Entrectinib

Entrectinib

SCHEMBL3512601

CN1CCN(c2ccc(C(=O)Nc3n[nH]c4ccc(Cc5cc(F)cc(F)c5)cc34)c(NC3CCOCC3)c2)CC1

nearest known ligand 1.00 ✓ in ChEMBL — recovers established targets

Full drug profile on Sugi Atlas →

Known targets — ChEMBL curated mechanism

ALKNTRK1NTRK2NTRK3ROS1

The experimentally established mechanism targets of Entrectinib. 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
ALK known ✓ Q9UM73 20/20 1.00
NTRK1 known ✓ P04629 1/20 1.00
ROS1 known ✓ P08922 1/20 1.00
NTRK3 known ✓ Q16288 1/20 1.00
NTRK2 known ✓ Q16620 1/20 1.00
INSR P06213 20/20 1.00
IGF1R P08069 14/20 1.00
AURKA O14965 3/20 1.00
AURKB Q96GD4 3/20 1.00
PLK4 O00444 1/20 1.00
DAPK3 O43293 1/20 1.00
JAK2 O60674 1/20 1.00
MAP4K4 O95819 1/20 1.00
ABL1 P00519 1/20 1.00
PRKCG P05129 1/20 1.00
LCK P06239 1/20 1.00
FYN P06241 1/20 1.00
CSF1R P07333 1/20 1.00
LYN P07948 1/20 1.00
RET P07949 1/20 1.00

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
Entrectinib SCHEMBL29394152 1.00 INSR (1.00) INSRALKIGF1RAURKAAURKB
Entrectinib SCHEMBL29358922 1.00 INSR (1.00) INSRALKIGF1RAURKAAURKB
SCHEMBL3511865 0.97 INSR (0.95) INSRALKIGF1RAURKAAURKB
Entrectinib SCHEMBL21802358 0.95 INSR (0.91) INSRALKIGF1RAURKAAURKB
SCHEMBL21966315 0.94 INSR (0.89) INSRALKIGF1RAURKAAURKB
SCHEMBL3514081 0.94 INSR (1.00) INSRALKIGF1RAURKAAURKB
SCHEMBL3511962 0.94 INSR (0.89) INSRALKIGF1RAURKAAURKB
SCHEMBL21700375 0.94 INSR (0.89) INSRALKIGF1RAURKAAURKB
SCHEMBL3510936 0.94 ALK (1.00) INSRALKIGF1RAURKAAURKB
Entrectinib SCHEMBL21802362 0.94 INSR (0.88) INSRALKIGF1RAURKAAURKB

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 544 patents — showing the first 20. claimed = in the patent's claims; disclosed = body only.

PatentTitleAssigneePublishedPriorityFilingCountryStatus
CN-119909073-A Novel pharmaceutical formulations 豪夫迈·罗氏有限公司 2025-05-02 CN claimed
CN-111225662-B Pharmaceutical compositions and dosage forms 伊尼塔公司 2022-11-22 CN claimed
US-20220218699-A1 New Pharmaceutical Formulation HOFFMANN-LA ROCHE INC. (US) 2022-07-14 US claimed
EP-4003309-A1 NEW PHARMACEUTICAL FORMULATION F. Hoffmann-La Roche AG (CH) 2022-06-01 EP claimed
US-20220144813-A1 SUBSTITUTED INDAZOLE DERIVATIVES ACTIVE AS KINASE INHIBITORS NERVIANO MEDICAL SCIENCES S.R.L. (IT) 2022-05-12 US claimed
CN-114206341-A Novel pharmaceutical formulations 豪夫迈·罗氏有限公司 2022-03-18 CN claimed
US-11253515-B2 Pharmaceutical compositions and dosage forms IGNYTA, INC. (US) 2022-02-22 US claimed
US-11091469-B2 Crystalline form of N-[5-(3,5-difluoro-benzyl)-1H-indazol-3-yl]-4-(4-methyl-piperazin-1-yl)-2-(tetrahydro-pyran-4-ylamino)-benzamide NERVIANO MEDICAL SCIENCES S.R.L. (IT) 2021-08-17 US claimed
US-20210164055-A1 POINT MUTATIONS IN TRK INHIBITOR-RESISTANT CANCER AND METHODS RELATING TO THE SAME ARRAY BIOPHARMA, INC. 2021-06-03 US claimed
US-11007191-B2 Pharmaceutical compositions and dosage forms IGNYTA, INC. (US) 2021-05-18 US claimed
WO-2015124697-A1 COMPOUNDS FOR TREATING PATIENTS WITH ROS1 MUTANT CANCER CELLS IGNYTA, INC. (US) 2015-08-27 WO claimed
US-9085565-B2 Process for the preparation of N-[5-(3,5-difluoro-benzyl)-1H-indazol-3-yl]-4-(4-methyl-piperazin-1-yl)-2-(tetrahydro-pyran-4-ylamino)-benzamide NERVIANO MEDICAL SCIENCES S.R.L. (IT) 2015-07-21 US claimed
US-9085558-B2 Substituted indazole derivatives active as kinase inhibitors NERVIANO MEDICAL SCIENCES S.R.L. (IT) 2015-07-21 US claimed
US-20150065520-A1 SUBSTITUTED INDAZOLE DERIVATIVES ACTIVE AS KINASE INHIBITORS NERVIANO MEDICAL SCIENCES S.R.L. (IT) 2015-03-05 US claimed
US-20150057291-A1 SUBSTITUTED INDAZOLE DERIVATIVES ACTIVE AS KINASE INHIBITORS NERVIANO MEDICAL SCIENCES S.R.L. (IT) 2015-02-26 US claimed
US-20150051222-A1 PROCESS FOR THE PREPARATION OF N-[5-(3,5-DIFLUORO-BENZYL)-1H-INDAZOL-3-YL]-4-(4-METHYL-PIPERAZIN-1-YL)-2-(TETRAHYDRO-PYRAN-4-YLAMINO)-BENZAMIDE NERVIANO MEDICAL SCIENCES S.R.L. (IT) 2015-02-19 US claimed
US-8299057-B2 Substituted indazole derivatives active as kinase inhibitors NERVIANO MEDICAL SCIENCES S.R.L. (IT) 2012-10-30 US claimed
US-20100292207-A1 SUBSTITUTED INDAZOLE DERIVATIVES ACTIVE AS KINASE INHIBITORS NERVIANO MEDICAL SCIENCES S.R.L. (IT) 2010-11-18 US claimed
EP-2176231-A1 SUBSTITUTED INDAZOLE DERIVATIVES ACTIVE AS KINASE INHIBITORS Nerviano Medical Sciences S.r.l. (IT) 2010-04-21 EP claimed
WO-2009013126-A1 SUBSTITUTED INDAZOLE DERIVATIVES ACTIVE AS KINASE INHIBITORS NERVIANO MEDICAL SCIENCES S.R.L. (IT) 2009-01-29 WO claimed

