diltiazem profile

Diltiazem: A benzothiazepine derivative with vasodilating action due to its antagonism of the actions of CALCIUM ion on membrane functions. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

diltiazem : A 5-[2-(dimethylamino)ethyl]-2-(4-methoxyphenyl)-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepin-3-yl acetate in which both stereocentres have S configuration. A calcium-channel blocker and vasodilator, it is used as the hydrochloride in the management of angina pectoris and hypertension. [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]

Pathways (1)

diltiazem is involved in 1 pathway(s), involving a total of 47 unique proteins and 8 unique compounds

ID Source	ID
PubMed CID	39186
CHEMBL ID	23
CHEBI ID	101278
SCHEMBL ID	17776
MeSH ID	M0006434

Synonym
BIDD:GT0548
AC-936
BRD-K24023109-001-02-5
BRD-K24023109-003-03-9
d-(cis)-diltiazem
dilacor-xr
gtpl2298
(2s,3s)-5-[2-(dimethylamino)ethyl]-2-[4-(methyloxy)phenyl]-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepin-3-yl acetate
einecs 255-796-4
dilzen
brn 3573079
dilta-hexal
incoril ap
hsdb 6528
dilcontin
surazem
diltiazemum [inn-latin]
anoheal
1,5-benzothiazepin-4(5h)-one, 3-(acetyloxy)-5-(2-(dimethylamino)ethyl)-2,3-dihydro-2-(4-methoxyphenyl)-, (2s-cis)-
acalix
dilticard
endrydil
diltiazem [inn:ban]
LOPAC0_000327
BPBIO1_000230
NCGC00024309-02
tocris-0685
BIO1_001349
BIO1_000860
BIO1_000371
BSPBIO_000208
[(2s,3s)-5-(2-dimethylaminoethyl)-2-(4-methoxyphenyl)-4-oxo-2,3-dihydro-1,5-benzothiazepin-3-yl] acetate
cardizem (hydrochloride)
mk-793 (malate)
rg 83606 (hydrochloride)
42399-41-7
C06958
diltiazem
(+)-cis-5-[2-(dimethylamino)ethyl]-2,3-dihydro-3-hydroxy-2-(p-methoxyphenyl)-1,5-benzothiazepin-4(5h)-one acetate ester
DB00343
acetic acid (2s,3s)-5-(2-dimethylamino-ethyl)-2-(4-methoxy-phenyl)-4-oxo-2,3,4,5-tetrahydro-benzo[b][1,4]thiazepin-3-yl ester
d-cis-diltiazem
(2s,3s)-5-(2-(dimethylamino)ethyl)-2-(4-methoxyphenyl)-4-oxo-2,3,4,5-tetrahydrobenzo[b][1,4]thiazepin-3-yl acetate
(2s-cis)-3-(acetyloxy)-5-[2-(dimethylamino)ethyl]-2,3-dihydro-2-(4-methoxyphenyl)-1,5-benzothiazepin-4(5h)-one
BSPBIO_001311
PRESTWICK3_000134
NCGC00024309-06
NCGC00024309-05
PRESTWICK1_000134
SPBIO_002147
PRESTWICK0_000134
PRESTWICK2_000134
NCGC00024309-08
NCGC00024309-04
NCGC00024309-07
NCGC00024309-09
HMS1989B13
HMS2089H09
NCGC00024309-10
diltiazem extended release
ditiaz
CHEMBL23 ,
surazem (tn)
diltiazem (inn)
D07845
HMS1791B13
cis-acetic acid 5-(2-dimethylamino-ethyl)-2-(4-methoxy-phenyl)-4-oxo-2,3,4,5-tetrahydro-benzo[b][1,4]thiazepin-3-yl ester
8-chloro-1-methyl-6-phenyl-4h-2,3,5,10b-tetraaza-benzo[e]azulene
acetic acid 5-(2-dimethylamino-ethyl)-2-(4-methoxy-phenyl)-4-oxo-2,3,4,5-tetrahydro-benzo[b][1,4]thiazepin-3-yl ester; hydrochloride
acetic acid (s)-5-(2-dimethylamino-ethyl)-2-(4-methoxy-phenyl)-4-oxo-2,3,4,5-tetrahydro-benzo[b][1,4]thiazepin-3-yl ester
bdbm50004704
acetic acid 5-(2-dimethylamino-ethyl)-2-(4-methoxy-phenyl)-4-oxo-2,3,4,5-tetrahydro-benzo[b][1,4]thiazepin-3-yl ester (diltiazem)
(+)-cis-diltiazem
acetic acid 5-(2-dimethylamino-ethyl)-2-(4-methoxy-phenyl)-4-oxo-2,3,4,5-tetrahydro-benzo[b][1,4]thiazepin-3-yl ester(cis-(+)-diltiazem)
5-(2-dimethylamino-ethyl)-2-(4-methoxy-phenyl)-4-oxo-2,3,4,5-tetrahydro-benzo[b][1,4]thiazepin-3-yl ester(diltiazem)acetic acid
diltiazem;acetic acid 5-(2-dimethylamino-ethyl)-2-(4-methoxy-phenyl)-4-oxo-2,3,4,5-tetrahydro-benzo[b][1,4]thiazepin-3-yl ester
(2s,3s)-5-[2-(dimethylamino)ethyl]-2-(4-methoxyphenyl)-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepin-3-yl acetate
CHEBI:101278 ,
diltiazemum
ethyl 3-amino-1,2,4-triazole-1-carboxylate
NCGC00024309-11
A825887
dtxcid202940
(+)-diltiazem
dtxsid9022940 ,
cas-42399-41-7
tox21_110898
CCG-204422
cis-3-acetoxy-5-(2-(dimethylamino)ethyl)-2,3-dihydro-2-(4-methoxyphenyl)-1,5-benzothiazepin-4(5h)-one
einecs 260-060-0
ee92bbp03h ,
unii-ee92bbp03h
diltiazem [inn]
diltiazem [hsdb]
diltiazem [who-dd]
diltiazem [mi]
diltiazem [vandf]
ditiaz [vandf]
1,5-benzothiazepin-4(5h)-one, 3-(acetyloxy)-5-(u2-(dimethylamino)ethyl)-2,3-dihydro-2-(4-methoxyphenyl)-, (+)-cis-
(+)-5-(2-(dimethylamino)ethyl)-cis-2,3-dihydro-3-hydroxy-2-(p-methoxyphenyl)-1,5-benzothiazepin-4(5h)-one acetate (ester)
AKOS015897257
SCHEMBL17776
NCGC00024309-17
tox21_110898_1
[(2s,3s)-5-[2-(dimethylamino)ethyl]-2-(4-methoxyphenyl)-4-oxo-2,3-dihydro-1,5-benzothiazepin-3-yl] acetate
diltiazen
lithiumdicyclohexylamide
W-106274
methoxyphenyl)-4-oxo-2,3,4,5-
tetrahydrobenzo
[b][1,4]thiazepin-3-yl acetate
(2s,3s)-5-(2-(dimethylamino)ethyl)-2-(4-
Q422229
C9F ,
BRD-K24023109-003-11-2
BRD-K24023109-003-20-3
SDCCGSBI-0050315.P002
NCGC00024309-27
diltiazem free base
42399-41-7 (free base)
NCGC00024309-21
EN300-22049448
CS-0009567
HY-B0632
(2s,3s)-5-(2-(dimethylamino)ethyl)-2-(4-methoxyphenyl)-4-oxo-2,3,4,5-tetrahydrobenzo[b][1,4]thiazepin-3-ylacetate
c08db01
(2s,3s)-5-(2-(dimethylamino)ethyl)-2-(4-methoxyphenyl)-4-oxo-2,3,4,5-tetrahydrobenzo(b)(1,4)thiazepin-3-yl acetate
(+)-cis-5-(2-(dimethylamino)ethyl)-2,3-dihydro-3-hydroxy-2-(p-methoxyphenyl)-1,5-benzothiazepin-4(5h)-one acetate ester
acetic acid (2s,3s)-5-(2-dimethylamino-ethyl)-2-(4-methoxy-phenyl)-4-oxo-2,3,4,5-tetrahydro-benzo(b)(1,4)thiazepin-3-yl ester
diltiazemum (inn-latin)
c05ae03
(2s,3s)-5-(2-(dimethylamino)ethyl)-2-(4-methoxyphenyl)-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepin-3-yl acetate
dtxcid30196864
(2s-cis)-3-(acetyloxy)-5-(2-(dimethylamino)ethyl)-2,3-dihydro-2-(4-methoxyphenyl)-1,5-benzothiazepin-4(5h)-one

Excerpt	Reference
"Diltiazem is a calcium antagonist widely used in the treatment of angina and hypertension. "	( Farmer, PS; Howlett, SE; Li, R; Pleasance, S; Quilliam, MA; Xie, M; Yeung, PK, 1992)
"Diltiazem is a commonly used medication in patients with atrial fibrillation (AF) with potential for a drug-drug interaction (DDI) with direct oral anticoagulants (DOACs). "	( Andrade, JG; Austin, PC; Caswell, J; Jackevicius, CA; Ko, DT; Michael, F; Qiu, F; Shurrab, M; Tu, K, 2023)
"Diltiazem is an antiarrhythmic drug widely used in the treatment of atrial fibrillation (AFib) with rapid ventricular response (RVR). "	( Akkaş, M; Batur, A; Küçük, SH; Metin Aksu, N, 2023)
"Diltiazem is a widely prescribed Ca"	( Catterall, WA; Gamal El-Din, TM; Lenaeus, MJ; Tang, L; Zheng, N, 2019)
"Diltiazem is a calcium-channel blocker commonly used for the treatment of hypertension. "	( Ko, CJ; Siegel, JD, 2020)
"Diltiazem is a benzothiazepine calcium blocker and widely used in renal transplant patients since it improves the level of tacrolimus or cyclosporine A concentration. "	( Ding, JJ; Guan, XF; Li, DY; Ma, RR; Wang, JL; Yin, WJ; Zhou, LY; Zuo, XC, 2018)
"Diltiazem is a nondihydropyridine calcium channel blocker that is used to control rapid ventricular response in patients who have atrial fibrillation or flutter. "	( Jandali, MB, 2018)
"Diltiazem hydrochloride is an antihypertensive agent which undergoes extensive first pass metabolism making it a possible candidate for buccal delivery. "	( Damineni, S; Penjuri, SC; Ravouru, N, 2013)
"Diltiazem is a human therapeutic drug and a member of the group of calcium channel blockers having widespread use in the treatment of angina pectoris and hypertension. "	( Fedorova, G; Golovko, O; Grabic, R; Grabicova, K; Koba, O; Kroupova, HK; Steinbach, C, 2016)
"Diltiazem is a pharmaceutical belonging to a group of calcium channel blockers (CCB) that is widely used in the treatment of angina pectoris and hypertension. "	( Burkina, V; Kolarova, J; Kroupova, HK; Randak, T; Schmidt-Posthaus, H; Stara, A; Steinbach, C; Velisek, J, 2016)
"Diltiazem hydrochloride is a commonly prescribed medication in the treatment of cardiovascular disease. "	( Hanson, M; Petronic-Rosic, V, 2008)
"Diltiazem is a lipophilic cardiotoxic drug, which could be sequestered in an expanded plasma lipid phase."	( Gougnard, T; Hantson, P; Montiel, V, 2011)
"Diltiazem is a calcium channel antagonist that has been commonly associated with currently used immunosuppressants to prevent acute graft rejection in humans. "	( Campanile, D; D'Ambrosio, A; Pugliese, O; Quintieri, F, 2011)
"Diltiazem is a calcium channel blocking agent used for the treatment of hypertension. "	( Jaka, A; Lobo, C; López-Núñez, M; López-Pestaña, A; Ormaechea, N; Tuneu, A, 2011)
"Diltiazem is a calcium channel blocker used to treat cardiovascular ailments. "	( Al-Husein, B; Al-Shabrawey, M; Bollag, WB; Choudhary, V; Davis, M; Dong, Z; El Gaish, M; Kaddour-Djebbar, I; Kumar, MV; Lakshmikanthan, V; Shirley, R; Zhong, R, 2012)
"Diltiazem is an antihypertensive belonging to the class of heart rate-slowing calcium channel blockers; its antihypertensive efficacy has been demonstrated for a long time. "	( Carré, A; Joire, JE; Lequeuche, B; Mounier-Vehier, C, 1999)
"Diltiazem is a benzothiazepine Ca2+ channel blocker used clinically for its antihypertensive and antiarrhythmic effects. "	( Hino, N; Niimi, Y; Ochi, R, 2003)
"Diltiazem is a calcium-channel antagonist commonly prescribed in the treatment of cardiovascular disease. "	( Boyer, M; Katta, R; Markus, R, 2003)
"Diltiazem is a calcium channel blocker that suppresses the activation of a variety of immune cells, such as T and B cells, NK cells, monocytes and dendritic cells (DCs). "	( Coccia, E; D'Ambrosio, A; Giordani, L; Quintieri, F; Severa, M, 2005)
"Diltiazem (DTZ) is an optically active calcium channel blocker having a benzodiazepine structure. "	( Bossù, E; Buiarelli, F; Donati, E; Fanali, S; Montinaro, A; Quaglia, MG, 2005)
"Diltiazem hydrochloride is a commonly prescribed benzothiazepine calcium channel blocker for the treatment of cardiovascular disease. "	( Cohen, SR; Persaud, AN; Phelps, RG; Rudikoff, D; Saladi, RN, 2006)
"Diltiazem is a calcium channel-blocking cardiac antiarrythmic, which also blocks tumor growth and P-glycoprotein."	( Altinoz, MA; Bilir, A; Del Maestro, RF; Gedikoglu, G; Ozcan, E; Tuna, S, 2006)
"Diltiazem (DTZ) is a calcium channel blocker, which is extensively metabolised in the intestine by esterases and different CYP450 isoforms."	( Alvarez, AI; Mendoza, G; Merino, G; Molina, AJ; Prieto, JG; Pulido, MM; Real, R, 2007)
"Diltiazem (DTZ) is a well-known cardiovascular drug used clinically in the treatment of angina pectoris and hypertension. "	( Arayne, MS; Shafi, N; Sultana, N, 2007)
"Diltiazem is a Class III Ca2+ -antagonist."	( Ferry, DR; Glossmann, H; Hofmann, F; Lübbecke, F; Mewes, R, 1983)
"Diltiazem is a potent inhibitor of the slow inward current in ventricular muscle."	( Kanaya, S; Katzung, BG, 1984)
"Diltiazem was found to be a highly effective drug for control of symptoms of active coronary arterial spasm, without side effects and with excellent patient tolerance."	( Baim, DS; Ginsburg, R; Lamb, IH; Rosenthal, SJ; Schroeder, JS, 1980)
"Diltiazem is a calcium slow-channel blocking drug that may be effective in the treatment of chronic stable angina pectoris. "	( Achard, F; Benacerraf, A; Bourassa, MG; Chaitman, BR; Delanguenhagen, B; Ferguson, RJ; Morin, B; Pasternac, A; Wagniart, P, 1982)
"Diltiazem (DZ) is a calcium channel blocking drug which has been shown to be a potent coronary artery dilating agent in the rat. "	( Flaim, SF; Zelis, R, 1981)
"Diltiazem was found to be a coronary vasodilator acting on the large coronary arteries and on collaterals."	( Bourassa, MG; Cote, P; Genain, C; Theroux, P; Tubau, JF; Waters, DD, 1980)
"Diltiazem (DTZ) is a calcium channel blocker widely used in the treatment of angina and hypertension. "	( Caillé, G; du Souich, P; Homsy, W; Lefebvre, M, 1995)
"Diltiazem hydrochloride is a benzothiazepine derivative calcium-channel blocker with proven antianginal and antihypertensive capabilities. "	( Weir, MR, 1995)
"Diltiazem is a calcium channel blocking agent known to be effective in the treatment of angina pectoris, hypertension and supraventricular arrhythmias. "	( Bagheri, H; Bianchetti, G; Dubruc, C; Houin, G; Thénot, JP, 1995)
"Diltiazem is a calcium channel blocker whose effects on left ventricular function (LVF) are controversial. "	( Campelo, M; Cardoso, J; Coutinho, J; Maciel, MJ; Ramalhao, C; Silva, JC; Simoes, L, 1995)
"Diltiazem demonstrated to be an important alternative for the treatment of mild to moderate hypertension due to its beneficial therapeutic effects associated to the once daily dosage."	( Nobre, F; Oigman, W, 1994)
"Diltiazem is a calcium antagonist used in angina pectoris and hypertension. "	( Caillé, G; Du Souich, P; Geadah, D; Gossard, D; Lacasse, Y; Landriault, H; Lefebvre, M; Moisan, R; Spénard, J, 1994)
"Diltiazem is a dihydropyridinic calcium-antagonist which acts an arterial muscle, producing an increase in vascular capacity. "	( Battaglia, M; Carrieri, G; Ciccone, M; D'Orazio, E; Disabato, G; Fiore, T; Martino, P; Nanna, G; Rizzon, P; Tempesta, A, 1994)
"Diltiazem is a calcium channel blocker with antihypertensive and antiarrhythmic actions. "	( Johansson, CG; Lind, L; Lithell, H; Ljunghall, S; Mörlin, C, 1994)
"Diltiazem is a widely used calcium channel blocker, and has been found to be effective in the treatment of hypertension, stable, variant and unstable angina, as well as oesophageal spasm. "	( Mantzoros, CS; Prabhu, AS; Sowers, JR, 1994)
"Diltiazem is an inhibitor of this isozyme and interacts with midazolam, another substrate of this enzyme."	( Neuvonen, PJ; Olkkola, KT; Varhe, A, 1996)
"Diltiazem (DTZ) is a calcium antagonist widely used in the treatment of angina and hypertension. "	( Barclay, KD; Buckley, SJ; Farmer, PS; Feng, JD; Hung, OR; Klassen, GA; Pollak, PT; Yeung, PK, 1996)
"Diltiazem is an inhibitor of this isozyme."	( Kimura, M; Kosuge, K; Nakashima, M; Nishimoto, M; Ohashi, K; Umemura, K, 1997)
"Diltiazem has proven to be an effective antihypertensive and antianginal agent, due to its potent calcium channel blocking activity. "	( Eradiri, O; Midha, KK, 1997)
"Diltiazem is a calcium antagonist widely used for the treatment of angina and hypertension. "	( Feng, JD; Tsui, BC; Yeung, PK, 1998)
"Diltiazem is a substrate and an inhibitor of CYP3A enzymes and is commonly coadministered with cholesterol-lowering agents such as simvastatin."	( Brater, DC; Hall, SD; Mousa, O; Sunblad, KJ, 2000)
"Diltiazem hydrochloride is a widely used calcium channel blocking agent. "	( Lee, MW; Lim, HW; Scherschun, L, 2001)
"Thus diltiazem appears to be a promising adjunct in the treatment of hemorrhagic shock even in the absence of blood resuscitation."	( Ba, ZF; Chaudry, IH; Meldrum, DR; Wang, P, 1992)
"Thus diltiazem is a useful adjuvant in the treatment of sepsis because it restores gut absorptive capacity to normal and allows for early enteral nutrition."	( Chaudry, IH; Chaudry, KI; Chudler, LC; Singh, G, 1992)
"Diltiazem is an excellent antianginal agent."	( Fagan, TC, 1991)
"Diltiazem (DTZ) is a calcium antagonist widely used in the treatment of angina and related heart diseases. "	( Klassen, GA; McGilveray, IJ; Mosher, SJ; Yeung, PK, 1991)
"Diltiazem is a commonly prescribed calcium-channel antagonist for hypertension and ischemic heart disease. "	( Geraets, DR; Wirebaugh, SR, 1990)
"Diltiazem is a calcium antagonist effective in the treatment of stable, variant and unstable angina pectoris and mild to moderate systemic hypertension, with a generally favourable adverse effect profile. "	( Buckley, MM; Goa, KL; Grant, SM; McTavish, D; Sorkin, EM, 1990)
"Diltiazem is an effective means for the treatment of PVCs and AF-mediated tachyarrhythmias during anesthesia."	( Amaha, K; Iwatsuki, N; Katoh, M; Ono, K, 1985)
"Diltiazem appears to be an effective detrusor muscle relaxant and may be useful for the treatment of disturbances of micturition due to detrusor hyperactivity."	( Conti, M; Faustini, S; Magistretti, MJ; Pizzi, P; Salvini, A; Vescovini, R, 1989)
"Diltiazem is a calcium channel blocker whose effects lie between those of the two other important calcium antagonists nifedipine and verapamil. "	( Bachmann, B; Boldt, J; Hempelmann, G; Kling, D; Moosdorf, R, 1988)
"Diltiazem is a calcium antagonist with demonstrated experimental cardioprotective effects. "	( Amor, M; Bertrand, A; Ethevenot, G; Gilgenkrantz, JM; Karcher, G; Maurin, P; Pernot, C; Sebag, C; Zannad, F, 1988)
"Diltiazem was found to be a safe and effective drug for controlling anginal attacks in patients with unstable angina."	( Colombo, G; Grieco, A; Planca, E; Vescovini, R; Zucchella, G, 1987)
"Diltiazem is an effective agent for control of ventricular response, both at rest and during exercise, in digoxin-treated patients with chronic atrial fibrillation."	( Bren, GB; Buff, LA; Katz, RJ; Steinberg, JS; Varghese, PJ, 1987)
"Diltiazem is an effective antianginal agent and may be beneficial as an antiarrhythmic agent, but it is largely untested in patients with systemic or pulmonary hypertension, Raynaud's disease, and hypertrophic cardiomyopathy."	( Hillis, LD; Winniford, MD, 1985)
"Diltiazem is an orally and intravenously active calcium channel blocking agent shown to be an effective and well-tolerated treatment for stable angina and angina due to coronary artery spasm. "	( Brogden, RN; Chaffman, M, 1985)

Excerpt	Reference
"Diltiazem has a negative inotropic effect and may cause hemodynamic decompensation in patients with reduced ejection fraction."	( Jandali, MB, 2018)
"Diltiazem cream has a better side effect profile than glyceryl trinitrate cream and is better tolerated. "	( King, Q; Marshall, D; Siva, G; Zargar, H, 2015)
"Diltiazem overdose has a high mortality rate due to cardiotoxicity associated with bradycardia and hypotension. "	( Fujita, Y; Kitamura, H; Maruyama, S; Nomura, A; Ohyama, Y; Ryuge, A; Shimizu, H; Yamaguchi, M, 2016)
"Diltiazem, which has an established role in the management of atrial fibrillation, may prove to be well suited for prophylaxis due to low cost and relative safety."	( Buchert, B; Dobrilovic, N; Vadlamani, L; Wright, CB, 2005)
"Diltiazem has a clinically significant interaction with oral triazolam. "	( Neuvonen, PJ; Olkkola, KT; Varhe, A, 1996)
"Diltiazem has a relatively favourable safety and tolerability profile, and is available in a once-daily dosage form."	( Boulet, AP; Chockalingam, A; Fodor, JG; Langer, A; Nadeau, C; Rakusan, K; Savard, D, 1997)
"Diltiazem.HCl has an aqueous solubility greater than 590 mg/ml (37 degrees C) and was released from controlled-porosity osmotic pump devices with first-order kinetics."	( Engle, K; McClelland, GA; Sutton, SC; Zentner, GM, 1991)
"Diltiazem has a protective effect against primary transplant failure following cadaver kidney transplantation. "	( Albrecht, S; Neumayer, HH; Wagner, K, 1986)
"Diltiazem has a negative inotropic effect and may cause hemodynamic decompensation in patients with reduced ejection fraction."	( Jandali, MB, 2018)
"Diltiazem cream has a better side effect profile than glyceryl trinitrate cream and is better tolerated. "	( King, Q; Marshall, D; Siva, G; Zargar, H, 2015)
"Diltiazem overdose has a high mortality rate due to cardiotoxicity associated with bradycardia and hypotension. "	( Fujita, Y; Kitamura, H; Maruyama, S; Nomura, A; Ohyama, Y; Ryuge, A; Shimizu, H; Yamaguchi, M, 2016)
"Diltiazem has been used for post-transplant hypertension, but the mechanism underlying its protective effect of endothelial cells against angiotensin II (Ang II) - induced impairment remains unclear. "	( Chen, Q; Guan, X; Guo, R; Jia, S; Wang, J; Yang, M; Zhou, L; Zuo, S; Zuo, X, 2017)
"Diltiazem has several advantages: the application frequency is only twice daily, no systemic side-effects have been reported, the total costs of treatment are lower than the costs of ISDN and a standard preparation of diltiazem ointment is available."	( Boeker, EB; Kruijer, MJ; Verbeek, PC, 2011)
"Diltiazem, which has an established role in the management of atrial fibrillation, may prove to be well suited for prophylaxis due to low cost and relative safety."	( Buchert, B; Dobrilovic, N; Vadlamani, L; Wright, CB, 2005)
"Diltiazem has been shown to exert beneficial effects in patients with acute coronary syndrome."	( Dubey, L; Hesong, Z, 2006)
"Diltiazem has been studied in a limited group of normal subjects, with considerable interindividual variation in plasma levels after fixed oral doses."	( McAllister, RG, 1982)
"Diltiazem has been proposed to act by blocking calcium channels of cardiac and smooth muscle since it has pharmacological [12-14] and clinical [10] effects that resemble those of verapamil, an agent that has been shown to block these channels [3]. "	( Arlock, P; Hondeghem, LM; Kanaya, S; Katzung, BG, 1983)
"Diltiazem, however, has the advantage of being a potent blood pressure-lowering agent, with afterload reduction and increased stroke index, with less pronounced catecholamine increase, and without tachycardia."	( Brandt, D; Härringer, M; Klein, W; Vrecko, K, 1983)
"Diltiazem at 100 microM has no effect on K+-evoked release of [3H]norepinephrine at 0.15 mM calcium but does inhibit release at 2.0 mM calcium."	( Daly, JW; Ebstein, RP, 1982)
"Diltiazem has been reported to prevent postreperfusion myocardial damage but its beneficial effects on coronary blood-flow regulation remain uncertain."	( Buluran, J; Cartier, R; Dagenais, F; Hollmann, C, 1995)
"Diltiazem has a clinically significant interaction with oral triazolam. "	( Neuvonen, PJ; Olkkola, KT; Varhe, A, 1996)
"Diltiazem has a relatively favourable safety and tolerability profile, and is available in a once-daily dosage form."	( Boulet, AP; Chockalingam, A; Fodor, JG; Langer, A; Nadeau, C; Rakusan, K; Savard, D, 1997)
"Diltiazem has proven to be an effective antihypertensive and antianginal agent, due to its potent calcium channel blocking activity. "	( Eradiri, O; Midha, KK, 1997)
"Diltiazem has been associated with a variety of cutaneous reactions that appear to occur more frequently than with other calcium channel blockers."	( Gupta, AK; Knowles, S; Shear, NH, 1998)
"Diltiazem has cardioprotective properties following myocardial ischemic injury. "	( Higuchi, H; Katsumata1, N; Ma, X, 2000)
"Diltiazem has electrophysiologic effects similar to those of verapamil. "	( Dias, VC; Dougherty, AH; Friday, KJ; Jackman, WM; Naccarelli, GV, 1992)
"Diltiazem has been reported to reduce the short-term in-hospital reinfarction rate in patients with a non-Q wave myocardial infarction. "	( Dwyer, EM; Greenberg, H; Hager, WD; Wong, SC, 1992)
"As diltiazem has been in use for more than 10 years and its dosage has been gradually diminished, the risk of a new long-term iatrogenic pathological process is becoming less and less conceivable."	( Djian, J, 1990)
"Diltiazem.HCl has an aqueous solubility greater than 590 mg/ml (37 degrees C) and was released from controlled-porosity osmotic pump devices with first-order kinetics."	( Engle, K; McClelland, GA; Sutton, SC; Zentner, GM, 1991)
"Diltiazem has recently been tested with apparent benefit in non-Q-wave myocardial infarction."	( Opie, LH, 1988)
"Diltiazem has been reported to decrease or not to affect digoxin elimination. "	( Andrejak, M; Andrejak, MT; Hary, L; Lesbre, JP, 1987)
"Diltiazem has a protective effect against primary transplant failure following cadaver kidney transplantation. "	( Albrecht, S; Neumayer, HH; Wagner, K, 1986)
"Diltiazem has also shown substantial efficacy in the treatment of unstable angina, hypertension, and supraventricular tachyarrhythmias, but further study is necessary before its place in the treatment of these diseases may be clearly established."	( Brogden, RN; Chaffman, M, 1985)

Excerpt	Reference
"diltiazem doses were lower than recommended and many of these patients required additional rate control medications to achieve a therapeutic response."	( DiDomenico, RJ; Gasbarro, NM, 2019)
"Diltiazem may suppress sympathetic activity in the hyperacute stage of aneurysmal SAH."	( Kurita, H; Nakajima, H; Ogura, T; Ooigawa, H; Takeda, R, 2015)
"Diltiazem did not increase Ca2+ uptake in the cch1Delta and mid1Delta single mutants and the cch1Delta mid1Delta double mutant, indicating that the diltiazem-induced increase in Ca2+ uptake is completely dependent on Cch1-Mid1."	( Goto, R; Iida, H; Iida, K; Kojima, I; Teng, J, 2008)
"Diltiazem can produce a characteristic lichenoid dermatitis with reticulated hyperpigmentation on sun-exposed areas."	( Jaka, A; Lobo, C; López-Núñez, M; López-Pestaña, A; Ormaechea, N; Tuneu, A, 2011)
"Diltiazem plays more important role than nitroglycerin in the prevention of vasospasm."	( Acikel, U; Aslan, O; Catalyürek, H; Elar, Z; Erdal, C; Hepağuşlar, H; Tabel, Y, 2004)
"Diltiazem does not inhibit intracellular calcium release nor cause net calcium extrusion up to concentrations of 10(-5) M."	( Fahim, M; Mangel, A; Meisheri, K; van Breemen, C, 1982)
"Diltiazem did not cause tachycardia in either strain."	( Nagao, T; Narita, H; Yabana, H; Yamaguchi, I, 1983)
"Diltiazem could increase significantly the RMBF in the border area."	( Ando, F; Kawakita, S; Kinoshita, M; Miyazaki, M; Mori, A; Okada, Y; Okunishi, H; Sono, J; Toda, N, 1981)
"SR diltiazem formulations enable safe and close regimen adjustments in mild-to-moderate essential hypertension."	( Ollivier, JP; Stalla-Bourdillon, A; Wajman, A, 1995)
"Diltiazem also seems to increase the free fraction of bupivacaine and thus to decrease the percentage of protein binding."	( Bruguerolle, B; Lorec, AM, 1994)
"Diltiazem did not increase urine volume significantly."	( Shimada, H; Sugino, H, 1997)
"Diltiazem prevented an increase in the weight of the right ventricle (0.69 +/- 0.03 g/kg, P < 0.05) and LVDd (7.7 +/- 0.2 mm, P < 0.05 to MI)."	( Akioka, K; Iwao, H; Izutani, S; Kim, S; Nakamura, Y; Omura, T; Takeuchi, K; Yoshikawa, J; Yoshiyama, M, 1999)
"Diltiazem can blunt acute hyperdynamic responses after electroconvulsive therapy, but seizure duration is also significantly reduced, possibly making this therapy less effective."	( Imanaga, K; Inoue, T; Ogawa, R; Ogura, A; Shiga, T; Wajima, Z; Yoshikawa, T, 2001)
"Diltiazem failed to inhibit the activation of HSF."	( Chang, J; Cornelussen, RN; Knowlton, AA; Wasser, JS, 2001)
"Diltiazem is known to increase the serum concentration of simvastatin."	( Byrd, RP; Fields, CL; Kanathur, N; Mathai, MG; Roy, TM, 2001)
"Diltiazem at a lower concentration (1.1 X 10(-7) M) caused a reduction in the contractile force of K-depolarized papillary muscle without producing significant changes in the resting and action potentials."	( Hoshiyama, M; Kiyomoto, A; Nakajima, H; Yamashita, K, 1976)
"Diltiazem causes an increase in systemic oxygen delivery index by promoting vasodilation, but it does not change systemic oxygen consumption index in comparison to placebo treatment. "	( Ahnefeld, FW; Ensinger, H; Lindner, KH; Prengel, AW; Schürmann, W, 1992)
"Diltiazem did not produce significant changes of AUC, Cl, and t1/2 for the acid metabolite of nifedipine."	( Ebihara, A; Hosoda, S; Kumagai, Y; Ohashi, K; Sakamoto, K; Sudo, T; Sugimoto, K; Tateishi, T; Toyo-oka, T; Toyosaki, N, 1990)
"Diltiazem and verapamil inhibit oxidative drug metabolism both in vivo and in vitro. "	( Bottorff, MB; Herring, VL; Hunt, BA; Lalonde, RL; Self, TH, 1990)
"Diltiazem did not inhibit the Ang-II-induced increases in both BP and TPRI."	( Aoki, K; Kawaguchi, Y; Sato, K, 1985)
"Diltiazem did not inhibit bindings of 3H-dihydromorphine (3H-DHM), 3H-ethylketocyclazocine (3H-EKCZ) and 3H-naloxone (3H-NOX) but inhibited binding of 3H-[D-Ala2, D-Leu5]-enkephalin (3H-DADLE)."	( Ishizuka, Y; Oka, T, 1987)
"Diltiazem may increase glomerular filtration rate via attenuation of the intrarenal effects of angiotensin II or norepinephrine."	( Bauer, JH; Reams, G; Sunderrajan, S, 1985)
"Diltiazem did not increase PGE2 and 6-keto PGF1a production by cultured cells nor did it affect the cellular level of endogenous sulfhydryls."	( Ivey, KJ; Razandi, M; Romano, M, 1988)
"Diltiazem may increase nifedipine drug levels when the drugs are combined."	( Allen, L; Charlap, S; Cinnamon, J; Frishman, W; Kimmel, B; Strom, J; Teicher, M, 1988)

