repaglinide profile

repaglinide is involved in 1 pathway(s), involving a total of 6 unique proteins and 5 unique compounds

ID Source	ID
PubMed CID	65981
CHEMBL ID	1272
CHEBI ID	8805
SCHEMBL ID	16137
MeSH ID	M0196126

Synonym
AC-726
BIDD:GT0338
AKOS005561792
BRD-K82846253-001-03-0
prandin
nn-623
surepost
actulin
novonorm
gluconorm
ag-ee-623 zw
ag-ee-388
smp-508
PRESTWICK3_001046
BPBIO1_001070
2-ethoxy-4-(2-{[(1s)-3-methyl-1-(2-piperidin-1-ylphenyl)butyl]amino}-2-oxoethyl)benzoic acid
repaglinide, >=98% (hplc), solid
repaglinide [usan]
(s)-2-ethoxy-4-(2-((methyl-1-(2-(1-piperidinyl)phenyl)butyl)amino)-2-oxoethyl)-benzoic acid
(s)-2-ethoxy-4-(2-((3-methyl-1-(2-(1-piperidinyl)-phenyl)butyl)amino)-2-oxoethyl)-benzoic acid
c27h36n2o4
repaglinida [inn-spanish]
ag-ee 623 zw
benzoic acid, 2-ethoxy-4-(2-((3-methyl-1-(2-(1-piperidinyl)phenyl)butyl)amino)-2-oxoethyl)-, (s)-
repaglinidum [inn-latin]
ag-ee 388 zw
(+)-2-ethoxy-alpha-(((s)-alpha-isobutyl-o-piperidinobenzyl)carbamoyl)-p-toluic acid
BSPBIO_000972
cas-135062-02-1
NCGC00016978-01
PRESTWICK2_001046
AB00514019
C07670
135062-02-1
repaglinide
smr000466305
MLS000759407
DB00912
repaglinide (jan/usp/inn)
prandin (tn)
surepost (tn)
D00594
PRESTWICK0_001046
PRESTWICK1_001046
SPBIO_002906
NCGC00016978-02
(+)-repaglinide
repa-glinide
ag-ee-623-zw
ag-ee-623zw
agee-623zw
MLS001076684
HMS2051N08
HMS2094C07
chebi:8805 ,
a10bx02
nsc-759893
CHEMBL1272 ,
2-ethoxy-4-[2-[[(1s)-3-methyl-1-[2-(1-piperidinyl)phenyl]butyl]amino]-2-oxoethyl]benzoic acid
111GE012 ,
2-ethoxy-4-[2-[[(1s)-3-methyl-1-(2-piperidin-1-ylphenyl)butyl]amino]-2-oxoethyl]benzoic acid
2-ethoxy-4-{[(s)-3-methyl-1-(2-piperidin-1-yl-phenyl)-butylcarbamoyl]-methyl}-benzoic acid
bdbm50153520
(s)-2-ethoxy-4-(2-(3-methyl-1-(2-(piperidin-1-yl)phenyl)butylamino)-2-oxoethyl)benzoic acid
HMS1571A14
STK629501
2-ethoxy-4-[2-({(1s)-3-methyl-1-[2-(piperidin-1-yl)phenyl]butyl}amino)-2-oxoethyl]benzoic acid
(2s)-2-[[(2s)-2-[[(2s,3s)-2-[[(2s)-4-amino-2-[[(2s,3s)-2-[[(2s)-2-[[2-[[(2s)-2-[[(2s)-1-[(2s)-2-[[(2s)-2-amino-5-guanidino-pentanoyl]amino]-4-carboxy-butanoyl]pyrrolidine-2-carbonyl]amino]propanoyl]amino]acetyl]amino]-4-methyl-pentanoyl]amino]-3-methyl-pe
A806877
HMS2098A14
reglin
nsc 759893
repaglinide [usan:usp:inn:ban]
repaglinida
repaglinidum
unii-668z8c33lu
668z8c33lu ,
nsc759893
pharmakon1600-01506035
MLS001424111
dtxcid603552
dtxsid3023552 ,
tox21_110721
(s)-2-ethoxy-4-(2-((3-methyl-1-(2-(piperidin-1-yl)phenyl)butyl)amino)-2-oxoethyl)benzoic acid
HMS2231M21
CCG-101013
HY-15209
CS-0979
NCGC00016978-05
repaglinide [ema epar]
repaglinide [inn]
repaglinide [jan]
repaglinide [mi]
repaglinide [who-dd]
repaglinide [usp-rs]
repaglinide [orange book]
repaglinide [usp monograph]
(s)-2-ethoxy-4-(2-(methyl-1-(2-(1-piperidinyl)phenyl)butylamino)-2-oxoethyl)-benzoic acid
(+)-2-ethoxy-.alpha.-(((s)-.alpha.-isobutyl-o-piperidinobenzyl)carbamoyl)-p-toluic acid
repaglinide [ep monograph]
repaglinide [mart.]
repaglinide [vandf]
S1426
gtpl6841
AB00514019-09
MLS006011560
AM20090697
NC00263
benzoic acid, 2-ethoxy-4-[2-[[(1s)-3-methyl-1-[2-(1-piperidinyl)phenyl]butyl]amino]-2-oxoethyl]-
SCHEMBL16137
BS-1010
(s)-2-ethoxy-4-[n-(1-(2-piperidino-phenyl)-3-methyl-1-butyl)-aminocarbonylmethyl]-benzoic acid
FAEKWTJYAYMJKF-QHCPKHFHSA-N
(s)-(+)-2-ethoxy-4-(2-oxo-2-[(alpha-isobutyl-2-piperidinobenzyl)amino]ethyl)-benzoic acid
NCGC00016978-04
Q-201663
ag-ee 623zw
HB1106
2-ethoxy-4-[2-[[(1s)-3-methyl-1-[2-(1-piperidinyl)phenyl]butyl]amino]-2-oxoethyl]benz oic acid
(s)-(+)-2-ethoxy-4-[n-[1-(2-piperidinophenyl)-3-methyl-1-butyl]aminocarbonylmethyl]benzoic acid
R0179
AB00514019_11
AB00514019_10
mfcd00906179
2-ethoxy-4-({[(1s)-3-methyl-1-[2-(piperidin-1-yl)phenyl]butyl]carbamoyl}methyl)benzoic acid
SR-01000759404-4
sr-01000759404
repaglinide, united states pharmacopeia (usp) reference standard
repaglinide for system suitability, european pharmacopoeia (ep) reference standard
repaglinide, european pharmacopoeia (ep) reference standard
SBI-0206942.P001
HMS3715A14
SW197344-4
BCP04250
F15001
HMS3678D09
repaglinide,(s)
Q2195995
BJX ,
HMS3414D09
(s)-2-ethoxy-4-[2-[[3-methyl-1-[2-(piperidin-1-yl)phenyl]butyl]amino]-2-oxoethyl]benzoic acid
(s)-2-ethoxy-4-(2-((3-methyl-1-(2-(piperidin-1-yl)phenyl)butyl)amino)-2-oxoethyl)benzoicacid
(s)-2-ethoxy-4-[2-[[[(1s)-3-methyl-1-[2-(1-piperidinyl)phenyl]butyl]amino]-2-oxoethyl]benzoic acid
repaglinide for system suitability
BR164332
repaglinide- bio-x
Z1501485370
repaglinide (usan:usp:inn:ban)
benzoic acid, 2-ethoxy-4-(2-((3-methyl-1-(2-(1-piperidinyl)phenyl)butyl)amino)-2-oxoethyl)-,(s)-
repaglinide (mart.)
repaglinide (usp monograph)
repaglinide (usp-rs)
repaglinida (inn-spanish)
(s)-2-ethoxy-4-(2-(3-methyl-1-(2-piperidinophenyl)butylamino)-2-oxoethyl)benzoic acid
repaglinidum (inn-latin)
repaglinide (ep monograph)

Excerpt	Reference
"Repaglinide turned out to be a useful therapeutic for type 2 diabetic patients; approval was granted recently by the FDA and the EMEA."	( Grell, W; Griss, G; Hurnaus, R; Luger, P; Mark, M; Müller, P; Nar, H; Rupprecht, E; Sauter, R; Wittneben, H, 1998)
"Repaglinide is an antidiabetic drug that works by stimulating insulin secretion from pancreatic beta cells. "	( Abdalhafez, A; Abu-Zaid, A; Albetawi, S, 2021)
"Repaglinide (RPG) is an oral insulin secretagogue used in the treatment of diabetes. "	( Abdollahi, M; Asgarian, S; Baeeri, M; Dehpour, AR; Emamgholipour, Z; Firoozpour, L; Foroumadi, A; Foroumadi, R; Gholami, M; Goli, F; Keykhaei, M, 2022)
"Repaglinide is an antidiabetic drug that, via the blocking of ATP-sensitive potassium channels (K-ATP channels), depolarization of the β-cell membrane, and opening of the voltage-gated calcium channels leads to an increase in intracellular calcium."	( Azadbakht, M; Jalilian, N; Kalehoei, E; Karimi, N; Keshavarzi, F; Nowrouzi, F, 2023)
"Repaglinide is an insulin secretagogue with a low hypoglycemic risk because of its rapid- and short-acting effects."	( Fujii, K; Hazama, Y; Kosugi, M; Miyoshi, Y; Nagata, S; Obata, Y; Takayama, K; Uehara, Y; Yamaguchi, H; Yasuda, T, 2021)
"Repaglinide is a hypoglycemic drug, causing depolarization of the cell membrane, opening the voltage-gated calcium channels, and then increasing intracellular calcium in the pancreatic B cells by inhibition of the K-ATP-sensitive channels. "	( Azadbakht, M; Kalehoei, E, 2017)
"Repaglinide (RG) is a prandial glucose regulator used for the treatment of type 2 diabetes. "	( Li, H; Li, J; Li, Q; Xue, Y, 2018)
"Repaglinide (RPG) is a short-acting insulin secretagogue widely prescribed for the treatment of type 2 diabetes. "	( Chen, L; Ding, D; Kang, Y; Wang, M; Wu, JX, 2019)
"Repaglinide is a short-acting insulin secretagogue, which often results in considerable interindividual variability in therapeutic efficacy when widely used in a clinical setting. "	( Cui, YW; Guo, H; Li, W; Lu, Q; Lv, DM; Song, JF; Wang, DD; Wang, T; Wang, Y; Yin, XX; Zhang, F; Zhou, XY; Zhu, J, 2015)
"Repaglinide (RG) is an efficient antihyperglycemic drug; however, due to its short half-life, patients are required to take the marketed products several times a day, which compromises the therapeutic effects. "	( He, W; Huang, S; Wu, M; Yin, L, 2015)
"Repaglinide is an efficient anti-diabetic drug which is prescribed widely as multi-dosage oral daily regimens. "	( Ebrahimi, HA; Hamidi, M; Jalali, MB; Javadzadeh, Y, 2015)
"Repaglinide is a short-acting insulin secretagogue with high interindividual variability in pharmacokinetics due to genetic polymorphisms. "	( Auwaerter, V; Elling, R; Hermanns-Clausen, M; Spehl, MS; Wohlfarth, A, 2016)
"Repaglinide (RPG) is a fast-acting prandial glucose regulator. "	( Akhtar, J; Aqil, M; Fareed, S; Khalid, M; Siddiqui, HH, 2016)
"Repaglinide is an insulin secretagogue that often exhibits considerable interindividual variability in therapeutic efficacy. "	( Adelusi, TI; Bao, Z; Li, W; Lu, Q; Lv, D; Shang, Z; Song, J; Sun, J; Wang, T; Wang, Y; Yin, X; Zhou, X; Zhu, J, 2016)
"Repaglinide (RPG) is an oral hypoglycemic agent with excellent bioavailability (90-98%) and a short plasma half-life (2-6 h). "	( Jain, S; Saraf, S, 2009)
"Repaglinide is an FDA-approved treatment for type 2 diabetes mellitus. "	( Cheung, PH; Ciallella, J; Saha, S; Tung, D, 2011)
"Repaglinide is a short-acting, oral, insulin secretagogue that is used in the treatment of type 2 diabetes mellitus."	( Reddy, PJ; Sekhar, MC, 2012)
"Repaglinide is an oral anti-diabetic agent that has a short duration of action, and is suitable for preventing post-prandial rises in glucose levels. "	( Garon, J; Gerstein, HC; Joyce, C; Rolfe, A; Walter, CM, 2004)
"Repaglinide is an effective oral hypoglycemic agent taken either as monotherapy or combination therapy. "	( Abrams, Z; Lieberman, N; Shapiro, MS, 2005)
"Repaglinide is a new oral antidiabetic agent with a possible antioxidant activity."	( Bojarska-Junak, A; Gumieniczek, A; Hopkała, H; Roliński, J, 2005)
"Repaglinide is an antidiabetic drug metabolised by cytochrome P450 (CYP) 2C8 and CYP3A4 enzymes. "	( Backman, JT; Kajosaari, LI; Laitila, J; Neuvonen, PJ, 2005)
"Repaglinide is an antidiabetic drug metabolized by cytochrome P450 (CYP) 2 C 8 and 3A4, and it appears to be a substrate of the hepatic uptake transporter organic anion transporting polypeptide 1B1 (OATP1B1). "	( Backman, JT; Kajosaari, LI; Laitila, J; Neuvonen, M; Neuvonen, PJ; Niemi, M, 2005)
"Repaglinide is a prandial glucose regulator indicated for management of type 2 diabetes. "	( Marshall, V; Shakir, S; Wilton, L, 2006)
"Repaglinide is an insulin secretagogue that lowers blood glucose levels in patients with T2DM."	( Birkeland, KI; Johansen, OE, 2007)
"Repaglinide is a novel insulin secretagogue being developed for the management of type 2 (non-insulin-dependent) diabetes mellitus. "	( Balfour, JA; Faulds, D, 1998)
"Repaglinide is a novel prandial glucose regulator (PGR) for the treatment of type 2 diabetes. "	( Hatorp, V; Oliver, S; Su, CA, 1998)
"Repaglinide is a newly developed oral blood glucose-lowering agent that exerts its effect by stimulating insulin secretion. "	( Landgraf, R; Wolffenbuttel, BH, 1999)
"Repaglinide is a safe and efficacious oral blood glucose-lowering agent, with a potency similar to that of glyburide. "	( Landgraf, R; Wolffenbuttel, BH, 1999)
"Repaglinide is a new carbamoylmethyl benzoic acid derivative that is structurally related to meglitinide. "	( Malaisse, WJ, 1999)
"Repaglinide is a novel, rapid-acting prandial glucose regulator. "	( Clauson, P; Damsbo, P; Hatorp, V; Marbury, TC; Müller, PG, 1999)
"Repaglinide is a new oral blood glucose lowering agent, a member of the carbamoylmethyl benzoic acid (CMBA) family. "	( Wolffenbuttel, BH, 1999)
"Repaglinide is a novel insulin secretagogue developed in response to the need for a fast-acting, oral prandial glucose regulator for the treatment of type 2 (non-insulin-dependent) diabetes mellitus. "	( Christensen, MS; Hatorp, V; Haug-Pihale, G; Walther, KH, 2000)
"Repaglinide is a novel oral antidiabetic agent, marking the development of a new class of drugs for type 2 diabetes. "	( Nattrass, M, 2000)
"Repaglinide is a new oral hypoglycemic agent that acts as a prandial glucose regulator proposed for the treatment of type 2 diabetes by stimulating insulin secretion. "	( Dejgaard, A; Hollingdal, M; Juhl, CB; Pincus, S; Pørksen, N; Schmitz, O; Sturis, J; Veldhuis, JD, 2000)
"Repaglinide is a suitable agent for first-line monotherapy in patients whose glucose metabolism cannot be optimally controlled by increasing physical activity and appropriate dietary measures."	( Landgraf, R, 2000)
"Repaglinide is a novel insulin secretagogue that was developed as a prandial glucose regulator for the treatment of people with Type 2 diabetes mellitus. "	( Moses, R, 2000)
"Repaglinide (NovoNorm) is an antidiabetic oral agent of the new glinide class with insulinotropic activity. "	( Scheen, AJ, 2001)
"Repaglinide is an insulin secretion enhancer with a different mechanism of action to the sulphonylureas, which means it does not continuously stimulate insulin secretion."	( Rutten, GE, 2001)
"Repaglinide is a novel, fast-acting prandial oral hypoglycaemic agent developed for the treatment of patients with type 2 diabetes whose disease cannot be controlled by diet and exercise alone. "	( Hatorp, V, 2002)

