General Information of the Protein
Protein ID
PT00848
Protein Name
Interstitial collagenase
Secondarily
Protein Name
Fibroblast collagenase
Matrix metalloproteinase-1
Gene Name
MMP1
Secondarily
Gene Name
CLG
Sequence
MHSFPPLLLLLFWGVVSHSFPATLETQEQDVDLVQKYLEKYYNLKNDGRQVEKRRNSGPVVEKLKQMQEFFGLKVTGKPDAETLKVMKQPRCGVPDVAQFVLTEGNPRWEQTHLTYRIENYTPDLPRADVDHAIEKAFQLWSNVTPLTFTKVSEGQADIMISFVRGDHRDNSPFDGPGGNLAHAFQPGPGIGGDAHFDEDERWTNNFREYNLHRVAAHELGHSLGLSHSTDIGALMYPSYTFSGDVQLAQDDIDGIQAIYGRSQNPVQPIGPQTPKACDSKLTFDAITTIRGEVMFFKDRFYMRTNPFYPEVELNFISVFWPQLPNGLEAAYEFADRDEVRFFKGNKYWAVQGQNVLHGYPKDIYSSFGFPRTVKHIDAALSEENTGKTYFFVANKYWRYDEYKRSMDPGYPKMIAHDFPGIGHKVDAVFMKDGFFYFFHGTRQYKFDPKTKRILTLQKANSWFNCRKN
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Protease
>
Metallo protease
>
Metallo protease MAM clan
>
Metallo protease M10A subfamily
Function
Cleaves collagens of types I, II, and III at one site in the helical domain. Also cleaves collagens of types VII and X (PubMed:2557822, PubMed:2153297, PubMed:1645757). In case of HIV infection, interacts and cleaves the secreted viral Tat protein, leading to a decrease in neuronal Tat's mediated neurotoxicity (PubMed:16807369).
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Uniprot ID
Primary ID:
P03956

Secondarily ID:
P08156
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HGNC ID
HGNC:7155
Subcellular Location
Secreted
Extracellular space
Extracellular matrix
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: CL000068 , A-549
Compound ID Compound Name Compound Formula
CP0206920
(8S,9R,10S,11S,13S,14S,16S,17R)-9-fluoro-11-hydroxy-17-(2-hydroxyacetyl)-10,13,16-trimethyl-3-oxo-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthren-17-yl neopentylcarbamate
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C28H40FNO6
 1
1
EC50 = 0.1 nM
   TI
   LI
   LO
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CP0269641
(8S,9R,10S,11S,13S,14S,16S,17R)-9-fluoro-11-hydroxy-17-(2-hydroxyacetyl)-10,13,16-trimethyl-3-oxo-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthren-17-yl sec-butylcarbamate
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C27H38FNO6
 1
1
EC50 = 0.8 nM
   TI
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CP0201812
(8S,9R,10S,11S,13S,14S,16S,17R)-9-fluoro-11-hydroxy-17-(2-hydroxyacetyl)-10,13,16-trimethyl-3-oxo-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthren-17-yl cyclohexylcarbamate
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C29H40FNO6
 1
1
EC50 = 1.3 nM
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CP0310368
(11beta,16beta)-9-Fluoro-11,21-dihydroxy-16-methyl-3,20-dioxopregna-1,4-dien-17-yl tert-butylcarbamate
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C27H38FNO6
 1
1
EC50 = 1.6 nM
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CP0068420
(11beta,16beta)-9-Fluoro-11,21-dihydroxy-16-methyl-3,20-dioxopregna-1,4-dien-17-yl isopropylcarbamate
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C26H36FNO6
 1
1
EC50 = 1.9 nM
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CP0285811
(11beta,16beta)-9-Fluoro-11,21-dihydroxy-16-methyl-3,20-dioxopregna-1,4-dien-17-yl cyclopentylcarbamate
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C28H38FNO6
 1
1
EC50 = 2.8 nM
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CP0269645
Adamantan-1-yl-carbamic acid (8S,9R,10S,11S,13S,14S,16S,17R)-9-fluoro-11-hydroxy-17-(2-hydroxy-acetyl)-10,13,16-trimethyl-3-oxo-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthren-17-yl este
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C33H44FNO6
 1
1
EC50 = 3.4 nM
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CP0264394
(11beta,16beta)-9-Fluoro-11,21-dihydroxy-16-methyl-3,20-dioxopregna-1,4-dien-17-yl (1S)-1-phenylethylcarbamate
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C31H38FNO6
 1
1
EC50 = 4.9 nM
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CP0071490
(11beta,16beta)-9-Fluoro-11,21-dihydroxy-16-methyl-3,20-dioxopregna-1,4-dien-17-yl ethylcarbamate
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C25H34FNO6
 1
1
EC50 = 15.9 nM
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CP0340421
(8S,9R,10S,11S,13S,14S,16S,17R)-9-fluoro-11-hydroxy-17-(2-hydroxyacetyl)-10,13,16-trimethyl-3-oxo-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthren-17-yl pentylcarbamate