Excerpt	Reference
"Diltiazem co-treatment, either with gemcitabine or 5-FU, synergistically reduced cell viability, induced apoptosis, and caused cell cycle arrest. "	( El-Husseiny, AA; El-Mahdy, HA; Gamal El-Din, AM; Kandil, YI, 2020)
"In diltiazem-treated animals, prestin levels were not elevated above baseline but ABR thresholds were elevated on days 1 to 3."	( Bonaiuto, G; Cox, R; Naples, J; Parham, K, 2018)
"Oral diltiazem treatment in therapeutic dosage before and during the implantation period did not cause any change in normal uterine milieu during the window of implantation."	( Banerjee, A; Nivsarkar, M; Padh, H, 2009)
"Diltiazem treatment (10 mg/kg/d) had essentially no effect on WT and V394L GCase protein or activity levels (<1.2-fold) in liver."	( Grabowski, GA; Liou, B; Quinn, B; Ran, H; Sun, Y; Xu, YH, 2009)
"This diltiazem co-treatment regime applied to the nearly 1800 surviving renal allograft patients followed up in Hospital Authority hospitals could have saved approximately HK dollars 14.3 million ( pound 1.17 million) annually, without adverse sequelae."	( Chan, TM; Haycox, A; Kou, M; Kumana, CR; Lauder, IJ; Lee, JS; Li, CS; Tong, MK; Walley, T, 2003)
"Diltiazem pretreatment was found to prevent cyanide induced changes in both the amines in the corpus striatum."	( Mathangi, DC; Namasivayam, A, 2004)
"As diltiazem pretreatment did not alter fexofenadine pharmacokinetics, therapeutic doses of diltiazem are unlikely to affect the P-glycoprotein activity in vivo."	( Shimizu, M; Sugawara, K; Tateishi, T; Uno, T, 2006)
"Diltiazem treatment induced a decrease in heart rate from 68 +/- 12 to 55 +/- 9 beats/min (p less than 0.001)."	( Collignon, P; Kulbertus, HE; Legrand, V; Materne, P; Vandormael, M, 1984)
"Diltiazem-treated male rats showed decreased VLDL particle size, together with a shift to shorter-chain fatty acids in the triacylglycerols."	( Dolphin, PJ; Graham, SE; Russell, JC; Stewart, B, 1995)
"Diltiazem or felodipine treatment significantly increased afferent diameter by 5.6 +/- 2.3 and 16.4 +/- 4.6%, respectively (P < 0.05)."	( Belott, TP; Cook, AK; Inscho, EW; Navar, LG; Ohishi, K, 1995)
"Diltiazem treatment was associated with reductions in fasting serum insulin levels in both the men (from 91 +/- 14 to 56 +/- 12 pmol/L; P < 0.03) and women (from 92 +/- 20 to 48 +/- 9 pmol/L; P = 0.05)."	( Beer, NA; Beer, RM; Jakubowicz, DJ; Nestler, JE, 1994)
"Diltiazem pretreatment increased QTc and PR intervals and decreased heart rate and diastolic blood pressure."	( Carignan, G; Carrier, K; Davies, RF; Foris, K; Goernert, L; Laganière, S; McGilveray, I; Pereira, C, 1996)
"Diltiazem treated animals showed a reduction in the lesion severity, at the level of aortic valves, coronary arteries and aortic arch; we assume that Diltiazem acts on the early phases of atherosclerosis by blocking the lipid transport and accumulation into the subendothelial space."	( Pojoga, L; Raicu, M; Simionescu, M; Simionescu, N, 1996)
"Diltiazem-treated patients received a slow intravenous loading dose of 20 mg, followed by 10 mg intravenously every 4 hours for 24 to 36 hours, then 180 to 240 mg orally daily for 1 month."	( Amar, D; Bains, MS; Burt, ME; Downey, RJ; Ginsberg, RJ; Leung, DH; Roistacher, N; Rusch, VW, 1997)
"Diltiazem pretreatment significantly increased the area under the triazolam concentration-time curve (8.0 +/- 2.4 to 18.2 +/- 3.1 ng ml-1 h; P < 0.001; mean +/- s.d.). "	( Kimura, M; Kosuge, K; Nakashima, M; Nishimoto, M; Ohashi, K; Umemura, K, 1997)
"Diltiazem pretreatment (DP) group: Diltiazem was administered intravenously 1.5 micrograms/kg/min before operation to after operation continuously."	( Kimura, H; Koike, R; Kondo, K; Morita, M; Oku, T; Ozeki, M; Satoh, H; Sawada, Y; Shiguma, S; Suma, H, 1989)
"Diltiazem-treated patients (n = 271) were similar to the control patients (n = 143) in terms of age (64 versus 61 years; p = 0.14), ejection fraction (0.46 versus 0.47; p = 0.61), baseline serum creatinine level (1.2 versus 1.1 mg/dL; p = 0.27), prevalence of comorbid conditions, and surgical characteristics. "	( Diab, A; Kirsh, MM; Young, EW, 1998)
"Diltiazem treatment had no effect on the increase in plasma ET-1 following CsA administration."	( Asberg, A; Berg, KJ; Christensen, H; Hartmann, A, 1998)
"The diltiazem+ radiation treated group showed significant tumor regression (in approximately/= 65% of the animals) and enhanced animal survival. "	( Jagannathan, NR; Jain, PC; Jain, V; Kasiviswanathan, A; Muruganandham, M; Raghunathan, P, 1999)
"Diltiazem treatment resulted in a significant mean increase in the area under the concentration time curve (AUC) for CsA of 51(8)% (P < 0.008) and a peak concentration (Cmax) of 34(8)% (P < 0.05), without altering time to peak concentration (tmax). "	( Asberg, A; Berg, KJ; Carlson, E; Christensen, H; Hartmann, A; Molden, E, 1999)
"Diltiazem pretreatment could be considered as only a second choice treatment in those patients in whom amiodarone is contraindicated."	( Capucci, A; Piepoli, MF; Terracciano, C; Villani, GQ, 2000)
"Diltiazem treatment decreased tumor growth over time compared to control groups. "	( Jensen, RL; Wurster, RD, 2001)
"Diltiazem treatment of septic rats significantly decreased basal cytosolic [Ca2+], cellular exchangeable Ca2+ content, Ca2+ flux, CD, and TBA-RS."	( Rose, S; Sayeed, MM; Thompson, KD, 1992)
"Diltiazem pretreatment afforded significant protection of left ventricular function."	( Gilliland, MG; Jolly, SR; Mehta, P; Movahed, A; Mozingo, S; Reeves, WC; Wilson, E, 1992)
"Diltiazem treatment resulted in reduced 24-hour mortality."	( Goto, M; Hurley, RM; Lichtenberg, RC; Zeller, WP, 1992)
"Diltiazem pretreatment slightly, but not significantly decreased blood pressure after MPC-1304 dosing."	( Ebihara, A; Fujimura, A; Kumagai, Y; Ohashi, K; Sakamoto, K; Shiga, T; Sudo, T; Tateishi, T, 1992)
"Diltiazem-treated animals were resuscitated faster and required fewer defibrillation attempts than did dogs in the other groups."	( Capparelli, EV; Chow, MS; Dipersio, DM; Fieldman, A; Hanyok, JJ; Kluger, J, 1992)
"Diltiazem treatment significantly reduced the plasma glucose and heart rate during hemorrhagic shock (P less than 0.05)."	( Dulchavsky, SA; Geller, ER; Kreis, DJ; Krikhely, M; Maitra, SR, 1991)
"Diltiazem-treated hearts showed a concentration-dependent decrease in tissue ATP utilization that was associated with the decrease in tissue lactate during ischemia."	( London, RE; Murphy, E; Norris, TA; Steenbergen, C; Watts, JA, 1990)
"Diltiazem-treated rats showed Ca granules in the bile canaliculi around the terminal hepatic veins and Kupffer cells 6 h after intragastric injection."	( Gohara, S; Inomata, R; Itoh, S; Matsuyama, Y; Yamagishi, F, 1990)
"The Diltiazem treatment do not increase the negative inotropic effect of Thiopental but the effect of Dobutamine is less important in pretreated group."	( Barale, F; Capellier, G; Coste, Y; Kantelip, JP; Magnin, P; Stimmesse, B, 1991)
"Diltiazem treatment (2 X 30 mg/kg p.o."	( Jurásková, V; Sládek, T, 1990)
"Diltiazem treatment increased net sodium efflux and potassium influx.(ABSTRACT TRUNCATED AT 250 WORDS)"	( Gadgil, UG; Khalil-Manesh, F; Samant, DR; Venkataraman, K, 1987)
"Diltiazem treatment returned the half-maximal Ca2+ uptake toward control values in bacteremic rat muscles."	( Sayeed, MM; Westfall, MV, 1989)
"Diltiazem treatment led to an effective but incomplete control of blood pressure (from 208 +/- 5 mm Hg in the untreated hypertensive group to 155 +/- 3 mm Hg in the treated hypertensive group; p less than 0.01) associated with a significant but incomplete decrease of the left ventricular mass (from 3.10 +/- 0.19 mg/g in untreated hypertensive rats to 2.35 +/- 0.04 mg/g in treated hypertensive rats; p less than 0.01)."	( Besse, PJ; Bonoron-Adèle, SM; Grellet, JP; Tariosse, LJ, 1988)
"Diltiazem treatment reduced blood pressure and ventricular weight in SHR."	( Kohno, M; Kurihara, N; Murakawa, K; Takeda, T; Yasunari, K; Yokokawa, K, 1988)
"Diltiazem pretreatment diminished the cocaine effect on skin temperature, but did not otherwise alter the response to cocaine."	( Hooker, WD; Jones, RT; Mendelson, J; Rowbotham, MC, 1987)
"With diltiazem treatment, 3-hydroxymethylantipyrine was decreased, with no significant change in 4-hydroxyantipyrine, norantipyrine or antipyrine."	( Abernethy, DR; Carrum, G; Dickinson, TH; Egan, JM, 1988)
"Diltiazem treatment of endotoxic rats restored the exchangeable Ca2+ level to that found in controls."	( Maitra, SR; Sayeed, MM, 1987)
"In diltiazem-treated SHR, cardiac index (CI) and stroke volume index (SI) were significantly increased and total peripheral resistance and the index of left ventricular compliance (delta P/delta V) were significantly decreased compared with untreated SHR."	( Horie, R; Kihara, M; Mori, C; Nishio, T; Watanabe, K; Yamori, Y, 1988)
"In diltiazem-treated hearts, a bell-shaped curve was also observed, however, its optimum was shifted to the right and downwards (20 min of ischemia gave maximum vulnerability [41%] to reperfusion-induced arrhythmias)."	( Hearse, DJ; Szekeres, L; Tosaki, A, 1987)
"Diltiazem treatment did not alter the mean (SD) cardiothoracic ratio on chest x ray (0.47 (0.06) before vs 0.48 (0.05) after) or the left ventricular ejection fraction at rest (0.28 (0.09) before vs 0.26 (0.08) after)."	( Mankes, S; Nikitopoulos, C; Perlmutter, S; Zema, MJ, 1987)
"3. Diltiazem treatment did not affect the pressor responses to i.v."	( Staszewska-Woolley, J, 1987)
"Diltiazem treatment was associated with an increase in high-density lipoprotein cholesterol (52 to 60 mg/dl, p less than 0.006) and a decrease in total cholesterol:high-density lipoprotein cholesterol ratio (4.7 to 4.2, p less than 0.05).(ABSTRACT TRUNCATED AT 250 WORDS)"	( Pool, PE; Salel, AF; Seagren, SC, 1985)
"Diltiazem-treated animals had decreased cerebral H2O content, but had a marked increase in the area of nonperfused brain, a finding associated with the high incidence of transtentorial herniation in the diltiazem-treated animals."	( Dempsey, RJ; Donaldson, DL; Meyer, KL; Roy, MW; Tibbs, PA; Young, AB, 1985)
"Treatment with diltiazem was associated with a greater incidence of bradycardia compared to IV metoprolol (13% vs."	( Barton, CA; Feeney, ME; Mah, ND; Ran, R; Rowe, SLB, 2018)
"PEI treated diltiazem resin complex loaded beads were characterized by morphology, drug entrapment efficiency, in vitro and in vivo release behaviour."	( Maiti, S; Ray, S; Sa, B, 2010)
"Pretreatment of diltiazem could protect the heart against hypoxia-reoxygenation injury by attenuation of dephosphorylation of Cx43. "	( Amano, A; Kurihara, H; Matsushita, S; Okada, T; Sakai, T; Watanabe, M, 2011)
"Pretreatment with diltiazem (40 and 80 mg/kg) and verapamil (40 mg/kg) also increased morphine level in the brain."	( Fukazawa, Y; Kishioka, S; Maeda, T; Ozaki, M; Shimizu, N; Yamamoto, C; Yamamoto, H, 2004)
"Treatment with diltiazem XC 180 mg was initiated in group 2 patients."	( Casanova, A; Fitchett, DH; Goodman, SG; Jaffer, S; Kornilova, O; Langer, A; Tan, M, 2006)
"Treatment with diltiazem (CAS 33286-22-5, 42399-41-7) was changed to treatment with benidipine (CAS 91599-74-5) and the parameters such as angina frequency, duration, blood pressure, heart rate, electrocardiogram and hematological parameters (serum NO(x), plasma cGMP) were measured and compared."	( Akimoto, Y; Daida, H; Suzuki, H; Yokoyama, K, 2007)
"Treatment with diltiazem prevented the loss of spheres from mitochondrial membranes during the calcium paradox (75.5 +20 5.0 micrometer)."	( Ashraf, M; Benedict, J; Rahamathulla, PM; Sato, S, 1982)
"Treatment with diltiazem resulted in a significant lengthening of sinus cycle length (SCL, p < 0.04), AH interval (p < 0.02), and Wenckebach CL (WCL, p < 0.001), and a trend towards an increase in sinus node recovery time (SNRT, p = 0.057)."	( Biscione, F; Lanza, GA; Manzoli, A; Natale, A; Santarelli, P, 1994)
"Treatment with diltiazem induced a non-significant reduction in heart rate with 3 beats min-1 and decreased blood pressure (-11/-9 mm Hg, p < 0.001)."	( Johansson, CG; Lind, L; Lithell, H; Ljunghall, S; Mörlin, C, 1994)
"Pretreatment with diltiazem at a dose of 2 mg kg-1 intravenously protected against sudden death induced by intravenous administration of endothelin-1 (ET-1, 5 nmol kg-1), with an apparent decrease in the plasma immunoreactive-ET-1 (IR-ET-1) in mice. "	( Ashizawa, N; Kobayashi, F; Matsuura, A; Okumura, H, 1994)
"Co-treatment with diltiazem, however, did not affect the response to potassium chloride (20-80 mM), endothelin-1 (10(-9) to 10(-7) M) or phenylephrine (10(-9) to 10(-6) M)."	( Auch-Schwelk, W; Bossaller, C; Fleck, E; Götze, S; Thelen, J, 1993)
"Treatment with diltiazem improved the recovery of left ventricular developed pressure to 96.9% +/- 3.5% at 3 x 10(-8) mol/L and reduced creatine kinase leakage and mitochondrial damage."	( Abe, T; Akita, T; Kato, S; Kodama, I; Toyama, J, 1993)
"Treatment with diltiazem and methyldopa augmented GFR, but only diltiazem decreased UP significantly."	( Bernheim, J; Green, J; Haskiah, A; Podjarny, E; Pomeranz, A; Rathaus, M, 1995)
"Pretreatment with diltiazem significantly reduced the number of cells of the spinal trigeminal nucleus labelled after corneal stimulation with acid."	( Belmonte, C; Martinez, S, 1996)
"Pretreatment with diltiazem significantly (p < 0.05) increased the area under the curve of quinidine from 7414 +/- 1965 to 11,213 +/- 2610 ng.hr/ml and increased its terminal elimination half-life (t1/2) from 6.8 +/- 1.1 to 9.3 +/- 1.5 hours. "	( Carignan, G; Carrier, K; Davies, RF; Foris, K; Goernert, L; Laganière, S; McGilveray, I; Pereira, C, 1996)
"Treatment with diltiazem or quinapril does not have undesirable effects on glucose metabolism."	( Araújo, D; Cabezas-Cerrato, J; Garcia-Estevez, DA; Iglesias, M, 1997)
"Pretreatment with diltiazem accelerated the recovery of radiation induced weight loss also."	( Ganguly, SK; Goel, HC; Jain, V; Prasad, J, 1996)
"Pretreatment with diltiazem inhibited AGEP-BSA-induced elevation in concentration- and time-dependent manners."	( Liu, NF; Xie, PL; Zhou, QG, 1997)
"Pretreatment with diltiazem inhibited the AGEP-induced elevation of cytosolic free calcium."	( Liu, NF; Xie, PL; Zhou, QG, 1997)
"Treatment with diltiazem before and during ischemia (bolus 200 microg/kg and 15 microg/kg per minute for 25 min, i.v.; 575 microg/kg total) showed slightly depressed hemodynamic parameters, while l-cis diltiazem (1150 microg/kg) had no effect."	( Nagao, T; Nishida, M; Sakamoto, K; Urushidani, T, 1999)
"Pretreatment with diltiazem (10-40 mg/kg, i.m.) 30 min before administration of morphine (0.3 to 10 mg/kg) or heroin (0.03 to 1.0 mg/kg) produced a dose-dependent potentiation of the opioid-induced analgesia."	( Kishioka, S; Ko, MC; Woods, JH, 2000)
"Treatment with diltiazem retard significantly decreased 24h average blood pressure and heart rate by 11.6+/-3.6/5.7+/-1.8mmHg and 5.0+/-1.1 beats/min, respectively. "	( Kawano, Y; Makino, Y; Okuda, N; Omae, T; Takishita, S, 2000)
"Treatment with diltiazem was more costly ($16,340 versus $1,096)."	( Aldea, GS; Alkon, JD; Keaney, JF; Macron, DS; Shapira, OM; Shemin, RJ; Vita, JA, 2000)
"Treatment with diltiazem completely suppressed the development of calcinosis."	( Akiyama, T; Ichiki, Y; Kitajima, Y; Kondo, N; Shimozawa, N; Suzuki, Y, 2001)
"Pretreatment with diltiazem prevented the reduction in both adenosine triphosphate and creatine phosphate induced by 2.5 mg/kg of isoproterenol."	( Takenaka, F; Takeo, S, 1977)
"Pretreatment with diltiazem did not fully prevent the effects of ischemic superfusion; however, the ischaemia-induced decrease in length constant was not significant in the presence of diltiazem."	( Fujiki, A; Knilans, TK; Lathrop, DA; Murphy, AM; Nánási, PP; Schwartz, A; Varró, A, 1992)
"Pretreatment with diltiazem (10(-4) M; n = 10) did not change the amplitude or shape of the ET-induced Cai transient."	( Sturek, M; Wagner-Mann, C, 1991)
"Treatment with diltiazem brought about a similar tendency, though the effect did not reach statistical significance."	( Jankowska, E; Kostowski, W; Pucilowski, O, 1991)
"Treatment with diltiazem resulted in a decrease in diastolic pressure only."	( Abraham, AS; Barchilon, E; Brooks, BA; Eylath, U; Grafstein, Y; Nubani, N; Shemesh, O, 1991)
"Pretreatment with diltiazem reduced the incidence of Z-disc damage, but the degree of alpha-actinin labeling at the endplate was less than that seen with diltiazem alone."	( Hopkins, WF; Kriho, N; Kriho, V; Matsumura, F; Meshul, CK; Pappas, GD, 1990)
"When treated with diltiazem, beginning 1 day before induction of hemorrhage and continuing to the time of sacrifice, arterial diameter was reduced at only 1 of the 6 standard sites of measurement and then by only a small amount."	( Bevan, JA; Bevan, RD; Frazee, JG, 1985)
"Pretreatment with diltiazem (10(-6) M) had no effect on endothelium-dependent relaxations to acetylcholine in femoral artery rings."	( Hoeffner, U; Rubanyi, GM; Schwartz, A; Vanhoutte, PM, 1988)
"Pretreatment with diltiazem (150 micrograms/kg), a calcium entry blocker, significantly attenuated the reduction of coronary vasodilatory responses, but glyceryl trinitrate (nitroglycerin) did not affect the phenomenon of coronary reactivity."	( Haraoka, S; Hasui, M; Hina, K; Kusachi, S; Mima, T; Saito, D; Tsuji, T; Ueeda, M; Watanabe, H; Yamada, N, 1989)
"Treatment with diltiazem alone, its dose adjusted on an individual basis, controlled arterial blood pressure in 58% of the patients."	( Ivleva, AIa; Krasnobaeva, GM; Lepakhin, VK; Moiseev, VS; Ogoliuk, LIu, 1989)
"Pretreatment with diltiazem modified an MH response."	( Denborough, MA; Foster, PS; Hopkinson, KC, 1989)
"Pretreatment with diltiazem did not prevent the drug-induced damage."	( Ivey, KJ; Razandi, M; Romano, M, 1988)
"Pretreatment with diltiazem and verapamil did not influence the magnitude of these changes but reduced the drop in s-urate."	( Hansen, O; Johansson, BW; Juul-Möller, S; Svensson, O, 1988)
"Treatment with diltiazem significantly improved contractile function, and metabolic parameters."	( Harwell, T; Maiorano, P; Watts, J, 1987)
"Pretreatment with diltiazem, a potent calcium antagonist, also definitely depressed the vasoconstriction by 5-HT, as well as that by potassium chloride (KCl)."	( Chiba, S; Tsuji, T, 1987)
"Pretreatment with diltiazem markedly attenuated the cyanide-induced tremors."	( Isom, GE; Johnson, JD; Meisenheimer, TL, 1986)
"pretreatment with diltiazem, diltiazem attenuated the pressor responses to angiotensin II."	( Ijichi, H; Inoue, A; Iyoda, I; Okajima, H; Sasaki, S; Takahashi, H; Takeda, K; Yoneda, S; Yoshimura, M, 1985)

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.
vasodilator agent	A drug used to cause dilation of the blood vessels.
antihypertensive agent	Any drug used in the treatment of acute or chronic vascular hypertension regardless of pharmacological mechanism.
[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
5-[2-(dimethylamino)ethyl]-2-(4-methoxyphenyl)-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepin-3-yl acetate	A lactam that is 2,3-dihydro-1,5-benzothiazepin-4(5H)-one in which positions 2 and 3 are substituted by 4-methoxyphenyl and acetoxy, respectively, while the hydrogen attached to the nitrogen is substituted by a 2-(dimethylamino)ethyl group.
[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]

