| ID Source | ID |
|---|---|
| PubMed CID | 5282138 |
| CHEMBL ID | 452076 |
| CHEBI ID | 31399 |
| CHEBI ID | 91506 |
| SCHEMBL ID | 25550 |
| MeSH ID | M0181082 |
| Synonym |
|---|
| 2-methoxyethyl (2e)-3-phenylprop-2-en-1-yl 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate |
| chebi:31399 , |
| AC-270 |
| LS-15175 |
| AKOS005558085 |
| AB01274755-01 |
| AB01274755-02 |
| BRD-A07875874-001-01-6 |
| cinaldipine |
| atelec |
| frc-8653 |
| cinalong |
| cilnidipine , |
| siscard |
| 2-methoxyethyl-3-phenyl-2-propen-1-yl-1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)pyridine-3,5-dicarboxylate |
| cilnidipine [inn] |
| frc 8653 |
| 3,5-pyridinedicarboxylic acid, 1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-, 2-methoxyethyl 3-phenyl-2-propenyl ester, (e)-(+-)- |
| (+-)-(e)-cinnamyl 2-methoxyethyl 1,4-dihydro-2,6-dimethyl-4-(m-nitrophenyl)-3,5-pyridinedicarboxylate |
| cilnidipine, >=98% (hplc), powder |
| D01173 |
| cilnidipine (jp17/inn) |
| atelec (tn) |
| 132203-70-4 |
| NCGC00162150-01 |
| NCGC00162150-02 |
| HMS2089J07 |
| NCGC00162150-03 |
| CHEMBL452076 |
| STK623341 |
| HMS3261E06 |
| 2-methoxyethyl (2e)-3-phenyl-2-propenyl 1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylate |
| C2564 |
| 3-o-(2-methoxyethyl) 5-o-[(e)-3-phenylprop-2-enyl] 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate |
| 97t5az1jip , |
| unii-97t5az1jip |
| dtxcid8026309 |
| dtxsid0046309 , |
| tox21_112001 |
| cas-132203-70-4 |
| HY-17404 |
| CS-1133 |
| LP00422 |
| S1293 |
| cilnidipine [mi] |
| 3,5-pyridinedicarboxylic acid, 1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-, 3-(2-methoxyethyl) 5-((2e)-3-phenyl-2-propen-1-yl) ester |
| cilnidipine [mart.] |
| cilnidipine [jan] |
| 102106-21-8 |
| (+/-)-(e)-cinnamyl 2-methoxyethyl 1,4-dihydro-2,6-dimethyl-4-(m-nitrophenyl)-3,5-pyridinedicarboxylate |
| cilnidipine [who-dd] |
| CCG-221726 |
| CCG-221188 |
| o3-(2-methoxyethyl) o5-(3-phenylprop-2-enyl) 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate |
| gtpl7767 |
| SCHEMBL25550 |
| tox21_112001_1 |
| NCGC00162150-04 |
| KS-1294 |
| 3-cinnamyl 5-(2-methoxyethyl) 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate |
| NCGC00261107-01 |
| tox21_500422 |
| F2173-0669 |
| AB01274755_03 |
| mfcd00865853 |
| DB09232 |
| SR-05000001454-2 |
| sr-05000001454 |
| CHEBI:91506 |
| SR-05000001454-1 |
| bdbm50101813 |
| J-006141 |
| HMS3715N17 |
| SW219784-1 |
| frc-8653; frc 8653; frc8653 |
| BCP22689 |
| HMS3677L13 |
| HMS3413L13 |
| Q731525 |
| SDCCGSBI-0633712.P001 |
| HMS3884K09 |
| NCGC00162150-16 |
| 3,5-pyridinedicarboxylic acid, 1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-, 3-(2-methoxyethyl) 5-[(2e)-3-phenyl-2-propen-1-yl] ester |
| (-)-frc-8653 |
| 4LNU2SU262 , |
| 3,5-pyridinedicarboxylic acid, 1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-, 2-methoxyethyl 3-phenyl-2-propenyl ester, (e)-(-)- |
| cilnidipine, (-)- |
| 118934-76-2 |
| T70209 |
| (e)-cinnamyl 2-methoxyethyl 1,4-dihydro-2,6-dimethyl-4-(m-nitrophenyl)-3,5-pyridinedicarboxylate |
| 3,5-pyridinedicarboxylic acid, 1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-, 2-methoxyethyl 3-phenyl-2-propenyl ester, (e)-(+)- |
| cilnidipine, (+)- |
| 118934-77-3 |
| S85436ZG85 , |
| (+)-frc-8653 |
| unii-4lnu2su262 |
| unii-s85436zg85 |
| 132295-21-7 |
| 132338-87-5 |
| cilnidipine- bio-x |
| BC164309 |
| (z)-cinnamylcilnidipine |
| 3-(2-methoxyethyl) 5-((2e)-3-phenylprop-2-en-1-yl) (4rs)-2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate |
| c08ca14 |
| cilnidipine (mart.) |
| cilnidipino |
| cilnidipinum |
Cilnidipine is a 1,4-dihydropyridine derived L/N-type calcium channel dual blocker possessing neuroprotective and analgesic effects. The drug exhibits a low oral bioavailability or limited clinical efficacy. Cilnodipine therapy is an effective and safe alternative in the treatment of essential hypertension.
