Compound	Dose	Time	Species	Model	Method	Action	Result	Positive criterion	Reference
Tamoxifen						affect	Positive		227
Perhexiline	100 μM	5 minutes preincubation; 10 minutes	mouse; Crl/CD-l(1CR)BR Swiss	liver mitochondria	Measurement of beta oxidation	decrease	Positive	p < 0.01	193
Perhexiline	100 μM	5 minutes preincubation; 10 minutes	mouse; Crl/CD-l(1CR)BR Swiss	liver mitochondria	Measurement of beta oxidation	decrease	Positive	p < 0.01	193
Perhexiline	200 μM		mouse; Crl/CD-l(1CR)BR Swiss	liver mitochondria	Measurement of activities of acyl-CoA dehydrogenases	decrease	Positive	p < 0.01	193
Perhexiline	400 μM		mouse; Crl/CD-l(1CR)BR Swiss	liver mitochondria	Measurement of activities of acyl-CoA dehydrogenases	decrease	Positive	p < 0.01	193
Perhexiline	800 μM		mouse; Crl/CD-l(1CR)BR Swiss	liver mitochondria	Measurement of activities of acyl-CoA dehydrogenases	decrease	Positive	p < 0.01	193
Perhexiline	1200 μM		mouse; Crl/CD-l(1CR)BR Swiss	liver mitochondria	Measurement of activities of acyl-CoA dehydrogenases	decrease	Positive	p < 0.01	193
Perhexiline	200 μM		mouse; Crl/CD-l(1CR)BR Swiss	liver mitochondria	Measurement of activities of acyl-CoA dehydrogenases	decrease	Positive	p < 0.01	193
Perhexiline	400 μM		mouse; Crl/CD-l(1CR)BR Swiss	liver mitochondria	Measurement of activities of acyl-CoA dehydrogenases	decrease	Positive	p < 0.01	193
Perhexiline	800 μM		mouse; Crl/CD-l(1CR)BR Swiss	liver mitochondria	Measurement of activities of acyl-CoA dehydrogenases	decrease	Positive	p < 0.01	193
Perhexiline	1200 μM		mouse; Crl/CD-l(1CR)BR Swiss	liver mitochondria	Measurement of activities of acyl-CoA dehydrogenases	decrease	Positive	p < 0.01	193
Perhexiline	1600 μM		mouse; Crl/CD-l(1CR)BR Swiss	liver mitochondria	Measurement of activities of acyl-CoA dehydrogenases	decrease	Positive	p < 0.01	193
Perhexiline	400 μM		mouse; Crl/CD-l(1CR)BR Swiss	liver mitochondria	Measurement of activities of acyl-CoA dehydrogenases	decrease	Positive	p < 0.05	193
Perhexiline	800 μM		mouse; Crl/CD-l(1CR)BR Swiss	liver mitochondria	Measurement of activities of acyl-CoA dehydrogenases	decrease	Positive	p < 0.01	193
Perhexiline	1200 μM		mouse; Crl/CD-l(1CR)BR Swiss	liver mitochondria	Measurement of activities of acyl-CoA dehydrogenases	decrease	Positive	p < 0.01	193
Perhexiline	1600 μM		mouse; Crl/CD-l(1CR)BR Swiss	liver mitochondria	Measurement of activities of acyl-CoA dehydrogenases	decrease	Positive	p < 0.01	193
Perhexiline						decrease	Positive		16
Perhexiline						decrease	Positive		16
buprenorphine	100 μM		rat	liver mitochondria	the mitochondrial membrane potential assessed by the fluorescence of safranine.	affect	Positive		235
Tianeptine	0.0625 mmol/kg i.p.		mouse		in vivo	affect	Positive		237
Perhexiline						decrease	Positive		17
Perhexiline						decrease	Positive		17
Trimetazidine						decrease	Positive		17
ranolazine						decrease	Positive		17
tetracyclines			mouse	liver mitochondria		affect	Positive		236
5-Hydroxydecanoate	100 μm					decrease	Positive		189
5-Hydroxydecanoate	K1/2 values 45-75 microM			heart and liver mitochondria from rat		decrease	Positive		190
Ibuprofen						affect	Positive		239
Perhexiline	77 μmol/L		rat	cardiac mitochondria	CPT-1 activity was measured by the formation of palmitoyl-[3H]-carnitine from palmitoyl-CoA and [3H]-I- carnitine,	affect	Positive	IC50	240
Perhexiline	148 μmol/L		rat	hepatic mitochondria	CPT-1 activity was measured by the formation of palmitoyl-[3H]-carnitine from palmitoyl-CoA and [3H]-I- carnitine,	affect	Positive	IC50	240
