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ChEMBL_787405 (CHEMBL1919284) Displacement of [3H]BMS-599240 from recombinant human BACE-1 ChEMBL_575802 (CHEMBL1057726) Binding affinity to BACE assessed as displacement of [3H]BMS-599240 ChEMBL_873597 (CHEMBL2187886) Displacement of [3H]BMS-599240 from BACE1 expressed in HEK293 cells ChEMBL_2362669 Inhibition of wild type human BCR-ABL1 using Tyr2 peptide as substrate incubated for 1 hrs in presence of dasatinib by FRET based Z-LYTE assay ChEMBL_1904780 (CHEMBL4407138) Displacement of [3H]BMS-986120 from His-tagged human PAR4 expressed in HEK293 cell membranes ChEMBL_775085 (CHEMBL1912344) Displacement of [3H]BMS-725519 from rat brain CB1 receptor after 90 mins by scintillation counting ChEMBL_1722333 (CHEMBL4137333) Inhibition of [3H]BMS-488043 binding to HIV-1 JRFL gp120 after 1 hr by scintillation counting method ChEMBL_1904779 (CHEMBL4407137) Displacement of [3H]BMS-986120 from His-tagged human PAR4 expressed in HEK293 cell membranes measured after 2 hrs ChEMBL_775084 (CHEMBL1912343) Displacement of [3H]BMS-725519 from human CB1 receptor expressed in CHO cells after 90 mins by scintillation counting ChEMBL_1523398 (CHEMBL3630425) Displacement of [3H]BMS-599240 from BACE1 (unknown origin) expressed in HEK293 cells at pH 5 after 1.5 hrs by Microbeta liquid scintillation counting analysis ChEMBL_1523399 (CHEMBL3630426) Displacement of [3H]BMS-599240 from BACE1 (unknown origin) expressed in HEK293 cells at pH 6.4 after 1.5 hrs by Microbeta liquid scintillation counting analysis Inhibition of SIK; Abl and Src Kinases by Other Kinase Inhibitor The IC50 for the inhibition of ABL1 by dasatinib, by C7 and by B3 is approximately 1.5 nM, 5.1 nM and 1.6 nM, and of SRC is 1.5 nM, 1.5 nM and 1.5 nM; each, respectively for dasatinib, C7 and by B3 (Table 3A). The compound C12 is also a strong inhibitor of SRC (<100 nM IC50), and is selective to SRC over ABL1. Briefly, a radiometric protein kinase assay (33PanQinase Activity Assay) was used for measuring the kinase activity of the five protein kinases. All kinase assays were performed in 96-well FlashPlates™ from PerkinElmer (Boston, MA, USA) in a 50 uL reaction volume. The reaction cocktail was pipetted in four steps in the following order:25 uL of assay buffer (standard buffer/[gamma-33P]-ATP)10 uL of ATP solution (in water)5 uL of test compound (in 10% DMSO)20 uL enzyme/substrate mix. The assay for all protein kinases contained 70 mM HEPES-NaOH pH7.5, 3 mM MgCl2, 3 mM MnCl2, 3 μM Na-orthovanadate, 1.2 mM DTT, ATP (variable concentrations, corresponding to the apparent ATP-Km of the respective kinase, see Table 2A), [gamma-33P]-ATP (approx. 8 105 cpm per well), protein kinase (variable amount, see Table 2A), and substrate (variable amounts, see Table 2A). hPD-1/hPD-L1 binding assay A negative control, a positive control and drug administration groups were set up, with two duplicate wells in each group. For the positive control group, added 2 μL diluent to a 96-well plate; 4 μL of PD-L1 and 4 uL of PD-1 as diluted according to the instructions; for the negative control group, added 6 μL diluent and 4 μL PD-L1 to a 96-well plate; for the administration group, 2 μL of the compound of the invention (or the positive compound BMS-202), 4 μL of PD-L1 and 4 μL of PD-1 were successively added to a 96-well plate. Sealed the plate with a sealing film, centrifuged at 1000 rpm for 1 minute, and incubated at room temperature for 15 minutes. Then mixed equal volumes of Anti-Tag-Eu3+ and Anti-tag-XL665 as diluted in buffer evenly, then added 10 μL of the mixture to each well, sealed the plate, centrifuged at 1000 rpm for 1 minute, and incubated at room temperature for 2 hours. Removed the sealing film, used EnVision to read the fluorescence intensity at 665 nm and 615 nm, and calculate ratio=Signal 665 nm/Signal 620 nm×104. IC50 of the compounds was calculated using Graphpad. In this experiment, BMS-202 in the patent WO2015034820 of BMS Company was selected as the positive drug. End Point Fluorescence Assay Reaction volumes of 50 μL were used in 96-well plates. Buffer A (1×, 34 μL; 100 mM Tris, pH 8, 10 mM MgCl2) was added to a single row, followed by 15 μL ofenzyme (3.3× concentration) in buffer A with 3-fold dilutions (typically, 125 nM and 42, 14, 4.6, 1.5, 0.5, 0.17, 0.06, 0.02, 0.01, and 0 μM final well concentrations in buffer A). Then, 1 μL of a 500 nM stock of the appropriate dasatinib