Cilnidipine has an advantage of causing less reflex tachycardia, less pedal edema and better control of proteinuria in comparison to L-type CCB. It has a blocking action against N-type calcium channels as well as L- type calcium channels.
Cilnidipine has potent inhibitory both on voltage gated L-type and N-type calcium channels with better anti-proteinuric effect and good tolerability. It has a similar capacity as amlodipine in reducing home BP variability, but the underlying mechanisms in reducing BP variability may differ.
Cilnidipine treatment increased the expression of p85aPI3K (phosphatidylinositol 3-kinase) phosphorylated Akt, and heat shock transcription factor (HSTF-1) in H(2)O(2)-injured nPC12 cells. The decreased blood pressure was maintained until the end of 12 months' observation.
Cilnidipine therapy is an effective and safe alternative in the treatment of essential hypertension. Patients in the cilnidsipine group experienced significantly less adverse effects such as pedal edema and palpitations when compared to those in the amlodipine groups.
| Excerpt | Reference | Relevance |
|---|---|---|
| " This study compared the pharmacokinetic (PK), pharmacodynamic (PD), and tolerability profiles of cilnidipine and valsartan, both alone and in combination, in healthy male subjects." | ( Evaluation of the pharmacokinetic and pharmacodynamic drug interactions between cilnidipine and valsartan, in healthy volunteers. Jang, K; Lee, H; Lee, J; Lim, KS; Shin, D; Yu, KS, 2014) | 0.85 |
Valsartan and cilnidipine are widely coadministered to patients with hypertension. Their drug-drug interaction potential has not been investigated.
| Excerpt | Reference | Relevance |
|---|---|---|
| " We have now compared the effects of the ARB valsartan combined with cilnidipine or amlodipine on cardiac pathophysiology in DS rats." | ( Comparative effects of valsartan in combination with cilnidipine or amlodipine on cardiac remodeling and diastolic dysfunction in Dahl salt-sensitive rats. Harada, E; Hattori, T; Matsuura, N; Murohara, T; Nagasawa, K; Nagata, K; Niinuma, K; Takahashi, K; Takatsu, M; Watanabe, S, 2015) | 0.9 |
| "Although cilnidipine and valsartan are widely coadministered to patients with hypertension, their drug-drug interaction potential has not been investigated." | ( Evaluation of the pharmacokinetic and pharmacodynamic drug interactions between cilnidipine and valsartan, in healthy volunteers. Jang, K; Lee, H; Lee, J; Lim, KS; Shin, D; Yu, KS, 2014) | 1.05 |
Cilnidipine (CND), an anti-hypertensive drug, possesses low oral bioavailability due to its poor aqueous solubility, low dissolution rate, and high gut wall metabolism. The study aimed to improve oralBioavailability of Cilnodipine by increasing its gastrointestinal transit-time and mucoadhesion.
| Excerpt | Reference | Relevance |
|---|---|---|
| " The increased release or bioavailability of NO may causally result from elevated endothelial [Ca(2+)](i) in arteries." | ( Cilnidipine, a slow-acting Ca2+ channel blocker, induces relaxation in porcine coronary artery: role of endothelial nitric oxide and [Ca2+]i. Chen, ZY; Gollasch, M; Huang, Y; Ko, WH; Leung, FP; Leung, HS; Yao, X, 2006) | 1.78 |
| "Cilnidipine (CN) is a novel dihydropyridine calcium antagonist that is practically insoluble in aqueous media and exhibits a low oral bioavailability or limited clinical efficacy." | ( Influence of different polymers on crystallization tendency and dissolution behavior of cilnidipine in solid dispersions. Chen, C; Li, Y; Song, Y; Xie, X; Yan, Z; Yang, X; Zhou, C, 2014) | 2.07 |
| " Thus it can be concluded that solid-SEDDS, amenable for development of solid dosage form, can be successfully developed using Neusilin US2 with the potential of enhancing the solubility, dissolution rate, and bioavailability of the drug." | ( Development and Characterization of Solid Self-emulsifying Drug Delivery System of Cilnidipine. Avari, JG; Bakhle, SS, 2015) | 0.64 |
| "Liquid-liquid phase separation (LLPS) occurs following amorphous solid dispersion (ASD) dissolution when the drug concentration exceeds the "amorphous solubility", and is emerging as an important characteristic of formulations that may enhance the oral bioavailability of poorly soluble drugs." | ( Congruent release of drug and polymer: A "sweet spot" in the dissolution of amorphous solid dispersions. Kestur, US; Mugheirbi, NA; Saboo, S; Taylor, LS; Zemlyanov, DY, 2019) | 0.51 |
| "The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs." | ( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019) | 0.51 |
| "The results demonstrated altered cardiovascular hemodynamics, disturbed cardiovascular autonomic balance, increased levels of VEGF and NOS3, and decreased bioavailability of NO on exposure to chronic sustained hypoxia." | ( Low oxygen microenvironment and cardiovascular remodeling: Role of dual L/N.type Ca Bagali, S; Das, KK; Kulkarni, RV; Naikwadi, AA; Nerune, SM; Patil, BS; Reddy, RC; Yendigeri, SM, ) | 0.13 |
