Crizotinib

Crizotinib

SCHEMBL1827232

CC(=O)O.C[C@@H](Oc1cc(-c2cnn(C3CCNCC3)c2)cnc1N)c1c(Cl)ccc(F)c1Cl

nearest known ligand 0.91

Full drug profile on Sugi Atlas →

Known targets — ChEMBL curated mechanism

ALKEML4METMST1RNPM1ROS1

The experimentally established mechanism targets of Crizotinib. The predicted profile below is derived independently by chemical similarity — agreement is a validation signal, a miss is honest.

Predicted protein targets (top 20)

geneUniProtsupporting neighboursconfidence
MET known ✓ P08581 11/20 0.91
ALK known ✓ Q9UM73 7/20 0.91
ROS1 known ✓ P08922 2/20 0.91
MST1R known ✓ Q04912 2/20 0.91
NPM1 known ✓ P06748 1/20 0.91
EML4 known ✓ Q9HC35 1/20 0.91
MAP4K3 Q8IVH8 8/20 0.91
JAK2 O60674 6/20 0.91
JAK3 P52333 3/20 0.91
PLK4 O00444 2/20 0.91
AURKA O14965 2/20 0.91
DCLK1 O15075 2/20 0.91
PRKD3 O94806 2/20 0.91
ABL1 P00519 2/20 0.91
NTRK1 P04629 2/20 0.91
INSR P06213 2/20 0.91
LCK P06239 2/20 0.91
FES P07332 2/20 0.91
CSF1R P07333 2/20 0.91
LYN P07948 2/20 0.91

Click a target to see other patent compounds predicted against it — the reverse direction, in place.

Similar compounds — the chemically nearest patent molecules

Nearest neighbours by Morgan-fingerprint cosine across the patent-compound collection, with each neighbour's top predicted target and the predicted targets it shares with this molecule.

Compoundsimilaritytop predictedshared targets
Acetic Acid SCHEMBL16324188 0.95 MET (0.82) METMAP4K3ALKJAK2JAK3
Crizotinib SCHEMBL29622387 0.95 MET (1.00) METMAP4K3ALKJAK2JAK3
Crizotinib SCHEMBL14811801 0.95 MET (1.00) METMAP4K3ALKJAK2JAK3
Crizotinib SCHEMBL94020 0.95 MET (1.00) METMAP4K3ALKJAK2JAK3
Crizotinib SCHEMBL30129754 0.95 MET (1.00) METMAP4K3ALKJAK2JAK3
Crizotinib SCHEMBL29351506 0.95 MET (1.00) METMAP4K3ALKJAK2JAK3
Crizotinib SCHEMBL28844303 0.95 MET (1.00) METMAP4K3ALKJAK2JAK3
Crizotinib SCHEMBL93829 0.95 MET (1.00) METMAP4K3ALKJAK2JAK3
Crizotinib SCHEMBL29831970 0.95 MET (1.00) METMAP4K3ALKJAK2JAK3
Crizotinib SCHEMBL28844302 0.95 MET (1.00) METMAP4K3ALKJAK2JAK3

Similarity is cosine over the 2,048-bit Morgan fingerprint (≈ Tanimoto). Identical fingerprints score 1.00.

Patent provenance — the patents this molecule appears in, and who filed them

Claimed or disclosed in 20 patents. claimed = in the patent's claims; disclosed = body only.

