arecoline [Ligand Id: 296] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL7303 (NSC-56321) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| M1 receptor/Muscarinic acetylcholine receptor M1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229] | ||||||||
| ChEMBL | Binding affinity to human cloned muscarinic M1 receptor expressed in CHO cells | B | 4.53 | pKi | 29512.09 | nM | Ki | Bioorg Med Chem (2008) 16: 3049-3058 [PMID:18182302] |
| ChEMBL | Binding affinity of compound was determined towards human Muscarinic acetylcholine receptor M1 using [3H]QNB radioligand | B | 4.54 | pKi | 29000 | nM | Ki | J Med Chem (2003) 46: 2216-2226 [PMID:12747793] |
| GtoPdb | - | - | 5.7 | pKi | - | - | - |
Br J Pharmacol (1995) 114: 1241-9 [PMID:7620715]; Mol Pharmacol (1997) 52: 172-9 [PMID:9224827]; Eur J Med Chem (2020) 204: 112623 [PMID:32717485] |
| ChEMBL | Inhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M1 expressed in CHO cell membranes | B | 7.85 | pKi | 14 | nM | Ki | J Med Chem (2000) 43: 2514-2522 [PMID:10891110] |
| ChEMBL | In vitro affinity against human Muscarinic acetylcholine receptor M1 using quinuclidynyl benzylate (QNB) | B | 4.19 | pIC50 | 65000 | nM | IC50 | J Med Chem (1997) 40: 4265-4280 [PMID:9435896] |
| ChEMBL | Efficacy at muscarinic acetylcholine receptor M1 measured by the ability to inhibit the electrically stimulated twitch of the rabbit vas deferens | F | 6.26 | pIC50 | 545 | nM | IC50 | J Med Chem (1992) 35: 4011-4019 [PMID:1433209] |
| ChEMBL | Ability to displace [3H]oxotremorine from Muscarinic acetylcholine receptor M1 expressed in CHO cells. | B | 6.94 | pIC50 | 115 | nM | IC50 | Bioorg Med Chem Lett (2001) 11: 2855-2857 [PMID:11597415] |
| ChEMBL | Stimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptor | F | 5.25 | pEC50 | 5603 | nM | EC50 | Bioorg Med Chem Lett (1998) 8: 2897-2902 [PMID:9873644] |
| ChEMBL | In Vitro evaluation activity at the cloned Human Muscarinic acetylcholine receptor M1 determined by receptor selection and amplification technology (R-SAT) | B | 5.49 | pEC50 | 3200 | nM | EC50 | J Med Chem (1995) 38: 2188-2195 [PMID:7783150] |
| M1 receptor/Muscarinic acetylcholine receptor M1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3733] [GtoPdb: 13] [UniProtKB: P12657] | ||||||||
| ChEMBL | Binding affinity of [3H]-(R)-QNB binding to Muscarinic acetylcholine receptor M1 expressed in A9 L cell line in the presence of 300 uM GTP-gamma-S | B | 8.26 | pKi | 5.45 | nM | Ki | J Med Chem (1997) 40: 1230-1246 [PMID:9111297] |
| ChEMBL | Binding affinity (low) of [3H](R)-QNB binding to Muscarinic acetylcholine receptor M1 expressed in A9 L cell line in the absence of 300 uM GTP-gamma-S | B | 8.48 | pKi | 3.33 | nM | Ki | J Med Chem (1997) 40: 1230-1246 [PMID:9111297] |
| ChEMBL | Tested against Muscarinic acetylcholine receptor M1 expressed in A9 L cell line | B | 4.57 | pEC50 | 27000 | nM | EC50 | J Med Chem (1997) 40: 1230-1246 [PMID:9111297] |
| M1 receptor/Muscarinic acetylcholine receptor M1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL276] [GtoPdb: 13] [UniProtKB: P08482] | ||||||||
| ChEMBL | Displacement of [3H]QNB from muscarinic M1 receptor in Wistar rat brain cortex after 2 hrs by liquid scintillation counting | B | 4.06 | pKi | 88000 | nM | Ki | Bioorg Med Chem (2009) 17: 5526-5534 [PMID:19595599] |