| "Cilnidipine (CND), an anti-hypertensive drug, possesses low oral bioavailability due to its poor aqueous solubility, low dissolution rate, and high gut wall metabolism." | ( Cilnidipine loaded poly (ε-caprolactone) nanoparticles for enhanced oral delivery: optimization using DoE, physical characterization, pharmacokinetic, and pharmacodynamic evaluation. Agarwal, SI; Aggarwal, V; Diwan, R; Ravi, PR, 2021) | 3.51 |
| " Thus the study aimed to improve oral bioavailability of Cilnidipine by increasing its gastrointestinal transit-time and mucoadhesion." | ( Gellan gum based gastroretentive tablets for bioavailability enhancement of cilnidipine in human volunteers. Bali, NR; Karemore, MN, 2021) | 1.1 |
The aim was to develop an eco-friendly, stability-indicating assay method to determine Chlorthalidone (CLD) and Cilnidipine (CIL) in bulk and tablet dosage f.
| Excerpt | Relevance | Reference |
|---|---|---|
| " We studied the effect of morning and bedtime dosing on circadian variation of blood pressure (BP), heart rate (HR), and activity of the autonomic nervous system, using an open randomized crossover study in 13 essential hypertensive patients." | ( Effect of morning and bedtime dosing with cilnidipine on blood pressure, heart rate, and sympathetic nervous activity in essential hypertensive patients. Akao, M; Fujita, H; Hino, T; Kanmatsuse, K; Kitahara, Y; Kushiro, T; Otsuka, Y; Saito, F; Taguchi, H; Takahashi, A, 2004) | 0.59 |
| " CCBs were increased in dosage or other drugs were added until blood pressure decreased below 140/90 mmHg, but no inhibitors of the renin-angiotensin (RA) system were added or changed in dosage." | ( Comparison between cilnidipine and amlodipine besilate with respect to proteinuria in hypertensive patients with renal diseases. Kojima, S; Shida, M; Yokoyama, H, 2004) | 0.65 |
| " Fifty-eight subjects diagnosed with both essential hypertension and morning hypertension (43 currently being treated, 15 new patients) were prescribed cilnidipine at a dosage of 10-20 mg per day for 8 weeks." | ( Beneficial effect of cilnidipine on morning hypertension and white-coat effect in patients with essential hypertension. Yamagishi, T, 2006) | 0.85 |
| " On the other hand, under the condition of Ang II-induced hypertension, administration of a hypotensive dosage of cilnidipine showed no effect on the plasma aldosterone levels, whereas a hypotensive dosage of nifedipine significantly increased the plasma aldosterone levels." | ( L/N-type calcium channel blocker suppresses reflex aldosterone production induced by antihypertensive action. Aritomi, S; Konda, T; Yoshimura, M, 2012) | 0.59 |
| " Thus it can be concluded that solid-SEDDS, amenable for development of solid dosage form, can be successfully developed using Neusilin US2 with the potential of enhancing the solubility, dissolution rate, and bioavailability of the drug." | ( Development and Characterization of Solid Self-emulsifying Drug Delivery System of Cilnidipine. Avari, JG; Bakhle, SS, 2015) | 0.64 |
| " According to literature reports several analytical techniques such as hyphenated techniques, high-performance thin-layer chromatography, high-performance liquid-chromatography, capillary electrophoresis, voltammetry, UV/Vis-spectrophotometry, and Fourier-transform infrared spectroscopy approaches have been used for determination of cilnidipine alone or in the combined dosage form." | ( An Investigative Review for Pharmaceutical Analysis of 1,4-Dihydropyridine-3,5-Dicarboxylic Acid Derivative: Cilnidipine. Chaudhari, SR; Shirkhedkar, AA, 2021) | 1.01 |
| " The aim was to develop an eco-friendly, stability-indicating assay method to determine Chlorthalidone (CLD) and Cilnidipine (CIL) in bulk and tablet dosage form using four different Ultra-Violet (UV) spectrophotometric methods." | ( Multiple spectrophotometric determinations of Chlorthalidone and Cilnidipine using propylene carbonate - As a step towards greenness. Chanduluru, HK; Kannaiah, KP; Sugumaran, A, 2022) | 1.17 |
| Role | Description |
|---|---|
| calcium channel blocker | One of a class of drugs that acts by selective inhibition of calcium influx through cell membranes or on the release and binding of calcium in intracellular pools. |
| antihypertensive agent | Any drug used in the treatment of acute or chronic vascular hypertension regardless of pharmacological mechanism. |
| cardiovascular drug | A drug that affects the rate or intensity of cardiac contraction, blood vessel diameter or blood volume. |
| [role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] | |
