Compounds > cep-28122
Page last updated: 2024-08-03 20:39:36

cep-28122

Description

CEP-28122: inhibits anaplastic lymphoma kinase; structure in first source [MeSH]

Cross-References

ID SourceID
PubMed CID57325421
CHEMBL ID2064666
SCHEMBL ID2061951
MeSH IDM0575076

Synonyms (26)

Synonym
bdbm50389154
CHEMBL2064666 ,
gtpl8139
compound 25b [pmid: 22564207]
(1s,2s,3r,4r)-3-[(5-chloro-2-{[(7s)-1-methoxy-7-(4-morpholinyl)-6,7,8,9-tetrahydro-5h-benzo[7]annulen-2-yl]amino}-4-pyrimidinyl)amino]bicyclo[2.2.1]hept-5-ene-2-carboxamide
LAJAFFLJAJMYLK-CVOKMOJFSA-N
(1s,2s,3r,4r)-3-[5-chloro-2-((s)-1-methoxy-7-morpholin-4-yl-6,7,8,9-tetrahydro-5h-benzocyclohepten-2-ylamino)-pyrimidin-4-ylamino]-bicyclo[2.2.1]hept-5-ene-2-carboxylic acid amide
CS-5176
HY-18030
SCHEMBL2061951
cep-28122
1022958-60-6
cep28122
cep 28122
(1s,2s,3r,4r)-3-[(5-chloro-2-{[(7s)-1-methoxy-7-(morpholin-4-yl)-6,7,8,9-tetrahydro-5h-benzo[7]annulen-2-yl]amino}pyrimidin-4-yl)amino]bicyclo[2.2.1]hept-5-ene-2-carboxamide
NCGC00387821-03
(1s,2s,3r,4r)-3-((5-chloro-2-(((s)-1-methoxy-7-morpholino-6,7,8,9-tetrahydro-5h-benzo[7]annulen-2-yl)amino)pyrimidin-4-yl)amino)bicyclo[2.2.1]hept-5-ene-2-carboxamide.
EX-A1541
Q27076467
(1s,2s,4r)-3-((5-chloro-2-(((s)-1-methoxy-7-morpholino-6,7,8,9-tetrahydro-5h-benzo[7]annulen-2-yl)amino)pyrimidin-4-yl)amino)bicyclo[2.2.1]hept-5-ene-2-carboxamide
(1s,2s,3r,4r)-3-[[5-chloro-2-[[(7s)-4-methoxy-7-morpholin-4-yl-6,7,8,9-tetrahydro-5h-benzo[7]annulen-3-yl]amino]pyrimidin-4-yl]amino]bicyclo[2.2.1]hept-5-ene-2-carboxamide
bicyclo[2.2.1]hept-5-ene-2-carboxamide, 3-[[5-chloro-2-[[(7r)-6,7,8,9-tetrahydro-1-methoxy-7-(4-morpholinyl)-5h-benzocyclohepten-2-yl]amino]-4-pyrimidinyl]amino]-, (1r,2r,3s,4s)-rel-
DTXSID501098750
1431697-87-8
AC-36009
AKOS040747418

Protein Targets (29)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency1.0684AID1645841
GVesicular stomatitis virusPotency6.0081AID1645842
cytochrome P450 2D6Homo sapiens (human)Potency18.9991AID1645840
Interferon betaHomo sapiens (human)Potency6.0081AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency6.0081AID1645842
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency6.0081AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency6.0081AID1645842

