atropine [Ligand Id: 320] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL517712 (Atropen, Atroject, Atrophate, Atropine (autoinjector), Atropine, Isopto Atropine)
  • acetylcholinesterase (Cartwright blood group)/Acetylcholinesterase in Mouse [ChEMBL: CHEMBL3198] [GtoPdb: 2465] [UniProtKB: P21836]
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  • α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100]
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  • M1 receptor/Muscarinic acetylcholine receptor M1 in Human [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
  • Muscarinic acetylcholine receptor M1 in Bovine [ChEMBL: CHEMBL2672] [UniProtKB: Q8WMX0]
  • M1 receptor/Muscarinic acetylcholine receptor M1 in Rat [ChEMBL: CHEMBL276] [GtoPdb: 13] [UniProtKB: P08482]
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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 Mouse [ChEMBL: CHEMBL3197] [GtoPdb: 14] [UniProtKB: Q9ERZ4]
  • 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]
  • M4 receptor/Muscarinic acetylcholine receptor M4 in Rat [ChEMBL: CHEMBL317] [GtoPdb: 16] [UniProtKB: P08485]
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  • M5 receptor/Muscarinic acetylcholine receptor M5 in Human [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912]
  • M5 receptor/Muscarinic acetylcholine receptor M5 in Rat [ChEMBL: CHEMBL277] [GtoPdb: 17] [UniProtKB: P08911]
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  • Nicotinic acetylcholine receptor alpha 5 subunit in Musca domestica [ChEMBL: CHEMBL2366408] [UniProtKB: A9XFY4]
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  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
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  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
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  • Organic cation transporter 1/Solute carrier family 22 member 1 in Human [ChEMBL: CHEMBL5685] [GtoPdb: 1019] [UniProtKB: O15245]
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  • α2A-adrenoceptor in Human [GtoPdb: 25] [UniProtKB: P08913]
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  • Glycine Receptor (All subtypes) in Human [GtoPdb: 428]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
acetylcholinesterase (Cartwright blood group)/Acetylcholinesterase in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3198] [GtoPdb: 2465] [UniProtKB: P21836]
ChEMBL Compound was evaluated for the binding affinity by displacing [3H]methylscopolamine [3H]NMS from mouse cerebral cortex tissue. B 9.15 pKi 0.7 nM Ki J. Med. Chem. (1992) 35: 1102-1108 [PMID:1552502]
ChEMBL Compound was evaluated for the binding affinity by displacing [3H]oxotremorine from mouse cerebral cortex tissue. B 9.46 pKi 0.35 nM Ki J. Med. Chem. (1992) 35: 1102-1108 [PMID:1552502]
α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100]
ChEMBL DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin) B 6.18 pKi 666 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin) B 5.87 pIC50 1354 nM IC50 DrugMatrix in vitro pharmacology data
M1 receptor/Muscarinic acetylcholine receptor M1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
ChEMBL Binding affinity towards muscarinic m1 receptor B 8.7 pKi 2 nM Ki J. Med. Chem. (1994) 37: 2285-2291 [PMID:8057277]
ChEMBL Competitive inhibition of EGFP-fused human M1 receptor N-terminal truncated at 17 residues expressed in HEK293 cells after 4 hrs by FRET assay in presence of para-LRB-AC42 B 8.92 pKi 1.2 nM Ki J. Med. Chem. (2012) 55: 2125-2143 [PMID:22329602]
ChEMBL Displacement of [3H] N-methylscopolamine from human muscarinic M1 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis B 9.04 pKi 0.92 nM Ki Bioorg. Med. Chem. (2013) 21: 2651-2662 [PMID:23523385]