analogue BODIPY probe in DMSO was added (2% DMSO final). Wells were incubated at rt for 30 min prior to end point read (ex/em 485/535 nm). Reactions had final concentrations of 10 nM BODIPY-probe, 100 mM Tris buffer (pH 8),and 10 mM MgCl2. Cell-Based Assays of c-Kit Mutant Kinase Activity The c-Kit mutant D816V inhibitors were assessed using an engineered BaF3-FL KIT D816V or BaF3-FL KIT V560G/D816V cell line. The BaF3-FL KIT D816V cell lines were created by introduction of KIT mutant (D816V) full length constructs that render the cells dependent on the introduced kinase for growth. Inhibitors of c-Kit mutant D816V kinase reduce or eliminate the mediated c-kit mutant D816V kinase activation, resulting in reduced cell proliferation of the BaF3-FL Kit mutant D816V cells. This inhibition is measured by the effect of compound concentration on cell growth to assess IC50 values. BaF3-FL KIT D816V cells were seeded at 1×104 cells per well of a 96 well cell culture plate in 50 μl of cell culture medium of RPMI Medium 1× (Invitrogen #11875-093) supplemented with 10% FBS (Invitrogen #10438), 1% Non Essential Amino Acids (Invitrogen #11140), 1% Penicillin Streptomycin (Invitrogen #15140), 1% L-Glutamine (Invitrogen #25030-081). Compounds were dissolved in DMSO at a concentration of 5 mM and were serially diluted 1:3 for a total of eight points and added to the cells to a final maximum concentration of 10 μM in 100 μl cell culture medium (final concentration 0.2% DMSO). Cells were also treated with Dasatinib as a positive control. The cells were incubated at 37° C., 5% CO2 for three days. ATPlite Buffer (Perkin Elmer #6016739) and substrate were equilibrated to room temperature, and enzyme/substrate Recombinant Firefly Luciferase/D-Luciferin was reconstituted. The cell plates were equilibrated to room temperature for 30 minutes, then lysed by addition of 25 uL per well of the ATPlite Reagent. The plate was mixed for 5 minutes on a plate shaker to lyse the cells. The plates were read on a Tecan Safire using Luminescence protocol modified to read 0.1s per well. The luminescence reading assesses the ATP content, which correlates directly with cell number such that the reading as a function of compound concentration is used to determine the IC50 value. Automated Whole-Cell Patch Clamp Assay Cell Culture and PreparationFisher rat thyroid (FRT) cells stably expressing human TMEM16A (TMEM16Aabc variant; Dr Luis Galietta, Insituto Giannina, Italy) were cultured in T-75 flasks in Hams F-12 media with Coon's modification (Sigma) supplemented with 10% (v/v) foetal bovine serum, penicillin-streptomycin (10,000 U/mL/10000 pg/mL), G-418 (750 pg/mL), L-glutamine (2 mM) and sodium bicarbonate solution (7.5% v/v). At −90% confluence cells were harvested for experiments by detachment with a 2:1 (v/v) mixture of Detachin (BMS Biotechnology) and 0.25% (w/v) trypsin-EDTA. Cells were diluted to a density of 3.5-4.5×106 cells/mL with media consisting of CHO-S-SFM (Sigma), 25 mM HEPES (Sigma) and Soy bean trypsin inhibitor (Sigma).Whole-Cell Patch Clamp RecordingFRT-TMEM16A cells were whole-cell patch clamped using an automated planar patch clamp system (Qpatch, Sophion). Briefly, once high resistance (GOhm) seals were established between the cells and the planar recording array the patch was ruptured using suction pulses to establish the whole-cell recording configuration of the patch clamp technique. The assay employed the following solutions (all reagents Sigma): Intracellular solution (mM): N-methyl-D-glucamine 130, CaCh 18.2, MgCh 1. HEPES 10, EGTA 10, BAPTA 20, Mg-ATP 2, pH 7.25, 325 mOsm with sucrose.Extracellular solution (mM): N-methyl-D-glucamine 130, CaCl2 2, MgCh 1, HEPES 10, pH 7.3, 320 mOsm with sucrose.The intracellular solution buffers intracellular calcium at levels required to give −20% activation of the maximal TMEM16A mediated current (EC20 for calcium ions). Cells were voltage clamped at a holding potential of −70 mV and a combined voltage step (to +70 mV)/ramp (−90 my to +90 mV) was applied at 0.05 Hz. After a period of current stabilisation test compounds, solubilised in 100% (v/v) DMSO and subsequently diluted into extracellular solution, were applied to generate a cumulative concentration response curve. Each concentration of test compound was incubated for 5 minutes before addition of the next concentration. After the final concentration was tested a supramaximal concentration of either