1)c1ccccn1 | - | |
(+)-chlorpheniramine | 918 | None | 42 | Human | Binding | IC50 | = | 1976.00 | 5.70 | -91 | 27 | DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine) | ChEMBL | 274.1 | 5 | 0 | 2 | 3.82 | CN(C)CC[C@@H](c1ccc(Cl)cc1)c1ccccn1 | - | |
(+)-chlorpheniramine | 918 | None | 42 | Human | Binding | pKi | = | 6.56 | 8.18 | -91 | 27 | DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine) | Drug Central | 274.1 | 5 | 0 | 2 | 3.82 | CN(C)CC[C@@H](c1ccc(Cl)cc1)c1ccccn1 | - | |
(1R,2S)-PHENYLPROPANOLAMINE | 27120 | 3H-QNB | 13 | Human | Binding | pKi | = | 10000.00 | 5.00 | -38 | 42 | - | PDSP KiDatabase | 151.1 | 2 | 2 | 2 | 1.07 | C[C@H](N)[C@H](O)c1ccccc1 | - | |
(R)-Hexbutinol | 218743 | 3H-NMS | 0 | Human | Binding | pKi | = | 19.50 | 7.71 | -1 | 5 | - | PDSP KiDatabase | 311.2 | 3 | 1 | 2 | 3.94 | OC(C#CCN1CCCCC1)(c1ccccc1)C1CCCCC1 | - | |
(R)-Hexbutinol | 218743 | 3H-NMS | 0 | Human | Binding | pKi | = | 3.02 | 8.52 | -1 | 5 | - | PDSP KiDatabase | 311.2 | 3 | 1 | 2 | 3.94 | OC(C#CCN1CCCCC1)(c1ccccc1)C1CCCCC1 | - | |
(S)-(+)-DIMETHINDENE | 199081 | None | 3 | Human | Binding | Ki | = | 3890.45 | 5.41 | -9332 | 6 | Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine | ChEMBL | 292.2 | 5 | 0 | 2 | 4.15 | C[C@H](C1=C(CCN(C)C)Cc2ccccc21)c1ccccn1 | https://dx.doi.org/10.1021/jm020895l | |
(S)-dimetindene | 3566 | None | 10 | Human | Binding | pKi | = | - | 6.53 | -9 | 7 | Binding to hM4 receptors expressed in CHO cells. | Guide to Pharmacology | 292.2 | 5 | 0 | 2 | 4.15 | C[C@@H](C1=C(CCN(C)C)Cc2ccccc21)c1ccccn1 | https://pubmed.ncbi.nlm.nih.gov/12593665 | |
(S)-dimetindene | 3566 | None | 10 | Human | Binding | Ki | = | 295.12 | 6.53 | -9 | 7 | Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine | ChEMBL | 292.2 | 5 | 0 | 2 | 4.15 | C[C@@H](C1=C(CCN(C)C)Cc2ccccc21)c1ccccn1 | https://dx.doi.org/10.1021/jm020895l | |
3-quinuclidinyl-benzilate | 112 | None | 21 | Human | Binding | pKi | = | - | 10.40 | -1 | 7 | Unclassified | Guide to Pharmacology | 337.2 | 4 | 1 | 4 | 2.56 | O=C(OC1CN2CCC1CC2)C(O)(c1ccccc1)c1ccccc1 | https://pubmed.ncbi.nlm.nih.gov/29860464 | |
3-quinuclidinyl-benzilate | 112 | None | 21 | Human | Binding | pKd | = | - | 10.10 | -1 | 7 | Unclassified | Guide to Pharmacology | 337.2 | 4 | 1 | 4 | 2.56 | O=C(OC1CN2CCC1CC2)C(O)(c1ccccc1)c1ccccc1 | https://pubmed.ncbi.nlm.nih.gov/2841607 | |
3-quinuclidinyl-benzilate | 112 | None | 21 | Human | Binding | pKd | = | - | 10.10 | -1 | 7 | Unclassified | Guide to Pharmacology | 337.2 | 4 | 1 | 4 | 2.56 | O=C(OC1CN2CCC1CC2)C(O)(c1ccccc1)c1ccccc1 | https://pubmed.ncbi.nlm.nih.gov/7562472 | |