| ChEMBL | Displacement of [3H]Quinuclidinyl benzilate from muscarinic M1 receptor in Wistar rat cortex synaptosomal membrane | B | 4.07 | pKi | 86000 | nM | Ki | Bioorg Med Chem (2008) 16: 5157-5163 [PMID:18359231] |
| ChEMBL | Displacement of [3H]QNB from muscarinic M1 receptor in Wistar rat brain cortex membrane after 2 hrs by liquid scintillation counting | B | 4.07 | pKi | 86000 | nM | Ki | Eur J Med Chem (2009) 44: 4848-4854 [PMID:19717214] |
| GtoPdb | - | - | 5.3 | pKi | - | - | - | J Pharmacol Exp Ther (1989) 248: 661-70 [PMID:2537406] |
| ChEMBL | Compound was evaluated for the displacement of the muscarinic QNB in a genetically transformed rat cell line (m1c2) transfected with cloned m1 receptors (m1-QNBm1c2) | B | 4.92 | pIC50 | 11920 | nM | IC50 | Bioorg Med Chem Lett (1991) 1: 147-150 |
| ChEMBL | Ability to displace [3H]pirenzepine (pir) from muscarinic acetylcholine receptor M1 in rat cortical tissue. | B | 5.76 | pIC50 | 1740 | nM | IC50 | J Med Chem (1992) 35: 15-27 [PMID:1732522] |
| ChEMBL | Evaluated for inhibition of binding of [3H]pirenzepine to homogenized rat cerebral cortex membranes | B | 5.76 | pIC50 | 1737.8 | nM | IC50 | Bioorg Med Chem Lett (1992) 2: 501-504 |
| ChEMBL | Binding activity against muscarinic acetylcholine receptor M1 in rat brain, using [3H]-Pz as the radioligand. | B | 5.89 | pIC50 | 1300 | nM | IC50 | J Med Chem (1995) 38: 3469-3481 [PMID:7658434] |
| ChEMBL | In vitro binding affinity against muscarinic acetylcholine receptor M1 from rat hippocampus, using [3H]pirenzepine (Pz) as radioligand | B | 5.89 | pIC50 | 1300 | nM | IC50 | J Med Chem (1992) 35: 2274-2283 [PMID:1613751] |
| ChEMBL | Displacement of [3H]-Pz (pirenzepine) from the muscarinic receptor M1 of the rat hippocampus | B | 5.89 | pIC50 | 1300 | nM | IC50 | Bioorg Med Chem Lett (1992) 2: 809-814 |
| ChEMBL | Displacement of [3H]pirenzepine (Pz) from rat hippocampus muscarinic acetylcholine receptor M1 | B | 5.89 | pIC50 | 1300 | nM | IC50 | J Med Chem (1992) 35: 4011-4019 [PMID:1433209] |
| ChEMBL | Inhibition of [3H]pirenzepine binding to rat brain membrane Muscarinic acetylcholine receptor M1 | B | 5.96 | pIC50 | 1100 | nM | IC50 | J Med Chem (1988) 31: 1312-1316 [PMID:3385727] |
| ChEMBL | In vitro binding affinity against muscarinic acetylcholine receptor M1 from rat hippocampus, using [3H]oxotremorine-M (Oxo-M) as radioligand | B | 7.11 | pIC50 | 77 | nM | IC50 | J Med Chem (1992) 35: 2274-2283 [PMID:1613751] |
| ChEMBL | Displacement of [3H]oxotremorine-M (Oxo-M) from rat hippocampus muscarinic acetylcholine receptor M1 | B | 7.11 | pIC50 | 77 | nM | IC50 | J Med Chem (1992) 35: 4011-4019 [PMID:1433209] |
| ChEMBL | Binding activity against muscarinic acetylcholine receptor M1 in rat brain, using [3H]OXO-M as the radioligand. | B | 7.11 | pIC50 | 77 | nM | IC50 | J Med Chem (1995) 38: 3469-3481 [PMID:7658434] |
| ChEMBL | M1 agonist activity estimated by rat superior cervical ganglion depolarization | F | 6.66 | pEC50 | >=220 | nM | EC50 | J Med Chem (1994) 37: 4085-4099 [PMID:7990109] |
| M2 receptor/Muscarinic acetylcholine receptor M2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172] | ||||||||
| GtoPdb | - | - | 5.2 | pKi | - | - | - |
Br J Pharmacol (1995) 114: 1241-9 [PMID:7620715]; Mol Pharmacol (1997) 52: 172-9 [PMID:9224827]; Eur J Med Chem (2020) 204: 112623 [PMID:32717485] |