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)
NUAK family SNF1-like kinase 1Homo sapiens (human)IC500.0260AID676085
Serine/threonine-protein kinase Chk2Homo sapiens (human)IC500.0290AID676087
Insulin receptorHomo sapiens (human)IC505.3310AID1319065; AID1319085
Tyrosine-protein kinase Fes/FpsHomo sapiens (human)IC500.0990AID676090
Cytochrome P450 3A4Homo sapiens (human)IC500.0019AID1319064
Cytochrome P450 2C9 Homo sapiens (human)IC500.0019AID1319064
Tyrosine-protein kinase FerHomo sapiens (human)IC500.0850AID676089
Cytochrome P450 2C19Homo sapiens (human)IC5010.0000AID1319070
Prostaglandin G/H synthase 2Homo sapiens (human)IC500.0019AID676080
Vascular endothelial growth factor receptor 3Homo sapiens (human)IC500.0480AID676092
Receptor-type tyrosine-protein kinase FLT3Homo sapiens (human)IC500.0880AID676091
Mitogen-activated protein kinase 8Homo sapiens (human)IC500.1120AID676094
Ribosomal protein S6 kinase alpha-3Homo sapiens (human)IC500.0130AID676096
Focal adhesion kinase 1Homo sapiens (human)IC500.3673AID1319069; AID1319086; AID676088
Activated CDC42 kinase 1Homo sapiens (human)IC500.0410AID676084
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC5010.0000AID1319070
Mitogen-activated protein kinase kinase kinase kinase 2Homo sapiens (human)IC500.0600AID676093
Protein-tyrosine kinase 6Homo sapiens (human)IC500.0730AID676086
Ribosomal protein S6 kinase alpha-2Homo sapiens (human)IC500.0070AID676097
Ribosomal protein S6 kinase alpha-1Homo sapiens (human)IC500.0610AID676095
Ribosomal protein S6 kinase alpha-6Homo sapiens (human)IC500.0190AID676098
ALK tyrosine kinase receptorHomo sapiens (human)IC500.0079AID1319064; AID1319068; AID676080

Bioassays (168)

