Details of the Target

General Information of Target

Target ID LDTP02508
Target Name Cytochrome P450 2D6 (CYP2D6)
Gene Name CYP2D6
Gene ID 1565
Synonyms
CYP2DL1; Cytochrome P450 2D6; EC 1.14.14.-; CYPIID6; Cholesterol 25-hydroxylase; Cytochrome P450-DB1; Debrisoquine 4-hydroxylase
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MGLEALVPLAVIVAIFLLLVDLMHRRQRWAARYPPGPLPLPGLGNLLHVDFQNTPYCFDQ
LRRRFGDVFSLQLAWTPVVVLNGLAAVREALVTHGEDTADRPPVPITQILGFGPRSQGVF
LARYGPAWREQRRFSVSTLRNLGLGKKSLEQWVTEEAACLCAAFANHSGRPFRPNGLLDK
AVSNVIASLTCGRRFEYDDPRFLRLLDLAQEGLKEESGFLREVLNAVPVLLHIPALAGKV
LRFQKAFLTQLDELLTEHRMTWDPAQPPRDLTEAFLAEMEKAKGNPESSFNDENLRIVVA
DLFSAGMVTTSTTLAWGLLLMILHPDVQRRVQQEIDDVIGQVRRPEMGDQAHMPYTTAVI
HEVQRFGDIVPLGVTHMTSRDIEVQGFRIPKGTTLITNLSSVLKDEAVWEKPFRFHPEHF
LDAQGHFVKPEAFLPFSAGRRACLGEPLARMELFLFFTSLLQHFSFSVPTGQPRPSHHGV
FAFLVSPSPYELCAVPR
Target Type
Successful
Target Bioclass
Enzyme
Family
Cytochrome P450 family
Subcellular location
Endoplasmic reticulum membrane
Function
A cytochrome P450 monooxygenase involved in the metabolism of fatty acids, steroids and retinoids. Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate, and reducing the second into a water molecule, with two electrons provided by NADPH via cytochrome P450 reductase (NADPH--hemoprotein reductase). Catalyzes the epoxidation of double bonds of polyunsaturated fatty acids (PUFA). Metabolizes endocannabinoid arachidonoylethanolamide (anandamide) to 20-hydroxyeicosatetraenoic acid ethanolamide (20-HETE-EA) and 8,9-, 11,12-, and 14,15-epoxyeicosatrienoic acid ethanolamides (EpETrE-EAs), potentially modulating endocannabinoid system signaling. Catalyzes the hydroxylation of carbon-hydrogen bonds. Metabolizes cholesterol toward 25-hydroxycholesterol, a physiological regulator of cellular cholesterol homeostasis. Catalyzes the oxidative transformations of all-trans retinol to all-trans retinal, a precursor for the active form all-trans-retinoic acid. Also involved in the oxidative metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic antidepressants.
TTD ID
T57392
Uniprot ID
P10635
DrugMap ID
TTVG215
Ensemble ID
ENST00000359033.4
HGNC ID
HGNC:2625
ChEMBL ID
CHEMBL289

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
HGC27 SNV: p.E222K .
HUH1 Deletion: p.Q52RfsTer41 .
RKO SNV: p.V495M .
SUPT1 Deletion: p.L9WfsTer3 .
