sc 78080 profile

ID Source	ID
PubMed CID	9892815
CHEMBL ID	1771212
SCHEMBL ID	5919470
MeSH ID	M0550616

ID Source

PubMed CID

9892815

CHEMBL ID

1771212

SCHEMBL ID

5919470

MeSH ID

M0550616

Synonyms (12)

Synonym
3kr ,
sd-2590
CHEMBL1771212 ,
bdbm50343077
n-hydroxy-1-(2-methoxyethyl)-4-(4-(4-(trifluoromethoxy)phenoxy)phenylsulfonyl)piperidine-4-carboxamide
SCHEMBL5919470
sc-78080
226396-25-4
NCGC00387451-01
n-hydroxy-1-(2-methoxyethyl)-4-[[4-[4-(trifluoro-methoxy)phenoxy]phenyl]sulfonyl]-4-piperidinecarboxamide
n-hydroxy-1-(2-methoxyethyl)-4-[[4-[4-(trifluoromethoxy)phenoxy]phenyl]sulfonyl]-4-piperidinecarboxamide
n-hydroxy-1-(2-methoxyethyl)-4-[4-[4-(trifluoromethoxy)phenoxy]phenyl]sulfonylpiperidine-4-carboxamide

Synonym

3kr ,

sd-2590

CHEMBL1771212 ,

bdbm50343077

n-hydroxy-1-(2-methoxyethyl)-4-(4-(4-(trifluoromethoxy)phenoxy)phenylsulfonyl)piperidine-4-carboxamide

SCHEMBL5919470

sc-78080

226396-25-4

NCGC00387451-01

n-hydroxy-1-(2-methoxyethyl)-4-[[4-[4-(trifluoro-methoxy)phenoxy]phenyl]sulfonyl]-4-piperidinecarboxamide

n-hydroxy-1-(2-methoxyethyl)-4-[[4-[4-(trifluoromethoxy)phenoxy]phenyl]sulfonyl]-4-piperidinecarboxamide

n-hydroxy-1-(2-methoxyethyl)-4-[4-[4-(trifluoromethoxy)phenoxy]phenyl]sulfonylpiperidine-4-carboxamide

Protein	Taxonomy	Measurement	Average (mM)	Bioassay(s)
Interstitial collagenase	Homo sapiens (human)	IC50	10.0000	AID604448
Interstitial collagenase	Homo sapiens (human)	Ki	10.0000	AID594798
72 kDa type IV collagenase	Homo sapiens (human)	IC50	0.0001	AID594799; AID604449
Stromelysin-1	Homo sapiens (human)	IC50	0.0288	AID594800; AID604450
Matrilysin	Homo sapiens (human)	IC50	7.0000	AID604451
Matrilysin	Homo sapiens (human)	Ki	7.0000	AID594801
Matrix metalloproteinase-9	Homo sapiens (human)	IC50	0.0002	AID594803; AID604453
Neutrophil collagenase	Homo sapiens (human)	IC50	0.0017	AID594802; AID604452
Collagenase 3	Homo sapiens (human)	IC50	0.0001	AID594804; AID604454
Matrix metalloproteinase-14	Homo sapiens (human)	IC50	0.0130	AID604455
Matrix metalloproteinase-14	Homo sapiens (human)	Ki	0.0140	AID594805

Protein

Taxonomy

Measurement

Average (mM)

Bioassay(s)

Interstitial collagenase

Homo sapiens (human)

IC50

10.0000

AID604448

Interstitial collagenase

Homo sapiens (human)

10.0000

AID594798

72 kDa type IV collagenase

Homo sapiens (human)

IC50

0.0001

AID594799; AID604449

Stromelysin-1

Homo sapiens (human)

IC50

0.0288

AID594800; AID604450

Matrilysin

Homo sapiens (human)

IC50

7.0000

AID604451

Matrilysin

Homo sapiens (human)

7.0000

AID594801

Matrix metalloproteinase-9

Homo sapiens (human)

IC50

0.0002

AID594803; AID604453

Neutrophil collagenase

Homo sapiens (human)