ChEMBL Displacement of [3H]NMS from EGFP-fused human M1 receptor N-terminal truncated at 17 residues expressed in HEK293 cells after 22 hrs by liquid scintillation counting B 9.24 pKi 0.58 nM Ki J. Med. Chem. (2012) 55: 2125-2143 [PMID:22329602]
ChEMBL DRUGMATRIX: Muscarinic M1 radioligand binding (ligand: [3H] N-Methylscopolamine) B 9.44 pKi 0.37 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Inhibition of [3H]QNB binding to CHO cells bearing transfected muscarinic acetylcholine receptor M3 B 9.48 pKi 0.33 nM Ki J. Med. Chem. (1991) 34: 1436-1440 [PMID:2016720]
ChEMBL Displacement of [3H]pirenzepine from muscarinic M1 receptor B 9.52 pKi 0.3 nM Ki J. Nat. Prod. (1993) 56: 441-455 [PMID:8496700]
GtoPdb - - 9.6 pKi - - - EMBO J. (1987) 6: 3923-9 [PMID:3443095];
Mol. Pharmacol. (1998) 53: 1120-30 [PMID:9614217];
AAPS PharmSci (2001) 3: E30 [PMID:12049493];
Mol. Pharmacol. (2006) 69: 1641-51 [PMID:16439611];
J. Pharmacol. Exp. Ther. (2001) 297: 790-7 [PMID:11303071];
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 9.6 pKi 0.25 nM Ki J. Med. Chem. (2002) 45: 984-987 [PMID:11831911]
ChEMBL DRUGMATRIX: Muscarinic M1 radioligand binding (ligand: [3H] N-Methylscopolamine) B 8.82 pIC50 1.52 nM IC50 DrugMatrix in vitro pharmacology data
Muscarinic acetylcholine receptor M1 in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2672] [UniProtKB: Q8WMX0]
ChEMBL Inhibition of [3H]NMS binding to cerebral cortex membranes which contain predominantly the Muscarinic acetylcholine receptor M1 subtypes B 8.62 pKi 2.4 nM Ki J. Med. Chem. (1989) 32: 1522-1528 [PMID:2738887]
ChEMBL Binding affinity against Muscarinic acetylcholine receptor M1 by displacement of [3H]pirenzepine in bovine striatum B 9.7 pKi 0.2 nM Ki J. Med. Chem. (1988) 31: 1463-1466 [PMID:3385735]
M1 receptor/Muscarinic acetylcholine receptor M1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL276] [GtoPdb: 13] [UniProtKB: P08482]
ChEMBL In vitro receptor binding against Muscarinic acetylcholine receptor M1 in rat cerebral cortex was determined using [3H]pirenzepine B 8.89 pKd 1.3 nM Kd J. Med. Chem. (1990) 33: 2108-2113 [PMID:2374141]
ChEMBL Displacement of [3H]NMS from rat muscarinic M1 receptor expressed in CHO cells after 3 hrs B 8.85 pKi 1.4 nM Ki Bioorg. Med. Chem. Lett. (2013) 23: 223-227 [PMID:23200253]
ChEMBL Displacement of [3H]NMS from rat muscarinic M1 receptor expressed in CHO cells after 3 hrs B 8.86 pKi 1.38 nM Ki Bioorg. Med. Chem. Lett. (2013) 23: 223-227 [PMID:23200253]
ChEMBL Displacement of [3H]NMS from rat recombinant muscarinic M1 receptor expressed in CHO cells after 2 hrs by microplate scintillation counting B 9.1 pKi 0.79 nM Ki Nat. Chem. Biol. (2008) 4: 42-50 [PMID:18059262]
ChEMBL Evaluated for the phosphatidyl inositol turnover at Muscarinic acetylcholine receptor M1 in rat cortex F 9.3 pKi 0.5 nM Ki J. Med. Chem. (1988) 31: 1463-1466 [PMID:3385735]
ChEMBL Ability to displace [3H]pirenzepine (PZ) from M1 receptor in rat cortex homogenate B 9.59 pKi 0.26 nM Ki J. Med. Chem. (1993) 36: 848-854 [PMID:8464039]
ChEMBL Displacement of [3H]pirenzepine from muscarinic acetylcholine receptor M1 in rat cortex homogenates B 9.59 pKi 0.26 nM Ki J. Med. Chem. (1991) 34: 2984-2989 [PMID:1920350]
GtoPdb - - 9.7 pKi - - - J. Pharmacol. Exp. Ther. (2002) 303: 29-35 [PMID:12235229];
Life Sci. (1992) 51: 955-71 [PMID:1325587];
Mol. Pharmacol. (1989) 35: 469-76 [PMID:2704370]
M2 receptor/Muscarinic acetylcholine receptor M2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172]
ChEMBL Antimuscarinic activity on the acetylcholine-induced inhibition of contraction of guinea pig ileum which has M2 muscarinic receptor subtype. F 8.7 pKd 2 nM Kd J. Med. Chem. (1989) 32: 1522-1528 [PMID:2738887]
