nimodipine [Ligand Id: 2523] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1428 (Admon, BAY E 9736, BAY-E-9736, Nemotan, Nimodipine, Nimodipine ap, Nimotop, NSC-758476, Nymalize, Periplum) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| A1 receptor/Adenosine A1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099] | ||||||||
| ChEMBL | Displacement of [3H](R)-PIA binding to Adenosine A1 receptor in rat brain membranes | B | 4.7 | pKi | 20100 | nM | Ki | J Med Chem (1996) 39: 2980-2989 [PMID:8709132] |
| A2A receptor/Adenosine A2a receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL302] [GtoPdb: 19] [UniProtKB: P30543] | ||||||||
| ChEMBL | Displacement of [3H]-CGS- 21680 binding to Adenosine A2A receptor in rat striatal membranes | B | 4.35 | pKi | 44300 | nM | Ki | J Med Chem (1996) 39: 2980-2989 [PMID:8709132] |
| A3 receptor/Adenosine A3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8] | ||||||||
| ChEMBL | Displacement of [125]AB-MECA binding to human Adenosine A3 receptor expressed in HEK cells | B | 5.07 | pKi | 8470 | nM | Ki | J Med Chem (1996) 39: 2980-2989 [PMID:8709132] |
| ABCG2/ATP-binding cassette sub-family G member 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5393] [GtoPdb: 792] [UniProtKB: Q9UNQ0] | ||||||||
| ChEMBL | Inhibition of ABCG2 (unknown origin) expressed in human HEK293 cells assessed as reversal of BCRP-mediated mitoxantrone resistance and measured after 90 mins by FACSflow cytometry analysis | B | 4.86 | pIC50 | 13700 | nM | IC50 | Eur J Med Chem (2022) 237: 114346-114346 [PMID:35483322] |
| Farnesoid X receptor/Bile acid receptor FXR in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2047] [GtoPdb: 603] [UniProtKB: Q96RI1] | ||||||||
| ChEMBL | Antagonist activity at human GTS-tagged FXR after 20 mins by TR-FRET assay | B | 5.05 | pIC50 | 8960 | nM | IC50 | Bioorg Med Chem (2013) 21: 4266-4278 [PMID:23688559] |
| CB1 receptor/Cannabinoid CB1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL218] [GtoPdb: 56] [UniProtKB: P21554] | ||||||||
| ChEMBL | DRUGMATRIX: Cannabinoid CB1 radioligand binding (ligand: [3H] SR141716A) | B | 5.86 | pKi | 1371 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Cannabinoid CB1 radioligand binding (ligand: [3H] SR141716A) | B | 5.76 | pIC50 | 1736 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| CYP2C19/Cytochrome P450 2C19 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3622] [GtoPdb: 1328] [UniProtKB: P33261] | ||||||||
| ChEMBL | DRUGMATRIX: CYP450, 2C19 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin) | B | 5.4 | pIC50 | 4000 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| CYP2C9/Cytochrome P450 2C9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3397] [GtoPdb: 1326] [UniProtKB: P11712] | ||||||||
| ChEMBL | DRUGMATRIX: CYP450, 2C9 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin) | B | 6 | pIC50 | 1000 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| Cav1.2/L-type calcium channel alpha-1c/beta-2/alpha2delta-1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL4106164] [GtoPdb: 529] [UniProtKB: P54289, Q08289, Q13936] | ||||||||
| ChEMBL | Inhibition of human alpha1c/beta2a/alpha2delta1 Cav1.2 expressed in HEK293 cells assessed as Ca2+ current at -80 mV holding potential by patch clamp technique | B | 7.53 | pIC50 | 29.8 | nM | IC50 | J Med Chem (2022) 65: 8444-8455 [PMID:35666471] |
| Cav1.2 in Rat [GtoPdb: 529] [UniProtKB: P22002] | ||||||||
| GtoPdb | - | - | 6.8 | pIC50 | - | - | - | J Neurosci (2001) 21: 5944-51 [PMID:11487617] |
| phosphodiesterase 1C/Phosphodiesterase 1C in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4619] [GtoPdb: 1296] [UniProtKB: Q14123] | ||||||||
| ChEMBL | Inhibition of PDE1C (147 to 531 residues) (unknown origin) expressed in Escherichia coli BL21 using [3H]-cGMP as substrate measured for 15 mins by liquid scintillation counter method | B | 5.91 | pIC50 | 1243 | nM | IC50 | J Med Chem (2022) 65: 8444-8455 [PMID:35666471] |