Pathway	Proteins	Compounds
Diltiazem Action Pathway	47	8

Protein	Taxonomy	Measurement	Average (µ)	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASE	Homo sapiens (human)	Potency	1.2589	0.0032	45.4673	12,589.2998	AID2517
thioredoxin reductase	Rattus norvegicus (Norway rat)	Potency	4.7444	0.1000	20.8793	79.4328	AID488773; AID588453
RAR-related orphan receptor gamma	Mus musculus (house mouse)	Potency	0.7498	0.0060	38.0041	19,952.5996	AID1159521
GLS protein	Homo sapiens (human)	Potency	16.9036	0.3548	7.9355	39.8107	AID624146; AID624170
TDP1 protein	Homo sapiens (human)	Potency	20.8611	0.0008	11.3822	44.6684	AID686978; AID686979
thyroid stimulating hormone receptor	Homo sapiens (human)	Potency	31.6228	0.0013	18.0743	39.8107	AID926; AID938
estrogen receptor 2 (ER beta)	Homo sapiens (human)	Potency	29.8493	0.0006	57.9133	22,387.1992	AID1259377
regulator of G-protein signaling 4	Homo sapiens (human)	Potency	0.5896	0.5318	15.4358	37.6858	AID504845
cytochrome P450 family 3 subfamily A polypeptide 4	Homo sapiens (human)	Potency	3.9046	0.0123	7.9835	43.2770	AID1645841
glucocorticoid receptor [Homo sapiens]	Homo sapiens (human)	Potency	24.0732	0.0002	14.3764	60.0339	AID720691; AID720692
retinoid X nuclear receptor alpha	Homo sapiens (human)	Potency	23.9145	0.0008	17.5051	59.3239	AID1159527
estrogen-related nuclear receptor alpha	Homo sapiens (human)	Potency	15.9464	0.0015	30.6073	15,848.9004	AID1224841; AID1224842; AID1224848; AID1224849; AID1259401; AID1259403
pregnane X nuclear receptor	Homo sapiens (human)	Potency	21.2020	0.0054	28.0263	1,258.9301	AID1346982; AID1346985
estrogen nuclear receptor alpha	Homo sapiens (human)	Potency	30.2510	0.0002	29.3054	16,493.5996	AID743069; AID743075; AID743080; AID743091
cytochrome P450 2D6	Homo sapiens (human)	Potency	38.9018	0.0010	8.3798	61.1304	AID1645840
glucocerebrosidase	Homo sapiens (human)	Potency	39.8107	0.0126	8.1569	44.6684	AID2101
euchromatic histone-lysine N-methyltransferase 2	Homo sapiens (human)	Potency	2.3088	0.0355	20.9770	89.1251	AID504332
D(1A) dopamine receptor	Homo sapiens (human)	Potency	0.8199	0.0224	5.9449	22.3872	AID488982
thyroid hormone receptor beta isoform 2	Rattus norvegicus (Norway rat)	Potency	29.8493	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
cytochrome P450 3A4 isoform 1	Homo sapiens (human)	Potency	3.9811	0.0316	10.2792	39.8107	AID884; AID885
histone acetyltransferase KAT2A isoform 1	Homo sapiens (human)	Potency	39.8107	0.2512	15.8432	39.8107	AID504327
lamin isoform A-delta10	Homo sapiens (human)	Potency	25.1189	0.8913	12.0676	28.1838	AID1487
Gamma-aminobutyric acid receptor subunit pi	Rattus norvegicus (Norway rat)	Potency	3.9811	1.0000	12.2248	31.6228	AID885
Polyunsaturated fatty acid lipoxygenase ALOX15B	Homo sapiens (human)	Potency	12.5893	0.3162	12.7657	31.6228	AID881
Cellular tumor antigen p53	Homo sapiens (human)	Potency	33.4915	0.0023	19.5956	74.0614	AID651631
Gamma-aminobutyric acid receptor subunit beta-1	Rattus norvegicus (Norway rat)	Potency	3.9811	1.0000	12.2248	31.6228	AID885
Gamma-aminobutyric acid receptor subunit delta	Rattus norvegicus (Norway rat)	Potency	3.9811	1.0000	12.2248	31.6228	AID885
Gamma-aminobutyric acid receptor subunit gamma-2	Rattus norvegicus (Norway rat)	Potency	3.9811	1.0000	12.2248	31.6228	AID885
Gamma-aminobutyric acid receptor subunit alpha-5	Rattus norvegicus (Norway rat)	Potency	3.9811	1.0000	12.2248	31.6228	AID885
Gamma-aminobutyric acid receptor subunit alpha-3	Rattus norvegicus (Norway rat)	Potency	3.9811	1.0000	12.2248	31.6228	AID885
Gamma-aminobutyric acid receptor subunit gamma-1	Rattus norvegicus (Norway rat)	Potency	3.9811	1.0000	12.2248	31.6228	AID885
Gamma-aminobutyric acid receptor subunit alpha-2	Rattus norvegicus (Norway rat)	Potency	3.9811	1.0000	12.2248	31.6228	AID885
Gamma-aminobutyric acid receptor subunit alpha-4	Rattus norvegicus (Norway rat)	Potency	3.9811	1.0000	12.2248	31.6228	AID885
Gamma-aminobutyric acid receptor subunit gamma-3	Rattus norvegicus (Norway rat)	Potency	3.9811	1.0000	12.2248	31.6228	AID885
Gamma-aminobutyric acid receptor subunit alpha-6	Rattus norvegicus (Norway rat)	Potency	3.9811	1.0000	12.2248	31.6228	AID885
Histamine H2 receptor	Cavia porcellus (domestic guinea pig)	Potency	12.5893	0.0063	8.2350	39.8107	AID881
Spike glycoprotein	Severe acute respiratory syndrome-related coronavirus	Potency	39.8107	0.0096	10.5250	35.4813	AID1479145
Gamma-aminobutyric acid receptor subunit alpha-1	Rattus norvegicus (Norway rat)	Potency	3.9811	1.0000	12.2248	31.6228	AID885
Gamma-aminobutyric acid receptor subunit beta-3	Rattus norvegicus (Norway rat)	Potency	3.9811	1.0000	12.2248	31.6228	AID885
Gamma-aminobutyric acid receptor subunit beta-2	Rattus norvegicus (Norway rat)	Potency	3.9811	1.0000	12.2248	31.6228	AID885
GABA theta subunit	Rattus norvegicus (Norway rat)	Potency	3.9811	1.0000	12.2248	31.6228	AID885
Gamma-aminobutyric acid receptor subunit epsilon	Rattus norvegicus (Norway rat)	Potency	3.9811	1.0000	12.2248	31.6228	AID885
[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)
Solute carrier family 22 member 1	Homo sapiens (human)	IC50 (µMol)	12.4000	0.2100	5.5537	10.0000	AID386625
ATP-binding cassette sub-family C member 3	Homo sapiens (human)	IC50 (µMol)	133.0000	0.6315	4.4531	9.3000	AID1473740
Multidrug resistance-associated protein 4	Homo sapiens (human)	IC50 (µMol)	133.0000	0.2000	5.6774	10.0000	AID1473741
Voltage-dependent L-type calcium channel subunit alpha-1C	Cavia porcellus (domestic guinea pig)	IC50 (µMol)	0.4500	0.0220	1.6422	8.9000	AID1207183
Voltage-dependent L-type calcium channel subunit alpha-1F	Homo sapiens (human)	IC50 (µMol)	0.6050	0.0003	2.6311	9.0000	AID1207183; AID1207736
Bile salt export pump	Homo sapiens (human)	IC50 (µMol)	134.0000	0.1100	7.1903	10.0000	AID1443980; AID1473738
ATP-dependent translocase ABCB1	Homo sapiens (human)	IC50 (µMol)	54.7351	0.0002	2.3185	10.0000	AID310120; AID310122; AID364884; AID395103; AID681335
Cytochrome P450 3A4	Homo sapiens (human)	IC50 (µMol)	109.5533	0.0001	1.7536	10.0000	AID428564; AID625251
Cytochrome P450 3A4	Homo sapiens (human)	Ki	1.3500	0.0001	1.4162	9.9000	AID589126; AID589142
Cytochrome P450 2C9	Homo sapiens (human)	IC50 (µMol)	50.0000	0.0000	2.8005	10.0000	AID1210069
Voltage-dependent L-type calcium channel subunit alpha-1C	Rattus norvegicus (Norway rat)	IC50 (µMol)	18.1376	0.0013	2.2495	6.9000	AID1207642; AID415101; AID566279; AID751691
Voltage-dependent L-type calcium channel subunit alpha-1C	Rattus norvegicus (Norway rat)	Ki	0.1323	0.0008	0.5796	5.4000	AID415111; AID751691; AID95603
Voltage-dependent L-type calcium channel subunit alpha-1D	Rattus norvegicus (Norway rat)	IC50 (µMol)	0.8960	0.0013	1.9915	10.0000	AID415101; AID566279; AID751691
Voltage-dependent L-type calcium channel subunit alpha-1D	Rattus norvegicus (Norway rat)	Ki	0.0585	0.0008	0.7410	5.4000	AID415111; AID751691
Sodium channel protein type 1 subunit alpha	Homo sapiens (human)	IC50 (µMol)	9.0000	0.0023	2.8296	9.0000	AID1207154
Sodium channel protein type 4 subunit alpha	Homo sapiens (human)	IC50 (µMol)	9.0000	0.0001	3.5075	10.0000	AID1207154
5-hydroxytryptamine receptor 7	Cavia porcellus (domestic guinea pig)	IC50 (µMol)	12.4000	2.0300	5.5313	9.9000	AID386625
Cytochrome P450 2J2	Homo sapiens (human)	IC50 (µMol)	50.0000	0.0120	2.5312	9.4700	AID1210069
Sodium channel protein type 7 subunit alpha	Homo sapiens (human)	IC50 (µMol)	9.0000	0.0360	3.7335	9.0000	AID1207154
Voltage-dependent L-type calcium channel subunit alpha-1D	Homo sapiens (human)	IC50 (µMol)	0.6050	0.0003	2.5955	9.0000	AID1207183; AID1207736
Voltage-dependent L-type calcium channel subunit alpha-1S	Rattus norvegicus (Norway rat)	IC50 (µMol)	0.8960	0.0013	1.6020	6.9000	AID415101; AID566279; AID751691
Voltage-dependent L-type calcium channel subunit alpha-1S	Rattus norvegicus (Norway rat)	Ki	0.0585	0.0008	0.6673	5.4000	AID415111; AID751691
Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)	IC50 (µMol)	17.3557	0.0009	1.9014	10.0000	AID1207213; AID161281; AID243151; AID243188; AID408340; AID420668; AID82355
Voltage-dependent L-type calcium channel subunit alpha-1S	Homo sapiens (human)	IC50 (µMol)	0.6050	0.0003	2.6311	9.0000	AID1207183; AID1207736
Voltage-dependent L-type calcium channel subunit alpha-1C	Homo sapiens (human)	IC50 (µMol)	15.0700	0.0003	2.2545	9.6000	AID1207183; AID1207642; AID1207736
Sodium channel protein type 5 subunit alpha	Homo sapiens (human)	IC50 (µMol)	9.0000	0.0003	3.6484	9.2000	AID1207154
Sodium channel protein type 9 subunit alpha	Homo sapiens (human)	IC50 (µMol)	9.0000	0.0060	2.7749	9.0000	AID1207154
Canalicular multispecific organic anion transporter 1	Homo sapiens (human)	IC50 (µMol)	133.0000	2.4100	6.3433	10.0000	AID1473739
Sodium channel protein type 2 subunit alpha	Homo sapiens (human)	IC50 (µMol)	9.0000	0.0000	3.7401	10.0000	AID1207154
Sodium channel protein type 3 subunit alpha	Homo sapiens (human)	IC50 (µMol)	9.0000	0.0053	2.8085	9.0000	AID1207154
Sodium channel protein type 11 subunit alpha	Homo sapiens (human)	IC50 (µMol)	9.0000	0.0300	4.3695	9.0000	AID1207154
Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)	IC50 (µMol)	851.1380	0.0040	1.9666	10.0000	AID364887
Sodium channel protein type 8 subunit alpha	Homo sapiens (human)	IC50 (µMol)	9.0000	0.0011	3.4705	9.0000	AID1207154
Sodium channel protein type 10 subunit alpha	Homo sapiens (human)	IC50 (µMol)	9.0000	0.0080	3.1752	9.0000	AID1207154
[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)
Cytochrome P450 3A4	Homo sapiens (human)	Km	23.0000	1.9300	5.9060	8.7000	AID1209243
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Process	via Protein(s)	Taxonomy
xenobiotic metabolic process	Solute carrier family 22 member 1	Homo sapiens (human)
neurotransmitter transport	Solute carrier family 22 member 1	Homo sapiens (human)
serotonin transport	Solute carrier family 22 member 1	Homo sapiens (human)
establishment or maintenance of transmembrane electrochemical gradient	Solute carrier family 22 member 1	Homo sapiens (human)
organic cation transport	Solute carrier family 22 member 1	Homo sapiens (human)
quaternary ammonium group transport	Solute carrier family 22 member 1	Homo sapiens (human)
prostaglandin transport	Solute carrier family 22 member 1	Homo sapiens (human)
monoamine transport	Solute carrier family 22 member 1	Homo sapiens (human)
putrescine transport	Solute carrier family 22 member 1	Homo sapiens (human)
spermidine transport	Solute carrier family 22 member 1	Homo sapiens (human)
acetylcholine transport	Solute carrier family 22 member 1	Homo sapiens (human)
dopamine transport	Solute carrier family 22 member 1	Homo sapiens (human)
norepinephrine transport	Solute carrier family 22 member 1	Homo sapiens (human)
thiamine transport	Solute carrier family 22 member 1	Homo sapiens (human)
xenobiotic transport	Solute carrier family 22 member 1	Homo sapiens (human)
epinephrine transport	Solute carrier family 22 member 1	Homo sapiens (human)
serotonin uptake	Solute carrier family 22 member 1	Homo sapiens (human)
norepinephrine uptake	Solute carrier family 22 member 1	Homo sapiens (human)
thiamine transmembrane transport	Solute carrier family 22 member 1	Homo sapiens (human)
metanephric proximal tubule development	Solute carrier family 22 member 1	Homo sapiens (human)
purine-containing compound transmembrane transport	Solute carrier family 22 member 1	Homo sapiens (human)
dopamine uptake	Solute carrier family 22 member 1	Homo sapiens (human)
monoatomic cation transmembrane transport	Solute carrier family 22 member 1	Homo sapiens (human)
transport across blood-brain barrier	Solute carrier family 22 member 1	Homo sapiens (human)
(R)-carnitine transmembrane transport	Solute carrier family 22 member 1	Homo sapiens (human)
acyl carnitine transmembrane transport	Solute carrier family 22 member 1	Homo sapiens (human)
spermidine transmembrane transport	Solute carrier family 22 member 1	Homo sapiens (human)
cellular detoxification	Solute carrier family 22 member 1	Homo sapiens (human)
xenobiotic transport across blood-brain barrier	Solute carrier family 22 member 1	Homo sapiens (human)
lipid metabolic process	Polyunsaturated fatty acid lipoxygenase ALOX15B	Homo sapiens (human)
phospholipid metabolic process	Polyunsaturated fatty acid lipoxygenase ALOX15B	Homo sapiens (human)
apoptotic process	Polyunsaturated fatty acid lipoxygenase ALOX15B	Homo sapiens (human)
negative regulation of cell population proliferation	Polyunsaturated fatty acid lipoxygenase ALOX15B	Homo sapiens (human)
positive regulation of macrophage derived foam cell differentiation	Polyunsaturated fatty acid lipoxygenase ALOX15B	Homo sapiens (human)
arachidonic acid metabolic process	Polyunsaturated fatty acid lipoxygenase ALOX15B	Homo sapiens (human)
negative regulation of cell migration	Polyunsaturated fatty acid lipoxygenase ALOX15B	Homo sapiens (human)
prostate gland development	Polyunsaturated fatty acid lipoxygenase ALOX15B	Homo sapiens (human)
regulation of epithelial cell differentiation	Polyunsaturated fatty acid lipoxygenase ALOX15B	Homo sapiens (human)
positive regulation of chemokine production	Polyunsaturated fatty acid lipoxygenase ALOX15B	Homo sapiens (human)
positive regulation of peroxisome proliferator activated receptor signaling pathway	Polyunsaturated fatty acid lipoxygenase ALOX15B	Homo sapiens (human)
positive regulation of keratinocyte differentiation	Polyunsaturated fatty acid lipoxygenase ALOX15B	Homo sapiens (human)
negative regulation of cell cycle	Polyunsaturated fatty acid lipoxygenase ALOX15B	Homo sapiens (human)
negative regulation of growth	Polyunsaturated fatty acid lipoxygenase ALOX15B	Homo sapiens (human)
hepoxilin biosynthetic process	Polyunsaturated fatty acid lipoxygenase ALOX15B	Homo sapiens (human)
endocannabinoid signaling pathway	Polyunsaturated fatty acid lipoxygenase ALOX15B	Homo sapiens (human)
cannabinoid biosynthetic process	Polyunsaturated fatty acid lipoxygenase ALOX15B	Homo sapiens (human)
lipoxin A4 biosynthetic process	Polyunsaturated fatty acid lipoxygenase ALOX15B	Homo sapiens (human)
linoleic acid metabolic process	Polyunsaturated fatty acid lipoxygenase ALOX15B	Homo sapiens (human)
lipid oxidation	Polyunsaturated fatty acid lipoxygenase ALOX15B	Homo sapiens (human)
lipoxygenase pathway	Polyunsaturated fatty acid lipoxygenase ALOX15B	Homo sapiens (human)
xenobiotic metabolic process	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
xenobiotic transmembrane transport	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
bile acid and bile salt transport	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
glucuronoside transport	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
xenobiotic transport	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
transmembrane transport	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
leukotriene transport	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
monoatomic anion transmembrane transport	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
transport across blood-brain barrier	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
prostaglandin secretion	Multidrug resistance-associated protein 4	Homo sapiens (human)
cilium assembly	Multidrug resistance-associated protein 4	Homo sapiens (human)
platelet degranulation	Multidrug resistance-associated protein 4	Homo sapiens (human)
xenobiotic metabolic process	Multidrug resistance-associated protein 4	Homo sapiens (human)
xenobiotic transmembrane transport	Multidrug resistance-associated protein 4	Homo sapiens (human)
bile acid and bile salt transport	Multidrug resistance-associated protein 4	Homo sapiens (human)
prostaglandin transport	Multidrug resistance-associated protein 4	Homo sapiens (human)
urate transport	Multidrug resistance-associated protein 4	Homo sapiens (human)
glutathione transmembrane transport	Multidrug resistance-associated protein 4	Homo sapiens (human)
transmembrane transport	Multidrug resistance-associated protein 4	Homo sapiens (human)
cAMP transport	Multidrug resistance-associated protein 4	Homo sapiens (human)
leukotriene transport	Multidrug resistance-associated protein 4	Homo sapiens (human)
monoatomic anion transmembrane transport	Multidrug resistance-associated protein 4	Homo sapiens (human)
export across plasma membrane	Multidrug resistance-associated protein 4	Homo sapiens (human)
transport across blood-brain barrier	Multidrug resistance-associated protein 4	Homo sapiens (human)
guanine nucleotide transmembrane transport	Multidrug resistance-associated protein 4	Homo sapiens (human)
visual perception	Voltage-dependent L-type calcium channel subunit alpha-1F	Homo sapiens (human)
detection of light stimulus involved in visual perception	Voltage-dependent L-type calcium channel subunit alpha-1F	Homo sapiens (human)
calcium ion import across plasma membrane	Voltage-dependent L-type calcium channel subunit alpha-1F	Homo sapiens (human)
fatty acid metabolic process	Bile salt export pump	Homo sapiens (human)
bile acid biosynthetic process	Bile salt export pump	Homo sapiens (human)
xenobiotic metabolic process	Bile salt export pump	Homo sapiens (human)
xenobiotic transmembrane transport	Bile salt export pump	Homo sapiens (human)
response to oxidative stress	Bile salt export pump	Homo sapiens (human)
bile acid metabolic process	Bile salt export pump	Homo sapiens (human)
response to organic cyclic compound	Bile salt export pump	Homo sapiens (human)
bile acid and bile salt transport	Bile salt export pump	Homo sapiens (human)
canalicular bile acid transport	Bile salt export pump	Homo sapiens (human)
protein ubiquitination	Bile salt export pump	Homo sapiens (human)
regulation of fatty acid beta-oxidation	Bile salt export pump	Homo sapiens (human)
carbohydrate transmembrane transport	Bile salt export pump	Homo sapiens (human)
bile acid signaling pathway	Bile salt export pump	Homo sapiens (human)
cholesterol homeostasis	Bile salt export pump	Homo sapiens (human)
response to estrogen	Bile salt export pump	Homo sapiens (human)
response to ethanol	Bile salt export pump	Homo sapiens (human)
xenobiotic export from cell	Bile salt export pump	Homo sapiens (human)
lipid homeostasis	Bile salt export pump	Homo sapiens (human)
phospholipid homeostasis	Bile salt export pump	Homo sapiens (human)
positive regulation of bile acid secretion	Bile salt export pump	Homo sapiens (human)
regulation of bile acid metabolic process	Bile salt export pump	Homo sapiens (human)
transmembrane transport	Bile salt export pump	Homo sapiens (human)
negative regulation of cell population proliferation	Cellular tumor antigen p53	Homo sapiens (human)
regulation of cell cycle	Cellular tumor antigen p53	Homo sapiens (human)
regulation of cell cycle G2/M phase transition	Cellular tumor antigen p53	Homo sapiens (human)
DNA damage response	Cellular tumor antigen p53	Homo sapiens (human)
ER overload response	Cellular tumor antigen p53	Homo sapiens (human)
cellular response to glucose starvation	Cellular tumor antigen p53	Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediator	Cellular tumor antigen p53	Homo sapiens (human)
regulation of apoptotic process	Cellular tumor antigen p53	Homo sapiens (human)
positive regulation of transcription by RNA polymerase II	Cellular tumor antigen p53	Homo sapiens (human)
positive regulation of miRNA transcription	Cellular tumor antigen p53	Homo sapiens (human)
negative regulation of transcription by RNA polymerase II	Cellular tumor antigen p53	Homo sapiens (human)
mitophagy	Cellular tumor antigen p53	Homo sapiens (human)
in utero embryonic development	Cellular tumor antigen p53	Homo sapiens (human)
somitogenesis	Cellular tumor antigen p53	Homo sapiens (human)
release of cytochrome c from mitochondria	Cellular tumor antigen p53	Homo sapiens (human)
hematopoietic progenitor cell differentiation	Cellular tumor antigen p53	Homo sapiens (human)
T cell proliferation involved in immune response	Cellular tumor antigen p53	Homo sapiens (human)
B cell lineage commitment	Cellular tumor antigen p53	Homo sapiens (human)
T cell lineage commitment	Cellular tumor antigen p53	Homo sapiens (human)
response to ischemia	Cellular tumor antigen p53	Homo sapiens (human)
nucleotide-excision repair	Cellular tumor antigen p53	Homo sapiens (human)
double-strand break repair	Cellular tumor antigen p53	Homo sapiens (human)
regulation of DNA-templated transcription	Cellular tumor antigen p53	Homo sapiens (human)
regulation of transcription by RNA polymerase II	Cellular tumor antigen p53	Homo sapiens (human)
protein import into nucleus	Cellular tumor antigen p53	Homo sapiens (human)
autophagy	Cellular tumor antigen p53	Homo sapiens (human)
DNA damage response	Cellular tumor antigen p53	Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in cell cycle arrest	Cellular tumor antigen p53	Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in transcription of p21 class mediator	Cellular tumor antigen p53	Homo sapiens (human)
transforming growth factor beta receptor signaling pathway	Cellular tumor antigen p53	Homo sapiens (human)
Ras protein signal transduction	Cellular tumor antigen p53	Homo sapiens (human)
gastrulation	Cellular tumor antigen p53	Homo sapiens (human)
neuroblast proliferation	Cellular tumor antigen p53	Homo sapiens (human)
negative regulation of neuroblast proliferation	Cellular tumor antigen p53	Homo sapiens (human)
protein localization	Cellular tumor antigen p53	Homo sapiens (human)
negative regulation of DNA replication	Cellular tumor antigen p53	Homo sapiens (human)
negative regulation of cell population proliferation	Cellular tumor antigen p53	Homo sapiens (human)
determination of adult lifespan	Cellular tumor antigen p53	Homo sapiens (human)
mRNA transcription	Cellular tumor antigen p53	Homo sapiens (human)
rRNA transcription	Cellular tumor antigen p53	Homo sapiens (human)
response to salt stress	Cellular tumor antigen p53	Homo sapiens (human)
response to inorganic substance	Cellular tumor antigen p53	Homo sapiens (human)
response to X-ray	Cellular tumor antigen p53	Homo sapiens (human)
response to gamma radiation	Cellular tumor antigen p53	Homo sapiens (human)
positive regulation of gene expression	Cellular tumor antigen p53	Homo sapiens (human)
cardiac muscle cell apoptotic process	Cellular tumor antigen p53	Homo sapiens (human)
positive regulation of cardiac muscle cell apoptotic process	Cellular tumor antigen p53	Homo sapiens (human)
glial cell proliferation	Cellular tumor antigen p53	Homo sapiens (human)
viral process	Cellular tumor antigen p53	Homo sapiens (human)
glucose catabolic process to lactate via pyruvate	Cellular tumor antigen p53	Homo sapiens (human)
cerebellum development	Cellular tumor antigen p53	Homo sapiens (human)
negative regulation of cell growth	Cellular tumor antigen p53	Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator	Cellular tumor antigen p53	Homo sapiens (human)
negative regulation of transforming growth factor beta receptor signaling pathway	Cellular tumor antigen p53	Homo sapiens (human)
mitotic G1 DNA damage checkpoint signaling	Cellular tumor antigen p53	Homo sapiens (human)
negative regulation of telomere maintenance via telomerase	Cellular tumor antigen p53	Homo sapiens (human)
T cell differentiation in thymus	Cellular tumor antigen p53	Homo sapiens (human)
tumor necrosis factor-mediated signaling pathway	Cellular tumor antigen p53	Homo sapiens (human)
regulation of tissue remodeling	Cellular tumor antigen p53	Homo sapiens (human)
cellular response to UV	Cellular tumor antigen p53	Homo sapiens (human)
multicellular organism growth	Cellular tumor antigen p53	Homo sapiens (human)
positive regulation of mitochondrial membrane permeability	Cellular tumor antigen p53	Homo sapiens (human)
cellular response to glucose starvation	Cellular tumor antigen p53	Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediator	Cellular tumor antigen p53	Homo sapiens (human)
positive regulation of apoptotic process	Cellular tumor antigen p53	Homo sapiens (human)
negative regulation of apoptotic process	Cellular tumor antigen p53	Homo sapiens (human)
entrainment of circadian clock by photoperiod	Cellular tumor antigen p53	Homo sapiens (human)
mitochondrial DNA repair	Cellular tumor antigen p53	Homo sapiens (human)
regulation of DNA damage response, signal transduction by p53 class mediator	Cellular tumor antigen p53	Homo sapiens (human)
positive regulation of neuron apoptotic process	Cellular tumor antigen p53	Homo sapiens (human)
transcription initiation-coupled chromatin remodeling	Cellular tumor antigen p53	Homo sapiens (human)
negative regulation of proteolysis	Cellular tumor antigen p53	Homo sapiens (human)
negative regulation of DNA-templated transcription	Cellular tumor antigen p53	Homo sapiens (human)
positive regulation of DNA-templated transcription	Cellular tumor antigen p53	Homo sapiens (human)
positive regulation of RNA polymerase II transcription preinitiation complex assembly	Cellular tumor antigen p53	Homo sapiens (human)
positive regulation of transcription by RNA polymerase II	Cellular tumor antigen p53	Homo sapiens (human)
response to antibiotic	Cellular tumor antigen p53	Homo sapiens (human)
fibroblast proliferation	Cellular tumor antigen p53	Homo sapiens (human)
negative regulation of fibroblast proliferation	Cellular tumor antigen p53	Homo sapiens (human)
circadian behavior	Cellular tumor antigen p53	Homo sapiens (human)
bone marrow development	Cellular tumor antigen p53	Homo sapiens (human)
embryonic organ development	Cellular tumor antigen p53	Homo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylation	Cellular tumor antigen p53	Homo sapiens (human)
protein stabilization	Cellular tumor antigen p53	Homo sapiens (human)
negative regulation of helicase activity	Cellular tumor antigen p53	Homo sapiens (human)
protein tetramerization	Cellular tumor antigen p53	Homo sapiens (human)
chromosome organization	Cellular tumor antigen p53	Homo sapiens (human)
neuron apoptotic process	Cellular tumor antigen p53	Homo sapiens (human)
regulation of cell cycle	Cellular tumor antigen p53	Homo sapiens (human)
hematopoietic stem cell differentiation	Cellular tumor antigen p53	Homo sapiens (human)
negative regulation of glial cell proliferation	Cellular tumor antigen p53	Homo sapiens (human)
type II interferon-mediated signaling pathway	Cellular tumor antigen p53	Homo sapiens (human)
cardiac septum morphogenesis	Cellular tumor antigen p53	Homo sapiens (human)
positive regulation of programmed necrotic cell death	Cellular tumor antigen p53	Homo sapiens (human)
protein-containing complex assembly	Cellular tumor antigen p53	Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to endoplasmic reticulum stress	Cellular tumor antigen p53	Homo sapiens (human)
thymocyte apoptotic process	Cellular tumor antigen p53	Homo sapiens (human)
positive regulation of thymocyte apoptotic process	Cellular tumor antigen p53	Homo sapiens (human)
necroptotic process	Cellular tumor antigen p53	Homo sapiens (human)
cellular response to hypoxia	Cellular tumor antigen p53	Homo sapiens (human)
cellular response to xenobiotic stimulus	Cellular tumor antigen p53	Homo sapiens (human)
cellular response to ionizing radiation	Cellular tumor antigen p53	Homo sapiens (human)
cellular response to gamma radiation	Cellular tumor antigen p53	Homo sapiens (human)
cellular response to UV-C	Cellular tumor antigen p53	Homo sapiens (human)
stem cell proliferation	Cellular tumor antigen p53	Homo sapiens (human)
signal transduction by p53 class mediator	Cellular tumor antigen p53	Homo sapiens (human)
intrinsic apoptotic signaling pathway by p53 class mediator	Cellular tumor antigen p53	Homo sapiens (human)
reactive oxygen species metabolic process	Cellular tumor antigen p53	Homo sapiens (human)
cellular response to actinomycin D	Cellular tumor antigen p53	Homo sapiens (human)
positive regulation of release of cytochrome c from mitochondria	Cellular tumor antigen p53	Homo sapiens (human)
cellular senescence	Cellular tumor antigen p53	Homo sapiens (human)
replicative senescence	Cellular tumor antigen p53	Homo sapiens (human)
oxidative stress-induced premature senescence	Cellular tumor antigen p53	Homo sapiens (human)
intrinsic apoptotic signaling pathway	Cellular tumor antigen p53	Homo sapiens (human)
oligodendrocyte apoptotic process	Cellular tumor antigen p53	Homo sapiens (human)
positive regulation of execution phase of apoptosis	Cellular tumor antigen p53	Homo sapiens (human)
negative regulation of mitophagy	Cellular tumor antigen p53	Homo sapiens (human)
regulation of mitochondrial membrane permeability involved in apoptotic process	Cellular tumor antigen p53	Homo sapiens (human)
regulation of intrinsic apoptotic signaling pathway by p53 class mediator	Cellular tumor antigen p53	Homo sapiens (human)
positive regulation of miRNA transcription	Cellular tumor antigen p53	Homo sapiens (human)
negative regulation of G1 to G0 transition	Cellular tumor antigen p53	Homo sapiens (human)
negative regulation of miRNA processing	Cellular tumor antigen p53	Homo sapiens (human)
negative regulation of glucose catabolic process to lactate via pyruvate	Cellular tumor antigen p53	Homo sapiens (human)
negative regulation of pentose-phosphate shunt	Cellular tumor antigen p53	Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to hypoxia	Cellular tumor antigen p53	Homo sapiens (human)
regulation of fibroblast apoptotic process	Cellular tumor antigen p53	Homo sapiens (human)
negative regulation of reactive oxygen species metabolic process	Cellular tumor antigen p53	Homo sapiens (human)
positive regulation of reactive oxygen species metabolic process	Cellular tumor antigen p53	Homo sapiens (human)
negative regulation of stem cell proliferation	Cellular tumor antigen p53	Homo sapiens (human)
positive regulation of cellular senescence	Cellular tumor antigen p53	Homo sapiens (human)
positive regulation of intrinsic apoptotic signaling pathway	Cellular tumor antigen p53	Homo sapiens (human)
G2/M transition of mitotic cell cycle	ATP-dependent translocase ABCB1	Homo sapiens (human)
xenobiotic metabolic process	ATP-dependent translocase ABCB1	Homo sapiens (human)
response to xenobiotic stimulus	ATP-dependent translocase ABCB1	Homo sapiens (human)
phospholipid translocation	ATP-dependent translocase ABCB1	Homo sapiens (human)
terpenoid transport	ATP-dependent translocase ABCB1	Homo sapiens (human)
regulation of response to osmotic stress	ATP-dependent translocase ABCB1	Homo sapiens (human)
transmembrane transport	ATP-dependent translocase ABCB1	Homo sapiens (human)
transepithelial transport	ATP-dependent translocase ABCB1	Homo sapiens (human)
stem cell proliferation	ATP-dependent translocase ABCB1	Homo sapiens (human)
ceramide translocation	ATP-dependent translocase ABCB1	Homo sapiens (human)
export across plasma membrane	ATP-dependent translocase ABCB1	Homo sapiens (human)
transport across blood-brain barrier	ATP-dependent translocase ABCB1	Homo sapiens (human)
positive regulation of anion channel activity	ATP-dependent translocase ABCB1	Homo sapiens (human)
carboxylic acid transmembrane transport	ATP-dependent translocase ABCB1	Homo sapiens (human)
xenobiotic detoxification by transmembrane export across the plasma membrane	ATP-dependent translocase ABCB1	Homo sapiens (human)
xenobiotic transport across blood-brain barrier	ATP-dependent translocase ABCB1	Homo sapiens (human)
regulation of chloride transport	ATP-dependent translocase ABCB1	Homo sapiens (human)
lipid hydroxylation	Cytochrome P450 3A4	Homo sapiens (human)
lipid metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
steroid catabolic process	Cytochrome P450 3A4	Homo sapiens (human)
xenobiotic metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
steroid metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
cholesterol metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
androgen metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
estrogen metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
alkaloid catabolic process	Cytochrome P450 3A4	Homo sapiens (human)
monoterpenoid metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
calcitriol biosynthetic process from calciol	Cytochrome P450 3A4	Homo sapiens (human)
xenobiotic catabolic process	Cytochrome P450 3A4	Homo sapiens (human)
vitamin D metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
vitamin D catabolic process	Cytochrome P450 3A4	Homo sapiens (human)
retinol metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
retinoic acid metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
long-chain fatty acid biosynthetic process	Cytochrome P450 3A4	Homo sapiens (human)
aflatoxin metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
oxidative demethylation	Cytochrome P450 3A4	Homo sapiens (human)
xenobiotic metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
steroid metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
cholesterol metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
estrogen metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
monoterpenoid metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
epoxygenase P450 pathway	Cytochrome P450 2C9	Homo sapiens (human)
urea metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
monocarboxylic acid metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
xenobiotic catabolic process	Cytochrome P450 2C9	Homo sapiens (human)
long-chain fatty acid biosynthetic process	Cytochrome P450 2C9	Homo sapiens (human)
amide metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
icosanoid biosynthetic process	Cytochrome P450 2C9	Homo sapiens (human)
oxidative demethylation	Cytochrome P450 2C9	Homo sapiens (human)
omega-hydroxylase P450 pathway	Cytochrome P450 2C9	Homo sapiens (human)
sodium ion transport	Sodium channel protein type 1 subunit alpha	Homo sapiens (human)
adult walking behavior	Sodium channel protein type 1 subunit alpha	Homo sapiens (human)
determination of adult lifespan	Sodium channel protein type 1 subunit alpha	Homo sapiens (human)
neuronal action potential propagation	Sodium channel protein type 1 subunit alpha	Homo sapiens (human)
neuronal action potential	Sodium channel protein type 1 subunit alpha	Homo sapiens (human)
nerve development	Sodium channel protein type 1 subunit alpha	Homo sapiens (human)
neuromuscular process controlling posture	Sodium channel protein type 1 subunit alpha	Homo sapiens (human)
detection of mechanical stimulus involved in sensory perception of pain	Sodium channel protein type 1 subunit alpha	Homo sapiens (human)
establishment of localization in cell	Sodium channel protein type 1 subunit alpha	Homo sapiens (human)
cardiac muscle cell action potential involved in contraction	Sodium channel protein type 1 subunit alpha	Homo sapiens (human)
membrane depolarization during action potential	Sodium channel protein type 1 subunit alpha	Homo sapiens (human)
regulation of presynaptic membrane potential	Sodium channel protein type 1 subunit alpha	Homo sapiens (human)
sodium ion transmembrane transport	Sodium channel protein type 1 subunit alpha	Homo sapiens (human)
sodium ion transport	Sodium channel protein type 4 subunit alpha	Homo sapiens (human)
muscle contraction	Sodium channel protein type 4 subunit alpha	Homo sapiens (human)
sodium ion transmembrane transport	Sodium channel protein type 4 subunit alpha	Homo sapiens (human)
regulation of skeletal muscle contraction by action potential	Sodium channel protein type 4 subunit alpha	Homo sapiens (human)
cardiac muscle cell action potential involved in contraction	Sodium channel protein type 4 subunit alpha	Homo sapiens (human)
fatty acid metabolic process	Cytochrome P450 2J2	Homo sapiens (human)
icosanoid metabolic process	Cytochrome P450 2J2	Homo sapiens (human)
xenobiotic metabolic process	Cytochrome P450 2J2	Homo sapiens (human)
regulation of heart contraction	Cytochrome P450 2J2	Homo sapiens (human)
epoxygenase P450 pathway	Cytochrome P450 2J2	Homo sapiens (human)
linoleic acid metabolic process	Cytochrome P450 2J2	Homo sapiens (human)
organic acid metabolic process	Cytochrome P450 2J2	Homo sapiens (human)
osmosensory signaling pathway	Sodium channel protein type 7 subunit alpha	Homo sapiens (human)
response to bacterium	Sodium channel protein type 7 subunit alpha	Homo sapiens (human)
cellular homeostasis	Sodium channel protein type 7 subunit alpha	Homo sapiens (human)
sodium ion homeostasis	Sodium channel protein type 7 subunit alpha	Homo sapiens (human)
cardiac muscle cell action potential involved in contraction	Sodium channel protein type 7 subunit alpha	Homo sapiens (human)
sodium ion transmembrane transport	Sodium channel protein type 7 subunit alpha	Homo sapiens (human)
calcium ion transport	Voltage-dependent L-type calcium channel subunit alpha-1D	Homo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathway	Voltage-dependent L-type calcium channel subunit alpha-1D	Homo sapiens (human)
sensory perception of sound	Voltage-dependent L-type calcium channel subunit alpha-1D	Homo sapiens (human)
positive regulation of adenylate cyclase activity	Voltage-dependent L-type calcium channel subunit alpha-1D	Homo sapiens (human)
positive regulation of calcium ion transport	Voltage-dependent L-type calcium channel subunit alpha-1D	Homo sapiens (human)
regulation of atrial cardiac muscle cell membrane repolarization	Voltage-dependent L-type calcium channel subunit alpha-1D	Homo sapiens (human)
calcium ion import	Voltage-dependent L-type calcium channel subunit alpha-1D	Homo sapiens (human)
calcium ion transmembrane transport	Voltage-dependent L-type calcium channel subunit alpha-1D	Homo sapiens (human)
cardiac muscle cell action potential involved in contraction	Voltage-dependent L-type calcium channel subunit alpha-1D	Homo sapiens (human)
membrane depolarization during cardiac muscle cell action potential	Voltage-dependent L-type calcium channel subunit alpha-1D	Homo sapiens (human)
membrane depolarization during SA node cell action potential	Voltage-dependent L-type calcium channel subunit alpha-1D	Homo sapiens (human)
regulation of heart rate by cardiac conduction	Voltage-dependent L-type calcium channel subunit alpha-1D	Homo sapiens (human)
regulation of potassium ion transmembrane transporter activity	Voltage-dependent L-type calcium channel subunit alpha-1D	Homo sapiens (human)
regulation of potassium ion transmembrane transport	Voltage-dependent L-type calcium channel subunit alpha-1D	Homo sapiens (human)
calcium ion import across plasma membrane	Voltage-dependent L-type calcium channel subunit alpha-1D	Homo sapiens (human)
startle response	Potassium voltage-gated channel subfamily A member 1	Homo sapiens (human)
regulation of muscle contraction	Potassium voltage-gated channel subfamily A member 1	Homo sapiens (human)
neuroblast proliferation	Potassium voltage-gated channel subfamily A member 1	Homo sapiens (human)
protein localization	Potassium voltage-gated channel subfamily A member 1	Homo sapiens (human)
cell communication by electrical coupling	Potassium voltage-gated channel subfamily A member 1	Homo sapiens (human)
magnesium ion homeostasis	Potassium voltage-gated channel subfamily A member 1	Homo sapiens (human)
neuronal action potential	Potassium voltage-gated channel subfamily A member 1	Homo sapiens (human)
optic nerve development	Potassium voltage-gated channel subfamily A member 1	Homo sapiens (human)
hippocampus development	Potassium voltage-gated channel subfamily A member 1	Homo sapiens (human)
cerebral cortex development	Potassium voltage-gated channel subfamily A member 1	Homo sapiens (human)
corpus callosum development	Potassium voltage-gated channel subfamily A member 1	Homo sapiens (human)
neuronal signal transduction	Potassium voltage-gated channel subfamily A member 1	Homo sapiens (human)
regulation of membrane potential	Potassium voltage-gated channel subfamily A member 1	Homo sapiens (human)
neuromuscular process	Potassium voltage-gated channel subfamily A member 1	Homo sapiens (human)
detection of mechanical stimulus involved in sensory perception of pain	Potassium voltage-gated channel subfamily A member 1	Homo sapiens (human)
detection of mechanical stimulus involved in sensory perception of touch	Potassium voltage-gated channel subfamily A member 1	Homo sapiens (human)
protein homooligomerization	Potassium voltage-gated channel subfamily A member 1	Homo sapiens (human)
regulation of postsynaptic membrane potential	Potassium voltage-gated channel subfamily A member 1	Homo sapiens (human)
axon development	Potassium voltage-gated channel subfamily A member 1	Homo sapiens (human)
cellular response to magnesium ion	Potassium voltage-gated channel subfamily A member 1	Homo sapiens (human)
potassium ion transmembrane transport	Potassium voltage-gated channel subfamily A member 1	Homo sapiens (human)
membrane repolarization during action potential	Potassium voltage-gated channel subfamily A member 1	Homo sapiens (human)
regulation of presynaptic membrane potential	Potassium voltage-gated channel subfamily A member 1	Homo sapiens (human)
action potential	Potassium voltage-gated channel subfamily A member 1	Homo sapiens (human)
regulation of heart rate by cardiac conduction	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
regulation of heart rate by hormone	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
regulation of membrane potential	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
positive regulation of DNA-templated transcription	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
potassium ion homeostasis	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
cardiac muscle contraction	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
regulation of membrane repolarization	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
regulation of ventricular cardiac muscle cell membrane repolarization	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
cellular response to xenobiotic stimulus	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
potassium ion transmembrane transport	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
ventricular cardiac muscle cell action potential	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
membrane repolarization	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
membrane depolarization during action potential	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
membrane repolarization during action potential	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
membrane repolarization during cardiac muscle cell action potential	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
regulation of heart rate by cardiac conduction	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
potassium ion export across plasma membrane	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
membrane repolarization during ventricular cardiac muscle cell action potential	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
regulation of potassium ion transmembrane transport	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
negative regulation of potassium ion transmembrane transport	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
positive regulation of potassium ion transmembrane transport	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
negative regulation of potassium ion export across plasma membrane	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
potassium ion import across plasma membrane	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
skeletal system development	Voltage-dependent L-type calcium channel subunit alpha-1S	Homo sapiens (human)
extraocular skeletal muscle development	Voltage-dependent L-type calcium channel subunit alpha-1S	Homo sapiens (human)
calcium ion transport	Voltage-dependent L-type calcium channel subunit alpha-1S	Homo sapiens (human)
muscle contraction	Voltage-dependent L-type calcium channel subunit alpha-1S	Homo sapiens (human)
striated muscle contraction	Voltage-dependent L-type calcium channel subunit alpha-1S	Homo sapiens (human)
endoplasmic reticulum organization	Voltage-dependent L-type calcium channel subunit alpha-1S	Homo sapiens (human)
myoblast fusion	Voltage-dependent L-type calcium channel subunit alpha-1S	Homo sapiens (human)
neuromuscular junction development	Voltage-dependent L-type calcium channel subunit alpha-1S	Homo sapiens (human)
skeletal muscle adaptation	Voltage-dependent L-type calcium channel subunit alpha-1S	Homo sapiens (human)
positive regulation of muscle contraction	Voltage-dependent L-type calcium channel subunit alpha-1S	Homo sapiens (human)
skeletal muscle fiber development	Voltage-dependent L-type calcium channel subunit alpha-1S	Homo sapiens (human)
release of sequestered calcium ion into cytosol	Voltage-dependent L-type calcium channel subunit alpha-1S	Homo sapiens (human)
calcium ion transmembrane transport	Voltage-dependent L-type calcium channel subunit alpha-1S	Homo sapiens (human)
cellular response to caffeine	Voltage-dependent L-type calcium channel subunit alpha-1S	Homo sapiens (human)
calcium ion import across plasma membrane	Voltage-dependent L-type calcium channel subunit alpha-1S	Homo sapiens (human)
immune system development	Voltage-dependent L-type calcium channel subunit alpha-1C	Homo sapiens (human)
positive regulation of cytosolic calcium ion concentration	Voltage-dependent L-type calcium channel subunit alpha-1C	Homo sapiens (human)
heart development	Voltage-dependent L-type calcium channel subunit alpha-1C	Homo sapiens (human)
regulation of cardiac muscle contraction by regulation of the release of sequestered calcium ion	Voltage-dependent L-type calcium channel subunit alpha-1C	Homo sapiens (human)
embryonic forelimb morphogenesis	Voltage-dependent L-type calcium channel subunit alpha-1C	Homo sapiens (human)
camera-type eye development	Voltage-dependent L-type calcium channel subunit alpha-1C	Homo sapiens (human)
positive regulation of adenylate cyclase activity	Voltage-dependent L-type calcium channel subunit alpha-1C	Homo sapiens (human)
positive regulation of muscle contraction	Voltage-dependent L-type calcium channel subunit alpha-1C	Homo sapiens (human)
calcium ion transport into cytosol	Voltage-dependent L-type calcium channel subunit alpha-1C	Homo sapiens (human)
cardiac conduction	Voltage-dependent L-type calcium channel subunit alpha-1C	Homo sapiens (human)
calcium ion transmembrane transport via high voltage-gated calcium channel	Voltage-dependent L-type calcium channel subunit alpha-1C	Homo sapiens (human)
calcium ion transmembrane transport	Voltage-dependent L-type calcium channel subunit alpha-1C	Homo sapiens (human)
cardiac muscle cell action potential involved in contraction	Voltage-dependent L-type calcium channel subunit alpha-1C	Homo sapiens (human)
membrane depolarization during cardiac muscle cell action potential	Voltage-dependent L-type calcium channel subunit alpha-1C	Homo sapiens (human)
membrane depolarization during AV node cell action potential	Voltage-dependent L-type calcium channel subunit alpha-1C	Homo sapiens (human)
cell communication by electrical coupling involved in cardiac conduction	Voltage-dependent L-type calcium channel subunit alpha-1C	Homo sapiens (human)
regulation of heart rate by cardiac conduction	Voltage-dependent L-type calcium channel subunit alpha-1C	Homo sapiens (human)
regulation of ventricular cardiac muscle cell action potential	Voltage-dependent L-type calcium channel subunit alpha-1C	Homo sapiens (human)
membrane depolarization during atrial cardiac muscle cell action potential	Voltage-dependent L-type calcium channel subunit alpha-1C	Homo sapiens (human)
calcium ion import across plasma membrane	Voltage-dependent L-type calcium channel subunit alpha-1C	Homo sapiens (human)
regulation of heart rate	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
cardiac conduction system development	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
cardiac ventricle development	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
brainstem development	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
sodium ion transport	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
positive regulation of sodium ion transport	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
response to denervation involved in regulation of muscle adaptation	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
telencephalon development	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
cerebellum development	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
sodium ion transmembrane transport	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
odontogenesis of dentin-containing tooth	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
positive regulation of action potential	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
positive regulation of epithelial cell proliferation	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
membrane depolarization	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
cardiac muscle contraction	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
regulation of ventricular cardiac muscle cell membrane repolarization	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
regulation of atrial cardiac muscle cell membrane depolarization	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
regulation of atrial cardiac muscle cell membrane repolarization	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
regulation of ventricular cardiac muscle cell membrane depolarization	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
cellular response to calcium ion	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
cardiac muscle cell action potential involved in contraction	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
regulation of cardiac muscle cell contraction	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
ventricular cardiac muscle cell action potential	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
membrane depolarization during action potential	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
membrane depolarization during cardiac muscle cell action potential	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
atrial cardiac muscle cell action potential	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
SA node cell action potential	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
AV node cell action potential	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
bundle of His cell action potential	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
membrane depolarization during AV node cell action potential	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
membrane depolarization during SA node cell action potential	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
membrane depolarization during Purkinje myocyte cell action potential	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
membrane depolarization during bundle of His cell action potential	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
AV node cell to bundle of His cell communication	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
regulation of heart rate by cardiac conduction	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
membrane depolarization during atrial cardiac muscle cell action potential	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
regulation of sodium ion transmembrane transport	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
sodium ion transport	Sodium channel protein type 9 subunit alpha	Homo sapiens (human)
inflammatory response	Sodium channel protein type 9 subunit alpha	Homo sapiens (human)
circadian rhythm	Sodium channel protein type 9 subunit alpha	Homo sapiens (human)
response to toxic substance	Sodium channel protein type 9 subunit alpha	Homo sapiens (human)
post-embryonic development	Sodium channel protein type 9 subunit alpha	Homo sapiens (human)
sensory perception of pain	Sodium channel protein type 9 subunit alpha	Homo sapiens (human)
sodium ion transmembrane transport	Sodium channel protein type 9 subunit alpha	Homo sapiens (human)
behavioral response to pain	Sodium channel protein type 9 subunit alpha	Homo sapiens (human)
detection of temperature stimulus involved in sensory perception of pain	Sodium channel protein type 9 subunit alpha	Homo sapiens (human)
detection of mechanical stimulus involved in sensory perception	Sodium channel protein type 9 subunit alpha	Homo sapiens (human)
cardiac muscle cell action potential involved in contraction	Sodium channel protein type 9 subunit alpha	Homo sapiens (human)
xenobiotic metabolic process	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
xenobiotic transmembrane transport	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
negative regulation of gene expression	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
bile acid and bile salt transport	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
bilirubin transport	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
heme catabolic process	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
xenobiotic export from cell	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
transmembrane transport	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
transepithelial transport	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
leukotriene transport	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
monoatomic anion transmembrane transport	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
transport across blood-brain barrier	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
xenobiotic transport across blood-brain barrier	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
sodium ion transport	Sodium channel protein type 2 subunit alpha	Homo sapiens (human)
nervous system development	Sodium channel protein type 2 subunit alpha	Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to osmotic stress	Sodium channel protein type 2 subunit alpha	Homo sapiens (human)
neuron apoptotic process	Sodium channel protein type 2 subunit alpha	Homo sapiens (human)
memory	Sodium channel protein type 2 subunit alpha	Homo sapiens (human)
determination of adult lifespan	Sodium channel protein type 2 subunit alpha	Homo sapiens (human)
neuronal action potential	Sodium channel protein type 2 subunit alpha	Homo sapiens (human)
dentate gyrus development	Sodium channel protein type 2 subunit alpha	Homo sapiens (human)
nerve development	Sodium channel protein type 2 subunit alpha	Homo sapiens (human)
myelination	Sodium channel protein type 2 subunit alpha	Homo sapiens (human)
cellular response to hypoxia	Sodium channel protein type 2 subunit alpha	Homo sapiens (human)
cardiac muscle cell action potential involved in contraction	Sodium channel protein type 2 subunit alpha	Homo sapiens (human)
sodium ion transmembrane transport	Sodium channel protein type 2 subunit alpha	Homo sapiens (human)
sodium ion transport	Sodium channel protein type 3 subunit alpha	Homo sapiens (human)
behavioral response to pain	Sodium channel protein type 3 subunit alpha	Homo sapiens (human)
cardiac muscle cell action potential involved in contraction	Sodium channel protein type 3 subunit alpha	Homo sapiens (human)
sodium ion transmembrane transport	Sodium channel protein type 3 subunit alpha	Homo sapiens (human)
thigmotaxis	Sodium channel protein type 11 subunit alpha	Homo sapiens (human)
acute inflammatory response	Sodium channel protein type 11 subunit alpha	Homo sapiens (human)
chronic inflammatory response	Sodium channel protein type 11 subunit alpha	Homo sapiens (human)
axonogenesis	Sodium channel protein type 11 subunit alpha	Homo sapiens (human)
circadian rhythm	Sodium channel protein type 11 subunit alpha	Homo sapiens (human)
response to heat	Sodium channel protein type 11 subunit alpha	Homo sapiens (human)
response to xenobiotic stimulus	Sodium channel protein type 11 subunit alpha	Homo sapiens (human)
response to toxic substance	Sodium channel protein type 11 subunit alpha	Homo sapiens (human)
response to high light intensity	Sodium channel protein type 11 subunit alpha	Homo sapiens (human)
protein kinase A signaling	Sodium channel protein type 11 subunit alpha	Homo sapiens (human)
response to auditory stimulus	Sodium channel protein type 11 subunit alpha	Homo sapiens (human)
neuronal action potential	Sodium channel protein type 11 subunit alpha	Homo sapiens (human)
sensory perception of pain	Sodium channel protein type 11 subunit alpha	Homo sapiens (human)