Assay IDTitleYearJournalArticle
AID676313Volume of distribution in SCID mouse at 1 mg/kg, iv2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID1319056Drug metabolism in rat liver microsomes assessed as oxidative/degradative M6 metabolite formation at 10 uM after 120 mins in presence of NADPH by LC/MS/MS analysis2016Journal of medicinal chemistry, 08-25, Volume: 59, Issue:16
ISSN: 1520-4804		Discovery of Clinical Candidate CEP-37440, a Selective Inhibitor of Focal Adhesion Kinase (FAK) and Anaplastic Lymphoma Kinase (ALK).
AID676589Selectivity ratio of IC50 for human GCK to IC50 for human ALK cytoplasmic domain2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID676352Tmax in cynomolgus monkey at 10 mg/kg, po2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID676096Inhibition of human Rsk22012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID1319058Drug metabolism in human liver microsomes assessed as oxidative/degradative M1 metabolite formation at 10 uM after 120 mins in presence of NADPH by LC/MS/MS analysis2016Journal of medicinal chemistry, 08-25, Volume: 59, Issue:16
ISSN: 1520-4804		Discovery of Clinical Candidate CEP-37440, a Selective Inhibitor of Focal Adhesion Kinase (FAK) and Anaplastic Lymphoma Kinase (ALK).
AID676590Selectivity ratio of IC50 for human JNK1alpha1 to IC50 for human ALK cytoplasmic domain2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID676348Half life in Beagle dog at 10 mg/kg, po2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID676347Tmax in Beagle dog at 10 mg/kg, po2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID676365Plasma concentration in SCID mouse xenografted with human KARPAS299 cells expressing NPM-ALK at 30 mg/kg, po after 2 hrs by LC-MS/MS analysis2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID676369Toxicity in SCID mouse xenografted with human KARPAS299 cells expressing NPM-ALK assessed as effect on body weight at 10 to 30 mg/kg, po bid2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID676323Half life in Beagle dog at 1 mg/kg, iv2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID1319085Inhibition of INSR (unknown origin) by cell based assay2016Journal of medicinal chemistry, 08-25, Volume: 59, Issue:16
ISSN: 1520-4804		Discovery of Clinical Candidate CEP-37440, a Selective Inhibitor of Focal Adhesion Kinase (FAK) and Anaplastic Lymphoma Kinase (ALK).
AID676593Plasma concentration in SCID mouse xenografted with human KARPAS299 cells expressing NPM-ALK at 30 mg/kg, po after 6 hrs by LC-MS/MS analysis2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID676090Inhibition of human Fes2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID676381Selectivity ratio of IC50 for human FAK to IC50 for human ALK cytoplasmic domain2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID676094Inhibition of human JNK1alpha12012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID676374Antitumor activity against human NB1643 cells expressing ALK mutant F1174L assessed as growth inhibition administered as po bid2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID1319131Dose normalized AUC in cynomolgus monkey at 10 mg/kg, po by LC/MS/MS analysis2016Journal of medicinal chemistry, 08-25, Volume: 59, Issue:16
ISSN: 1520-4804		Discovery of Clinical Candidate CEP-37440, a Selective Inhibitor of Focal Adhesion Kinase (FAK) and Anaplastic Lymphoma Kinase (ALK).
AID676316Plasma clearance in CD-1 mouse at 1 mg/kg, iv2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID1319070Inhibition of human ERG2016Journal of medicinal chemistry, 08-25, Volume: 59, Issue:16
ISSN: 1520-4804		Discovery of Clinical Candidate CEP-37440, a Selective Inhibitor of Focal Adhesion Kinase (FAK) and Anaplastic Lymphoma Kinase (ALK).
AID1319079Selectivity ratio of IC50 for human FAK expressed in baculovirus to IC50 for human ALK expressed in baculovirus2016Journal of medicinal chemistry, 08-25, Volume: 59, Issue:16
ISSN: 1520-4804		Discovery of Clinical Candidate CEP-37440, a Selective Inhibitor of Focal Adhesion Kinase (FAK) and Anaplastic Lymphoma Kinase (ALK).
AID676312Plasma clearance in SCID mouse at 1 mg/kg, iv2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID676087Inhibition of human CHK22012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID676370Plasma concentration in SCID/beige mouse xenografted with human KARPAS299 cells expressing NPM-ALK at 10 mg/kg, po bid after 2 hrs post last dose by LC-MS/MS analysis2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID1319078AUC (0 to infinity) in Sprague-Dawley rat at 5 mg/kg, po by LC/MS/MS analysis2016Journal of medicinal chemistry, 08-25, Volume: 59, Issue:16
ISSN: 1520-4804		Discovery of Clinical Candidate CEP-37440, a Selective Inhibitor of Focal Adhesion Kinase (FAK) and Anaplastic Lymphoma Kinase (ALK).
AID676598Drug level in SCID mouse tumor xenografted with human KARPAS299 cells expressing NPM-ALK at 30 mg/kg, po after 24 hrs by LC-MS/MS analysis2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID676328Plasma clearance in cynomolgus monkey at 1 mg/kg, iv2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID1319057Drug metabolism in rat liver microsomes assessed as (1S,5R,6S,7R)-7-[5-Chloro-2-((S)-1-methoxy-7-morpholin-4-yl-6,7,8,9-tetrahydro-5H-benzocyclohepten-2-ylamino)-pyrimidin-4-ylamino]-3-oxa-tricyclo[3.2.1.0(2,4)]octane-6-carboxylic acid amide formation at 2016Journal of medicinal chemistry, 08-25, Volume: 59, Issue:16
ISSN: 1520-4804		Discovery of Clinical Candidate CEP-37440, a Selective Inhibitor of Focal Adhesion Kinase (FAK) and Anaplastic Lymphoma Kinase (ALK).
