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)
  • A1 receptor/Adenosine A1 receptor in Rat [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099]
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  • A2A receptor/Adenosine A2a receptor in Rat [ChEMBL: CHEMBL302] [GtoPdb: 19] [UniProtKB: P30543]
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  • A3 receptor/Adenosine A3 receptor in Human [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
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  • Farnesoid X receptor/Bile acid receptor FXR in Human [ChEMBL: CHEMBL2047] [GtoPdb: 603] [UniProtKB: Q96RI1]
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  • CB1 receptor/Cannabinoid CB1 receptor in Human [ChEMBL: CHEMBL218] [GtoPdb: 56] [UniProtKB: P21554]
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  • TRPA1/Transient receptor potential cation channel subfamily A member 1 in Mouse [ChEMBL: CHEMBL1075310] [GtoPdb: 485] [UniProtKB: Q8BLA8]
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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 Rat [GtoPdb: 529] [UniProtKB: P22002]
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  • Mineralocorticoid receptor in Human [GtoPdb: 626] [UniProtKB: P08235]
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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]
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
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 33:

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]