3-quinuclidinyl-benzilate | 112 | 3H-QNB | 21 | Human | Binding | pKi | = | 0.04 | 10.43 | -1 | 7 | - | PDSP KiDatabase | 337.2 | 4 | 1 | 4 | 2.56 | O=C(OC1CN2CCC1CC2)C(O)(c1ccccc1)c1ccccc1 | - | |
3-quinuclidinyl-benzilate | 112 | 3H-QNB | 21 | Human | Binding | pKi | = | 0.03 | 10.47 | -1 | 7 | - | PDSP KiDatabase | 337.2 | 4 | 1 | 4 | 2.56 | O=C(OC1CN2CCC1CC2)C(O)(c1ccccc1)c1ccccc1 | - | |
4-DAMP | 116 | None | 5 | Human | Binding | pKi | = | - | 8.90 | -1 | 12 | Unclassified | Guide to Pharmacology | 324.2 | 4 | 0 | 2 | 3.60 | C[N+]1(C)CCC(OC(=O)C(c2ccccc2)c2ccccc2)CC1 | https://pubmed.ncbi.nlm.nih.gov/1994002 | |
4-DAMP | 116 | 3H-NMS | 5 | Human | Binding | pKi | = | 1.17 | 8.93 | -1 | 12 | - | PDSP KiDatabase | 324.2 | 4 | 0 | 2 | 3.60 | C[N+]1(C)CCC(OC(=O)C(c2ccccc2)c2ccccc2)CC1 | - | |
4-DAMP | 116 | 3H-NMS | 5 | Human | Binding | pKi | = | 1.41 | 8.85 | -1 | 12 | - | PDSP KiDatabase | 324.2 | 4 | 0 | 2 | 3.60 | C[N+]1(C)CCC(OC(=O)C(c2ccccc2)c2ccccc2)CC1 | - | |
4-DAMP | 116 | 3H-4-DAMP | 5 | Human | Binding | pKi | = | 1.26 | 8.90 | -1 | 12 | - | PDSP KiDatabase | 324.2 | 4 | 0 | 2 | 3.60 | C[N+]1(C)CCC(OC(=O)C(c2ccccc2)c2ccccc2)CC1 | - | |
4-DAMP | 116 | 3H-QNB | 5 | Human | Binding | pKi | = | 1.69 | 8.77 | -1 | 12 | - | PDSP KiDatabase | 324.2 | 4 | 0 | 2 | 3.60 | C[N+]1(C)CCC(OC(=O)C(c2ccccc2)c2ccccc2)CC1 | - | |
4-DAMP | 116 | 3H-QNB | 5 | Human | Binding | pKi | = | 0.58 | 9.24 | -1 | 12 | - | PDSP KiDatabase | 324.2 | 4 | 0 | 2 | 3.60 | C[N+]1(C)CCC(OC(=O)C(c2ccccc2)c2ccccc2)CC1 | - |
Showing 1 to 20 of 1,828 entries
Ligands | Receptor | Activity | Chemical information | ||||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Common name | GPCRdb ID | Reference ligand | Vendors | Species | Assay Type | Activity Type | Activity Relation | Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description | Source | Mol weight | Rot Bonds | H don | H acc | LogP | Smiles | DOI | |
Ligands | Receptor | Activity | Chemical information | ||||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Common name | GPCRdb ID | Reference ligand | Vendors | Species | Assay Type | Activity Type | Activity Relation | Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description | Source | Mol weight | Rot Bonds | H don | H acc | LogP | Smiles | DOI | |
(+)-aceclidine | 251 | None | 0 | Human | Functional | pEC50 | None | - | 5.40 | -7 | 5 | Unclassified | Guide to Pharmacology | 170.1 | 1 | 1 | 2 | -0.77 | CC(=O)O[C@@H]1C[NH+]2CCC1CC2 | https://pubmed.ncbi.nlm.nih.gov/8968358 | |
(-)-aceclidine | 252 | None | 0 | Human | Functional | pEC50 | None | - | 4.80 | -7 | 5 | Unclassified | Guide to Pharmacology | 170.1 | 1 | 1 | 2 | -0.77 | CC(=O)O[C@H]1C[NH+]2CCC1CC2 | https://pubmed.ncbi.nlm.nih.gov/8968358 | |