AID676335Oral bioavailability in SCID mouse at 10 mg/kg2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID676594Plasma concentration in SCID mouse xenografted with human KARPAS299 cells expressing NPM-ALK at 30 mg/kg, po after 12 hrs by LC-MS/MS analysis2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID676098Inhibition of human Rsk42012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID676364Inhibition of NPM-ALK phosphorylation in human KARPAS299 cells xenografted in SCID mouse tumor at 30 mg/kg, po qd after 12 hrs by immunoblotting2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID676330AUC in cynomolgus monkey at 1 mg/kg, iv2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID676341Cmax in Sprague-Dawley rat at 10 mg/kg, po2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID1319072Inhibition of CYP2C9 in human liver microsomes using diclofenac as substrate in presence of NADPH by LC/MS/MS analysis2016Journal of medicinal chemistry, 08-25, Volume: 59, Issue:16
ISSN: 1520-4804		Discovery of Clinical Candidate CEP-37440, a Selective Inhibitor of Focal Adhesion Kinase (FAK) and Anaplastic Lymphoma Kinase (ALK).
AID676344AUC in Sprague-Dawley rat at 10 mg/kg, po2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID676351Cmax in cynomolgus monkey at 10 mg/kg, po2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID1319054Drug metabolism in rat liver microsomes assessed as oxidative/degradative M1 metabolite formation at 10 uM after 120 mins in presence of NADPH by LC/MS/MS analysis2016Journal of medicinal chemistry, 08-25, Volume: 59, Issue:16
ISSN: 1520-4804		Discovery of Clinical Candidate CEP-37440, a Selective Inhibitor of Focal Adhesion Kinase (FAK) and Anaplastic Lymphoma Kinase (ALK).
AID676319Half life in Sprague-Dawley rat at 1 mg/kg, iv2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID676367Antitumor activity against human KARPAS299 cells expressing NPM-ALK xenografted in SCID mouse assessed as tumor regression administered as po bid for 12 days2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID676592Ratio of AUC (0 to 12 h) at 10 mg/kg, po to AUC (0 to 12 h) at 100 mg/kg, po in rat2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID1319066Half life in rat liver microsomes by LC/MS/MS analysis2016Journal of medicinal chemistry, 08-25, Volume: 59, Issue:16
ISSN: 1520-4804		Discovery of Clinical Candidate CEP-37440, a Selective Inhibitor of Focal Adhesion Kinase (FAK) and Anaplastic Lymphoma Kinase (ALK).
AID676089Inhibition of human Fer2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID676092Inhibition of human Flt42012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID676100Inhibition of human ARK5 at 1 uM2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID1319048Drug metabolism in rat liver microsomes assessed as oxidative/degradative M5 metabolite formation at 10 uM after 120 mins in presence of NADPH by LC/MS/MS analysis2016Journal of medicinal chemistry, 08-25, Volume: 59, Issue:16
ISSN: 1520-4804		Discovery of Clinical Candidate CEP-37440, a Selective Inhibitor of Focal Adhesion Kinase (FAK) and Anaplastic Lymphoma Kinase (ALK).
AID676360AUC (0 to 12 hrs) in rat 10 mg/kg, po2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID676322AUC in Sprague-Dawley rat at 1 mg/kg, iv2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID1319069Inhibition of human FAK expressed in baculovirus after 30 mins using biotinyl-amino-hexanoyl-EQEDEPEGDYFEWLE-amide as substrate by TRF assay2016Journal of medicinal chemistry, 08-25, Volume: 59, Issue:16
ISSN: 1520-4804		Discovery of Clinical Candidate CEP-37440, a Selective Inhibitor of Focal Adhesion Kinase (FAK) and Anaplastic Lymphoma Kinase (ALK).
AID676384Selectivity ratio of IC50 for human Flt3 to IC50 for human ALK cytoplasmic domain2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID676307Inhibition of human Rsk1 at 1 uM2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID676597Drug level in SCID mouse tumor xenografted with human KARPAS299 cells expressing NPM-ALK at 30 mg/kg, po after 12 hrs by LC-MS/MS analysis2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID676345Oral bioavailability in Sprague-Dawley rat at 10 mg/kg2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID1319067Half life in human liver microsomes by LC/MS/MS analysis2016Journal of medicinal chemistry, 08-25, Volume: 59, Issue:16
ISSN: 1520-4804		Discovery of Clinical Candidate CEP-37440, a Selective Inhibitor of Focal Adhesion Kinase (FAK) and Anaplastic Lymphoma Kinase (ALK).
AID1319074Inhibition of CYP2D6 in human liver microsomes using dextromethorphan as substrate in presence of NADPH by LC/MS/MS analysis2016Journal of medicinal chemistry, 08-25, Volume: 59, Issue:16
ISSN: 1520-4804		Discovery of Clinical Candidate CEP-37440, a Selective Inhibitor of Focal Adhesion Kinase (FAK) and Anaplastic Lymphoma Kinase (ALK).
AID676321Volume of distribution in Sprague-Dawley rat at 1 mg/kg, iv2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID676107Inhibition of human Flt4 at 1 uM2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID676375Antitumor activity against human SH-SY5Y cells expressing ALK mutant R1275Q assessed as growth inhibition administered as po bid2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID676596Drug level in SCID mouse tumor xenografted with human KARPAS299 cells expressing NPM-ALK at 30 mg/kg, po after 6 hrs by LC-MS/MS analysis2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID676333Half life in SCID mouse at 10 mg/kg, po2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID1319050Clearance in CD-1 mouse at 1 mg/kg, iv by LC/MS/MS analysis2016Journal of medicinal chemistry, 08-25, Volume: 59, Issue:16
