General Information of the Protein
Protein ID
PT02750
Protein Name
Microsomal triglyceride transfer protein large subunit
Gene Name
MTTP
Secondarily
Gene Name
MTP
Sequence
MILLAVLFLCFISSYSASVKGHTTGLSLNNDRLYKLTYSTEVLLDRGKGKLQDSVGYRISSNVDVALLWRNPDGDDDQLIQITMKDVNVENVNQQRGEKSIFKGKSPSKIMGKENLEALQRPTLLHLIHGKVKEFYSYQNEAVAIENIKRGLASLFQTQLSSGTTNEVDISGNCKVTYQAHQDKVIKIKALDSCKIARSGFTTPNQVLGVSSKATSVTTYKIEDSFVIAVLAEETHNFGLNFLQTIKGKIVSKQKLELKTTEAGPRLMSGKQAAAIIKAVDSKYTAIPIVGQVFQSHCKGCPSLSELWRSTRKYLQPDNLSKAEAVRNFLAFIQHLRTAKKEEILQILKMENKEVLPQLVDAVTSAQTSDSLEAILDFLDFKSDSSIILQERFLYACGFASHPNEELLRALISKFKGSIGSSDIRETVMIITGTLVRKLCQNEGCKLKAVVEAKKLILGGLEKAEKKEDTRMYLLALKNALLPEGIPSLLKYAEAGEGPISHLATTALQRYDLPFITDEVKKTLNRIYHQNRKVHEKTVRTAAAAIILNNNPSYMDVKNILLSIGELPQEMNKYMLAIVQDILRFEMPASKIVRRVLKEMVAHNYDRFSRSGSSSAYTGYIERSPRSASTYSLDILYSGSGILRRSNLNIFQYIGKAGLHGSQVVIEAQGLEALIAATPDEGEENLDSYAGMSAILFDVQLRPVTFFNGYSDLMSKMLSASGDPISVVKGLILLIDHSQELQLQSGLKANIEVQGGLAIDISGAMEFSLWYRESKTRVKNRVTVVITTDITVDSSFVKAGLETSTETEAGLEFISTVQFSQYPFLVCMQMDKDEAPFRQFEKKYERLSTGRGYVSQKRKESVLAGCEFPLHQENSEMCKVVFAPQPDSTSSGWF
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Organism
Homo sapiens, Human
Protein Classification
Other cytosolic protein
Function
Catalyzes the transport of triglyceride, cholesteryl ester, and phospholipid between phospholipid surfaces (PubMed:23475612, PubMed:8939939, PubMed:26224785, PubMed:25108285, PubMed:22236406, PubMed:16478722, PubMed:15897609, PubMed:8876250). Required for the assembly and secretion of plasma lipoproteins that contain apolipoprotein B (PubMed:23475612, PubMed:8939939, PubMed:26224785, PubMed:8876250, PubMed:16478722). May be involved in regulating cholesteryl ester biosynthesis in cells that produce lipoproteins (By similarity).