IC50

0.0017

AID594802; AID604452

Collagenase 3

Homo sapiens (human)

IC50

0.0001

AID594804; AID604454

Matrix metalloproteinase-14

Homo sapiens (human)

IC50

0.0130

AID604455

Matrix metalloproteinase-14

Homo sapiens (human)

0.0140

AID594805

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 ISSN: 2472-5560	Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347160	Primary screen NINDS Rhodamine 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 ISSN: 1091-6490	Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
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 ISSN: 1521-0111	A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346986	P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen	2019	Molecular pharmacology, 11, Volume: 96, Issue:5 ISSN: 1521-0111	A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347159	Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay	2020	Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 ISSN: 1091-6490	Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID594812	Bioavailability in rat	2011	Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10 ISSN: 1464-3405	MMP-13 selective α-sulfone hydroxamates: a survey of P1' heterocyclic amide isosteres.
AID604535	Cmax in male rat at 20 mg/kg, po after 24 hrs	2010	Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18 ISSN: 1520-4804	Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.
AID594804	Inhibition of human MMP-13	2011	Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10 ISSN: 1464-3405	MMP-13 selective α-sulfone hydroxamates: a survey of P1' heterocyclic amide isosteres.
AID604607	Antiangiogenic activity in cornea of mouse bFGF-induced corneal micropocket model assessed as inhibition of angiogenesis administered as BID	2010	Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18 ISSN: 1520-4804	Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.
AID594805	Inhibition of human MMP-14	2011	Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10 ISSN: 1464-3405	MMP-13 selective α-sulfone hydroxamates: a survey of P1' heterocyclic amide isosteres.
AID604449	Inhibition of human MMP2 assessed as cleavage of fluorogenic peptide MCAPro-Leu-Gly-Leu-Dpa-Ala-Arg-NH2 by fluorometric assay	2010	Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18 ISSN: 1520-4804	Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.
AID604455	Inhibition of human MMP14 assessed as cleavage of fluorogenic peptide MCAPro-Leu-Gly-Leu-Dpa-Ala-Arg-NH2 by fluorometric assay	2010	Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18 ISSN: 1520-4804	Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.
AID604529	Selectivity ratio of IC50 for human MMP1 to IC50 for human MMP9	2010	Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18 ISSN: 1520-4804	Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.
AID604623	Oral bioavailability in female dog at 20 mg/kg after 24 hrs	2010	Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18 ISSN: 1520-4804	Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.
AID604541	AUC (0 to infinity) in male dog at 20 mg/kg, po after 24 hrs	2010	Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18 ISSN: 1520-4804	Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.
AID604452	Inhibition of human MMP8 assessed as cleavage of fluorogenic peptide MCAPro-Leu-Gly-Leu-Dpa-Ala-Arg-NH2 by fluorometric assay	2010	Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18 ISSN: 1520-4804	Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.
AID604537	Cmax in male mouse at 20 mg/kg, po after 24 hrs	2010	Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18 ISSN: 1520-4804	Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.
AID604460	Cmax in rat at 20 mg/kg, po	2010	Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18 ISSN: 1520-4804	Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.
AID604463	Oral bioavailability in rat at 20 mg/kg	2010	Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18 ISSN: 1520-4804	Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.
AID604617	Cmax in female mouse at 20 mg/kg, po after 24 hrs	2010	Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18 ISSN: 1520-4804	Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.
AID604540	AUC (0 to infinity) in male rat at 20 mg/kg, po after 24 hrs	2010	Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18 ISSN: 1520-4804	Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.
AID604471	Cardioprotective activity in rat myocardial infarction model assessed inhibition of postinfection left ventricular dilation administered po qd for 4 weeks	2010	Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18 ISSN: 1520-4804	Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.
AID604534	Tmax in cynomolgus monkey at 20 mg/kg, po after 24 hrs	2010	Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18 ISSN: 1520-4804	Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.
AID604448	Inhibition of human MMP1 expressed in human HT-1080 cells assessed as cleavage of fluorogenic peptide MCAPro-Leu-Gly-Leu-Dpa-Ala-Arg-NH2 by fluorometric assay	2010	Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18 ISSN: 1520-4804	Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.
AID594803	Inhibition of human MMP-9	2011	Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10 ISSN: 1464-3405	MMP-13 selective α-sulfone hydroxamates: a survey of P1' heterocyclic amide isosteres.
AID594809	Cmax in rat	2011	Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10 ISSN: 1464-3405	MMP-13 selective α-sulfone hydroxamates: a survey of P1' heterocyclic amide isosteres.
AID594802	Inhibition of human MMP-8	2011	Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10 ISSN: 1464-3405	MMP-13 selective α-sulfone hydroxamates: a survey of P1' heterocyclic amide isosteres.
AID594800	Inhibition of human MMP-3	2011	Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10 ISSN: 1464-3405	MMP-13 selective α-sulfone hydroxamates: a survey of P1' heterocyclic amide isosteres.
AID604622	Oral bioavailability in female rat at 20 mg/kg after 24 hrs	2010	Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18 ISSN: 1520-4804	Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.
AID604451	Inhibition of human MMP7 assessed as cleavage of fluorogenic peptide MCAPro-Leu-Gly-Leu-Dpa-Ala-Arg-NH2 by fluorometric assay	2010	Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18 ISSN: 1520-4804	Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.
AID594799	Inhibition of human MMP-2	2011	Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10 ISSN: 1464-3405	MMP-13 selective α-sulfone hydroxamates: a survey of P1' heterocyclic amide isosteres.
AID604542	AUC (0 to infinity) in cynomolgus monkey at 20 mg/kg, po after 24 hrs	2010	Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18 ISSN: 1520-4804	Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.