ISSN: 1520-4804		Discovery of Clinical Candidate CEP-37440, a Selective Inhibitor of Focal Adhesion Kinase (FAK) and Anaplastic Lymphoma Kinase (ALK).
AID676331Cmax in SCID mouse at 10 mg/kg, po2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID676097Inhibition of human Rsk32012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID676095Inhibition of human Rsk12012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID676314AUC in SCID mouse at 1 mg/kg, iv2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID676101Inhibition of human BRK at 1 uM2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID676081Inhibition of ALK tyrosine phosphorylation in human Karpas-299 cells after 2 hrs in presence of mouse plasma2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID676325Volume of distribution in Beagle dog at 1 mg/kg, iv2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID676324Plasma clearance in Beagle dog at 1 mg/kg, iv2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID676595Plasma concentration in SCID mouse xenografted with human KARPAS299 cells expressing NPM-ALK at 30 mg/kg, po after 24 hrs by LC-MS/MS analysis2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID676103Inhibition of human FAK at 1 uM2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID1319071Inhibition of CYP1A2 in human liver microsomes using phenacetin as substrate in presence of NADPH by LC/MS/MS analysis2016Journal of medicinal chemistry, 08-25, Volume: 59, Issue:16
ISSN: 1520-4804		Discovery of Clinical Candidate CEP-37440, a Selective Inhibitor of Focal Adhesion Kinase (FAK) and Anaplastic Lymphoma Kinase (ALK).
AID676327Half life in cynomolgus monkey at 1 mg/kg, iv2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID676340Oral bioavailability in CD-1 mouse at 10 mg/kg2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID676349AUC in Beagle dog at 10 mg/kg, po2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID676599Selectivity ratio of IC50 for human CHK2 to IC50 for human ALK cytoplasmic domain2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID1319064Inhibition of human ALK expressed in baculovirus using recombinant GST PLC-gamma as substrate assessed as phosphorylation of the substrate after 15 mins by TRF assay2016Journal of medicinal chemistry, 08-25, Volume: 59, Issue:16
ISSN: 1520-4804		Discovery of Clinical Candidate CEP-37440, a Selective Inhibitor of Focal Adhesion Kinase (FAK) and Anaplastic Lymphoma Kinase (ALK).
AID676357Cmax in rat at 30 mg/kg, po2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID1319073Inhibition of CYP2C19 in human liver microsomes using S-mephenytoin as substrate in presence of NADPH by LC/MS/MS analysis2016Journal of medicinal chemistry, 08-25, Volume: 59, Issue:16
ISSN: 1520-4804		Discovery of Clinical Candidate CEP-37440, a Selective Inhibitor of Focal Adhesion Kinase (FAK) and Anaplastic Lymphoma Kinase (ALK).
AID676354AUC in cynomolgus monkey at 10 mg/kg, po2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID676106Inhibition of human Flt3 at 1 uM2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID676088Inhibition of human FAK2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID676382Selectivity ratio of IC50 for human Fer to IC50 for human ALK cytoplasmic domain2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID1319053Half life in CD-1 mouse liver microsomes by LC/MS/MS analysis2016Journal of medicinal chemistry, 08-25, Volume: 59, Issue:16
ISSN: 1520-4804		Discovery of Clinical Candidate CEP-37440, a Selective Inhibitor of Focal Adhesion Kinase (FAK) and Anaplastic Lymphoma Kinase (ALK).
AID676320Plasma clearance in Sprague-Dawley rat at 1 mg/kg, iv2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID676373Selectivity ratio of IC50 for human ACK1 to IC50 for human ALK cytoplasmic domain2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID676385Selectivity ratio of IC50 for human Flt4 to IC50 for human ALK cytoplasmic domain2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID676339AUC in CD-1 mouse at 10 mg/kg, po2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID676337Tmax in CD-1 mouse at 10 mg/kg, po2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID1319052Clearance in cynomolgus monkey at 1 mg/kg, iv by LC/MS/MS analysis2016Journal of medicinal chemistry, 08-25, Volume: 59, Issue:16
ISSN: 1520-4804		Discovery of Clinical Candidate CEP-37440, a Selective Inhibitor of Focal Adhesion Kinase (FAK) and Anaplastic Lymphoma Kinase (ALK).
AID676380Selectivity ratio of IC50 for human BRK to IC50 for human ALK cytoplasmic domain2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID676366Drug level in SCID mouse tumor xenografted with human KARPAS299 cells expressing NPM-ALK at 30 mg/kg, po after 2 hrs by LC-MS/MS analysis2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID676359Cmax in rat at 100 mg/kg, po2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID676334AUC in SCID mouse at 10 mg/kg, po2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID676091Inhibition of human Flt32012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID676371Drug level in SCID/beige mouse tumor xenografted with human KARPAS299 cells expressing NPM-ALK at 10 mg/kg, po bid after 2 hrs post last dose by LC-MS/MS analysis2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID676093Inhibition of human GCK2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID676317Volume of distribution in CD-1 mouse at 1 mg/kg, iv2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID676346Cmax in Beagle dog at 10 mg/kg, po2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID676086Inhibition of human BRK2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID676361AUC (0 to 12 hrs) in rat 30 mg/kg, po2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID1319059Drug metabolism in human liver microsomes assessed as oxidative/degradative M2 metabolite formation at 10 uM after 120 mins in presence of NADPH by LC/MS/MS analysis2016Journal of medicinal chemistry, 08-25, Volume: 59, Issue:16