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Uniprot ID
Primary ID:
P55157

Secondarily ID:
A8K428
Q08AM4
Q6P5T3
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Ensembl ID
ENSG00000138823
HGNC ID
HGNC:7467
Subcellular Location
Endoplasmic reticulum
Golgi apparatus
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: CL000063 , Hep-G2
Compound ID Compound Name Compound Formula
CP0258517
9-(4-{5-Methyl-4-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-benzoimidazol-1-yl}-butyl)-9H-fluorene-9-carboxylic acid (2,2,2-trifluoro-ethyl)-amide
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C42H34F6N4O2
 1
1
IC50 = 0.02 nM
   TI
   LI
   LO
   TS
CP0250596
9-(4-{2,5-Dimethyl-4-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-benzoimidazol-1-yl}-butyl)-9H-fluorene-9-carboxylic acid (2,2,2-trifluoro-ethyl)-amide
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C43H36F6N4O2
 1
1
IC50 = 0.03 nM
   TI
   LI
   LO
   TS
CP0101923
9-(4-{2-Isopropyl-4-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-benzoimidazol-1-yl}-butyl)-9H-fluorene-9-carboxylic acid (2,2,2-trifluoro-ethyl)-amide
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C44H38F6N4O2
 1
1
IC50 = 0.06 nM
   TI
   LI
   LO
   TS
CP0409230
9-(4-{2-Methyl-4-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-benzoimidazol-1-yl}-butyl)-9H-fluorene-9-carboxylic acid (2,2,2-trifluoro-ethyl)-amide
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C42H34F6N4O2
 1
1
IC50 = 0.15 nM
   TI
   LI
   LO
   TS
CP0225408
9-(4-{4-[(4'-Trifluoromethyl-biphenyl-2-carbonyl)-amino]-benzoimidazol-1-yl}-butyl)-9H-fluorene-9-carboxylic acid (2,2,2-trifluoro-ethyl)-amide
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C41H32F6N4O2
 1
1
IC50 = 0.24 nM
   TI
   LI
   LO
   TS
CP0392790
N-[(1S)-2-[(4-fluorophenyl)methyl-methylamino]-2-oxo-1-phenylethyl]-2-[[2-(4-propylphenyl)benzoyl]amino]quinoline-6-carboxamide
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C42H37FN4O3
 1
1
IC50 = 0.44 nM
   TI
   LI
   LO
   TS
CP0482559
2-[[2-(4-ethylphenyl)benzoyl]amino]-N-[(1S)-2-[(4-fluorophenyl)methyl-methylamino]-2-oxo-1-phenylethyl]quinoline-6-carboxamide
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C41H35FN4O3
 1
1
IC50 = 0.55 nM
   TI
   LI
   LO
   TS
CP0392799
2-[[2-(4-tert-butylphenyl)benzoyl]amino]-N-[(1S)-2-(methylamino)-2-oxo-1-phenylethyl]quinoline-6-carboxamide
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C36H34N4O3
 1
1
IC50 = 0.56 nM
   TI
   LI
   LO
   TS
CP0372888
(R)-6-methyl-N-(2-(thiazol-2-ylmethylamino)-2,3-dihydro-1H-inden-5-yl)-4'-(trifluoromethyl)biphenyl-2-carboxamide
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C28H24F3N3OS
 1
1
IC50 = 0.6 nM
   TI
   LI
   LO
   TS
CP0381022
N-[(1S)-2-[(4-fluorophenyl)methyl-methylamino]-2-oxo-1-phenylethyl]-2-[[2-(4-propan-2-ylphenyl)benzoyl]amino]quinoline-6-carboxamide
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C42H37FN4O3
 1
1
IC50 = 0.6 nM
   TI
   LI
   LO
   TS
CP0452615
N-[(1S)-2-(methylamino)-2-oxo-1-phenylethyl]-2-[[2-(4-propan-2-yloxyphenyl)benzoyl]amino]quinoline-6-carboxamide
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C35H32N4O4
 1
1
IC50 = 0.63 nM
   TI
   LI
   LO
   TS
CP0392788
N-[(1S)-2-[(4-fluorophenyl)methyl-methylamino]-2-oxo-1-phenylethyl]-2-[[2-[4-(trifluoromethyl)phenyl]benzoyl]amino]quinoline-6-carboxamide