AID604538	Cmax in cynomolgus monkey at 20 mg/kg, po after 24 hrs	2010	Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18 ISSN: 1520-4804	Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.
AID604533	Tmax in male dog at 20 mg/kg, po after 24 hrs	2010	Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18 ISSN: 1520-4804	Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.
AID604543	Oral bioavailability in male mouse at 20 mg/kg after 24 hrs	2010	Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18 ISSN: 1520-4804	Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.
AID604530	Antiangiogenic activity in cornea of mouse bFGF-induced corneal micropocket model assessed as inhibition of angiogenesis at 5 mg/kg administered as BID	2010	Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18 ISSN: 1520-4804	Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.
AID604618	AUC (0 to infinity) in female mouse at 20 mg/kg, po after 24 hrs	2010	Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18 ISSN: 1520-4804	Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.
AID604462	Half life in rat at 20 mg/kg, po	2010	Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18 ISSN: 1520-4804	Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.
AID604461	Plasma concentration in rat at 20 mg/kg, po	2010	Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18 ISSN: 1520-4804	Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.
AID604454	Inhibition of human MMP13 assessed as cleavage of fluorogenic peptide MCAPro-Leu-Gly-Leu-Dpa-Ala-Arg-NH2 by fluorometric assay	2010	Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18 ISSN: 1520-4804	Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.
AID594801	Inhibition of human MMP-7	2011	Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10 ISSN: 1464-3405	MMP-13 selective α-sulfone hydroxamates: a survey of P1' heterocyclic amide isosteres.
AID604614	Tmax in female dog at 20 mg/kg, po after 24 hrs	2010	Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18 ISSN: 1520-4804	Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.
AID594798	Inhibition of human MMP-1	2011	Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10 ISSN: 1464-3405	MMP-13 selective α-sulfone hydroxamates: a survey of P1' heterocyclic amide isosteres.
AID604539	AUC (0 to infinity) in male mouse at 20 mg/kg, po after 24 hrs	2010	Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18 ISSN: 1520-4804	Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.
AID604606	Oral bioavailability in cynomolgus monkey at 20 mg/kg after 24 hrs	2010	Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18 ISSN: 1520-4804	Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.
AID604450	Inhibition of human MMP3 assessed as cleavage of fluorogenic peptide MCAPro-Leu-Gly-Leu-Dpa-Ala-Arg-NH2 by fluorometric assay	2010	Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18 ISSN: 1520-4804	Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.
AID604531	Tmax in male mouse at 20 mg/kg, po after 24 hrs	2010	Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18 ISSN: 1520-4804	Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.
AID604616	Cmax in female dog at 20 mg/kg, po after 24 hrs	2010	Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18 ISSN: 1520-4804	Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.
AID604464	Antitumor activity against human PC3 cells xenografted in po dosed BALB/c nu/nu mouse assessed as tumor growth inhibition administered BID measured on 25 to 30 days	2010	Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18 ISSN: 1520-4804	Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.
AID604604	Oral bioavailability in male rat at 20 mg/kg after 24 hrs	2010	Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18 ISSN: 1520-4804	Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.
AID604615	Cmax in female rat at 20 mg/kg, po after 24 hrs	2010	Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18 ISSN: 1520-4804	Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.
AID604620	AUC (0 to infinity) in female dog at 20 mg/kg, po after 24 hrs	2010	Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18 ISSN: 1520-4804	Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.
AID604528	Selectivity ratio of IC50 for human MMP1 to IC50 for human MMP2	2010	Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18 ISSN: 1520-4804	Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.
AID604532	Tmax in male rat at 20 mg/kg, po after 24 hrs	2010	Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18 ISSN: 1520-4804	Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.
AID604619	AUC (0 to infinity) in female rat at 20 mg/kg, po after 24 hrs	2010	Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18 ISSN: 1520-4804	Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.
AID604621	Oral bioavailability in female mouse at 20 mg/kg after 24 hrs	2010	Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18 ISSN: 1520-4804	Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.
AID604612	Tmax in female mouse at 20 mg/kg, po after 24 hrs	2010	Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18 ISSN: 1520-4804	Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.
AID604526	Cardioprotective activity in rat myocardial infarction model assessed inhibition of left ventricular dilation at 10 mg/kg, po qd for 4 weeks (Rvb = 0.59 +/- 0.02 mL)	2010	Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18 ISSN: 1520-4804	Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.
AID604453	Inhibition of human MMP9 assessed as cleavage of fluorogenic peptide MCAPro-Leu-Gly-Leu-Dpa-Ala-Arg-NH2 by fluorometric assay	2010	Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18 ISSN: 1520-4804	Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.
AID604527	Selectivity ratio of IC50 for human MMP13 to IC50 for human MMP1	2010	Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18 ISSN: 1520-4804	Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.
AID594808	Half life in rat	2011	Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10 ISSN: 1464-3405	MMP-13 selective α-sulfone hydroxamates: a survey of P1' heterocyclic amide isosteres.
AID604605	Oral bioavailability in male dog at 20 mg/kg after 24 hrs	2010	Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18 ISSN: 1520-4804	Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.
AID604536	Cmax in male dog at 20 mg/kg, po after 24 hrs	2010	Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18 ISSN: 1520-4804	Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.
AID604613	Tmax in female rat at 20 mg/kg, po after 24 hrs	2010	Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18 ISSN: 1520-4804	Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.