ChEMBL Antagonist potency against muscarinic receptors was assed by antagonism of carbachol induced inhibition of electrically stimulated guinea pig atria F 8.87 pKd 1.35 nM Kd J. Med. Chem. (1989) 32: 79-84 [PMID:2909747]
ChEMBL Displacement of [3H]-AFDX-384 from human muscarinic M2 receptor expressed in CHO-K1 cells B 8.72 pKi 1.9 nM Ki J. Med. Chem. (2010) 53: 6386-6397 [PMID:20684563]
ChEMBL Binding affinity (Ki) against binding of [3H]NMS to membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M2 B 8.82 pKi 1.5 nM Ki J. Med. Chem. (2002) 45: 984-987 [PMID:11831911]
ChEMBL Displacement of [3H] N-methylscopolamine from human muscarinic M2 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis B 8.84 pKi 1.44 nM Ki Bioorg. Med. Chem. (2013) 21: 2651-2662 [PMID:23523385]
ChEMBL DRUGMATRIX: Muscarinic M2 radioligand binding (ligand: [3H] N-Methylscopolamine) B 8.88 pKi 1.33 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Binding affinity towards muscarinic m2 receptor B 9 pKi 1 nM Ki J. Med. Chem. (1994) 37: 2285-2291 [PMID:8057277]
GtoPdb - - 9.2 pKi - - - Mol. Pharmacol. (1989) 35: 469-76 [PMID:2704370];
J. Pharmacol. Exp. Ther. (2002) 303: 29-35 [PMID:12235229];
J. Pharmacol. Exp. Ther. (2001) 297: 790-7 [PMID:11303071];
AAPS PharmSci (2001) 3: E30 [PMID:12049493];
J. Pharmacol. Exp. Ther. (1998) 284: 500-7 [PMID:9454790];
J. Pharmacol. Exp. Ther. (2006) 316: 279-88 [PMID:16188951];
EMBO J. (1987) 6: 3923-9 [PMID:3443095]
ChEMBL muscarinic acetylcholine receptor M1 B 9.46 pKi 0.34 nM Ki J. Med. Chem. (1991) 34: 1436-1440 [PMID:2016720]
ChEMBL DRUGMATRIX: Muscarinic M2 radioligand binding (ligand: [3H] N-Methylscopolamine) B 8.43 pIC50 3.73 nM IC50 DrugMatrix in vitro pharmacology data
M2 receptor/Muscarinic acetylcholine receptor M2 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3197] [GtoPdb: 14] [UniProtKB: Q9ERZ4]
ChEMBL Ability to displace [3H]methylscopolamine ([3H]NMS) from mouse cerebral cortex B 9.15 pKi 0.7 nM Ki J. Med. Chem. (1992) 35: 3141-3147 [PMID:1507203]
ChEMBL Ability to displace [3H]oxotremorine ([3H]-OXO-M) from mouse cerebral cortex B 9.46 pKi 0.35 nM Ki J. Med. Chem. (1992) 35: 3141-3147 [PMID:1507203]
M2 receptor/Muscarinic acetylcholine receptor M2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL309] [GtoPdb: 14] [UniProtKB: P10980]
ChEMBL In vitro receptor binding against Muscarinic acetylcholine receptor M2 in rat heart was determined using [3H]pirenzepine B 8.57 pKd 2.7 nM Kd J. Med. Chem. (1990) 33: 2108-2113 [PMID:2374141]
ChEMBL Evaluated for the inhibition of adenylate cyclase at M2 receptor in rat heart B 8.12 pKi 7.5 nM Ki J. Med. Chem. (1988) 31: 1463-1466 [PMID:3385735]
ChEMBL Inhibition of carbachol-induced release of alpha-amylase from pancreatic acinar cells from that of rat ileum contained the M2 receptor subtypes B 8.8 pKi 1.6 nM Ki J. Med. Chem. (1989) 32: 1522-1528 [PMID:2738887]
ChEMBL Displacement of [3H]NMS from rat recombinant muscarinic M2 receptor expressed in CHO cells after 2 hrs by microplate scintillation counting B 8.84 pKi 1.45 nM Ki Nat. Chem. Biol. (2008) 4: 42-50 [PMID:18059262]
GtoPdb - - 9.1 pKi - - - Life Sci. (1992) 51: 955-71 [PMID:1325587];
J. Pharmacol. Exp. Ther. (1998) 284: 500-7 [PMID:9454790]
ChEMBL Ability to displace [3H](-)-quinuclidinyl benzilate(QNB) from M2 receptor in rat heart homogenate B 9.12 pKi 0.76 nM Ki J. Med. Chem. (1993) 36: 848-854 [PMID:8464039]
ChEMBL Displacement of [3H](-)-quinuclidinyl benzilate(QNB) from muscarinic (M2) receptor in rat heart homogenates B 9.12 pKi 0.76 nM Ki J. Med. Chem. (1991) 34: 2984-2989 [PMID:1920350]
ChEMBL Binding affinity against Muscarinic acetylcholine receptor M2 by displacement of [3H]QNB in rat myocardium B 9.15 pKi 0.7 nM Ki J. Med. Chem. (1988) 31: 1463-1466 [PMID:3385735]