ISSN: 1520-4804		Discovery of Clinical Candidate CEP-37440, a Selective Inhibitor of Focal Adhesion Kinase (FAK) and Anaplastic Lymphoma Kinase (ALK).
AID676310Inhibition of human Rsk4 at 1 uM2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID1319068Inhibition of NPM-ALK phosphorylation in human SUP-M2 cells after 2 to 3 hrs by ELISA2016Journal of medicinal chemistry, 08-25, Volume: 59, Issue:16
ISSN: 1520-4804		Discovery of Clinical Candidate CEP-37440, a Selective Inhibitor of Focal Adhesion Kinase (FAK) and Anaplastic Lymphoma Kinase (ALK).
AID676338Half life in CD-1 mouse at 10 mg/kg, po2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID1319061Drug metabolism in human liver microsomes assessed as oxidative/degradative M6 metabolite formation at 10 uM after 120 mins in presence of NADPH by LC/MS/MS analysis2016Journal of medicinal chemistry, 08-25, Volume: 59, Issue:16
ISSN: 1520-4804		Discovery of Clinical Candidate CEP-37440, a Selective Inhibitor of Focal Adhesion Kinase (FAK) and Anaplastic Lymphoma Kinase (ALK).
AID1319130Dose normalized AUC in Sprague-Dawley rat at 5 mg/kg, po by LC/MS/MS analysis2016Journal of medicinal chemistry, 08-25, Volume: 59, Issue:16
ISSN: 1520-4804		Discovery of Clinical Candidate CEP-37440, a Selective Inhibitor of Focal Adhesion Kinase (FAK) and Anaplastic Lymphoma Kinase (ALK).
AID676080Inhibition of human ALK cytoplasmic domain expressed in baculovirus using GST-PLCgamma as substrate preincubated for 15 mins before substrate addition measured after 1 hr by time resolved fluorescence assay2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID676600Plasma concentration in SCID/beige mouse xenografted with human KARPAS299 cells expressing NPM-ALK at 30 mg/kg, po bid after 2 hrs post last dose by LC-MS/MS analysis2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID676108Inhibition of human GCK at 1 uM2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID676591Ratio of Cmax at 10 mg/kg, po to Cmax at 100 mg/kg, po in rat2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID676084Inhibition of human ACK12012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID676332Tmax in SCID mouse at 10 mg/kg, po2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID676311Half life in SCID mouse at 1 mg/kg, iv2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID1319060Drug metabolism in human liver microsomes assessed as oxidative/degradative M5 metabolite formation at 10 uM after 120 mins in presence of NADPH by LC/MS/MS analysis2016Journal of medicinal chemistry, 08-25, Volume: 59, Issue:16
ISSN: 1520-4804		Discovery of Clinical Candidate CEP-37440, a Selective Inhibitor of Focal Adhesion Kinase (FAK) and Anaplastic Lymphoma Kinase (ALK).
AID676377Antitumor activity against human KARPAS299 cells expressing NPM-ALK xenografted in SCID mouse assessed as tumor regression at 30 mg/kg, po bid for 12 days2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID676329Volume of distribution in cynomolgus monkey at 1 mg/kg, iv2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID676350Oral bioavailability in Beagle dog at 10 mg/kg2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID1319075Inhibition of CYP3A4 in human liver microsomes using testosterone/midazolam as substrate in presence of NADPH by LC/MS/MS analysis2016Journal of medicinal chemistry, 08-25, Volume: 59, Issue:16
ISSN: 1520-4804		Discovery of Clinical Candidate CEP-37440, a Selective Inhibitor of Focal Adhesion Kinase (FAK) and Anaplastic Lymphoma Kinase (ALK).
AID1319086Inhibition of FAK phosphorylation in human HCC827 cells after 2 to 2.5 hrs by immunoblot analysis2016Journal of medicinal chemistry, 08-25, Volume: 59, Issue:16
ISSN: 1520-4804		Discovery of Clinical Candidate CEP-37440, a Selective Inhibitor of Focal Adhesion Kinase (FAK) and Anaplastic Lymphoma Kinase (ALK).
AID676315Half life in CD-1 mouse at 1 mg/kg, iv2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID1319077Oral bioavailability in Sprague-Dawley rat at 5 mg/kg by LC/MS/MS analysis2016Journal of medicinal chemistry, 08-25, Volume: 59, Issue:16
ISSN: 1520-4804		Discovery of Clinical Candidate CEP-37440, a Selective Inhibitor of Focal Adhesion Kinase (FAK) and Anaplastic Lymphoma Kinase (ALK).
AID676109Inhibition of human JNK1alpha1 at 1 uM2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID676372Drug level in SCID/beige mouse tumor xenografted with human KARPAS299 cells expressing NPM-ALK at 30 mg/kg, po bid after 2 hrs post last dose by LC-MS/MS analysis2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID1319076Half life in cynomolgus monkey liver microsomes by LC/MS/MS analysis2016Journal of medicinal chemistry, 08-25, Volume: 59, Issue:16
ISSN: 1520-4804		Discovery of Clinical Candidate CEP-37440, a Selective Inhibitor of Focal Adhesion Kinase (FAK) and Anaplastic Lymphoma Kinase (ALK).
AID676326AUC in Beagle dog at 1 mg/kg, iv2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID676343Half life in Sprague-Dawley rat at 10 mg/kg, po2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID676104Inhibition of human Fer at 1 uM2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID1319051Clearance in Sprague-Dawley rat at 1 mg/kg, iv by LC/MS/MS analysis2016Journal of medicinal chemistry, 08-25, Volume: 59, Issue:16
