[3H]darifenacin [Ligand Id: 319] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1346 (Darifenacin, Darifenacin extended release, Enablex, UK-88525)
  • β1-adrenoceptor/Beta-1 adrenergic receptor in Human [ChEMBL: CHEMBL213] [GtoPdb: 28] [UniProtKB: P08588]
  • β1-adrenoceptor/Beta-1 adrenergic receptor in Rat [ChEMBL: CHEMBL3252] [GtoPdb: 28] [UniProtKB: P18090]
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  • β2-adrenoceptor/Beta-2 adrenergic receptor in Human [ChEMBL: CHEMBL210] [GtoPdb: 29] [UniProtKB: P07550]
  • Beta-2 adrenergic receptor in Guinea pig [ChEMBL: CHEMBL5414] [UniProtKB: Q8K4Z4]
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  • D2 receptor/Dopamine D2 receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
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  • M1 receptor/Muscarinic acetylcholine receptor M1 in Human [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
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  • M2 receptor/Muscarinic acetylcholine receptor M2 in Human [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172]
  • M2 receptor/Muscarinic acetylcholine receptor M2 in Rat [ChEMBL: CHEMBL309] [GtoPdb: 14] [UniProtKB: P10980]
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  • M3 receptor/Muscarinic acetylcholine receptor M3 in Human [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309]
  • M3 receptor/Muscarinic acetylcholine receptor M3 in Rat [ChEMBL: CHEMBL320] [GtoPdb: 15] [UniProtKB: P08483]
  • Muscarinic acetylcholine receptor M3 in Guinea pig [ChEMBL: CHEMBL5498] [UniProtKB: Q8VH26]
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  • M4 receptor/Muscarinic acetylcholine receptor M4 in Human [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173]
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  • M5 receptor/Muscarinic acetylcholine receptor M5 in Human [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912]
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  • Nav1.5/Sodium channel protein type V alpha subunit in Human [ChEMBL: CHEMBL1980] [GtoPdb: 582] [UniProtKB: Q14524]
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  • Kv7.1/Voltage-gated potassium channel, IKs; KCNQ1(Kv7.1)/KCNE1(MinK) in Human [ChEMBL: CHEMBL2221347] [GtoPdb: 560] [UniProtKB: P15382, P51787]
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  • Kv4.3/Voltage-gated potassium channel subunit Kv4.3 in Human [ChEMBL: CHEMBL1964] [GtoPdb: 554] [UniProtKB: Q9UK17]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
β1-adrenoceptor/Beta-1 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL213] [GtoPdb: 28] [UniProtKB: P08588]
ChEMBL Binding affinity to human beta1-adrenoceptor by radioligand binding assay B 6.74 pKi 180 nM Ki Bioorg. Med. Chem. Lett. (2012) 22: 6280-6285 [PMID:22932315]
ChEMBL Binding affinity to adrenergic beta1 receptor B 6.5 pIC50 316.23 nM IC50 Bioorg. Med. Chem. Lett. (2011) 21: 4612-4616 [PMID:21723724]
ChEMBL Agonist activity at adrenergic beta1 receptor F 7.4 pEC50 39.81 nM EC50 Bioorg. Med. Chem. Lett. (2011) 21: 4612-4616 [PMID:21723724]
β1-adrenoceptor/Beta-1 adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3252] [GtoPdb: 28] [UniProtKB: P18090]
ChEMBL Agonist activity at beta1 adrenoceptor in rat left atria assessed as induction of ionotropic effect F 5.64 pEC50 2310 nM EC50 Bioorg. Med. Chem. Lett. (2011) 21: 1545-1548 [PMID:21277205]
β2-adrenoceptor/Beta-2 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL210] [GtoPdb: 29] [UniProtKB: P07550]