| ChEMBL | Binding affinity to human cloned muscarinic M2 receptor expressed in CHO cells | B | 5.61 | pKi | 2454.71 | nM | Ki | Bioorg Med Chem (2008) 16: 3049-3058 [PMID:18182302] |
| ChEMBL | Binding affinity of compound was determined towards human Muscarinic acetylcholine receptor M2 using [3H]QNB radioligand | B | 5.62 | pKi | 2400 | nM | Ki | J Med Chem (2003) 46: 2216-2226 [PMID:12747793] |
| ChEMBL | Inhibition of [3H]- quinuclidinyl benzilate binding to human Muscarinic acetylcholine receptor M2 expressed in CHO cell membrane | B | 7.4 | pKi | 40 | nM | Ki | J Med Chem (2000) 43: 2514-2522 [PMID:10891110] |
| ChEMBL | The binding affinity was measured as inhibition of binding of [3H]- oxotremorine-M m2 toMuscarinic acetylcholine receptor M2 in membranes of CHO cells | B | 7.4 | pKi | 40 | nM | Ki | J Med Chem (2000) 43: 2514-2522 [PMID:10891110] |
| ChEMBL | Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M2 | B | 7.4 | pKi | 40 | nM | Ki | J Med Chem (1998) 41: 2047-2055 [PMID:9622546] |
| ChEMBL | Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M2 | B | 5.35 | pIC50 | 4500 | nM | IC50 | J Med Chem (1998) 41: 109-116 [PMID:9438027] |
| ChEMBL | In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M2 | B | 5.74 | pIC50 | 1800 | nM | IC50 | J Med Chem (1997) 40: 4265-4280 [PMID:9435896] |
| ChEMBL | Stimulation of cAMP in CHO cells expressing human m2 receptor | F | 5 | pEC50 | 10000 | nM | EC50 | Bioorg Med Chem Lett (1998) 8: 2897-2902 [PMID:9873644] |
| ChEMBL | In vitro binding affinity for muscarinic M1 receptor by displacing [3H]Pirenzepine binding on rat brain homogenate | B | 7.08 | pEC50 | 83 | nM | EC50 | J Med Chem (1994) 37: 4085-4099 [PMID:7990109] |
| ChEMBL | In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M2 determined by receptor selection and amplification technology (R-SAT). | B | 7.6 | pEC50 | 25 | nM | EC50 | J Med Chem (1995) 38: 2188-2195 [PMID:7783150] |
| M2 receptor/Muscarinic acetylcholine receptor M2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL309] [GtoPdb: 14] [UniProtKB: P10980] | ||||||||
| ChEMBL | Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M2 in rat cerebral cortical membranes | B | 7.4 | pKi | 40 | nM | Ki | J Med Chem (1998) 41: 2047-2055 [PMID:9622546] |
| ChEMBL | Inhibition of [3H]quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M2 in rat brain membrane | B | 4.96 | pIC50 | 11000 | nM | IC50 | J Med Chem (1988) 31: 1312-1316 [PMID:3385727] |
| ChEMBL | Compound was evaluated for the displacement of the muscarinic QNB in rat heart homogenate containing the pharmacologic M2 receptor (M2-QNB heart) | B | 5.04 | pIC50 | 9150 | nM | IC50 | Bioorg Med Chem Lett (1991) 1: 147-150 |
| ChEMBL | Inhibition of [3H]quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M2 of rat heart | B | 6.23 | pIC50 | 590 | nM | IC50 | J Med Chem (1988) 31: 1312-1316 [PMID:3385727] |
| M3 receptor/Muscarinic acetylcholine receptor M3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309] | ||||||||
| ChEMBL | Binding affinity of compound was determined towards human Muscarinic acetylcholine receptor M3 using [3H]QNB radioligand | B | 4.37 | pKi | 43000 | nM | Ki | J Med Chem (2003) 46: 2216-2226 [PMID:12747793] |
| ChEMBL | Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M3 | B | 5.24 | pKi | 5700 | nM | Ki | J Med Chem (1998) 41: 2047-2055 [PMID:9622546] |
| GtoPdb | - | - | 5.4 | pKi | - | - | - |