SW756 SNV: p.Y33H .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 1 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
CY-1
 Probe Info  		N.A.  LDD0246  [1]

The Interaction Atlas With This Target

The Drug(s) Related To This Target

Approved
Click To Hide/Show 334 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Peginterferon Alfa-2b BiotechDrug DB00022
Cyclosporine Protein/peptide DB00091
Abemaciclib Small molecular drug DB12001
Abiraterone Small molecular drug DB05812
Acebutolol Small molecular drug DB01193
Acetaminophen Small molecular drug DB00316
Almotriptan Small molecular drug DB00918
Alogliptin Small molecular drug DB06203
Amiodarone Small molecular drug DB01118
Amitriptyline Small molecular drug DB00321
Amlodipine Small molecular drug DB00381
Amodiaquine Small molecular drug DB00613
Amoxapine Small molecular drug DB00543
Amphetamine Small molecular drug DB00182
Amprenavir Small molecular drug DB00701
Antipyrine Small molecular drug DB01435
Arformoterol Small molecular drug DB01274
Aripiprazole Small molecular drug DB01238
Asenapine Small molecular drug DB06216
Astemizole Small molecular drug DB00637
Asunaprevir Small molecular drug DB11586
Atenolol Small molecular drug DB00335
Atomoxetine Small molecular drug DB00289
Atorvastatin Small molecular drug DB01076
Azelastine Small molecular drug DB00972
Benzocaine Small molecular drug DB01086
Bepridil Small molecular drug DB01244
Berotralstat Small molecular drug DB15982
Betaxolol Small molecular drug DB00195
Bicalutamide Small molecular drug DB01128
Biperiden Small molecular drug DB00810
Bortezomib Small molecular drug DB00188
Brexpiprazole Small molecular drug DB09128
Brincidofovir Small molecular drug DB12151
Bupivacaine Small molecular drug DB00297
Buprenorphine Small molecular drug DB00921
Bupropion Small molecular drug DB01156
Buspirone Small molecular drug DB00490
Caffeine Small molecular drug DB00201
Cannabidiol Small molecular drug DB09061
Cariprazine Small molecular drug DB06016
Carteolol Small molecular drug DB00521
Carvedilol Small molecular drug DB01136
Celecoxib Small molecular drug DB00482
Celiprolol Small molecular drug DB04846
Cerivastatin Small molecular drug DB00439
Cevimeline Small molecular drug DB00185
Chloroquine Small molecular drug DB00608
Chlorpheniramine Small molecular drug DB01114
Chlorpromazine Small molecular drug DB00477
Chlorzoxazone Small molecular drug DB00356
Ciclesonide Small molecular drug DB01410
Cilostazol Small molecular drug DB01166
Cimetidine Small molecular drug DB00501
Cinacalcet Small molecular drug DB01012
Cinnarizine Small molecular drug DB00568
Cisapride Small molecular drug DB00604
Citalopram Small molecular drug DB00215
Clascoterone Small molecular drug DB12499
Clemastine Small molecular drug DB00283
Clevidipine Small molecular drug DB04920
Clofazimine Small molecular drug DB00845
Clomipramine Small molecular drug DB01242
Clonidine Small molecular drug DB00575
Clotrimazole Small molecular drug DB00257
Clozapine Small molecular drug DB00363
Cobicistat Small molecular drug DB09065
Cobimetinib Small molecular drug DB05239
Cocaine Small molecular drug DB00907
Codeine Small molecular drug DB00318
Curcumin Small molecular drug DB11672
Cyclobenzaprine Small molecular drug DB00924
Dacomitinib Small molecular drug DB11963
Dapagliflozin Small molecular drug DB06292
Darifenacin Small molecular drug DB00496
Darunavir Small molecular drug DB01264
Dasabuvir Small molecular drug DB09183
Debrisoquine Small molecular drug DB04840
Delavirdine Small molecular drug DB00705
Desipramine Small molecular drug DB01151
Desvenlafaxine Small molecular drug DB06700