a known active positive modulator or the TMEM16A inhibitor. CaCCinhAOI (Del La Fuente et al, 2008) was added to define the upper and lower limits of the assay.Compound activity was quantified by measuring the increase in current upon compound addition and expressing this as a percentage increase of baseline TMEM16A current level. Percentage increases in current were determined for each concentration and the data plotted as a function of concentration using either the Qpatch software or Graphpad Prism v6.05 providing the concentration which gave 50% of its maximal effect (EC50) and maximum efficacy (percentage of baseline increase). Automated Electrophysiology (Barra) Ion Works Barracuda population patch clamp (PPC). PPC measurements were performed using an IonWorks Barracuda instrument (Molecular Devices Corporation, Union City, Calif.) using either PatchPlate PPC substrates (Molecular Devices Corporation) with 64 apertures per well. The ability to average currents from 64 recordings from each well greatly improves data consistency and recording success rates in the measurement of NaV1.7 mediated ionic currents. Calculated leak current was digitally subtracted from the total cell NaV1.7 current for each sample point acquired.NaV1.7 currents were elicited by a voltage clamp protocol designed to bias the NaV1.7 channels to their inactivated state as follows. From holding potential of −60 mV cells were briefly hyperpolarized to −100 mV for 1.25 sec, then stepped to −20 mV for 20 sec to inactivate the channels. This was followed by a relatively brief hyperpolarization to −100 mv for 300 ms, then a 20 msec test pulse to −20 mV to elicit the NaV1.7 current used to measure the pharmacology of all test compounds. Compounds were incubated for 600 sec between the pre- and post-compound reads. The external recording solution used was (in mM) 137 NaCl, 4 KCl, 1 MgCl2, 1.8 CaCl2, 10 Hepes, 10 glucose, pH to 7.4 with NaOH, and the internal solution used was (in mM) 100 K-gluconate, 40 KCl, 3.2 zMgCl2, 5 EGTA, 10 HEPES pH to 7.2 with KOH. The same solutions were used to record NaV1.5 currents, with the following voltage clamp protocol. NaV1.5 currents were elicited by a voltage clamp protocol designed to bias the NaV1.5 channels to their inactivated state as follows. From holding potential of −40 mV cells were briefly hyperpolarized to −100 mV for 300 ms, then stepped to −10 mV for 20 sec to inactivate the channels. This was followed by a relatively brief hyperpolarization to −100 mv for 30 ms, then a 20 msec test pulse to −10 mV to elicit the NaV1.5 current used to measure the pharmacology of all test compounds. HEK 293 cells expressing NaV1.7 and NaV1.5 channels, were used (Essen Biosciences, Ann Arbor, Mich.). Cells were cultured in T-175 flasks and passaged every 2 to 3 days at 1:3 to 1:6 seeding density dilutions. Cells were grown to 70% to 90% confluence in a flask and removed from the incubator (37° C., 5% CO2) 1 to 3 days after plating. Growth medium was aspirated from the culture flasks. Cells were gently rinsed with 10 ml of PBS (Catalog number: 14190144, Gibco) to remove residual media. Next a total of 2 mL TrypLE (Gibco) solution was added, and the flasks containing cells were sat for 3 min at RT, after which, the cells became visibly rounded and were easily dislodged from the bottom of the flask with a few brief taps on a solid surface. A total of 8 mL of media was added to the flask to inactivate the TrypLE, and the mixture was centrifuged at 910 rpm for 4 min. The cell supernatant was decanted, and the cell pellets were resuspended in 5-6 mL of external solution followed by gentle triturations using a 10 ml pipette, and transferred to a 15 ml conical tube and immediately brought to the IW Barracuda instrument. The cell suspension had a final concentration of 2 to 3 million cells per ml; this corresponds to 10,000 cells added per well.Peak membrane currents were analyzed with IW Barracuda software and exported to Excel for further analysis. Concentration response curve fitting was performed with BMS in-house software. IC50 values were obtained by fits of the Hill equation to the average percent inhibition data plotted versus compound concentration. Concentration-response curves for all test compounds were fitted to a 4-parameter equation: % of control=100 (1+([drug]/IC50)p)−1, where IC50 is the concentration of drug required to inhibit current by 50% and p is the Hill slope.