ChEMBL Displacement of [3H]-dihydroalprenolol from human beta2-adrenoceptor expressed in HEK cells after 4 hrs B 7.21 pKi 61 nM Ki Bioorg. Med. Chem. Lett. (2011) 21: 1354-1358 [PMID:21310610]
ChEMBL Binding affinity to human beta2-adrenoceptor by radioligand binding assay B 7.8 pKi 15.9 nM Ki Bioorg. Med. Chem. Lett. (2012) 22: 6280-6285 [PMID:22932315]
ChEMBL Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins F 7.8 pEC50 15.85 nM EC50 Bioorg. Med. Chem. Lett. (2011) 21: 4612-4616 [PMID:21723724]
ChEMBL Agonist activity at beta2-adrenoceptor in human bronchial smooth-muscle cell by cAMP assay F 8.69 pEC50 2.05 nM EC50 Bioorg. Med. Chem. Lett. (2012) 22: 6280-6285 [PMID:22932315]
ChEMBL Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay F 9.09 pEC50 0.82 nM EC50 Bioorg. Med. Chem. Lett. (2011) 21: 1354-1358 [PMID:21310610]
ChEMBL Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting F 9.1 pEC50 0.79 nM EC50 J. Med. Chem. (2015) 58: 2609-2622 [PMID:25629394]
Beta-2 adrenergic receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5414] [UniProtKB: Q8K4Z4]
ChEMBL Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation F 9 pEC50 1 nM EC50 Bioorg. Med. Chem. Lett. (2011) 21: 1545-1548 [PMID:21277205]
D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
ChEMBL Binding affinity to dopamine 2 receptor B 4.6 pIC50 25118.86 nM IC50 Bioorg. Med. Chem. Lett. (2011) 21: 4612-4616 [PMID:21723724]
ChEMBL Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase in GTPgamma35S binding by scintillation proximity assay F 5 pEC50 >10000 nM EC50 Bioorg. Med. Chem. Lett. (2012) 22: 6280-6285 [PMID:22932315]
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Inhibition of rapid delayed inward rectifying potassium current (IKr) in Chinese hamster ovary (CHO) K1 cells stably expressing hERG measured using IonWorks Quattro automated patch clamp platform F 5.8 pIC50 1584.89 nM IC50 J Pharmacol Toxicol Methods (2014) 70: 246-254 [PMID:25087753]
ChEMBL Inhibition of rapid delayed inward rectifying potassium current (IKr) measured using manual patch clamp assay F 7.1 pIC50 79.43 nM IC50 J Pharmacol Toxicol Methods (2014) 70: 246-254 [PMID:25087753]
M1 receptor/Muscarinic acetylcholine receptor M1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
GtoPdb - - 8.8 pKd - - - J Recept Signal Transduct Res (1997) 17: 177-84 [PMID:9029489]
ChEMBL Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M1 B 8.26 pKi 5.5 nM Ki J. Med. Chem. (2002) 45: 984-987 [PMID:11831911]
ChEMBL Displacement of [3H]N-methylscopolamine from human muscarinic M1 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method B 8.26 pKi 5.5 nM Ki J Med Chem (2020) 63: 4349-4369 [PMID:32202101]
M2 receptor/Muscarinic acetylcholine receptor M2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172]
ChEMBL Antagonism at muscarinic M2 receptor in isolated guinea pig urinary bladder F 7.8 pKd 15.85 nM Kd Bioorg. Med. Chem. Lett. (2006) 16: 373-377 [PMID:16275087]
ChEMBL Binding affinity to human muscarinic M2 receptor B 7.3 pKi 50 nM Ki Bioorg. Med. Chem. Lett. (2006) 16: 373-377 [PMID:16275087]
ChEMBL Binding affinity (Ki) against binding of [3H]NMS to membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M2 B 7.33 pKi 47 nM Ki J. Med. Chem. (2002) 45: 984-987 [PMID:11831911]
M2 receptor/Muscarinic acetylcholine receptor M2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL309] [GtoPdb: 14] [UniProtKB: P10980]
ChEMBL Displacement of [3H]N-methylscopolamine from muscarinic M2 receptor in rat heart B 7.2 pKi 63 nM Ki Bioorg. Med. Chem. Lett. (2007) 17: 5256-5260 [PMID:17629699]
M3 receptor/Muscarinic acetylcholine receptor M3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309]