Deutetrabenazine Small molecular drug DB12161
Dexchlorpheniramine Maleate Small molecular drug DB09555
Dexfenfluramine Small molecular drug DB01191
Dexmedetomidine Small molecular drug DB00633
Dextroamphetamine Small molecular drug DB01576
Dextromethorphan Small molecular drug DB00514
Dextropropoxyphene Small molecular drug DB00647
Diacerein Small molecular drug DB11994
Diltiazem Small molecular drug DB00343
Diphenhydramine Small molecular drug DB01075
Dolasetron Small molecular drug DB00757
Domperidone Small molecular drug DB01184
Donepezil Small molecular drug DB00843
Doxazosin Small molecular drug DB00590
Doxepin Small molecular drug DB01142
Doxorubicin Small molecular drug DB00997
Dronabinol Small molecular drug DB00470
Dronedarone Small molecular drug DB04855
Duloxetine Small molecular drug DB00476
Efavirenz Small molecular drug DB00625
Elagolix Small molecular drug DB11979
Eletriptan Small molecular drug DB00216
Eliglustat Small molecular drug DB09039
Encainide Small molecular drug DB01228
Encorafenib Small molecular drug DB11718
Entacapone Small molecular drug DB00494
Epinastine Small molecular drug DB00751
Erlotinib Small molecular drug DB00530
Escitalopram Small molecular drug DB01175
Esmolol Small molecular drug DB00187
Ethambutol Small molecular drug DB00330
Etoricoxib Small molecular drug DB01628
Everolimus Small molecular drug DB01590
Fedratinib Small molecular drug DB12500
Felodipine Small molecular drug DB01023
Fenfluramine Small molecular drug DB00574
Fesoterodine Small molecular drug DB06702
Flecainide Small molecular drug DB01195
Flunarizine Small molecular drug DB04841
Fluoxetine Small molecular drug DB00472
Fluphenazine Small molecular drug DB00623
Fluvastatin Small molecular drug DB01095
Fluvoxamine Small molecular drug DB00176
Formoterol Small molecular drug DB00983
Fusidic Acid Small molecular drug DB02703
Galantamine Small molecular drug DB00674
Gefitinib Small molecular drug DB00317
Glutethimide Small molecular drug D0Z9NZ
Glycopyrronium Small molecular drug DB00986
Halofantrine Small molecular drug DB01218
Haloperidol Small molecular drug DB00502
Hydrocodone Small molecular drug DB00956
Hydroxychloroquine Small molecular drug DB01611
Hydroxyurea Small molecular drug DB01005
Hydroxyzine Small molecular drug DB00557
Ibrutinib Small molecular drug DB09053
Idarubicin Small molecular drug DB01177
Iloperidone Small molecular drug DB04946
Imatinib Small molecular drug DB00619
Imipramine Small molecular drug DB00458
Indinavir Small molecular drug DB00224
Isavuconazole Small molecular drug DB11633
Isoniazid Small molecular drug DB00951
Istradefylline Small molecular drug DB11757
Ketoconazole Small molecular drug DB01026
Labetalol Small molecular drug DB00598
Lansoprazole Small molecular drug DB00448
Lasmiditan Small molecular drug DB11732
Lenvatinib Small molecular drug DB09078
Lercanidipine Small molecular drug DB00528
Levobetaxolol Small molecular drug DB09351
Levobunolol Small molecular drug DB01210
Levomilnacipran Small molecular drug DB08918
Lidocaine Small molecular drug DB00281
Lisdexamfetamine Small molecular drug DB01255
Lofexidine Small molecular drug DB04948
Lomustine Small molecular drug DB01206
Loperamide Small molecular drug DB00836
Lopinavir Small molecular drug DB01601
Loratadine Small molecular drug DB00455
Lorcaserin Small molecular drug DB04871
Manidipine Small molecular drug DB09238
Maprotiline Small molecular drug DB00934
Meclizine Small molecular drug DB00737
Menadione Small molecular drug DB00170
Meperidine Small molecular drug DB00454
Mephenytoin Small molecular drug DB00532
Mepyramine Small molecular drug DB06691