M3 receptor/Muscarinic acetylcholine receptor M3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309]
ChEMBL Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis B 8.66 pKi 2.18 nM Ki Bioorg. Med. Chem. (2013) 21: 2651-2662 [PMID:23523385]
ChEMBL Displacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cells B 9.05 pKi 0.9 nM Ki J. Med. Chem. (2010) 53: 6386-6397 [PMID:20684563]
ChEMBL Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3 B 9.3 pKi 0.5 nM Ki J. Med. Chem. (2002) 45: 984-987 [PMID:11831911]
ChEMBL DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine) B 9.36 pKi 0.44 nM Ki DrugMatrix in vitro pharmacology data
GtoPdb - - 9.8 pKi - - - EMBO J. (1987) 6: 3923-9 [PMID:3443095];
AAPS PharmSci (2001) 3: E30 [PMID:12049493];
Mol. Pharmacol. (1989) 35: 469-76 [PMID:2704370];
J. Pharmacol. Exp. Ther. (2001) 297: 790-7 [PMID:11303071];
J. Recept. Signal Transduct. Res. (1997) 17: 177-84 [PMID:9029489];
Br. J. Pharmacol. (2006) 148: 927-37 [PMID:16847442]
ChEMBL DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine) B 8.68 pIC50 2.07 nM IC50 DrugMatrix in vitro pharmacology data
M3 receptor/Muscarinic acetylcholine receptor M3 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL320] [GtoPdb: 15] [UniProtKB: P08483]
ChEMBL In vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepine B 9.2 pKd 0.63 nM Kd J. Med. Chem. (1990) 33: 2108-2113 [PMID:2374141]
ChEMBL Displacement of [3H]NMS from rat recombinant muscarinic M3 receptor expressed in CHO cells after 2 hrs by microplate scintillation counting B 9.1 pKi 0.8 nM Ki Nat. Chem. Biol. (2008) 4: 42-50 [PMID:18059262]
GtoPdb - - 9.3 pKi - - - J. Pharmacol. Exp. Ther. (2002) 303: 29-35 [PMID:12235229];
Life Sci. (1992) 51: 955-71 [PMID:1325587]
ChEMBL Ability to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenate B 9.92 pKi 0.12 nM Ki J. Med. Chem. (1993) 36: 848-854 [PMID:8464039]
Muscarinic acetylcholine receptor M3 in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5498] [UniProtKB: Q8VH26]
ChEMBL Antagonist potency against carbachol induced contractions of isolated guinea pig ileum Muscarinic acetylcholine receptor F 8.83 pKd 1.48 nM Kd J. Med. Chem. (1989) 32: 79-84 [PMID:2909747]
ChEMBL Antagonism to the H1 receptor of guinea pig ileum was determined F 9.11 pKd 0.78 nM Kd Bioorg. Med. Chem. Lett. (1995) 5: 667-672
M4 receptor/Muscarinic acetylcholine receptor M4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173]
ChEMBL Displacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cells B 8.52 pKi 3 nM Ki J. Med. Chem. (2010) 53: 6386-6397 [PMID:20684563]
ChEMBL Displacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis B 8.86 pKi 1.39 nM Ki Bioorg. Med. Chem. (2013) 21: 2651-2662 [PMID:23523385]
ChEMBL Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4 B 9.47 pKi 0.34 nM Ki J. Med. Chem. (2002) 45: 984-987 [PMID:11831911]
GtoPdb - - 9.5 pKi - - - EMBO J. (1987) 6: 3923-9 [PMID:3443095];
AAPS PharmSci (2001) 3: E30 [PMID:12049493];
Mol. Pharmacol. (1989) 35: 469-76 [PMID:2704370];
J. Pharmacol. Exp. Ther. (2001) 297: 790-7 [PMID:11303071]
GtoPdb - - 9.85 pKi 0.14 nM Ki Invest. Ophthalmol. Vis. Sci. (2018) 59: 2778-2791 [PMID:29860464]
ChEMBL DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine) B 9.98 pKi 0.1 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine) B 9.13 pIC50 0.74 nM IC50 DrugMatrix in vitro pharmacology data
M4 receptor/Muscarinic acetylcholine receptor M4 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL317] [GtoPdb: 16] [UniProtKB: P08485]
ChEMBL Displacement of [3H]NMS from rat recombinant muscarinic M4 receptor expressed in CHO cells after 2 hrs by microplate scintillation counting B 9.28 pKi 0.52 nM Ki Nat. Chem. Biol. (2008) 4: 42-50 [PMID:18059262]