Amiodarone	228 μmol/L		rat	cardiac and hepatic mitochondria	CPT-1 activity was measured by the formation of palmitoyl-[3H]-carnitine from palmitoyl-CoA and [3H]-I- carnitine,	affect	Positive	IC50	240
FOX-988						decrease	Positive		28
Acetaminophen	>400μM	>400	mice	Lean mice vs Ob/ob mice	Measurement of oxygen consumption in the presence of ADP (state 3) and the different substrates was carried out on the Mitologics screening platform		Positive	EC20	227
Sdz-51641						decrease	Positive		28
Salicylic acid						decrease	Positive		32
Irinotecan	6μM	10	mice	Lean mice vs Ob/ob mice	Measurement of oxygen consumption in the presence of ADP (state 3) and the different substrates was carried out on the Mitologics screening platform		Positive	EC20	227
Methotrexate	44μM	42	mice	Lean mice vs Ob/ob mice	Measurement of oxygen consumption in the presence of ADP (state 3) and the different substrates was carried out on the Mitologics screening platform		Positive	EC20	227
Troglitazone						affect	Positive		227
Valproic Acid						affect	Positive		227
Perhexiline						decrease	Positive		35
Amiodarone	20 μmol/L		rat; Sprague–Dawley	liver mitochondria	Measurement of beta oxidation and ketone body formation	decrease	Positive	p < 0.01	4
Amiodarone	50 μmol/L		rat; Sprague–Dawley	liver mitochondria	Measurement of beta oxidation and ketone body formation	decrease	Positive	p < 0.01	4
Amiodarone	80 μmol/L		rat; Sprague–Dawley	liver mitochondria	Measurement of beta oxidation and ketone body formation	decrease	Positive	p < 0.01	4
Amiodarone	100 μmol/L		rat; Sprague–Dawley	liver mitochondria	Measurement of beta oxidation and ketone body formation	decrease	Positive	p < 0.01	4
benzarone	20 μmol/L		rat; Sprague–Dawley	liver mitochondria	Measurement of beta oxidation and ketone body formation	decrease	Positive	p < 0.01	4
benzarone	50 μmol/L		rat; Sprague–Dawley	liver mitochondria	Measurement of beta oxidation and ketone body formation	decrease	Positive	p < 0.01	4
benzarone	100 μmol/L		rat; Sprague–Dawley	liver mitochondria	Measurement of beta oxidation and ketone body formation	decrease	Positive	p < 0.01	4
benzbromarone	2 μmol/L		rat; Sprague–Dawley	liver mitochondria	Measurement of beta oxidation and ketone body formation	decrease	Positive	p < 0.05	4
benzbromarone	5 μmol/L		rat; Sprague–Dawley	liver mitochondria	Measurement of beta oxidation and ketone body formation	decrease	Positive	p < 0.01	4
benzbromarone	10 μmol/L		rat; Sprague–Dawley	liver mitochondria	Measurement of beta oxidation and ketone body formation	decrease	Positive	p < 0.01	4
benzbromarone	50 μmol/L		rat; Sprague–Dawley	liver mitochondria	Measurement of beta oxidation and ketone body formation	decrease	Positive	p < 0.01	4
2‐Butylbenzofuran	100 μmol/L		rat; Sprague–Dawley	liver mitochondria	Measurement of beta oxidation and ketone body formation	decrease	Positive	p < 0.01	4
Etomoxir						decrease	Positive		35
Salicylic acid						decrease	Positive		35
Carbamazepine	>400μM	341	mice	Lean mice vs Ob/ob mice	Measurement of oxygen consumption in the presence of ADP (state 3) and the different substrates was carried out on the Mitologics screening platform		Positive	EC20	227
Diclofenac	47μM	11*	mice	Lean mice vs Ob/ob mice	Measurement of oxygen consumption in the presence of ADP (state 3) and the different substrates was carried out on the Mitologics screening platform		Positive	EC20	227
Ibuprofen	287μM	80*	mice	Lean mice vs Ob/ob mice	Measurement of oxygen consumption in the presence of ADP (state 3) and the different substrates was carried out on the Mitologics screening platform		Positive	EC20	227
