Known targets — ChEMBL curated mechanism
The experimentally established mechanism targets of Darusentan. The predicted profile below is derived independently by chemical similarity — agreement is a validation signal, a miss is honest.
Predicted protein targets (top 6)
| gene | UniProt | supporting neighbours | confidence | |
|---|---|---|---|---|
| ▸ | EDNRB known ✓ | P24530 | 20/20 | 1.00 |
| ▸ | EDNRA known ✓ | P25101 | 20/20 | 1.00 |
| ▸ | NR1I2 | O75469 | 1/20 | 0.74 |
| ▸ | KCNE1 | P15382 | 1/20 | 0.74 |
| ▸ | KCNQ1 | P51787 | 1/20 | 0.74 |
| ▸ | POLB | P06746 | 1/20 | 0.74 |
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.
| Compound | similarity | top predicted | shared targets | |
|---|---|---|---|---|
| Darusentan SCHEMBL795084 | 1.00 | EDNRB (1.00) | EDNRBEDNRANR1I2KCNE1KCNQ1 | |
| SCHEMBL7934042 | 0.93 | EDNRB (1.00) | EDNRBEDNRANR1I2KCNE1KCNQ1 | |
| SCHEMBL13066899 | 0.93 | EDNRB (0.86) | EDNRBEDNRANR1I2KCNE1KCNQ1 | |
| SCHEMBL8021756 | 0.92 | EDNRB (0.86) | EDNRBEDNRANR1I2KCNE1KCNQ1 | |
| SCHEMBL2350734 | 0.90 | EDNRB (0.81) | EDNRBEDNRANR1I2KCNE1KCNQ1 | |
| SCHEMBL1068402 | 0.90 | EDNRB (0.81) | EDNRBEDNRANR1I2KCNE1KCNQ1 | |
| Darusentan SCHEMBL6895168 | 0.89 | EDNRB (0.80) | EDNRBEDNRANR1I2KCNE1KCNQ1 | |
| Darusentan SCHEMBL14026681 | 0.88 | EDNRB (0.78) | EDNRBEDNRANR1I2KCNE1KCNQ1 | |
| SCHEMBL7071036 | 0.88 | EDNRB (1.00) | EDNRBEDNRA | |
| SCHEMBL15999837 | 0.87 | EDNRB (0.76) | EDNRBEDNRANR1I2KCNE1KCNQ1 |
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 75 patents — showing the first 20. claimed = in the patent's claims; disclosed = body only.
| Patent | Title | Assignee | Published | Priority | Filing | Country | Status |
|---|---|---|---|---|---|---|---|
| US-20060276645-A1 | Novel carboxylic acid derivatives, their preparation and use | RIECHERS HARTMUT | 2006-12-07 | — | — | US | claimed |
| EP-1110952-B9 | Carboxylic acid derivatives, their preparation and use | ABBOTT GMBH & CO KG (DE) | 2004-12-15 | — | — | EP | claimed |
| US-20030232787-A1 | Combinations of an endothelin receptor antagonist and an antiepileptic compound having pain alleviating properties or analgesic | DOOLEY DAVID JAMES (US) | 2003-12-18 | — | — | US | claimed |
| US-20170079978-A1 | THERAPY FOR COMPLICATIONS OF DIABETES | ABBVIE DEUTSCHLAND (DE) | 2017-03-23 | — | — | US | disclosed |
| US-9592231-B2 | Therapy for complications of diabetes | AbbVie Deutschland GmbH & Co. KG (DE) | 2017-03-14 | — | — | US | disclosed |
| US-9040698-B2 | Method for preparing optically pure (+)-ambrisentan and (+)-darusentan | INSTITUTE OF CHEMISTRY CHINESE ACADEMY OF SCIENCES (CN) | 2015-05-26 | — | — | US | disclosed |
| US-20150051234-A1 | THERAPY FOR COMPLICATIONS OF DIABETES | ABBVIE DEUTSCHLAND (DE) | 2015-02-19 | — | — | US | disclosed |
| US-8865650-B2 | Therapy for complications of diabetes | AbbVie Deutschland GmbH & Co. KG (DE) | 2014-10-21 | — | — | US | disclosed |