| Class | Description |
|---|---|
| dihydropyridine | |
| 2-methoxyethyl ester | A carboxylic ester resulting from the formal condensation between a carboxylic acid and the hydroxy group of 2-methoxyethanol. In contrast to many other water-solubilising esters, the 2-methoxyethyl esters of many amino acids are crystalline, allowing them to be easily purified. |
| C-nitro compound | A nitro compound having the nitro group (-NO2) attached to a carbon atom. |
| [compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] | |
| Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Chain A, Ferritin light chain | Equus caballus (horse) | Potency | 14.1254 | 5.6234 | 17.2929 | 31.6228 | AID485281 |
| thioredoxin reductase | Rattus norvegicus (Norway rat) | Potency | 25.1189 | 0.1000 | 20.8793 | 79.4328 | AID588456 |
| hypoxia-inducible factor 1 alpha subunit | Homo sapiens (human) | Potency | 16.9301 | 3.1890 | 29.8841 | 59.4836 | AID1224846 |
| RAR-related orphan receptor gamma | Mus musculus (house mouse) | Potency | 32.8788 | 0.0060 | 38.0041 | 19,952.5996 | AID1159521; AID1159523 |
| ATAD5 protein, partial | Homo sapiens (human) | Potency | 19.4683 | 0.0041 | 10.8903 | 31.5287 | AID493106; AID493107 |
| Fumarate hydratase | Homo sapiens (human) | Potency | 35.4813 | 0.0030 | 8.7949 | 48.0869 | AID1347053 |
| USP1 protein, partial | Homo sapiens (human) | Potency | 28.3709 | 0.0316 | 37.5844 | 354.8130 | AID504865 |
| TDP1 protein | Homo sapiens (human) | Potency | 25.1618 | 0.0008 | 11.3822 | 44.6684 | AID686978; AID686979 |
| GLI family zinc finger 3 | Homo sapiens (human) | Potency | 23.8675 | 0.0007 | 14.5928 | 83.7951 | AID1259369; AID1259392 |
| AR protein | Homo sapiens (human) | Potency | 24.2241 | 0.0002 | 21.2231 | 8,912.5098 | AID1259243; AID1259247; AID743035; AID743042; AID743054; AID743063 |
| estrogen receptor 2 (ER beta) | Homo sapiens (human) | Potency | 10.5909 | 0.0006 | 57.9133 | 22,387.1992 | AID1259378 |
| nuclear receptor subfamily 1, group I, member 3 | Homo sapiens (human) | Potency | 25.2134 | 0.0010 | 22.6508 | 76.6163 | AID1224838; AID1224839; AID1224893 |
| progesterone receptor | Homo sapiens (human) | Potency | 4.2163 | 0.0004 | 17.9460 | 75.1148 | AID1346795 |
| cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 0.9870 | 0.0123 | 7.9835 | 43.2770 | AID1346984; AID1645841 |
| glucocorticoid receptor [Homo sapiens] | Homo sapiens (human) | Potency | 5.4607 | 0.0002 | 14.3764 | 60.0339 | AID720691; AID720692 |
| retinoic acid nuclear receptor alpha variant 1 | Homo sapiens (human) | Potency | 31.0634 | 0.0030 | 41.6115 | 22,387.1992 | AID1159552; AID1159553; AID1159555 |
| retinoid X nuclear receptor alpha | Homo sapiens (human) | Potency | 10.6822 | 0.0008 | 17.5051 | 59.3239 | AID1159527 |
| estrogen-related nuclear receptor alpha | Homo sapiens (human) | Potency | 14.1245 | 0.0015 | 30.6073 | 15,848.9004 | AID1224819; AID1224820; AID1224821; AID1224841; AID1224842; AID1224848; AID1224849; AID1259401; AID1259403 |
| farnesoid X nuclear receptor | Homo sapiens (human) | Potency | 16.8082 | 0.3758 | 27.4851 | 61.6524 | AID743217; AID743220; AID743239 |
| pregnane X nuclear receptor | Homo sapiens (human) | Potency | 6.0879 | 0.0054 | 28.0263 | 1,258.9301 | AID1346982; AID1346985 |
| estrogen nuclear receptor alpha | Homo sapiens (human) | Potency | 25.2215 | 0.0002 | 29.3054 | 16,493.5996 | AID1259244; AID1259248; AID743069; AID743078; AID743079 |
| G | Vesicular stomatitis virus | Potency | 0.0617 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| cytochrome P450 2D6 | Homo sapiens (human) | Potency | 9.7717 | 0.0010 | 8.3798 | 61.1304 | AID1645840 |
| polyprotein | Zika virus | Potency | 35.4813 | 0.0030 | 8.7949 | 48.0869 | AID1347053 |
| Parkin | Homo sapiens (human) | Potency | 5.1735 | 0.8199 | 14.8306 | 44.6684 | AID720572 |
| peroxisome proliferator-activated receptor delta | Homo sapiens (human) | Potency | 36.5242 | 0.0010 | 24.5048 | 61.6448 | AID743212; AID743227 |
| peroxisome proliferator activated receptor gamma | Homo sapiens (human) | Potency | 14.7553 | 0.0010 | 19.4141 | 70.9645 | AID743094; AID743140; AID743191 |
| vitamin D (1,25- dihydroxyvitamin D3) receptor | Homo sapiens (human) | Potency | 17.2311 | 0.0237 | 23.2282 | 63.5986 | AID743222; AID743241 |
| arylsulfatase A | Homo sapiens (human) | Potency | 5.3582 | 1.0691 | 13.9551 | 37.9330 | AID720538 |
| aryl hydrocarbon receptor | Homo sapiens (human) | Potency | 0.9439 | 0.0007 | 23.0674 | 1,258.9301 | AID743085; AID743122 |
| cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_a | Homo sapiens (human) | Potency | 29.8493 | 0.0017 | 23.8393 | 78.1014 | AID743083 |
| thyroid stimulating hormone receptor | Homo sapiens (human) | Potency | 29.2874 | 0.0016 | 28.0151 | 77.1139 | AID1224843; AID1224895 |