PatentTitleAssigneePublishedPriorityFilingCountryStatus
EP-2315601-B1 COMBINATION OF A C-MET ANTAGONIST AND AN AMINOHETEROARYL COMPOUND FOR THE TREATMENT OF CANCER PF MEDICAMENT (FR) 2018-02-14 EP disclosed
US-9375425-B2 Combination of a C-Met antagonist and an aminoheteroaryl compound for the treatment of cancer PIERRE FABRE MEDICAMENT (FR) 2016-06-28 US disclosed
US-20150250780-A1 COMBINATION OF A C-MET ANTAGONIST AND AN AMINOHETEROARYL COMPOUND FOR THE TREATMENT OF CANCER PIERRE FABRE MEDICAMENT (FR) 2015-09-10 US disclosed
US-9011865-B2 Combination of a c-Met antagonist and an aminoheteroaryl compound for the treatment of cancer Pierre Gabre Medicament (FR) 2015-04-21 US disclosed
US-20140288086-A1 ENANTIOMERICALLY PURE AMINOHETEROARYL COMPOUNDS AS PROTEIN KINASE INHIBITORS PFIZER INC. (US) 2014-09-25 US disclosed
US-8785632-B2 Enantiomerically pure aminoheteroaryl compounds as protein kinase inhibitors AGOURON PHARMACEUTICALS, INC. (US) 2014-07-22 US disclosed
US-20140186356-A1 COMBINATION OF A C-MET ANTAGONIST AND AN AMINOHETEROARYL COMPOUND FOR THE TREATMENT OF CANCER PIERRE FABRE MEDICAMENT (FR) 2014-07-03 US disclosed
US-8623359-B2 Combination of a c-Met antagonist and an aminoheteroaryl compound for the treatment of cancer PIERRE FABRE MEDICAMENT (FR) 2014-01-07 US disclosed
EP-1786785-B9 ENANTIOMERICALLY PURE AMINOHETEROARYL COMPOUNDS AS PROTEIN KINASE INHIBITORS PFIZER (US) 2013-05-22 EP disclosed
US-20120263706-A1 ENANTIOMERICALLY PURE AMINOHETEROARYL COMPOUNDS AS PROTEIN KINASE INHIBITORS AGOURON PHARMACEUTICALS, INC. 2012-10-18 US disclosed
US-20110117098-A1 COMBINATION OF A C-MET ANTAGONIST AND AN AMINOHETEROARYL COMPOUND FOR THE TREATMENT OF CANCER PIERRE FABRE MEDICAMENT (FR) 2011-05-19 US disclosed
EP-2315601-A1 COMBINATION OF A C-MET ANTAGONIST AND AN AMINOHETEROARYL COMPOUND FOR THE TREATMENT OF CANCER Pierre Fabre Médicament (FR) 2011-05-04 EP disclosed
US-7858643-B2 Crizotinib, a c-Met protein kinase inhibitor anticancer agent; 3-[(R)-1-(2,6-dichloro-3-fluoro-phenyl)-ethoxy]-5-(1-piperidin-4-yl-1H-pyrazol-4-yl)-pyridin-2-ylamine is crizotinib AGOURON PHARMACEUTICALS, INC. (US) 2010-12-28 US disclosed
US-20100324061-A1 including crizotinib which is 3-[(R)-1-(2-chloro-3,6-difluoro-phenyl)-ethoxy]-5-(1-piperidin-4-yl-1H-pyrazol-4-yl)-pyridin-2-ylamine; c-met inhibitors; hepatocyte growth factor (HGF) receptor (c-MET) receptor tyrosine kinase (RTK) AGOURON PHARMACEUTICALS, INC. 2010-12-23 US disclosed
EP-1784396-B1 PYRAZOLE-SUBSTITUTED AMINOHETEROARYL COMPOUNDS AS PROTEIN KINASE INHIBITORS PFIZER (US) 2010-12-22 EP disclosed
EP-1786785-B1 ENANTIOMERICALLY PURE AMINOHETEROARYL COMPOUNDS AS PROTEIN KINASE INHIBITORS PFIZER (US) 2010-04-07 EP disclosed
WO-2010003992-A1 COMBINATION OF A C-MET ANTAGONIST AND AN AMINOHETEROARYL COMPOUND FOR THE TREATMENT OF CANCER PIERRE FABRE MEDICAMENT (FR) 2010-01-14 WO disclosed
EP-2143441-A1 Combination of a c-Met antagonist and an aminoheteroaryl compound for the treatment of cancer Pierre Fabre Medicament (FR) 2010-01-13 EP disclosed
US-20060128724-A1 Pyrazole-substituted aminoheteroaryl compounds as protein kinase inhibitors AGOURON PHARMACEUTICALS, INC. 2006-06-15 US disclosed
US-20060046991-A1 Crizotinib, a c-Met protein kinase inhibitor anticancer agent; 3-[(R)-1-(2,6-dichloro-3-fluoro-phenyl)-ethoxy]-5-(1-piperidin-4-yl-1H-pyrazol-4-yl)-pyridin-2-ylamine is crizotinib AGOURON PHARMACEUTICALS, INC. 2006-03-02 US disclosed

Patent text — is the patent's own abstract consistent with the prediction?

For each of this compound's patents that has machine-readable text (8 of them — usually the abstract, not the full specification), we ask MedCPT which protein the text reads most about, and where the chemistry-predicted target lands among 4885 human targets. A high rank means the patent's own wording is consistent with the prediction — a weak, independent signal, not proof of activity.

PatentTitleText reads most aboutPredicted target · text-rank
US-20110117098-A1 COMBINATION OF A C-MET ANTAGONIST AND AN AMINOHETEROARYL COMPOUND FOR THE TREATMENT OF CANCER MET, HGF, EGFR MET 1/4885ALK 26/4885ROS1 2043/4885
US-20060128724-A1 Pyrazole-substituted aminoheteroaryl compounds as protein kinase inhibitors MET, MAP3K15, MAP3K19 MET 1/4885ALK 136/4885ROS1 52/4885
US-20060046991-A1 Crizotinib, a c-Met protein kinase inhibitor anticancer agent; 3-[(R)-1-(2,6-dichloro-3-fluoro-phenyl)-ethoxy]-5-(1-piperidin-4-yl-1H-pyrazol-4-yl)-pyridin-2-ylamine is crizotinib ALK, MET, ERBB2 MET 2/4885ALK 1/4885ROS1 5/4885
US-20100324061-A1 including crizotinib which is 3-[(R)-1-(2-chloro-3,6-difluoro-phenyl)-ethoxy]-5-(1-piperidin-4-yl-1H-pyrazol-4-yl)-pyridin-2-ylamine; c-met inhibitors; hepatocyte growth factor (HGF) receptor (c-MET) receptor tyrosine kinase (RTK) MET, HGF, ALK MET 1/4885ALK 3/4885ROS1 20/4885
US-20120263706-A1 ENANTIOMERICALLY PURE AMINOHETEROARYL COMPOUNDS AS PROTEIN KINASE INHIBITORS MET, MAP3K15, MAP3K1 MET 1/4885ALK 190/4885ROS1 199/4885
US-20150250780-A1 COMBINATION OF A C-MET ANTAGONIST AND AN AMINOHETEROARYL COMPOUND FOR THE TREATMENT OF CANCER MET, HGF, EGFR MET 1/4885ALK 26/4885ROS1 2043/4885
US-20140186356-A1 COMBINATION OF A C-MET ANTAGONIST AND AN AMINOHETEROARYL COMPOUND FOR THE TREATMENT OF CANCER MET, HGF, EGFR MET 1/4885ALK 26/4885ROS1 2043/4885
US-20140288086-A1 ENANTIOMERICALLY PURE AMINOHETEROARYL COMPOUNDS AS PROTEIN KINASE INHIBITORS MET, MAP3K15, MAP3K1 MET 1/4885ALK 190/4885ROS1 199/4885

“Text reads most about” is the patent abstract's nearest protein in MedCPT space (background-debiased). Only ~1.4% of patents have machine-readable text, so most compounds won't have this panel.