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
ISSN: 2472-5560

Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.

AID1347160

Primary screen NINDS Rhodamine 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
ISSN: 1091-6490

Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.

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
ISSN: 1521-0111

A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.

AID1346986

P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen

2019

Molecular pharmacology, 11, Volume: 96, Issue:5
ISSN: 1521-0111

A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.

AID1347159

Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay

2020

Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
ISSN: 1091-6490

Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.

AID594812

Bioavailability in rat

2011

Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10
ISSN: 1464-3405

MMP-13 selective α-sulfone hydroxamates: a survey of P1' heterocyclic amide isosteres.

AID604535

Cmax in male rat at 20 mg/kg, po after 24 hrs

2010

Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
ISSN: 1520-4804

Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.

AID594804

Inhibition of human MMP-13

2011

Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10
ISSN: 1464-3405

MMP-13 selective α-sulfone hydroxamates: a survey of P1' heterocyclic amide isosteres.

AID604607

Antiangiogenic activity in cornea of mouse bFGF-induced corneal micropocket model assessed as inhibition of angiogenesis administered as BID

2010

Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
ISSN: 1520-4804

Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.

AID594805

Inhibition of human MMP-14

2011

Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10
ISSN: 1464-3405

MMP-13 selective α-sulfone hydroxamates: a survey of P1' heterocyclic amide isosteres.