ACECLIDINE | 77355 | None | 47 | Human | Functional | pEC50 | = | 4.80 | 8.32 | 1 | 9 | None | Drug Central | 169.1 | 1 | 0 | 3 | 0.64 | CC(=O)OC1CN2CCC1CC2 | - | |
acetylcholine | 255 | None | 24 | Human | Functional | EC50 | = | 57.00 | 7.24 | 1 | 12 | Positive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as as increase in acteylcholine-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol/acetylcholine by Glosensor cAMP reagent/plate reader based luminescence assay | ChEMBL | 146.1 | 3 | 0 | 2 | 0.26 | CC(=O)OCC[N+](C)(C)C | https://dx.doi.org/10.1021/acsmedchemlett.9b00106 | |
acetylcholine | 255 | None | 24 | Human | Functional | EC50 | = | 43.00 | 7.37 | 1 | 12 | Agonist activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as decrease in isoproterenol-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol by Glosensor cAMP reagent/plate reader based luminescence assay | ChEMBL | 146.1 | 3 | 0 | 2 | 0.26 | CC(=O)OCC[N+](C)(C)C | https://dx.doi.org/10.1021/acsmedchemlett.9b00106 | |
acetylcholine | 255 | None | 24 | Human | Functional | EC50 | = | 48.80 | 7.31 | 1 | 12 | Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay | ChEMBL | 146.1 | 3 | 0 | 2 | 0.26 | CC(=O)OCC[N+](C)(C)C | https://dx.doi.org/10.1016/j.bmcl.2015.08.011 | |
acetylcholine | 255 | None | 24 | Human | Functional | EC50 | = | 10.00 | 8.00 | 1 | 12 | Agonist activity at muscarinic human M4 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining | ChEMBL | 146.1 | 3 | 0 | 2 | 0.26 | CC(=O)OCC[N+](C)(C)C | https://dx.doi.org/10.1016/j.bmcl.2012.05.048 | |
acetylcholine | 255 | None | 24 | Human | Functional | EC50 | = | 10.00 | 8.00 | 1 | 12 | Agonist activity at human muscarinic M4 receptor expressed in BHK-21 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assay | ChEMBL | 146.1 | 3 | 0 | 2 | 0.26 | CC(=O)OCC[N+](C)(C)C | https://dx.doi.org/10.1021/jm100697g | |
benzatropine | 597 | None | 17 | Human | Functional | IC50 | = | 5.01 | 8.30 | -1 | 27 | Antagonist activity at human recombinant muscarinic receptor M4 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 mins | ChEMBL | 307.2 | 4 | 0 | 2 | 4.42 | CN1[C@H]2CC[C@@H]1C[C@H](OC(c1ccccc1)c1ccccc1)C2 | https://dx.doi.org/10.1021/acsmedchemlett.0c00626 | |
carbachol | 794 | None | 13 | Human | Functional | EC50 | = | 60000.00 | 4.22 | -4 | 14 | Reversal of forskolin-stimulated accumulation of adenylate cyclase in transfected CHO cells, against Muscarinic acetylcholine receptor M4 | ChEMBL | 147.1 | 3 | 1 | 2 | -0.21 | C[N+](C)(C)CCOC(N)=O | https://dx.doi.org/10.1021/jm960683m | |
CARBACHOL | 218453 | None | 0 | Human | Functional | pEC50 | = | 7.58 | 8.12 | 1 | 12 | None | Drug Central | 182.1 | 3 | 1 | 2 | -3.21 | C[N+](C)(C)CCOC(N)=O.[Cl-] | - | |