Process	via Protein(s)	Taxonomy
acetylcholine transmembrane transporter activity	Solute carrier family 22 member 1	Homo sapiens (human)
neurotransmitter transmembrane transporter activity	Solute carrier family 22 member 1	Homo sapiens (human)
dopamine:sodium symporter activity	Solute carrier family 22 member 1	Homo sapiens (human)
norepinephrine:sodium symporter activity	Solute carrier family 22 member 1	Homo sapiens (human)
protein binding	Solute carrier family 22 member 1	Homo sapiens (human)
monoamine transmembrane transporter activity	Solute carrier family 22 member 1	Homo sapiens (human)
secondary active organic cation transmembrane transporter activity	Solute carrier family 22 member 1	Homo sapiens (human)
organic anion transmembrane transporter activity	Solute carrier family 22 member 1	Homo sapiens (human)
organic cation transmembrane transporter activity	Solute carrier family 22 member 1	Homo sapiens (human)
prostaglandin transmembrane transporter activity	Solute carrier family 22 member 1	Homo sapiens (human)
pyrimidine nucleoside transmembrane transporter activity	Solute carrier family 22 member 1	Homo sapiens (human)
thiamine transmembrane transporter activity	Solute carrier family 22 member 1	Homo sapiens (human)
putrescine transmembrane transporter activity	Solute carrier family 22 member 1	Homo sapiens (human)
spermidine transmembrane transporter activity	Solute carrier family 22 member 1	Homo sapiens (human)
quaternary ammonium group transmembrane transporter activity	Solute carrier family 22 member 1	Homo sapiens (human)
toxin transmembrane transporter activity	Solute carrier family 22 member 1	Homo sapiens (human)
identical protein binding	Solute carrier family 22 member 1	Homo sapiens (human)
xenobiotic transmembrane transporter activity	Solute carrier family 22 member 1	Homo sapiens (human)
(R)-carnitine transmembrane transporter activity	Solute carrier family 22 member 1	Homo sapiens (human)
iron ion binding	Polyunsaturated fatty acid lipoxygenase ALOX15B	Homo sapiens (human)
calcium ion binding	Polyunsaturated fatty acid lipoxygenase ALOX15B	Homo sapiens (human)
protein binding	Polyunsaturated fatty acid lipoxygenase ALOX15B	Homo sapiens (human)
lipid binding	Polyunsaturated fatty acid lipoxygenase ALOX15B	Homo sapiens (human)
linoleate 13S-lipoxygenase activity	Polyunsaturated fatty acid lipoxygenase ALOX15B	Homo sapiens (human)
arachidonate 8(S)-lipoxygenase activity	Polyunsaturated fatty acid lipoxygenase ALOX15B	Homo sapiens (human)
arachidonate 15-lipoxygenase activity	Polyunsaturated fatty acid lipoxygenase ALOX15B	Homo sapiens (human)
linoleate 9S-lipoxygenase activity	Polyunsaturated fatty acid lipoxygenase ALOX15B	Homo sapiens (human)
ATP binding	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
ABC-type xenobiotic transporter activity	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
glucuronoside transmembrane transporter activity	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activity	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
ABC-type bile acid transporter activity	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
ATP hydrolysis activity	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
ATPase-coupled transmembrane transporter activity	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
xenobiotic transmembrane transporter activity	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activity	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
icosanoid transmembrane transporter activity	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
ABC-type transporter activity	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
guanine nucleotide transmembrane transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
protein binding	Multidrug resistance-associated protein 4	Homo sapiens (human)
ATP binding	Multidrug resistance-associated protein 4	Homo sapiens (human)
ABC-type xenobiotic transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
prostaglandin transmembrane transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
urate transmembrane transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
purine nucleotide transmembrane transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
ABC-type bile acid transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
efflux transmembrane transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
15-hydroxyprostaglandin dehydrogenase (NAD+) activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
ATP hydrolysis activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
glutathione transmembrane transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
ATPase-coupled transmembrane transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
xenobiotic transmembrane transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
ABC-type transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
voltage-gated calcium channel activity	Voltage-dependent L-type calcium channel subunit alpha-1F	Homo sapiens (human)
metal ion binding	Voltage-dependent L-type calcium channel subunit alpha-1F	Homo sapiens (human)
high voltage-gated calcium channel activity	Voltage-dependent L-type calcium channel subunit alpha-1F	Homo sapiens (human)
protein binding	Bile salt export pump	Homo sapiens (human)
ATP binding	Bile salt export pump	Homo sapiens (human)
ABC-type xenobiotic transporter activity	Bile salt export pump	Homo sapiens (human)
bile acid transmembrane transporter activity	Bile salt export pump	Homo sapiens (human)
canalicular bile acid transmembrane transporter activity	Bile salt export pump	Homo sapiens (human)
carbohydrate transmembrane transporter activity	Bile salt export pump	Homo sapiens (human)
ABC-type bile acid transporter activity	Bile salt export pump	Homo sapiens (human)
ATP hydrolysis activity	Bile salt export pump	Homo sapiens (human)
transcription cis-regulatory region binding	Cellular tumor antigen p53	Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA binding	Cellular tumor antigen p53	Homo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specific	Cellular tumor antigen p53	Homo sapiens (human)
cis-regulatory region sequence-specific DNA binding	Cellular tumor antigen p53	Homo sapiens (human)
core promoter sequence-specific DNA binding	Cellular tumor antigen p53	Homo sapiens (human)
TFIID-class transcription factor complex binding	Cellular tumor antigen p53	Homo sapiens (human)
DNA-binding transcription repressor activity, RNA polymerase II-specific	Cellular tumor antigen p53	Homo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specific	Cellular tumor antigen p53	Homo sapiens (human)
protease binding	Cellular tumor antigen p53	Homo sapiens (human)
p53 binding	Cellular tumor antigen p53	Homo sapiens (human)
DNA binding	Cellular tumor antigen p53	Homo sapiens (human)
chromatin binding	Cellular tumor antigen p53	Homo sapiens (human)
DNA-binding transcription factor activity	Cellular tumor antigen p53	Homo sapiens (human)
mRNA 3'-UTR binding	Cellular tumor antigen p53	Homo sapiens (human)
copper ion binding	Cellular tumor antigen p53	Homo sapiens (human)
protein binding	Cellular tumor antigen p53	Homo sapiens (human)
zinc ion binding	Cellular tumor antigen p53	Homo sapiens (human)
enzyme binding	Cellular tumor antigen p53	Homo sapiens (human)
receptor tyrosine kinase binding	Cellular tumor antigen p53	Homo sapiens (human)
ubiquitin protein ligase binding	Cellular tumor antigen p53	Homo sapiens (human)
histone deacetylase regulator activity	Cellular tumor antigen p53	Homo sapiens (human)
ATP-dependent DNA/DNA annealing activity	Cellular tumor antigen p53	Homo sapiens (human)
identical protein binding	Cellular tumor antigen p53	Homo sapiens (human)
histone deacetylase binding	Cellular tumor antigen p53	Homo sapiens (human)
protein heterodimerization activity	Cellular tumor antigen p53	Homo sapiens (human)
protein-folding chaperone binding	Cellular tumor antigen p53	Homo sapiens (human)
protein phosphatase 2A binding	Cellular tumor antigen p53	Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor binding	Cellular tumor antigen p53	Homo sapiens (human)
14-3-3 protein binding	Cellular tumor antigen p53	Homo sapiens (human)
MDM2/MDM4 family protein binding	Cellular tumor antigen p53	Homo sapiens (human)
disordered domain specific binding	Cellular tumor antigen p53	Homo sapiens (human)
general transcription initiation factor binding	Cellular tumor antigen p53	Homo sapiens (human)
molecular function activator activity	Cellular tumor antigen p53	Homo sapiens (human)
promoter-specific chromatin binding	Cellular tumor antigen p53	Homo sapiens (human)
protein binding	ATP-dependent translocase ABCB1	Homo sapiens (human)
ATP binding	ATP-dependent translocase ABCB1	Homo sapiens (human)
ABC-type xenobiotic transporter activity	ATP-dependent translocase ABCB1	Homo sapiens (human)
efflux transmembrane transporter activity	ATP-dependent translocase ABCB1	Homo sapiens (human)
ATP hydrolysis activity	ATP-dependent translocase ABCB1	Homo sapiens (human)
transmembrane transporter activity	ATP-dependent translocase ABCB1	Homo sapiens (human)
ubiquitin protein ligase binding	ATP-dependent translocase ABCB1	Homo sapiens (human)
ATPase-coupled transmembrane transporter activity	ATP-dependent translocase ABCB1	Homo sapiens (human)
xenobiotic transmembrane transporter activity	ATP-dependent translocase ABCB1	Homo sapiens (human)
carboxylic acid transmembrane transporter activity	ATP-dependent translocase ABCB1	Homo sapiens (human)
phosphatidylcholine floppase activity	ATP-dependent translocase ABCB1	Homo sapiens (human)
phosphatidylethanolamine flippase activity	ATP-dependent translocase ABCB1	Homo sapiens (human)
ceramide floppase activity	ATP-dependent translocase ABCB1	Homo sapiens (human)
floppase activity	ATP-dependent translocase ABCB1	Homo sapiens (human)
monooxygenase activity	Cytochrome P450 3A4	Homo sapiens (human)
steroid binding	Cytochrome P450 3A4	Homo sapiens (human)
iron ion binding	Cytochrome P450 3A4	Homo sapiens (human)
protein binding	Cytochrome P450 3A4	Homo sapiens (human)
steroid hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
retinoic acid 4-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
oxidoreductase activity	Cytochrome P450 3A4	Homo sapiens (human)
oxygen binding	Cytochrome P450 3A4	Homo sapiens (human)
enzyme binding	Cytochrome P450 3A4	Homo sapiens (human)
heme binding	Cytochrome P450 3A4	Homo sapiens (human)
vitamin D3 25-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
caffeine oxidase activity	Cytochrome P450 3A4	Homo sapiens (human)
quinine 3-monooxygenase activity	Cytochrome P450 3A4	Homo sapiens (human)
testosterone 6-beta-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
1-alpha,25-dihydroxyvitamin D3 23-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
anandamide 8,9 epoxidase activity	Cytochrome P450 3A4	Homo sapiens (human)
anandamide 11,12 epoxidase activity	Cytochrome P450 3A4	Homo sapiens (human)
anandamide 14,15 epoxidase activity	Cytochrome P450 3A4	Homo sapiens (human)
aromatase activity	Cytochrome P450 3A4	Homo sapiens (human)
vitamin D 24-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
estrogen 16-alpha-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
estrogen 2-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
1,8-cineole 2-exo-monooxygenase activity	Cytochrome P450 3A4	Homo sapiens (human)
monooxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
iron ion binding	Cytochrome P450 2C9	Homo sapiens (human)
arachidonic acid epoxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
steroid hydroxylase activity	Cytochrome P450 2C9	Homo sapiens (human)
arachidonic acid 14,15-epoxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
arachidonic acid 11,12-epoxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
oxidoreductase activity	Cytochrome P450 2C9	Homo sapiens (human)
(S)-limonene 6-monooxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
(S)-limonene 7-monooxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
caffeine oxidase activity	Cytochrome P450 2C9	Homo sapiens (human)
(R)-limonene 6-monooxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
aromatase activity	Cytochrome P450 2C9	Homo sapiens (human)
heme binding	Cytochrome P450 2C9	Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen	Cytochrome P450 2C9	Homo sapiens (human)
voltage-gated sodium channel activity	Sodium channel protein type 1 subunit alpha	Homo sapiens (human)
voltage-gated monoatomic ion channel activity involved in regulation of presynaptic membrane potential	Sodium channel protein type 1 subunit alpha	Homo sapiens (human)
voltage-gated sodium channel activity	Sodium channel protein type 4 subunit alpha	Homo sapiens (human)
protein binding	Sodium channel protein type 4 subunit alpha	Homo sapiens (human)
monooxygenase activity	Cytochrome P450 2J2	Homo sapiens (human)
iron ion binding	Cytochrome P450 2J2	Homo sapiens (human)
arachidonic acid epoxygenase activity	Cytochrome P450 2J2	Homo sapiens (human)
arachidonic acid 14,15-epoxygenase activity	Cytochrome P450 2J2	Homo sapiens (human)
arachidonic acid 11,12-epoxygenase activity	Cytochrome P450 2J2	Homo sapiens (human)
isomerase activity	Cytochrome P450 2J2	Homo sapiens (human)
linoleic acid epoxygenase activity	Cytochrome P450 2J2	Homo sapiens (human)
hydroperoxy icosatetraenoate isomerase activity	Cytochrome P450 2J2	Homo sapiens (human)
arachidonic acid 5,6-epoxygenase activity	Cytochrome P450 2J2	Homo sapiens (human)
heme binding	Cytochrome P450 2J2	Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen	Cytochrome P450 2J2	Homo sapiens (human)
sodium channel activity	Sodium channel protein type 7 subunit alpha	Homo sapiens (human)
transmembrane transporter binding	Sodium channel protein type 7 subunit alpha	Homo sapiens (human)
osmolarity-sensing monoatomic cation channel activity	Sodium channel protein type 7 subunit alpha	Homo sapiens (human)
voltage-gated sodium channel activity	Sodium channel protein type 7 subunit alpha	Homo sapiens (human)
high voltage-gated calcium channel activity	Voltage-dependent L-type calcium channel subunit alpha-1D	Homo sapiens (human)
voltage-gated calcium channel activity	Voltage-dependent L-type calcium channel subunit alpha-1D	Homo sapiens (human)
calcium channel activity	Voltage-dependent L-type calcium channel subunit alpha-1D	Homo sapiens (human)
protein binding	Voltage-dependent L-type calcium channel subunit alpha-1D	Homo sapiens (human)
ankyrin binding	Voltage-dependent L-type calcium channel subunit alpha-1D	Homo sapiens (human)
metal ion binding	Voltage-dependent L-type calcium channel subunit alpha-1D	Homo sapiens (human)
alpha-actinin binding	Voltage-dependent L-type calcium channel subunit alpha-1D	Homo sapiens (human)
voltage-gated calcium channel activity involved in cardiac muscle cell action potential	Voltage-dependent L-type calcium channel subunit alpha-1D	Homo sapiens (human)
voltage-gated calcium channel activity involved SA node cell action potential	Voltage-dependent L-type calcium channel subunit alpha-1D	Homo sapiens (human)
voltage-gated potassium channel activity	Potassium voltage-gated channel subfamily A member 1	Homo sapiens (human)
delayed rectifier potassium channel activity	Potassium voltage-gated channel subfamily A member 1	Homo sapiens (human)
protein binding	Potassium voltage-gated channel subfamily A member 1	Homo sapiens (human)
disordered domain specific binding	Potassium voltage-gated channel subfamily A member 1	Homo sapiens (human)
voltage-gated monoatomic ion channel activity involved in regulation of presynaptic membrane potential	Potassium voltage-gated channel subfamily A member 1	Homo sapiens (human)
voltage-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potential	Potassium voltage-gated channel subfamily A member 1	Homo sapiens (human)
transcription cis-regulatory region binding	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
inward rectifier potassium channel activity	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
voltage-gated potassium channel activity	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
delayed rectifier potassium channel activity	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
protein binding	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
ubiquitin protein ligase binding	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
identical protein binding	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
protein homodimerization activity	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
C3HC4-type RING finger domain binding	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
voltage-gated potassium channel activity involved in cardiac muscle cell action potential repolarization	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
scaffold protein binding	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
voltage-gated potassium channel activity involved in ventricular cardiac muscle cell action potential repolarization	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
voltage-gated calcium channel activity	Voltage-dependent L-type calcium channel subunit alpha-1S	Homo sapiens (human)
protein binding	Voltage-dependent L-type calcium channel subunit alpha-1S	Homo sapiens (human)
calmodulin binding	Voltage-dependent L-type calcium channel subunit alpha-1S	Homo sapiens (human)
high voltage-gated calcium channel activity	Voltage-dependent L-type calcium channel subunit alpha-1S	Homo sapiens (human)
small molecule binding	Voltage-dependent L-type calcium channel subunit alpha-1S	Homo sapiens (human)
metal ion binding	Voltage-dependent L-type calcium channel subunit alpha-1S	Homo sapiens (human)
molecular function activator activity	Voltage-dependent L-type calcium channel subunit alpha-1S	Homo sapiens (human)
high voltage-gated calcium channel activity	Voltage-dependent L-type calcium channel subunit alpha-1C	Homo sapiens (human)
voltage-gated calcium channel activity involved in cardiac muscle cell action potential	Voltage-dependent L-type calcium channel subunit alpha-1C	Homo sapiens (human)
voltage-gated calcium channel activity	Voltage-dependent L-type calcium channel subunit alpha-1C	Homo sapiens (human)
protein binding	Voltage-dependent L-type calcium channel subunit alpha-1C	Homo sapiens (human)
calmodulin binding	Voltage-dependent L-type calcium channel subunit alpha-1C	Homo sapiens (human)
high voltage-gated calcium channel activity	Voltage-dependent L-type calcium channel subunit alpha-1C	Homo sapiens (human)
metal ion binding	Voltage-dependent L-type calcium channel subunit alpha-1C	Homo sapiens (human)
alpha-actinin binding	Voltage-dependent L-type calcium channel subunit alpha-1C	Homo sapiens (human)
voltage-gated calcium channel activity involved in cardiac muscle cell action potential	Voltage-dependent L-type calcium channel subunit alpha-1C	Homo sapiens (human)
voltage-gated calcium channel activity involved in AV node cell action potential	Voltage-dependent L-type calcium channel subunit alpha-1C	Homo sapiens (human)
voltage-gated sodium channel activity	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
protein binding	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
calmodulin binding	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
fibroblast growth factor binding	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
enzyme binding	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
protein kinase binding	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
protein domain specific binding	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
ankyrin binding	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
ubiquitin protein ligase binding	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
transmembrane transporter binding	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
nitric-oxide synthase binding	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
voltage-gated sodium channel activity involved in cardiac muscle cell action potential	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
voltage-gated sodium channel activity involved in AV node cell action potential	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
voltage-gated sodium channel activity involved in bundle of His cell action potential	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
voltage-gated sodium channel activity involved in Purkinje myocyte action potential	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
voltage-gated sodium channel activity involved in SA node cell action potential	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
scaffold protein binding	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
voltage-gated sodium channel activity	Sodium channel protein type 9 subunit alpha	Homo sapiens (human)
protein binding	Sodium channel protein type 9 subunit alpha	Homo sapiens (human)
protein binding	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
ATP binding	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
organic anion transmembrane transporter activity	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
ABC-type xenobiotic transporter activity	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
bilirubin transmembrane transporter activity	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activity	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
ATP hydrolysis activity	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
ATPase-coupled transmembrane transporter activity	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
xenobiotic transmembrane transporter activity	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activity	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
ABC-type transporter activity	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
voltage-gated sodium channel activity	Sodium channel protein type 2 subunit alpha	Homo sapiens (human)
protein binding	Sodium channel protein type 2 subunit alpha	Homo sapiens (human)
calmodulin binding	Sodium channel protein type 2 subunit alpha	Homo sapiens (human)
voltage-gated sodium channel activity	Sodium channel protein type 3 subunit alpha	Homo sapiens (human)
voltage-gated sodium channel activity	Sodium channel protein type 11 subunit alpha	Homo sapiens (human)
protein binding	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
ATP binding	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
organic anion transmembrane transporter activity	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
ABC-type xenobiotic transporter activity	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
urate transmembrane transporter activity	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
biotin transmembrane transporter activity	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
efflux transmembrane transporter activity	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
ATP hydrolysis activity	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
riboflavin transmembrane transporter activity	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
ATPase-coupled transmembrane transporter activity	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
identical protein binding	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
protein homodimerization activity	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
xenobiotic transmembrane transporter activity	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
sphingolipid transporter activity	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
voltage-gated sodium channel activity	Sodium channel protein type 8 subunit alpha	Homo sapiens (human)
protein binding	Sodium channel protein type 8 subunit alpha	Homo sapiens (human)
ATP binding	Sodium channel protein type 8 subunit alpha	Homo sapiens (human)
sodium ion binding	Sodium channel protein type 8 subunit alpha	Homo sapiens (human)
voltage-gated sodium channel activity	Sodium channel protein type 10 subunit alpha	Homo sapiens (human)
transmembrane transporter binding	Sodium channel protein type 10 subunit alpha	Homo sapiens (human)
voltage-gated monoatomic ion channel activity involved in regulation of presynaptic membrane potential	Sodium channel protein type 10 subunit alpha	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
plasma membrane	Solute carrier family 22 member 1	Homo sapiens (human)
basal plasma membrane	Solute carrier family 22 member 1	Homo sapiens (human)
membrane	Solute carrier family 22 member 1	Homo sapiens (human)
basolateral plasma membrane	Solute carrier family 22 member 1	Homo sapiens (human)
apical plasma membrane	Solute carrier family 22 member 1	Homo sapiens (human)
lateral plasma membrane	Solute carrier family 22 member 1	Homo sapiens (human)
presynapse	Solute carrier family 22 member 1	Homo sapiens (human)
nucleus	Polyunsaturated fatty acid lipoxygenase ALOX15B	Homo sapiens (human)
cytosol	Polyunsaturated fatty acid lipoxygenase ALOX15B	Homo sapiens (human)
cytoskeleton	Polyunsaturated fatty acid lipoxygenase ALOX15B	Homo sapiens (human)
plasma membrane	Polyunsaturated fatty acid lipoxygenase ALOX15B	Homo sapiens (human)
adherens junction	Polyunsaturated fatty acid lipoxygenase ALOX15B	Homo sapiens (human)
focal adhesion	Polyunsaturated fatty acid lipoxygenase ALOX15B	Homo sapiens (human)
membrane	Polyunsaturated fatty acid lipoxygenase ALOX15B	Homo sapiens (human)
extracellular exosome	Polyunsaturated fatty acid lipoxygenase ALOX15B	Homo sapiens (human)
plasma membrane	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
basal plasma membrane	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
basolateral plasma membrane	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
membrane	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
nucleolus	Multidrug resistance-associated protein 4	Homo sapiens (human)
Golgi apparatus	Multidrug resistance-associated protein 4	Homo sapiens (human)
plasma membrane	Multidrug resistance-associated protein 4	Homo sapiens (human)
membrane	Multidrug resistance-associated protein 4	Homo sapiens (human)
basolateral plasma membrane	Multidrug resistance-associated protein 4	Homo sapiens (human)
apical plasma membrane	Multidrug resistance-associated protein 4	Homo sapiens (human)
platelet dense granule membrane	Multidrug resistance-associated protein 4	Homo sapiens (human)
external side of apical plasma membrane	Multidrug resistance-associated protein 4	Homo sapiens (human)
plasma membrane	Multidrug resistance-associated protein 4	Homo sapiens (human)
photoreceptor outer segment	Voltage-dependent L-type calcium channel subunit alpha-1F	Homo sapiens (human)
membrane	Voltage-dependent L-type calcium channel subunit alpha-1F	Homo sapiens (human)
perikaryon	Voltage-dependent L-type calcium channel subunit alpha-1F	Homo sapiens (human)
voltage-gated calcium channel complex	Voltage-dependent L-type calcium channel subunit alpha-1F	Homo sapiens (human)
basolateral plasma membrane	Bile salt export pump	Homo sapiens (human)
Golgi membrane	Bile salt export pump	Homo sapiens (human)
endosome	Bile salt export pump	Homo sapiens (human)
plasma membrane	Bile salt export pump	Homo sapiens (human)
cell surface	Bile salt export pump	Homo sapiens (human)
apical plasma membrane	Bile salt export pump	Homo sapiens (human)
intercellular canaliculus	Bile salt export pump	Homo sapiens (human)
intracellular canaliculus	Bile salt export pump	Homo sapiens (human)
recycling endosome	Bile salt export pump	Homo sapiens (human)
recycling endosome membrane	Bile salt export pump	Homo sapiens (human)
extracellular exosome	Bile salt export pump	Homo sapiens (human)
membrane	Bile salt export pump	Homo sapiens (human)
nuclear body	Cellular tumor antigen p53	Homo sapiens (human)
nucleus	Cellular tumor antigen p53	Homo sapiens (human)
nucleoplasm	Cellular tumor antigen p53	Homo sapiens (human)
replication fork	Cellular tumor antigen p53	Homo sapiens (human)
nucleolus	Cellular tumor antigen p53	Homo sapiens (human)
cytoplasm	Cellular tumor antigen p53	Homo sapiens (human)
mitochondrion	Cellular tumor antigen p53	Homo sapiens (human)
mitochondrial matrix	Cellular tumor antigen p53	Homo sapiens (human)
endoplasmic reticulum	Cellular tumor antigen p53	Homo sapiens (human)
centrosome	Cellular tumor antigen p53	Homo sapiens (human)
cytosol	Cellular tumor antigen p53	Homo sapiens (human)
nuclear matrix	Cellular tumor antigen p53	Homo sapiens (human)
PML body	Cellular tumor antigen p53	Homo sapiens (human)
transcription repressor complex	Cellular tumor antigen p53	Homo sapiens (human)
site of double-strand break	Cellular tumor antigen p53	Homo sapiens (human)
germ cell nucleus	Cellular tumor antigen p53	Homo sapiens (human)
chromatin	Cellular tumor antigen p53	Homo sapiens (human)
transcription regulator complex	Cellular tumor antigen p53	Homo sapiens (human)
protein-containing complex	Cellular tumor antigen p53	Homo sapiens (human)
cytoplasm	ATP-dependent translocase ABCB1	Homo sapiens (human)
plasma membrane	ATP-dependent translocase ABCB1	Homo sapiens (human)
cell surface	ATP-dependent translocase ABCB1	Homo sapiens (human)
membrane	ATP-dependent translocase ABCB1	Homo sapiens (human)
apical plasma membrane	ATP-dependent translocase ABCB1	Homo sapiens (human)
extracellular exosome	ATP-dependent translocase ABCB1	Homo sapiens (human)
external side of apical plasma membrane	ATP-dependent translocase ABCB1	Homo sapiens (human)
plasma membrane	ATP-dependent translocase ABCB1	Homo sapiens (human)
cytoplasm	Cytochrome P450 3A4	Homo sapiens (human)
endoplasmic reticulum membrane	Cytochrome P450 3A4	Homo sapiens (human)
intracellular membrane-bounded organelle	Cytochrome P450 3A4	Homo sapiens (human)
endoplasmic reticulum membrane	Cytochrome P450 2C9	Homo sapiens (human)
plasma membrane	Cytochrome P450 2C9	Homo sapiens (human)
intracellular membrane-bounded organelle	Cytochrome P450 2C9	Homo sapiens (human)
cytoplasm	Cytochrome P450 2C9	Homo sapiens (human)
intracellular membrane-bounded organelle	Cytochrome P450 2C9	Homo sapiens (human)
plasma membrane	Gamma-aminobutyric acid receptor subunit gamma-2	Rattus norvegicus (Norway rat)
plasma membrane	Sodium channel protein type 1 subunit alpha	Homo sapiens (human)
nucleoplasm	Sodium channel protein type 1 subunit alpha	Homo sapiens (human)
plasma membrane	Sodium channel protein type 1 subunit alpha	Homo sapiens (human)
intercalated disc	Sodium channel protein type 1 subunit alpha	Homo sapiens (human)
nuclear body	Sodium channel protein type 1 subunit alpha	Homo sapiens (human)
Z disc	Sodium channel protein type 1 subunit alpha	Homo sapiens (human)
T-tubule	Sodium channel protein type 1 subunit alpha	Homo sapiens (human)
node of Ranvier	Sodium channel protein type 1 subunit alpha	Homo sapiens (human)
neuronal cell body	Sodium channel protein type 1 subunit alpha	Homo sapiens (human)
axon initial segment	Sodium channel protein type 1 subunit alpha	Homo sapiens (human)
voltage-gated sodium channel complex	Sodium channel protein type 1 subunit alpha	Homo sapiens (human)
plasma membrane	Sodium channel protein type 4 subunit alpha	Homo sapiens (human)
voltage-gated sodium channel complex	Sodium channel protein type 4 subunit alpha	Homo sapiens (human)
endoplasmic reticulum membrane	Cytochrome P450 2J2	Homo sapiens (human)
extracellular exosome	Cytochrome P450 2J2	Homo sapiens (human)
cytoplasm	Cytochrome P450 2J2	Homo sapiens (human)
intracellular membrane-bounded organelle	Cytochrome P450 2J2	Homo sapiens (human)
virion membrane	Spike glycoprotein	Severe acute respiratory syndrome-related coronavirus
plasma membrane	Gamma-aminobutyric acid receptor subunit alpha-1	Rattus norvegicus (Norway rat)
plasma membrane	Gamma-aminobutyric acid receptor subunit beta-2	Rattus norvegicus (Norway rat)
plasma membrane	Sodium channel protein type 7 subunit alpha	Homo sapiens (human)
glial cell projection	Sodium channel protein type 7 subunit alpha	Homo sapiens (human)
voltage-gated sodium channel complex	Sodium channel protein type 7 subunit alpha	Homo sapiens (human)
plasma membrane	Voltage-dependent L-type calcium channel subunit alpha-1D	Homo sapiens (human)
Z disc	Voltage-dependent L-type calcium channel subunit alpha-1D	Homo sapiens (human)
voltage-gated calcium channel complex	Voltage-dependent L-type calcium channel subunit alpha-1D	Homo sapiens (human)
L-type voltage-gated calcium channel complex	Voltage-dependent L-type calcium channel subunit alpha-1D	Homo sapiens (human)
endoplasmic reticulum	Potassium voltage-gated channel subfamily A member 1	Homo sapiens (human)
cytosol	Potassium voltage-gated channel subfamily A member 1	Homo sapiens (human)
plasma membrane	Potassium voltage-gated channel subfamily A member 1	Homo sapiens (human)
cell surface	Potassium voltage-gated channel subfamily A member 1	Homo sapiens (human)
apical plasma membrane	Potassium voltage-gated channel subfamily A member 1	Homo sapiens (human)
cell junction	Potassium voltage-gated channel subfamily A member 1	Homo sapiens (human)
dendrite	Potassium voltage-gated channel subfamily A member 1	Homo sapiens (human)
cytoplasmic vesicle	Potassium voltage-gated channel subfamily A member 1	Homo sapiens (human)
paranode region of axon	Potassium voltage-gated channel subfamily A member 1	Homo sapiens (human)
presynaptic membrane	Potassium voltage-gated channel subfamily A member 1	Homo sapiens (human)
neuronal cell body	Potassium voltage-gated channel subfamily A member 1	Homo sapiens (human)
axon initial segment	Potassium voltage-gated channel subfamily A member 1	Homo sapiens (human)
perikaryon	Potassium voltage-gated channel subfamily A member 1	Homo sapiens (human)
axon terminus	Potassium voltage-gated channel subfamily A member 1	Homo sapiens (human)
juxtaparanode region of axon	Potassium voltage-gated channel subfamily A member 1	Homo sapiens (human)
calyx of Held	Potassium voltage-gated channel subfamily A member 1	Homo sapiens (human)
synapse	Potassium voltage-gated channel subfamily A member 1	Homo sapiens (human)
postsynaptic membrane	Potassium voltage-gated channel subfamily A member 1	Homo sapiens (human)
anchoring junction	Potassium voltage-gated channel subfamily A member 1	Homo sapiens (human)
glutamatergic synapse	Potassium voltage-gated channel subfamily A member 1	Homo sapiens (human)
voltage-gated potassium channel complex	Potassium voltage-gated channel subfamily A member 1	Homo sapiens (human)
dendrite	Potassium voltage-gated channel subfamily A member 1	Homo sapiens (human)
paranode region of axon	Potassium voltage-gated channel subfamily A member 1	Homo sapiens (human)
membrane	Potassium voltage-gated channel subfamily A member 1	Homo sapiens (human)
synapse	Potassium voltage-gated channel subfamily A member 1	Homo sapiens (human)
juxtaparanode region of axon	Potassium voltage-gated channel subfamily A member 1	Homo sapiens (human)
neuronal cell body	Potassium voltage-gated channel subfamily A member 1	Homo sapiens (human)
plasma membrane	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
cell surface	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
perinuclear region of cytoplasm	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
voltage-gated potassium channel complex	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
inward rectifier potassium channel complex	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
plasma membrane	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
cytoplasm	Voltage-dependent L-type calcium channel subunit alpha-1S	Homo sapiens (human)
plasma membrane	Voltage-dependent L-type calcium channel subunit alpha-1S	Homo sapiens (human)
sarcoplasmic reticulum	Voltage-dependent L-type calcium channel subunit alpha-1S	Homo sapiens (human)
T-tubule	Voltage-dependent L-type calcium channel subunit alpha-1S	Homo sapiens (human)
I band	Voltage-dependent L-type calcium channel subunit alpha-1S	Homo sapiens (human)
L-type voltage-gated calcium channel complex	Voltage-dependent L-type calcium channel subunit alpha-1S	Homo sapiens (human)
voltage-gated calcium channel complex	Voltage-dependent L-type calcium channel subunit alpha-1S	Homo sapiens (human)
cytoplasm	Voltage-dependent L-type calcium channel subunit alpha-1C	Homo sapiens (human)
plasma membrane	Voltage-dependent L-type calcium channel subunit alpha-1C	Homo sapiens (human)
postsynaptic density	Voltage-dependent L-type calcium channel subunit alpha-1C	Homo sapiens (human)
membrane	Voltage-dependent L-type calcium channel subunit alpha-1C	Homo sapiens (human)
Z disc	Voltage-dependent L-type calcium channel subunit alpha-1C	Homo sapiens (human)
dendrite	Voltage-dependent L-type calcium channel subunit alpha-1C	Homo sapiens (human)
perikaryon	Voltage-dependent L-type calcium channel subunit alpha-1C	Homo sapiens (human)
postsynaptic density membrane	Voltage-dependent L-type calcium channel subunit alpha-1C	Homo sapiens (human)
L-type voltage-gated calcium channel complex	Voltage-dependent L-type calcium channel subunit alpha-1C	Homo sapiens (human)
voltage-gated calcium channel complex	Voltage-dependent L-type calcium channel subunit alpha-1C	Homo sapiens (human)
caveola	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
nucleoplasm	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
nucleolus	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
endoplasmic reticulum	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
plasma membrane	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
caveola	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
cell surface	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
intercalated disc	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
membrane	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
lateral plasma membrane	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
Z disc	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
T-tubule	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
sarcolemma	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
perinuclear region of cytoplasm	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
voltage-gated sodium channel complex	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
plasma membrane	Sodium channel protein type 9 subunit alpha	Homo sapiens (human)
axon	Sodium channel protein type 9 subunit alpha	Homo sapiens (human)
voltage-gated sodium channel complex	Sodium channel protein type 9 subunit alpha	Homo sapiens (human)
plasma membrane	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
cell surface	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
apical plasma membrane	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
intercellular canaliculus	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
apical plasma membrane	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
plasma membrane	Sodium channel protein type 2 subunit alpha	Homo sapiens (human)
plasma membrane	Sodium channel protein type 2 subunit alpha	Homo sapiens (human)
intercalated disc	Sodium channel protein type 2 subunit alpha	Homo sapiens (human)
T-tubule	Sodium channel protein type 2 subunit alpha	Homo sapiens (human)
axon	Sodium channel protein type 2 subunit alpha	Homo sapiens (human)
node of Ranvier	Sodium channel protein type 2 subunit alpha	Homo sapiens (human)
paranode region of axon	Sodium channel protein type 2 subunit alpha	Homo sapiens (human)
presynaptic membrane	Sodium channel protein type 2 subunit alpha	Homo sapiens (human)
glutamatergic synapse	Sodium channel protein type 2 subunit alpha	Homo sapiens (human)
voltage-gated sodium channel complex	Sodium channel protein type 2 subunit alpha	Homo sapiens (human)
membrane	Sodium channel protein type 2 subunit alpha	Homo sapiens (human)
sarcoplasm	Sodium channel protein type 3 subunit alpha	Homo sapiens (human)
voltage-gated sodium channel complex	Sodium channel protein type 3 subunit alpha	Homo sapiens (human)
plasma membrane	Sodium channel protein type 11 subunit alpha	Homo sapiens (human)
axon	Sodium channel protein type 11 subunit alpha	Homo sapiens (human)
neuronal cell body	Sodium channel protein type 11 subunit alpha	Homo sapiens (human)
axonal growth cone	Sodium channel protein type 11 subunit alpha	Homo sapiens (human)
C-fiber	Sodium channel protein type 11 subunit alpha	Homo sapiens (human)
extracellular exosome	Sodium channel protein type 11 subunit alpha	Homo sapiens (human)
voltage-gated sodium channel complex	Sodium channel protein type 11 subunit alpha	Homo sapiens (human)
nucleoplasm	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
plasma membrane	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
apical plasma membrane	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
brush border membrane	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
mitochondrial membrane	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
membrane raft	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
external side of apical plasma membrane	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
plasma membrane	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
plasma membrane	Sodium channel protein type 8 subunit alpha	Homo sapiens (human)
membrane	Sodium channel protein type 8 subunit alpha	Homo sapiens (human)
Z disc	Sodium channel protein type 8 subunit alpha	Homo sapiens (human)
cell junction	Sodium channel protein type 8 subunit alpha	Homo sapiens (human)
axon	Sodium channel protein type 8 subunit alpha	Homo sapiens (human)
cytoplasmic vesicle	Sodium channel protein type 8 subunit alpha	Homo sapiens (human)
node of Ranvier	Sodium channel protein type 8 subunit alpha	Homo sapiens (human)
axon initial segment	Sodium channel protein type 8 subunit alpha	Homo sapiens (human)
presynaptic active zone membrane	Sodium channel protein type 8 subunit alpha	Homo sapiens (human)
parallel fiber to Purkinje cell synapse	Sodium channel protein type 8 subunit alpha	Homo sapiens (human)
postsynaptic density membrane	Sodium channel protein type 8 subunit alpha	Homo sapiens (human)
glutamatergic synapse	Sodium channel protein type 8 subunit alpha	Homo sapiens (human)
voltage-gated sodium channel complex	Sodium channel protein type 8 subunit alpha	Homo sapiens (human)
plasma membrane	Sodium channel protein type 10 subunit alpha	Homo sapiens (human)
axon	Sodium channel protein type 10 subunit alpha	Homo sapiens (human)
presynaptic membrane	Sodium channel protein type 10 subunit alpha	Homo sapiens (human)
extracellular exosome	Sodium channel protein type 10 subunit alpha	Homo sapiens (human)
glutamatergic synapse	Sodium channel protein type 10 subunit alpha	Homo sapiens (human)
voltage-gated sodium channel complex	Sodium channel protein type 10 subunit alpha	Homo sapiens (human)
clathrin complex	Sodium channel protein type 10 subunit alpha	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (544)