Amiodarone	100 μmol/L		rat; Sprague–Dawley	liver mitochondria	Measurement of acyl‐CoA dehydrogenase activity	decrease	Positive	28% inhibition	4
benzarone	100 μmol/L		rat; Sprague–Dawley	liver mitochondria	Measurement of acyl‐CoA dehydrogenase activity	decrease	Positive	33% inhibition	4
benzbromarone	100 μmol/L		rat; Sprague–Dawley	liver mitochondria	Measurement of acyl‐CoA dehydrogenase activity	decrease	Positive	34% inhibition	4
2‐Butylbenzofuran	100 μmol/L		rat; Sprague–Dawley	liver mitochondria	Measurement of acyl‐CoA dehydrogenase activity	decrease	Positive	22% inhibition	4
benzarone	100 μmol/L		rat; Sprague–Dawley	liver mitochondria	Measurement of β‐ketothiolase activity	decrease	Positive	11% inhibition	4
benzbromarone	100 μmol/L		rat; Sprague–Dawley	liver mitochondria	Measurement of β‐ketothiolase activity	decrease	Positive	25% inhibition	4
Salicylic acid	>400μM	>400	mice	Lean mice vs Ob/ob mice	Measurement of oxygen consumption in the presence of ADP (state 3) and the different substrates was carried out on the Mitologics screening platform		Positive	EC20	227
Tamoxifen	4μM	11	mice	Lean mice vs Ob/ob mice	Measurement of oxygen consumption in the presence of ADP (state 3) and the different substrates was carried out on the Mitologics screening platform		Positive	EC20	227
Perhexiline			rat	hepatocytes		affect	Positive		238
Zidovudine	79μM	83	mice	Lean mice vs Ob/ob mice	Measurement of oxygen consumption in the presence of ADP (state 3) and the different substrates was carried out on the Mitologics screening platform		Positive	EC20	227
Acetaminophen						affect	Positive		227
amineptine						decrease	Positive		54
pirprofen						decrease	Positive		59
Propofol							Positive		197
Salicylic acid						affect	Positive		227
Ibuprofen						affect	Positive		227
Dronedarone	10µM	24hr		isolated rat liver mitochondria, and the human hepatoma cell line HepG2		inhibit	Positive		271
Amiodarone	20µM	24hr		isolated rat liver mitochondria, and the human hepatoma cell line HepG2		inhibit	Positive		271
ranolazine	25μM	24hr		T47D cells	quantifies the conversion of [9,10-3H(N)]-palmitic acid to 3H2O with diffusion	stimulate	Positive	Student’s two-tail t-test, where p < 0.05	273
Trimetazidine	100 μM	24hr		T47D cells	quantifies the conversion of [9,10-3H(N)]-palmitic acid to 3H2O with diffusion	stimulate	Positive	Student’s two-tail t-test, where p < 0.05	273
Etomoxir	0.1 to 50 μM	24hr		MCF-7 and T47D cells	quantifies the conversion of [9,10-3H(N)]-palmitic acid to 3H2O with diffusion	inhibition	Positive	Student’s two-tail t-test, where p < 0.05	273
Oxfenicine	1.5 to 4.5mM	24hr		T47D cells	quantifies the conversion of [9,10-3H(N)]-palmitic acid to 3H2O with diffusion	inhibition	Positive	Student’s two-tail t-test, where p < 0.05	273
Carnitine	0.5mM	24hr		U-937, MCF-7, and T47D	quantifies the conversion of [9,10-3H(N)]-palmitic acid to 3H2O with diffusion	stimulate	Positive		273
AICAR	1mM	24hr		U-937, MCF-7, and T47D	quantifies the conversion of [9,10-3H(N)]-palmitic acid to 3H2O with diffusion	stimulate	Positive		273
AICAR						stimulate	Positive		273
TDGA	<0.05/0.04		human/rat	hepatocytes	Fatty acid oxidation (FAO) was determined by measuring 14CO2 release from 14C-labeled palmitate	inhibition	Positive	IC50 (μM)	333
POCA	10.4/95.9		human/rat	hepatocytes	Fatty acid oxidation (FAO) was determined by measuring 14CO2 release from 14C-labeled palmitate	inhibition	Positive	IC50 (μM)	333