ISSN: 1520-4804		Discovery of Clinical Candidate CEP-37440, a Selective Inhibitor of Focal Adhesion Kinase (FAK) and Anaplastic Lymphoma Kinase (ALK).
AID676082Selectivity ratio of IC50 for human recombinant IR cytoplasmic domain to IC50 for human ALK cytoplasmic domain2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID676309Inhibition of human Rsk3 at 1 uM2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID676085Inhibition of human ARK52012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID676102Inhibition of human CHK2 at 1 uM2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID676099Inhibition of human ACK1 at 1 uM2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID1319055Drug metabolism in rat liver microsomes assessed as oxidative/degradative M2 metabolite formation at 10 uM after 120 mins in presence of NADPH by LC/MS/MS analysis2016Journal of medicinal chemistry, 08-25, Volume: 59, Issue:16
ISSN: 1520-4804		Discovery of Clinical Candidate CEP-37440, a Selective Inhibitor of Focal Adhesion Kinase (FAK) and Anaplastic Lymphoma Kinase (ALK).
AID676105Inhibition of human Fes at 1 uM2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID1319129Dose normalized AUC in CD-1 mouse at 10 mg/kg, po by LC/MS/MS analysis2016Journal of medicinal chemistry, 08-25, Volume: 59, Issue:16
ISSN: 1520-4804		Discovery of Clinical Candidate CEP-37440, a Selective Inhibitor of Focal Adhesion Kinase (FAK) and Anaplastic Lymphoma Kinase (ALK).
AID676356Cmax in rat at 10 mg/kg, po2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID676355Oral bioavailability in cynomolgus monkey at 10 mg/kg2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID676376Antitumor activity against human SK-N-AS cells expressing wild type ALK assessed as growth inhibition administered as po bid2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID676318AUC in CD-1 mouse at 1 mg/kg, iv2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID676342Tmax in Sprague-Dawley rat at 10 mg/kg, po2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID676383Selectivity ratio of IC50 for human Fes to IC50 for human ALK cytoplasmic domain2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID676379Selectivity ratio of IC50 for human ARK5 to IC50 for human ALK cytoplasmic domain2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID676378Toxicity in SCID mouse xenografted with human KARPAS299 cells expressing NPM-ALK assessed as overt toxicity at 10 to 30 mg/kg, po bid2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID676353Half life in cynomolgus monkey at 10 mg/kg, po2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID676601Selectivity ratio of IC50 for human Rsk1 to IC50 for human ALK cytoplasmic domain2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID676336Cmax in CD-1 mouse at 10 mg/kg, po2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID676363AUC (0 to 12 hrs) in rat 100 mg/kg, po2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID1319065Inhibition of recombinant human INSR expressed in baculovirus using ATP as substrate after 15 mins by TRF assay2016Journal of medicinal chemistry, 08-25, Volume: 59, Issue:16
ISSN: 1520-4804		Discovery of Clinical Candidate CEP-37440, a Selective Inhibitor of Focal Adhesion Kinase (FAK) and Anaplastic Lymphoma Kinase (ALK).
AID676308Inhibition of human Rsk2 at 1 uM2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID676358Cmax in rat at 55 mg/kg, po2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID676362AUC (0 to 12 hrs) in rat 55 mg/kg, po2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID1319062Drug metabolism in human liver microsomes assessed as (1S,5R,6S,7R)-7-[5-Chloro-2-((S)-1-methoxy-7-morpholin-4-yl-6,7,8,9-tetrahydro-5H-benzocyclohepten-2-ylamino)-pyrimidin-4-ylamino]-3-oxa-tricyclo[3.2.1.0(2,4)]octane-6-carboxylic acid amide formation a2016Journal of medicinal chemistry, 08-25, Volume: 59, Issue:16
ISSN: 1520-4804		Discovery of Clinical Candidate CEP-37440, a Selective Inhibitor of Focal Adhesion Kinase (FAK) and Anaplastic Lymphoma Kinase (ALK).
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
ISSN: 1521-0111		A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS 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.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
ISSN: 1521-0111		A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings 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.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings 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.
AID1345648Human checkpoint kinase 2 (RAD53 family)2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID1345381Human ribosomal protein S6 kinase A3 (RSK subfamily)2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID1345310Human ribosomal protein S6 kinase A6 (RSK subfamily)2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID1345627Human FES proto-oncogene, tyrosine kinase (Fer family)2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID1345741Human NUAK family kinase 1 (NuaK subfamily)2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID1345701Human ribosomal protein S6 kinase A2 (RSK subfamily)2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID1345608Human FER tyrosine kinase (Fer family)2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
AID1345550Human ALK receptor tyrosine kinase (Type XIX RTKs: Leukocyte tyrosine kinase (LTK) receptor family)2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.