AID604449

Inhibition of human MMP2 assessed as cleavage of fluorogenic peptide MCAPro-Leu-Gly-Leu-Dpa-Ala-Arg-NH2 by fluorometric assay

2010

Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
ISSN: 1520-4804

Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.

AID604455

Inhibition of human MMP14 assessed as cleavage of fluorogenic peptide MCAPro-Leu-Gly-Leu-Dpa-Ala-Arg-NH2 by fluorometric assay

2010

Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
ISSN: 1520-4804

Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.

AID604529

Selectivity ratio of IC50 for human MMP1 to IC50 for human MMP9

2010

Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
ISSN: 1520-4804

Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.

AID604623

Oral bioavailability in female dog at 20 mg/kg after 24 hrs

2010

Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
ISSN: 1520-4804

Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.

AID604541

AUC (0 to infinity) in male dog at 20 mg/kg, po after 24 hrs

2010

Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
ISSN: 1520-4804

Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.

AID604452

Inhibition of human MMP8 assessed as cleavage of fluorogenic peptide MCAPro-Leu-Gly-Leu-Dpa-Ala-Arg-NH2 by fluorometric assay

2010

Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
ISSN: 1520-4804

Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.

AID604537

Cmax in male mouse at 20 mg/kg, po after 24 hrs

2010

Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
ISSN: 1520-4804

Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.

AID604460

Cmax in rat at 20 mg/kg, po

2010

Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
ISSN: 1520-4804

Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.

AID604463

Oral bioavailability in rat at 20 mg/kg

2010

Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
ISSN: 1520-4804

Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.

AID604617

Cmax in female mouse at 20 mg/kg, po after 24 hrs

2010

Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
ISSN: 1520-4804

Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.

AID604540

AUC (0 to infinity) in male rat at 20 mg/kg, po after 24 hrs

2010

Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
ISSN: 1520-4804

Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.

AID604471

Cardioprotective activity in rat myocardial infarction model assessed inhibition of postinfection left ventricular dilation administered po qd for 4 weeks

2010

Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
ISSN: 1520-4804

Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.

AID604534

Tmax in cynomolgus monkey at 20 mg/kg, po after 24 hrs

2010

Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
ISSN: 1520-4804

Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.

AID604448

Inhibition of human MMP1 expressed in human HT-1080 cells assessed as cleavage of fluorogenic peptide MCAPro-Leu-Gly-Leu-Dpa-Ala-Arg-NH2 by fluorometric assay

2010

Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
ISSN: 1520-4804

Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.

AID594803

Inhibition of human MMP-9

2011

Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10
ISSN: 1464-3405

MMP-13 selective α-sulfone hydroxamates: a survey of P1' heterocyclic amide isosteres.

AID594809

Cmax in rat

2011

Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10
ISSN: 1464-3405

MMP-13 selective α-sulfone hydroxamates: a survey of P1' heterocyclic amide isosteres.

AID594802

Inhibition of human MMP-8

2011

Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10
ISSN: 1464-3405

MMP-13 selective α-sulfone hydroxamates: a survey of P1' heterocyclic amide isosteres.

AID594800

Inhibition of human MMP-3

2011

Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10
ISSN: 1464-3405

MMP-13 selective α-sulfone hydroxamates: a survey of P1' heterocyclic amide isosteres.

AID604622

Oral bioavailability in female rat at 20 mg/kg after 24 hrs

2010

Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
ISSN: 1520-4804

Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.

AID604451

Inhibition of human MMP7 assessed as cleavage of fluorogenic peptide MCAPro-Leu-Gly-Leu-Dpa-Ala-Arg-NH2 by fluorometric assay

2010

Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
ISSN: 1520-4804

Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.

AID594799

Inhibition of human MMP-2

2011

Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10
ISSN: 1464-3405

MMP-13 selective α-sulfone hydroxamates: a survey of P1' heterocyclic amide isosteres.

AID604542

AUC (0 to infinity) in cynomolgus monkey at 20 mg/kg, po after 24 hrs

2010

Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
ISSN: 1520-4804

Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.

AID604538

Cmax in cynomolgus monkey at 20 mg/kg, po after 24 hrs

2010

Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
ISSN: 1520-4804

Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.

AID604533

Tmax in male dog at 20 mg/kg, po after 24 hrs

2010

Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
ISSN: 1520-4804

Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.