ChEMBL Displacement of [3H]NMS from rat recombinant muscarinic M4 receptor expressed in CHO cells after 2 hrs by microplate scintillation counting B 9.28 pKi 0.52 nM Ki Nat. Chem. Biol. (2008) 4: 42-50 [PMID:18059262]
GtoPdb - - 9.7 pKi - - - Life Sci. (1992) 51: 955-71 [PMID:1325587]
M5 receptor/Muscarinic acetylcholine receptor M5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912]
ChEMBL Displacement of [3H]NMS from human muscarinic acetylcholine receptor subtype 5 expressed in CHO cell membranes by scintillation counting method B 8.83 pKi 1.47 nM Ki J. Med. Chem. (2014) 57: 7804-7810 [PMID:25147929]
ChEMBL Displacement of [3H]-4-DAMP from human muscarinic M5 receptor expressed in BHK-21 cells B 9 pKi 1 nM Ki J. Med. Chem. (2010) 53: 6386-6397 [PMID:20684563]
ChEMBL DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine) B 9.18 pKi 0.66 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M5 B 9.27 pKi 0.54 nM Ki J. Med. Chem. (2002) 45: 984-987 [PMID:11831911]
ChEMBL Displacement of [3H]QNB from muscarinic acetylcholine M5 receptor after 1.5 hrs by scintillation counting B 9.4 pKi 0.4 nM Ki Bioorg. Med. Chem. (2011) 19: 5756-5762 [PMID:21907583]
ChEMBL 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 control F 9.68 pKi 0.21 nM Ki J. Med. Chem. (2009) 52: 3445-3448 [PMID:19438238]
GtoPdb - - 9.7 pKi - - - Mol. Pharmacol. (1989) 35: 469-76 [PMID:2704370];
J. Pharmacol. Exp. Ther. (2001) 297: 790-7 [PMID:11303071]
ChEMBL DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine) B 9.04 pIC50 0.92 nM IC50 DrugMatrix in vitro pharmacology data
M5 receptor/Muscarinic acetylcholine receptor M5 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL277] [GtoPdb: 17] [UniProtKB: P08911]
ChEMBL Displacement of [3H]NMS from rat recombinant muscarinic M5 receptor expressed in CHO cells after 2 hrs by microplate scintillation counting B 9.07 pKi 0.86 nM Ki Nat. Chem. Biol. (2008) 4: 42-50 [PMID:18059262]
GtoPdb - - 9.4 pKi - - - Life Sci. (1992) 51: 955-71 [PMID:1325587]
Nicotinic acetylcholine receptor alpha 5 subunit in Musca domestica (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2366408] [UniProtKB: A9XFY4]
ChEMBL Displacement of [3H]alpha-bungarotoxin from nAChR in Musca domestica (house fly) head membrane after 60 min by scintillation counting B 4.49 pKi 32500 nM Ki J Pesticide Sci (1992) 17: 231-236
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
ChEMBL Binding affinity towards 5-hydroxytryptamine 1A receptor by the displacement of [125I]trans-8-OH-PIPAT in membrane homogenates of hippocampal tissue of rat brain B 4.7 pKi >20000 nM Ki J. Med. Chem. (1993) 36: 3161-3165 [PMID:8230102]
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine) B 6.28 pKi 530 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine) B 5.99 pIC50 1012 nM IC50 DrugMatrix in vitro pharmacology data
Organic cation transporter 1/Solute carrier family 22 member 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5685] [GtoPdb: 1019] [UniProtKB: O15245]
ChEMBL Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy B 4.91 pIC50 12200 nM IC50 J. Med. Chem. (2008) 51: 5932-5942 [PMID:18788725]
α2A-adrenoceptor in Human [GtoPdb: 25] [UniProtKB: P08913]
GtoPdb - - 4.85 pKi 14000 nM Ki Invest. Ophthalmol. Vis. Sci. (2018) 59: 2778-2791 [PMID:29860464]
Glycine Receptor (All subtypes) in Human [GtoPdb: 428]
GtoPdb - - 3.6 pIC50 - - - J. Neurochem. (1999) 73: 802-6 [PMID:10428078];
J. Neurochem. (2007) 100: 758-69 [PMID:17181559]

ChEMBL data shown on this page come from version 26:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos 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]