Excerpt	Reference
"Repaglinide has a good safety and efficacy profile in type 2 diabetic patients complicated by renal impairment and is an appropriate treatment choice, even for individuals with more severe degrees of renal impairment."	( Hasslacher, C, 2003)
"Repaglinide has an equivalent safety and efficacy profile to the sulphonylureas, although it is superior to glipizide in maintaining long-term glycaemic control The postprandial glucose levels are significantly lower with repaglinide compared with glibenclamide."	( Owens, DR, 1999)
"Repaglinide has no significant inhibitory effect on the metabolism of pioglitazone in vivo, which is inconsistent with the in vitro results. "	( Qian, W; Tang, L; Xiao, Q; Xu, R; Yang, J, 2015)
"Repaglinide has a good safety and efficacy profile in type 2 diabetic patients complicated by renal impairment and is an appropriate treatment choice, even for individuals with more severe degrees of renal impairment."	( Hasslacher, C, 2003)
"Repaglinide has minimal physiological advantage over gliclazide, but both therapies for type 2 diabetes fall far short of correcting the endocrine and metabolic abnormalities."	( Caumo, A; Cobelli, C; Singhal, P; Taylor, R, 2005)
"Repaglinide has primarily a role in the treatment of T2DM when metformin cannot be used due to adverse effects, when metformin fails to adequately control blood glucose levels, when there is a need for flexible dosing (i.e."	( Birkeland, KI; Johansen, OE, 2007)
"Repaglinide has an equivalent safety and efficacy profile to the sulphonylureas, although it is superior to glipizide in maintaining long-term glycaemic control The postprandial glucose levels are significantly lower with repaglinide compared with glibenclamide."	( Owens, DR, 1999)
"Repaglinide has few contraindications or drug interactions and can be used in a wide range of patients."	( McDougall, A; Owens, DR, 2000)
"Repaglinide has been found to be particularly effective in sulphonylurea-naïve patients."	( Rutten, GE, 2001)

Excerpt	Reference
"Repaglinide and metformin enhance insulin secretion and decrease hepatic gluconeogenesis, respectively, and are commonly coadministered as separate formulations to treat patients with type 2 diabetes mellitus. "	( Chu, PL; Hoelscher, D; Lyness, W, 2008)
"Repaglinide does not cause insulin release in the absence of exogenous glucose, nor does it inhibit the biosynthesis of proinsulin."	( Malaisse, WJ, 1999)

Excerpt	Reference
"Repaglinide plus acarbose treatment significantly reduced the mean increase in postprandial blood glucose levels (24.2+/-18.2 mg/dl) compared to repaglinide alone (51.1+/-29.0 mg/dl; p<0.001)."	( Hofmann, U; Paulwitz, O; Rosak, C, 2004)
"Repaglinide treatment reduced fasting ADP-induced P-selectin expression compared with baseline (P = 0.01), but did not influence meal-induced platelet hyper-reactivity (P = 0.32)."	( Hjemdahl, P; Ostenson, CG; Wallén, NH; Yngen, M, 2006)
"repaglinide treatment for 2 x 4 months."	( Frandsen, M; Lund, SS; Parving, HH; Pedersen, O; Schalkwijk, CG; Smidt, UM; Stehouwer, CD; Tarnow, L; Vaag, A, 2007)
"pretreatment with repaglinide attenuated the KA-induced neuronal cell death in CA3 region of the hippocampus and hyperglycemia."	( Jung, JS; Kim, CH; Kim, SJ; Kim, SS; Lim, SM; Park, SH; Sim, YB; Suh, HW, 2014)
"Treatment with repaglinide significantly improved glycemic control with respect to baseline and placebo, reducing HbA1c by 1.14% from baseline and fasting plasma glucose by 1.8 mmol/l. "	( Dedov, I; Frandsen, KB; Gomis, R; Moses, RG; Schlienger, JL, 2001)
"Treatment with repaglinide produced a sustained hypoglycemic effect up to 6 h postdose."	( Kalbag, JB; McLeod, JF; Nedelman, JR; Walter, YH, 2001)

Class	Description
piperidines
[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
Repaglinide Action Pathway	6	5

Protein	Taxonomy	Measurement	Average (µ)	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Chain A, Putative fructose-1,6-bisphosphate aldolase	Giardia intestinalis	Potency	17.7407	0.1409	11.1940	39.8107	AID2451
Luciferase	Photinus pyralis (common eastern firefly)	Potency	8.4921	0.0072	15.7588	89.3584	AID588342
AR protein	Homo sapiens (human)	Potency	10.1683	0.0002	21.2231	8,912.5098	AID743040; AID743042; AID743054
cytochrome P450 family 3 subfamily A polypeptide 4	Homo sapiens (human)	Potency	9.5221	0.0123	7.9835	43.2770	AID1645841
EWS/FLI fusion protein	Homo sapiens (human)	Potency	0.5258	0.0013	10.1577	42.8575	AID1259255
glucocorticoid receptor [Homo sapiens]	Homo sapiens (human)	Potency	6.9255	0.0002	14.3764	60.0339	AID720691; AID720719
peroxisome proliferator activated receptor gamma	Homo sapiens (human)	Potency	8.7567	0.0010	19.4141	70.9645	AID743140
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_a	Homo sapiens (human)	Potency	10.1235	0.0017	23.8393	78.1014	AID743083
vitamin D3 receptor isoform VDRA	Homo sapiens (human)	Potency	11.2202	0.3548	28.0659	89.1251	AID504847
nuclear factor erythroid 2-related factor 2 isoform 2	Homo sapiens (human)	Potency	23.1093	0.0041	9.9848	25.9290	AID504444
mitogen-activated protein kinase 1	Homo sapiens (human)	Potency	6.3096	0.0398	16.7842	39.8107	AID1454
nuclear receptor ROR-gamma isoform 1	Mus musculus (house mouse)	Potency	35.4813	0.0079	8.2332	1,122.0200	AID2551
cytochrome P450 3A4 isoform 1	Homo sapiens (human)	Potency	12.5893	0.0316	10.2792	39.8107	AID884; AID885
histone acetyltransferase KAT2A isoform 1	Homo sapiens (human)	Potency	11.2202	0.2512	15.8432	39.8107	AID504327
lamin isoform A-delta10	Homo sapiens (human)	Potency	0.3981	0.8913	12.0676	28.1838	AID1487
Gamma-aminobutyric acid receptor subunit pi	Rattus norvegicus (Norway rat)	Potency	12.5893	1.0000	12.2248	31.6228	AID885
Gamma-aminobutyric acid receptor subunit beta-1	Rattus norvegicus (Norway rat)	Potency	12.5893	1.0000	12.2248	31.6228	AID885
Gamma-aminobutyric acid receptor subunit delta	Rattus norvegicus (Norway rat)	Potency	12.5893	1.0000	12.2248	31.6228	AID885
Gamma-aminobutyric acid receptor subunit gamma-2	Rattus norvegicus (Norway rat)	Potency	12.5893	1.0000	12.2248	31.6228	AID885
Gamma-aminobutyric acid receptor subunit alpha-5	Rattus norvegicus (Norway rat)	Potency	12.5893	1.0000	12.2248	31.6228	AID885
Gamma-aminobutyric acid receptor subunit alpha-3	Rattus norvegicus (Norway rat)	Potency	12.5893	1.0000	12.2248	31.6228	AID885
Gamma-aminobutyric acid receptor subunit gamma-1	Rattus norvegicus (Norway rat)	Potency	12.5893	1.0000	12.2248	31.6228	AID885
Gamma-aminobutyric acid receptor subunit alpha-2	Rattus norvegicus (Norway rat)	Potency	12.5893	1.0000	12.2248	31.6228	AID885
Gamma-aminobutyric acid receptor subunit alpha-4	Rattus norvegicus (Norway rat)	Potency	12.5893	1.0000	12.2248	31.6228	AID885
Gamma-aminobutyric acid receptor subunit gamma-3	Rattus norvegicus (Norway rat)	Potency	12.5893	1.0000	12.2248	31.6228	AID885
Gamma-aminobutyric acid receptor subunit alpha-6	Rattus norvegicus (Norway rat)	Potency	12.5893	1.0000	12.2248	31.6228	AID885
Gamma-aminobutyric acid receptor subunit alpha-1	Rattus norvegicus (Norway rat)	Potency	12.5893	1.0000	12.2248	31.6228	AID885
Gamma-aminobutyric acid receptor subunit beta-3	Rattus norvegicus (Norway rat)	Potency	12.5893	1.0000	12.2248	31.6228	AID885
Guanine nucleotide-binding protein G	Homo sapiens (human)	Potency	31.6228	1.9953	25.5327	50.1187	AID624288
Gamma-aminobutyric acid receptor subunit beta-2	Rattus norvegicus (Norway rat)	Potency	12.5893	1.0000	12.2248	31.6228	AID885
Rap guanine nucleotide exchange factor 4	Homo sapiens (human)	Potency	35.4813	3.9811	46.7448	112.2020	AID720708
GABA theta subunit	Rattus norvegicus (Norway rat)	Potency	12.5893	1.0000	12.2248	31.6228	AID885
Gamma-aminobutyric acid receptor subunit epsilon	Rattus norvegicus (Norway rat)	Potency	12.5893	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)	9.2000	0.2100	5.5537	10.0000	AID386625
ATP-binding cassette sub-family C member 3	Homo sapiens (human)	IC50 (µMol)	16.7000	0.6315	4.4531	9.3000	AID1473740
Multidrug resistance-associated protein 4	Homo sapiens (human)	IC50 (µMol)	53.9000	0.2000	5.6774	10.0000	AID1473741
Bile salt export pump	Homo sapiens (human)	IC50 (µMol)	22.0000	0.1100	7.1903	10.0000	AID1473738
5-hydroxytryptamine receptor 7	Cavia porcellus (domestic guinea pig)	IC50 (µMol)	9.2000	2.0300	5.5313	9.9000	AID386625
ATP-binding cassette sub-family C member 8	Homo sapiens (human)	IC50 (µMol)	0.1060	0.0043	1.0703	8.2000	AID242637
Canalicular multispecific organic anion transporter 1	Homo sapiens (human)	IC50 (µMol)	72.3000	2.4100	6.3433	10.0000	AID1473739
[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)
ATP-binding cassette sub-family C member 8	Homo sapiens (human)	Kd	0.0500	0.0500	0.0500	0.0500	AID238081
[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	27.8500	1.9300	5.9060	8.7000	AID1213578; AID1213614
Cytochrome P450 2C8	Homo sapiens (human)	Km	15.3500	0.0500	2.9825	5.7000	AID1213580; AID1213616
[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)
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)
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)
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)
lipid hydroxylation	Cytochrome P450 2C8	Homo sapiens (human)
organic acid metabolic process	Cytochrome P450 2C8	Homo sapiens (human)
xenobiotic metabolic process	Cytochrome P450 2C8	Homo sapiens (human)
steroid metabolic process	Cytochrome P450 2C8	Homo sapiens (human)
estrogen metabolic process	Cytochrome P450 2C8	Homo sapiens (human)
epoxygenase P450 pathway	Cytochrome P450 2C8	Homo sapiens (human)
xenobiotic catabolic process	Cytochrome P450 2C8	Homo sapiens (human)
retinol metabolic process	Cytochrome P450 2C8	Homo sapiens (human)
retinoic acid metabolic process	Cytochrome P450 2C8	Homo sapiens (human)
long-chain fatty acid biosynthetic process	Cytochrome P450 2C8	Homo sapiens (human)
icosanoid biosynthetic process	Cytochrome P450 2C8	Homo sapiens (human)
oxidative demethylation	Cytochrome P450 2C8	Homo sapiens (human)
omega-hydroxylase P450 pathway	Cytochrome P450 2C8	Homo sapiens (human)
lipid hydroxylation	Cytochrome P450 3A5	Homo sapiens (human)
xenobiotic metabolic process	Cytochrome P450 3A5	Homo sapiens (human)
steroid metabolic process	Cytochrome P450 3A5	Homo sapiens (human)
estrogen metabolic process	Cytochrome P450 3A5	Homo sapiens (human)
alkaloid catabolic process	Cytochrome P450 3A5	Homo sapiens (human)
xenobiotic catabolic process	Cytochrome P450 3A5	Homo sapiens (human)
retinol metabolic process	Cytochrome P450 3A5	Homo sapiens (human)
retinoic acid metabolic process	Cytochrome P450 3A5	Homo sapiens (human)
aflatoxin metabolic process	Cytochrome P450 3A5	Homo sapiens (human)
oxidative demethylation	Cytochrome P450 3A5	Homo sapiens (human)
negative regulation of inflammatory response to antigenic stimulus	Guanine nucleotide-binding protein G	Homo sapiens (human)
renal water homeostasis	Guanine nucleotide-binding protein G	Homo sapiens (human)
G protein-coupled receptor signaling pathway	Guanine nucleotide-binding protein G	Homo sapiens (human)
regulation of insulin secretion	Guanine nucleotide-binding protein G	Homo sapiens (human)
cellular response to glucagon stimulus	Guanine nucleotide-binding protein G	Homo sapiens (human)
intracellular glucose homeostasis	ATP-binding cassette sub-family C member 8	Homo sapiens (human)
potassium ion transport	ATP-binding cassette sub-family C member 8	Homo sapiens (human)
female pregnancy	ATP-binding cassette sub-family C member 8	Homo sapiens (human)
memory	ATP-binding cassette sub-family C member 8	Homo sapiens (human)
visual learning	ATP-binding cassette sub-family C member 8	Homo sapiens (human)
response to pH	ATP-binding cassette sub-family C member 8	Homo sapiens (human)
response to xenobiotic stimulus	ATP-binding cassette sub-family C member 8	Homo sapiens (human)
response to zinc ion	ATP-binding cassette sub-family C member 8	Homo sapiens (human)
negative regulation of low-density lipoprotein particle clearance	ATP-binding cassette sub-family C member 8	Homo sapiens (human)
negative regulation of angiogenesis	ATP-binding cassette sub-family C member 8	Homo sapiens (human)
response to lipopolysaccharide	ATP-binding cassette sub-family C member 8	Homo sapiens (human)
positive regulation of tumor necrosis factor production	ATP-binding cassette sub-family C member 8	Homo sapiens (human)
response to insulin	ATP-binding cassette sub-family C member 8	Homo sapiens (human)
positive regulation of insulin secretion involved in cellular response to glucose stimulus	ATP-binding cassette sub-family C member 8	Homo sapiens (human)
positive regulation of potassium ion transport	ATP-binding cassette sub-family C member 8	Homo sapiens (human)
negative regulation of insulin secretion	ATP-binding cassette sub-family C member 8	Homo sapiens (human)
neuromuscular process	ATP-binding cassette sub-family C member 8	Homo sapiens (human)
negative regulation of glial cell proliferation	ATP-binding cassette sub-family C member 8	Homo sapiens (human)
glutamate secretion, neurotransmission	ATP-binding cassette sub-family C member 8	Homo sapiens (human)
negative regulation of neuroblast migration	ATP-binding cassette sub-family C member 8	Homo sapiens (human)
cellular response to organic substance	ATP-binding cassette sub-family C member 8	Homo sapiens (human)
potassium ion transmembrane transport	ATP-binding cassette sub-family C member 8	Homo sapiens (human)
inorganic cation transmembrane transport	ATP-binding cassette sub-family C member 8	Homo sapiens (human)
positive regulation of uterine smooth muscle relaxation	ATP-binding cassette sub-family C member 8	Homo sapiens (human)
positive regulation of tight junction disassembly	ATP-binding cassette sub-family C member 8	Homo sapiens (human)
negative regulation of blood-brain barrier permeability	ATP-binding cassette sub-family C member 8	Homo sapiens (human)
potassium ion import across plasma membrane	ATP-binding cassette sub-family C member 8	Homo sapiens (human)
transmembrane transport	ATP-binding cassette sub-family C member 8	Homo sapiens (human)
adaptive immune response	Rap guanine nucleotide exchange factor 4	Homo sapiens (human)
G protein-coupled receptor signaling pathway	Rap guanine nucleotide exchange factor 4	Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathway	Rap guanine nucleotide exchange factor 4	Homo sapiens (human)
calcium-ion regulated exocytosis	Rap guanine nucleotide exchange factor 4	Homo sapiens (human)
regulation of exocytosis	Rap guanine nucleotide exchange factor 4	Homo sapiens (human)
insulin secretion	Rap guanine nucleotide exchange factor 4	Homo sapiens (human)
positive regulation of insulin secretion	Rap guanine nucleotide exchange factor 4	Homo sapiens (human)
regulation of synaptic vesicle cycle	Rap guanine nucleotide exchange factor 4	Homo sapiens (human)
Ras protein signal transduction	Rap guanine nucleotide exchange factor 4	Homo sapiens (human)
regulation of insulin secretion	Rap guanine nucleotide exchange factor 4	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)
[Information is prepared from geneontology information from the June-17-2024 release]