| phosphodiesterase 4D/Phosphodiesterase 4D in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL288] [GtoPdb: 1303] [UniProtKB: Q08499] | ||||||||
| ChEMBL | Inhibition of PDE4D (unknown origin) expressed in Escherichia coli BL21 [3H]-cAMP as substrate measured for 15 mins by liquid scintillation counter method | B | 5.15 | pIC50 | 7150 | nM | IC50 | J Med Chem (2022) 65: 8444-8455 [PMID:35666471] |
| Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364] | ||||||||
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum D10 after 72 hrs by SYBR green assay | F | 4.9 | pIC50 | 12589.25 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum Dd2 after 72 hrs by SYBR green assay | F | 5 | pIC50 | 10000 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay | F | 5 | pIC50 | 10000 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR green assay | F | 5 | pIC50 | 10000 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay | F | 5.1 | pIC50 | 7943.28 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay | F | 5.1 | pIC50 | 7943.28 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay | F | 5.3 | pIC50 | 5011.87 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| Pregnane X receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3401] [GtoPdb: 606] [UniProtKB: O75469] | ||||||||
| ChEMBL | Agonist activity at PXR (unknown origin) expressed in human HepG2 cells assessed as induction of CYP3A4 transactivation after 16 hrs by luciferase reporter gene assay | B | 6.41 | pEC50 | 390 | nM | EC50 | Bioorg Med Chem (2013) 21: 4266-4278 [PMID:23688559] |
| TRPA1/Transient receptor potential cation channel subfamily A member 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075310] [GtoPdb: 485] [UniProtKB: Q8BLA8] | ||||||||
| ChEMBL | Agonist activity at mouse TRPA1 channel expressed in CHO cells assessed as increase in intracellular calcium influx | F | 6.1 | pEC50 | 800 | nM | EC50 | J Med Chem (2010) 53: 5085-5107 [PMID:20356305] |
| 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 | 6.52 | pIC50 | 300 | nM | IC50 | J Appl Toxicol (2012) 32: 858-866 [PMID:22761000] |
| Cav2.1/Cav3.1/Cav1.4/Cav3.2/Cav2.2/Cav1.3/Cav1.1/Cav1.2/Cav2.3/Cav3.3/Voltage-gated calcium channel in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2363032] [GtoPdb: 532, 535, 531, 536, 533, 530, 528, 529, 534, 537] [UniProtKB: O00305, O00555, O43497, O60359, O60840, O95180, P54284, P54289, P62955, Q00975, Q01668, Q02641, Q06432, Q08289, Q13698, Q13936, Q15878, Q7Z3S7, Q8IZS8, Q8WXS5, Q9BXT2, Q9NY47, Q9P0X4, Q9UBN1, Q9UF02, Q9Y698] | ||||||||
| ChEMBL | Inhibition of K+-induced voltage gated calcium channel opening in human SH-SY5Y cells assessed as decrease in Ca2+ level after 10 mins by Fluo-4 dye-based fluorescence assay | B | 4.85 | pIC50 | 14000 | nM | IC50 | Eur J Med Chem (2019) 163: 394-402 [PMID:30530190] |
| GtoPdb | - | - | 6 | pIC50 | ~1000 | nM | IC50 | |
| GtoPdb | - | - | 6 | pIC50 | ~1000 | nM | IC50 | |
| Cav2.1/Cav3.1/Cav1.4/Cav3.2/Cav2.2/Cav1.3/Cav1.1/Cav1.2/Cav2.3/Cav3.3 in Rat [GtoPdb: 532, 535, 531, 536, 533, 530, 528, 529, 534, 537] [UniProtKB: P54282, O54898, Q9EQ60, Q02294, P27732, Q02485, P22002, Q07652, Q9Z0Y8] | ||||||||
| GtoPdb | - | - | 6.6 | pIC50 | - | - | - |
J Neurosci (2001) 21: 5944-51 [PMID:11487617]; J Biol Chem (2001) 276: 38727-37 [PMID:11514547] |
| GtoPdb | - | - | 6.8 | pIC50 | - | - | - | J Neurosci (2001) 21: 5944-51 [PMID:11487617] |
| 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 | 6.96 | pIC50 | 110 | nM | IC50 | J Appl Toxicol (2012) 32: 858-866 [PMID:22761000] |
| Cav1.2 in Rat [GtoPdb: 529] [UniProtKB: P22002] | ||||||||
| GtoPdb | - | - | 6.8 | pIC50 | - | - | - | J Neurosci (2001) 21: 5944-51 [PMID:11487617] |
| Mineralocorticoid receptor in Human [GtoPdb: 626] [UniProtKB: P08235] | ||||||||
| GtoPdb | - | - | 6.8 | pIC50 | 160 | nM | IC50 | Hypertension (2008) 51: 742-8 [PMID:18250364] |
ChEMBL data shown on this page come from version 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]