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C40H30F4N4O3
 1
1
IC50 = 0.74 nM
   TI
   LI
   LO
   TS
CP0392798
N-[(1S)-2-[(4-fluorophenyl)methyl-methylamino]-2-oxo-1-phenylethyl]-2-[[2-(4-propan-2-yloxyphenyl)benzoyl]amino]quinoline-6-carboxamide
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C42H37FN4O4
 1
1
IC50 = 0.77 nM
   TI
   LI
   LO
   TS
CP0459904
9-(4-{4-[(4''-Trifluoromethyl-biphenyl-2-carbonyl)-amino]-piperidin-1-yl}-butyl)-9H-fluorene-9-carboxylic acid (2,2,2-trifluoro-ethyl)-amide
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C39H37F6N3O2
 1
1
IC50 = 0.8 nM
   TI
   LI
   LO
   TS
CP0525493
N-[(1S)-2-[(4-fluorophenyl)methyl-methylamino]-2-oxo-1-phenylethyl]-2-[[2-[4-[(2-methylpropan-2-yl)oxy]phenyl]benzoyl]amino]quinoline-6-carboxamide
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C43H39FN4O4
 1
1
IC50 = 0.83 nM
   TI
   LI
   LO
   TS
CP0245589
(R)-methyl 5-(6-methyl-4'-(trifluoromethyl)biphenyl-2-ylcarboxamido)-2,3-dihydro-1H-inden-2-ylcarbamate
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C26H23F3N2O3
 1
1
IC50 = 0.9 nM
   TI
   LI
   LO
   TS
CP0381024
N-[(1S)-2-[(4-fluorophenyl)methyl-methylamino]-2-oxo-1-phenylethyl]-2-[[2-[4-(1-hydroxy-2-methylpropan-2-yl)phenyl]benzoyl]amino]quinoline-6-carboxamide
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C43H39FN4O4
 1
1
IC50 = 1.1 nM
   TI
   LI
   LO
   TS
CP0376544
2-[[2-(4-tert-butylphenyl)benzoyl]amino]-N-[(1S)-2-[(4-fluorophenyl)methyl-methylamino]-2-oxo-1-phenylethyl]quinoline-6-carboxamide
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C43H39FN4O3
 1
1
IC50 = 1.2 nM
   TI
   LI
   LO
   TS
CP0381026
2-[[2-(4-tert-butylphenyl)benzoyl]amino]-N-[(1S)-2-[(4-fluorophenyl)methylamino]-2-oxo-1-phenylethyl]quinoline-6-carboxamide
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C42H37FN4O3
 1
1
IC50 = 1.2 nM
   TI
   LI
   LO
   TS
CP0449532
N-[(1S)-2-[(4-fluorophenyl)methylamino]-2-oxo-1-phenylethyl]-2-[[2-(4-propan-2-yloxyphenyl)benzoyl]amino]quinoline-6-carboxamide
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C41H35FN4O4
 1
1
IC50 = 1.21 nM
   TI
   LI
   LO
   TS
CP0453313
N-[(1S)-2-amino-2-oxo-1-phenylethyl]-1-methyl-5-[[2-[4-(trifluoromethyl)phenyl]benzoyl]amino]indole-2-carboxamide
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C32H25F3N4O3
 1
1
IC50 = 1.5 nM
   TI
   LI
   LO
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CP0482558
1-methyl-N-[(1S)-2-(methylamino)-2-oxo-1-phenylethyl]-5-[[2-[4-(trifluoromethyl)phenyl]benzoyl]amino]indole-2-carboxamide
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C33H27F3N4O3
 1
1
IC50 = 1.8 nM
   TI
   LI
   LO
   TS
CP0447979
N-[(1S)-2-[(4-fluorophenyl)methyl-methylamino]-2-oxo-1-phenylethyl]-2-[[2-(4-methylphenyl)benzoyl]amino]quinoline-6-carboxamide
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C40H33FN4O3
 1
1
IC50 = 2.2 nM
   TI
   LI
   LO
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CP0039065
N-[(1S)-2-[benzyl(methyl)amino]-2-oxo-1-phenylethyl]-1-methyl-5-[[2-[4-(trifluoromethyl)phenyl]benzoyl]amino]indole-2-carboxamide
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C40H33F3N4O3
 1
1
IC50 = 2.7 nM
   TI
   LI
   LO
   TS
CP0392789
N-[(1S)-2-[(4-fluorophenyl)methyl-methylamino]-2-oxo-1-phenylethyl]-2-[(2-phenylbenzoyl)amino]quinoline-6-carboxamide