Br J Pharmacol (1995) 114: 1241-9 [PMID:7620715]; Mol Pharmacol (1997) 52: 172-9 [PMID:9224827]; Eur J Med Chem (2020) 204: 112623 [PMID:32717485] |
| ChEMBL | Compound was evaluated for its ability to displace [3H]N-methylscopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M3 | B | 4.24 | pIC50 | 58000 | nM | IC50 | J Med Chem (1998) 41: 109-116 [PMID:9438027] |
| ChEMBL | In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3 | B | 4.96 | pIC50 | 11000 | nM | IC50 | J Med Chem (1997) 40: 4265-4280 [PMID:9435896] |
| ChEMBL | In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M3 determined by receptor selection and amplification technology (R-SAT) | B | 6.47 | pEC50 | 340 | nM | EC50 | J Med Chem (1995) 38: 2188-2195 [PMID:7783150] |
| ChEMBL | Contraction of guinea pig ileum by muscarinic AChR activation, which could be inhibited by application of atropine | B | 7 | pEC50 | 100 | nM | EC50 | J Med Chem (1986) 29: 1004-1009 [PMID:3712371] |
| M3 receptor/Muscarinic acetylcholine receptor M3 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5105] [GtoPdb: 15] [UniProtKB: Q9ERZ3] | ||||||||
| ChEMBL | Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line | F | 4.92 | pEC50 | 12000 | nM | EC50 | J Med Chem (1997) 40: 1230-1246 [PMID:9111297] |
| M3 receptor/Muscarinic acetylcholine receptor M3 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL320] [GtoPdb: 15] [UniProtKB: P08483] | ||||||||
| ChEMBL | Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M3 in rat cerebral cortical membranes | B | 5.24 | pKi | 5700 | nM | Ki | J Med Chem (1998) 41: 2047-2055 [PMID:9622546] |
| M4 receptor/Muscarinic acetylcholine receptor M4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173] | ||||||||
| ChEMBL | Binding affinity of compound was determined towards human Muscarinic acetylcholine receptor M4 using [3H]QNB radioligand | B | 4.22 | pKi | 60000 | nM | Ki | J Med Chem (2003) 46: 2216-2226 [PMID:12747793] |
| GtoPdb | - | - | 5.5 | pKi | - | - | - |
Br J Pharmacol (1995) 114: 1241-9 [PMID:7620715]; Mol Pharmacol (1997) 52: 172-9 [PMID:9224827]; Eur J Med Chem (2020) 204: 112623 [PMID:32717485] |
| ChEMBL | Inhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranes | B | 5.62 | pKi | 2400 | nM | Ki | J Med Chem (2000) 43: 2514-2522 [PMID:10891110] |
| ChEMBL | Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M4 | B | 5.62 | pKi | 2400 | nM | Ki | J Med Chem (1998) 41: 2047-2055 [PMID:9622546] |
| ChEMBL | Inhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranes | B | 7.59 | pKi | 26 | nM | Ki | J Med Chem (2000) 43: 2514-2522 [PMID:10891110] |
| ChEMBL | Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]-NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M4 | B | 4.32 | pIC50 | 47500 | nM | IC50 | J Med Chem (1998) 41: 109-116 [PMID:9438027] |
| ChEMBL | In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4 | B | 4.87 | pIC50 | 13500 | nM | IC50 | J Med Chem (1997) 40: 4265-4280 [PMID:9435896] |
| ChEMBL | In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M4 determined by receptor selection and amplification technology (R-SAT) | B | 6.89 | pEC50 | 130 | nM | EC50 | J Med Chem (1995) 38: 2188-2195 [PMID:7783150] |
| M4 receptor/Muscarinic acetylcholine receptor M4 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL317] [GtoPdb: 16] [UniProtKB: P08485] | ||||||||
