diltiazem [Ligand Id: 2298] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL23 (Diltiazem, Tiazac, Diltzac, Tiamate, Cardizem, Dilt-CD)
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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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  • Voltage-dependent L-type calcium channel subunit alpha-1C in Guinea pig [ChEMBL: CHEMBL2366456] [UniProtKB: O35505]
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  • Cav1.2/Voltage-gated L-type calcium channel alpha-1C subunit in Human [ChEMBL: CHEMBL1940] [GtoPdb: 529] [UniProtKB: Q13936]
  • Cav1.2 in Ferret [GtoPdb: 529]
  • Voltage-gated L-type calcium channel alpha-1C subunit in Rabbit [ChEMBL: CHEMBL2830] [UniProtKB: P15381]
  • Cav1.2/Voltage-gated L-type calcium channel alpha-1C subunit in Rat [ChEMBL: CHEMBL3762] [GtoPdb: 529] [UniProtKB: P22002]
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  • Cav1.3 in Mouse [GtoPdb: 530] [UniProtKB: Q99246]
  • Cav1.3/Voltage-gated L-type calcium channel alpha-1D subunit in Rat [ChEMBL: CHEMBL4132] [GtoPdb: 530] [UniProtKB: P27732]
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  • Cav1.1/Voltage-gated L-type calcium channel alpha-1S subunit in Human [ChEMBL: CHEMBL3805] [GtoPdb: 528] [UniProtKB: Q13698]
  • Cav1.1 in Rabbit [GtoPdb: 528]
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  • 5-HT3A in Human [GtoPdb: 379]
  • 5-HT3A in Mouse [GtoPdb: 379]
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  • Cav1.4 in Mouse [GtoPdb: 531] [UniProtKB: Q9JIS7]
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  • Kv1.1 in Mouse [GtoPdb: 538] [UniProtKB: P16388]
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  • Kv1.2 in Rat [GtoPdb: 539] [UniProtKB: P63142]
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  • Kv1.5 in Human [GtoPdb: 542] [UniProtKB: P22460]
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  • Kv1.7 in Mouse [GtoPdb: 544] [UniProtKB: Q17ST2]
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  • Kv3.1 in Mouse [GtoPdb: 548] [UniProtKB: P15388]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
CYP3A4/Cytochrome P450 3A4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL340] [GtoPdb: 1337] [UniProtKB: P08684]
ChEMBL DRUGMATRIX: CYP450, 3A4 enzyme inhibition (substrate: 7-Benzyloxy-4-(trifluoromethyl)-coumarin) B 5.74 pIC50 1836.6 nM IC50 DrugMatrix in vitro pharmacology data
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Inhibitory concentration against potassium channel HERG B 4.76 pIC50 17378.01 nM IC50 Bioorg. Med. Chem. Lett. (2005) 15: 2886-2890 [PMID:15911273]
ChEMBL Inhibition of human Potassium channel HERG expressed in mammalian cells B 4.76 pIC50 17378.01 nM IC50 Bioorg. Med. Chem. Lett. (2003) 13: 2773-2775 [PMID:12873512]
ChEMBL Inhibition of human voltage-gated potassium channel subunit Kv11.1 (ERG K+ channel) in open state F 4.76 pIC50 17378.01 nM IC50 Bioorg. Med. Chem. Lett. (2005) 15: 1737-1741 [PMID:15745831]
ChEMBL Inhibition of human ERG expressed in CHO cells by whole cell patch clamp technique B 4.76 pIC50 17378.01 nM IC50 Bioorg. Med. Chem. (2008) 16: 6252-6260 [PMID:18448342]
ChEMBL Inhibition of human ERG in MCF7 cells B 4.76 pIC50 17378.01 nM IC50 Eur. J. Med. Chem. (2009) 44: 1926-1932 [PMID:19110341]
ChEMBL K+ channel blocking activity in human embryonic kidney cells expressing HERG Kv11.1 F 4.76 pIC50 17300 nM IC50 J. Med. Chem. (2002) 45: 3844-3853 [PMID:12190308]
ChEMBL Inhibition of hERG K channel F 4.76 pIC50 17300 nM IC50 Cardiovasc. Res. (2011) 91: 53-61 [PMID:21300721]
ABCB1/P-glycoprotein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183]
ChEMBL TP_TRANSPORTER: inhibition of Digoxin transepithelial transport (basal to apical) (Digoxin: 0.1 uM) in MDR1-expressing LLC-PK1 cells F 4.11 pIC50 77700 nM IC50 Eur. J. Pharm. Sci. (2002) 16: 159-165 [PMID:12128170]
ChEMBL Inhibition of P-glycoprotein by Hoechst assay B 4.21 pIC50 61659.5 nM IC50 Bioorg. Med. Chem. (2007) 15: 7470-7479 [PMID:17890094]
ChEMBL Inhibition of P-glycoprotein-mediated multidrug resistance in adriamycin-resistant human A2780/ADR cells by calcein AM assay B 4.31 pIC50 49000 nM IC50 Bioorg. Med. Chem. (2009) 17: 2524-2535 [PMID:19250834]
ChEMBL Inhibition of P-glycoprotein expressed in A2780/ADR cells by calcein AM assay B 4.37 pIC50 42657.95 nM IC50 Bioorg. Med. Chem. (2007) 15: 7470-7479 [PMID:17890094]
ChEMBL Inhibition of P-gp in human adriamycin-resistant A2780 cells by Hoechst 33342 assay B 4.37 pIC50 42657.95 nM IC50 Bioorg. Med. Chem. (2008) 16: 8224-8236 [PMID:18678495]