Research

Studies (6)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's4 (66.67)24.3611
2020's2 (33.33)2.80

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other6 (100.00%)84.16%
ConditionIndicatedStudiesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
Anaplastic Large-Cell Lymphoma0
1
2012201212.0low000010
Benign Neoplasms0
1
2012201212.0low000010
Cancer of Lung0
1
2012201212.0low000010
Carcinoma, Non-Small Cell Lung0
1
2012201212.0low000010
Carcinoma, Non-Small-Cell Lung0
1
2012201212.0low000010
Congenital Zika Syndrome0
1
202020204.0low000010
Diffuse Large B-Cell Lymphoma0
1
2012201212.0low000010
Disease Models, Animal0
1
202020204.0low000010
Experimental Neoplasms0
1
201620168.0low000010
Lung Neoplasms0
1
2012201212.0low000010
Lymphoma, Large B-Cell, Diffuse0
1
2012201212.0low000010
Lymphoma, Large-Cell, Anaplastic0
1
2012201212.0low000010
Neoplasms0
1
2012201212.0low000010
Neuroblastoma0
1
2012201212.0low000010
Zika Virus Infection0
1
202020204.0low000010

Bioavailability (1)

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

Dosage (2)

ArticleYear
Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
Journal of medicinal chemistry, , May-24, Volume: 55, Issue:10		2012
CEP-28122, a highly potent and selective orally active inhibitor of anaplastic lymphoma kinase with antitumor activity in experimental models of human cancers.
Molecular cancer therapeutics, , Volume: 11, Issue:3		2012