AID604543

Oral bioavailability in male mouse at 20 mg/kg after 24 hrs

2010

Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
ISSN: 1520-4804

Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.

AID604530

Antiangiogenic activity in cornea of mouse bFGF-induced corneal micropocket model assessed as inhibition of angiogenesis at 5 mg/kg administered as BID

2010

Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
ISSN: 1520-4804

Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.

AID604618

AUC (0 to infinity) in female mouse at 20 mg/kg, po after 24 hrs

2010

Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
ISSN: 1520-4804

Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.

AID604462

Half life in rat at 20 mg/kg, po

2010

Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
ISSN: 1520-4804

Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.

AID604461

Plasma concentration in rat at 20 mg/kg, po

2010

Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
ISSN: 1520-4804

Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.

AID604454

Inhibition of human MMP13 assessed as cleavage of fluorogenic peptide MCAPro-Leu-Gly-Leu-Dpa-Ala-Arg-NH2 by fluorometric assay

2010

Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
ISSN: 1520-4804

Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.

AID594801

Inhibition of human MMP-7

2011

Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10
ISSN: 1464-3405

MMP-13 selective α-sulfone hydroxamates: a survey of P1' heterocyclic amide isosteres.

AID604614

Tmax in female dog at 20 mg/kg, po after 24 hrs

2010

Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
ISSN: 1520-4804

Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.

AID594798

Inhibition of human MMP-1

2011

Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10
ISSN: 1464-3405

MMP-13 selective α-sulfone hydroxamates: a survey of P1' heterocyclic amide isosteres.

AID604539

AUC (0 to infinity) in male mouse at 20 mg/kg, po after 24 hrs

2010

Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
ISSN: 1520-4804

Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.

AID604606

Oral bioavailability in cynomolgus monkey at 20 mg/kg after 24 hrs

2010

Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
ISSN: 1520-4804

Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.

AID604450

Inhibition of human MMP3 assessed as cleavage of fluorogenic peptide MCAPro-Leu-Gly-Leu-Dpa-Ala-Arg-NH2 by fluorometric assay

2010

Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
ISSN: 1520-4804

Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.

AID604531

Tmax in male mouse at 20 mg/kg, po after 24 hrs

2010

Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
ISSN: 1520-4804

Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.

AID604616

Cmax in female dog at 20 mg/kg, po after 24 hrs

2010

Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
ISSN: 1520-4804

Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.

AID604464

Antitumor activity against human PC3 cells xenografted in po dosed BALB/c nu/nu mouse assessed as tumor growth inhibition administered BID measured on 25 to 30 days

2010

Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
ISSN: 1520-4804

Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.

AID604604

Oral bioavailability in male rat at 20 mg/kg after 24 hrs

2010

Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
ISSN: 1520-4804

Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.

AID604615

Cmax in female rat at 20 mg/kg, po after 24 hrs

2010

Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
ISSN: 1520-4804

Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.

AID604620

AUC (0 to infinity) in female dog at 20 mg/kg, po after 24 hrs

2010

Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
ISSN: 1520-4804

Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.

AID604528

Selectivity ratio of IC50 for human MMP1 to IC50 for human MMP2

2010

Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
ISSN: 1520-4804

Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.

AID604532

Tmax in male rat at 20 mg/kg, po after 24 hrs

2010

Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
ISSN: 1520-4804

Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.

AID604619

AUC (0 to infinity) in female rat at 20 mg/kg, po after 24 hrs

2010

Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
ISSN: 1520-4804

Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.

AID604621

Oral bioavailability in female mouse at 20 mg/kg after 24 hrs

2010

Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
ISSN: 1520-4804

Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.

AID604612

Tmax in female mouse at 20 mg/kg, po after 24 hrs

2010

Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
ISSN: 1520-4804

Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.

AID604526

Cardioprotective activity in rat myocardial infarction model assessed inhibition of left ventricular dilation at 10 mg/kg, po qd for 4 weeks (Rvb = 0.59 +/- 0.02 mL)

2010

Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
ISSN: 1520-4804

Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.