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)
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)
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)
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 2C8	Homo sapiens (human)
iron ion binding	Cytochrome P450 2C8	Homo sapiens (human)
protein binding	Cytochrome P450 2C8	Homo sapiens (human)
arachidonic acid epoxygenase activity	Cytochrome P450 2C8	Homo sapiens (human)
retinoic acid 4-hydroxylase activity	Cytochrome P450 2C8	Homo sapiens (human)
caffeine oxidase activity	Cytochrome P450 2C8	Homo sapiens (human)
aromatase activity	Cytochrome P450 2C8	Homo sapiens (human)
estrogen 16-alpha-hydroxylase activity	Cytochrome P450 2C8	Homo sapiens (human)
heme binding	Cytochrome P450 2C8	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 2C8	Homo sapiens (human)
monooxygenase activity	Cytochrome P450 3A5	Homo sapiens (human)
iron ion binding	Cytochrome P450 3A5	Homo sapiens (human)
protein binding	Cytochrome P450 3A5	Homo sapiens (human)
retinoic acid 4-hydroxylase activity	Cytochrome P450 3A5	Homo sapiens (human)
oxidoreductase activity	Cytochrome P450 3A5	Homo sapiens (human)
oxygen binding	Cytochrome P450 3A5	Homo sapiens (human)
heme binding	Cytochrome P450 3A5	Homo sapiens (human)
aromatase activity	Cytochrome P450 3A5	Homo sapiens (human)
estrogen 16-alpha-hydroxylase activity	Cytochrome P450 3A5	Homo sapiens (human)
testosterone 6-beta-hydroxylase activity	Cytochrome P450 3A5	Homo sapiens (human)
G protein activity	Guanine nucleotide-binding protein G	Homo sapiens (human)
adenylate cyclase activator activity	Guanine nucleotide-binding protein G	Homo sapiens (human)
ATP-activated inward rectifier potassium channel activity	ATP-binding cassette sub-family C member 8	Homo sapiens (human)
potassium channel activity	ATP-binding cassette sub-family C member 8	Homo sapiens (human)
ATP binding	ATP-binding cassette sub-family C member 8	Homo sapiens (human)
sulfonylurea receptor activity	ATP-binding cassette sub-family C member 8	Homo sapiens (human)
ATP-activated inward rectifier potassium channel activity	ATP-binding cassette sub-family C member 8	Homo sapiens (human)
ATP hydrolysis activity	ATP-binding cassette sub-family C member 8	Homo sapiens (human)
ATPase-coupled monoatomic cation transmembrane transporter activity	ATP-binding cassette sub-family C member 8	Homo sapiens (human)
ADP binding	ATP-binding cassette sub-family C member 8	Homo sapiens (human)
transmembrane transporter binding	ATP-binding cassette sub-family C member 8	Homo sapiens (human)
ABC-type transporter activity	ATP-binding cassette sub-family C member 8	Homo sapiens (human)
ATPase-coupled transmembrane transporter activity	ATP-binding cassette sub-family C member 8	Homo sapiens (human)
guanyl-nucleotide exchange factor activity	Rap guanine nucleotide exchange factor 4	Homo sapiens (human)
protein binding	Rap guanine nucleotide exchange factor 4	Homo sapiens (human)
cAMP binding	Rap guanine nucleotide exchange factor 4	Homo sapiens (human)
protein-macromolecule adaptor activity	Rap guanine nucleotide exchange factor 4	Homo sapiens (human)
small GTPase binding	Rap guanine nucleotide exchange factor 4	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)
[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)
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)
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)
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 2C8	Homo sapiens (human)
plasma membrane	Cytochrome P450 2C8	Homo sapiens (human)
intracellular membrane-bounded organelle	Cytochrome P450 2C8	Homo sapiens (human)
cytoplasm	Cytochrome P450 2C8	Homo sapiens (human)
intracellular membrane-bounded organelle	Cytochrome P450 2C8	Homo sapiens (human)
plasma membrane	Gamma-aminobutyric acid receptor subunit gamma-2	Rattus norvegicus (Norway rat)
endoplasmic reticulum membrane	Cytochrome P450 3A5	Homo sapiens (human)
intracellular membrane-bounded organelle	Cytochrome P450 3A5	Homo sapiens (human)
plasma membrane	Gamma-aminobutyric acid receptor subunit alpha-1	Rattus norvegicus (Norway rat)
plasma membrane	Guanine nucleotide-binding protein G	Homo sapiens (human)
plasma membrane	Gamma-aminobutyric acid receptor subunit beta-2	Rattus norvegicus (Norway rat)
plasma membrane	ATP-binding cassette sub-family C member 8	Homo sapiens (human)
inward rectifying potassium channel	ATP-binding cassette sub-family C member 8	Homo sapiens (human)
synaptic vesicle membrane	ATP-binding cassette sub-family C member 8	Homo sapiens (human)
sarcolemma	ATP-binding cassette sub-family C member 8	Homo sapiens (human)
potassium ion-transporting ATPase complex	ATP-binding cassette sub-family C member 8	Homo sapiens (human)
membrane	ATP-binding cassette sub-family C member 8	Homo sapiens (human)
cytosol	Rap guanine nucleotide exchange factor 4	Homo sapiens (human)
plasma membrane	Rap guanine nucleotide exchange factor 4	Homo sapiens (human)
membrane	Rap guanine nucleotide exchange factor 4	Homo sapiens (human)
hippocampal mossy fiber to CA3 synapse	Rap guanine nucleotide exchange factor 4	Homo sapiens (human)
plasma membrane	Rap guanine nucleotide exchange factor 4	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)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (352)