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 12400 nM IC50 J. Med. Chem. (2008) 51: 5932-5942 [PMID:18788725]
Voltage-dependent L-type calcium channel subunit alpha-1C in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2366456] [UniProtKB: O35505]
ChEMBL Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes F 4.13 pIC50 74000 nM IC50 Journal of Applied Toxicology (2012) 32: 858-866 [PMID:22761000]
ChEMBL Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes F 4.52 pIC50 30000 nM IC50 Journal of Applied Toxicology (2012) 32: 858-866 [PMID:22761000]
ChEMBL Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes F 6.2 pIC50 630 nM IC50 Journal of Applied Toxicology (2012) 32: 858-866 [PMID:22761000]
Cav1.2/Voltage-gated L-type calcium channel alpha-1C subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1940] [GtoPdb: 529] [UniProtKB: Q13936]
ChEMBL Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in human embryonic kidney cells heterologically expressing alpha-1C subunit F 4.36 pIC50 44000 nM IC50 Journal of Applied Toxicology (2012) 32: 858-866 [PMID:22761000]
Cav1.2 in Ferret [GtoPdb: 529]
GtoPdb - - 6.3 pIC50 - - - J Pharmacol Exp Ther (1984) 228: 245-51 [PMID:6694106]
Voltage-gated L-type calcium channel alpha-1C subunit in Rabbit (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2830] [UniProtKB: P15381]
ChEMBL Inhibition of [3H]nitrendipine binding to calcium channels in rabbit cardiac muscle B 4.52 pIC50 30000 nM IC50 J. Med. Chem. (1988) 31: 2221-2227 [PMID:3184128]
Cav1.2/Voltage-gated L-type calcium channel alpha-1C subunit in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3762] [GtoPdb: 529] [UniProtKB: P22002]
ChEMBL Calcium antagonistic activity by measuring [3H]nitrendipine displacement from rat heart L-type [Ca2+] channel F 6.55 pKi 280 nM Ki J. Med. Chem. (1995) 38: 4393-4410 [PMID:7473567]
ChEMBL Binding of [3H]nitrendipine to calcium channel in rat heart membranes was determined B 6 pIC50 >1000 nM IC50 Bioorg. Med. Chem. Lett. (1994) 4: 351-354
ChEMBL In vitro inhibition of K+ induced contractions of the isolated rat aorta. F 7 pIC50 100 nM IC50 J. Med. Chem. (1998) 41: 4309-4316 [PMID:9784106]
ChEMBL Ability to inhibit [3H]nitrendipine binding to the L-type calcium channel receptor(CCR) in rat heart homogenate. B 7.27 pIC50 54 nM IC50 J. Med. Chem. (1996) 39: 2922-2938 [PMID:8709127]
Cav1.3 in Mouse [GtoPdb: 530] [UniProtKB: Q99246]
GtoPdb - - 3.5 pIC50 - - - Eur J Pharmacol (2007) 573: 39-48 [PMID:17651721]
Cav1.3/Voltage-gated L-type calcium channel alpha-1D subunit in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4132] [GtoPdb: 530] [UniProtKB: P27732]
ChEMBL Inhibition of [3H]nitrendipine binding to L-type [Ca2+] channel in rat cortex homogenate, activity expressed as pIC50 B 7.34 pIC50 45.71 nM IC50 J. Med. Chem. (1997) 40: 125-131 [PMID:9016337]
Cav1.1/Voltage-gated L-type calcium channel alpha-1S subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3805] [GtoPdb: 528] [UniProtKB: Q13698]
ChEMBL Displacement of [3H]diltiazem from L-type calcium channel of guinea pig striated muscle B 6.42 pKi 380 nM Ki Bioorg. Med. Chem. Lett. (1993) 3: 2797-2800
Cav1.1 in Rabbit [GtoPdb: 528]
GtoPdb - - 4.2 pIC50 63096 nM IC50 J Pharmacol Exp Ther (1986) 236: 403-7 [PMID:2418195]
5-HT3A in Human [GtoPdb: 379]
GtoPdb - - 4.68 pIC50 21000 nM IC50 Mol Pharmacol (2011) 80: 183-90 [PMID:21505038]
5-HT3A in Mouse [GtoPdb: 379]
GtoPdb - - 5.26 pIC50 5500 nM IC50 J Physiol (Lond.) (1999) 519 Pt 3: 713-22 [PMID:10457085];
Biol Pharm Bull (2009) 32: 861-7 [PMID:19420755]
Cav1.4 in Mouse [GtoPdb: 531] [UniProtKB: Q9JIS7]
GtoPdb - - 4 pIC50 - - - Invest Ophthalmol Vis Sci (2004) 45: 708-13 [PMID:14744918]
Kv1.1 in Mouse [GtoPdb: 538] [UniProtKB: P16388]
GtoPdb - - 3.8 pIC50 - - - Mol Pharmacol (1994) 45: 1227-34 [PMID:7517498]
Kv1.2 in Rat [GtoPdb: 539] [UniProtKB: P63142]
GtoPdb - - 3.7 pKd 187000 nM Kd Mol Pharmacol (1994) 45: 1227-34 [PMID:7517498]
Kv1.5 in Human [GtoPdb: 542] [UniProtKB: P22460]
GtoPdb - - 3.9 pKd 115000 nM Kd Mol Pharmacol (1994) 45: 1227-34 [PMID:7517498]
Kv1.7 in Mouse [GtoPdb: 544] [UniProtKB: Q17ST2]
GtoPdb - - 4.2 pIC50 - - - J Biol Chem (1998) 273: 5851-7 [PMID:9488722]
Kv3.1 in Mouse [GtoPdb: 548] [UniProtKB: P15388]
GtoPdb - - 4 pIC50 - - - Mol Pharmacol (1994) 45: 1227-34 [PMID:7517498]

ChEMBL data shown on this page come from version 28:

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]