GtoPdb - - 9.5 pKd 0.32 nM Kd J Recept Signal Transduct Res (1997) 17: 177-84 [PMID:9029489]
ChEMBL Displacement of [3H]NMS from human muscarinic M3 receptor expressing CHO-K1 cells incubated for 60 mins or 6 hrs by liquid scintillation counting B 5 pKi >10000 nM Ki J. Med. Chem. (2015) 58: 2609-2622 [PMID:25629394]
ChEMBL Binding affinity to human muscarinic M3 receptor B 8.89 pKi 1.3 nM Ki Bioorg. Med. Chem. Lett. (2006) 16: 373-377 [PMID:16275087]
ChEMBL Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3 B 9.08 pKi 0.84 nM Ki J. Med. Chem. (2002) 45: 984-987 [PMID:11831911]
ChEMBL Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method B 9.13 pKi 0.74 nM Ki J Med Chem (2020) 63: 4349-4369 [PMID:32202101]
ChEMBL Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay F 7.35 pEC50 45 nM EC50 J Med Chem (2020) 63: 4349-4369 [PMID:32202101]
ChEMBL Agonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assay F 7.49 pEC50 32 nM EC50 J Med Chem (2020) 63: 4349-4369 [PMID:32202101]
ChEMBL Antagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition and measured after 90 mins by PathHunter assay B 7.96 pEC50 11 nM EC50 J Med Chem (2020) 63: 4349-4369 [PMID:32202101]
M3 receptor/Muscarinic acetylcholine receptor M3 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL320] [GtoPdb: 15] [UniProtKB: P08483]
ChEMBL Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland B 8.6 pKi 2.5 nM Ki Bioorg. Med. Chem. Lett. (2007) 17: 5256-5260 [PMID:17629699]
Muscarinic acetylcholine receptor M3 in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5498] [UniProtKB: Q8VH26]
ChEMBL Antagonism in muscarinic M3 receptor in guinea pig left atria F 7.3 pKd 50.12 nM Kd Bioorg. Med. Chem. Lett. (2006) 16: 373-377 [PMID:16275087]
M4 receptor/Muscarinic acetylcholine receptor M4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173]
ChEMBL Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4 B 8.07 pKi 8.6 nM Ki J. Med. Chem. (2002) 45: 984-987 [PMID:11831911]
M5 receptor/Muscarinic acetylcholine receptor M5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912]
ChEMBL Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M5 B 8.64 pKi 2.3 nM Ki J. Med. Chem. (2002) 45: 984-987 [PMID:11831911]
Nav1.5/Sodium channel protein type V alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1980] [GtoPdb: 582] [UniProtKB: Q14524]
ChEMBL Inhibition of fast sodium current (INa) in Chinese Hamster Ovary (CHO) K1 cells transfected with human Nav1.5 measured using IonWorks Quattro automated patch clamp platform F 5.8 pIC50 1584.89 nM IC50 J Pharmacol Toxicol Methods (2014) 70: 246-254 [PMID:25087753]
Kv7.1/Voltage-gated potassium channel, IKs; KCNQ1(Kv7.1)/KCNE1(MinK) in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2221347] [GtoPdb: 560] [UniProtKB: P15382, P51787]
ChEMBL Inhibition of slow delayed inward rectifying potassium current (Iks) in Chinese Hamster Ovary (CHO) cells expressing hKvLQT1/hminK measured using IonWorks Quattro automated patch clamp platform F 4.7 pIC50 19952.62 nM IC50 J Pharmacol Toxicol Methods (2014) 70: 246-254 [PMID:25087753]
Kv4.3/Voltage-gated potassium channel subunit Kv4.3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1964] [GtoPdb: 554] [UniProtKB: Q9UK17]
ChEMBL Inhibition of transient outward potassium current (Ito) current in Chinese Hamster Ovary (CHO) K1 cells expressing human Kv4.3 measured using IonWorks Quattro automated patch clamp platform F 4.9 pIC50 12589.25 nM IC50 J Pharmacol Toxicol Methods (2014) 70: 246-254 [PMID:25087753]

ChEMBL data shown on this page come from version 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]