Assay ID	Title	Year	Journal	Article
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.
AID1346986	P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen	2019	Molecular pharmacology, 11, Volume: 96, Issue:5	A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346987	P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen	2019	Molecular pharmacology, 11, Volume: 96, Issue:5	A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID651635	Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
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.
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.
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.
AID1213537	Fraction metabolism via UGT in human liver microsomes	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
AID1213581	Unbound intrinsic clearance in human hepatocytes assessed as 2-despiperidyl-2-amino repaglinide formation measured per 10'6 cells at 0.5 to 150 uM by LC-MS/MS method	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
AID1213592	Activity of human recombinant CYP2C8 expressed in insect cells assessed as enzyme-mediated 2-despiperidyl-2-(5-carboxypentylamine) repaglinide formation per picomole of protein at 0.5 to 150 uM by LC-MS/MS method	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
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).
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.
AID1213583	Unbound intrinsic clearance in human hepatic S9 fraction assessed as 2-despiperidyl-2-amino repaglinide formation measured per mg of protein at 0.5 to 150 uM by LC-MS/MS method	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
AID1213530	Fraction metabolism via CYP3A4 in human hepatocytes	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
AID1221986	Mean change in blood glucose concentration in healthy white human plasma with CYP2C81/1 genotype at 2 mg, po up to 6 hrs	2011	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5	Effect of the CYP2C8 genotype on the pharmacokinetics and pharmacodynamics of repaglinide.
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
AID598526	1-Octanol-water distribution coefficient, log D of the compound at pH 7.4 by shake-flask method	2011	Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12	Lipophilicity of acidic compounds: impact of ion pair partitioning on drug design.
AID1698007	Ratio of drug level in human blood to plasma administered through iv dosing by LC-MS/MS analysis
AID1222066	Maximal change in insulin concentration in healthy white human plasma with CYP2C81/1 genotype at 2 mg, po up to 6 hrs	2011	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5	Effect of the CYP2C8 genotype on the pharmacokinetics and pharmacodynamics of repaglinide.
AID1213534	Fraction metabolism via UGT in human hepatic S9 fraction	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
AID1222028	Cmax in healthy white human with CYP2C81/3 genotype at 2 mg, po	2011	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5	Effect of the CYP2C8 genotype on the pharmacokinetics and pharmacodynamics of repaglinide.
AID1213621	Unbound intrinsic clearance in human recombinant CYP3A5 expressed in insect cells assessed as enzyme-mediated 3'-hydroxy repaglinide formation per nanomole of protein at 0.5 to 150 uM by LC-MS/MS method	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
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.
AID1213591	Activity of human recombinant CYP3A5 expressed in insect cells assessed as enzyme-mediated 2-despiperidyl-2-(5-carboxypentylamine) repaglinide formation per picomole of protein at 0.5 to 150 uM by LC-MS/MS method	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
AID1222017	Mean change in blood glucose concentration in healthy white human plasma SLCO1B1 521CC/CYP2C81/3 combined genotype at 2 mg, po	2011	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5	Effect of the CYP2C8 genotype on the pharmacokinetics and pharmacodynamics of repaglinide.
AID1079944	Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID1221989	Maximal change in blood glucose concentration in healthy white human plasma at 2 mg, po up to 6 hrs	2011	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5	Effect of the CYP2C8 genotype on the pharmacokinetics and pharmacodynamics of repaglinide.
AID1222001	Mean change in insulin concentration in healthy white human plasma with SLCO1B1 521TC/CYP2C81/1 combined genotype at 2 mg, po	2011	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5	Effect of the CYP2C8 genotype on the pharmacokinetics and pharmacodynamics of repaglinide.
AID1581633	Antidiabetic activity in glucose-treated rat INS1(832/13) cells assessed as increase in insulin release in presence of 3 mM glucose measured after 2 hrs by radioimmunoassay	2020	European journal of medicinal chemistry, Feb-01, Volume: 187	Synthesis and discovery of triazolo-pyridazine-6-yl-substituted piperazines as effective anti-diabetic drugs; evaluated over dipeptidyl peptidase-4 inhibition mechanism and insulinotropic activities.
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).
AID1222044	Mean change in blood glucose concentration in healthy white human plasma SLCO1B1 521TC/CYP2C83/3 combined genotype at 2 mg, po	2011	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5	Effect of the CYP2C8 genotype on the pharmacokinetics and pharmacodynamics of repaglinide.
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.
AID1213561	Ratio of AUC in human patient at 0.25 mg to AUC in human patient at 0.25 mg co-treated with gemfibrozil and itraconazole	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
AID588962	Substrates of transporters of clinical importance in the absorption and disposition of drugs, OATP1B1	2010	Nature reviews. Drug discovery, Mar, Volume: 9, Issue:3	Membrane transporters in drug development.
AID1698011	Fraction unbound in human plasma
AID1473814	AUC in human at 0.5 to 4 mg, po BID/TID/QID after 6 hrs	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.
AID1213513	Drug metabolism in human patient assessed as fold change in metabolite M2/M4 AUC ratio at 0.25 mg co-treated with atorvastatin relative to atorvastatin non-treated patient	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
AID1213626	Drug metabolism in human hepatic S9 fraction assessed as 2-despiperidyl-2-amino repaglinide formation measured per mg of protein at 0.5 to 150 uM by LC-MS/MS method	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
AID1079949	Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID1213622	Unbound intrinsic clearance in human recombinant CYP2C8 expressed in insect cells assessed as enzyme-mediated 3'-hydroxy repaglinide formation per nanomole of protein at 0.5 to 150 uM by LC-MS/MS method	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
AID1221997	Mean change in blood glucose concentration in healthy white human plasma SLCO1B1 521TT/CYP2C81/1 combined genotype at 2 mg, po	2011	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5	Effect of the CYP2C8 genotype on the pharmacokinetics and pharmacodynamics of repaglinide.
AID1222009	Cmax in healthy white human with SLCO1B1 521TC/CYP2C81/3 combined genotype at 2 mg, po	2011	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5	Effect of the CYP2C8 genotype on the pharmacokinetics and pharmacodynamics of repaglinide.
AID1213510	Drug metabolism in human patient assessed as fold change in metabolite M2/M1 AUC ratio at 0.25 mg co-treated with montelukast relative to montelukast non-treated patient	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
AID1213567	Ratio of AUC in human patient at 0.25 mg to AUC in human patient at 0.25 mg co-treated with telithromycin and montelukast	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
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.
AID1221987	Mean change in blood glucose concentration in healthy white human plasma with CYP2C81/3 genotype at 2 mg, po up to 6 hrs	2011	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5	Effect of the CYP2C8 genotype on the pharmacokinetics and pharmacodynamics of repaglinide.
AID1698016	Dissociation constant, basic pKa of compound measured up to 18 mins by capillary electrophoresis
AID1221991	Maximal change in blood glucose concentration in healthy white human plasma with CYP2C81/3 genotype at 2 mg, po up to 6 hrs	2011	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5	Effect of the CYP2C8 genotype on the pharmacokinetics and pharmacodynamics of repaglinide.
AID1222011	Mean change in insulin concentration in healthy white human plasma with SLCO1B1 521TC/CYP2C81/3 combined genotype at 2 mg, po	2011	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5	Effect of the CYP2C8 genotype on the pharmacokinetics and pharmacodynamics of repaglinide.
AID1079948	Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID1213521	Drug metabolism in human liver microsomes assessed as glucuronide formation by LC-MS/MS method	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
AID1473817	Ratio of drug concentration at steady state in human at 0.5 to 4 mg, po BID/TID/QID after 6 hrs to IC50 for human MRP2 overexpressed in Sf9 insect cells	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.
AID1222024	AUC (0 to infinity) in healthy white human with CYP2C81/3 genotype at 2 mg, po	2011	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5	Effect of the CYP2C8 genotype on the pharmacokinetics and pharmacodynamics of repaglinide.
AID1222016	Mean change in insulin concentration in healthy white human plasma with SLCO1B1 521CC/CYP2C81/3 combined genotype at 2 mg, po	2011	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5	Effect of the CYP2C8 genotype on the pharmacokinetics and pharmacodynamics of repaglinide.
AID1079946	Presence of at least one case with successful reintroduction. [column 'REINT' in source]
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.
AID1221983	Maximal change in insulin concentration in healthy white human plasma with CYP2C81/3 genotype at 2 mg, po up to 6 hrs	2011	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5	Effect of the CYP2C8 genotype on the pharmacokinetics and pharmacodynamics of repaglinide.
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.
AID1213533	Fraction metabolism via CYP3A4 in human hepatic S9 fraction	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
AID1222012	Mean change in blood glucose concentration in healthy white human plasma SLCO1B1 521TC/CYP2C81/3 combined genotype at 2 mg, po	2011	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5	Effect of the CYP2C8 genotype on the pharmacokinetics and pharmacodynamics of repaglinide.
AID1213532	Fraction metabolism via CYP2C8 in human hepatic S9 fraction	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
AID1222052	Mean change in insulin concentration in healthy white human plasma at 2 mg, po up to 6 hrs	2011	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5	Effect of the CYP2C8 genotype on the pharmacokinetics and pharmacodynamics of repaglinide.
AID1213566	Ratio of AUC in human patient at 0.25 mg to AUC in human patient at 0.25 mg co-treated with telithromycin	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
AID1591620	Antihyperglycemic activity in alloxan-induced diabetic BALB/c mouse model assessed as blood glucose level at 10 mg/kg measured after 8 hrs by glucometry analysis	2019	Bioorganic & medicinal chemistry, 08-01, Volume: 27, Issue:15	Synthesis and molecular modeling of novel non-sulfonylureas as hypoglycemic agents and selective ALR2 inhibitors.
AID1213615	Activity of human recombinant CYP3A5 expressed in insect cells assessed as enzyme-mediated 3'-hydroxy repaglinide formation by LC-MS/MS method	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
AID1222041	Cmax in healthy white human with SLCO1B1 521TC/CYP2C83/3 combined genotype at 2 mg, po	2011	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5	Effect of the CYP2C8 genotype on the pharmacokinetics and pharmacodynamics of repaglinide.
AID1213602	Unbound intrinsic clearance in human recombinant CYP3A4 expressed in insect cells assessed as enzyme-mediated 2-despiperidyl-2-(5-carboxypentylamine) repaglinide formation per nanomole of protein at 0.5 to 150 uM by LC-MS/MS method	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
AID1213562	Ratio of AUC in human patient at 0.25 mg to AUC in human patient at 0.25 mg co-treated with gemfibrozil on various time intervals	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
AID1222032	Oral clearance in healthy white human with CYP2C81/3 genotype at 2 mg, po	2011	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5	Effect of the CYP2C8 genotype on the pharmacokinetics and pharmacodynamics of repaglinide.
AID598527	1-Octanol-sodium citrate buffer distribution coefficient, log D of the compound at pH 5.5 by shake-flask method	2011	Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12	Lipophilicity of acidic compounds: impact of ion pair partitioning on drug design.
AID1221984	Maximal change in insulin concentration in healthy white human plasma with CYP2C83/3 genotype at 2 mg, po up to 6 hrs	2011	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5	Effect of the CYP2C8 genotype on the pharmacokinetics and pharmacodynamics of repaglinide.
AID1222055	Mean change in insulin concentration in healthy white human plasma with CYP2C83/3 genotype at 2 mg, po up to 6 hrs	2011	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5	Effect of the CYP2C8 genotype on the pharmacokinetics and pharmacodynamics of repaglinide.
AID1222060	Maximal change in blood glucose concentration in healthy human plasma with SLCO1B1 521TT genotype at 0.5 mg	2011	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5	Effect of the CYP2C8 genotype on the pharmacokinetics and pharmacodynamics of repaglinide.
AID1213565	Ratio of AUC in variable OATP1B1 genotype human patient at 0.25 mg to AUC in ariable OATP1B1 genotype human patient at 0.25 mg co-treated with gemfibrozil on various time intervals	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
AID1213624	Drug metabolism in human hepatocytes assessed as 2-despiperidyl-2-amino repaglinide formation measured per 10'6 cells at 0.5 to 150 uM by LC-MS/MS method	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
AID1222031	Oral clearance in healthy white human with CYP2C81/1 genotype at 2 mg, po	2011	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5	Effect of the CYP2C8 genotype on the pharmacokinetics and pharmacodynamics of repaglinide.
AID194732	Maximum % decrease of blood glucose (deltaBG) was observed within 4 hour after administration orally at 0.1 mg/kg dose to fasted adult female rats versus a control group	1998	Journal of medicinal chemistry, Dec-17, Volume: 41, Issue:26	Repaglinide and related hypoglycemic benzoic acid derivatives.
AID1213627	Activity of human recombinant CYP3A4 expressed in insect cells assessed as enzyme-mediated 2-despiperidyl-2-amino repaglinide formation per picomole of protein at 0.5 to 150 uM by LC-MS/MS method	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
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).
AID1698010	Hepatic clearance in human administered through iv dosing
AID1222007	Mean change in blood glucose concentration in healthy white human plasma SLCO1B1 521TT/CYP2C81/3 combined genotype at 2 mg, po	2011	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5	Effect of the CYP2C8 genotype on the pharmacokinetics and pharmacodynamics of repaglinide.
AID1473816	Ratio of drug concentration at steady state in human at 0.5 to 4 mg, po BID/TID/QID after 6 hrs to IC50 for human BSEP overexpressed in Sf9 insect cells	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.
AID252790	In vitro ability to stimulate insulin was determined at (15 mM glucose)	2004	Bioorganic & medicinal chemistry letters, Oct-18, Volume: 14, Issue:20	Synthesis and in vitro evaluation of (S)-2-([11C]methoxy)-4-[3-methyl-1-(2-piperidine-1-yl-phenyl)-butyl-carbamoyl]-benzoic acid ([11C]methoxy-repaglinide): a potential beta-cell imaging agent.