Mesoridazine Small molecular drug DB00933
Metamfetamine Small molecular drug DB01577
Methadone Small molecular drug DB00333
Methimazole Small molecular drug DB00763
Methotrimeprazine Small molecular drug DB01403
Methoxyflurane Small molecular drug DB01028
Metipranolol Small molecular drug DB01214
Metoclopramide Small molecular drug DB01233
Metoprolol Small molecular drug DB00264
Mexiletine Small molecular drug DB00379
Mianserin Small molecular drug DB06148
Miconazole Small molecular drug DB01110
Midodrine Small molecular drug DB00211
Midostaurin Small molecular drug DB06595
Mifepristone Small molecular drug DB00834
Minaprine Small molecular drug DB00805
Mirabegron Small molecular drug DB08893
Mirtazapine Small molecular drug DB00370
Moclobemide Small molecular drug DB01171
Modafinil Small molecular drug DB00745
Naloxegol Small molecular drug DB09049
Nateglinide Small molecular drug DB00731
Nebivolol Small molecular drug DB04861
Nefazodone Small molecular drug DB01149
Nelfinavir Small molecular drug DB00220
Netupitant Small molecular drug DB09048
Nevirapine Small molecular drug DB00238
Niacin Small molecular drug DB00627
Nicardipine Small molecular drug DB00622
Nicergoline Small molecular drug DB00699
Nicotinamide Small molecular drug DB02701
Nicotine Small molecular drug DB00184
Nifedipine Small molecular drug DB01115
Nilotinib Small molecular drug DB04868
Nortriptyline Small molecular drug DB00540
Olanzapine Small molecular drug DB00334
Oliceridine Small molecular drug DB14881
Omeprazole Small molecular drug DB00338
Ondansetron Small molecular drug DB00904
Orphenadrine Small molecular drug DB01173
Osilodrostat Small molecular drug DB11837
Ospemifene Small molecular drug DB04938
Oxprenolol Small molecular drug DB01580
Oxybutynin Small molecular drug DB01062
Oxycodone Small molecular drug DB00497
Oxymetholone Small molecular drug DB06412
Oxymorphone Small molecular drug DB01192
Paliperidone Small molecular drug DB01267
Palonosetron Small molecular drug DB00377
Paroxetine Small molecular drug DB00715
Pazopanib Small molecular drug DB06589
Penbutolol Small molecular drug DB01359
Pentamidine Small molecular drug DB00738
Perhexiline Small molecular drug DB01074
Perphenazine Small molecular drug DB00850
Phenelzine Small molecular drug DB00780
Phenformin Small molecular drug DB00914
Phenytoin Small molecular drug DB00252
Pimavanserin Small molecular drug DB05316
Pimozide Small molecular drug DB01100
Pindolol Small molecular drug DB00960
Piperazine Small molecular drug DB00592
Pipotiazine Small molecular drug DB01621
Pitolisant Small molecular drug DB11642
Ponatinib Small molecular drug DB08901
Practolol Small molecular drug DB01297
Primaquine Small molecular drug DB01087
Procainamide Small molecular drug DB01035
Prochlorperazine Small molecular drug DB00433
Progesterone Small molecular drug DB00396
Proguanil Small molecular drug DB01131
Promazine Small molecular drug DB00420
Promethazine Small molecular drug DB01069
Propafenone Small molecular drug DB01182
Propranolol Small molecular drug DB00571
Quetiapine Small molecular drug DB01224
Quinidine Small molecular drug DB00908
Quinine Small molecular drug DB00468
Rabeprazole Small molecular drug DB01129
Ranitidine Small molecular drug DB00863
Ranolazine Small molecular drug DB00243
Reboxetine Small molecular drug DB00234
Remdesivir Small molecular drug DB14761
Remoxipride Small molecular drug DB00409
Rifamycin Small molecular drug DB11753
Rilpivirine Small molecular drug DB08864
Risperidone Small molecular drug DB00734
Ritonavir Small molecular drug DB00503
Rolapitant Small molecular drug DB09291