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C28H40FNO6
 1
1
EC50 = 18 nM
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CP0264395
(11beta,16beta)-9-Fluoro-11,21-dihydroxy-16-methyl-3,20-dioxopregna-1,4-dien-17-yl propylcarbamate
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C26H36FNO6
 1
1
EC50 = 18.7 nM
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CP0201809
(8S,9R,10S,11S,13S,14S,16S,17R)-9-fluoro-11-hydroxy-17-(2-hydroxyacetyl)-10,13,16-trimethyl-3-oxo-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthren-17-yl 3,3-dimethylbutylcarbamate
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C29H42FNO6
 1
1
EC50 = 21 nM
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CP0285810
(11beta,16beta)-9-Fluoro-11,21-dihydroxy-16-methyl-3,20-dioxopregna-1,4-dien-17-yl (1R)-1-phenylethylcarbamate
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C31H38FNO6
 1
1
EC50 = 21.5 nM
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CP0310369
(11beta,16beta)-9-Fluoro-11,21-dihydroxy-16-methyl-3,20-dioxopregna-1,4-dien-17-yl butylcarbamate
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C27H38FNO6
 1
1
EC50 = 22 nM
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CP0340420
(8S,9R,10S,11S,13S,14S,16S,17R)-9-fluoro-11-hydroxy-17-(2-hydroxyacetyl)-10,13,16-trimethyl-3-oxo-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthren-17-yl 2,4,4-trimethylpentan-2-ylcarbamate
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C31H46FNO6
 1
1
EC50 = 23.2 nM
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CP0285814
(11beta,16beta)-9-Fluoro-11,21-dihydroxy-16-methyl-3,20-dioxopregna-1,4-dien-17-yl allylcarbamate
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C26H34FNO6
 1
1
EC50 = 39 nM
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CP0310367
(8S,9R,10S,11S,13S,14S,16S,17R)-9-fluoro-11-hydroxy-17-(2-hydroxyacetyl)-10,13,16-trimethyl-3-oxo-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthren-17-yl tert-pentylcarbamate
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C28H40FNO6
 1
1
EC50 = 53.3 nM
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CP0269642
(11beta,16beta)-9-Fluoro-11,21-dihydroxy-16-methyl-3,20-dioxopregna-1,4-dien-17-yl (1S)-1-(methoxycarbonyl)-ethylcarbamate
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C27H36FNO8
 1
1
EC50 = 83 nM
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Biochemical Assays
Compound ID Compound Name Compound Formula
CP0228996
N-(2-hydroxyethyl)-4-[4-[(4-oxo-3,5,6,7-tetrahydrocyclopenta[d]pyrimidin-2-yl)sulfanylmethyl]phenyl]benzenesulfonamide
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C22H23N3O4S2
 1
1 IC50 = 4000 nM
CP0035755
N-hydroxy-4-(4-phenylsulfanylphenyl)sulfonyl-1-prop-2-ynylpiperidine-4-carboxamide
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C21H22N2O4S2
 2
1 IC50 = 8660 nM
2 IC50 > 5000 nM
CP0036560
4-{[4-(4-Chlorophenoxy)phenyl]sulfonyl}-N-hydroxy tetrahydro-2H-pyran-4-carboxamide
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C18H18ClNO6S
 1
1 Ki = 590 nM
CP0041534
N-hydroxy-1-(2-methoxyethyl)-4-[4-[4-(trifluoromethoxy)phenoxy]phenyl]sulfonylpiperidine-4-carboxamide
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C22H25F3N2O7S
 1
1 Ki > 10000 nM
Clinical Information about the Protein
Target 1 ( Matrix metalloproteinase-1 (MMP-1) )
Target Type Successful Target
Disease 8 Target-related Diseases  8
1 Lung cancer [ICD-11: 2C25.0]
2 Rheumatoid arthritis [ICD-11: FA20]
3 Pancreatic cancer [ICD-11: 2C10]
4 Corneal ulcer [ICD-11: 9A76]
5 Hepatitis C virus infection [ICD-11: 1E51.1]
6 Multiple sclerosis [ICD-11: 8A40]
7 Solid tumour/cancer [ICD-11: 2A00-2F9Z]
8 Arthritis [ICD-11: FA20]
Approved Drug(s) 1 Approved Drug  1
1 Prinomastat Approved
Lung cancer
Clinical Trial Drug(s) 3 Clinical Trial Drugs  3
1 CIPEMASTAT Phase 3
Rheumatoid arthritis
2 Apratastat Phase 2
Rheumatoid arthritis
3 Marimastat Phase 3
Pancreatic cancer
Discontinued Drug(s) 6 Discontinued Drugs  6
1 GM6001 Discontinued in Phase 2
Corneal ulcer
2 RS-130830 Discontinued in Phase 2
Hepatitis C virus infection
3 BB-1101 Terminated
Multiple sclerosis
4 BB-3644 Terminated
Solid tumour/cancer
5 Ro-31-4724 Terminated
Arthritis
6 RO-319790 Terminated
Rheumatoid arthritis