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).
AID1213607	Drug metabolism in human hepatic S9 fraction assessed as 3'-hydroxy repaglinide formation measured per mg of protein at 0.5 to 150 uM by LC-MS/MS method	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
AID1698004	Fraction unbound in cynomolgus monkey plasma
AID1213590	Activity of human recombinant CYP3A4 expressed in insect cells assessed as enzyme-mediated 2-despiperidyl-2-(5-carboxypentylamine) repaglinide formation per picomole of protein at 0.5 to 150 uM by LC-MS/MS method	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
AID1221988	Mean change in blood glucose concentration in healthy white human plasma with CYP2C83/3 genotype at 2 mg, po up to 6 hrs	2011	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5	Effect of the CYP2C8 genotype on the pharmacokinetics and pharmacodynamics of repaglinide.
AID1213595	Drug metabolism in human hepatic S9 fraction assessed as 2-despiperidyl-2-(5-carboxypentylamine) repaglinide formation by LC-MS/MS method	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
AID1213619	Unbound intrinsic clearance in human hepatic S9 fraction assessed as 3'-hydroxy repaglinide formation measured per mg of protein at 0.5 to 150 uM by LC-MS/MS method	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
AID1213571	Drug metabolism in human patient assessed as fold change in metabolite M2/M1 AUC ratio at 0.25 mg co-treated with gemfibrozil on various time intervals relative to gemfibrozil non-treated patient	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
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.
AID1581634	Antidiabetic activity in glucose-treated rat INS1(832/13) cells assessed as increase in insulin release at 10 ug/ml in presence of 3 mM glucose measured after 2 hrs by radioimmunoassay (Rvb = 52.25 +/- 2.15 %)	2020	European journal of medicinal chemistry, Feb-01, Volume: 187	Synthesis and discovery of triazolo-pyridazine-6-yl-substituted piperazines as effective anti-diabetic drugs; evaluated over dipeptidyl peptidase-4 inhibition mechanism and insulinotropic activities.
AID176587	Half-maximal effective dose was measured on rat blood glucose after administrating at 4 hr	1998	Journal of medicinal chemistry, Dec-17, Volume: 41, Issue:26	Repaglinide and related hypoglycemic benzoic acid derivatives.
AID1221999	Cmax in healthy white human with SLCO1B1 521TC/CYP2C81/1 combined genotype at 2 mg, po	2011	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5	Effect of the CYP2C8 genotype on the pharmacokinetics and pharmacodynamics of repaglinide.
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.
AID1221990	Maximal change in blood glucose concentration in healthy white human plasma with CYP2C81/1 genotype at 2 mg, po up to 6 hrs	2011	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5	Effect of the CYP2C8 genotype on the pharmacokinetics and pharmacodynamics of repaglinide.
AID1079940	Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
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.
AID1213563	Ratio of AUC in human patient at 0.25 mg to AUC in human patient at 0.25 mg co-treated with atorvastatin	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
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.
AID1591616	Antihyperglycemic activity in alloxan-induced diabetic BALB/c mouse model assessed as blood glucose level at 10 mg/kg measured immediately by glucometry analysis	2019	Bioorganic & medicinal chemistry, 08-01, Volume: 27, Issue:15	Synthesis and molecular modeling of novel non-sulfonylureas as hypoglycemic agents and selective ALR2 inhibitors.
AID1213593	Drug metabolism in human hepatocytes assessed as 2-despiperidyl-2-(5-carboxypentylamine) repaglinide formation by LC-MS/MS method	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
AID1222019	Cmax in healthy white human with SLCO1B1 521TT/CYP2C83/3 combined genotype at 2 mg, po	2011	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5	Effect of the CYP2C8 genotype on the pharmacokinetics and pharmacodynamics of repaglinide.
AID194587	Maximum % decrease of blood glucose (deltaBG) was observed within 0.5 hour after administration orally at 0.1 mg/kg dose to fasted adult female rats versus a control group	1998	Journal of medicinal chemistry, Dec-17, Volume: 41, Issue:26	Repaglinide and related hypoglycemic benzoic acid derivatives.
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).
AID425653	Renal clearance in human	2009	Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15	Physicochemical determinants of human renal clearance.
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.
AID1591619	Antihyperglycemic activity in alloxan-induced diabetic BALB/c mouse model assessed as blood glucose level at 10 mg/kg measured after 6 hrs by glucometry analysis	2019	Bioorganic & medicinal chemistry, 08-01, Volume: 27, Issue:15	Synthesis and molecular modeling of novel non-sulfonylureas as hypoglycemic agents and selective ALR2 inhibitors.
AID1213599	Unbound intrinsic clearance in human hepatocytes assessed as 2-despiperidyl-2-(5-carboxypentylamine) repaglinide formation measured per 10'6 cells at 0.5 to 150 uM by LC-MS/MS method	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
AID1210299	Apparent intrinsic clearance in Sprague-Dawley rat hepatocytes assessed per 10'6 cells at 0.1 to 10 uM up to 90 mins by conventional assay	2012	Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 40, Issue:8	Utility of drug depletion-time profiles in isolated hepatocytes for accessing hepatic uptake clearance: identifying rate-limiting steps and role of passive processes.
AID1213516	Drug metabolism in human patient assessed as fold change in metabolite M2/M4 AUC ratio at 0.25 mg co-treated with montelukast relative to montelukast non-treated patient	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
AID1213559	Ratio of AUC in human patient at 0.25 mg to AUC in human patient at 0.25 mg co-treated with gemfibrozil	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
AID1213579	Activity of human recombinant CYP3A5 expressed in insect cells assessed as enzyme-mediated 2-despiperidyl-2-amino repaglinide formation by LC-MS/MS method	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
AID1222029	Cmax in healthy white human with CYP2C83/3 genotype at 2 mg, po	2011	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5	Effect of the CYP2C8 genotype on the pharmacokinetics and pharmacodynamics of repaglinide.
AID1698009	Hepatic clearance in cynomolgus monkey at < 1 mg/kg, iv administered as cassette dosing
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.
AID418684	Antidiabetic activity in po dosed type 2 diabetes mellitus patient assessed as reduction in HbA1C level in pancreas	2009	Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7	Development of the renal glucose reabsorption inhibitors: a new mechanism for the pharmacotherapy of diabetes mellitus type 2.
AID1222013	AUC (0 to infinity) in healthy white human with SLCO1B1 521CC/CYP2C81/3 combined genotype at 2 mg, po	2011	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5	Effect of the CYP2C8 genotype on the pharmacokinetics and pharmacodynamics of repaglinide.
AID1213569	Ratio of AUC in human patient at 0.25 mg to AUC in human patient at 0.25 mg co-treated with trimethoprim	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
AID252791	In vitro ability to stimulate insulin was determined at (5 mM glucose+0.1 uM compound)	2004	Bioorganic & medicinal chemistry letters, Oct-18, Volume: 14, Issue:20	Synthesis and in vitro evaluation of (S)-2-([11C]methoxy)-4-[3-methyl-1-(2-piperidine-1-yl-phenyl)-butyl-carbamoyl]-benzoic acid ([11C]methoxy-repaglinide): a potential beta-cell imaging agent.
AID1222065	Tmax in healthy white human with CYP2C83/3 genotype at 2 mg, po	2011	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5	Effect of the CYP2C8 genotype on the pharmacokinetics and pharmacodynamics of repaglinide.
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).
AID1222048	Mean change in insulin concentration in healthy white human plasma with SLCO1B1 521CC/CYP2C83/3 combined genotype at 2 mg, po	2011	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5	Effect of the CYP2C8 genotype on the pharmacokinetics and pharmacodynamics of repaglinide.
AID1222039	Mean change in blood glucose concentration in healthy white human plasma SLCO1B1 521TT/CYP2C83/3 combined genotype at 2 mg, po	2011	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5	Effect of the CYP2C8 genotype on the pharmacokinetics and pharmacodynamics of repaglinide.
AID1221994	Cmax in healthy white human with SLCO1B1 521TT/CYP2C81/1 combined genotype at 2 mg, po	2011	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5	Effect of the CYP2C8 genotype on the pharmacokinetics and pharmacodynamics of repaglinide.
AID1213524	Unbound intrinsic clearance in human liver microsomes assessed as glucuronide formation measured per mg of protein at 0.5 to 150 uM by LC-MS/MS method	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
AID1222053	Mean change in insulin concentration in healthy white human plasma with CYP2C81/1 genotype at 2 mg, po up to 6 hrs	2011	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5	Effect of the CYP2C8 genotype on the pharmacokinetics and pharmacodynamics of repaglinide.
AID1213618	Unbound intrinsic clearance in human liver microsomes assessed as 3'-hydroxy repaglinide formation measured per mg of protein at 0.5 to 150 uM by LC-MS/MS method	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
AID1213535	Fraction metabolism via CYP2C8 in human liver microsomes	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
AID1213605	Drug metabolism in human hepatocytes assessed as 3'-hydroxy repaglinide formation measured per 10'6 cells at 0.5 to 150 uM by LC-MS/MS method	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
AID1213609	Activity of human recombinant CYP3A5 expressed in insect cells assessed as enzyme-mediated 3'-hydroxy repaglinide formation per picomole of protein at 0.5 to 150 uM by LC-MS/MS method	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
AID1222023	AUC (0 to infinity) in healthy white human with CYP2C81/1 genotype at 2 mg, po	2011	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5	Effect of the CYP2C8 genotype on the pharmacokinetics and pharmacodynamics of repaglinide.
AID1221992	Maximal change in blood glucose concentration in healthy white human plasma with CYP2C83/3 genotype at 2 mg, po up to 6 hrs	2011	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5	Effect of the CYP2C8 genotype on the pharmacokinetics and pharmacodynamics of repaglinide.
AID1213525	Unbound intrinsic clearance in human hepatic S9 fraction assessed as glucuronide formation measured per mg of protein at 0.5 to 150 uM by LC-MS/MS method	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
AID1213608	Activity of human recombinant CYP3A4 expressed in insect cells assessed as enzyme-mediated 3'-hydroxy repaglinide formation per picomole of protein at 0.5 to 150 uM by LC-MS/MS method	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
AID1222059	Maximal change in blood glucose concentration in healthy human plasma with SLCO1B1 521TC genotype at 0.5 mg	2011	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5	Effect of the CYP2C8 genotype on the pharmacokinetics and pharmacodynamics of repaglinide.
AID1222045	AUC (0 to infinity) in healthy white human with SLCO1B1 521CC/CYP2C83/3 combined genotype at 2 mg, po	2011	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5	Effect of the CYP2C8 genotype on the pharmacokinetics and pharmacodynamics of repaglinide.
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.
AID1079945	Animal toxicity known. [column 'TOXIC' in source]
AID1222057	Mean change in blood glucose concentration in healthy white human plasma SLCO1B1 521CC/CYP2C83/3 combined genotype at 2 mg, po	2011	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5	Effect of the CYP2C8 genotype on the pharmacokinetics and pharmacodynamics of repaglinide.
AID1079932	Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID1213577	Drug metabolism in human hepatic S9 fraction assessed as 2-despiperidyl-2-amino repaglinide formation by LC-MS/MS method	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
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.
AID1213514	Drug metabolism in variable SLCO1B1 genotype containing human patient assessed as fold change in metabolite M2/M4 AUC ratio at 0.25 mg co-treated with gemfibrozil relative to gemfibrozil non-treated patient	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
AID1213597	Activity of human recombinant CYP3A5 expressed in insect cells assessed as enzyme-mediated 2-despiperidyl-2-(5-carboxypentylamine) repaglinide formation by LC-MS/MS method	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
AID1213574	Drug metabolism in human patient assessed as fold change in metabolite M2/M1 AUC ratio at 0.25 mg co-treated with telithromycin relative to telithromycin non-treated patient	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
AID1222054	Mean change in insulin concentration in healthy white human plasma with CYP2C81/3 genotype at 2 mg, po up to 6 hrs	2011	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5	Effect of the CYP2C8 genotype on the pharmacokinetics and pharmacodynamics of repaglinide.
AID1473815	Drug concentration at steady state in human at 0.5 to 4 mg, po BID/TID/QID after 6 hrs	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.
AID1591618	Antihyperglycemic activity in alloxan-induced diabetic BALB/c mouse model assessed as blood glucose level at 10 mg/kg measured after 4 hrs by glucometry analysis	2019	Bioorganic & medicinal chemistry, 08-01, Volume: 27, Issue:15	Synthesis and molecular modeling of novel non-sulfonylureas as hypoglycemic agents and selective ALR2 inhibitors.
AID1213614	Activity of human recombinant CYP3A4 expressed in insect cells assessed as enzyme-mediated 3'-hydroxy repaglinide formation by LC-MS/MS method	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
AID1213572	Drug metabolism in human patient assessed as fold change in metabolite M2/M1 AUC ratio at 0.25 mg co-treated with atorvastatin relative to atorvastatin non-treated patient	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
AID1213522	Drug metabolism in human hepatic S9 fraction assessed as glucuronide formation by LC-MS/MS method	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
AID425652	Total body clearance in human	2009	Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15	Physicochemical determinants of human renal clearance.
AID1222035	Terminal half life in healthy white human with CYP2C81/1 genotype at 2 mg, po	2011	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5	Effect of the CYP2C8 genotype on the pharmacokinetics and pharmacodynamics of repaglinide.
AID1213519	Drug metabolism in human hepatic S9 fraction assessed as glucuronide formation measured per mg of protein at 0.5 to 150 uM by LC-MS/MS method	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
AID1079943	Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID1213523	Unbound intrinsic clearance in human hepatocytes assessed as glucuronide formation measured per 10'6 cells at 0.5 to 150 uM by LC-MS/MS method	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
AID1222058	Maximal change in blood glucose concentration in healthy human plasma with SLCO1B1 521CC genotype at 0.5 mg	2011	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5	Effect of the CYP2C8 genotype on the pharmacokinetics and pharmacodynamics of repaglinide.
AID1213589	Drug metabolism in human hepatic S9 fraction assessed as 2-despiperidyl-2-(5-carboxypentylamine) repaglinide formation measured per mg of protein at 0.5 to 150 uM by LC-MS/MS method	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
