General Information of the Protein
Protein ID
PT00969
Protein Name
Monocarboxylate transporter 1
Secondarily
Protein Name
Solute carrier family 16 member 1
Gene Name
SLC16A1
Secondarily
Gene Name
MCT1
Sequence
MPPAVGGPVGYTPPDGGWGWAVVIGAFISIGFSYAFPKSITVFFKEIEGIFHATTSEVSWISSIMLAVMYGGGPISSILVNKYGSRIVMIVGGCLSGCGLIAASFCNTVQQLYVCIGVIGGLGLAFNLNPALTMIGKYFYKRRPLANGLAMAGSPVFLCTLAPLNQVFFGIFGWRGSFLILGGLLLNCCVAGALMRPIGPKPTKAGKDKSKASLEKAGKSGVKKDLHDANTDLIGRHPKQEKRSVFQTINQFLDLTLFTHRGFLLYLSGNVIMFFGLFAPLVFLSSYGKSQHYSSEKSAFLLSILAFVDMVARPSMGLVANTKPIRPRIQYFFAASVVANGVCHMLAPLSTTYVGFCVYAGFFGFAFGWLSSVLFETLMDLVGPQRFSSAVGLVTIVECCPVLLGPPLLGRLNDMYGDYKYTYWACGVVLIISGIYLFIGMGINYRLLAKEQKANEQKKESKEEETSIDVAGKPNEVTKAAESPDQKDTDGGPKEEESPV
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Organism
Homo sapiens, Human
Protein Classification
Transporter
>
Electrochemical transporter
>
SLC superfamily of solute carriers
>
SLC16 family of monocarboxylate transporters
Function
Bidirectional proton-coupled monocarboxylate transporter (PubMed:12946269, PubMed:33333023, PubMed:32946811). Catalyzes the rapid transport across the plasma membrane of many monocarboxylates such as lactate, pyruvate, acetate and the ketone bodies acetoacetate and beta-hydroxybutyrate, and thus contributes to the maintenance of intracellular pH (PubMed:12946269, PubMed:33333023). The transport direction is determined by the proton motive force and the concentration gradient of the substrate monocarboxylate. MCT1 is a major lactate exporter (By similarity). Plays a role in cellular responses to a high-fat diet by modulating the cellular levels of lactate and pyruvate that contribute to the regulation of central metabolic pathways and insulin secretion, with concomitant effects on plasma insulin levels and blood glucose homeostasis (By similarity). Facilitates the protonated monocarboxylate form of succinate export, that its transient protonation upon muscle cell acidification in exercising muscle and ischemic heart (PubMed:32946811). Functions via alternate outward- and inward-open conformation states. Protonation and deprotonation of 309-Asp is essential for the conformational transition (PubMed:33333023).
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Uniprot ID
Primary ID:
P53985

Secondarily ID:
Q49A45
Q5T8R6
Q9NSJ9
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Ensembl ID
ENSG00000155380
HGNC ID
HGNC:10922
Subcellular Location
Cell membrane
Basolateral cell membrane
Apical cell membrane
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000127 , INS-1
Compound ID Compound Name Compound Formula
CP0159148
5-[(3-hydroxypropyl)sulfanyl]-3-methyl-1-(2-methylpropyl)-6-(naphthalen-1-ylmethyl)-1H,2H,3H,4H-thieno[2,3-d]pyrimidine-2,4-dione
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C25H28N2O3S2
 1
1
Ki = 0.302 nM
   TI
   LI
   LO
   TS
CP0303011
5-[(3-hydroxypropyl)sulfanyl]-3-methyl-1-(2-methylpropyl)-6-{[2-(trifluoromethyl)phenyl]methyl}-1H,2H,3H,4H-thieno[2,3-d]pyrimidine-2,4-dione
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C22H25F3N2O3S2
 1
1
Ki = 0.5012 nM
   TI
   LI
   LO
   TS
CP0035405
7-[(3-hydroxypropyl)sulfanyl]-2-methyl-4-(2-methylpropyl)-6-(naphthalen-1-ylmethyl)-1H,2H,6H-pyrrolo[3,4-d]pyridazin-1-one
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C25H29N3O2S