Assay ID	Title	Year	Journal	Article
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.
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.
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.
AID1579936	Induction of CSPG-treated human induced sensory neuron growth at 2 uM for 24 hrs by immunostaining method relative to control	2020	Journal of medicinal chemistry, 01-23, Volume: 63, Issue:2	The Rise of Molecules Able To Regenerate the Central Nervous System.
AID269354	Cardiac activity in guinea pig heart measured as decrease in heart rate at 1 uM by ECG relative to control	2006	Journal of medicinal chemistry, Aug-24, Volume: 49, Issue:17	Calcium channel antagonists discovered by a multidisciplinary approach.
AID167362	Inhibition of contraction in rabbit aorta, K+.	1983	Journal of medicinal chemistry, Jun, Volume: 26, Issue:6	New developments in Ca2+ channel antagonists.
AID76399	Vasorelaxant activity calculated from log concentration-response curves; Range is from 2.2-3.1 (10e-6 M)	2002	Journal of medicinal chemistry, Aug-01, Volume: 45, Issue:16	Cardiovascular characterization of [1,4]thiazino[3,4-c][1,2,4]oxadiazol-1-one derivatives: selective myocardial calcium channel modulators.
AID249569	Compound was tested for percent change in heart rate in isolated guinea pig atrium	2005	Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7	A new class of selective myocardial calcium channel modulators. 2. Role of the acetal chain in oxadiazol-3-one derivatives.
AID411047	Blockade of L-type calcium channel	2009	Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2	Inhibition of MDR1 activity in vitro by a novel class of diltiazem analogues: toward new candidates.
AID1079941	Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID243151	Inhibitory concentration against potassium channel HERG	2005	Bioorganic & medicinal chemistry letters, Jun-02, Volume: 15, Issue:11	A discriminant model constructed by the support vector machine method for HERG potassium channel inhibitors.
AID363997	Negative inotropic activity in guinea pig left atrium assessed as decrease in atrial tension relative to control	2008	Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18	Discovery of novel and cardioselective diltiazem-like calcium channel blockers via virtual screening.
AID27167	Delta logD (logD6.5 - logD7.4)	2000	Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13	QSAR model for drug human oral bioavailability.
AID625285	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1221965	Transporter substrate index of efflux ratio in human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of P-gp inhibitor LY335979	2011	Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2	Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID411048	Antiproliferative activity against human A2780 cells after 3 days by MTT assay	2009	Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2	Inhibition of MDR1 activity in vitro by a novel class of diltiazem analogues: toward new candidates.
AID1307839	Relaxant activity in potassium depolarized guinea pig ileum longitudinal smooth muscle assessed as inhibition of calcium-induced contraction at 5 uM after 30 mins	2016	Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7	Understanding Oxadiazolothiazinone Biological Properties: Negative Inotropic Activity versus Cytochrome P450-Mediated Metabolism.
AID1221963	Transporter substrate index ratio of permeability from apical to basolateral side in human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of P-gp inhibitor LY335979	2011	Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2	Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID88404	In Vitro evaluation on percentage inhibition in Heme Oxygenase at concentration 100(uM) of Cell-free parasite Plasmodium yoelii	2000	Journal of medicinal chemistry, Sep-07, Volume: 43, Issue:18	A new class of potential chloroquine-resistance reversal agents for Plasmodia: syntheses and biological evaluation of 1-(3'-diethylaminopropyl)-3-(substituted phenylmethylene)pyrrolidines.
AID444057	Fraction escaping hepatic elimination in human	2010	Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3	Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID269342	Negative inotropic activity in guinea pig left atrium	2006	Journal of medicinal chemistry, Aug-24, Volume: 49, Issue:17	Calcium channel antagonists discovered by a multidisciplinary approach.
AID496820	Antimicrobial activity against Trypanosoma brucei	2010	Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6	Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID269343	Negative chronotropic activity in guinea pig right atrium	2006	Journal of medicinal chemistry, Aug-24, Volume: 49, Issue:17	Calcium channel antagonists discovered by a multidisciplinary approach.
AID1197220	Antagonist activity at Cav1.2a in K+-depolarized guinea pig aortic strips assessed as inhibition of calcium-induced contraction at 10'-4 M relative to control	2015	European journal of medicinal chemistry, Mar-06, Volume: 92	Synthesis and L-type calcium channel blocking activity of new chiral oxadiazolothiazinones.
AID496818	Antimicrobial activity against Trypanosoma brucei brucei	2010	Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6	Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID165788	In vitro inhibition of development of isometric tension, in response to norepinephrine (NE, 10 uM) in rabbit aorta	1988	Journal of medicinal chemistry, Mar, Volume: 31, Issue:3	2-Ethynylbenzenealkanamines. A new class of calcium entry blockers.
AID173685	Percent decrease in blood pressure in hypertensive rat at 60 mg/kg po	1987	Journal of medicinal chemistry, Apr, Volume: 30, Issue:4	Synthesis and biological activity of novel calcium channel blockers: 2,5-dihydro-4-methyl-2-phenyl-1,5-benzothiazepine-3-carboxylic acid esters and 2,5-dihydro-4-methyl-2-phenyl-1,5-benzodiazepine-3-carboxylic acid esters.
AID592681	Apparent permeability across human Caco2 cell membrane after 2 hrs by LC-MS/MS analysis	2011	Bioorganic & medicinal chemistry, Apr-15, Volume: 19, Issue:8	QSAR-based permeability model for drug-like compounds.
AID624628	Drug-stimulated Pgp ATPase activity ratio determined in MDR1-Sf9 cell membranes with test compound at a concentration of 20uM	2001	The Journal of pharmacology and experimental therapeutics, Nov, Volume: 299, Issue:2	Rational use of in vitro P-glycoprotein assays in drug discovery.
AID1079935	Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source]
AID496829	Antimicrobial activity against Leishmania infantum	2010	Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6	Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID21851	In vitro clearance in human in 1000000 cells	1999	Journal of medicinal chemistry, Dec-16, Volume: 42, Issue:25	Combining in vitro and in vivo pharmacokinetic data for prediction of hepatic drug clearance in humans by artificial neural networks and multivariate statistical techniques.
AID231901	Ratio between the EC30 values of aortic contracture and atrial rate	1990	Journal of medicinal chemistry, May, Volume: 33, Issue:5	Specific bradycardic agents. 1. Chemistry, pharmacology, and structure-activity relationships of substituted benzazepinones, a-new class of compounds exerting antiischemic properties.
AID540209	Volume of distribution at steady state in human after iv administration	2008	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7	Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID60874	Percent inhibition of calcium-dependent potassium-polarized smooth muscle contraction in canine trachea	1988	Journal of medicinal chemistry, Nov, Volume: 31, Issue:11	Synthesis of (aryloxy)alkylamines. 2. Novel imidazo-fused heterocycles with calcium channel blocking and local anesthetic activity.
AID588216	FDA HLAED, serum glutamic oxaloacetic transaminase (SGOT) increase	2004	Current drug discovery technologies, Dec, Volume: 1, Issue:4	Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID251138	Negative chronotropic activity was determined as percent decrease in the artial rate in spontaneously beating guinea pig artium at 5x10E-5 M (n=6-8)	2005	Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7	A new class of selective myocardial calcium channel modulators. 2. Role of the acetal chain in oxadiazol-3-one derivatives.
AID496832	Antimicrobial activity against Trypanosoma brucei rhodesiense	2010	Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6	Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID415105	Effect on cardiac activity in guinea pig spontaneously beating heart assessed as change in coronary perfusion pressure at 1 uM relative to control	2009	Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8	L-Type calcium channel blockers: from diltiazem to 1,2,4-oxadiazol-5-ones via thiazinooxadiazol-3-one derivatives.
AID58832	Antihypertensive activity by the increase in the vertebral blood flow in anesthetized dogs expressed as duration of half of the maximum change in blood flow.	1991	Journal of medicinal chemistry, Feb, Volume: 34, Issue:2	Synthesis of halogen-substituted 1,5-benzothiazepine derivatives and their vasodilating and hypotensive activities.
AID540228	Clearance in human after iv administration	2006	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 34, Issue:7	Extrapolation of preclinical pharmacokinetics and molecular feature analysis of "discovery-like" molecules to predict human pharmacokinetics.
AID1307802	Vasorelaxant activity in potassium depolarized guinea pig aorta assessed as relaxation of calcium-induced contraction	2016	Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7	Understanding Oxadiazolothiazinone Biological Properties: Negative Inotropic Activity versus Cytochrome P450-Mediated Metabolism.
AID175822	Diuretic effect was evaluated in the conscious female rat by natriuretic assay involving metabolic caging at dose 20 mg/kg	1996	Journal of medicinal chemistry, Mar-15, Volume: 39, Issue:6	Endogenous natriuretic factors. 5. Synthesis and biological activity of a natriuretic metabolite of diltiazem and its derivatives.
AID76235	Displacement of [3H]nitrendipine binding to L-type calcium channel of Guinea pig cerebral cortex membranes	1992	Journal of medicinal chemistry, Mar-20, Volume: 35, Issue:6	A novel class of calcium-entry blockers: the 1[[4-(aminoalkoxy)phenyl]sulfonyl]indolizines.
AID496830	Antimicrobial activity against Leishmania major	2010	Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6	Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1394667	Stability in horse serum assessed as compound receovery after 24 hrs by LC/MS analysis	2018	European journal of medicinal chemistry, Apr-25, Volume: 150	Inhibition of trypanosome alternative oxidase without its N-terminal mitochondrial targeting signal (ΔMTS-TAO) by cationic and non-cationic 4-hydroxybenzoate and 4-alkoxybenzaldehyde derivatives active against T. brucei and T. congolense.
AID415107	Effect on cardiac activity in guinea pig spontaneously beating heart assessed as change in left ventricular pressure	2009	Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8	L-Type calcium channel blockers: from diltiazem to 1,2,4-oxadiazol-5-ones via thiazinooxadiazol-3-one derivatives.
AID161281	Inhibition of human Potassium channel HERG expressed in mammalian cells	2003	Bioorganic & medicinal chemistry letters, Aug-18, Volume: 13, Issue:16	Prediction of hERG potassium channel affinity by traditional and hologram qSAR methods.
AID173379	In vivo evaluation for the percentage decrease in blood pressure at 135 umol/kg administered through oral route in spontaneously hypertensive rats and observed for 12-18 h.	1992	Journal of medicinal chemistry, Feb-21, Volume: 35, Issue:4	Benzazepinone calcium channel blockers. 2. Structure-activity and drug metabolism studies leading to potent antihypertensive agents. Comparison with benzothiazepinones.
AID237685	Lipophilicity determined as logarithm of the partition coefficient in the alkane/water system	2005	Journal of medicinal chemistry, May-05, Volume: 48, Issue:9	Calculating virtual log P in the alkane/water system (log P(N)(alk)) and its derived parameters deltalog P(N)(oct-alk) and log D(pH)(alk).
AID193222	Antihypertensive activity 12-18 hr after 135 umol/kg p.o. in rats.	1992	Journal of medicinal chemistry, Jul-10, Volume: 35, Issue:14	Benzazepinone calcium channel blockers. 5. Effects on antihypertensive activity associated with N1 and aromatic substituents.
AID1218851	Ratio of IC50 for CYP3A4 in human liver microsomes using midazolam as substrate preincubated for 30 mins to IC50 for CYP3A4 in human liver microsomes using midazolam as substrate preincubated for 30 mins in presence of NADPH	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme.
AID625291	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID171866	Antihypertensive activity expressed as change in mean arterial blood pressure (MABP) in spontaneously hypertensive rats (SHR), at 3-6h after 30 mg/kg oral administration	1991	Journal of medicinal chemistry, Oct, Volume: 34, Issue:10	Synthesis, calcium-channel-blocking activity, and antihypertensive activity of 4-(diarylmethyl)-1-[3-(aryloxy)propyl]piperidines and structurally related compounds.
AID168010	Preventive effect of compound was measured on vasopressin-induced ST depression rats at 3 mg/kg po dose after 1 hr of administration; -=No significance	1991	Journal of medicinal chemistry, Mar, Volume: 34, Issue:3	A new class of calcium antagonists. 2. Synthesis and biological activity of 11-[[4-[4-(4-fluorophenyl)-1-piperazinyl]butyryl]amino]-6,11- dihydrodibenzo[b,e]-thiepin maleate and related compounds.
AID496828	Antimicrobial activity against Leishmania donovani	2010	Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6	Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID781326	pKa (acid-base dissociation constant) as determined by Avdeef ref: DOI: 10.1002/047145026X	2014	Pharmaceutical research, Apr, Volume: 31, Issue:4	Comparison of the accuracy of experimental and predicted pKa values of basic and acidic compounds.
AID1079933	Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is
AID1079947	Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID781328	pKa (acid-base dissociation constant) as determined by Luan ref: Pharm. Res. 2005	2014	Pharmaceutical research, Apr, Volume: 31, Issue:4	Comparison of the accuracy of experimental and predicted pKa values of basic and acidic compounds.
AID1284957	Half life in rat plasma at 1 uM by LC-MS/MS analysis	2016	European journal of medicinal chemistry, Apr-13, Volume: 112	Systematic diversification of benzylidene heterocycles yields novel inhibitor scaffolds selective for Dyrk1A, Clk1 and CK2.
AID1307825	Negative inotropic activity in potassium depolarized guinea pig left atrium assessed as reduction in developed tension at 10'-5 M after 30 mins	2016	Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7	Understanding Oxadiazolothiazinone Biological Properties: Negative Inotropic Activity versus Cytochrome P450-Mediated Metabolism.
AID59092	Compound was tested for its hemodynamic effect for percentage change in heart rate in anesthetized Dogs	1989	Journal of medicinal chemistry, Jan, Volume: 32, Issue:1	5-Isoquinolinesulfonamide derivatives. 2. Synthesis and vasodilatory activity of N-(2-aminoethyl)-5-isoquinolinesulfonamide derivatives.
AID173501	In vivo evaluation for the percentage decrease in blood pressure at 135 umol/kg administered through oral route in spontaneously hypertensive rats and observed for 6-12 h.	1992	Journal of medicinal chemistry, Feb-21, Volume: 35, Issue:4	Benzazepinone calcium channel blockers. 2. Structure-activity and drug metabolism studies leading to potent antihypertensive agents. Comparison with benzothiazepinones.
AID1579935	Induction of CSPG-treated C57BL/6J mouse DRG neuron growth at 25 uM incubated for 24 hrs by Alexa Fluor 488 staining based assay relative to control	2020	Journal of medicinal chemistry, 01-23, Volume: 63, Issue:2	The Rise of Molecules Able To Regenerate the Central Nervous System.
AID1823669	Stability in rat plasma assessed as parent compound remaining at 10 uM measured after 30 mins by LC-MS analysis	2021	Journal of medicinal chemistry, 05-27, Volume: 64, Issue:10	Discovery of New Imidazo[2,1-
AID1823670	Stability in rat plasma assessed as parent compound remaining at 10 uM measured after 120 mins by LC-MS analysis	2021	Journal of medicinal chemistry, 05-27, Volume: 64, Issue:10	Discovery of New Imidazo[2,1-
AID540222	Clearance in rat after iv administration	2006	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 34, Issue:7	Extrapolation of preclinical pharmacokinetics and molecular feature analysis of "discovery-like" molecules to predict human pharmacokinetics.
AID1473739	Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay	2013	Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1	A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID188409	Natriuretic effect was evaluated in the conscious female rat by natriuretic assay involving metabolic caging at dose 10 mg/kg	1996	Journal of medicinal chemistry, Mar-15, Volume: 39, Issue:6	Endogenous natriuretic factors. 5. Synthesis and biological activity of a natriuretic metabolite of diltiazem and its derivatives.
AID624629	Inhibition of Pgp expressed in MDR1-MDCKII cells measured by calcein-AM assay	2001	The Journal of pharmacology and experimental therapeutics, Nov, Volume: 299, Issue:2	Rational use of in vitro P-glycoprotein assays in drug discovery.
AID1209259	Drug metabolism in human liver microsomes assessed as maximum rate of reaction per mg protein by optimal design approach	2012	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12	Optimized experimental design for the estimation of enzyme kinetic parameters: an experimental evaluation.
AID1218844	Time dependent inhibition of CYP3A4 in human liver microsomes using testosterone as substrate preincubated for 30 mins followed by substrate addition by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme.
AID731591	Induction of beta glucosidase N370S mutant activity in primary skin fibroblasts derived from Gaucher disease type 1 patient at 10 to 20 mM after 7 days relative to control	2013	Journal of medicinal chemistry, Apr-11, Volume: 56, Issue:7	Pharmacological chaperones as therapeutics for lysosomal storage diseases.
AID21852	In vitro clearance in rat in 1000000 cells	1999	Journal of medicinal chemistry, Dec-16, Volume: 42, Issue:25	Combining in vitro and in vivo pharmacokinetic data for prediction of hepatic drug clearance in humans by artificial neural networks and multivariate statistical techniques.
AID678714	Inhibition of human CYP2C19 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 3-butyryl-7-methoxycoumarin as substrate after 30 mins	2012	Chemical research in toxicology, Oct-15, Volume: 25, Issue:10	Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID1207154	Inhibition of Na channel (species unknown)	2011	Cardiovascular research, Jul-01, Volume: 91, Issue:1	Simulation of multiple ion channel block provides improved early prediction of compounds' clinical torsadogenic risk.
AID540223	Volume of distribution at steady state in rat after iv administration	2006	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 34, Issue:7	Extrapolation of preclinical pharmacokinetics and molecular feature analysis of "discovery-like" molecules to predict human pharmacokinetics.
AID496825	Antimicrobial activity against Leishmania mexicana	2010	Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6	Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID170565	Preventive effect of compound was measured on methacholine-induced ST elevation in anesthetized rats at 0.3 mg/kg iv dose with test compound (0-90 min)	1991	Journal of medicinal chemistry, Mar, Volume: 34, Issue:3	A new class of calcium antagonists. 2. Synthesis and biological activity of 11-[[4-[4-(4-fluorophenyl)-1-piperazinyl]butyryl]amino]-6,11- dihydrodibenzo[b,e]-thiepin maleate and related compounds.
AID88411	In Vitro inhibition of Heme Oxygenase in Cell-free parasite Plasmodium yoelii at concentration 50 uM	2000	Journal of medicinal chemistry, Sep-07, Volume: 43, Issue:18	A new class of potential chloroquine-resistance reversal agents for Plasmodia: syntheses and biological evaluation of 1-(3'-diethylaminopropyl)-3-(substituted phenylmethylene)pyrrolidines.
AID467405	Muscle relaxant activity in 80 mM K+-depolarized guinea pig ileum longitudinal smooth muscle assessed as inhibition of calcium-induced contraction at 10 uM	2009	Journal of medicinal chemistry, Nov-12, Volume: 52, Issue:21	Stereoselective behavior of the functional diltiazem analogue 1-[(4-chlorophenyl)sulfonyl]-2-(2-thienyl)pyrrolidine, a new L-type calcium channel blocker.
AID170564	Preventive effect of compound was measured on methacholine-induced ST elevation in anesthetized rats at 0.1 mg/kg iv dose without test compound	1991	Journal of medicinal chemistry, Mar, Volume: 34, Issue:3	A new class of calcium antagonists. 2. Synthesis and biological activity of 11-[[4-[4-(4-fluorophenyl)-1-piperazinyl]butyryl]amino]-6,11- dihydrodibenzo[b,e]-thiepin maleate and related compounds.
AID496817	Antimicrobial activity against Trypanosoma cruzi	2010	Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6	Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID167814	Vasorelaxant effects in circumferential strips of potassium-depolarized rabbit aorta. (IC50 in rabbit aorta strips contracted with KCl(95% confidence interval))	1992	Journal of medicinal chemistry, Feb-21, Volume: 35, Issue:4	Benzazepinone calcium channel blockers. 2. Structure-activity and drug metabolism studies leading to potent antihypertensive agents. Comparison with benzothiazepinones.
AID467613	Volume of distribution at steady state in human	2009	European journal of medicinal chemistry, Nov, Volume: 44, Issue:11	Prediction of volume of distribution values in human using immobilized artificial membrane partitioning coefficients, the fraction of compound ionized and plasma protein binding data.
AID1218820	Time dependent inhibition of CYP3A4 in human liver microsomes using testosterone as substrate preincubated for 90 mins followed by 10-fold dilution and substrate addition by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme.
AID45795	Inhibition of [3H]nitrendipine binding to L-type calcium channel receptor(CCR) in rat cerebral cortex homogenate	1996	Journal of medicinal chemistry, Jul-19, Volume: 39, Issue:15	Cardiovascular characterization of pyrrolo[2,1-d][1,5]benzothiazepine derivatives binding selectively to the peripheral-type benzodiazepine receptor (PBR): from dual PBR affinity and calcium antagonist activity to novel and selective calcium entry blocker
AID1218819	Time dependent inhibition of CYP3A4 in human liver microsomes using midazolam as substrate preincubated for 90 mins followed by 10-fold dilution and substrate addition by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme.
AID540227	Volume of distribution at steady state in monkey after iv administration	2006	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 34, Issue:7	Extrapolation of preclinical pharmacokinetics and molecular feature analysis of "discovery-like" molecules to predict human pharmacokinetics.
AID625279	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1079945	Animal toxicity known. [column 'TOXIC' in source]
AID195197	Inhibition of [Ca2+] induced contraction of K+ depolarized rat aorta by 50%	1993	Journal of medicinal chemistry, May-14, Volume: 36, Issue:10	Novel heterocyclic analogues of the new potent class of calcium entry blockers: 1-[[4-(aminoalkoxy)phenyl]sulfonyl]indolizines.
AID625287	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID680119	TP_TRANSPORTER: transepithelial transport (basal to apical) in MDR1-expressing LLC-PK1 cells	1993	FEBS letters, Jun-07, Volume: 324, Issue:1	P-glycoprotein-mediated transcellular transport of MDR-reversing agents.
AID678722	Covalent binding affinity to human liver microsomes assessed per mg of protein at 10 uM after 60 mins presence of NADPH	2012	Chemical research in toxicology, Oct-15, Volume: 25, Issue:10	Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID425653	Renal clearance in human	2009	Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15	Physicochemical determinants of human renal clearance.
AID415101	Inhibition of L-type calcium channel in Wistar rat tail artery smooth muscle cells assessed as blockade of barium-sensitive inward rectifying current by whole cell patch-clamp assay	2009	Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8	L-Type calcium channel blockers: from diltiazem to 1,2,4-oxadiazol-5-ones via thiazinooxadiazol-3-one derivatives.
AID73880	Effective drug concentration for negative inotropic activity was determined; Range is from 0.70-0.85 (10e-6 M)	2002	Journal of medicinal chemistry, Aug-01, Volume: 45, Issue:16	Cardiovascular characterization of [1,4]thiazino[3,4-c][1,2,4]oxadiazol-1-one derivatives: selective myocardial calcium channel modulators.
AID396645	Inhibition of calcium channel	2009	European journal of medicinal chemistry, Jan, Volume: 44, Issue:1	Mechanistic aspects of benzothiazepines: a class of antiarrhythmic drugs.
AID80746	Evaluated in vitro for the effect on spontaneous atrial rate in isolated guinea pig atria	1990	Journal of medicinal chemistry, May, Volume: 33, Issue:5	Specific bradycardic agents. 1. Chemistry, pharmacology, and structure-activity relationships of substituted benzazepinones, a-new class of compounds exerting antiischemic properties.
AID79711	Inotropic negative potency on stimulated guinea pig left atrium	1995	Journal of medicinal chemistry, Oct-27, Volume: 38, Issue:22	Pyrrolo[2,1-c][1,4]benzothiazines: synthesis, structure-activity relationships, molecular modeling studies, and cardiovascular activity.
AID1218826	Ratio of IC50 for CYP3A4 in human liver microsomes using testosterone as substrate preincubated for 30 mins followed by 10-fold dilution and substrate addition to IC50 for CYP3A4 in human liver microsomes using testosterone as substrate preincubated for 3	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme.
AID589142	Mechanism based inhibition of human cytochrome P450 3A4 measured by testosterone 6-beta hydroxylation	2005	Current drug metabolism, Oct, Volume: 6, Issue:5	Cytochrome p450 enzymes mechanism based inhibitors: common sub-structures and reactivity.
AID249604	Compound was tested for percent change in maximal rate of the rise in left ventricular pressure in isolated guinea pig atrium	2005	Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7	A new class of selective myocardial calcium channel modulators. 2. Role of the acetal chain in oxadiazol-3-one derivatives.
AID1091958	Hydrophobicity, log P of the compound in octanol-water by shaking-flask method	2011	Journal of agricultural and food chemistry, Apr-13, Volume: 59, Issue:7	Importance of physicochemical properties for the design of new pesticides.
AID173376	In vivo evaluation for the percentage decrease in blood pressure at 135 umol/kg administered through oral route in spontaneously hypertensive rats and observed for 0-6 h.	1992	Journal of medicinal chemistry, Feb-21, Volume: 35, Issue:4	Benzazepinone calcium channel blockers. 2. Structure-activity and drug metabolism studies leading to potent antihypertensive agents. Comparison with benzothiazepinones.
AID540210	Clearance in human after iv administration	2008	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7	Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID681335	TP_TRANSPORTER: inhibition of Digoxin transepithelial transport (basal to apical) (Digoxin: 0.1 uM) in MDR1-expressing LLC-PK1 cells	2002	European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences, Aug, Volume: 16, Issue:3	Effects of 12 Ca2+ antagonists on multidrug resistance, MDR1-mediated transport and MDR1 mRNA expression.
AID95592	Inhibition of [3H]nitrendipine binding at L-type [Ca2+] channel in rat cortex homogenate by 50%.	1995	Journal of medicinal chemistry, Oct-27, Volume: 38, Issue:22	Pyrrolo[2,1-c][1,4]benzothiazines: synthesis, structure-activity relationships, molecular modeling studies, and cardiovascular activity.
AID1215350	Time dependent inhibition of CYP3A4 in human liver microsomes assessed as conversion of testosterone to 6beta-hydroxytestosterone at 0.01 to 100 uM preincubated for 60 mins followed by testosterone treatment measured after 10 mins by refined CYP450 IC50 s	2011	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 39, Issue:6	A refined cytochrome P540 IC₅₀ shift assay for reliably identifying CYP3A time-dependent inhibitors.
AID363998	Vasorelaxant activity in K+-depolarized guinea pig aorta assessed as inhibition of calcium-induced contraction at 100 uM	2008	Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18	Discovery of novel and cardioselective diltiazem-like calcium channel blockers via virtual screening.
AID1517041	Stability in human plasma assessed as remaining compound at 10 uM incubated for 30 mins by LC-MS analysis
AID60585	Antihypertensive activity expressed as the ratio of the potency evaluated by increased vertebral blood flow (VBF) to that of diltiazem.	1991	Journal of medicinal chemistry, Feb, Volume: 34, Issue:2	Synthesis of halogen-substituted 1,5-benzothiazepine derivatives and their vasodilating and hypotensive activities.
AID79690	Tested for the negative inotropic activity on isolated guinea pig left atrium at 10e-5 M	1995	Journal of medicinal chemistry, Oct-27, Volume: 38, Issue:22	Pyrrolo[2,1-c][1,4]benzothiazines: synthesis, structure-activity relationships, molecular modeling studies, and cardiovascular activity.
AID21854	In vivo clearance in dog.	1999	Journal of medicinal chemistry, Dec-16, Volume: 42, Issue:25	Combining in vitro and in vivo pharmacokinetic data for prediction of hepatic drug clearance in humans by artificial neural networks and multivariate statistical techniques.
AID222726	Percent decrease of negative inotropic activity on isolated guinea pig left atrium at 1*10e-5 M	1996	Journal of medicinal chemistry, Jul-19, Volume: 39, Issue:15	Cardiovascular characterization of pyrrolo[2,1-d][1,5]benzothiazepine derivatives binding selectively to the peripheral-type benzodiazepine receptor (PBR): from dual PBR affinity and calcium antagonist activity to novel and selective calcium entry blocker
AID1218852	Ratio of IC50 for CYP3A4 in human liver microsomes using testosterone as substrate preincubated for 30 mins to IC50 for CYP3A4 in human liver microsomes using testosterone as substrate preincubated for 30 mins in presence of NADPH	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme.
AID588215	FDA HLAED, alkaline phosphatase increase	2004	Current drug discovery technologies, Dec, Volume: 1, Issue:4	Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID246472	Negative inotropic potency is determined by decrease in the developed tension on isolated left ventricular papillary muscle (n=5-7)	2005	Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7	A new class of selective myocardial calcium channel modulators. 2. Role of the acetal chain in oxadiazol-3-one derivatives.
AID415108	Effect on cardiac activity in guinea pig spontaneously beating heart assessed as change in coronary perfusion pressure	2009	Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8	L-Type calcium channel blockers: from diltiazem to 1,2,4-oxadiazol-5-ones via thiazinooxadiazol-3-one derivatives.
AID1394655	Half life in mouse serum by LC/MS analysis	2018	European journal of medicinal chemistry, Apr-25, Volume: 150	Inhibition of trypanosome alternative oxidase without its N-terminal mitochondrial targeting signal (ΔMTS-TAO) by cationic and non-cationic 4-hydroxybenzoate and 4-alkoxybenzaldehyde derivatives active against T. brucei and T. congolense.
AID589126	Mechanism based inhibition of human cytochrome P450 3A4 measured by midazolam hydroxylase activity	2005	Current drug metabolism, Oct, Volume: 6, Issue:5	Cytochrome p450 enzymes mechanism based inhibitors: common sub-structures and reactivity.
AID1307821	Vasorelaxant activity in potassium depolarized guinea pig aorta assessed as inhibition of calcium-induced contraction at 10'-4 M	2016	Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7	Understanding Oxadiazolothiazinone Biological Properties: Negative Inotropic Activity versus Cytochrome P450-Mediated Metabolism.
AID589127	Mechanism based inhibition of human cytochrome P450 3A4 measured by midazolam hydroxylase activity	2005	Current drug metabolism, Oct, Volume: 6, Issue:5	Cytochrome p450 enzymes mechanism based inhibitors: common sub-structures and reactivity.
AID19424	Partition coefficient (logD7.4)	2001	Journal of medicinal chemistry, Jul-19, Volume: 44, Issue:15	ElogD(oct): a tool for lipophilicity determination in drug discovery. 2. Basic and neutral compounds.
AID1211298	Dissociation constant, pKa of the compound	2011	Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3	Control and measurement of plasma pH in equilibrium dialysis: influence on drug plasma protein binding.
AID496827	Antimicrobial activity against Leishmania amazonensis	2010	Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6	Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID269332	Negative inotropic activity in guinea pig left atrium at 10 uM	2006	Journal of medicinal chemistry, Aug-24, Volume: 49, Issue:17	Calcium channel antagonists discovered by a multidisciplinary approach.
AID1079939	Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID170569	Preventive effect of compound was measured on vasopressin-induced ST depression rats at 10 mg/kg po dose after 1 hr of administration; +=Differ from control value	1991	Journal of medicinal chemistry, Mar, Volume: 34, Issue:3	A new class of calcium antagonists. 2. Synthesis and biological activity of 11-[[4-[4-(4-fluorophenyl)-1-piperazinyl]butyryl]amino]-6,11- dihydrodibenzo[b,e]-thiepin maleate and related compounds.
AID625290	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1079946	Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID751691	Displacement of [3H]Diltiazem from L-type calcium channel benzothiazepine binding site in Wistar rat brain after 3 hrs	2013	Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6	Cinnamides as selective small-molecule inhibitors of a cellular model of breast cancer stem cells.
AID1221964	Transporter substrate index ratio of permeability from basolateral to apical side in human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of P-gp inhibitor LY335979	2011	Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2	Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID699541	Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake at 20 uM incubated for 5 mins by scintillation counting	2012	Journal of medicinal chemistry, May-24, Volume: 55, Issue:10	Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
AID625292	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1209241	Drug metabolism in assessed as human CYP3A4-mediated intrinsic clearance per mg protein	2012	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12	Optimized experimental design for the estimation of enzyme kinetic parameters: an experimental evaluation.
AID1218817	Time dependent inhibition of CYP3A4 in human liver microsomes using midazolam as substrate preincubated for 30 mins followed by 10-fold dilution and substrate addition by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme.
AID80726	The compound was tested for the calcium antagonistic activity on K+-depolarized guinea pig aortic strips	1995	Journal of medicinal chemistry, Oct-27, Volume: 38, Issue:22	Pyrrolo[2,1-c][1,4]benzothiazines: synthesis, structure-activity relationships, molecular modeling studies, and cardiovascular activity.
AID1221959	Efflux ratio of permeability from apical to basolateral over basolateral to apical side of MDCK cells expressing MDR1	2011	Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2	Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID171865	Antihypertensive activity expressed as change in mean arterial blood pressure (MABP) in spontaneously hypertensive rats (SHR),at 0.5-2h after 30 mg/kg oral administration	1991	Journal of medicinal chemistry, Oct, Volume: 34, Issue:10	Synthesis, calcium-channel-blocking activity, and antihypertensive activity of 4-(diarylmethyl)-1-[3-(aryloxy)propyl]piperidines and structurally related compounds.
AID180514	In vitro inhibition of K+ induced contractions of the isolated rat aorta.	1998	Journal of medicinal chemistry, Oct-22, Volume: 41, Issue:22	Novel calcium antagonists with both calcium overload inhibition and antioxidant activity. 1. 2-(3, 5-di-tert-butyl-4-hydroxyphenyl)-3-(aminopropyl)thiazolidinones.
AID1079931	Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source]
AID28681	Partition coefficient (logD6.5)	2000	Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13	QSAR model for drug human oral bioavailability.
AID205267	Inhibition of binding of Batrachotoxinin [3H]BTX-B to high affinity sites on voltage dependent sodium channels in a vesicular preparation from guinea pig cerebral cortex	1985	Journal of medicinal chemistry, Mar, Volume: 28, Issue:3	[3H]Batrachotoxinin A 20 alpha-benzoate binding to voltage-sensitive sodium channels: a rapid and quantitative assay for local anesthetic activity in a variety of drugs.
AID444052	Hepatic clearance in human	2010	Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3	Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID625286	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID288185	Permeability coefficient through artificial membrane in presence of stirred water layer	2007	Bioorganic & medicinal chemistry, Jun-01, Volume: 15, Issue:11	QSAR study on permeability of hydrophobic compounds with artificial membranes.
AID425652	Total body clearance in human	2009	Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15	Physicochemical determinants of human renal clearance.
AID1529182	Protein binding in plasma (unknown origin)	2020	Journal of medicinal chemistry, 02-27, Volume: 63, Issue:4	Human Serum Albumin Binding in a Vial: A Novel UV-pH Titration Method To Assist Drug Design.
AID29925	Volume of distribution in man (IV dose)	2002	Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13	Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data.
AID196205	Compound was tested for [Ca2+] overload inhibitory activity in the veratridine-induced [Ca2+] overload model of rat cardiac myocytes.	1999	Journal of medicinal chemistry, Aug-12, Volume: 42, Issue:16	Novel calcium antagonists with both calcium overload inhibition and antioxidant activity. 2. Structure-activity relationships of thiazolidinone derivatives.
AID231902	Ratio between the EC30 values of atrial contractility and atrial rate	1990	Journal of medicinal chemistry, May, Volume: 33, Issue:5	Specific bradycardic agents. 1. Chemistry, pharmacology, and structure-activity relationships of substituted benzazepinones, a-new class of compounds exerting antiischemic properties.
AID1091957	Apparent permeability of the compound by PAMPA	2011	Journal of agricultural and food chemistry, Apr-13, Volume: 59, Issue:7	Importance of physicochemical properties for the design of new pesticides.
AID56042	In Vitro evaluation for the affinity for the diltiazem receptor in isolated guinea pig skeletal muscle microsomal preparations by inhibiting [3H]diltiazem binding	1992	Journal of medicinal chemistry, Feb-21, Volume: 35, Issue:4	Benzazepinone calcium channel blockers. 2. Structure-activity and drug metabolism studies leading to potent antihypertensive agents. Comparison with benzothiazepinones.
AID166960	in vitro inhibitory activity on soybean lipoxygenase-induced lipid peroxidations of rabbit low-density lipoprotein (LDL) at 0.5 uM dosage	1999	Journal of medicinal chemistry, Aug-12, Volume: 42, Issue:16	Novel calcium antagonists with both calcium overload inhibition and antioxidant activity. 2. Structure-activity relationships of thiazolidinone derivatives.
AID1218821	Time dependent inhibition of CYP3A4 in human liver microsomes using midazolam as substrate preincubated for 30 mins followed by 10-fold dilution and substrate addition by LC-MS/MS analysis in presence of NADPH	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme.
AID75923	Effective drug concentration (EC30) for negative chronotropic activity was determined; Range is from 0.064-0.075 (10e-6 M)	2002	Journal of medicinal chemistry, Aug-01, Volume: 45, Issue:16	Cardiovascular characterization of [1,4]thiazino[3,4-c][1,2,4]oxadiazol-1-one derivatives: selective myocardial calcium channel modulators.
AID29337	Ionisation constant (pKa)	2002	Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13	Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data.
AID1218848	Time dependent inhibition of CYP3A4 in human liver microsomes using testosterone as substrate preincubated for 30 mins followed by substrate addition by LC-MS/MS analysis in presence of NADPH	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme.
AID269359	Antagonist activity against calcium channel assessed as inhibition of calcium-induced contraction of potassium ion-depolarized guinea pig ileum longitudinal smooth muscle at 1 uM	2006	Journal of medicinal chemistry, Aug-24, Volume: 49, Issue:17	Calcium channel antagonists discovered by a multidisciplinary approach.
AID467398	Negative chronotropic activity in guinea pig right atrium assessed as decrease in atrial rate	2009	Journal of medicinal chemistry, Nov-12, Volume: 52, Issue:21	Stereoselective behavior of the functional diltiazem analogue 1-[(4-chlorophenyl)sulfonyl]-2-(2-thienyl)pyrrolidine, a new L-type calcium channel blocker.
AID168017	Preventive effect of compound was measured on vasopressin-induced ST depression rats at 30 mg/kg po dose after 7 hr of administration; -=No significance	1991	Journal of medicinal chemistry, Mar, Volume: 34, Issue:3	A new class of calcium antagonists. 2. Synthesis and biological activity of 11-[[4-[4-(4-fluorophenyl)-1-piperazinyl]butyryl]amino]-6,11- dihydrodibenzo[b,e]-thiepin maleate and related compounds.
AID95597	Calcium antagonistic activity by measuring [3H]nitrendipine displacement at L-type [Ca2+] channel in rat cortex homogenate	1995	Journal of medicinal chemistry, Oct-27, Volume: 38, Issue:22	Pyrrolo[2,1-c][1,4]benzothiazines: synthesis, structure-activity relationships, molecular modeling studies, and cardiovascular activity.
AID411034	Antiproliferative activity against human A2780 cells at 1.3 uM after 3 days by MTT assay	2009	Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2	Inhibition of MDR1 activity in vitro by a novel class of diltiazem analogues: toward new candidates.
AID1218846	Time dependent inhibition of CYP3A4 in human liver microsomes using testosterone as substrate preincubated for 90 mins followed by substrate addition by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme.
AID1079937	Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID588217	FDA HLAED, serum glutamic pyruvic transaminase (SGPT) increase	2004	Current drug discovery technologies, Dec, Volume: 1, Issue:4	Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID1221960	Apparent permeability from apical to basolateral side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of P-gp inhibitor LY335979	2011	Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2	Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID170563	Preventive effect of compound was measured on methacholine-induced ST elevation in anesthetized rats at 0.1 mg/kg iv dose with test compound (0-90 min)	1991	Journal of medicinal chemistry, Mar, Volume: 34, Issue:3	A new class of calcium antagonists. 2. Synthesis and biological activity of 11-[[4-[4-(4-fluorophenyl)-1-piperazinyl]butyryl]amino]-6,11- dihydrodibenzo[b,e]-thiepin maleate and related compounds.
AID167361	Inhibition of [Ca2+] uptake in rabbit aorta, K+.	1983	Journal of medicinal chemistry, Jun, Volume: 26, Issue:6	New developments in Ca2+ channel antagonists.
AID185881	Ability to lower blood pressure in the spontaneously hypertensive rat (SHR) at 30 mg/kg (p.o.)	1988	Journal of medicinal chemistry, Mar, Volume: 31, Issue:3	2-Ethynylbenzenealkanamines. A new class of calcium entry blockers.
AID1079932	Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID1474166	Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index	2016	Drug discovery today, Apr, Volume: 21, Issue:4	DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID288194	Intrinsic artificial membrane permeability coefficient, log P0 of the compound	2007	Bioorganic & medicinal chemistry, Jun-01, Volume: 15, Issue:11	QSAR study on permeability of hydrophobic compounds with artificial membranes.