AID1213515	Drug metabolism in human patient assessed as fold change in metabolite M2/M4 AUC ratio at 0.25 mg co-treated with telithromycin relative to telithromycin non-treated patient	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
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.
AID1079939	Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID1213517	Drug metabolism in human patient assessed as fold change in metabolite M2/M4 AUC ratio at 0.25 mg co-treated with telithromycin and montelukast relative to telithromycin and montelukast non-treated patient	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
AID1213598	Activity of human recombinant CYP2C8 expressed in insect cells assessed as enzyme-mediated 2-despiperidyl-2-(5-carboxypentylamine) repaglinide formation by LC-MS/MS method	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
AID1213604	Unbound intrinsic clearance in human recombinant CYP2C8 expressed in insect cells assessed as enzyme-mediated 2-despiperidyl-2-(5-carboxypentylamine) repaglinide formation per nanomole of protein at 0.5 to 150 uM by LC-MS/MS method	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
AID1222027	Cmax in healthy white human with CYP2C81/1 genotype at 2 mg, po	2011	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5	Effect of the CYP2C8 genotype on the pharmacokinetics and pharmacodynamics of repaglinide.
AID1213610	Activity of human recombinant CYP2C8 expressed in insect cells assessed as enzyme-mediated 3'-hydroxy repaglinide formation per picomole of protein at 0.5 to 150 uM by LC-MS/MS method	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
AID1581632	Antidiabetic activity in glucose-treated rat INS1(832/13) cells assessed as increase in insulin release at 1 ug/ml in presence of 3 mM glucose measured after 2 hrs by radioimmunoassay (Rvb = 52.25 +/- 2.15 %)	2020	European journal of medicinal chemistry, Feb-01, Volume: 187	Synthesis and discovery of triazolo-pyridazine-6-yl-substituted piperazines as effective anti-diabetic drugs; evaluated over dipeptidyl peptidase-4 inhibition mechanism and insulinotropic activities.
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.
AID1222063	Tmax in healthy white human with CYP2C81/1 genotype at 2 mg, po	2011	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5	Effect of the CYP2C8 genotype on the pharmacokinetics and pharmacodynamics of repaglinide.
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).
AID1213580	Activity of human recombinant CYP2C8 expressed in insect cells assessed as enzyme-mediated 2-despiperidyl-2-amino repaglinide formation by LC-MS/MS method	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
AID1698000	Apparent permeability in dog MDCKII-LE cells at pH 7.4
AID1213568	Ratio of AUC in human patient at 0.25 mg to AUC in human patient at 0.25 mg co-treated with clarithromycin	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
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).
AID1213582	Unbound intrinsic clearance in human liver microsomes assessed as 2-despiperidyl-2-amino repaglinide formation measured per mg of protein at 0.5 to 150 uM by LC-MS/MS method	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
AID1222037	Terminal half life in healthy white human with CYP2C83/3 genotype at 2 mg, po	2011	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5	Effect of the CYP2C8 genotype on the pharmacokinetics and pharmacodynamics of repaglinide.
AID1213588	Drug metabolism in human liver microsomes assessed as 2-despiperidyl-2-(5-carboxypentylamine) repaglinide formation measured per mg of protein at 0.5 to 150 uM by LC-MS/MS method	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
AID1213564	Ratio of AUC in variable SLCO1B1 genotype human patient at 0.25 mg to AUC in variable SLCO1B1 genotype human patient at 0.25 mg co-treated with gemfibrozil	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
AID1213603	Unbound intrinsic clearance in human recombinant CYP3A5 expressed in insect cells assessed as enzyme-mediated 2-despiperidyl-2-(5-carboxypentylamine) repaglinide formation per nanomole of protein at 0.5 to 150 uM by LC-MS/MS method	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
AID1213606	Drug metabolism in human liver microsomes assessed as 3'-hydroxy repaglinide formation measured per mg of protein at 0.5 to 150 uM by LC-MS/MS method	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
AID1213601	Unbound intrinsic clearance in human hepatic S9 fraction assessed as 2-despiperidyl-2-(5-carboxypentylamine) repaglinide formation measured per mg of protein at 0.5 to 150 uM by LC-MS/MS method	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
AID1222008	AUC (0 to infinity) in healthy white human with SLCO1B1 521TC/CYP2C81/3 combined genotype at 2 mg, po	2011	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5	Effect of the CYP2C8 genotype on the pharmacokinetics and pharmacodynamics of repaglinide.
AID1222006	Mean change in insulin concentration in healthy white human plasma with SLCO1B1 521TT/CYP2C81/3 combined genotype at 2 mg, po	2011	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5	Effect of the CYP2C8 genotype on the pharmacokinetics and pharmacodynamics of repaglinide.
AID1213596	Activity of human recombinant CYP3A4 expressed in insect cells assessed as enzyme-mediated 2-despiperidyl-2-(5-carboxypentylamine) repaglinide formation by LC-MS/MS method	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
AID1213578	Activity of human recombinant CYP3A4 expressed in insect cells assessed as enzyme-mediated 2-despiperidyl-2-amino repaglinide formation by LC-MS/MS method	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
AID1213587	Drug metabolism in human hepatocytes assessed as 2-despiperidyl-2-(5-carboxypentylamine) repaglinide formation measured per 10'6 cells at 0.5 to 150 uM by LC-MS/MS method	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
AID1222002	Mean change in blood glucose concentration in healthy white human plasma SLCO1B1 521TC/CYP2C81/1 combined genotype at 2 mg, po	2011	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5	Effect of the CYP2C8 genotype on the pharmacokinetics and pharmacodynamics of repaglinide.
AID1222004	Cmax in healthy white human with SLCO1B1 521TT/CYP2C81/3 combined genotype at 2 mg, po	2011	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5	Effect of the CYP2C8 genotype on the pharmacokinetics and pharmacodynamics of repaglinide.
AID1222021	Mean change in insulin concentration in healthy white human plasma with SLCO1B1 521TT/CYP2C83/3 combined genotype at 2 mg, po	2011	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5	Effect of the CYP2C8 genotype on the pharmacokinetics and pharmacodynamics of repaglinide.
AID598252	Inhibition of human ABCB1-mediated rhodamine 123 efflux in mouse L5178 cells expressing human MDR1 at 0.1 mM after 20 mins by FACS analysis relative to 5 mM sodium orthovanadate	2011	Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6	A novel approach for predicting P-glycoprotein (ABCB1) inhibition using molecular interaction fields.
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.
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).
AID194591	Maximum % decrease of blood glucose (deltaBG) was observed within 1 hour after administration orally at 0.1 mg/kg dose to fasted adult female rats versus a control group	1998	Journal of medicinal chemistry, Dec-17, Volume: 41, Issue:26	Repaglinide and related hypoglycemic benzoic acid derivatives.
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]
AID1213612	Drug metabolism in human liver microsomes assessed as 3'-hydroxy repaglinide formation by LC-MS/MS method	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
AID1213511	Drug metabolism in human patient assessed as fold change in metabolite M2/M1 AUC ratio at 0.25 mg co-treated with telithromycin and montelukast relative to telithromycin and montelukast non-treated patient	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
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.
AID1222034	Terminal half life in healthy white human at 2 mg, po	2011	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5	Effect of the CYP2C8 genotype on the pharmacokinetics and pharmacodynamics of repaglinide.
AID1079934	Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID1213584	Unbound intrinsic clearance in human recombinant CYP3A4 expressed in insect cells assessed as enzyme-mediated 2-despiperidyl-2-amino repaglinide formation per nanomole of protein at 0.5 to 150 uM by LC-MS/MS method	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
AID194730	Maximum % decrease of blood glucose (deltaBG) was observed within 4 hour after administration orally at 0.01 mg/kg dose to fasted adult female rats versus a control group	1998	Journal of medicinal chemistry, Dec-17, Volume: 41, Issue:26	Repaglinide and related hypoglycemic benzoic acid derivatives.
AID1698002	Intrinsic clearance in cryopreserved human hepatocytes at 1 uM measured up to 120 mins by LC-MS/MS analysis
AID1213628	Activity of human recombinant CYP3A5 expressed in insect cells assessed as enzyme-mediated 2-despiperidyl-2-amino repaglinide formation per picomole of protein at 0.5 to 150 uM by LC-MS/MS method	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
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]
AID599064	Plasma protein binding in human	2011	Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12	Lipophilicity of acidic compounds: impact of ion pair partitioning on drug design.
AID1213576	Drug metabolism in human liver microsomes assessed as 2-despiperidyl-2-amino repaglinide formation by LC-MS/MS method	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
AID1213623	Drug metabolism in human hepatocytes assessed as glucuronide formation measured per 10'6 cells at 0.5 to 150 uM by LC-MS/MS method	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
AID1222026	Cmax in healthy white human at 2 mg, po	2011	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5	Effect of the CYP2C8 genotype on the pharmacokinetics and pharmacodynamics of repaglinide.
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).
AID1222022	AUC (0 to infinity) in healthy white human at 2 mg, po	2011	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5	Effect of the CYP2C8 genotype on the pharmacokinetics and pharmacodynamics of repaglinide.
AID1210301	Apparent intrinsic clearance in Sprague-Dawley rat hepatocytes assessed per 10'6 cells at 0.1 to 10 uM up to 90 mins by media-loss method	2012	Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 40, Issue:8	Utility of drug depletion-time profiles in isolated hepatocytes for accessing hepatic uptake clearance: identifying rate-limiting steps and role of passive processes.
AID1213538	Half life in type 2 diabetes patient	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
AID669781	Inhibition of human recombinant MDR1 expressed in mouse L5178Y cells assessed as inhibition of rhodamine-123 efflux at 10'-4 M preincubated for 10 mins measured after 20 mins by FACS analysis	2012	ACS medicinal chemistry letters, Mar-08, Volume: 3, Issue:3	Ligand Promiscuity between the Efflux Pumps Human P-Glycoprotein and S. aureus NorA.
AID1473819	Ratio of drug concentration at steady state in human at 0.5 to 4 mg, po BID/TID/QID after 6 hrs to IC50 for human MRP4 overexpressed in Sf9 insect cells	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.
AID1698001	Lipophilicity, log D of the compound at pH 7.4 by by shake flask method
AID1213625	Drug metabolism in human liver microsomes assessed as 2-despiperidyl-2-amino repaglinide formation measured per mg of protein at 0.5 to 150 uM by LC-MS/MS method	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
AID1222014	Cmax in healthy white human with SLCO1B1 521CC/CYP2C81/3 combined genotype at 2 mg, po	2011	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5	Effect of the CYP2C8 genotype on the pharmacokinetics and pharmacodynamics of repaglinide.
AID1591621	Antihyperglycemic activity in alloxan-induced diabetic BALB/c mouse model assessed as reduction in blood glucose level at 10 mg/kg measured after 8 hrs by glucometry analysis relative to control	2019	Bioorganic & medicinal chemistry, 08-01, Volume: 27, Issue:15	Synthesis and molecular modeling of novel non-sulfonylureas as hypoglycemic agents and selective ALR2 inhibitors.
AID1222793	Dissociation constant, pKa of the compound	2013	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 41, Issue:5	Which metabolites circulate?
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.
AID238081	Displacement of [3H]glibenclamide from COS-1 cells expressing Sulfonylurea receptor 1 (SUR-1)	2004	Bioorganic & medicinal chemistry letters, Oct-18, Volume: 14, Issue:20	Synthesis and in vitro evaluation of (S)-2-([11C]methoxy)-4-[3-methyl-1-(2-piperidine-1-yl-phenyl)-butyl-carbamoyl]-benzoic acid ([11C]methoxy-repaglinide): a potential beta-cell imaging agent.
AID1213518	Drug metabolism in human liver microsomes assessed as glucuronide formation measured per mg of protein at 0.5 to 150 uM by LC-MS/MS method	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
AID1079937	Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
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]
AID194595	Maximum % decrease of blood glucose (deltaBG) was observed within 2 hour after administration orally at 0.1 mg/kg dose to fasted adult female rats versus a control group	1998	Journal of medicinal chemistry, Dec-17, Volume: 41, Issue:26	Repaglinide and related hypoglycemic benzoic acid derivatives.
AID1222025	AUC (0 to infinity) in healthy white human with CYP2C83/3 genotype at 2 mg, po	2011	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5	Effect of the CYP2C8 genotype on the pharmacokinetics and pharmacodynamics of repaglinide.
AID1213570	Ratio of AUC in human patient at 0.25 mg to AUC in human patient at 0.25 mg co-treated with cyclosporine	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
AID1213531	Fraction metabolism via UGT in human hepatocytes	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
AID1213529	Fraction metabolism via CYP2C8 in human hepatocytes	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
AID1213573	Drug metabolism in variable SLCO1B1 genotype containing human patient assessed as fold change in metabolite M2/M1 AUC ratio at 0.25 mg co-treated with gemfibrozil relative to gemfibrozil non-treated patient	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
AID1698006	Ratio of drug level in cynomolgus monkey blood to plasma administered through iv dosing by LC-MS/MS analysis
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.
AID252958	Percent stimulation index to stimulate insulin was determined	2004	Bioorganic & medicinal chemistry letters, Oct-18, Volume: 14, Issue:20	Synthesis and in vitro evaluation of (S)-2-([11C]methoxy)-4-[3-methyl-1-(2-piperidine-1-yl-phenyl)-butyl-carbamoyl]-benzoic acid ([11C]methoxy-repaglinide): a potential beta-cell imaging agent.
AID1213620	Unbound intrinsic clearance in human recombinant CYP3A4 expressed in insect cells assessed as enzyme-mediated 3'-hydroxy repaglinide formation per nanomole of protein at 0.5 to 150 uM by LC-MS/MS method	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
AID1222003	AUC (0 to infinity) in healthy white human with SLCO1B1 521TT/CYP2C81/3 combined genotype at 2 mg, po	2011	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5	Effect of the CYP2C8 genotype on the pharmacokinetics and pharmacodynamics of repaglinide.
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).
AID1222056	Maximal change in insulin concentration in healthy white human plasma at 2 mg, po up to 6 hrs	2011	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5	Effect of the CYP2C8 genotype on the pharmacokinetics and pharmacodynamics of repaglinide.
AID1213585	Unbound intrinsic clearance in human recombinant CYP3A5 expressed in insect cells assessed as enzyme-mediated 2-despiperidyl-2-amino repaglinide formation per nanomole of protein at 0.5 to 150 uM by LC-MS/MS method	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
