Initializing potency table...
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 | = | 749.00 | 6.13 | -144 | 27 | DRUGMATRIX: Muscarinic M5 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 | = | 1043.00 | 5.98 | -144 | 27 | DRUGMATRIX: Muscarinic M5 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 | AC50 | = | 6117.70 | 5.21 | -144 | 27 | Binding affinity towards human CHRM5 in an in vitro assay with cellular components measured by membrane filtration | ChEMBL | 274.1 | 5 | 0 | 2 | 3.82 | CN(C)CC[C@@H](c1ccc(Cl)cc1)c1ccccn1 | https://dx.doi.org/10.1038/s41467-023-40064-9 | |
(+)-chlorpheniramine | 918 | None | 42 | Human | Binding | pKi | = | 6.13 | 8.21 | -144 | 27 | DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine) | Drug Central | 274.1 | 5 | 0 | 2 | 3.82 | CN(C)CC[C@@H](c1ccc(Cl)cc1)c1ccccn1 | - | |
(-)-stepholidine | 3691 | 3H-QNB | 40 | Human | Binding | pKi | = | 10000.00 | 5.00 | -2290 | 35 | - | PDSP KiDatabase | 327.1 | 2 | 2 | 5 | 2.77 | COc1cc2c(cc1O)[C@@H]1Cc3ccc(O)c(OC)c3CN1CC2 | - | |
(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 | = | 75.86 | 7.12 | -2 | 5 | - | PDSP KiDatabase | 311.2 | 3 | 1 | 2 | 3.94 | OC(C#CCN1CCCCC1)(c1ccccc1)C1CCCCC1 | - | |
(R)-Hexbutinol | 218743 | 3H-NMS | 0 | Human | Binding | pKi | = | 5.50 | 8.26 | -2 | 5 | - | PDSP KiDatabase | 311.2 | 3 | 1 | 2 | 3.94 | OC(C#CCN1CCCCC1)(c1ccccc1)C1CCCCC1 | - | |
(S)-(+)-DIMETHINDENE | 199081 | None | 3 | Human | Binding | Ki | = | 2691.53 | 5.57 | -6456 | 6 | Binding affinity towards cloned human muscarinic acetylcholine receptor M5 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 | = | - | 6.12 | -25 | 7 | Binding to hM5 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 | = | 758.58 | 6.12 | -25 | 7 | Binding affinity towards cloned human muscarinic acetylcholine receptor M5 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 | |
3,3'-difluorobenzaldazine | 91 | None | 30 | Human | Binding | EC50 | = | 2600.00 | 5.58 | - | 2 | Positive allosteric modulator activity at human muscarinic acetylcholine receptor M5 expressed in CHO cells by fluorometric imaging plate reader | ChEMBL | 244.1 | 3 | 0 | 2 | 3.42 | Fc1cccc(/C=N/N=C/c2cccc(F)c2)c1 | https://dx.doi.org/10.1021/jm5011786 | |
3-quinuclidinyl-benzilate | 112 | None | 21 | Human | Binding | pKd | = | - | 10.46 | -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 | 10.37 | -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 | = | 0.07 | 10.19 | -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 | = | - | 9.00 | -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 | = | 1.05 | 8.98 | -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 | None | 5 | Human | Binding | IC50 | = | 0.32 | 9.49 | -1 | 12 | Displacement of [3H]4-DAMP from human recombinant M5 receptor expressed in CHO cells measured after 60 mins by scintillation counting method | ChEMBL | 324.2 | 4 | 0 | 2 | 3.60 | C[N+]1(C)CCC(OC(=O)C(c2ccccc2)c2ccccc2)CC1 | https://dx.doi.org/10.1016/j.bmc.2016.11.014 | |
4-DAMP | 116 | None | 5 | Human | Binding | IC50 | = | 0.32 | 9.49 | -1 | 12 | Displacement of [3H]4-DAMP from human recombinant muscarinic M5 receptor expressed in CHO cells | ChEMBL | 324.2 | 4 | 0 | 2 | 3.60 | C[N+]1(C)CCC(OC(=O)C(c2ccccc2)c2ccccc2)CC1 | https://dx.doi.org/10.1016/j.bmc.2016.03.006 | |
4-DAMP | 116 | None | 5 | Human | Binding | Ki | = | 0.48 | 9.32 | -1 | 12 | Displacement of [3H]4-DAMP from human recombinant M5 receptor expressed in CHO cells | ChEMBL | 324.2 | 4 | 0 | 2 | 3.60 | C[N+]1(C)CCC(OC(=O)C(c2ccccc2)c2ccccc2)CC1 | https://dx.doi.org/10.1021/jm401895u |
Showing 1 to 20 of 1,439 entries
Ligands | Receptor | Activity | Chemical information | ||||||||||||||||||
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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 | |