 1
1
Ki = 0.7079 nM
   TI
   LI
   LO
   TS
CP0194005
5-{[(3R)-3-hydroxypyrrolidin-1-yl]carbonyl}-3-methyl-1-(2-methylpropyl)-6-(quinolin-4-ylmethyl)-1H,2H,3H,4H-thieno[2,3-d]pyrimidine-2,4-dione
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C26H28N4O4S
 1
1
Ki = 3.311 nM
   TI
   LI
   LO
   TS
CP0159143
3-methyl-1-(2-methylpropyl)-5-(pyrrolidin-1-ylcarbonyl)-6-{[2-(trifluoromethyl)phenyl]methyl}-1H,2H,3H,4H-thieno[2,3-d]pyrimidine-2,4-dione
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C24H26F3N3O3S
 1
1
Ki = 5.623 nM
   TI
   LI
   LO
   TS
CP0172933
5-{[(3R)-3-hydroxypyrrolidin-1-yl]carbonyl}-6-(1H-indol-3-ylmethyl)-3-methyl-1-(2-methylpropyl)-1H,2H,3H,4H-thieno[2,3-d]pyrimidine-2,4-dione
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C25H28N4O4S
 1
1
Ki = 6.31 nM
   TI
   LI
   LO
   TS
CP0384188
5-(2,5-dihydropyrrole-1-carbonyl)-3-methyl-1-(2-methylpropyl)-6-[[2-(trifluoromethyl)phenyl]methyl]thieno[2,3-d]pyrimidine-2,4-dione
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C24H24F3N3O3S
 1
1
Ki = 10.72 nM
   TI
   LI
   LO
   TS
CP0903610
6-[[4-azido-3-(iodo-125I)phenyl]methyl]-2,6-dihydro-2-methyl-4-(2-methylpropyl)-1H-pyrrolo[3,4-d]pyridazin-1-one
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C18H19IN6O
 1
1
Ki = 23 nM
   TI
   LI
   LO
   TS
CP0411900
1-Isobutyl-3-methyl-6-naphthalen-1-ylmethyl-1,6-dihydro-pyrrolo[3,4-d]pyrimidine-2,4-dione
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C22H23N3O2
 1
1
Ki = 46.77 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0159148
5-[(3-hydroxypropyl)sulfanyl]-3-methyl-1-(2-methylpropyl)-6-(naphthalen-1-ylmethyl)-1H,2H,3H,4H-thieno[2,3-d]pyrimidine-2,4-dione
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C25H28N2O3S2
 2
1 Ki = 0.08 nM
2 Ki = 0.28 nM
CP0035405
7-[(3-hydroxypropyl)sulfanyl]-2-methyl-4-(2-methylpropyl)-6-(naphthalen-1-ylmethyl)-1H,2H,6H-pyrrolo[3,4-d]pyridazin-1-one
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C25H29N3O2S
 1
1 Ki = 0.1 nM
CP0255268
5-[(3-hydroxypropyl)sulfanyl]-3-methyl-1-(2-methylpropyl)-6-(naphthalen-1-ylmethyl)-1H,2H,3H,4H,6H-pyrrolo[3,4-d]pyrimidine-2,4-dione
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C25H29N3O3S
 1
1 Ki = 0.33 nM
CP0303011
5-[(3-hydroxypropyl)sulfanyl]-3-methyl-1-(2-methylpropyl)-6-{[2-(trifluoromethyl)phenyl]methyl}-1H,2H,3H,4H-thieno[2,3-d]pyrimidine-2,4-dione
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C22H25F3N2O3S2
 1
1 Ki = 0.35 nM
CP0172933
5-{[(3R)-3-hydroxypyrrolidin-1-yl]carbonyl}-6-(1H-indol-3-ylmethyl)-3-methyl-1-(2-methylpropyl)-1H,2H,3H,4H-thieno[2,3-d]pyrimidine-2,4-dione
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C25H28N4O4S
 1
1 Ki = 0.79 nM
CP0194005
5-{[(3R)-3-hydroxypyrrolidin-1-yl]carbonyl}-3-methyl-1-(2-methylpropyl)-6-(quinolin-4-ylmethyl)-1H,2H,3H,4H-thieno[2,3-d]pyrimidine-2,4-dione
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C26H28N4O4S
 1
1 Ki = 4.8 nM
CP0159143
3-methyl-1-(2-methylpropyl)-5-(pyrrolidin-1-ylcarbonyl)-6-{[2-(trifluoromethyl)phenyl]methyl}-1H,2H,3H,4H-thieno[2,3-d]pyrimidine-2,4-dione
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C24H26F3N3O3S
 1
1 Ki = 5.5 nM
Clinical Information about the Protein
Target 1 ( Monocarboxylate transporter 1 (SLC16A1) )
Target Type Literature-reported Target