Lofexidine

Lofexidine

SCHEMBL48960

CC(Oc1c(Cl)cccc1Cl)C1=NCCN1

nearest known ligand 1.00 ✓ in ChEMBL — recovers established targets

Full drug profile on Sugi Atlas →

Known targets — ChEMBL curated mechanism

ADRA2AADRA2BADRA2C

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

Predicted protein targets (top 11)

geneUniProtsupporting neighboursconfidence
ADRA2A known ✓ P08913 16/20 1.00
ADRA2B known ✓ P18089 16/20 1.00
ADRA2C known ✓ P18825 16/20 1.00
HTR1A P08908 2/20 1.00
SLC6A4 P31645 1/20 1.00
ADRA1A P35348 1/20 1.00
OPRK1 P41145 1/20 1.00
KCNH2 Q12809 1/20 1.00
MAOA P21397 6/20 0.61
MAOB P27338 6/20 0.61
NISCH Q9Y2I1 5/20 0.61

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
Levlofexidine SCHEMBL947241 1.00 ADRA2A (1.00) ADRA2AADRA2BADRA2CHTR1ASLC6A4
Dexlofexidine SCHEMBL124602 1.00 ADRA2A (1.00) ADRA2AADRA2BADRA2CHTR1ASLC6A4
Lofexidine SCHEMBL678553 0.98 ADRA2A (0.97) ADRA2AADRA2BADRA2CHTR1ASLC6A4
Lofexidine SCHEMBL22616208 0.98 ADRA2A (0.97) ADRA2AADRA2BADRA2CHTR1ASLC6A4
Lofexidine SCHEMBL3500726 0.98 ADRA2A (0.97) ADRA2AADRA2BADRA2CHTR1ASLC6A4
Lofexidine SCHEMBL124601 0.98 ADRA2A (0.97) ADRA2AADRA2BADRA2CHTR1ASLC6A4
Lofexidine SCHEMBL22616113 0.92 ADRA2A (0.85) ADRA2AADRA2BADRA2CHTR1ASLC6A4
Lofexidine SCHEMBL22616152 0.92 ADRA2A (0.85) ADRA2AADRA2BADRA2CHTR1ASLC6A4
Lofexidine SCHEMBL22616174 0.92 ADRA2A (0.85) ADRA2AADRA2BADRA2CHTR1ASLC6A4
Lofexidine SCHEMBL22616269 0.91 ADRA2A (0.82) ADRA2AADRA2BADRA2CHTR1ASLC6A4

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

Appears in 4326 patents — a generic fragment claimed broadly, so it's down-weighted as IP noise. Top by claim status then date:

PatentTitleAssigneePublishedPriorityFilingCountryStatus
EP-4704839-A2 IMIDAZOLE CONTAINING COMPOUNDS, DERIVATIVES THEREFORE, AND USES THEREOF ALPHERABIO LLC (US) 2026-03-11 EP claimed
EP-4704826-A1 COMPOSITIONS AND METHODS FOR TREATING POST-TRAUMATIC STRESS DISORDER Yale University (US) 2026-03-11 EP claimed
WO-2025245279-A1 NON-NATURALLY OCCURRING MELANOCORTIN RECEPTOR AGONISTS AND USE THEREFORE IN TREATMENT OF ADDICTION AND/OR PAIN ENDEVICA BIO, INC. (US) 2025-11-27 WO claimed
US-12472158-B2 Methods of treating trigeminal nerve pain VANDERBILT UNIVERSITY (US) 2025-11-18 US claimed
US-20250255781-A1 PROCESSES FOR PREPARATION OF 3-D PRINTED PHARMACEUTICAL PRODUCTS BRISTOL-MYERS SQUIBB COMPANY (US) 2025-08-14 US claimed
US-12383743-B2 Treatment of addiction and dependency TACA JR ARTURO C (US) 2025-08-12 US claimed
US-20250246289-A1 DYNAMICALLY TARGETING SUBSTANCE USE DISORDERS AND CONDITIONS VIA PERSONALIZED DIGITAL THERAPEUTICS Click Therapeutics, Inc. (US) 2025-07-31 US claimed
US-12351558-B2 Process for the synthesis of lofexidine MEDICHEM, S.A. (ES) 2025-07-08 US claimed
US-20250213647-A1 CHEMOKINE RECEPTORS AND ALPHA1 ADRENERGIC RECEPTORS/VASOPRESSIN RECEPTORS 1A HETEROMERS AS DRUG TARGETS FOR DISEASE UNIVERSITY OF SOUTH FLORIDA 2025-07-03 US claimed
US-20250195450-A1 BIOERODIBLE DRUG DELIVERY IMPLANTS HERA HEALTH SOLUTIONS INC. 2025-06-19 US claimed
EP-0081748-B1 PROCESS FOR THE PREPARATION OF (-)-2-(1-(2,6-DICHLOROPHENOXY)-ETHYL)-1,3-DIAZACYCLOPENT-2-ENE A. Nattermann & Cie. GmbH (DE) 1987-02-25 EP claimed
EP-0082364-B1 (+)-2-(1-(2,6-DICHLOROPHENOXY)-ETHYL)-1,3-DIAZACYCLOPENT-2-ENE, PROCESS FOR ITS PREPARATION AND ITS USE IN PHARMACEUTICAL COMPOSITIONS A. Nattermann & Cie. GmbH (DE) 1986-04-23 EP claimed
US-4575510-A LOFEXIDINE MERRELL DOW PHARMACEUTICALS INC. (US) 1986-03-11 US claimed
EP-0170193-A2 Feedstuff additive for the growth promoting of agricultural useful animals BOEHRINGER INGELHEIM VETMEDICA GMBH (DE) 1986-02-05 EP claimed
US-4518783-A Process for producing (-)-2-[1-(2,6-dichlorophenoxy)-ethyl]-1,3-diazacyclopent-2-ene A. NATTERMANN & CIE GMBH (DE) 1985-05-21 US claimed
US-4443464-A (+)-2-[1-(2,6-Dichlorophenoxy)-ethyl]-1,3-diazacyclopent-2-ene and the method for the treatment of human beings suffering from nervous disarrangements, in particular migraine A. NATTERMANN & CIE GMBH (DE) 1984-04-17 US claimed
EP-0081748-A2 Process for the preparation of (-)-2-(1-(2,6-dichlorophenoxy)-ethyl)-1,3-diazacyclopent-2-ene A. Nattermann & Cie. GmbH (DE) 1983-06-22 EP claimed
US-4382946-A Method of alleviating withdrawal symptoms MERRELL DOW PHARMACEUTICALS INC. (US) 1983-05-10 US claimed
US-4312879-A Clonidine and lofexidine as antidiarrheal agents RICHARDSON-MERRELL INC. (US) 1982-01-26 US claimed
US-4189492-A SYNERGISTIC RICHARDSON-MERRELL INC. (US) 1980-02-19 US claimed