Rosiglitazone Small molecular drug DB00412
Rotigotine Small molecular drug DB05271
Rucaparib Small molecular drug DB12332
Rupatadine Small molecular drug DB11614
Safinamide Small molecular drug DB06654
Saquinavir Small molecular drug DB01232
Selegiline Small molecular drug DB01037
Sertindole Small molecular drug DB06144
Sertraline Small molecular drug DB01104
Sildenafil Small molecular drug DB00203
Simvastatin Small molecular drug DB00641
Solifenacin Small molecular drug DB01591
Sorafenib Small molecular drug DB00398
Sotagliflozin Small molecular drug DB12713
Sotalol Small molecular drug DB00489
Stiripentol Small molecular drug DB09118
Sulfaphenazole Small molecular drug DB06729
Tamoxifen Small molecular drug DB00675
Tamsulosin Small molecular drug DB00706
Tapentadol Small molecular drug DB06204
Tegaserod Small molecular drug DB01079
Telotristat Ethyl Small molecular drug DB12095
Temsirolimus Small molecular drug DB06287
Terbinafine Small molecular drug DB00857
Terfenadine Small molecular drug DB00342
Tetrabenazine Small molecular drug DB04844
Theophylline Small molecular drug DB00277
Thioridazine Small molecular drug DB00679
Thiothixene Small molecular drug DB01623
Ticlopidine Small molecular drug DB00208
Timolol Small molecular drug DB00373
Tiotropium Small molecular drug DB01409
Tipranavir Small molecular drug DB00932
Tirbanibulin Small molecular drug DB06137
Tolterodine Small molecular drug DB01036
Tramadol Small molecular drug DB00193
Tranylcypromine Small molecular drug DB00752
Trazodone Small molecular drug DB00656
Trimipramine Small molecular drug DB00726
Tripelennamine Small molecular drug DB00792
Trospium Small molecular drug DB00209
Ubrogepant Small molecular drug DB15328
Umeclidinium Small molecular drug DB09076
Valbenazine Small molecular drug DB11915
Vemurafenib Small molecular drug DB08881
Venlafaxine Small molecular drug DB00285
Verapamil Small molecular drug DB00661
Vernakalant Small molecular drug DB06217
Vilazodone Small molecular drug DB06684
Vinblastine Small molecular drug DB00570
Vinorelbine Small molecular drug DB00361
Vortioxetine Small molecular drug DB09068
Yohimbine Small molecular drug DB01392
Zafirlukast Small molecular drug DB00549
Zolpidem Small molecular drug DB00425
Zuclopenthixol Small molecular drug DB01624
Adagrasib . DB15568
Aripiprazole Lauroxil . DB14185
Artenimol . DB11638
Belumosudil . DB16703
Deucravacitinib . DB16650
Dimethyl Sulfoxide . DB01093
Dosulepin . DB09167
Elexacaftor . DB15444
Enasidenib . DB13874
Futibatinib . DB15149
Letermovir . DB12070
Lorpiprazole . DB09195
Mavacamten . DB14921
Methylene Blue . DB09241
Opium . DB11130
Pralsetinib . DB15822
Ripretinib . DB14840
Tapinarof . DB06083
Upadacitinib . DB15091
Viloxazine . DB09185
Phase 1
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Isoquine Small molecular drug D03GNI
Investigative
Click To Hide/Show 71 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
(2-hydroxy-3-phenoxypropyl)(Propan-2-yl)Amine Small molecular drug D0C7PK
(5-(Pyridin-3-yl)Furan-2-yl)Methanamine Small molecular drug D06QFO
(5-phenylfuran-2-yl)Methanamine Small molecular drug D0YQ8U
(5-pyridin-3-yl-furan-2-yl)Methanethiol Small molecular drug D0YP4A
1,5-bis(4-hydroxyphenyl)Penta-1,4-dien-3-one Small molecular drug D0J6RQ
1-(3,4-dichlorophenyl)-6-(Methoxymethyl)-3-azabicyclo[4.1.0]Heptane (Enantiomeric Mix) Small molecular drug D0G6BJ
1-(4-butoxy-phenyl)-1h-imidazole Small molecular drug D07VHB
1-(Methoxymethyl)-6-(Naphthalen-2-yl)-3-azabicyclo[4.1.0]Heptane (Enantiomeric Mix) Small molecular drug D0J4CB
1h-1,2,3-benzotriazol-1-amine Small molecular drug D07ANY