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C39H31FN4O3
 1
1
IC50 = 2.8 nM
   TI
   LI
   LO
   TS
CP0525495
2-[[2-(4-ethoxyphenyl)benzoyl]amino]-N-[(1S)-2-[(4-fluorophenyl)methyl-methylamino]-2-oxo-1-phenylethyl]quinoline-6-carboxamide
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C41H35FN4O4
 1
1
IC50 = 2.8 nM
   TI
   LI
   LO
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CP0435527
N-[(1S)-2-[(4-fluorophenyl)methyl-methylamino]-2-oxo-1-phenylethyl]-2-[[2-(4-methoxyphenyl)benzoyl]amino]quinoline-6-carboxamide
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C40H33FN4O4
 1
1
IC50 = 3 nM
   TI
   LI
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CP0290967
(R)-6-methyl-N-(2-(pyridin-2-ylmethylamino)-2,3-dihydro-1H-inden-5-yl)-4'-(trifluoromethyl)biphenyl-2-carboxamide
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C30H26F3N3O
 1
1
IC50 = 3.5 nM
   TI
   LI
   LO
   TS
CP0089850
(S)-methyl 5-(6-methyl-4'-(trifluoromethyl)biphenyl-2-ylcarboxamido)-2,3-dihydro-1H-inden-2-ylcarbamate
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C26H23F3N2O3
 1
1
IC50 = 4.3 nM
   TI
   LI
   LO
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CP0381023
N-[(1S)-2-[(4-fluorophenyl)methylamino]-2-oxo-1-phenylethyl]-2-[[2-[4-(1-hydroxy-2-methylpropan-2-yl)phenyl]benzoyl]amino]quinoline-6-carboxamide
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C42H37FN4O4
 1
1
IC50 = 4.3 nM
   TI
   LI
   LO
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CP0527198
2-[4-[2-[[6-[[(1S)-2-[(4-fluorophenyl)methyl-methylamino]-2-oxo-1-phenylethyl]carbamoyl]quinolin-2-yl]carbamoyl]phenyl]phenyl]-2-methylpropanoic acid
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C43H37FN4O5
 1
1
IC50 = 7.5 nM
   TI
   LI
   LO
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CP0404902
N-[(1S)-2-[(4-fluorophenyl)methyl-methylamino]-2-oxo-1-phenylethyl]-2-[[2-[4-(1-hydroxypropan-2-yloxy)phenyl]benzoyl]amino]quinoline-6-carboxamide
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C42H37FN4O5
 1
1
IC50 = 9.4 nM
   TI
   LI
   LO
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CP0404904
N-[(1S)-2-[(4-fluorophenyl)methyl-methylamino]-2-oxo-1-phenylethyl]-2-[[2-(4-hydroxyphenyl)benzoyl]amino]quinoline-6-carboxamide
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C39H31FN4O4
 1
1
IC50 = 11 nM
   TI
   LI
   LO
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CP0381025
2-[4-[2-[[6-[[(1S)-2-[(4-fluorophenyl)methylamino]-2-oxo-1-phenylethyl]carbamoyl]quinolin-2-yl]carbamoyl]phenyl]phenyl]-2-methylpropanoic acid
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C42H35FN4O5
 1
1
IC50 = 12 nM
   TI
   LI
   LO
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CP0447981
2-[4-[2-[[6-[[(1S)-2-[(4-fluorophenyl)methyl-methylamino]-2-oxo-1-phenylethyl]carbamoyl]quinolin-2-yl]carbamoyl]phenyl]phenoxy]propanoic acid
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C42H35FN4O6
 1
1
IC50 = 22 nM
   TI
   LI
   LO
   TS
CP0506425
(S)-6-methyl-N-(2-(thiazol-2-ylmethylamino)-2,3-dihydro-1H-inden-5-yl)-4'-(trifluoromethyl)biphenyl-2-carboxamide
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C28H24F3N3OS
 1
1
IC50 = 140 nM
   TI
   LI
   LO
   TS
CP0510053