carbachol | 794 | None | 13 | Human | Functional | EC50 | = | 290.00 | 6.54 | -4 | 14 | Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells. | ChEMBL | 147.1 | 3 | 1 | 2 | -0.21 | C[N+](C)(C)CCOC(N)=O | https://dx.doi.org/10.1021/jm0102405 | |
carbachol | 794 | None | 13 | Human | Functional | ED50 | = | 100.00 | 7.00 | -4 | 14 | Amplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M4 | ChEMBL | 147.1 | 3 | 1 | 2 | -0.21 | C[N+](C)(C)CCOC(N)=O | https://dx.doi.org/10.1021/jm960683m | |
carbachol | 794 | None | 13 | Human | Functional | IC50 | = | 50.12 | 7.30 | -4 | 14 | Activity at human M4 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation | ChEMBL | 147.1 | 3 | 1 | 2 | -0.21 | C[N+](C)(C)CCOC(N)=O | https://dx.doi.org/10.1021/jm0606995 | |
carbachol | 794 | None | 13 | Human | Functional | EC50 | = | 3981.07 | 5.40 | -4 | 14 | Agonist activity at human muscarinic M4 receptor expressed in CHO cells | ChEMBL | 147.1 | 3 | 1 | 2 | -0.21 | C[N+](C)(C)CCOC(N)=O | https://dx.doi.org/10.1016/j.bmc.2006.10.040 | |
carbachol | 794 | None | 13 | Rat | Functional | IC50 | = | 230.00 | 6.64 | -2 | 14 | Inhibitory activity against [3H]-cyclic AMP accumulation in CHO transfected cells mediated by Muscarinic acetylcholine receptor M4 | ChEMBL | 147.1 | 3 | 1 | 2 | -0.21 | C[N+](C)(C)CCOC(N)=O | https://dx.doi.org/10.1021/jm9705115 | |
cevimeline | 883 | None | 21 | Human | Functional | pEC50 | = | 5.88 | 8.23 | 1 | 5 | None | Drug Central | 199.1 | 0 | 0 | 3 | 1.56 | CC1OC2(CS1)CN1CCC2CC1 | - | |
CHEMBL1084941 | 7063 | None | 0 | Rat | Functional | EC50 | = | 2710.00 | 5.57 | -1 | 4 | PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: PAM Calcium Assay Dose-Response with M4. (Class of assay: confirmatory) | ChEMBL | 317.1 | 3 | 0 | 4 | 2.82 | Cn1cc(-c2ccc(CN3C(=O)C(=O)c4ccccc43)cc2)cn1 | - | |
CHEMBL1090096 | 7895 | None | 0 | Human | Functional | IC50 | = | 3700.00 | 5.43 | -1 | 4 | Antagonist activity at human muscarinic M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 chimeric G-protein assessed as inhibition of acetylcholine-induced calcium mobilization | ChEMBL | 411.1 | 4 | 1 | 3 | 4.75 | CCN1CCN(c2ccc(NC(=O)c3cccc(C(F)(F)F)c3)cc2Cl)CC1 | https://dx.doi.org/10.1016/j.bmcl.2010.02.041 | |
CHEMBL1090097 | 7896 | None | 0 | Human | Functional | IC50 | = | 1500.00 | 5.82 | -3 | 5 | Antagonist activity at human muscarinic M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 chimeric G-protein assessed as inhibition of acetylcholine-induced calcium mobilization | ChEMBL | 479.1 | 4 | 1 | 3 | 5.77 | CCN1CCN(c2ccc(NC(=O)c3cc(C(F)(F)F)ccc3C(F)(F)F)cc2Cl)CC1 | https://dx.doi.org/10.1016/j.bmcl.2010.02.041 |
Showing 1 to 20 of 1,019 entries