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

For each of this compound's patents that has machine-readable text (10 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-20100292207-A1 SUBSTITUTED INDAZOLE DERIVATIVES ACTIVE AS KINASE INHIBITORS MAP3K19, MAP3K3, MAP3K5 ALK 401/4885NTRK1 1510/4885ROS1 227/4885
US-20150051222-A1 PROCESS FOR THE PREPARATION OF N-[5-(3,5-DIFLUORO-BENZYL)-1H-INDAZOL-3-YL]-4-(4-METHYL-PIPERAZIN-1-YL)-2-(TETRAHYDRO-PYRAN-4-YLAMINO)-BENZAMIDE MAP4K2, MAP3K2, MAP3K5 ALK 564/4885NTRK1 803/4885ROS1 516/4885
US-11091469-B2 Crystalline form of N-[5-(3,5-difluoro-benzyl)-1H-indazol-3-yl]-4-(4-methyl-piperazin-1-yl)-2-(tetrahydro-pyran-4-ylamino)-benzamide CSNK2A1, CSNK2A2, CSNK1A1 ALK 932/4885NTRK1 1801/4885ROS1 668/4885
US-20210164055-A1 POINT MUTATIONS IN TRK INHIBITOR-RESISTANT CANCER AND METHODS RELATING TO THE SAME NTRK3, NTRK1, NTRK2 ALK 89/4885NTRK1 2/4885ROS1 914/4885
US-20220218699-A1 New Pharmaceutical Formulation H4C1; H4C2; H4C3; H4C4; H4C5; H4C6; H4C8; H4C9; H4C11; H4C12; H4C13; H4C14; H4C15; H4C16, CYP3A5, DPYD ALK 781/4885NTRK1 3914/4885ROS1 4706/4885
US-11007191-B2 Pharmaceutical compositions and dosage forms H4C1; H4C2; H4C3; H4C4; H4C5; H4C6; H4C8; H4C9; H4C11; H4C12; H4C13; H4C14; H4C15; H4C16, TP53, CYP3A5 ALK 1045/4885NTRK1 4510/4885ROS1 4374/4885
US-20150065520-A1 SUBSTITUTED INDAZOLE DERIVATIVES ACTIVE AS KINASE INHIBITORS MAP3K19, ABL1, MAP3K20 ALK 397/4885NTRK1 1467/4885ROS1 86/4885
US-20220144813-A1 SUBSTITUTED INDAZOLE DERIVATIVES ACTIVE AS KINASE INHIBITORS MAP3K19, ABL1, MAP3K20 ALK 397/4885NTRK1 1467/4885ROS1 86/4885
US-11253515-B2 Pharmaceutical compositions and dosage forms CYP3A5, H4C1; H4C2; H4C3; H4C4; H4C5; H4C6; H4C8; H4C9; H4C11; H4C12; H4C13; H4C14; H4C15; H4C16, PAICS ALK 1518/4885NTRK1 4511/4885ROS1 4806/4885
US-20150057291-A1 SUBSTITUTED INDAZOLE DERIVATIVES ACTIVE AS KINASE INHIBITORS MAP3K19, ABL1, MAP3K20 ALK 397/4885NTRK1 1467/4885ROS1 86/4885

“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.