| US-20140249309-A1 | Method for Preparing Optically Pure (+)-Ambrisentan and (+)-Darusentan | INSTITUTE OF CHEMISTRY CHINESE ACADEMY OF SCIENCES (CN) | 2014-09-04 | — | — | US | disclosed |
| EP-2768811-A1 | PROCESS FOR THE PREPARATION OF AN ENDOTHELIN RECEPTOR ANTAGONIST | Cipla Limited (IN) | 2014-08-27 | — | — | EP | disclosed |
| US-20140073574-A1 | THERAPY FOR COMPLICATIONS OF DIABETES | AbbVie Deutschland GmbH & Co. KG (DE) | 2014-03-13 | — | — | US | disclosed |
| EP-1110952-A1 | Carboxylic acid derivates, their preparation and use | BASF AKTIENGESELLSCHAFT (DE) | 2001-06-27 | — | — | EP | disclosed |
| US-6197958-B1 | CYCLOPENTAPYRIMIDINE DERIVATIVES; ENDOTHELIN RECEPTOR INHIBITORS | BASF AKTIENGESELLSCHAFT (DE) | 2001-03-06 | — | — | US | disclosed |
| US-6030975-A | ANTAGONIST OF ENDOTHELINS, I.E. INHIBITION OF BINDING WITH RECEPTOR; ANTITUMOR AND -CARCINOGENIC AGENTS; SIDE EFFECT REDUCTION | BASF AKTIENGESELLSCHAFT (DE) | 2000-02-29 | — | — | US | disclosed |
| EP-0969841-A1 | USE OF CARBOXYLIC ACID DERIVATIVES FOR TREATING CANCER | BASF AKTIENGESELLSCHAFT (DE) | 2000-01-12 | — | — | EP | disclosed |
| US-5969134-A | CARDIOVASCULAR DISORDERS, VASOCONSTRICTION, HYPOTENSIVE AGENTS AND RELEASE OF ENDOTHELINS | BASF AKTIENGESELLSCHAFT (DE) | 1999-10-19 | — | — | US | disclosed |
| US-5932730-A | Carboxylic acid derivatives, their preparation and use | BASF AKTIENGESELLSCHAFT (DE) | 1999-08-03 | — | — | US | disclosed |
| WO-1998041206-A1 | NOVEL CARBOXYLIC ACID DERIVATIVES, THEIR PREPARATION AND USE IN TREATING CANCER | BASF AKTIENGESELLSCHAFT (DE) | 1998-09-24 | — | — | WO | disclosed |
| EP-0785926-A1 | NEW CARBOXYLIC ACID DERIVATIVES, THEIR PREPARATION AND THEIR USE | BASF AKTIENGESELLSCHAFT (DE) | 1997-07-30 | — | — | EP | disclosed |
| WO-1996011914-A1 | NEW CARBOXYLIC ACID DERIVATIVES, THEIR PREPARATION AND THEIR USE | BASF AKTIENGESELLSCHAFT (DE) | 1996-04-25 | — | — | WO | 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 (6 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.
| Patent | Title | Text reads most about | Predicted target · text-rank |
|---|---|---|---|
| US-20140073574-A1 | THERAPY FOR COMPLICATIONS OF DIABETES | EDNRA, EDNRB, GPR119 | EDNRB 2/4885EDNRA 1/4885NR1I2 1002/4885 |
| US-20150051234-A1 | THERAPY FOR COMPLICATIONS OF DIABETES | GPR119, ECE1, EDNRA | EDNRB 5/4885EDNRA 3/4885NR1I2 935/4885 |
| US-20170079978-A1 | THERAPY FOR COMPLICATIONS OF DIABETES | EDNRA, EDNRB, GPR119 | EDNRB 2/4885EDNRA 1/4885NR1I2 1007/4885 |
| US-20060276645-A1 | Novel carboxylic acid derivatives, their preparation and use | HCAR1, HCAR2, HCAR3 | EDNRB 374/4885EDNRA 373/4885NR1I2 1121/4885 |
| US-20140249309-A1 | Method for Preparing Optically Pure (+)-Ambrisentan and (+)-Darusentan | AKR1D1, AKR1C2, AKR1C1 | EDNRB 47/4885EDNRA 30/4885NR1I2 2176/4885 |
| US-20030232787-A1 | Combinations of an endothelin receptor antagonist and an antiepileptic compound having pain alleviating properties or analgesic | EDNRA, EDNRB, ECE1 | EDNRB 2/4885EDNRA 1/4885NR1I2 773/4885 |
“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.