| nuclear receptor subfamily 1, group I, member 2 | Rattus norvegicus (Norway rat) | Potency | 10.0000 | 0.1000 | 9.1916 | 31.6228 | AID1346983 |
| chromobox protein homolog 1 | Homo sapiens (human) | Potency | 25.1189 | 0.0060 | 26.1688 | 89.1251 | AID488953 |
| thyroid hormone receptor beta isoform 2 | Rattus norvegicus (Norway rat) | Potency | 12.8690 | 0.0003 | 23.4451 | 159.6830 | AID743065; AID743067 |
| huntingtin isoform 2 | Homo sapiens (human) | Potency | 35.4813 | 0.0006 | 18.4198 | 1,122.0200 | AID1688 |
| nuclear factor erythroid 2-related factor 2 isoform 1 | Homo sapiens (human) | Potency | 20.2186 | 0.0006 | 27.2152 | 1,122.0200 | AID743202; AID743219 |
| nuclear receptor ROR-gamma isoform 1 | Mus musculus (house mouse) | Potency | 11.6766 | 0.0079 | 8.2332 | 1,122.0200 | AID2546; AID2551 |
| geminin | Homo sapiens (human) | Potency | 29.8554 | 0.0046 | 11.3741 | 33.4983 | AID624297 |
| peripheral myelin protein 22 | Rattus norvegicus (Norway rat) | Potency | 7.2080 | 0.0056 | 12.3677 | 36.1254 | AID624032 |
| Voltage-dependent calcium channel gamma-2 subunit | Mus musculus (house mouse) | Potency | 29.8493 | 0.0015 | 57.7890 | 15,848.9004 | AID1259244 |
| Interferon beta | Homo sapiens (human) | Potency | 11.8160 | 0.0033 | 9.1582 | 39.8107 | AID1347407; AID1645842 |
| HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 0.0617 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| Cellular tumor antigen p53 | Homo sapiens (human) | Potency | 33.4915 | 0.0023 | 19.5956 | 74.0614 | AID651631 |
| Glutamate receptor 2 | Rattus norvegicus (Norway rat) | Potency | 29.8493 | 0.0015 | 51.7393 | 15,848.9004 | AID1259244 |
| Spike glycoprotein | Severe acute respiratory syndrome-related coronavirus | Potency | 1.1220 | 0.0096 | 10.5250 | 35.4813 | AID1479145 |
| Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 0.0617 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| ATPase family AAA domain-containing protein 5 | Homo sapiens (human) | Potency | 26.6032 | 0.0119 | 17.9420 | 71.5630 | AID651632 |
| Ataxin-2 | Homo sapiens (human) | Potency | 31.0423 | 0.0119 | 12.2221 | 68.7989 | AID588378; AID651632 |
| cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 0.0617 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Voltage-dependent L-type calcium channel subunit alpha-1C | Cavia porcellus (domestic guinea pig) | IC50 (µMol) | 5.3000 | 0.0220 | 1.6422 | 8.9000 | AID1207626 |
| Voltage-dependent T-type calcium channel subunit alpha-1H | Homo sapiens (human) | IC50 (µMol) | 24.0000 | 0.0320 | 1.0479 | 3.6000 | AID1724015 |
| Voltage-dependent L-type calcium channel subunit alpha-1C | Rattus norvegicus (Norway rat) | IC50 (µMol) | 5.3000 | 0.0013 | 2.2495 | 6.9000 | AID1207626 |
| Voltage-dependent N-type calcium channel subunit alpha-1B | Homo sapiens (human) | IC50 (µMol) | 17.8667 | 0.0400 | 4.1137 | 10.0000 | AID1724014; AID1850268; AID260460 |
| Voltage-dependent L-type calcium channel subunit alpha-1C | Homo sapiens (human) | IC50 (µMol) | 9.0000 | 0.0003 | 2.2545 | 9.6000 | AID1207626; AID1207627 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1508630 | Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4 | A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
| AID1347154 | Primary screen GU AMC qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1347425 | Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1) | 2019 | The Journal of biological chemistry, 11-15, Volume: 294, Issue:46 | Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens. |
| AID1347105 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347407 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| AID1347097 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
| AID1347107 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347101 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1 | Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
| AID1347098 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347100 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347091 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347106 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347093 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347096 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347089 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
| AID1347103 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347108 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347104 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347082 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1347424 | RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1) | 2019 | The Journal of biological chemistry, 11-15, Volume: 294, Issue:46 | Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens. |