AID427811	Antileishmanial activity against Leishmania donovani MHOH/IN/1983/AD83 promastigotes assessed as inhibition of oxygen consumption at 30 ug/mL after 2 hrs by polarographically with Clark electrode	2008	Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1	Oral Therapy with Amlodipine and Lacidipine, 1,4-Dihydropyridine Derivatives Showing Activity against Experimental Visceral Leishmaniasis.
AID1221958	Efflux ratio of permeability from apical to basolateral side over basolateral to apical side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis	2011	Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2	Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID588212	Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents	2010	Chemical research in toxicology, Jan, Volume: 23, Issue:1	Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID496819	Antimicrobial activity against Plasmodium falciparum	2010	Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6	Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID444053	Renal clearance in human	2010	Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3	Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID588218	FDA HLAED, lactate dehydrogenase (LDH) increase	2004	Current drug discovery technologies, Dec, Volume: 1, Issue:4	Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID467395	Negative inotropic activity in guinea pig left atrium assessed as decrease in atrial tension	2009	Journal of medicinal chemistry, Nov-12, Volume: 52, Issue:21	Stereoselective behavior of the functional diltiazem analogue 1-[(4-chlorophenyl)sulfonyl]-2-(2-thienyl)pyrrolidine, a new L-type calcium channel blocker.
AID540226	Clearance in monkey after iv administration	2006	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 34, Issue:7	Extrapolation of preclinical pharmacokinetics and molecular feature analysis of "discovery-like" molecules to predict human pharmacokinetics.
AID1197232	Selectivity ratio of IC50 for Cav1.2a in K+-depolarized guinea pig aortic strips to IC50 for Cav1.2b in K+-depolarized guinea pig ileum longitudinal smooth muscle	2015	European journal of medicinal chemistry, Mar-06, Volume: 92	Synthesis and L-type calcium channel blocking activity of new chiral oxadiazolothiazinones.
AID186230	Vasorelaxing activity expressed as maximum smooth muscle relaxation at 1*10e-4 M	2000	Bioorganic & medicinal chemistry letters, Aug-21, Volume: 10, Issue:16	Synthesis and preliminary biological evaluation of 4,6-disubstituted 3-cyanopyridin-2(1H)-ones, a new class of calcium entry blockers.
AID195195	Inhibitory effect of compound on calcium influx by high potassium in isolated rat aorta	1991	Journal of medicinal chemistry, Mar, Volume: 34, Issue:3	A new class of calcium antagonists. 2. Synthesis and biological activity of 11-[[4-[4-(4-fluorophenyl)-1-piperazinyl]butyryl]amino]-6,11- dihydrodibenzo[b,e]-thiepin maleate and related compounds.
AID681121	TP_TRANSPORTER: inhibition of Calcein-AM efflux in MDR1-expressing MDCKII cells	2001	The Journal of pharmacology and experimental therapeutics, Nov, Volume: 299, Issue:2	Rational use of in vitro P-glycoprotein assays in drug discovery.
AID1207640	Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes	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.
AID540211	Fraction unbound in human after iv administration	2008	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7	Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID625289	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID82355	K+ channel blocking activity in human embryonic kidney cells expressing HERG Kv11.1	2002	Journal of medicinal chemistry, Aug-29, Volume: 45, Issue:18	Toward a pharmacophore for drugs inducing the long QT syndrome: insights from a CoMFA study of HERG K(+) channel blockers.
AID415111	Displacement of [3H]diltiazem from L-type calcium channel in Sprague-Dawley rat cardiac myocytes by liquid scintillation counting	2009	Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8	L-Type calcium channel blockers: from diltiazem to 1,2,4-oxadiazol-5-ones via thiazinooxadiazol-3-one derivatives.
AID1079949	Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID167119	Electrophysiological effect in isolated rabbit hearts as molar concentration that prolongs the His bundle ventricular (H-V) conduction time by 10%	1988	Journal of medicinal chemistry, May, Volume: 31, Issue:5	Novel calcium antagonists. Synthesis and structure-activity relationship studies of benzothiazoline derivatives.
AID1197213	Negative ionotropic activity in guinea pig left atrium assessed as decrease in developed tension driven at 1 Hz	2015	European journal of medicinal chemistry, Mar-06, Volume: 92	Synthesis and L-type calcium channel blocking activity of new chiral oxadiazolothiazinones.
AID427804	Antileishmanial activity against Leishmania donovani MHOH/IN/1983/AD83 promastigotes assessed as viability after 2 hrs by MTT assay	2008	Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1	Oral Therapy with Amlodipine and Lacidipine, 1,4-Dihydropyridine Derivatives Showing Activity against Experimental Visceral Leishmaniasis.
AID1218825	Ratio of IC50 for CYP3A4 in human liver microsomes using midazolam as substrate preincubated for 30 mins followed by 10-fold dilution and substrate addition to IC50 for CYP3A4 in human liver microsomes using midazolam as substrate preincubated for 30 mins	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme.
AID1211293	Unbound fraction in plasma (unknown origin) under normal atmospheric condition at pH 7.22 after 6 hrs by equilibrium dialysis method	2011	Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3	Control and measurement of plasma pH in equilibrium dialysis: influence on drug plasma protein binding.
AID496826	Antimicrobial activity against Entamoeba histolytica	2010	Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6	Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID415113	Negative inotropic activity in guinea pig left atrium assessed as decrease in atrial tension at 10 uM relative to control	2009	Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8	L-Type calcium channel blockers: from diltiazem to 1,2,4-oxadiazol-5-ones via thiazinooxadiazol-3-one derivatives.
AID1209247	Drug metabolism in human liver microsomes assessed as intrinsic clearance per mg protein by multiple depletion curves method	2012	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12	Optimized experimental design for the estimation of enzyme kinetic parameters: an experimental evaluation.
AID88416	In Vitro evaluation on percentage inhibition in Heme Oxygenase at concentration 50(uM) of infected host	2000	Journal of medicinal chemistry, Sep-07, Volume: 43, Issue:18	A new class of potential chloroquine-resistance reversal agents for Plasmodia: syntheses and biological evaluation of 1-(3'-diethylaminopropyl)-3-(substituted phenylmethylene)pyrrolidines.
AID625288	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID496823	Antimicrobial activity against Trichomonas vaginalis	2010	Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6	Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID444056	Fraction escaping gut-wall elimination in human	2010	Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3	Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID170567	Preventive effect of compound was measured on methacholine-induced ST elevation in anesthetized rats at 1 mg/kg iv dose with test compound (0-90 min)	1991	Journal of medicinal chemistry, Mar, Volume: 34, Issue:3	A new class of calcium antagonists. 2. Synthesis and biological activity of 11-[[4-[4-(4-fluorophenyl)-1-piperazinyl]butyryl]amino]-6,11- dihydrodibenzo[b,e]-thiepin maleate and related compounds.
AID78242	Negative inotropic activity in isolated guinea pig left atrium.	2002	Journal of medicinal chemistry, Aug-01, Volume: 45, Issue:16	Cardiovascular characterization of [1,4]thiazino[3,4-c][1,2,4]oxadiazol-1-one derivatives: selective myocardial calcium channel modulators.
AID1211297	Drug recovery in plasma (unknown origin)	2011	Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3	Control and measurement of plasma pH in equilibrium dialysis: influence on drug plasma protein binding.
AID269353	Cardiac activity in guinea pig heart measured as decrease in left ventricular pressure at 1 uM relative to control	2006	Journal of medicinal chemistry, Aug-24, Volume: 49, Issue:17	Calcium channel antagonists discovered by a multidisciplinary approach.
AID269348	Negative inotropic activity in guinea pig left ventricular papillary muscle at 10 uM	2006	Journal of medicinal chemistry, Aug-24, Volume: 49, Issue:17	Calcium channel antagonists discovered by a multidisciplinary approach.
AID180510	Tested in vitro on K+ -depolarized rat aorta strips to evaluate its ability to relax the initial contraction induced by K	2000	Bioorganic & medicinal chemistry letters, Aug-21, Volume: 10, Issue:16	Synthesis and preliminary biological evaluation of 4,6-disubstituted 3-cyanopyridin-2(1H)-ones, a new class of calcium entry blockers.
AID1197214	Negative chronotropic activity in guinea pig left atrium assessed as decrease in atrial rate on spontaneous beating at 10'-6 M relative to control	2015	European journal of medicinal chemistry, Mar-06, Volume: 92	Synthesis and L-type calcium channel blocking activity of new chiral oxadiazolothiazinones.
AID269344	Vasorelaxant activity assessed as inhibition of calcium-induced contraction of potassium ion-depolarized guinea pig aortic strips at 100 uM	2006	Journal of medicinal chemistry, Aug-24, Volume: 49, Issue:17	Calcium channel antagonists discovered by a multidisciplinary approach.
AID1209242	Drug metabolism in assessed as human CYP3A4-mediated maximum rate of reaction per mg protein	2012	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12	Optimized experimental design for the estimation of enzyme kinetic parameters: an experimental evaluation.
AID170568	Preventive effect of compound was measured on methacholine-induced ST elevation in anesthetized rats at 1 mg/kg iv dose without test compound	1991	Journal of medicinal chemistry, Mar, Volume: 34, Issue:3	A new class of calcium antagonists. 2. Synthesis and biological activity of 11-[[4-[4-(4-fluorophenyl)-1-piperazinyl]butyryl]amino]-6,11- dihydrodibenzo[b,e]-thiepin maleate and related compounds.
AID411052	Reversal of P-gp 170-mediated multidrug resistance in human A2780/DX3 cells assessed as reduction in doxorubicin IC50 at IC0 pretreated for 6 hrs before doxorubicin administration measured after 3 days by MTT assay	2009	Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2	Inhibition of MDR1 activity in vitro by a novel class of diltiazem analogues: toward new candidates.
AID674363	Inhibition of human voltage-dependent L-type calcium channel subunit alpha1C/alpha2delta/beta2a expressed in C1-6-37-3 cells assessed as inhibition of K+-induced calcium influx incubated for 30 mins prior to K+-induction by Fluo-4-AM based FLIPR assay	2012	Journal of natural products, Jun-22, Volume: 75, Issue:6	Isolation and structural elucidation of cyclic tetrapeptides from Onychocola sclerotica.
AID1823668	Stability in human plasma assessed as parent compound remaining at 10 uM measured after 120 mins by LC-MS analysis	2021	Journal of medicinal chemistry, 05-27, Volume: 64, Issue:10	Discovery of New Imidazo[2,1-
AID251141	Negative inotropic activity as decrease in the developed tension in isolated guinea pig left artium at 10E-5 M (n=4-6)	2005	Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7	A new class of selective myocardial calcium channel modulators. 2. Role of the acetal chain in oxadiazol-3-one derivatives.
AID95605	Inhibition of [3H]nitrendipine binding to L-type [Ca2+] channel in rat cortex homogenate, activity expressed as pIC50	1997	Journal of medicinal chemistry, Jan-03, Volume: 40, Issue:1	Diltiazem-like calcium entry blockers: a hypothesis of the receptor-binding site based on a comparative molecular field analysis model.
AID1215348	Time dependent inhibition of CYP3A4 in human liver microsomes assessed as conversion of testosterone to 6beta-hydroxytestosterone at 0.01 to 100 uM preincubated for 60 mins followed by testosterone treatment measured after 10 mins by LC-MS/MS analysis	2011	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 39, Issue:6	A refined cytochrome P540 IC₅₀ shift assay for reliably identifying CYP3A time-dependent inhibitors.
AID540224	Clearance in dog after iv administration	2006	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 34, Issue:7	Extrapolation of preclinical pharmacokinetics and molecular feature analysis of "discovery-like" molecules to predict human pharmacokinetics.
AID112426	Effect on acute thrombic death induced by collagen in mice	1988	Journal of medicinal chemistry, May, Volume: 31, Issue:5	Novel calcium antagonists. Synthesis and structure-activity relationship studies of benzothiazoline derivatives.
AID540225	Volume of distribution at steady state in dog after iv administration	2006	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 34, Issue:7	Extrapolation of preclinical pharmacokinetics and molecular feature analysis of "discovery-like" molecules to predict human pharmacokinetics.
AID1207641	Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes	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.
AID310122	Inhibition of P-glycoprotein by Hoechst assay	2007	Bioorganic & medicinal chemistry, Dec-01, Volume: 15, Issue:23	New functional assay of P-glycoprotein activity using Hoechst 33342.
AID167822	In vitro evaluation for the vasorelaxant effects in circumferential strips of potassium-depolarized rabbit aorta. (IC50 in rabbit aorta strips contracted with KCl)	1992	Journal of medicinal chemistry, Feb-21, Volume: 35, Issue:4	Benzazepinone calcium channel blockers. 3. Synthesis and structure-activity studies of 3-alkylbenzazepinones.
AID415123	Vasorelaxant activity in potassium-depolarized guinea pig thoracic aorta assessed as inhibition of calcium-induced contraction at 100 uM	2009	Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8	L-Type calcium channel blockers: from diltiazem to 1,2,4-oxadiazol-5-ones via thiazinooxadiazol-3-one derivatives.
AID1209251	Drug metabolism in human liver microsomes by optimal design approach	2012	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12	Optimized experimental design for the estimation of enzyme kinetic parameters: an experimental evaluation.
AID175821	Diuretic effect was evaluated in the conscious female rat by natriuretic assay involving metabolic caging at dose 10 mg/kg	1996	Journal of medicinal chemistry, Mar-15, Volume: 39, Issue:6	Endogenous natriuretic factors. 5. Synthesis and biological activity of a natriuretic metabolite of diltiazem and its derivatives.
AID310121	Inhibition of P-glycoprotein expressed in MDCK-MDR1 cells by calcein AM assay	2007	Bioorganic & medicinal chemistry, Dec-01, Volume: 15, Issue:23	New functional assay of P-glycoprotein activity using Hoechst 33342.
AID222725	Percent decrease of negative chronotropic activity on isolated guinea pig spontaneously beating right atrium at 1*10e-6 M	1996	Journal of medicinal chemistry, Jul-19, Volume: 39, Issue:15	Cardiovascular characterization of pyrrolo[2,1-d][1,5]benzothiazepine derivatives binding selectively to the peripheral-type benzodiazepine receptor (PBR): from dual PBR affinity and calcium antagonist activity to novel and selective calcium entry blocker
AID1218822	Time dependent inhibition of CYP3A4 in human liver microsomes using testosterone as substrate preincubated for 30 mins followed by 10-fold dilution and substrate addition by LC-MS/MS analysis in presence of NADPH	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme.
AID1079944	Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID699540	Inhibition of human liver OATP1B3 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E17-betaG uptake at 20 uM incubated for 5 mins by scintillation counting	2012	Journal of medicinal chemistry, May-24, Volume: 55, Issue:10	Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
AID167568	Calcium channel-blocking activity by determined by ability to antagonize calcium-induced contractions of isolated rabbit aortic strips	1991	Journal of medicinal chemistry, Oct, Volume: 34, Issue:10	Synthesis, calcium-channel-blocking activity, and antihypertensive activity of 4-(diarylmethyl)-1-[3-(aryloxy)propyl]piperidines and structurally related compounds.
AID588214	FDA HLAED, liver enzyme composite activity	2004	Current drug discovery technologies, Dec, Volume: 1, Issue:4	Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID415104	Effect on cardiac activity in guinea pig spontaneously beating heart assessed as change in heart rate at 1 uM relative to control	2009	Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8	L-Type calcium channel blockers: from diltiazem to 1,2,4-oxadiazol-5-ones via thiazinooxadiazol-3-one derivatives.
AID427814	Antileishmanial activity against Leishmania donovani MHOH/IN/1983/AD83 promastigotes assessed as inhibition of calcium uptake	2008	Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1	Oral Therapy with Amlodipine and Lacidipine, 1,4-Dihydropyridine Derivatives Showing Activity against Experimental Visceral Leishmaniasis.
AID588219	FDA HLAED, gamma-glutamyl transferase (GGT) increase	2004	Current drug discovery technologies, Dec, Volume: 1, Issue:4	Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID420669	Lipophilicity, log D at pH 7.0	2009	European journal of medicinal chemistry, May, Volume: 44, Issue:5	GRIND-based 3D-QSAR and CoMFA to investigate topics dominated by hydrophobic interactions: the case of hERG K+ channel blockers.
AID497005	Antimicrobial activity against Pneumocystis carinii	2010	Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6	Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID415121	Negative chronotropic activity in guinea pig spontaneously beating right atrium assessed as decrease in atrial rate at 1 uM relative to control	2009	Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8	L-Type calcium channel blockers: from diltiazem to 1,2,4-oxadiazol-5-ones via thiazinooxadiazol-3-one derivatives.
AID1307831	Negative chronotropic activity in potassium depolarized guinea pig right atrium assessed as reduction in atrial rate at 10'-6 M after 30 mins	2016	Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7	Understanding Oxadiazolothiazinone Biological Properties: Negative Inotropic Activity versus Cytochrome P450-Mediated Metabolism.
AID310120	Inhibition of P-glycoprotein expressed in A2780/ADR cells by calcein AM assay	2007	Bioorganic & medicinal chemistry, Dec-01, Volume: 15, Issue:23	New functional assay of P-glycoprotein activity using Hoechst 33342.
AID80745	Evaluated in vitro for its effect on spontaneous atrial contractility in isolated guinea pig atria	1990	Journal of medicinal chemistry, May, Volume: 33, Issue:5	Specific bradycardic agents. 1. Chemistry, pharmacology, and structure-activity relationships of substituted benzazepinones, a-new class of compounds exerting antiischemic properties.
AID1218818	Time dependent inhibition of CYP3A4 in human liver microsomes using testosterone as substrate preincubated for 30 mins followed by 10-fold dilution and substrate addition by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme.
AID625280	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID395103	Inhibition of P-glycoprotein-mediated multidrug resistance in adriamycin-resistant human A2780/ADR cells by calcein AM assay	2009	Bioorganic & medicinal chemistry, Mar-15, Volume: 17, Issue:6	Synthesis and biological evaluation of a small molecule library of 3rd generation multidrug resistance modulators.
AID1207642	Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in human embryonic kidney cells 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.
AID1222759	Unbound hepatobiliary clearance in human at 120 mg, po	2013	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 41, Issue:5	Which metabolites circulate?
AID1079943	Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID145966	The compound was tested for inhibition of calcium influx into neuronal (NG108-15) cells.	1991	Journal of medicinal chemistry, May, Volume: 34, Issue:5	Aminoalkynyldithianes. A new class of calcium channel blockers.
AID1207213	Inhibition of hERG K channel	2011	Cardiovascular research, Jul-01, Volume: 91, Issue:1	Simulation of multiple ion channel block provides improved early prediction of compounds' clinical torsadogenic risk.
AID29423	HPLC capacity factor (k')	2002	Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13	Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data.
AID173502	In vivo evaluation for the percentage decrease in blood pressure at 135 umol/kg administered through oral route in spontaneously hypertensive rats and observed for 6-12 h	1992	Journal of medicinal chemistry, Feb-21, Volume: 35, Issue:4	Benzazepinone calcium channel blockers. 3. Synthesis and structure-activity studies of 3-alkylbenzazepinones.
AID224185	Evaluated in vitro for the effect on K+ induced aortic contraction in isolated aortic strips of rabbit	1990	Journal of medicinal chemistry, May, Volume: 33, Issue:5	Specific bradycardic agents. 1. Chemistry, pharmacology, and structure-activity relationships of substituted benzazepinones, a-new class of compounds exerting antiischemic properties.
AID45630	Inhibition of [3H]nitrendipine binding to calcium channels in rabbit cardiac muscle	1988	Journal of medicinal chemistry, Nov, Volume: 31, Issue:11	Synthesis of (aryloxy)alkylamines. 2. Novel imidazo-fused heterocycles with calcium channel blocking and local anesthetic activity.
AID269357	Cardiac activity in guinea pig heart measured as prolongation of atrioventricular conduction time at 1 uM relative to control	2006	Journal of medicinal chemistry, Aug-24, Volume: 49, Issue:17	Calcium channel antagonists discovered by a multidisciplinary approach.
AID411067	Antiproliferative activity against human A2780/DX3 cells at 2.2 uM after 3 days by MTT assay	2009	Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2	Inhibition of MDR1 activity in vitro by a novel class of diltiazem analogues: toward new candidates.
AID678713	Inhibition of human CYP2C9 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 7-methoxy-4-trifluoromethylcoumarin-3-acetic acid as substrate after 30 mins	2012	Chemical research in toxicology, Oct-15, Volume: 25, Issue:10	Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID55903	Effect on coronary blood flow (CBF) by intravenous administration of compound in anesthetized dogs.	1999	Journal of medicinal chemistry, Aug-12, Volume: 42, Issue:16	Novel calcium antagonists with both calcium overload inhibition and antioxidant activity. 2. Structure-activity relationships of thiazolidinone derivatives.
AID1307844	Relaxant activity in potassium depolarized guinea pig ileum longitudinal smooth muscle assessed as inhibition of calcium-induced contraction after 30 mins	2016	Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7	Understanding Oxadiazolothiazinone Biological Properties: Negative Inotropic Activity versus Cytochrome P450-Mediated Metabolism.
AID624623	Apparent permeability (Papp) from basolateral to apical side determined in MDR1-MDCKII cells	2001	The Journal of pharmacology and experimental therapeutics, Nov, Volume: 299, Issue:2	Rational use of in vitro P-glycoprotein assays in drug discovery.
AID1517044	Stability in rat plasma assessed as remaining compound at 10 uM incubated for 30 mins by LC-MS analysis
AID1091955	Dissociation constant, pKa of the compound at pH 7.3	2011	Journal of agricultural and food chemistry, Apr-13, Volume: 59, Issue:7	Importance of physicochemical properties for the design of new pesticides.
AID1307797	Negative inotropic activity in potassium depolarized guinea pig left atrium assessed as reduction in developed tension	2016	Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7	Understanding Oxadiazolothiazinone Biological Properties: Negative Inotropic Activity versus Cytochrome P450-Mediated Metabolism.
AID1221956	Apparent permeability from apical to basolateral side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis	2011	Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2	Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID78315	In vitro molar concentration required to block [Ca2+] -induced contraction of K+-depolarized taenia cecum of guinea pigs	1988	Journal of medicinal chemistry, May, Volume: 31, Issue:5	Novel calcium antagonists. Synthesis and structure-activity relationship studies of benzothiazoline derivatives.
AID173500	In vivo evaluation for the percentage decrease in blood pressure at 135 umol/kg administered through oral route in spontaneously hypertensive rats and observed for 12-18 h	1992	Journal of medicinal chemistry, Feb-21, Volume: 35, Issue:4	Benzazepinone calcium channel blockers. 3. Synthesis and structure-activity studies of 3-alkylbenzazepinones.
AID252261	Selectivity ratio against negative inotropic potency on left atrium to that of negative inotropic potency on left ventricular papillary muscle in guinea pig	2005	Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7	A new class of selective myocardial calcium channel modulators. 2. Role of the acetal chain in oxadiazol-3-one derivatives.
AID186984	Kaliuretic effect was evaluated in the conscious female rat by natriuretic assay involving metabolic caging at dose 10 mg/kg	1996	Journal of medicinal chemistry, Mar-15, Volume: 39, Issue:6	Endogenous natriuretic factors. 5. Synthesis and biological activity of a natriuretic metabolite of diltiazem and its derivatives.
AID404304	Effect on human MRP2-mediated estradiol-17-beta-glucuronide transport in Sf9 cells inverted membrane vesicles relative to control	2008	Journal of medicinal chemistry, Jun-12, Volume: 51, Issue:11	Prediction and identification of drug interactions with the human ATP-binding cassette transporter multidrug-resistance associated protein 2 (MRP2; ABCC2).
AID411053	Reversal of P-gp 170-mediated multidrug resistance in human A2780/DX3 cells assessed as increase in intracellular doxorubicin accumulation at 5 times IC5 pretreated for 2 hrs before doxorubicin administration measured after 2 hrs by flow cytometry	2009	Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2	Inhibition of MDR1 activity in vitro by a novel class of diltiazem analogues: toward new candidates.
AID243188	Inhibition of human voltage-gated potassium channel subunit Kv11.1 (ERG K+ channel) in open state	2005	Bioorganic & medicinal chemistry letters, Mar-15, Volume: 15, Issue:6	A two-state homology model of the hERG K+ channel: application to ligand binding.
AID1849438	Stability in rat plasma assessed as compound remaining and measured after 120 mins by LC-MS/MS analysis
AID168014	Preventive effect of compound was measured on vasopressin-induced ST depression rats at 30 mg/kg po dose after 1 hr of administration; +=Differ from control value	1991	Journal of medicinal chemistry, Mar, Volume: 34, Issue:3	A new class of calcium antagonists. 2. Synthesis and biological activity of 11-[[4-[4-(4-fluorophenyl)-1-piperazinyl]butyryl]amino]-6,11- dihydrodibenzo[b,e]-thiepin maleate and related compounds.
AID363994	Negative chronotropic activity in guinea pig spontaneously beating right atrium assessed as decrease in atrial rate at 5 uM relative to control	2008	Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18	Discovery of novel and cardioselective diltiazem-like calcium channel blockers via virtual screening.
AID45635	Calcium channel blocking activity in rabbit	1987	Journal of medicinal chemistry, Apr, Volume: 30, Issue:4	Synthesis and biological activity of novel calcium channel blockers: 2,5-dihydro-4-methyl-2-phenyl-1,5-benzothiazepine-3-carboxylic acid esters and 2,5-dihydro-4-methyl-2-phenyl-1,5-benzodiazepine-3-carboxylic acid esters.
AID699539	Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake at 20 uM by scintillation counting	2012	Journal of medicinal chemistry, May-24, Volume: 55, Issue:10	Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
AID444055	Fraction absorbed in human	2010	Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3	Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID166961	in vitro inhibitory activity on soybean lipoxygenase-induced lipid peroxidations of rabbit low-density lipoprotein (LDL) at 5 uM dosage.	1999	Journal of medicinal chemistry, Aug-12, Volume: 42, Issue:16	Novel calcium antagonists with both calcium overload inhibition and antioxidant activity. 2. Structure-activity relationships of thiazolidinone derivatives.
AID288192	Partition coefficient, log P of the compound	2007	Bioorganic & medicinal chemistry, Jun-01, Volume: 15, Issue:11	QSAR study on permeability of hydrophobic compounds with artificial membranes.
AID165790	Inhibition of [Ca2+] influx in response to a stimulus of KCL (60 uM)	1988	Journal of medicinal chemistry, Mar, Volume: 31, Issue:3	2-Ethynylbenzenealkanamines. A new class of calcium entry blockers.
AID467392	Negative inotropic activity in guinea pig left atrium assessed as decrease in atrial tension at 10 uM relative to control	2009	Journal of medicinal chemistry, Nov-12, Volume: 52, Issue:21	Stereoselective behavior of the functional diltiazem analogue 1-[(4-chlorophenyl)sulfonyl]-2-(2-thienyl)pyrrolidine, a new L-type calcium channel blocker.
AID269352	Negative inotropic activity in guinea pig left ventricular papillary muscle	2006	Journal of medicinal chemistry, Aug-24, Volume: 49, Issue:17	Calcium channel antagonists discovered by a multidisciplinary approach.
AID195587	In vitro inhibition of veratridine induced rat myocardiac cell death.	1998	Journal of medicinal chemistry, Oct-22, Volume: 41, Issue:22	Novel calcium antagonists with both calcium overload inhibition and antioxidant activity. 1. 2-(3, 5-di-tert-butyl-4-hydroxyphenyl)-3-(aminopropyl)thiazolidinones.
AID1211296	Unbound fraction in plasma (unknown origin) under normal atmospheric condition at pH 7.72 after 6 hrs by equilibrium dialysis method	2011	Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3	Control and measurement of plasma pH in equilibrium dialysis: influence on drug plasma protein binding.
AID288193	Flux ionization constant, pKa of the membrane permeability coefficient of the compound	2007	Bioorganic & medicinal chemistry, Jun-01, Volume: 15, Issue:11	QSAR study on permeability of hydrophobic compounds with artificial membranes.
AID80731	Activity of [Ca2+] antagonistic potency on K+ depolarized guinea pig aortic strips.	1996	Journal of medicinal chemistry, Jul-19, Volume: 39, Issue:15	Cardiovascular characterization of pyrrolo[2,1-d][1,5]benzothiazepine derivatives binding selectively to the peripheral-type benzodiazepine receptor (PBR): from dual PBR affinity and calcium antagonist activity to novel and selective calcium entry blocker
AID411049	Antiproliferative activity against human A2780/DX3 cells after 3 days by MTT assay	2009	Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2	Inhibition of MDR1 activity in vitro by a novel class of diltiazem analogues: toward new candidates.
AID1307838	Vasorelaxant activity in potassium depolarized guinea pig aorta assessed as inhibition of calcium-induced contraction after 30 mins	2016	Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7	Understanding Oxadiazolothiazinone Biological Properties: Negative Inotropic Activity versus Cytochrome P450-Mediated Metabolism.
AID80725	Inhibitory concentration required to block Ca+2 induced contraction of K+ depolarized guinea pig aorta	1990	Journal of medicinal chemistry, Jul, Volume: 33, Issue:7	Synthesis and Ca2+ antagonistic activity of 2-[2-[(aminoalkyl)oxy]-5-methoxyphenyl]-3,4-dihydro-4-methyl-3-oxo-2H- 1,4-benzothiazines.
AID373867	Hepatic clearance in human hepatocytes in absence of fetal calf serum	2009	European journal of medicinal chemistry, Apr, Volume: 44, Issue:4	First-principle, structure-based prediction of hepatic metabolic clearance values in human.
AID751756	Displacement of [3H]Diltiazem from L-type calcium channel benzothiazepine binding site in Wistar rat brain at 10 uM after 3 hrs relative to control	2013	Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6	Cinnamides as selective small-molecule inhibitors of a cellular model of breast cancer stem cells.
AID165670	In vitro inhibition of development of isometric tension, in response to KCl (60 uM) in rabbit aorta	1988	Journal of medicinal chemistry, Mar, Volume: 31, Issue:3	2-Ethynylbenzenealkanamines. A new class of calcium entry blockers.
AID467403	Vasorelaxant activity in 80 mM K+-depolarized guinea pig thoracic aortic strip assessed as inhibition of calcium-induced contraction	2009	Journal of medicinal chemistry, Nov-12, Volume: 52, Issue:21	Stereoselective behavior of the functional diltiazem analogue 1-[(4-chlorophenyl)sulfonyl]-2-(2-thienyl)pyrrolidine, a new L-type calcium channel blocker.
AID415122	Negative chronotropic activity in guinea pig spontaneously beating right atrium assessed as decrease in atrial rate	2009	Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8	L-Type calcium channel blockers: from diltiazem to 1,2,4-oxadiazol-5-ones via thiazinooxadiazol-3-one derivatives.
AID588211	Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans	2010	Chemical research in toxicology, Jan, Volume: 23, Issue:1	Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID408340	Inhibition of human ERG expressed in CHO cells by whole cell patch clamp technique	2008	Bioorganic & medicinal chemistry, Jun-01, Volume: 16, Issue:11	Support vector machines classification of hERG liabilities based on atom types.
AID1307806	Negative inotropic activity in potassium depolarized guinea pig left atrium assessed as reduction in developed tension at 10'-5 M	2016	Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7	Understanding Oxadiazolothiazinone Biological Properties: Negative Inotropic Activity versus Cytochrome P450-Mediated Metabolism.
AID1215347	Time dependent inhibition of CYP3A4 in human liver microsomes assessed as conversion of testosterone to 6beta-hydroxytestosterone at 0.01 to 100 uM preincubated for 60 mins followed by testosterone treatment measured after 10 mins by LC-MS/MS analysis in	2011	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 39, Issue:6	A refined cytochrome P540 IC₅₀ shift assay for reliably identifying CYP3A time-dependent inhibitors.
AID1079938	Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source]
AID288184	Permeability coefficient through artificial membrane in presence of unstirred water layer by PAMPA	2007	Bioorganic & medicinal chemistry, Jun-01, Volume: 15, Issue:11	QSAR study on permeability of hydrophobic compounds with artificial membranes.
AID1307836	Vasorelaxant activity in potassium depolarized guinea pig aorta assessed as inhibition of calcium-induced contraction at 10'-4 M after 30 mins	2016	Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7	Understanding Oxadiazolothiazinone Biological Properties: Negative Inotropic Activity versus Cytochrome P450-Mediated Metabolism.
AID45792	Ability to inhibit [3H]nitrendipine binding to the calcium channel receptor(CCR) in rat cerebral cortex homogenate.	1996	Journal of medicinal chemistry, Jul-19, Volume: 39, Issue:15	Cardiovascular characterization of pyrrolo[2,1-d][1,5]benzothiazepine derivatives binding selectively to the peripheral-type benzodiazepine receptor (PBR): from dual PBR affinity and calcium antagonist activity to novel and selective calcium entry blocker
AID1218849	Time dependent inhibition of CYP3A4 in human liver microsomes using midazolam as substrate preincubated for 90 mins followed by substrate addition by LC-MS/MS analysis in presence of NADPH	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme.
AID246447	Negative inotropic potency as decrease in the developed tension in isolated guinea pig left artium	2005	Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7	A new class of selective myocardial calcium channel modulators. 2. Role of the acetal chain in oxadiazol-3-one derivatives.
AID194016	Hypotensive activity in SHR (spontaneously hypertensive rats) expressed as change in blood pressure(mmHg) after 4 hr dosing at a concentration of 30 mg/kg	1991	Journal of medicinal chemistry, Feb, Volume: 34, Issue:2	Synthesis of halogen-substituted 1,5-benzothiazepine derivatives and their vasodilating and hypotensive activities.
AID78241	Negative chronotropic activity in isolated guinea pig right atrium.	2002	Journal of medicinal chemistry, Aug-01, Volume: 45, Issue:16	Cardiovascular characterization of [1,4]thiazino[3,4-c][1,2,4]oxadiazol-1-one derivatives: selective myocardial calcium channel modulators.
AID411056	Down regulation of P-gp 170 expression in human A2780/DX3 cells after 72 hrs by flow cytometry	2009	Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2	Inhibition of MDR1 activity in vitro by a novel class of diltiazem analogues: toward new candidates.
AID227701	Anticonvulsant activity; NC denotes that compound is not classified	2003	Bioorganic & medicinal chemistry letters, Aug-18, Volume: 13, Issue:16	Topological virtual screening: a way to find new anticonvulsant drugs from chemical diversity.
AID540229	Volume of distribution at steady state in human after iv administration	2006	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 34, Issue:7	Extrapolation of preclinical pharmacokinetics and molecular feature analysis of "discovery-like" molecules to predict human pharmacokinetics.
AID1222760	Systemic clearance in human at 120 mg, po	2013	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 41, Issue:5	Which metabolites circulate?
AID269364	Antagonist activity against calcium channel assessed as inhibition of carbachol-induced tonic contraction of guinea pig ileum longitudinal smooth muscle	2006	Journal of medicinal chemistry, Aug-24, Volume: 49, Issue:17	Calcium channel antagonists discovered by a multidisciplinary approach.
AID167264	Electrophysiological effect in isolated rabbit hearts as molar concentration that prolongs the atrio-His bundle (A-H) conduction time by 30%	1988	Journal of medicinal chemistry, May, Volume: 31, Issue:5	Novel calcium antagonists. Synthesis and structure-activity relationship studies of benzothiazoline derivatives.
AID80317	Inhibitory concentration required to suppress the rate of contraction of guinea pig right atria	1990	Journal of medicinal chemistry, Jul, Volume: 33, Issue:7	Synthesis and Ca2+ antagonistic activity of 2-[2-[(aminoalkyl)oxy]-5-methoxyphenyl]-3,4-dihydro-4-methyl-3-oxo-2H- 1,4-benzothiazines.
AID625281	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID588213	Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in non-rodents	2010	Chemical research in toxicology, Jan, Volume: 23, Issue:1	Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID1091956	Apparent hydrophobicity, log D of the compound in Octanol-buffer	2011	Journal of agricultural and food chemistry, Apr-13, Volume: 59, Issue:7	Importance of physicochemical properties for the design of new pesticides.
AID95603	Calcium antagonistic activity by measuring [3H]nitrendipine displacement from rat heart L-type [Ca2+] channel	1995	Journal of medicinal chemistry, Oct-27, Volume: 38, Issue:22	Pyrrolo[2,1-c][1,4]benzothiazines: synthesis, structure-activity relationships, molecular modeling studies, and cardiovascular activity.
AID1473741	Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay	2013	Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1	A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1218847	Time dependent inhibition of CYP3A4 in human liver microsomes using midazolam as substrate preincubated for 30 mins followed by substrate addition by LC-MS/MS analysis in presence of NADPH	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme.
AID1211294	Unbound fraction in plasma (unknown origin) at pH 7.4 after 6 hrs by equilibrium dialysis method in presence of 5% CO2	2011	Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3	Control and measurement of plasma pH in equilibrium dialysis: influence on drug plasma protein binding.
AID420668	Inhibition of human ERG in MCF7 cells	2009	European journal of medicinal chemistry, May, Volume: 44, Issue:5	GRIND-based 3D-QSAR and CoMFA to investigate topics dominated by hydrophobic interactions: the case of hERG K+ channel blockers.
AID21849	In vitro clearance in dog in 1000000 cells	1999	Journal of medicinal chemistry, Dec-16, Volume: 42, Issue:25	Combining in vitro and in vivo pharmacokinetic data for prediction of hepatic drug clearance in humans by artificial neural networks and multivariate statistical techniques.
AID76345	Percent inhibition of calcium-induced contraction on K+-depolarized guinea-pig aortic strip at 5 x 10 e-5M	2002	Journal of medicinal chemistry, Aug-01, Volume: 45, Issue:16	Cardiovascular characterization of [1,4]thiazino[3,4-c][1,2,4]oxadiazol-1-one derivatives: selective myocardial calcium channel modulators.
AID444050	Fraction unbound in human plasma	2010	Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3	Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1307830	Negative inotropic activity in potassium depolarized guinea pig left atrium assessed as reduction in developed tension after 30 mins	2016	Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7	Understanding Oxadiazolothiazinone Biological Properties: Negative Inotropic Activity versus Cytochrome P450-Mediated Metabolism.
AID170566	Preventive effect of compound was measured on methacholine-induced ST elevation in anesthetized rats at 0.3 mg/kg iv dose without test compound	1991	Journal of medicinal chemistry, Mar, Volume: 34, Issue:3	A new class of calcium antagonists. 2. Synthesis and biological activity of 11-[[4-[4-(4-fluorophenyl)-1-piperazinyl]butyryl]amino]-6,11- dihydrodibenzo[b,e]-thiepin maleate and related compounds.
AID222116	Activity of chronotropic negative potency on guinea pig spontaneously beating right atrium.	1996	Journal of medicinal chemistry, Jul-19, Volume: 39, Issue:15	Cardiovascular characterization of pyrrolo[2,1-d][1,5]benzothiazepine derivatives binding selectively to the peripheral-type benzodiazepine receptor (PBR): from dual PBR affinity and calcium antagonist activity to novel and selective calcium entry blocker
AID1443980	Inhibition of human BSEP expressed in fall armyworm sf9 cell plasma membrane vesicles assessed as reduction in vesicle-associated [3H]-taurocholate transport preincubated for 10 mins prior to ATP addition measured after 15 mins in presence of [3H]-tauroch	2010	Toxicological sciences : an official journal of the Society of Toxicology, Dec, Volume: 118, Issue:2	Interference with bile salt export pump function is a susceptibility factor for human liver injury in drug development.
AID28236	Unbound fraction (tissues)	2002	Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13	Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data.
AID227625	Calcium antagonistic activity assessed against calcium-induced constriction of potassium-depolarized rat aorta.	1991	Journal of medicinal chemistry, Feb, Volume: 34, Issue:2	A new class of calcium antagonists. Synthesis and biological activity of 11-[(omega-aminoalkanoyl)amino]-6,6a,7,8,9,10,10a,11-octahydrodibenzo [b,e]thiepin derivatives.
AID1221962	Efflux ratio of permeability from apical to basolateral side over basolateral to apical side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of P-gp inhibitor LY335979	2011	Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2	Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID231461	Ratio between EC10 and EC30 in isolated rabbit hearts in His bundle ventricular intervals	1988	Journal of medicinal chemistry, May, Volume: 31, Issue:5	Novel calcium antagonists. Synthesis and structure-activity relationship studies of benzothiazoline derivatives.
AID415109	Negative inotropic activity in guinea pig left atrium assessed as decrease in atrial tension	2009	Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8	L-Type calcium channel blockers: from diltiazem to 1,2,4-oxadiazol-5-ones via thiazinooxadiazol-3-one derivatives.
AID75504	Concentration needed to achieve a 75% increase in coronary blood flow in 'Langendorff', guinea pig heart (in vitro negative inotropic activity)	1988	Journal of medicinal chemistry, Mar, Volume: 31, Issue:3	2-Ethynylbenzenealkanamines. A new class of calcium entry blockers.