AID1213617	Unbound intrinsic clearance in human hepatocytes assessed as 3'-hydroxy repaglinide formation measured per 10'6 cells at 0.5 to 150 uM by LC-MS/MS method	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
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.
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.
AID253246	Percent relative stimulation index to stimulate insulin was determined	2004	Bioorganic & medicinal chemistry letters, Oct-18, Volume: 14, Issue:20	Synthesis and in vitro evaluation of (S)-2-([11C]methoxy)-4-[3-methyl-1-(2-piperidine-1-yl-phenyl)-butyl-carbamoyl]-benzoic acid ([11C]methoxy-repaglinide): a potential beta-cell imaging agent.
AID1213629	Activity of human recombinant CYP2C8 expressed in insect cells assessed as enzyme-mediated 2-despiperidyl-2-amino repaglinide formation per picomole of protein at 0.5 to 150 uM by LC-MS/MS method	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
AID1222061	Oral bioavailability in human	2011	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5	Effect of the CYP2C8 genotype on the pharmacokinetics and pharmacodynamics of repaglinide.
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).
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.
AID242637	In vitro displacement of [3H]glibenclamide (IC50=0.61) from COS-1 cells expressing Sulfonylurea receptor 1 (SUR-1)	2004	Bioorganic & medicinal chemistry letters, Oct-18, Volume: 14, Issue:20	Synthesis and in vitro evaluation of (S)-2-([11C]methoxy)-4-[3-methyl-1-(2-piperidine-1-yl-phenyl)-butyl-carbamoyl]-benzoic acid ([11C]methoxy-repaglinide): a potential beta-cell imaging agent.
AID1213560	Ratio of AUC in human patient at 0.25 mg to AUC in human patient at 0.25 mg co-treated with itraconazole	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
AID1697999	Dissociation constant, acidic pKa of compound measured up to 18 mins by capillary electrophoresis
AID1213520	Drug metabolism in human hepatocytes assessed as glucuronide formation by LC-MS/MS method	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
AID665544	Hypoglycemic activity in glucose-fed normoglycemic Wistar rat assessed as decrease in rise of blood glucose at 4 mg/kg, po single dose measured up to 4 hrs post dose by oral glucose tolerance test	2012	European journal of medicinal chemistry, Jul, Volume: 53	Synthesis, in vitro and in silico screening of ethyl 2-(6-substituted benzo[d]thiazol-2-ylamino)-2-oxoacetates as protein-tyrosine phosphatase 1B inhibitors.
AID342843	Increase in insulin secretion in Sprague-Dawley rat pancreatic Langerhans islets at 200 uM	2008	Bioorganic & medicinal chemistry letters, Aug-01, Volume: 18, Issue:15	Synthesis of hydantoin analogues of (2S,3R,4S)-4-hydroxyisoleucine with insulinotropic properties.
AID1213611	Drug metabolism in human hepatocytes assessed as 3'-hydroxy repaglinide formation by LC-MS/MS method	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
AID1213512	Drug metabolism in human patient assessed as fold change in metabolite M2/M4 AUC ratio at 0.25 mg co-treated with gemfibrozil on various time intervals relative to gemfibrozil non-treated patient	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
AID1222036	Terminal half life in healthy white human with CYP2C81/3 genotype at 2 mg, po	2011	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5	Effect of the CYP2C8 genotype on the pharmacokinetics and pharmacodynamics of repaglinide.
AID342841	Increase in insulin secretion in Sprague-Dawley rat pancreas assessed per Langerhans islet	2008	Bioorganic & medicinal chemistry letters, Aug-01, Volume: 18, Issue:15	Synthesis of hydantoin analogues of (2S,3R,4S)-4-hydroxyisoleucine with insulinotropic properties.
AID1222043	Mean change in insulin concentration in healthy white human plasma with SLCO1B1 521TC/CYP2C83/3 combined genotype at 2 mg, po	2011	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5	Effect of the CYP2C8 genotype on the pharmacokinetics and pharmacodynamics of repaglinide.
AID1213594	Drug metabolism in human liver microsomes assessed as 2-despiperidyl-2-(5-carboxypentylamine) repaglinide formation by LC-MS/MS method	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
AID669779	Inhibition of norA-mediated ethidium bromide efflux in Staphylococcus aureus SA-1199B harboring grlA A116E mutant at 50 uM after 5 mins by fluorometric analysis	2012	ACS medicinal chemistry letters, Mar-08, Volume: 3, Issue:3	Ligand Promiscuity between the Efflux Pumps Human P-Glycoprotein and S. aureus NorA.
AID1221996	Mean change in insulin concentration in healthy white human plasma with SLCO1B1 521TT/CYP2C81/1 combined genotype at 2 mg, po	2011	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5	Effect of the CYP2C8 genotype on the pharmacokinetics and pharmacodynamics of repaglinide.
AID1222064	Tmax in healthy white human with CYP2C81/3 genotype at 2 mg, po	2011	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5	Effect of the CYP2C8 genotype on the pharmacokinetics and pharmacodynamics of repaglinide.
AID1213575	Drug metabolism in human hepatocytes assessed as 2-despiperidyl-2-amino repaglinide formation by LC-MS/MS method	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
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.
AID1222040	AUC (0 to infinity) in healthy white human with SLCO1B1 521TC/CYP2C83/3 combined genotype at 2 mg, po	2011	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5	Effect of the CYP2C8 genotype on the pharmacokinetics and pharmacodynamics of repaglinide.
AID598251	Inhibition of human ABCB1-mediated rhodamine 123 efflux in mouse L5178 cells expressing human MDR1 after 20 mins by FACS analysis	2011	Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6	A novel approach for predicting P-glycoprotein (ABCB1) inhibition using molecular interaction fields.
AID1213600	Unbound intrinsic clearance in human liver microsomes assessed as 2-despiperidyl-2-(5-carboxypentylamine) repaglinide formation measured per mg of protein at 0.5 to 150 uM by LC-MS/MS method	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
AID1221993	AUC (0 to infinity) in healthy white human with SLCO1B1 521TT/CYP2C81/1 combined genotype at 2 mg, po	2011	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5	Effect of the CYP2C8 genotype on the pharmacokinetics and pharmacodynamics of repaglinide.
AID1213616	Activity of human recombinant CYP2C8 expressed in insect cells assessed as enzyme-mediated 3'-hydroxy repaglinide formation by LC-MS/MS method	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
AID1213536	Fraction metabolism via CYP3A4 in human liver microsomes	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
AID1222018	AUC (0 to infinity) in healthy white human with SLCO1B1 521TT/CYP2C83/3 combined genotype at 2 mg, po	2011	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5	Effect of the CYP2C8 genotype on the pharmacokinetics and pharmacodynamics of repaglinide.
AID1079942	Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID194598	Maximum % decrease of blood glucose (deltaBG) was observed within 3 hour after administration orally at 0.1 mg/kg dose to fasted adult female rats versus a control group	1998	Journal of medicinal chemistry, Dec-17, Volume: 41, Issue:26	Repaglinide and related hypoglycemic benzoic acid derivatives.
AID1222030	Oral clearance in healthy white human at 2 mg, po	2011	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5	Effect of the CYP2C8 genotype on the pharmacokinetics and pharmacodynamics of repaglinide.
AID1221985	Mean change in blood glucose concentration in healthy white human plasma at 2 mg, po up to 6 hrs	2011	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5	Effect of the CYP2C8 genotype on the pharmacokinetics and pharmacodynamics of repaglinide.
AID1213613	Drug metabolism in human hepatic S9 fraction assessed as 3'-hydroxy repaglinide formation by LC-MS/MS method	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
AID1222033	Oral clearance in healthy white human with CYP2C83/3 genotype at 2 mg, po	2011	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5	Effect of the CYP2C8 genotype on the pharmacokinetics and pharmacodynamics of repaglinide.
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]
AID1213586	Unbound intrinsic clearance in human recombinant CYP2C8 expressed in insect cells assessed as enzyme-mediated 2-despiperidyl-2-amino repaglinide formation per nanomole of protein at 0.5 to 150 uM by LC-MS/MS method	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
AID1222062	Tmax in healthy white human at 2 mg, po	2011	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5	Effect of the CYP2C8 genotype on the pharmacokinetics and pharmacodynamics of repaglinide.
AID1591617	Antihyperglycemic activity in alloxan-induced diabetic BALB/c mouse model assessed as blood glucose level at 10 mg/kg measured after 2 hrs by glucometry analysis	2019	Bioorganic & medicinal chemistry, 08-01, Volume: 27, Issue:15	Synthesis and molecular modeling of novel non-sulfonylureas as hypoglycemic agents and selective ALR2 inhibitors.
AID1079947	Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID1221998	AUC (0 to infinity) in healthy white human with SLCO1B1 521TC/CYP2C81/1 combined genotype at 2 mg, po	2011	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5	Effect of the CYP2C8 genotype on the pharmacokinetics and pharmacodynamics of repaglinide.
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.
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]
AID1473818	Ratio of drug concentration at steady state in human at 0.5 to 4 mg, po BID/TID/QID after 6 hrs to IC50 for human MRP3 overexpressed in Sf9 insect cells	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.
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).
AID1222046	Cmax in healthy white human with SLCO1B1 521CC/CYP2C83/3 combined genotype at 2 mg, po	2011	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5	Effect of the CYP2C8 genotype on the pharmacokinetics and pharmacodynamics of repaglinide.
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.
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).
AID194733	Maximum % decrease of blood glucose (deltaBG) was observed within 4 hour after administration orally at 0.1 mg/kg dose to fasted adult female rats versus a control group; ND = 'not determined'	1998	Journal of medicinal chemistry, Dec-17, Volume: 41, Issue:26	Repaglinide and related hypoglycemic benzoic acid derivatives.
AID588499	High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set	2010	Current protocols in cytometry, Oct, Volume: Chapter 13	Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499	High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set	2006	Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5	Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499	High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set	2010	Assay and drug development technologies, Feb, Volume: 8, Issue:1	High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588497	High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set	2010	Current protocols in cytometry, Oct, Volume: Chapter 13	Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497	High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set	2006	Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5	Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497	High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set	2010	Assay and drug development technologies, Feb, Volume: 8, Issue:1	High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID1745845	Primary qHTS for Inhibitors of ATXN expression
AID588501	High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set	2010	Current protocols in cytometry, Oct, Volume: Chapter 13	Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501	High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set	2006	Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5	Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501	High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set	2010	Assay and drug development technologies, Feb, Volume: 8, Issue:1	High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID1347116	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
AID1347121	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
AID1347117	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
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.
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.
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.
AID1347118	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
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.
AID1347115	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
AID1347113	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
AID1347111	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
AID1347123	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
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.
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.
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.
AID1347112	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
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.
AID1347127	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
AID1347122	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
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.
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.
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.
AID1347126	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
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.
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.
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.
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.
AID1347129	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
AID1347128	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
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.
AID1347109	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
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.
AID1347125	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
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.
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.
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.
AID1347110	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
AID1347119	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
AID1347124	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
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.
AID1347114	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
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.
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.
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.
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.
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.
AID540299	A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis	2010	Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21	Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.
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.
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.
AID1345983	Human ATP-binding cassette, sub-family C (CFTR/MRP), member 8 (ABCC subfamily)	2004	Bioorganic & medicinal chemistry letters, Oct-18, Volume: 14, Issue:20	Synthesis and in vitro evaluation of (S)-2-([11C]methoxy)-4-[3-methyl-1-(2-piperidine-1-yl-phenyl)-butyl-carbamoyl]-benzoic acid ([11C]methoxy-repaglinide): a potential beta-cell imaging agent.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	69 (11.75)	18.2507
2000's	243 (41.40)	29.6817
2010's	230 (39.18)	24.3611
2020's	45 (7.67)	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	152 (24.92%)	5.53%
Reviews	91 (14.92%)	6.00%
Case Studies	24 (3.93%)	4.05%
Observational	1 (0.16%)	0.25%
Other	342 (56.07%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (62)