(S)-6-methyl-N-(2-(thiophen-2-ylmethylamino)-2,3-dihydro-1H-inden-5-yl)-4'-(trifluoromethyl)biphenyl-2-carboxamide
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C29H25F3N2OS
 1
1
IC50 = 140 nM
   TI
   LI
   LO
   TS
CP0421789
(S)-N-(2-(furan-2-ylmethylamino)-2,3-dihydro-1H-inden-5-yl)-6-methyl-4'-(trifluoromethyl)biphenyl-2-carboxamide
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C29H25F3N2O2
 1
1
IC50 = 150 nM
   TI
   LI
   LO
   TS
CP0452610
6-methyl-N-((2S)-2-(1-phenylethylamino)-2,3-dihydro-1H-inden-5-yl)-4'-(trifluoromethyl)biphenyl-2-carboxamide
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C32H29F3N2O
 1
1
IC50 = 180 nM
   TI
   LI
   LO
   TS
CP0510097
(S)-6-methyl-N-(2-(quinolin-3-ylmethylamino)-2,3-dihydro-1H-inden-5-yl)-4'-(trifluoromethyl)biphenyl-2-carboxamide
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C34H28F3N3O
 1
1
IC50 = 1400 nM
   TI
   LI
   LO
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CP0187300
(S)-6-methyl-N-(2-(pyridin-2-ylmethylamino)-2,3-dihydro-1H-inden-5-yl)-4'-(trifluoromethyl)biphenyl-2-carboxamide
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C30H26F3N3O
 1
1
IC50 = 2350 nM
   TI
   LI
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Biochemical Assays
Compound ID Compound Name Compound Formula
CP0250596
9-(4-{2,5-Dimethyl-4-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-benzoimidazol-1-yl}-butyl)-9H-fluorene-9-carboxylic acid (2,2,2-trifluoro-ethyl)-amide
   Show/Hide
C43H36F6N4O2
 1
1 IC50 = 1 nM
CP0258517
9-(4-{5-Methyl-4-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-benzoimidazol-1-yl}-butyl)-9H-fluorene-9-carboxylic acid (2,2,2-trifluoro-ethyl)-amide
   Show/Hide
C42H34F6N4O2
 1
1 IC50 = 1 nM
CP0409230
9-(4-{2-Methyl-4-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-benzoimidazol-1-yl}-butyl)-9H-fluorene-9-carboxylic acid (2,2,2-trifluoro-ethyl)-amide
   Show/Hide
C42H34F6N4O2
 1
1 IC50 = 1 nM
CP0101923
9-(4-{2-Isopropyl-4-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-benzoimidazol-1-yl}-butyl)-9H-fluorene-9-carboxylic acid (2,2,2-trifluoro-ethyl)-amide
   Show/Hide
C44H38F6N4O2
 1
1 IC50 = 4 nM
CP0225408
9-(4-{4-[(4'-Trifluoromethyl-biphenyl-2-carbonyl)-amino]-benzoimidazol-1-yl}-butyl)-9H-fluorene-9-carboxylic acid (2,2,2-trifluoro-ethyl)-amide
   Show/Hide
C41H32F6N4O2
 1
1 IC50 = 5 nM
CP0089850
(S)-methyl 5-(6-methyl-4'-(trifluoromethyl)biphenyl-2-ylcarboxamido)-2,3-dihydro-1H-inden-2-ylcarbamate
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C26H23F3N2O3
 1
1 IC50 = 70 nM
CP0245589
(R)-methyl 5-(6-methyl-4'-(trifluoromethyl)biphenyl-2-ylcarboxamido)-2,3-dihydro-1H-inden-2-ylcarbamate
   Show/Hide
C26H23F3N2O3
 1
1 IC50 = 70 nM
CP0187300
(S)-6-methyl-N-(2-(pyridin-2-ylmethylamino)-2,3-dihydro-1H-inden-5-yl)-4'-(trifluoromethyl)biphenyl-2-carboxamide
   Show/Hide
C30H26F3N3O
 1
1 IC50 = 100 nM
CP0290967
(R)-6-methyl-N-(2-(pyridin-2-ylmethylamino)-2,3-dihydro-1H-inden-5-yl)-4'-(trifluoromethyl)biphenyl-2-carboxamide
   Show/Hide
C30H26F3N3O
 1
1 IC50 = 410 nM
Clinical Information about the Protein
Target 1 ( Microsomal triglyceride transfer protein (MTTP) )
Target Type Successful Target
Disease 1 Target-related Disease  1
1 Familial hypercholesterolemia [ICD-11: 5C80.00]
Approved Drug(s) 1 Approved Drug  1
1 BMS-201038 Approved
Familial hypercholesterolemia