| ChEMBL | Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranes | B | 5.62 | pKi | 2400 | nM | Ki | J Med Chem (1998) 41: 2047-2055 [PMID:9622546] |
| M5 receptor/Muscarinic acetylcholine receptor M5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912] | ||||||||
| ChEMBL | Binding affinity to human cloned muscarinic M5 receptor expressed in CHO cells | B | 4.25 | pKi | 56234.13 | nM | Ki | Bioorg Med Chem (2008) 16: 3049-3058 [PMID:18182302] |
| ChEMBL | Binding affinity of compound was determined towards human Muscarinic acetylcholine receptor M5 using [3H]QNB radioligand | B | 4.25 | pKi | 56000 | nM | Ki | J Med Chem (2003) 46: 2216-2226 [PMID:12747793] |
| ChEMBL | Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M5 | B | 4.2 | pIC50 | 62500 | nM | IC50 | J Med Chem (1998) 41: 109-116 [PMID:9438027] |
| ChEMBL | In Vitro activity at the cloned Human Muscarinic acetylcholine receptor M5 determined by receptor selection and amplification technology (R-SAT) | B | 6.22 | pEC50 | 600 | nM | EC50 | J Med Chem (1995) 38: 2188-2195 [PMID:7783150] |
| nicotinic acetylcholine receptor α3 subunit/nicotinic acetylcholine receptor α4 subunit/nicotinic acetylcholine receptor α2 subunit/nicotinic acetylcholine receptor β2 subunit/nicotinic acetylcholine receptor β3 subunit/nicotinic acetylcholine receptor β4 subunit/nicotinic acetylcholine receptor α5 subunit/nicotinic acetylcholine receptor α6 subunit/nicotinic acetylcholine receptor α9 subunit/nicotinic acetylcholine receptor α7 subunit/nicotinic acetylcholine receptor α10 subunit/Neuronal acetylcholine receptor in Rat (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2094110] [GtoPdb: 464, 465, 463, 472, 473, 474, 466, 467, 469, 468, 470] [UniProtKB: P04757, P09483, P12389, P12390, P12391, P12392, P20420, P43143, P43144, Q05941, Q9JLB5] | ||||||||
| ChEMBL | Binding affinity for Nicotinic acetylcholine receptor site in rat cortex was determined using [3H]MCC as radioligand | B | 6.65 | pKi | 224 | nM | Ki | Bioorg Med Chem Lett (1994) 4: 573-578 |
| nicotinic acetylcholine receptor α4 subunit/nicotinic acetylcholine receptor β2 subunit/Neuronal acetylcholine receptor; alpha4/beta2 in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907596] [GtoPdb: 465, 472] [UniProtKB: P09483, P12390] | ||||||||
| ChEMBL | The compound was evaluated for percentage inhibition of binding of [3H]- nicotine to Nicotinic acetylcholine receptor alpha4-beta2 in Rat Cerebral Cortical Membranes | B | 6.57 | pKi | 270 | nM | Ki | J Med Chem (1998) 41: 2047-2055 [PMID:9622546] |
| ChEMBL | Inhibition of binding of [3H]nicotine to Nicotinic acetylcholine receptor alpha4-beta2 in rat cerebral cortical membranes at 100 uM concentration | B | 6.57 | pKi | 270 | nM | Ki | J Med Chem (1998) 41: 2047-2055 [PMID:9622546] |
| Voltage-dependent L-type calcium channel subunit alpha-1C in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2366456] [UniProtKB: O35505] | ||||||||
| ChEMBL | Inhibition of Cav1.2 calcium current measured using whole cell patch clamp in guinea pig ventricular myocytes | F | 4.47 | pIC50 | 33730 | nM | IC50 | IC50 data for the L-type calcium channel extracted from a set of literature articles |
ChEMBL data shown on this page come from version 32:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]
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