Etomoxir	0.29/0.34		human/rat	hepatocytes	Fatty acid oxidation (FAO) was determined by measuring 14CO2 release from 14C-labeled palmitate	inhibition	Positive	IC50 (μM)	333
DET	1.8/4.4		human/rat	hepatocytes	Fatty acid oxidation (FAO) was determined by measuring 14CO2 release from 14C-labeled palmitate	inhibition	Positive	IC50 (μM)	333
aminocarnitine	−/−		human/rat	hepatocytes	Fatty acid oxidation (FAO) was determined by measuring 14CO2 release from 14C-labeled palmitate	inhibition	Positive	IC50 (μM)	333
palmitoylaminocarnitine	2.8/0.27		human/rat	hepatocytes	Fatty acid oxidation (FAO) was determined by measuring 14CO2 release from 14C-labeled palmitate	inhibition	Positive	IC50 (μM)	333
ST1326	4.0/0.98		human/rat	hepatocytes	Fatty acid oxidation (FAO) was determined by measuring 14CO2 release from 14C-labeled palmitate	inhibition	Positive	IC50 (μM)	333
ST2425	0.73/0.03		human/rat	hepatocytes	Fatty acid oxidation (FAO) was determined by measuring 14CO2 release from 14C-labeled palmitate	inhibition	Positive	IC50 (μM)	333
Trimetazidine	20.5/>100		human/rat	hepatocytes	Fatty acid oxidation (FAO) was determined by measuring 14CO2 release from 14C-labeled palmitate	inhibition	Positive	IC50 (μM)	333
Perhexiline	22.4/21.4		human/rat	hepatocytes	Fatty acid oxidation (FAO) was determined by measuring 14CO2 release from 14C-labeled palmitate	inhibition	Positive	IC50 (μM)	333
Amiodarone	28.5/>100		human/rat	hepatocytes	Fatty acid oxidation (FAO) was determined by measuring 14CO2 release from 14C-labeled palmitate	inhibition	Positive	IC50 (μM)	333
Oxfenicine	>100/>100		human/rat	hepatocytes	Fatty acid oxidation (FAO) was determined by measuring 14CO2 release from 14C-labeled palmitate	inhibition	Positive	IC50 (μM)	333
oxfenicine metabolite	33.3/>100		human/rat	hepatocytes	Fatty acid oxidation (FAO) was determined by measuring 14CO2 release from 14C-labeled palmitate	inhibition	Positive	IC50 (μM)	333
RO-25-0187	25.5/>100		human/rat	hepatocytes	Fatty acid oxidation (FAO) was determined by measuring 14CO2 release from 14C-labeled palmitate	inhibition	Positive	IC50 (μM)	333
Hypoglycin A							Positive		232
4-Pentenoic acid							Positive		232
2-bromooctanoic acid							Positive		232
2-tetradecylglycidic acid							Positive		232
2-bromopalmitic acid							Positive		232
Palmitoylcarnitine							Positive		232
Perhexiline	5 μM	72 hours	rat; Sprague-Dawley Crl:CD-1 (ICR) BR	hepatocytes	Measurement of beta oxidation	decrease	Positive	p < 0.05	193
Perhexiline	25 μM	24 hours	rat; Sprague-Dawley Crl:CD-1 (ICR) BR	hepatocytes	Measurement of beta oxidation	decrease	Positive	p < 0.05	193
Amiodarone						affect	Positive		227
Tamoxifen						affect	Positive		227

F02060101. mitochondrial fatty acid beta oxidation
F02060102. fatty acyl-CoA biosynthesis
F02060103. carnitine shuttle
F02060104. carnitine biosynthesis
F02060105. fatty acid biosynthetic
F02060106. acetyl-CoA biosynthesis

T021. carnitine palmitoyltransferases I
T022. Carnitine O-palmitoyltransferase 2, mitochondrial, EC 2.3.1.21
T026. 3-ketoacyl-CoA thiolase, mitochondrial
T027. Long-chain-fatty-acid--CoA ligase
T027001. Long-chain-fatty-acid--CoA ligase 1
T028. Short-chain specific acyl-CoA dehydrogenase, mitochondrial
T029. Medium-chain specific acyl-CoA dehydrogenase, mitochondrial
T030. Long-chain specific acyl-CoA dehydrogenase, mitochondrial
T032. Short/branched chain specific acyl-CoA dehydrogenase, mitochondrial
T034. Medium-chain acyl-CoA ligase ACSF2, mitochondrial
T047. Acetyl-CoA carboxylase 2
T056. Isovaleryl-CoA dehydrogenase, mitochondrial
T417. 5'-AMP-activated protein kinase catalytic subunit alpha-2