AID77593	Increase in the coronary blood flow (CBF) was determined in isolated guinea pig heart at a dose of 30 ug/heart	1991	Journal of medicinal chemistry, Feb, Volume: 34, Issue:2	Synthesis of halogen-substituted 1,5-benzothiazepine derivatives and their vasodilating and hypotensive activities.
AID168007	Preventive effect of compound was measured on vasopressin-induced ST depression rats at 10 mg/kg po dose after 3h of administration; -=No significance	1991	Journal of medicinal chemistry, Mar, Volume: 34, Issue:3	A new class of calcium antagonists. 2. Synthesis and biological activity of 11-[[4-[4-(4-fluorophenyl)-1-piperazinyl]butyryl]amino]-6,11- dihydrodibenzo[b,e]-thiepin maleate and related compounds.
AID1079936	Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source]
AID1197211	Negative ionotropic activity in guinea pig left atrium assessed as decrease in developed tension driven at 1 Hz at 10'-5 M relative to control	2015	European journal of medicinal chemistry, Mar-06, Volume: 92	Synthesis and L-type calcium channel blocking activity of new chiral oxadiazolothiazinones.
AID1218845	Time dependent inhibition of CYP3A4 in human liver microsomes using midazolam as substrate preincubated for 90 mins followed by substrate addition by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme.
AID232671	Selectivity ratio of IC50 for [Ca2+] antagonistic activity in aorta / IC50 for suppressive effect on rate of contraction	1990	Journal of medicinal chemistry, Jul, Volume: 33, Issue:7	Synthesis and Ca2+ antagonistic activity of 2-[2-[(aminoalkyl)oxy]-5-methoxyphenyl]-3,4-dihydro-4-methyl-3-oxo-2H- 1,4-benzothiazines.
AID467397	Negative chronotropic activity in guinea pig right atrium assessed as decrease in atrial rate at 5 uM relative to control	2009	Journal of medicinal chemistry, Nov-12, Volume: 52, Issue:21	Stereoselective behavior of the functional diltiazem analogue 1-[(4-chlorophenyl)sulfonyl]-2-(2-thienyl)pyrrolidine, a new L-type calcium channel blocker.
AID1823667	Stability in human plasma assessed as parent compound remaining at 10 uM measured after 30 mins by LC-MS analysis	2021	Journal of medicinal chemistry, 05-27, Volume: 64, Issue:10	Discovery of New Imidazo[2,1-
AID28235	Unbound fraction (plasma)	2002	Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13	Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data.
AID1207244	Effective free therapeutic plasma concentration (EFTPC): the concentration of unbound compund in the blood plasma at therapeutic dose (mean of range)	2011	Cardiovascular research, Jul-01, Volume: 91, Issue:1	Simulation of multiple ion channel block provides improved early prediction of compounds' clinical torsadogenic risk.
AID1529184	Protein binding in immobilized human serum albumin by HPLC analysis	2020	Journal of medicinal chemistry, 02-27, Volume: 63, Issue:4	Human Serum Albumin Binding in a Vial: A Novel UV-pH Titration Method To Assist Drug Design.
AID193718	Hypotensive effect in Spontaneously hypertensive rats as maximum decrease in systolic blood pressure at 100 mg/kg, po dose	1988	Journal of medicinal chemistry, May, Volume: 31, Issue:5	Novel calcium antagonists. Synthesis and structure-activity relationship studies of benzothiazoline derivatives.
AID1211295	Unbound fraction in plasma (unknown origin) at pH 7.63 after 6 hrs by equilibrium dialysis method in presence of 5% CO2	2011	Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3	Control and measurement of plasma pH in equilibrium dialysis: influence on drug plasma protein binding.
AID269338	Negative chronotropic activity in guinea pig right atrium at 5 uM	2006	Journal of medicinal chemistry, Aug-24, Volume: 49, Issue:17	Calcium channel antagonists discovered by a multidisciplinary approach.
AID193719	Hypotensive effect in Spontaneously hypertensive rats as maximum decrease in systolic blood pressure at 30 mg/kg, po dose	1988	Journal of medicinal chemistry, May, Volume: 31, Issue:5	Novel calcium antagonists. Synthesis and structure-activity relationship studies of benzothiazoline derivatives.
AID188410	Natriuretic effect was evaluated in the conscious female rat by natriuretic assay involving metabolic caging at dose 20 mg/kg	1996	Journal of medicinal chemistry, Mar-15, Volume: 39, Issue:6	Endogenous natriuretic factors. 5. Synthesis and biological activity of a natriuretic metabolite of diltiazem and its derivatives.
AID20050	Human absorption A (%)	1998	Journal of medicinal chemistry, Mar-26, Volume: 41, Issue:7	Physicochemical high throughput screening: parallel artificial membrane permeation assay in the description of passive absorption processes.
AID1474167	Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status	2016	Drug discovery today, Apr, Volume: 21, Issue:4	DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID59091	Compound was tested for its hemodynamic effect for percentage change in coronary blood flow in anesthetized Dogs	1989	Journal of medicinal chemistry, Jan, Volume: 32, Issue:1	5-Isoquinolinesulfonamide derivatives. 2. Synthesis and vasodilatory activity of N-(2-aminoethyl)-5-isoquinolinesulfonamide derivatives.
AID467611	Dissociation constant, pKa of the compound	2009	European journal of medicinal chemistry, Nov, Volume: 44, Issue:11	Prediction of volume of distribution values in human using immobilized artificial membrane partitioning coefficients, the fraction of compound ionized and plasma protein binding data.
AID60859	Increasing effect on femoral blood flow in anesthetized dogs compared to the effect of trapidil	1989	Journal of medicinal chemistry, Jan, Volume: 32, Issue:1	5-Isoquinolinesulfonamide derivatives. 2. Synthesis and vasodilatory activity of N-(2-aminoethyl)-5-isoquinolinesulfonamide derivatives.
AID194014	Change in blood pressure in spontaneously hypertensive rats 1 hr following 30 mg/kg p.o.	1991	Journal of medicinal chemistry, Feb, Volume: 34, Issue:2	Synthesis of halogen-substituted 1,5-benzothiazepine derivatives and their vasodilating and hypotensive activities.
AID1207736	Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits	2013	Scientific reports, , Volume: 3	MICE models: superior to the HERG model in predicting Torsade de Pointes.
AID249519	Negative inotropic potency as maximal rate of the rise in left ventricular pressure in isolated guinea pig atrium	2005	Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7	A new class of selective myocardial calcium channel modulators. 2. Role of the acetal chain in oxadiazol-3-one derivatives.
AID311524	Oral bioavailability in human	2007	Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24	Hologram QSAR model for the prediction of human oral bioavailability.
AID80316	Inhibitory concentration required to suppress the contractile force of guinea pig right atria	1990	Journal of medicinal chemistry, Jul, Volume: 33, Issue:7	Synthesis and Ca2+ antagonistic activity of 2-[2-[(aminoalkyl)oxy]-5-methoxyphenyl]-3,4-dihydro-4-methyl-3-oxo-2H- 1,4-benzothiazines.
AID250135	Inhibition of compound against MES-SA/DX5 cell line was determined using P-glycoprotein assay	2005	Journal of medicinal chemistry, Apr-21, Volume: 48, Issue:8	A pharmacophore hypothesis for P-glycoprotein substrate recognition using GRIND-based 3D-QSAR.
AID78492	Molar concentration needed to increase e binding by 50% of maximal stimulation	1993	Journal of medicinal chemistry, May-14, Volume: 36, Issue:10	Novel heterocyclic analogues of the new potent class of calcium entry blockers: 1-[[4-(aminoalkoxy)phenyl]sulfonyl]indolizines.
AID186985	Kaliuretic effect was evaluated in the conscious female rat by natriuretic assay involving metabolic caging at dose 20 mg/kg	1996	Journal of medicinal chemistry, Mar-15, Volume: 39, Issue:6	Endogenous natriuretic factors. 5. Synthesis and biological activity of a natriuretic metabolite of diltiazem and its derivatives.
AID221137	Concentration (10 e-6 M) required to block [Ca2+]-induced contraction of K+-depolarized hamster aorta	1992	Journal of medicinal chemistry, Aug-21, Volume: 35, Issue:17	Synthesis, characterization, and Ca2+ antagonistic activity of diltiazem metabolites.
AID29359	Ionization constant (pKa)	2000	Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13	QSAR model for drug human oral bioavailability.
AID76313	Concentration needed to achieve a 75% increase in coronary blood flow in 'Langendorff', guinea pig heart (in vitro Negative inotropic potency)	1988	Journal of medicinal chemistry, Mar, Volume: 31, Issue:3	2-Ethynylbenzenealkanamines. A new class of calcium entry blockers.
AID678717	Inhibition of human CYP3A4 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 7-benzyloxyquinoline as substrate after 30 mins	2012	Chemical research in toxicology, Oct-15, Volume: 25, Issue:10	Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID1218828	Ratio of IC50 for CYP3A4 in human liver microsomes using testosterone as substrate preincubated for 90 mins followed by 10-fold dilution and substrate addition to IC50 for CYP3A4 in human liver microsomes using testosterone as substrate preincubated for 9	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme.
AID1207183	Inhibition of voltage-gated L-type Ca channel (species unknown)	2011	Cardiovascular research, Jul-01, Volume: 91, Issue:1	Simulation of multiple ion channel block provides improved early prediction of compounds' clinical torsadogenic risk.
AID1209258	Drug metabolism in human liver microsomes assessed as maximum rate of reaction per mg protein by multiple depletion curves method	2012	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12	Optimized experimental design for the estimation of enzyme kinetic parameters: an experimental evaluation.
AID467402	Vasorelaxant activity in 80 mM K+-depolarized guinea pig thoracic aortic strip assessed as inhibition of calcium-induced contraction at 100 uM	2009	Journal of medicinal chemistry, Nov-12, Volume: 52, Issue:21	Stereoselective behavior of the functional diltiazem analogue 1-[(4-chlorophenyl)sulfonyl]-2-(2-thienyl)pyrrolidine, a new L-type calcium channel blocker.
AID168005	Preventive effect of compound was measured on vasopressin-induced ST depression rats at 10 mg/kg po dose after 2 hr of administration; +=Differ from control value	1991	Journal of medicinal chemistry, Mar, Volume: 34, Issue:3	A new class of calcium antagonists. 2. Synthesis and biological activity of 11-[[4-[4-(4-fluorophenyl)-1-piperazinyl]butyryl]amino]-6,11- dihydrodibenzo[b,e]-thiepin maleate and related compounds.
AID1207639	Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes	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.
AID1079940	Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID678715	Inhibition of human CYP2D6 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 4-methylaminoethyl-7-methoxycoumarin as substrate after 30 mins	2012	Chemical research in toxicology, Oct-15, Volume: 25, Issue:10	Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID499784	Activation of phospholipase A2/C in human OC2 cells assessed as increase in intracellular calcium level at 1 uM	2010	Journal of natural products, Aug-27, Volume: 73, Issue:8	Effect of [6]-shogaol on cytosolic Ca2+ levels and proliferation in human oral cancer cells (OC2).
AID28233	Fraction ionized (pH 7.4)	2002	Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13	Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data.
AID80443	Inotropic negative potency on spontaneously beating right atrium of guinea pig	1995	Journal of medicinal chemistry, Oct-27, Volume: 38, Issue:22	Pyrrolo[2,1-c][1,4]benzothiazines: synthesis, structure-activity relationships, molecular modeling studies, and cardiovascular activity.
AID1218850	Time dependent inhibition of CYP3A4 in human liver microsomes using testosterone as substrate preincubated for 90 mins followed by substrate addition by LC-MS/MS analysis in presence of NADPH	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme.
AID467612	Fraction unbound in human plasma	2009	European journal of medicinal chemistry, Nov, Volume: 44, Issue:11	Prediction of volume of distribution values in human using immobilized artificial membrane partitioning coefficients, the fraction of compound ionized and plasma protein binding data.
AID1197219	Negative chronotropic activity in guinea pig left atrium assessed as decrease in atrial rate on spontaneous beating	2015	European journal of medicinal chemistry, Mar-06, Volume: 92	Synthesis and L-type calcium channel blocking activity of new chiral oxadiazolothiazinones.
AID193356	Antihypertensive activity 6-12h after 135 umol/kg p.o. in rats.	1992	Journal of medicinal chemistry, Jul-10, Volume: 35, Issue:14	Benzazepinone calcium channel blockers. 5. Effects on antihypertensive activity associated with N1 and aromatic substituents.
AID243422	log (1/Km) value for human liver microsome cytochrome P450 3A4	2005	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 15, Issue:18	Modeling K(m) values using electrotopological state: substrates for cytochrome P450 3A4-mediated metabolism.
AID386623	Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells at 100 uM by confocal microscopy	2008	Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19	Structural requirements for drug inhibition of the liver specific human organic cation transport protein 1.
AID1218853	Ratio of IC50 for CYP3A4 in human liver microsomes using midazolam as substrate preincubated for 90 mins to IC50 for CYP3A4 in human liver microsomes using midazolam as substrate preincubated for 90 mins in presence of NADPH	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme.
AID1849441	Stability in rat plasma assessed as half life and measured after 120 mins by LC-MS/MS analysis
AID364000	Vasorelaxant activity in K+-depolarized guinea pig ileum longitudinal smooth muscle assessed as inhibition of calcium-induced contraction at 1 uM	2008	Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18	Discovery of novel and cardioselective diltiazem-like calcium channel blockers via virtual screening.
AID540213	Half life in human after iv administration	2008	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7	Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1209243	Drug metabolism in assessed as human CYP3A4-mediated metabolism	2012	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12	Optimized experimental design for the estimation of enzyme kinetic parameters: an experimental evaluation.
AID249597	Compound was tested for percent change in atrioventricular conduction time in isolated guinea pig atrium	2005	Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7	A new class of selective myocardial calcium channel modulators. 2. Role of the acetal chain in oxadiazol-3-one derivatives.
AID1218843	Time dependent inhibition of CYP3A4 in human liver microsomes using midazolam as substrate preincubated for 30 mins followed by substrate addition by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme.
AID1222761	Fraction unbound in human at 120 mg, po	2013	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 41, Issue:5	Which metabolites circulate?
AID168015	Preventive effect of compound was measured on vasopressin-induced ST depression rats at 30 mg/kg po dose after 3h of administration; +=Differ from control value	1991	Journal of medicinal chemistry, Mar, Volume: 34, Issue:3	A new class of calcium antagonists. 2. Synthesis and biological activity of 11-[[4-[4-(4-fluorophenyl)-1-piperazinyl]butyryl]amino]-6,11- dihydrodibenzo[b,e]-thiepin maleate and related compounds.
AID77644	The compound was tested for antagonism of calcium-induced contractions of guinea pig ileal strips.	1991	Journal of medicinal chemistry, May, Volume: 34, Issue:5	Aminoalkynyldithianes. A new class of calcium channel blockers.
AID1079934	Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID173377	In vivo evaluation for the percentage decrease in blood pressure at 135 umol/kg administered through oral route in spontaneously hypertensive rats and observed for 0-6 h	1992	Journal of medicinal chemistry, Feb-21, Volume: 35, Issue:4	Benzazepinone calcium channel blockers. 3. Synthesis and structure-activity studies of 3-alkylbenzazepinones.
AID249511	Negative inotropic potency as coronary perfusion pressure in isolated guinea pig atrium	2005	Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7	A new class of selective myocardial calcium channel modulators. 2. Role of the acetal chain in oxadiazol-3-one derivatives.
AID624626	Ratio of apparent permeability from basolateral to apical side over apical to basolateral side determined in MDR1-MDCKII cells	2001	The Journal of pharmacology and experimental therapeutics, Nov, Volume: 299, Issue:2	Rational use of in vitro P-glycoprotein assays in drug discovery.
AID496824	Antimicrobial activity against Toxoplasma gondii	2010	Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6	Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID444054	Oral bioavailability in human	2010	Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3	Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID167813	In Vitro evaluation for the vasorelaxant effects in circumferential strips of potassium-depolarized rabbit aorta. (IC50 in rabbit aorta strips contracted with KCl	1992	Journal of medicinal chemistry, Feb-21, Volume: 35, Issue:4	Benzazepinone calcium channel blockers. 2. Structure-activity and drug metabolism studies leading to potent antihypertensive agents. Comparison with benzothiazepinones.
AID1218823	Time dependent inhibition of CYP3A4 in human liver microsomes using midazolam as substrate preincubated for 90 mins followed by 10-fold dilution and substrate addition by LC-MS/MS analysis in presence of NADPH	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme.
AID496821	Antimicrobial activity against Leishmania	2010	Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6	Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID444058	Volume of distribution at steady state in human	2010	Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3	Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID220639	Preventive effects on the methacholine-induced ST elevation in anesthetized rats in the presence of compound.(1 mg/kg given intravenously (iv) and tested for 0-10 min)	1991	Journal of medicinal chemistry, Feb, Volume: 34, Issue:2	A new class of calcium antagonists. Synthesis and biological activity of 11-[(omega-aminoalkanoyl)amino]-6,6a,7,8,9,10,10a,11-octahydrodibenzo [b,e]thiepin derivatives.
AID269347	Vasorelaxant activity assessed as inhibition of calcium-induced contraction of potassium ion-depolarized guinea pig aortic strips	2006	Journal of medicinal chemistry, Aug-24, Volume: 49, Issue:17	Calcium channel antagonists discovered by a multidisciplinary approach.
AID80735	[Ca2+] antagonistic activity on K+ depolarized guinea pig aortic strips at 10e-4 M	1996	Journal of medicinal chemistry, Jul-19, Volume: 39, Issue:15	Cardiovascular characterization of pyrrolo[2,1-d][1,5]benzothiazepine derivatives binding selectively to the peripheral-type benzodiazepine receptor (PBR): from dual PBR affinity and calcium antagonist activity to novel and selective calcium entry blocker
AID1210069	Inhibition of human recombinant CYP2J2 assessed as reduction in astemizole O-demethylation by LC-MS/MS method	2013	Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1	Discovery and characterization of novel, potent, and selective cytochrome P450 2J2 inhibitors.
AID415106	Effect on cardiac activity in guinea pig spontaneously beating heart assessed as change in atrioventricular conduction time at 1 uM relative to control	2009	Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8	L-Type calcium channel blockers: from diltiazem to 1,2,4-oxadiazol-5-ones via thiazinooxadiazol-3-one derivatives.
AID1197223	Antagonist activity at Cav1.2a in K+-depolarized guinea pig aortic strips assessed as inhibition of calcium-induced contraction	2015	European journal of medicinal chemistry, Mar-06, Volume: 92	Synthesis and L-type calcium channel blocking activity of new chiral oxadiazolothiazinones.
AID411051	Reversal of P-gp 170-mediated multidrug resistance in human A2780/DX3 cells assessed as reduction in doxorubicin IC50 at IC5 pretreated for 6 hrs before doxorubicin administration measured after 3 days by MTT assay	2009	Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2	Inhibition of MDR1 activity in vitro by a novel class of diltiazem analogues: toward new candidates.
AID195205	inhibitory effect of compound on contraction induced by high potassium in isolated rat aorta	1991	Journal of medicinal chemistry, Mar, Volume: 34, Issue:3	A new class of calcium antagonists. 2. Synthesis and biological activity of 11-[[4-[4-(4-fluorophenyl)-1-piperazinyl]butyryl]amino]-6,11- dihydrodibenzo[b,e]-thiepin maleate and related compounds.
AID411057	Down regulation of P-gp 170 expression in human A2780 cells after 72 hrs by flow cytometry	2009	Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2	Inhibition of MDR1 activity in vitro by a novel class of diltiazem analogues: toward new candidates.
AID1079942	Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID220638	Preventive effects on the methacholine-induced ST elevation in anesthetized rats in the absence of compound.	1991	Journal of medicinal chemistry, Feb, Volume: 34, Issue:2	A new class of calcium antagonists. Synthesis and biological activity of 11-[(omega-aminoalkanoyl)amino]-6,6a,7,8,9,10,10a,11-octahydrodibenzo [b,e]thiepin derivatives.
AID566279	Inhibition of rat L-type Ca2+ channel diltiazem site	2010	Bioorganic & medicinal chemistry, Nov-01, Volume: 18, Issue:21	Discovery of {1-[4-(2-{hexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl}-1H-benzimidazol-1-yl)piperidin-1-yl]cyclooctyl}methanol, systemically potent novel non-peptide agonist of nociceptin/orphanin FQ receptor as analgesic for the treatment of neuropathic pain: de
AID80729	Tested for the calcium antagonistic activity on K+-depolarized guinea pig aortic strips at 10e-4 M.	1995	Journal of medicinal chemistry, Oct-27, Volume: 38, Issue:22	Pyrrolo[2,1-c][1,4]benzothiazines: synthesis, structure-activity relationships, molecular modeling studies, and cardiovascular activity.
AID625282	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID386625	Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy	2008	Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19	Structural requirements for drug inhibition of the liver specific human organic cation transport protein 1.
AID467406	Muscle relaxant activity in 80 mM K+-depolarized guinea pig ileum longitudinal smooth muscle assessed as inhibition of calcium-induced contraction	2009	Journal of medicinal chemistry, Nov-12, Volume: 52, Issue:21	Stereoselective behavior of the functional diltiazem analogue 1-[(4-chlorophenyl)sulfonyl]-2-(2-thienyl)pyrrolidine, a new L-type calcium channel blocker.
AID1209250	Drug metabolism in human liver microsomes by multiple depletion curves method	2012	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12	Optimized experimental design for the estimation of enzyme kinetic parameters: an experimental evaluation.
AID1221982	Fraction absorbed in human	2011	Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2	Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID1441978	Inhibition of Kv1.1 (unknown origin)	2017	Journal of medicinal chemistry, 03-23, Volume: 60, Issue:6	A Rational Design of a Selective Inhibitor for Kv1.1 Channels Prevalent in Demyelinated Nerves That Improves Their Impaired Axonal Conduction.
AID364003	Vasorelaxant activity in K+-depolarized guinea pig ileum longitudinal smooth muscle assessed as inhibition of calcium-induced contraction	2008	Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18	Discovery of novel and cardioselective diltiazem-like calcium channel blockers via virtual screening.
AID455986	Permeability across human Caco-2 cells	2009	Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19	Computational modeling of novel inhibitors targeting the Akt pleckstrin homology domain.
AID1079948	Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID165792	Inhibition of [Ca2+] influx in response to a stimulus of norepinephrine (NE, 10 uM)	1988	Journal of medicinal chemistry, Mar, Volume: 31, Issue:3	2-Ethynylbenzenealkanamines. A new class of calcium entry blockers.
AID251134	Vasorelaxant activity determined by percentage inhibition of calcium-induced contraction on K+ depolarized guinea pig aortic strip at 5x10E-5 M	2005	Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7	A new class of selective myocardial calcium channel modulators. 2. Role of the acetal chain in oxadiazol-3-one derivatives.
AID678712	Inhibition of human CYP1A2 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using ethoxyresorufin as substrate after 30 mins	2012	Chemical research in toxicology, Oct-15, Volume: 25, Issue:10	Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID444051	Total clearance in human	2010	Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3	Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID411054	Reversal of P-gp 170-mediated multidrug resistance in human A2780 cells assessed as increase in intracellular doxorubicin accumulation at 5 times IC5 pretreated for 2 hrs before doxorubicin administration measured after 2 hrs by flow cytometry	2009	Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2	Inhibition of MDR1 activity in vitro by a novel class of diltiazem analogues: toward new candidates.
AID678721	Metabolic stability in human liver microsomes assessed as GSH adduct formation at 100 uM after 90 mins by HPLC-MS analysis	2012	Chemical research in toxicology, Oct-15, Volume: 25, Issue:10	Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID1218827	Ratio of IC50 for CYP3A4 in human liver microsomes using midazolam as substrate preincubated for 90 mins followed by 10-fold dilution and substrate addition to IC50 for CYP3A4 in human liver microsomes using midazolam as substrate preincubated for 90 mins	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme.
AID705595	Inhibition of CYP3A4-mediated N-demethylation in human liver microsomes	2012	Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11	Mechanism-based inactivation (MBI) of cytochrome P450 enzymes: structure-activity relationships and discovery strategies to mitigate drug-drug interaction risks.
AID75198	Concentration needed to elicit a 75% increase beyond control in coronary flow in ''Langendorff'', guinea pig heart (in vitro)	1988	Journal of medicinal chemistry, Mar, Volume: 31, Issue:3	2-Ethynylbenzenealkanamines. A new class of calcium entry blockers.
AID166113	In vitro inhibition of rabbit LDL oxidation by soybean lipoxygenase at 5 uM	1998	Journal of medicinal chemistry, Oct-22, Volume: 41, Issue:22	Novel calcium antagonists with both calcium overload inhibition and antioxidant activity. 1. 2-(3, 5-di-tert-butyl-4-hydroxyphenyl)-3-(aminopropyl)thiazolidinones.
AID428564	Inhibition of CYP3A4	2009	European journal of medicinal chemistry, Jul, Volume: 44, Issue:7	Comparative chemometric modeling of cytochrome 3A4 inhibitory activity of structurally diverse compounds using stepwise MLR, FA-MLR, PLS, GFA, G/PLS and ANN techniques.
AID678716	Inhibition of human CYP3A4 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using diethoxyfluorescein as substrate after 30 mins	2012	Chemical research in toxicology, Oct-15, Volume: 25, Issue:10	Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID1218824	Time dependent inhibition of CYP3A4 in human liver microsomes using testosterone as substrate preincubated for 90 mins followed by 10-fold dilution and substrate addition by LC-MS/MS analysis in presence of NADPH	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme.
AID269355	Cardiac activity in guinea pig heart measured as decrease in coronary perfusion pressure at 1 uM relative to control	2006	Journal of medicinal chemistry, Aug-24, Volume: 49, Issue:17	Calcium channel antagonists discovered by a multidisciplinary approach.
AID1517043	Stability in human plasma assessed as remaining compound at 10 uM incubated for 120 mins by LC-MS analysis
AID193782	Extent of hydrolysis of C3 acetyl group of 0.4 mM of compound 30 min after exposure by rat liver homogenate	1992	Journal of medicinal chemistry, Jul-10, Volume: 35, Issue:14	Benzazepinone calcium channel blockers. 5. Effects on antihypertensive activity associated with N1 and aromatic substituents.
AID21857	In vivo clearance in human.	1999	Journal of medicinal chemistry, Dec-16, Volume: 42, Issue:25	Combining in vitro and in vivo pharmacokinetic data for prediction of hepatic drug clearance in humans by artificial neural networks and multivariate statistical techniques.
AID625284	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1197231	Antagonist activity at Cav1.2b in K+-depolarized guinea pig ileum longitudinal smooth muscle assessed as inhibition of calcium-induced contraction	2015	European journal of medicinal chemistry, Mar-06, Volume: 92	Synthesis and L-type calcium channel blocking activity of new chiral oxadiazolothiazinones.
AID364884	Inhibition of P-gp in human adriamycin-resistant A2780 cells by Hoechst 33342 assay	2008	Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17	Structure-activity relationships of new inhibitors of breast cancer resistance protein (ABCG2).
AID79710	Activity of inotropic negative potency on stimulated guinea pig left atrium.	1996	Journal of medicinal chemistry, Jul-19, Volume: 39, Issue:15	Cardiovascular characterization of pyrrolo[2,1-d][1,5]benzothiazepine derivatives binding selectively to the peripheral-type benzodiazepine receptor (PBR): from dual PBR affinity and calcium antagonist activity to novel and selective calcium entry blocker
AID1529186	Binding affinity to human serum albumin assessed as change in dissociation constant pKa1 of compound in aqueous medium to presence of human serum albumin by UV-pH titration based spectrophotometric analysis	2020	Journal of medicinal chemistry, 02-27, Volume: 63, Issue:4	Human Serum Albumin Binding in a Vial: A Novel UV-pH Titration Method To Assist Drug Design.
AID415102	Effect on cardiac activity in guinea pig spontaneously beating heart assessed as change in left ventricular pressure at 1 uM relative to control	2009	Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8	L-Type calcium channel blockers: from diltiazem to 1,2,4-oxadiazol-5-ones via thiazinooxadiazol-3-one derivatives.
AID249596	Compound was tested for percent change in coronary perfusion pressure in isolated guinea pig atrium	2005	Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7	A new class of selective myocardial calcium channel modulators. 2. Role of the acetal chain in oxadiazol-3-one derivatives.
AID193783	Extent of hydrolysis of C3 acetyl group of 0.4 mM of compound 5 min after exposure by rat liver homogenate	1992	Journal of medicinal chemistry, Jul-10, Volume: 35, Issue:14	Benzazepinone calcium channel blockers. 5. Effects on antihypertensive activity associated with N1 and aromatic substituents.
AID1307835	Negative chronotropic activity in potassium depolarized guinea pig right atrium assessed as reduction in atrial rate after 30 mins	2016	Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7	Understanding Oxadiazolothiazinone Biological Properties: Negative Inotropic Activity versus Cytochrome P450-Mediated Metabolism.
AID166114	In vitro inhibition of rabbit LDL oxidation by soybean lipoxygenase at 0.5 uM	1998	Journal of medicinal chemistry, Oct-22, Volume: 41, Issue:22	Novel calcium antagonists with both calcium overload inhibition and antioxidant activity. 1. 2-(3, 5-di-tert-butyl-4-hydroxyphenyl)-3-(aminopropyl)thiazolidinones.
AID1209248	Drug metabolism in human liver microsomes assessed as intrinsic clearance per mg protein by optimal design approach	2012	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12	Optimized experimental design for the estimation of enzyme kinetic parameters: an experimental evaluation.
AID364887	Inhibition of ABCG2 in human mitoxantrone-resistant MCF7 cells by Hoechst 33342 assay	2008	Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17	Structure-activity relationships of new inhibitors of breast cancer resistance protein (ABCG2).
AID45790	Ability to inhibit [3H]nitrendipine binding to the L-type calcium channel receptor(CCR) in rat heart homogenate.	1996	Journal of medicinal chemistry, Jul-19, Volume: 39, Issue:15	Cardiovascular characterization of pyrrolo[2,1-d][1,5]benzothiazepine derivatives binding selectively to the peripheral-type benzodiazepine receptor (PBR): from dual PBR affinity and calcium antagonist activity to novel and selective calcium entry blocker
AID195351	Inhibition of calcium activation was assessed against calcium-induced constriction of potassium-depolarized rat aorta (Negative logarithm of the molar concentration)	1991	Journal of medicinal chemistry, Mar, Volume: 34, Issue:3	A new class of calcium antagonists. 2. Synthesis and biological activity of 11-[[4-[4-(4-fluorophenyl)-1-piperazinyl]butyryl]amino]-6,11- dihydrodibenzo[b,e]-thiepin maleate and related compounds.
AID205268	Inhibition of binding of Batrachotoxinin [3H]BTX-B to high affinity sites on voltage dependent sodium channels in a vesicular preparation from guinea pig cerebral cortex at 10 uM	1985	Journal of medicinal chemistry, Mar, Volume: 28, Issue:3	[3H]Batrachotoxinin A 20 alpha-benzoate binding to voltage-sensitive sodium channels: a rapid and quantitative assay for local anesthetic activity in a variety of drugs.
AID1221961	Apparent permeability from basolateral to apical side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of P-gp inhibitor LY335979	2011	Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2	Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID63267	Increasing effect on vertebral blood flow in anesthetized dogs compared to the effect of trapidil	1989	Journal of medicinal chemistry, Jan, Volume: 32, Issue:1	5-Isoquinolinesulfonamide derivatives. 2. Synthesis and vasodilatory activity of N-(2-aminoethyl)-5-isoquinolinesulfonamide derivatives.
AID59093	Compound was tested for its hemodynamic effect for percentage change in mean blood pressure in anesthetized Dogs	1989	Journal of medicinal chemistry, Jan, Volume: 32, Issue:1	5-Isoquinolinesulfonamide derivatives. 2. Synthesis and vasodilatory activity of N-(2-aminoethyl)-5-isoquinolinesulfonamide derivatives.
AID540212	Mean residence time in human after iv administration	2008	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7	Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID232670	Selectivity ratio of IC50 for [Ca2+] antagonistic activity in aorta / IC50 for suppressive effect on contractile force	1990	Journal of medicinal chemistry, Jul, Volume: 33, Issue:7	Synthesis and Ca2+ antagonistic activity of 2-[2-[(aminoalkyl)oxy]-5-methoxyphenyl]-3,4-dihydro-4-methyl-3-oxo-2H- 1,4-benzothiazines.
AID269363	Antagonist activity against calcium channel assessed as inhibition of calcium-induced contraction of potassium ion-depolarized guinea pig ileum longitudinal smooth muscle	2006	Journal of medicinal chemistry, Aug-24, Volume: 49, Issue:17	Calcium channel antagonists discovered by a multidisciplinary approach.
AID59094	Compound was tested for its hemodynamic effect for percentage change in vertebral blood flow in anesthetized dogs	1989	Journal of medicinal chemistry, Jan, Volume: 32, Issue:1	5-Isoquinolinesulfonamide derivatives. 2. Synthesis and vasodilatory activity of N-(2-aminoethyl)-5-isoquinolinesulfonamide derivatives.
AID1473740	Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 10 mins by membrane vesicle transport assay	2013	Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1	A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1473738	Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to 20 mins by membrane vesicle transport assay	2013	Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1	A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID363989	Negative inotropic activity in guinea pig left atrium assessed as decrease in atrial tension at 10 uM relative to control	2008	Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18	Discovery of novel and cardioselective diltiazem-like calcium channel blockers via virtual screening.
AID624622	Apparent permeability (Papp) from apical to basolateral side determined in MDR1-MDCKII cells	2001	The Journal of pharmacology and experimental therapeutics, Nov, Volume: 299, Issue:2	Rational use of in vitro P-glycoprotein assays in drug discovery.
AID80439	Tested for the negative chronotropic activity on isolated guinea pig spontaneously beating right atrium at 5*10e-5 M.	1995	Journal of medicinal chemistry, Oct-27, Volume: 38, Issue:22	Pyrrolo[2,1-c][1,4]benzothiazines: synthesis, structure-activity relationships, molecular modeling studies, and cardiovascular activity.
AID1221957	Apparent permeability from basolateral to apical side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis	2011	Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2	Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID1197225	Antagonist activity at Cav1.2b in K+-depolarized guinea pig ileum longitudinal smooth muscle assessed as inhibition of calcium-induced contraction at 10'-6 M relative to control	2015	European journal of medicinal chemistry, Mar-06, Volume: 92	Synthesis and L-type calcium channel blocking activity of new chiral oxadiazolothiazinones.
AID127919	Concentration causing local anesthetic activity in mice; Not tested	1988	Journal of medicinal chemistry, Nov, Volume: 31, Issue:11	Synthesis of (aryloxy)alkylamines. 2. Novel imidazo-fused heterocycles with calcium channel blocking and local anesthetic activity.
AID195193	Compound was tested in vitro for [Ca2+] antagonistic activity in K+-depolarized isolated rat aorta	1999	Journal of medicinal chemistry, Aug-12, Volume: 42, Issue:16	Novel calcium antagonists with both calcium overload inhibition and antioxidant activity. 2. Structure-activity relationships of thiazolidinone derivatives.
AID625283	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1215349	Time dependent inhibition of CYP3A4 in human liver microsomes assessed as conversion of testosterone to 6beta-hydroxytestosterone at 0.01 to 100 uM preincubated for 60 mins followed by testosterone treatment measured after 10 mins by refined CYP450 IC50 s	2011	Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 39, Issue:6	A refined cytochrome P540 IC₅₀ shift assay for reliably identifying CYP3A time-dependent inhibitors.
AID193221	Antihypertensive activity 0-6 hr after 135 umol/kg p.o. in rats.	1992	Journal of medicinal chemistry, Jul-10, Volume: 35, Issue:14	Benzazepinone calcium channel blockers. 5. Effects on antihypertensive activity associated with N1 and aromatic substituents.
AID1218854	Ratio of IC50 for CYP3A4 in human liver microsomes using testosterone as substrate preincubated for 90 mins to IC50 for CYP3A4 in human liver microsomes using testosterone as substrate preincubated for 90 mins in presence of NADPH	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme.
AID1517045	Stability in rat plasma assessed as remaining compound at 10 uM incubated for 120 mins by LC-MS analysis
AID180478	Molar concentration required to block [Ca2+] induced contraction of K+ depolarized rat aorta by 50%	1992	Journal of medicinal chemistry, Mar-20, Volume: 35, Issue:6	A novel class of calcium-entry blockers: the 1[[4-(aminoalkoxy)phenyl]sulfonyl]indolizines.
AID19419	Partition coefficient (logD7.4)	1998	Journal of medicinal chemistry, Mar-26, Volume: 41, Issue:7	Physicochemical high throughput screening: parallel artificial membrane permeation assay in the description of passive absorption processes.
AID21859	In vivo clearance in rat.	1999	Journal of medicinal chemistry, Dec-16, Volume: 42, Issue:25	Combining in vitro and in vivo pharmacokinetic data for prediction of hepatic drug clearance in humans by artificial neural networks and multivariate statistical techniques.
AID167353	In vitro vasorelaxant activity in circumferential strips of potassium-depolarized rabbit aorta.	1992	Journal of medicinal chemistry, Jul-10, Volume: 35, Issue:14	Benzazepinone calcium channel blockers. 5. Effects on antihypertensive activity associated with N1 and aromatic substituents.
AID496831	Antimicrobial activity against Cryptosporidium parvum	2010	Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6	Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID29812	Oral bioavailability in human	2000	Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13	QSAR model for drug human oral bioavailability.
AID88415	In Vitro evaluation on percentage inhibition in Heme Oxygenase at concentration 100 (uM) of infected host	2000	Journal of medicinal chemistry, Sep-07, Volume: 43, Issue:18	A new class of potential chloroquine-resistance reversal agents for Plasmodia: syntheses and biological evaluation of 1-(3'-diethylaminopropyl)-3-(substituted phenylmethylene)pyrrolidines.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID651635	Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
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.
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.
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.
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.
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.
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.
AID1745845	Primary qHTS for Inhibitors of ATXN expression
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID1346690	Mouse Kv1.1 (Voltage-gated potassium channels)	1994	Molecular pharmacology, Jun, Volume: 45, Issue:6	Pharmacological characterization of five cloned voltage-gated K+ channels, types Kv1.1, 1.2, 1.3, 1.5, and 3.1, stably expressed in mammalian cell lines.
AID1346704	Rat Kv1.2 (Voltage-gated potassium channels)	1994	Molecular pharmacology, Jun, Volume: 45, Issue:6	Pharmacological characterization of five cloned voltage-gated K+ channels, types Kv1.1, 1.2, 1.3, 1.5, and 3.1, stably expressed in mammalian cell lines.
AID1346684	Human Kv1.5 (Voltage-gated potassium channels)	1994	Molecular pharmacology, Jun, Volume: 45, Issue:6	Pharmacological characterization of five cloned voltage-gated K+ channels, types Kv1.1, 1.2, 1.3, 1.5, and 3.1, stably expressed in mammalian cell lines.
AID1346681	Mouse Kv3.1 (Voltage-gated potassium channels)	1994	Molecular pharmacology, Jun, Volume: 45, Issue:6	Pharmacological characterization of five cloned voltage-gated K+ channels, types Kv1.1, 1.2, 1.3, 1.5, and 3.1, stably expressed in mammalian cell lines.
AID1346659	Mouse Kv1.7 (Voltage-gated potassium channels)	1998	The Journal of biological chemistry, Mar-06, Volume: 273, Issue:10	Genomic organization, chromosomal localization, tissue distribution, and biophysical characterization of a novel mammalian Shaker-related voltage-gated potassium channel, Kv1.7.
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.
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.
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.
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.
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.
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.
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.
AID588349	qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
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.
AID588378	qHTS for Inhibitors of ATXN expression: Validation
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.
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.
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.
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.
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.
AID1347411	qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary	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.
AID1159607	Screen for inhibitors of RMI FANCM (MM2) intereaction	2016	Journal of biomolecular screening, Jul, Volume: 21, Issue:6	A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
AID588519	A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities	2011	Antiviral research, Sep, Volume: 91, Issue:3	High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	2083 (34.76)	18.7374
1990's	2207 (36.83)	18.2507
2000's	1043 (17.41)	29.6817
2010's	529 (8.83)	24.3611
2020's	130 (2.17)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Publication Type	This drug (%)	All Drugs (%)
Trials	1,073 (16.76%)	5.53%
Reviews	378 (5.90%)	6.00%
Case Studies	552 (8.62%)	4.05%
Observational	10 (0.16%)	0.25%
Other	4,389 (68.56%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (85)