| AID1347094 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347083 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1347099 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347090 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347086 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1347092 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347102 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347095 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID504749 | qHTS profiling for inhibitors of Plasmodium falciparum proliferation | 2011 | Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043 | Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets. |
| AID588378 | qHTS for Inhibitors of ATXN expression: Validation | |||
| AID1347151 | Optimization of GU AMC qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID504812 | Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
| AID1347087 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Confirmatory Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1347059 | CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation | 2019 | PloS one, , Volume: 14, Issue:7 | Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors. |
| AID1347405 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC collection | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| AID1347088 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): Viability assay - Alamar blue signal for LCMV Confirmatory Screen | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1347081 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Confirmatory Screen | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID504836 | Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation | 2002 | The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16 | Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells. |
| AID1347057 | CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation | 2019 | PloS one, , Volume: 14, Issue:7 | Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors. |
| AID588349 | qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay | |||
| AID1347084 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Confirmatory Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1347045 | Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line | 2019 | Science translational medicine, 07-10, Volume: 11, Issue:500 | Inhibition of natriuretic peptide receptor 1 reduces itch in mice. |
| AID1347410 | qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library | 2019 | Cellular signalling, 08, Volume: 60 | A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening. |
| AID1347058 | CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation | 2019 | PloS one, , Volume: 14, Issue:7 | Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors. |
| AID1347049 | Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen | 2019 | Science translational medicine, 07-10, Volume: 11, Issue:500 | Inhibition of natriuretic peptide receptor 1 reduces itch in mice. |
| AID504810 | Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
| AID1347050 | Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay | 2019 | Science translational medicine, 07-10, Volume: 11, Issue:500 | Inhibition of natriuretic peptide receptor 1 reduces itch in mice. |
| AID537132 | Antileishmanial activity against promastigotes of Leishmania amazonensis WHO/BR/00/LT0016 after 18 hrs by MTT assay | 2010 | Bioorganic & medicinal chemistry, Nov-15, Volume: 18, Issue:22 | Anti-leishmanial and anti-trypanosomal activities of 1,4-dihydropyridines: In vitro evaluation and structure-activity relationship study. |
| AID1207627 | Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in Xenopus oocyte heterologically expressing alpha-1C subunit | 2012 | Journal of applied toxicology : JAT, Oct, Volume: 32, Issue:10 | Predictive model for L-type channel inhibition: multichannel block in QT prolongation risk assessment. |
| AID365407 | Inhibition of voltage-dependent L-type calcium channel in rat thoracic aorta ring assessed as effect on high K+ induced contraction by Magnus method | 2008 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 18, Issue:17 | The structure-activity relationship study on 2-, 5-, and 6-position of the water soluble 1,4-dihydropyridine derivatives blocking N-type calcium channels. |
| AID597536 | Inhibition of Voltage-dependent N-type calcium channel- mediated calcium influx in human IMR-32 cells | 2011 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 21, Issue:11 | Asymmetric synthesis and biological evaluations of (+)- and (-)-6-dimethoxymethyl-1,4-dihydropyridine-3-carboxylic acid derivatives blocking N-type calcium channels. |