AID604453

Inhibition of human MMP9 assessed as cleavage of fluorogenic peptide MCAPro-Leu-Gly-Leu-Dpa-Ala-Arg-NH2 by fluorometric assay

2010

Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
ISSN: 1520-4804

Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.

AID604527

Selectivity ratio of IC50 for human MMP13 to IC50 for human MMP1

2010

Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
ISSN: 1520-4804

Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.

AID594808

Half life in rat

2011

Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10
ISSN: 1464-3405

MMP-13 selective α-sulfone hydroxamates: a survey of P1' heterocyclic amide isosteres.

AID604605

Oral bioavailability in male dog at 20 mg/kg after 24 hrs

2010

Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
ISSN: 1520-4804

Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.

AID604536

Cmax in male dog at 20 mg/kg, po after 24 hrs

2010

Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
ISSN: 1520-4804

Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.

AID604613

Tmax in female rat at 20 mg/kg, po after 24 hrs

2010

Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
ISSN: 1520-4804

Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	0 (0.00)	18.2507
2000's	0 (0.00)	29.6817
2010's	3 (60.00)	24.3611
2020's	2 (40.00)	2.80

Timeframe

Studies, This Drug (%)

All Drugs %

pre-1990

0 (0.00)

18.7374

1990's

0 (0.00)

18.2507

2000's

0 (0.00)

29.6817

2010's

3 (60.00)

24.3611

2020's

2 (40.00)

2.80

Publication Type	This drug (%)	All Drugs (%)
Trials	0 (0.00%)	5.53%
Reviews	0 (0.00%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	5 (100.00%)	84.16%

Publication Type

This drug (%)

All Drugs (%)

Trials

0 (0.00%)

5.53%

Reviews

0 (0.00%)

6.00%

Case Studies

0 (0.00%)

4.05%

Observational

0 (0.00%)

0.25%

Other

5 (100.00%)

84.16%

Related Drugs (1)

Substance	Studies	Classes	Roles	First Year	Last Year	Average Age	Relationship Strength	Trials	pre-1990	1990's	2000's	2010's	post-2020
rs-130830	1			2010	2010	14.0	high	0	0	0	1	0	0

Substance

Studies

Classes

Roles

First Year

Last Year

Average Age

Relationship Strength

Trials

pre-1990

1990's

2000's

2010's

post-2020

rs-130830

2010

14.0

high

Condition	Studies	First Year	Last Year	Average Age	Relationship Strength	2000's	2010's
Congenital Zika Syndrome	1	2020	2020	4.0	medium	0	1
Disease Models, Animal	1	2020	2020	4.0	medium	0	1
Hypertrophy, Left Ventricular	1	2010	2010	14.0	medium	1	0
Left Ventricular Hypertrophy	1	2010	2010	14.0	medium	1	0
Zika Virus Infection	1	2020	2020	4.0	medium	0	1

Condition

Indicated

Studies

First Year

Last Year

Average Age

Relationship Strength

Trials

pre-1990

1990's

2000's

2010's

post-2020

Congenital Zika Syndrome

2020

4.0

medium

Disease Models, Animal

2020

4.0

medium

Hypertrophy, Left Ventricular

2010

14.0

medium

Left Ventricular Hypertrophy

2010

14.0

medium

Zika Virus Infection

2020

4.0

medium

Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
Proceedings of the National Academy of Sciences of the United States of America, , 12-08, Volume: 117, Issue:49, 2020

Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.
Journal of medicinal chemistry, , Sep-23, Volume: 53, Issue:18, 2010

Bioavailability (1)

Article	Year
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Molecular pharmacology, , Volume: 96, Issue:5	2019

Article

Year

A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Molecular pharmacology, , Volume: 96, Issue:5

2019

sc 78080

Description

Cross-References

Synonyms (12)

Protein Targets (8)

Inhibition Measurements

Bioassays (64)

Research

Studies (5)

Study Types

Bioavailability (1)

sc 78080

Description

Cross-References

Synonyms (12)

Protein Targets (8)

Inhibition Measurements

Bioassays (64)

Research

Studies (5)

Study Types

Related Drugs (1)

Drugs Involved in Assays Together (1)

Related Conditions (5)

Bioavailability (1)