Trial Overview

Trial	Phase	Enrollment	Study Type	Start Date	Status
A First-in-Human Study to Evaluate the Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of Single and Multiple Doses of BMS-986209 in Healthy Participants[NCT04154800]	Phase 1	114 participants (Actual)	Interventional	2019-12-06	Completed
Effect of Diltiazem on the Pharmacokinetics of BMS-914392 and on Heart Rate After Single-dose Administration of BMS-914392 in Healthy Subjects[NCT01211808]	Phase 1	24 participants (Actual)	Interventional	2010-09-30	Completed
A Phase I, Single Center, Open Label, 2-consecutive-group, 2-period, 1-sequence Crossover Study to Assess the Effect of Diltiazem (Cardizem), a Moderate CYP3A4 Inhibitor, or Ketoconazole, a Potent CYP3A4 Inhibitor, on the Pharmacokinetics of a Single Intr[NCT01124760]	Phase 1	28 participants (Actual)	Interventional	2010-05-31	Completed
Comparison of Vascular Remodeling Between Different Antianginal Medication Evaluated by Noninvasive ECG-gated Fundus Photographic Evaluation[NCT01162902]	Phase 4	150 participants (Anticipated)	Interventional	2013-09-30	Not yet recruiting
A Single-center, Open-label, Randomized, Two-way Crossover Study to Investigate the Effect of Multiple-dose Diltiazem on the Pharmacokinetics of a Single Dose of 25 mg ACT-541468 in Healthy Male Subjects[NCT02526888]	Phase 1	14 participants (Actual)	Interventional	2015-09-01	Completed
Randomized Controlled Trial Comparing the Efficacy of Polyethylene Glycol Alone and Polyethylene Glycol Combined With Topical Diltiazem in Treating Anal ﬁssure in Children[NCT02419534]	Phase 4	46 participants (Anticipated)	Interventional	2014-11-30	Recruiting
Prevention of Postoperative Cardiac Arrythmias in Thoracic Surgery : Celiprolol Versus Diltiazem[NCT03752931]	Phase 2	30 participants (Anticipated)	Interventional	2018-12-31	Not yet recruiting
An Open-label, Single-Sequence Study to Evaluate the Effects of Diltiazem, a Moderate CYP3A4/A5 Inhibitor, on the Pharmacokinetics and Pharmacodynamics of E5555 and Its Metabolites in Healthy Subjects[NCT01261156]	Phase 1	24 participants (Actual)	Interventional	2010-10-31	Completed
Effect of Nicorandil, Diltiazem or Isosorbide Mononitrate for Oral Antispastic Therapy After Coronary Artery Bypass Grafting Using Radial Artery Grafts - A Pilot Randomized Controlled Trial[NCT04310995]	Phase 4	150 participants (Actual)	Interventional	2020-06-02	Completed
TCD Monitoring Technology Guides the Precise Control of Blood Pressure After EVT[NCT03529149]	Phase 4	90 participants (Anticipated)	Interventional	2018-04-08	Recruiting
Effect of Additional Topical Diltiazem on Botulinum Toxin Injection for Chronic Anal Fissure: Retrospective Analysis of 217 Patients[NCT05797220]		217 participants (Actual)	Observational	2016-11-04	Completed
Heart Rate Controller in Computed Tomography Coronary Angiography: A Randomized Controlled Trial of Metoprolol, Diltiazem and Ivabradine[NCT05261464]	Phase 4	246 participants (Anticipated)	Interventional	2021-01-30	Recruiting
Efficacy of Medical Therapy in Women and Men With Angina and Myocardial Bridging[NCT04130438]	Phase 2	360 participants (Anticipated)	Interventional	2020-10-15	Suspended(stopped due to Low enrollment, modifying study protocol)
The Effect of Nebivolol in Hypertensive Patients With Coronary Arterial Spasm[NCT03930433]	Phase 4	51 participants (Actual)	Interventional	2018-01-01	Completed
Rate Control in Atrial Fibrillation II[NCT02695992]	Phase 4	122 participants (Actual)	Interventional	2016-02-29	Completed
Single-center, Open-label, Randomized, Multiple-dose, Parallel-group Study to Investigate Safety and Effects on Heart Rate, Blood Pressure, and Pharmacokinetic Interactions of ACT-334441 Combined With Calcium-channel Blocker (Diltiazem) or Beta-blocker (A[NCT02479204]	Phase 1	10 participants (Actual)	Interventional	2015-04-28	Terminated(stopped due to Based on results from the pilot phase, the study is terminated. No safety events leading to discontinuation were reported)
Validation of the Efficiency of Molecules Reproposed on the Basis of Their Cellular Transcriptomic Signature, Antagonist of the Signature Determined in Infection Due to Virus Influenza A.[NCT03212716]	Phase 2	85 participants (Actual)	Interventional	2017-12-23	Terminated(stopped due to rate of inclusion and study affected by covid-19 epidemic)
A Prospective, Multicentre, Double-Blinded Randomised Controlled Trial Comparing Topical Metronidazole, Diltiazem and Lidocaine on Post-Operative Pain Following Excisional Haemorrhoidectomy[NCT04276298]	Phase 2/Phase 3	192 participants (Actual)	Interventional	2020-09-01	Completed
[NCT00834925]	Phase 4	380 participants (Anticipated)	Interventional	2009-08-31	Recruiting
Treatment Of Chronic Anal Fissure (TOCA): a Randomized Clinical Trial on Levorag® Emulgel Versus Diltiazem Gel 2%[NCT02158013]		55 participants (Actual)	Interventional	2014-09-01	Terminated(stopped due to Slow inclusion rate)
Assessment of Efficacy and Side Effects of Dlitiazem Ointment With Lidocaine vs. Diltiazem Ointment With Lidocaine for Treatment of Chronic Anal Fissure: Randomized Clinical Trial[NCT04887818]	Phase 2/Phase 3	430 participants (Anticipated)	Interventional	2021-06-30	Not yet recruiting
Emergency Department Atrial Fibrillation Oral Diltiazem Observation Protocol[NCT05391893]	Phase 4	444 participants (Actual)	Interventional	2020-06-19	Completed
Efficacy of Diltiazem to Improve Coronary Microvascular Dysfunction: a Randomized Clinical Trial[NCT04777045]	Phase 3	85 participants (Anticipated)	Interventional	2019-10-25	Active, not recruiting
Association Between Angiotensin Converting Enzyme Inhibitor or Angiotensin Receptor Blocker Use and COVID-19 Severity and Mortality Among US Veterans[NCT04467931]		22,213 participants (Actual)	Observational	2020-01-19	Completed
An Open-Label Single-Sequence Study to Evaluate the Effect of Co-administration of Itraconazole or Diltiazem on the Single-Dose Pharmacokinetics of BMS-986177 in Healthy Subjects[NCT02807909]	Phase 1	28 participants (Actual)	Interventional	2016-07-31	Completed
Screening for Colorectal Cancer in Average and High Risk Iraqi Population: A Pilot Study[NCT04017845]	Early Phase 1	537 participants (Actual)	Interventional	2015-04-01	Completed
A Single Dose Pilot Study to Evaluate the Safety and Dose-Response of Smell to Intranasal Diltiazem[NCT01021176]	Phase 1	12 participants (Actual)	Interventional	2009-10-31	Terminated
A Safety and Efficacy Study of Blood Pressure Control in Acute Heart Failure - A Pilot Study (PRONTO)[NCT00803634]	Phase 3	117 participants (Actual)	Interventional	2008-12-31	Completed
Drug Discrimination in Methadone-Maintained Humans Study 2[NCT00733239]	Phase 1	15 participants (Actual)	Interventional	2008-08-31	Completed
A Drug-Drug Interaction Study of Zanubrutinib With Moderate and Strong CYP3A Inhibitors in Patients With B-Cell Malignancies[NCT04551963]	Phase 1	26 participants (Actual)	Interventional	2020-11-15	Completed
Multicenter, Double-blind, Randomized, Placebo-controlled Study Evaluating Diltiazem in Combination With Standard Treatment in the Management of Patients Hospitalized With COVID-19 Pneumonia - A Phase IIB, Proof of Concept Study[NCT05563168]	Phase 2	0 participants (Actual)	Interventional	2023-04-30	Withdrawn(stopped due to the epidemiological situation has changed considerably.)
[NCT00000478]	Phase 3	0 participants	Interventional	1990-11-30	Completed
[NCT00000556]	Phase 3	0 participants	Interventional	1995-03-31	Completed
An Open-label, Single-Sequence, Drug-Drug Interaction Study to Evaluate the Effect of Diltiazem Extended Release on the Pharmacokinetics of E2027 in Healthy Subjects[NCT02947711]	Phase 1	16 participants (Actual)	Interventional	2016-10-31	Completed
Evaluation of Pain Reduction After Hemorrhoidectomy With Use of Diltiazim Ointment 2%[NCT00893100]	Phase 4	1 participants (Actual)	Interventional	2007-10-31	Completed
Treatment of Preclinical Hypertrophic Cardiomyopathy With Diltiazem[NCT00319982]	Phase 2/Phase 3	39 participants (Actual)	Interventional	2006-01-31	Completed
A Phase I, Single-center, Open-label, 3-group, Fixed-sequence Study to Assess the Effect of Itraconazole, a Potent CYP3A4 Inhibitor, or Diltiazem, a Moderate CYP3A4 Inhibitor, on the Pharmacokinetics of AZD3293 and the Effects of AZD3293 on the Pharmacoki[NCT02010970]	Phase 1	56 participants (Actual)	Interventional	2013-12-31	Completed
Short Term Effect of Diltiazem on Myocardial Perfusion in Patients With Isolated Coronary Artery Ectasia- a Prospective Clinical Study[NCT02024919]		60 participants (Actual)	Interventional	2012-06-30	Completed
Randomized Trial Comparing Diltiazem and Metoprolol For Atrial Fibrillation Rate Control[NCT02025465]	Phase 4	150 participants (Anticipated)	Interventional	2013-12-31	Recruiting
Calcium Channel Blockers in Nitric Oxide Non-responder Pulmonary Arterial Hypertension.[NCT01645826]		0 participants (Actual)	Interventional	2012-07-31	Withdrawn(stopped due to no participants agreed to enroll since study start)
Drug Discrimination in Methadone-Maintained Humans Study 1[NCT00593463]	Phase 1	40 participants (Anticipated)	Interventional	2006-09-30	Completed
Reversal of No-reflow/Slow-flow During Percutaneous Coronary Intervention in Patients With Acute Myocardial Infarction--a Prospective Randomized Study Comparing Intracoronary Infusion of Diltiazem, Verapamil and Nitroglycerin[NCT00712894]	Phase 4	102 participants (Actual)	Interventional	2006-12-31	Completed
Efficacy of Diltiazem for the Control of Blood Pressure in Puerperal Patients With Severe Preeclampsia: A Randomized Controlled Trial[NCT04222855]		42 participants (Actual)	Interventional	2009-01-01	Completed
Improving Outcomes in Atrial Fibrillation Patients Aided by Implantable Cardiac Monitor: Evaluation of Chronic Beta-blocker Use Versus As-needed Pharmacological Rate Control[NCT05745337]	Phase 1	20 participants (Anticipated)	Interventional	2023-02-06	Recruiting
Assessing and Comparing the Effect of Diltiazem Gel Versus Nitroglycerin Ointment in Healing Process of Scleroderma Digital Ulcers.[NCT02801305]	Phase 2	90 participants (Actual)	Interventional	2016-06-30	Completed
A Comparative Study in the Control of Emergence Blood Pressure During Craniotomy for Tumor Surgery Between Labetolol (Avexa) and Diltiazem[NCT01408524]	Phase 1/Phase 2	184 participants (Actual)	Interventional	2010-02-28	Completed
Is Visceral Hyperalgesia the Culprit of Noncardiac Chest Pain in Chinese? Part 2: Effect of GABAB Agonist on Visceral Hyperalgesia in NCCP Patients[NCT00164801]		60 participants (Actual)	Interventional	2004-11-30	Terminated(stopped due to Funding ended)
An Open-Label, Three Period, Single Sequence Study To Determine The Effect Of Repeat Oral Dosing Of Diltiazem On The Pharmacokinetics Of Repeat Oral Dosing Of Darapladib (SB-480848).[NCT01852565]	Phase 1	36 participants (Actual)	Interventional	2013-05-14	Completed
The Surrogate Marker of Rate Control in Patients With Atrial Fibrillation[NCT04513509]		50 participants (Anticipated)	Interventional	2020-08-07	Not yet recruiting
Evaluation of Potential Pharmacokinetic Interactions Between HIV Protease Inhibitors and Calcium Channel Blockers[NCT00039975]	Phase 1	32 participants	Interventional		Completed
Diltiazem vs. Metoprolol in the Acute Management of Atrial Fibrillation in Patients With Heart Failure With Reduced Ejection Fraction[NCT02938260]		48 participants (Actual)	Observational	2016-10-31	Completed
Gradual Diltiazem Infusion as an Approach to Initial Rate Control in Atrial Fibrillation or Atrial Flutter With Rapid Ventricular Response in the Emergency Setting[NCT04141553]	Phase 4	300 participants (Anticipated)	Interventional	2019-12-01	Not yet recruiting
Comprehensive in Vitro Proarrhythmia Assay (CiPA) Clinical Phase 1 ECG Biomarker Validation Study (CiPA Phase 1 ECG Biomarker Study)[NCT03070470]	Phase 1	60 participants (Actual)	Interventional	2017-03-14	Completed
Comparative Evaluation of MEBO Ointment and Topical Diltiazem Ointment in the Treatment of Acute Anal Fissure: a Randomized Clinical Trial[NCT04153032]	Phase 2	183 participants (Anticipated)	Interventional	2019-12-01	Recruiting
Rhythm Control Versus Rate Control for New Onset Atrial Fibrillation After Non-cardiac Non-thoracic Surgery[NCT05950971]		1 participants (Actual)	Interventional	2021-07-01	Terminated(stopped due to Study enrollment too slow, 1 over 6 months)
A Drug Interaction Study Investigating the Effect of Boceprevir on the Pharmacokinetics of the Calcium Channel Blockers Amlodipine and Diltiazem and Vice Versa in Healthy Volunteers[NCT01549496]	Phase 1	0 participants (Actual)	Interventional	2012-05-31	Withdrawn(stopped due to Investigator left this hospital)
Action to Control Cardiovascular Risk in Diabetes (ACCORD)[NCT00000620]	Phase 3	10,251 participants (Actual)	Interventional	1999-09-30	Completed
The Pathophysiology and Treatment of Supine Hypertension in Patients With Autonomic Failure[NCT00223717]	Phase 1	152 participants (Actual)	Interventional	2001-01-31	Completed
An Open-label, Non-randomized, Fixed Sequence Study Assessing the Pharmacokinetics of AZD7986 When Administered Alone and With Multiple Doses of Verapamil and Itraconazole or Diltiazem in Healthy Subjects[NCT02653872]	Phase 1	15 participants (Actual)	Interventional	2016-01-22	Completed
The Effect of Concomitant Administration of Erythromycin and Diltiazem on CYP3A Activity in Healthy Volunteers[NCT00318201]	Phase 4	7 participants (Actual)	Interventional	2006-04-30	Completed
Rate Control in Atrial Fibrillation[NCT00313157]	Phase 3	80 participants (Actual)	Interventional	2006-04-30	Completed
Efficacy of HYdroxychloroquine and DILtiazem-nIClosamide Combination for the Treatment of Non-severe Forms of SARS-CoV2 Infection in Patients With Co-morbidities: Multicenter, Randomized, Open-labeled Controlled Trial[NCT04372082]	Phase 3	0 participants (Actual)	Interventional	2020-05-31	Withdrawn(stopped due to evidence showed chloroquine is not effective against COVID-19)
Oral Propranolol, Diltiazem, Metoprolol and Verapamil in Atrial Fibrillation Rate Control in Patients With Stable Hemodynamic Status[NCT01655303]	Phase 4	90 participants (Actual)	Interventional	2011-02-28	Completed
A Phase 3B, Randomized, Double-Blind, Placebo-Controlled, Parallel-Treatment Group, Multicenter Efficacy and Safety Study of Topical Diltiazem Hydrochloride 2% Cream in Subjects With Anal Fissure[NCT01690221]	Phase 3	434 participants (Actual)	Interventional	2012-10-31	Completed
First Prospective Randomized Trial to Examine a Differential Therapeutic Response in Symptomatic Patients With Non-obstructive Coronary Artery Disease After Coronary Physiological Testing[NCT05294887]	Phase 4	132 participants (Anticipated)	Interventional	2022-03-04	Recruiting
Drug-Drug Interaction Study to Assess the Effects of Steady-State Cardizem LA (Diltiazem Hydrochloride) and Steady-State Pitavastatin on Their Respective Pharmacokinetics in Healthy Adult Volunteers[NCT01422382]	Phase 4	28 participants (Actual)	Interventional	2011-05-31	Completed
Effects of Diltiazem and/or N-Acétylcystéine Versus Placebo on hémodynamiques and Biological Repercussions of the Ischaemia-réperfusion During the Coronary Surgery With Beating Heart[NCT01771978]	Phase 3	120 participants (Anticipated)	Interventional	2002-06-30	Active, not recruiting
An Open-Label, Single- and Multi-Dose Pharmacokinetic (PK) Study of Oral Diltiazem and Topical Diltiazem Hydrochloride[NCT01816191]	Phase 1	12 participants (Anticipated)	Interventional	2013-02-28	Active, not recruiting
A Randomized, Controlled Study to Evaluate the Sensitizing Potential of Diltiazem Hydrochloride 2% Cream in Healthy Subjects Using a Repeat Insult Patch Test Design[NCT01816529]	Phase 1	200 participants (Anticipated)	Interventional	2013-03-31	Active, not recruiting
A 21-Day, Randomized, Controlled Study to Evaluate the Irritation Potential of Diltiazem Hydrochloride 2% Cream in Healthy Subjects, Using a Cumulative Irritant Patch Test Design[NCT01821274]	Phase 1	30 participants (Anticipated)	Interventional	2013-03-31	Active, not recruiting
A One-Directional, Open-Label Drug Interaction Study to Investigate the Effects of Multiple-Dose Diltiazem ER on Single-Dose Pharmacokinetics of Colchicine in Healthy Volunteers[NCT00983372]	Phase 1	24 participants (Actual)	Interventional	2008-08-31	Completed
An Open-label, Randomized, 2-Period Crossover Study to Evaluate the Effect of Co-administration of Itraconazole or Diltiazem on the Single-dose Pharmacokinetics of Danicamtiv in Healthy Participants[NCT05162222]	Phase 1	30 participants (Actual)	Interventional	2021-12-15	Completed
The CORONAvirus Disease 2019 Angiotensin Converting Enzyme Inhibitor/Angiotensin Receptor Blocker InvestigatiON (CORONACION) Randomized Clinical Trial[NCT04330300]	Phase 4	2,414 participants (Anticipated)	Interventional	2020-04-30	Suspended(stopped due to Challenges with funding and very low incidence of COVID-19 at Irish study site)
A Randomised,Double-Blind, Placebo-Controlled Trial of the Safety and Efficacy of Diltiazem Hydrochloride Cream in Subjects With Anal Fissure[NCT01217515]	Phase 3	465 participants (Actual)	Interventional	2010-10-31	Completed
An Open-label, Sequential, 3-period Study to Assess the Effects of Diltiazem on the Pharmacokinetics of Naloxegol in Healthy Subjects[NCT01594619]	Phase 1	44 participants (Actual)	Interventional	2012-05-31	Completed
A Study to Determine the Effect of CYP3A Inhibition on the Pharmacokinetics of LY2623091 and the Effect of LY2623091 on the Pharmacokinetics of CYP3A Substrates in Healthy Subjects[NCT02300259]	Phase 1	48 participants (Actual)	Interventional	2014-11-30	Completed
Oral vs Intravenous Diltiazem for Rapid Atrial Fibrillation/Flutter Trial[NCT03472495]	Phase 4	19 participants (Actual)	Interventional	2018-06-01	Completed
Comparative Study Between the Efficacy of Oral Verapamil and Oral Diltiazim on Reduction of Intraoperative Bleeding During Endoscopic Sinus Surgery Under General Anesthesia[NCT04790331]	Early Phase 1	135 participants (Anticipated)	Interventional	2021-03-01	Not yet recruiting
Efficacy of Oral Diltiazem Versus Combination of Oral Diltiazem With Intravenous Tranexamic Acid on the Intraoperative Bleeding in Functional Endoscopic Sinus Surgery[NCT03580590]	Early Phase 1	40 participants (Anticipated)	Interventional	2018-09-01	Not yet recruiting
Phase 1, Open-label, Drug-drug Interaction Study to Evaluate the Interaction Potential of Clarithromycin XL on Diltiazem Hydrochloride Cream 2% in Healthy Subjects[NCT02080780]	Phase 1	24 participants (Actual)	Interventional	2013-09-30	Completed
DiME Study: Comparison of Diltiazem and Metoprolol in the Management of Acute Atrial Fibrillation or Atrial Flutter With Rapid Ventricular Response: A Prospective Randomized and Double-Blinded Non-Inferiority Trial of Safety and Efficacy[NCT01914926]	Phase 4	54 participants (Actual)	Interventional	2009-06-30	Completed
A Phase 1, Randomized, Open-label, 3-sequence, 4-treatment, Incomplete Block Design To Estimate The Effect Of Steady State Cyp3a4 Inhibitors (Itraconazole, Diltiazem Or Verapamil) On The Pharmacokinetics Of Singe Dose Pf-00489791 In Healthy Volunteers[NCT02319148]	Phase 1	22 participants (Actual)	Interventional	2014-07-31	Completed
Assessment of Intravenous Rate Control Response in Atrial Fibrillation Trial Pilot Study (AIRCRAFT)[NCT04234477]	Phase 4	0 participants (Actual)	Interventional	2021-12-31	Withdrawn(stopped due to The study was not IRB approved and there were anticipated challenges in recruiting participants.)
Phase 1-2 Study of Development of Rational Ways of Medical and Non-medical Treatment Methods for Metabolic Syndrome[NCT02503865]	Phase 1/Phase 2	351 participants (Actual)	Interventional	2003-01-31	Completed
Five Period Crossover Study of the Ability of Late Sodium or Calcium Current Block (Mexiletine, Lidocaine, or Diltiazem) to Balance the Electrocardiographic Effects of hERG Potassium Current Block (Dofetilide or Moxifloxacin)[NCT02308748]	Phase 1	22 participants (Actual)	Interventional	2014-05-31	Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

Number of Patients That Require Intubation During Study Drug Administration up to 96 Hours

The number of patients requiring intubation was calculated based on the total number of mITT patients. (NCT00803634)
Timeframe: Initiation through termination of study drug (up to 96 hours)

Intervention	Patients (Number)
Clevidipine	0
Standard of Care	0

Percentage Falling Below Lower Limit of SBP Target Range at Any Time During Study

The percentage of patients in whom the SBP fell below the lower limit of the prespecified target range at any time during the entire study drug treatment period (up to 96 hours) was calculated within each treatment group using the number of mITT patients achieving the endpoint divided by the number of mITT patients and multiplied by 100. Two-tailed 95% CIs were computed for these percentages. (NCT00803634)
Timeframe: Initiation through termination of study drug (up to 96 hours)

Intervention	Percentage of patients (Number)
Clevidipine	68.2
Standard of Care	70.7

Percentage Falling Below Lower Limit of SBP Target Range Within First 30 Minutes

The percentage of patients in whom the SBP fell below the lower limit of the prespecified target range at any time during the first 30 minutes was calculated within each treatment group using the number of mITT patients achieving the endpoint divided by the number of mITT patients and multiplied by 100. Two-tailed 95% CIs were computed for these percentages. (NCT00803634)
Timeframe: Initiation of study drug through the initial 30-minutes

Intervention	Percentage of patients (Number)
Clevidipine	34.1
Standard of Care	2.4

Percentage of Patients Who Received Any Alternative IV Antihypertensive Drug at Any Time During Study Drug Treatment

The percentage of patients who received any alternative IV antihypertensive drug at any time during the study drug treatment period (up to 96 hours) was calculated using mITT patients within each treatment group. (NCT00803634)
Timeframe: Initiation through termination of study drug (up to 96 hours)

Intervention	Percentage of patients (Number)
Clevidipine	15.9
Standard of Care	51.2

Percentage of Patients With at Least One Episode of SBP < 90 mm Hg During Study Drug Administration (up to 96 Hours)

The percent of patients with at least one episode of SBP <90 mm Hg was calculated as the number of mITT patients who had at least one episode of SBP<90 mm Hg during study drug administration up to 96 hours divided by mITT patients, and multiplied by 100 for each treatment group. (NCT00803634)
Timeframe: Initiation through termination of study drug (up to 96 hours)

Intervention	Percentage of patients (Number)
Clevidipine	5.9
Standard of Care	1.9

Percentage Reaching Prespecified Target Range Without Falling Below Lower Limit of Target Range Within First 30 Minutes

The percentage of patients reaching this endpoint was calculated within each treatment group using the number of mITT patients reaching the endpoint divided by the number of mITT patients, and multiplied by 100. Two-tailed 95% CIs were computed for these percentages. (NCT00803634)
Timeframe: Initiation of study drug through the initial 30-minutes

Intervention	Percentage of patients (Number)
Clevidipine	45.5
SOC IV Therapy	51.2

Percentage to First Achieve Initial Prespecified SBP Target Range [≥20 mm Hg and ≤40 mm Hg Apart] and 15% Reduction From Baseline Within First 30 Minutes

Analysis of the percentage of patients achieving both components of this composite endpoint (attainment of the initial prespecified SBP target range and a 15% reduction in SBP from baseline) was calculated within each treatment group using the number of mITT patients achieving the SBP reduction goal divided by the number of mITT patients, and multiplied by 100. (NCT00803634)
Timeframe: Initiation of study drug through the initial 30-minutes

Intervention	Percentage of patients (Number)
Clevidipine	70.5
Standard of Care	36.6

SBP Area Under the Curve (AUC) Outside Prespecified Target Range

The magnitude and duration of SBP excursions was calculated as the area under the curve (AUC) for each patient, using the trapezoidal rule, related to time (in minutes) that each patient's SBP was outside the target range. AUC was determined based on data collected from the initiation of study medication through the end of monotherapy treatment up to 96 hours, normalized per hour, and expressed as mmHg × minute/hour. (NCT00803634)
Timeframe: Initiation of study drug through end of monotherapy (up to 96 hours)

Intervention	mm Hg x min/h (Mean)
Clevidipine	494.96
Standard of Care	966.15

Time to First Achieve Initial Prespecified SBP Target Range and 15% Reduction From Baseline Within First 30 Minutes

Time to first achieve the initial pre-specified systolic blood pressure (SBP) target range and a 15% SBP reduction from baseline is the time in minutes between the initiation of study medication and the time the patient first achieved both components. Median time was estimated using Kaplan Meier method. 95% two-sided confidence interval of the median time is from 'Simon and Lee, 1982'. If patients did not reach both components within 30 minutes from the initial treatment with study medication, or another antihypertensive agent was administered, the patient was censored at 30 minutes or the time when another antihypertensive agent is given, whichever came first. (NCT00803634)
Timeframe: Initiation of study drug through the initial 30-minutes

Intervention	Minutes (Median)
Clevidipine	15.0
Standard of Care	NA

Time to Use Other IV Antihypertensives During the Study Drug Administration

The length of time to use other IV antihypertensive agents was defined as the duration in hours from the initiation of study drug through the time when any other concomitant IV antihypertensive agent was administered, thus, representing the time period without use of any other concomitant IV antihypertensive agent. Median time to use other IV antihypertensive agents was obtained using Kaplan-Meier method. If a patient did not receive any concomitant IV antihypertensive during the 96-hour treatment period, this patient was considered censored at 96 hours. If study drug was stopped less than 96 hours and the patient has no concomitant IV antihypertensive agent, the patient was considered censored when study drug was stopped. (NCT00803634)
Timeframe: Initiation of study drug through any other concomitant IV antihypertensive agent administered, up to 96 hours

Intervention	Hours (Median)
Clevidipine	NA
Standard of Care	5.7

Change From Baseline in Dyspnea (Measured By VAS) at Each Time Point

A validated visual analog scale (VAS) with a horizontal ruler showing increments from 0 to 100 mm with 0 = Best and 100 = Worst was used. The test was asked from the patient's perspective and had to be administered with patient sitting. Relative change in VAS from baseline is the value at each time point minus the baseline value. Relative change from baseline was summarized descriptively (with associated two-tailed 95% CIs of the mean values) at 15, 30 and 45 minutes and at 1, 2, 3 hours and 12 hours, and 1 hour post termination of study drug treatment. (NCT00803634)
Timeframe: Baseline (immediately prior to study drug administration) through 1 hour after study drug termination

Intervention	millimeters (mm) (Mean)
	Baseline Through Initial 15 Min- CLV n=44;SOC n=38	Baseline Through Initial 30 Min- CLV n=43;SOC n=39	Baseline Through Initial 45 Min- CLV n=43;SOC n=39	Baseline Through Initial 1 H- CLV n=41;SOC n=38	Baseline Through Initial 2 H- CLV n=29;SOC n=29	Baseline Through Initial 3 H- CLV n=14;SOC n=22	Baseline Through Initial 12 H- CLV n=0;SOC n=7	Baseline Through 1 H Post Drug- CLV n=41;SOC n=33
Clevidipine	-18.6	-28.8	-37.1	-43.6	-45.2	-47.9	NA	-50.1
Standard of Care	-16.1	-22.8	-27.9	-34.6	-35.3	-40.5	-57.9	-50.1