Trial Overview

Trial	Phase	Enrollment	Study Type	Start Date	Status
"Is Beta Cell Rest by Insulin Treatment Beneficial Compared to State-of-the Art Enhancers of Insulin Secretion in Preserving Beta Cell Function in Subjects With Latent Autoimmune Diabetes of the Adult (LADA)?"[NCT01140438]		64 participants (Actual)	Interventional	2009-03-31	Completed
Incretin-based Drugs and the Risk of Heart Failure: A Multi-center Network Observational Study[NCT02456428]		1,499,650 participants (Actual)	Observational	2014-03-31	Completed
Multi-centre, Multinational, Open-labelled, Randomised, Parallel, Controlled Trial in Type 2 Diabetic Subjects Inadequately Controlled on Repaglinide, to Compare the Efficacy and Safety of Repaglinide Combined With Bedtime NPH Insulin Versus Twice Daily N[NCT01562561]	Phase 3	213 participants (Actual)	Interventional	2001-06-01	Completed
Evaluation of the Effect of LY3871801 on the Pharmacokinetics of CYP450 Substrates and an OAT1/3 Substrate in Healthy Participants[NCT05602675]	Phase 1	39 participants (Actual)	Interventional	2022-11-02	Completed
A Phase 1, Open-Label, Fixed-sequence, 5-part, Drug-drug Interaction Study of Tucatinib to Evaluate the Effects of CYP3A4 and CYP2C8 Inhibition and Induction on the Pharmacokinetics of Tucatinib and to Evaluate the Effects of Tucatinib on the Pharmacokine[NCT03723395]	Phase 1	116 participants (Actual)	Interventional	2018-09-17	Completed
The Clinical Safety and Effectiveness of Repaglinide in Treatment-naive Type 2 Diabetes Subjects in China. A 16-week Multicentre, Prospective, Open Label, Non-interventional Study.[NCT01077570]		2,033 participants (Actual)	Observational	2010-03-31	Completed
The Use of Incretin-based Drugs and the Risk of Acute Pancreatitis in Patients With Type 2 Diabetes[NCT02476760]		1,417,914 participants (Actual)	Observational	2014-03-31	Completed
A Phase 1 Open-label, Multicenter Study to Evaluate the Effect of Ripretinib on the Pharmacokinetics of a CYP2C8 Probe Substrate (Repaglinide) in Patients With Advanced Gastrointestinal Stromal Tumors (GIST)[NCT04530981]	Phase 1	30 participants (Anticipated)	Interventional	2021-09-22	Recruiting
A 26-week, Multicentre, Open-labelled, Non-randomised, Non-interventional, Observational, Safety Study of NovoNorm® (Repaglinide) and Insulin Analogue Combination Therapy in Type 2 Diabetes in Korea[NCT01355718]		120 participants (Actual)	Observational	2011-08-31	Completed
A Phase 1 Open Label Study to Evaluate the Effect of Multiple Doses of Isavuconazole on the Pharmacokinetics of Repaglinide and Caffeine[NCT02128321]	Phase 1	24 participants (Actual)	Interventional	2014-01-31	Completed
An Open-Label, Multicenter, Two-Part, Phase 1 Study to Characterize the Effects of a Moderate CYP3A Inhibitor on the Pharmacokinetics of Tazemetostat (EPZ-6438) (Part A), the Effects of Tazemetostat on the Pharmacokinetics of CYP2C8 and CYP2C19 Substrates[NCT03028103]	Phase 1	32 participants (Actual)	Interventional	2017-03-27	Completed
A Phase 1, Open-Label, 4-Part, Drug-Drug Interaction Study With Omaveloxolone in Healthy Subjects[NCT04008186]	Phase 1	61 participants (Actual)	Interventional	2019-06-14	Completed
A Randomised, Single-Blind, Three-Period Crossover Study Examining the Single Dose Pharmacokinetics of Concomitantly Administered Repaglinide and Metformin Versus Combination Tablet Dosing (NN4440) in Fed Healthy Male Volunteers[NCT00959101]	Phase 1	42 participants (Actual)	Interventional	2009-08-31	Completed
Comparison of the Effects of Repaglinide and Metformin on Glucose Excursions in Newly Diagnosed Type 2 Diabetes Patients in China[NCT00832481]		60 participants (Anticipated)	Interventional	2009-01-31	Recruiting
A 3-month, Open-label, Randomized, Multi-center Study of Repaglinide in Combination With Metformin as Compared to Metformin or Repaglinide Given as Monotherapy for the Treatment of Type 2 Diabetes.[NCT01720290]	Phase 4	150 participants (Actual)	Interventional	2002-07-25	Completed
A 16-week, Open-label, Multicentre, Randomised, Parallel Study to Evaluate Efficacy and Safety of Repaglinide and Metformin Combination Therapy Compared to Repaglinide Monotherapy in Chinese OAD Naive Type 2 Diabetic Patients[NCT00819741]	Phase 4	433 participants (Actual)	Interventional	2009-02-28	Completed
Observational Study Investigating the Efficacy of Switching From Metformin Monotherapy to a Dual Therapy of Metformin and Repaglinide on Glycaemic Control in Type 2 Diabetes[NCT00709917]		2,171 participants (Actual)	Observational	2007-03-31	Completed
A 16-week, Multicentre, Randomised, Open-label, Parallel Group Study to Investigate the Efficacy and Safety Profiles of Repaglinide Monotherapy Compared to Gliclazide Monotherapy in Chinese Antidiabetic-naïve Subjects With Type 2 Diabetes[NCT01022762]	Phase 4	440 participants (Actual)	Interventional	2009-11-30	Completed
An Open Label, Drug-drug Interaction Study to Assess the Effect of Multiple Doses of Gemfibrozil on the Single Dose Pharmacokinetics of ASP3652 and to Assess the Effect of Multiple Doses of ASP3652 on the Single Dose Pharmacokinetics of Repaglinide[NCT01797198]	Phase 1	48 participants (Actual)	Interventional	2012-04-30	Completed
Comparison of Metformin and Repaglinide Monotherapy in the Treatment of New Onset Type 2 Diabetes Mellitus in China[NCT02040246]	Phase 4	107 participants (Actual)	Interventional	2009-02-28	Completed
Multi-centre, Open, Randomised, Parallel, Controlled Trial in Type 2 Diabetic Subjects Inadequately Controlled With SU +/ Biguanide Therapy, to Compare the Efficacy and Safety of Repaglinide Combined With Bedtime Insulin vs. Insulin Alone[NCT00799448]	Phase 4	40 participants (Actual)	Interventional	2003-09-16	Terminated(stopped due to Low recruitment status)
Repaglinide for Adolescents With Cystic Fibrosis-Related Diabetes[NCT00231192]		0 participants (Actual)	Interventional	2005-10-31	Withdrawn(stopped due to Unable to recruit any subjects)
Efficacy and Safety of Repaglinide and Metformin Combined in Type 2 Diabetes Mellitus[NCT00568984]	Phase 4	324 participants (Actual)	Interventional	2002-11-21	Completed
A Phase I Dose Escalation Study of Ascending Single and Multiple Doses of the MEK Inhibitor Zapnometinib in Healthy Subjects to Evaluate the Safety & Tolerability Compared to Placebo, Additionally Evaluating Pharmacokinetics and Pharmacodynamics of Target[NCT05555823]	Phase 1	96 participants (Actual)	Interventional	2022-06-23	Completed
Efficacy and Safety of Repaglinide, Glurenorm® and Glucobay® in Chinese Subjects With Type 2 Diabetes Mellitus[NCT00568074]	Phase 4	131 participants (Actual)	Interventional	2003-12-16	Completed
A Single-center, Open-label, Fixed-sequence Phase I Drug-drug Interaction Clinical Study to Investigate the Pharmacokinetics of SHR3680 With Repaglinide (CYP2C8 Substrates) and Bupropion (CYP2B6 Substrates) in Prostate Cancer Patients[NCT04664725]	Phase 1	18 participants (Anticipated)	Interventional	2020-06-01	Recruiting
Repaglinide Versus Glyburide: Comparitive Effect on Postprandial Lipemia: An Open-labeled, Randomized, Parallel Group Study in Patients With Type 2 Diabetes[NCT01605773]	Phase 4	51 participants (Actual)	Interventional	2001-11-08	Completed
A Randomised Controlled Trial for People With Established Type 2 Diabetes During Ramadan: Canagliflozin (Invokana™) vs. Standard Dual Therapy Regimen: The 'Can Do Ramadan' Study[NCT02694263]	Phase 4	25 participants (Actual)	Interventional	2016-07-31	Completed
Open Randomised Prospective Comparative Multi-centre Intervention Study of Patients With Cystic Fibrosis and Early Diagnosed Diabetes Mellitus[NCT00662714]	Phase 3	73 participants (Actual)	Interventional	2001-09-30	Completed
A Single-center, Open-label, Single-arm, Fixed-sequence Study to Evaluate the Pharmacokinetic Effects of SHR0302 Tablets on Substrates of CYP3A4, CYP2C8, CYP2C9, CYP2C19 in Healthy Volunteers[NCT05392127]	Phase 1	24 participants (Actual)	Interventional	2022-07-15	Completed
A Double-Blind, Randomized, Parallel, Comparative Study to Evaluate the Efficacy and Safety of an Antidiabetic Agent Repaglinide for the Treatment of Type 2 Diabetes Mellitus Patients[NCT00336310]	Phase 4	50 participants	Interventional	2006-07-31	Not yet recruiting
A Phase 1, Open-Label, Two-Part, Fixed-Sequence, Drug-Drug Interaction Study to Evaluate the Effect of Voxelotor on the Pharmacokinetics of Selected CYP and Transporter Probe Substrates in Healthy Participants[NCT05981365]	Phase 1	18 participants (Actual)	Interventional	2023-04-17	Completed
A Randomized, Single-Blind, Four-Period Crossover Study Examining the Single Dose Pharmacokinetics of Repaglinide, Metformin and Combination Tablet Dosing (NN4440) in Fasting and Fed Healthy Volunteers[NCT01489644]	Phase 1	62 participants (Actual)	Interventional	2006-06-30	Completed
A Randomized, Single-Blind, Three-Period Crossover Study Examining the Single Dose Pharmacokinetics of Concomitantly Administered Repaglinide and Metformin Versus Combination Tablet Dosing (NN4440) in Fed Healthy Volunteers[NCT01490658]	Phase 1	93 participants (Actual)	Interventional	2006-06-30	Completed
An Open-Label, Fixed-Sequence Study to Evaluate the Effect of Multiple Doses of LOXO-292 on the Single Dose Pharmacokinetics of Repaglinide in Healthy Adult Subjects[NCT05469113]	Phase 1	13 participants (Actual)	Interventional	2019-01-29	Completed
The Effect of Imlunestrant on CYP2C8, CYP2C19, CYP2D6, P-gp, and BCRP Activity and the Effect of P-gp Inhibition on Imlunestrant Pharmacokinetics in Healthy Women of Non-childbearing Potential[NCT05444556]	Phase 1	113 participants (Actual)	Interventional	2022-07-07	Completed
Effect of Metformin Versus Repaglinide Treatment on Glycemic Control and Non-Glycaemic Cardiovascular Risk Factors in Non-Obese Type 2 Diabetic Patients Uncontrolled by Diet[NCT00118950]	Phase 4	100 participants	Interventional	2001-03-31	Completed
A Multi-centre, Single Armed, Open Labelled Trial to Study the Efficacy and Safety Profile of Repaglinide & Metformin Combination Therapy in Chinese Type 2 Diabetics[NCT00491725]	Phase 4	187 participants (Actual)	Interventional	2005-09-30	Completed
Effect of BIA 9-1067 on the Pharmacokinetics of Repaglinide in Healthy Volunteers[NCT01536366]	Phase 1	27 participants (Actual)	Interventional	2009-06-30	Completed
REPAMET 2: Observational Study of the Switch From Metformin Monotherapy to Bitherapy With Metformin and Repaglinide[NCT00745433]		906 participants (Actual)	Observational	2008-01-31	Completed
A Single Arm, Open and Fixed Sequence Study to Investigate the Pharmacokinetic Effects of Apatinib Mesylate on CYP2C8 Substrate Repaglinide or CYP2B6 Substrate in Advanced Solid Tumor Subjects[NCT04457180]	Phase 1	18 participants (Actual)	Interventional	2020-11-16	Completed
Effect of Repaglinide Versus Metformin Treatment in Combination With Insulin Biasp30 (Novologmix 70/30) Predinner on Glycemic and Non-Glycemic Cardiovascular Risk-Factors in Non-Obese Patients With Type-2-Diabetes With Unsatisfactory Glycaemic Control Wit[NCT00118963]	Phase 4	102 participants (Actual)	Interventional	2003-01-31	Completed
Action to Control Cardiovascular Risk in Diabetes (ACCORD)[NCT00000620]	Phase 3	10,251 participants (Actual)	Interventional	1999-09-30	Completed
Diabetes Therapy to Improve BMI and Lung Function in CF[NCT00072904]	Phase 3	108 participants (Actual)	Interventional	2001-06-30	Completed
Multicentre, Randomised, Comparative, Open, Three Armed Parallel Group Study on the Use of Metformin, Repaglinide or the Combination of Both in Type 2 Diabetic Patients After Failure of Dietary Measures[NCT01465152]	Phase 4	182 participants (Actual)	Interventional	2002-03-06	Completed
Repaglinide and Metformin Combination Tablet (NN4440) in a TID Regimen Compared to a BID Regimen and BID Avandamet in Subjects With Type 2 Diabetes: A Twenty-Six Week, Open-Label, Multicenter, Randomized, Parallel Group Trial to Investigate Efficacy and S[NCT00399711]	Phase 3	560 participants (Actual)	Interventional	2006-11-30	Completed
A Multi-centre, Open, Randomised, Parallel, Controlled Trial to Compare the Efficacy and Safety of Repaglinide Combined With Bedtime Insulin With Insulin Alone in Type 2 Diabetic Subjects Inadequately Controlled With Sulphonylurea ± Biguanide Therapy[NCT01720303]	Phase 4	159 participants (Actual)	Interventional	2002-09-19	Completed
A Phase I, Open-label, Fixed-sequence, Drug Interaction Study to Investigate the Effect of Multiple Oral Doses of Pirtobrutinib (LOXO-305) on the Pharmacokinetics of Repaglinide (CYP2C8 Substrate) in Healthy Subjects[NCT06165146]	Phase 1	16 participants (Actual)	Interventional	2020-11-10	Completed
A Multi-center, Prospective, Non-interventional Evaluation of Efficacy, Safety and Convenience of Using NovoNorm® in the Treatment of Type 2 Diabetic Patients in Routine Clinical Practice[NCT01498900]		30,554 participants (Actual)	Observational	2004-08-31	Completed
NovoNorm Post Marketing Surveillance Study[NCT01498913]		5,841 participants (Actual)	Observational	2001-08-30	Completed
Efficacy of Repaglinide Compared to Glyburide and Placebo on Hepatic Glucose Metabolism in Type 2 Diabetic Subjects Treated With Diet or With Antidiabetic Oral Agents. A Randomized, Open, Cross-over Single-centre Placebo-controlled Trial[NCT01698931]	Phase 4	9 participants (Actual)	Interventional	2002-04-26	Completed
An Open-label, Randomized, Single-dose, 2-way Crossover Trial to Compare the Pharmacokinetics of Repaglinide2mg and MetforminHCl 500mg Complex to Combination Preparation of Repaglinide 2mg and MetforminHCl 500mg in Healthy Male Volunteers.[NCT01780051]	Phase 1	48 participants (Actual)	Interventional	2013-03-31	Completed
A Phase I, Open-label, Fixed-sequence, Crossover, Drug-drug Interaction Study to Investigate the Inhibition Potential of KL1333 on CYP1A2, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, and CYP3A4 in Healthy Subjects[NCT04643249]	Phase 1	14 participants (Actual)	Interventional	2020-11-10	Completed
A Phase I, Multi-center Study to Determine the Effect of Fluzoparib on Pharmacokinetics of Caffeine, S-Warfarin, Omeprazole, Midazolam, Repaglinide and Bupropion in Patients With Recurrent Ovarian Cancer[NCT04718740]	Phase 1	33 participants (Actual)	Interventional	2021-06-25	Completed
Arterial Stiffness and Endothelial Function Indexes, Relationships With Clinical and Laboratory Variables in a Group of Diabetic Patients in Treatment With Dulaglutide: a Case-control Study[NCT03824002]	Phase 4	92 participants (Actual)	Interventional	2017-04-01	Completed
A Multicenter, Randomized, Active-Controlled, Open-label Clinical Trial to Evaluate the Safety and Efficacy of Glimepiride, Gliclazide, Repaglinide or Acarbose as a Third OAHA on Top of Sitagliptin+Metformin Combination Therapy in Chinese Patients With Ty[NCT01709305]	Phase 4	5,570 participants (Actual)	Interventional	2012-11-08	Completed
A Phase I, Open-label, Fixed-sequence, Two-period, Crossover, Drug-drug Interaction Study to Evaluate the Effect of Multiple Doses of Ganaplacide and Lumefantrine Combination on the Pharmacokinetics of Midazolam, Repaglinide, Dextromethorphan, Metformin, [NCT05236530]	Phase 1	48 participants (Actual)	Interventional	2022-03-09	Completed
Pilot and Feasibility Study for the Treatment of Pre-diabetes in Patients With Cystic Fibrosis[NCT00763412]		31 participants (Actual)	Interventional	2006-11-30	Completed
The Effect of Multiple Doses of BI 187004 on the Single-dose Pharmacokinetics of Repaglinide and Bupropion Following Oral Administration in Healthy Male Subjects (an Open-label, One-sequence Trial)[NCT02305901]	Phase 1	18 participants (Actual)	Interventional	2014-12-31	Completed
A Phase 1, Single-Center, Open-Label, Fixed-Sequence Study to Evaluate the Effect of DC-806 on the Single Dose Pharmacokinetics of CYP450 Enzyme and Transporter Substrates in Healthy Participants[NCT06092931]	Phase 1	28 participants (Anticipated)	Interventional	2023-10-16	Active, not recruiting
The Use of Incretin-based Drugs and the Risk of Pancreatic Cancer in Patients With Type 2 Diabetes[NCT02475499]		886,172 participants (Actual)	Observational	2014-03-31	Completed
A 26-Week, Multi-Center, Open-label, Randomized, Parallel-group Study to Evaluate the Efficacy and Safety of Two Treatment Regimens in Patients With Type 2 Diabetes After Short-Term Intensive Insulin Therapy: Basal Insulin Based Treatment (With Prandial O[NCT03359837]	Phase 4	384 participants (Actual)	Interventional	2018-01-20	Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

Part A: Cmax of Fluconazole After Administration of 400mg Once Daily for 4 Days

(NCT03028103)
Timeframe: Day 19, 0 to 8 hours post-dose

Intervention	ng/mL (Geometric Mean)
Part A	25900

Part A: Exposure of Fluconazole After Administration of 400 mg Once Daily for 4 Days (AUC0-8)

(NCT03028103)
Timeframe: Day 19, 0 to 8 hours post-dose

Intervention	h*ng/mL (Geometric Mean)
Part A	170000

Part A: Tmax of Fluconazole After Administration of 400mg Once Daily for 4 Days

(NCT03028103)
Timeframe: Day 19, 0 to 8 hours post-dose

Intervention	hours (Median)
Part A	1.48

Incidence of Treatment-emergent Adverse Events as a Measure of Safety

(NCT03028103)
Timeframe: From the first dose of study treatment until the earlier of either 30 days after the discontinuation of study treatment or until the initiation of subsequent anticancer therapy, up to 2 years.

Intervention	Participants (Count of Participants)
	Any TEAE	Any TEAE Grade 3 or 4	Any Treatment-Related TEAE	Any Treatment-Related TEAE Grade 3 or 4	Any TEAE Leading to Dose Reduction	Any TEAE Leading to Study Drug Interruption	Any TEAE Leading to Study Drug Discontinuation	Any TESAE	Any Treatment-Related TESAE	Any Protocol Defined AE of Special Interest
Part A	12	7	9	4	2	3	0	4	1	0
Part B	14	8	10	3	2	6	0	6	0	0