| AID597537 | Inhibition of Voltage-dependent L-type calcium channel in rat thoracic aorta ring | 2011 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 21, Issue:11 | Asymmetric synthesis and biological evaluations of (+)- and (-)-6-dimethoxymethyl-1,4-dihydropyridine-3-carboxylic acid derivatives blocking N-type calcium channels. |
| AID537135 | Antitrypanosomal activity against trypomastigotes of Trypanosoma cruzi infected in rhesus monkey LLC-MK2 cells after 48 hrs by MTT assay | 2010 | Bioorganic & medicinal chemistry, Nov-15, Volume: 18, Issue:22 | Anti-leishmanial and anti-trypanosomal activities of 1,4-dihydropyridines: In vitro evaluation and structure-activity relationship study. |
| AID537133 | Antileishmanial activity against promastigotes of Leishmania major MHOM/1L/80/Fredlin after 18 hrs by MTT assay | 2010 | Bioorganic & medicinal chemistry, Nov-15, Volume: 18, Issue:22 | Anti-leishmanial and anti-trypanosomal activities of 1,4-dihydropyridines: In vitro evaluation and structure-activity relationship study. |
| AID260460 | Inhibitory activity against N-type calcium channel by calcium influx into IMR32 cells | 2006 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 16, Issue:4 | Structure-activity relationship study of 1,4-dihydropyridine derivatives blocking N-type calcium channels. |
| AID537136 | Cytotoxicity against rhesus monkey LLC-MK2 cells after 48 hrs by MTT assay | 2010 | Bioorganic & medicinal chemistry, Nov-15, Volume: 18, Issue:22 | Anti-leishmanial and anti-trypanosomal activities of 1,4-dihydropyridines: In vitro evaluation and structure-activity relationship study. |
| AID537139 | Cytotoxicity in BALB/c mouse erythrocytes assessed as hemolysis at 50 uM after 3 hrs | 2010 | Bioorganic & medicinal chemistry, Nov-15, Volume: 18, Issue:22 | Anti-leishmanial and anti-trypanosomal activities of 1,4-dihydropyridines: In vitro evaluation and structure-activity relationship study. |
| AID537134 | Antileishmanial activity against promastigotes of Leishmania braziliensis MHO/BR/75/M2903 after 18 hrs by MTT assay | 2010 | Bioorganic & medicinal chemistry, Nov-15, Volume: 18, Issue:22 | Anti-leishmanial and anti-trypanosomal activities of 1,4-dihydropyridines: In vitro evaluation and structure-activity relationship study. |
| AID537131 | Antileishmanial activity against amastigotes of Leishmania chagasi MHOM/BR/1972/LD after 24 hrs by MTT assay | 2010 | Bioorganic & medicinal chemistry, Nov-15, Volume: 18, Issue:22 | Anti-leishmanial and anti-trypanosomal activities of 1,4-dihydropyridines: In vitro evaluation and structure-activity relationship study. |
| AID537137 | Selectivity index, ratio of IC50 for rhesus monkey LLC-MK2 cells to IC50 for amastigotes of Leishmania chagasi MHOM/BR/1972/LD | 2010 | Bioorganic & medicinal chemistry, Nov-15, Volume: 18, Issue:22 | Anti-leishmanial and anti-trypanosomal activities of 1,4-dihydropyridines: In vitro evaluation and structure-activity relationship study. |
| AID260462 | Analgesic effect in rat following foot-pad injection of formalin at 30 mg/kg, po | 2006 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 16, Issue:4 | Structure-activity relationship study of 1,4-dihydropyridine derivatives blocking N-type calcium channels. |
| AID365406 | Inhibition of voltage-dependent N-type calcium channel in human IMR32 cells assessed as effect on calcium influx | 2008 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 18, Issue:17 | The structure-activity relationship study on 2-, 5-, and 6-position of the water soluble 1,4-dihydropyridine derivatives blocking N-type calcium channels. |
| AID1207626 | Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in Xenopus oocyte heterologically expressing alpha-1C subunit | 2012 | Journal of applied toxicology : JAT, Oct, Volume: 32, Issue:10 | Predictive model for L-type channel inhibition: multichannel block in QT prolongation risk assessment. |
| AID1850268 | Inhibition of endogenous human CaV2.2 in human SH-SY5Y cells in presence of nifedipine by Calcium 4 dye based calcium influx fluorescence-imaging assay | 2022 | RSC medicinal chemistry, Feb-23, Volume: 13, Issue:2 | Inhibition of N-type calcium ion channels by tricyclic antidepressants - experimental and theoretical justification for their use for neuropathic pain. |
| AID1724015 | Inhibition of human T type calcium channel Cav3.2 expressed in HEK-293T cells assessed as calcium influx by FRIPR assay | 2020 | Bioorganic & medicinal chemistry, 09-15, Volume: 28, Issue:18 | The neuronal calcium ion channel activity of constrained analogues of MONIRO-1. |
| AID537130 | Antileishmanial activity against promastigotes of Leishmania chagasi MHOM/BR/1972/LD after 18 hrs by MTT assay | 2010 | Bioorganic & medicinal chemistry, Nov-15, Volume: 18, Issue:22 | Anti-leishmanial and anti-trypanosomal activities of 1,4-dihydropyridines: In vitro evaluation and structure-activity relationship study. |