2-(4-imidazol-1-yl-phenoxymethyl)-pyridine Small molecular drug D0B0LC
2-fluoro-4-[5-(3-hydroxyphenyl)-2-thienyl]Phenol Small molecular drug D0M0KX
2-hexyloxy-5-imidazol-1-yl-pyridine Small molecular drug D00AEX
2-[3-(4-imidazol-1-yl-phenoxy)-propyl]-pyridine Small molecular drug D0U7BJ
3-(6-methoxynaphthalen-2-yl)Pyridin-4-amine Small molecular drug D02GFK
3-[3-(4-imidazol-1-yl-phenoxy)-propyl]-pyridine Small molecular drug D02DTR
4-(3-pent-1-ynyl-benzyl)-1h-imidazole Small molecular drug D01DAU
4-(3-phenylethynyl-benzyl)-1h-imidazole Small molecular drug D0FF0Z
4-(Spiro[Chromene-2,4'-piperidine]-4-yl)Benzamide Small molecular drug D0L9YP
4-methylaminomethyl-7-methoxycoumarin Small molecular drug D0QH6F
4-[2-(4-imidazol-1-yl-phenoxy)-ethyl]-morpholine Small molecular drug D00PYW
4-[3-(4-imidazol-1-yl-phenoxy)-propyl]-pyridine Small molecular drug D03KXT
4-[5-(3-hydroxyphenyl)-2-thienyl)-2-methyl]Phenol Small molecular drug D0Y2RL
4-[5-(3-hydroxyphenyl)-3-thienyl]-2-methylphenol Small molecular drug D01RZP
6-(3,4-dichlorophenyl)-1-[1-(Methyloxy)-3-buten-1-yl]-3-azabicyclo[4.1.0]Heptane (Diastereomeric Mix) Small molecular drug D0K3EW
Alprenolol Small molecular drug DB00866
Aprindine Small molecular drug DB01429
Azimilide Small molecular drug DB04957
Bevantolol Small molecular drug DB01295
Bicifadine Small molecular drug DB04889
Bis-(5-pyridin-3-yl-thiophen-2-ylmethyl)-amine Small molecular drug D0M0IQ
Bms-694153 Small molecular drug D05MSG
Bopindolol Small molecular drug DB08807
Bs 7581 Small molecular drug D0SE3C
Bs 7840 Small molecular drug D0J9SO
Bs 9106 Small molecular drug D0ZZ2L
Bupranolol Small molecular drug DB08808
Dapoxetine Small molecular drug DB04884
Deramciclane Small molecular drug DB06512
Desethyl Isoquine Small molecular drug D0IM5E
Dihydrocubebin Small molecular drug D00TOF
Gb-12819 Small molecular drug D0C4XQ
Gbr 12530 Small molecular drug D0X4DE
Gbr-12289 Small molecular drug D0G8KT
Gnf-pf-2094 Small molecular drug D0ZY7X
Gnf-pf-4292 Small molecular drug D0FQ1Z
Gnf-pf-5411 Small molecular drug D05ROV
Go-y022 Small molecular drug D0IO0I
Ici-199441 Small molecular drug D03SAV
Kaempferol-3-o-methyl Ether Small molecular drug D0S6NP
Mequitazine Small molecular drug DB01071
Methyl-(5-pyridin-3-yl-thiophen-2-yl)-amine Small molecular drug D01ARE
Mibefradil Small molecular drug DB01388
Ml-3163 Small molecular drug D08DSJ
Nabiximols Small molecular drug DB14011
Perospirone Small molecular drug DB08922
Prodipine Small molecular drug D0P2DU
Quercetin Small molecular drug DB04216
Repinotan Small molecular drug DB06506
Resveratrol Small molecular drug DB02709
Rhein Small molecular drug DB13174
Ritanserin Small molecular drug DB12693
Sb-210313 Small molecular drug D00XOQ
Tesmilifene Small molecular drug DB04905
2-(2-(4-tert-butylphenylthio)Ethyl)-1h-imidazole . D01JXM
Arotinolol . DB09204
Befunolol . DB09013
Curcumin Sulfate . DB14635
Esmirtazapine . DB06678
Medical Cannabis . DB14009
Melperone . DB09224
Propacetamol . DB09288
Discontinued
Click To Hide/Show 7 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
4-methoxyamphetamine Small molecular drug DB01472
Ethylmorphine Small molecular drug DB01466
Lysergic Acid Diethylamide Small molecular drug DB04829
Midomafetamine Small molecular drug DB01454
Phenacetin Small molecular drug DB03783
5-methoxy-nn-dimethyltryptamine . DB14010
Butyrfentanyl . DB09173

References

1 Cyclopropenone, Cyclopropeniminium Ion, and Cyclopropenethione as Novel Electrophilic Warheads for Potential Target Discovery of Triple-Negative Breast Cancer. J Med Chem. 2023 Feb 23;66(4):2851-2864. doi: 10.1021/acs.jmedchem.2c01889. Epub 2023 Feb 10.