| AID537138 | Selectivity index, ratio of IC50 for rhesus monkey LLC-MK2 cells to IC50 for trypomastigotes of Trypanosoma cruzi | 2010 | Bioorganic & medicinal chemistry, Nov-15, Volume: 18, Issue:22 | Anti-leishmanial and anti-trypanosomal activities of 1,4-dihydropyridines: In vitro evaluation and structure-activity relationship study. |
| AID597538 | Ratio of inhibition of L-type calcium channel to inhibition of N-type calcium channel in rat hypertension model at 3 ug/ml, iv | 2011 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 21, Issue:11 | Asymmetric synthesis and biological evaluations of (+)- and (-)-6-dimethoxymethyl-1,4-dihydropyridine-3-carboxylic acid derivatives blocking N-type calcium channels. |
| AID717844 | Inhibition of mouse Ido2 transfected in HEK293T cells using L-tryptophan as substrate assessed as kynurenine formation at 20 uM after 45 mins by spectrophotometric analysis relative to control | 2012 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 22, Issue:24 | Identification of selective inhibitors of indoleamine 2,3-dioxygenase 2. |
| AID1724014 | Inhibition of human N type calcium channel Cav2.2 endogenously expressed in SH-SY5Y cells assessed as calcium influx by FRIPR assay | 2020 | Bioorganic & medicinal chemistry, 09-15, Volume: 28, Issue:18 | The neuronal calcium ion channel activity of constrained analogues of MONIRO-1. |
| AID260461 | Inhibitory activity against L-type calcium channel in SD rat thoracic aorta by Magnus method | 2006 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 16, Issue:4 | Structure-activity relationship study of 1,4-dihydropyridine derivatives blocking N-type calcium channels. |
| AID1794808 | Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL). | 2014 | Journal of biomolecular screening, Jul, Volume: 19, Issue:6 | A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum. |
| AID1794808 | Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL). | |||
| AID1346693 | Rat Cav2.2 (Voltage-gated calcium channels) | 1997 | The Journal of pharmacology and experimental therapeutics, Mar, Volume: 280, Issue:3 | Effect of cilnidipine, a novel dihydropyridine Ca++-channel antagonist, on N-type Ca++ channel in rat dorsal root ganglion neurons. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 26 (10.92) | 18.2507 |
| 2000's | 84 (35.29) | 29.6817 |
| 2010's | 100 (42.02) | 24.3611 |
| 2020's | 28 (11.76) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.
| This Compound (100.22) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 58 (23.58%) | 5.53% |
| Reviews | 8 (3.25%) | 6.00% |
| Case Studies | 4 (1.63%) | 4.05% |
| Observational | 4 (1.63%) | 0.25% |
| Other | 172 (69.92%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
| Trial | Phase | Enrollment | Study Type | Start Date | Status | ||
|---|---|---|---|---|---|---|---|
| A Randomized, Open-label, Single Dosing, Two-way Crossover Clinical Trial to Compare the Safety/Tolerability and Pharmacokinetics of the Combination of Cilnidipine 10mg and Valsartan 160mg in Comparison to Each Component Coadministered in Healthy Male Vol [NCT02343250] | Phase 1 | 54 participants (Actual) | Interventional | 2015-03-31 | Completed | ||
| Comparison of the Efficacy and Safety of Cilnidipine 10mg/Valsartan 160mg Combination Therapy, Cilnidipine 5mg/Valsartan 160mg Combination Therapy and Valsartan 160mg Monotherapy in Hypertensive Patients Inadequately Controlled With Valsartan 160mg Monoth [NCT02145104] | Phase 3 | 286 participants (Actual) | Interventional | 2014-06-17 | Completed | ||
| Phase II Study for the Second-Line Treatment of Hypertension in Patients With Autosomal Dominant Polycystic Kidney Disease; ACEI vs. CCB [NCT00890279] | Phase 2 | 160 participants (Anticipated) | Interventional | 2009-07-31 | Recruiting | ||
| Comparison Between ARB and ARB Plus CCB on Incidence of Renal and Cardiovascular Events in Hypertensive ADPKD Patients [NCT00541853] | Phase 4 | 150 participants (Anticipated) | Interventional | 2007-12-31 | Not yet recruiting | ||
| A Multi-Center, Double-Blind, Randomized, Superiority Clinical Study to Compare the Effects of Cilnidipine on Metabolic Syndrome Improvement With Nifedipine GITS in Hypertensive Patients With Metabolic Syndrome (Phase IV) [SLIMS] [NCT00325936] | Phase 4 | 186 participants (Actual) | Interventional | 2005-07-31 | Completed | ||
| A Multi-Center, Double Blind, Randomized and Non-Inferiority Clinical Study of Cilnidipine to Compare the Effects on Cerebral Blood Flow With Losartan in Patients With Ischemic Stroke Hypertension [NCT00325637] | Phase 3 | 250 participants (Actual) | Interventional | 2005-01-31 | Completed | ||
| [information is prepared from clinicaltrials.gov, extracted Sep-2024] | |||||||