DASATINIB BDBM31089
Dasatinib BDBM82130
BMS 708163 BMS-70816301 BMS-708163 BMS-708163-01 Avagacestat BDBM50458169
BDBM50578294 Bms 813160 Bms-813160
med.21724, Compound Dasatinib US20230348453, Compound A8 US10294227, Code Dasatinib BDBM13216 BMS-354825 CHEMBL1421 DASATINIB cid_3062316 N-(2-Chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1-piperazinyl)]-2-methyl-4-pyrimidinyl]amino)]-1,3-thiazole-5-carboxamide N-(2-chloro-6-methylphenyl)-2-({6-[4-(2-hydroxyethyl)piperazin-1-yl]-2-methylpyrimidin-4-yl}amino)-1,3-thiazole-5-carboxamide
BMS 650032 BMS-650032 Asunaprevir BDBM50287594
BDBM35316 BMS-344577
BDBM50409914 BMS-191095
BDBM50507371 BMS-823778
BDBM50541922 Bms-986251
BDBM50558765 Bms-986104
BDBM50563973 Bms-986166
BDBM50633961 Bms-986299
BMS-911543 BDBM50122318
Bms-986278 BDBM50581552
BDBM50564768 NSC-747973 Ixempra kit BMS 247550-01 BMS-247550-01 Ixempra BMS-247550 CHEBI:63605 Azaepothilone b Ixabepilone
BDBM50217824 CHEMBL70738 BMS-363130
BDBM50353371 BMS-345541 CHEMBL471496
BDBM50387084 BMS-790052 DACLATASVIR
BDBM50449917 CHEMBL2021417 BMS-180560
BDBM50449918 CHEMBL2021416 BMS-181688
BMS-180291 BDBM50212318 Ifetroban
BMS-189090 CHEMBL138877 BDBM50366780
BMS-204493 CHEMBL472172 BDBM50447840
BMS-262084 CHEMBL71037 BDBM50220841
BMS-564929 CHEMBL229264 BDBM50598597
BMS-582664 CHEMBL408444 BDBM50371876
BMS-626529 BDBM50236759 Temsavir
BMS-645737 CHEMBL261592 BDBM50377352
BMS-817693 CHEMBL2333637 BDBM50428760
Beclabuvir BDBM50448498 BMS-791325
CHEMBL243876 BMS-433771 BDBM50088178
CHEMBL247361 BMS-433796 BDBM50477516
CHEMBL247471 BMS-299897 BDBM50477339
CHEMBL401068 BDBM50487722 BMS-201620
Liafensine BDBM50459930 BMS-820836
Hetlioz BMS-214778 BMS-214,778 BDBM50621041 Hetlioz lq CHEBI:79042 TASIMELTEON VEC-162
BDBM31889 BMS 961 BMS270394 BMS961
BMS-204352 BDBM50426567 FLINDOKALNER MaxiPost
Bms-955176 GSK-3532795 BDBM50450015
Bms-986205 F 001287 BMS 986205 F-001287 BDBM50590772 LINRODOSTAT ONO-7701 ONO 7701
US11578058, Compound Reference (BMS-986165) US11021475, Example 67 US11731956, Example control US20240246944, Control (BMS-986165) BDBM500288 US11021475, Example 52 US20240101548, Compound BMS-986165
BDBM50008057 CHEBI:64153 BMS-722782 TANESPIMYCIN
BDBM50011476 ER-30346 RAVUCONAZOLE BMS-207147
BDBM50507816 Deucravacitinib US12351572, Example control Bms-986165
BMS-245782 CHEMBL189548 BDBM50156330 N-arylpiperazine derivative
BMS-665139 oxazolidin-2-imine, 6c BDBM29320
BMS-908662 BDBM50457451 EXEL-2819 XL-281
Bms-986020 AP-3152 FREE ACID BDBM50581550
Baraclude Entecavir BDBM50248008 CHEBI:473990 BMS-200475-01 SQ-34676
BDBM50299148 BMS-754807 CHEMBL575448 1-{4-[(3-cyclopropyl-1H-pyrazol-5-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl}-N-(6-fluoropyridin-3-yl)-2-methyl-L-prolinamide (S)-1-(4-(5-cyclopropyl-1H-pyrazol-3-ylamino)pyrrolo[1,2-f][1,2,4]triazin-2-yl)-N-(6-fluoropyridin-3-yl)-2-methylpyrrolidine-2-carboxamide
BDBM50108168 CHEMBL76222 Rebimastat 2-[2-Mercapto-4-(3,4,4-trimethyl-2,5-dioxo-imidazolidin-1-yl)-butyrylamino]-4-methyl-pentanoic acid (2,2-dimethyl-1-methylcarbamoyl-propyl)-amide(BMS-275291) BMS-275291
N-[3-(2,3-Dihydro-benzofuran-4-yl)-2,2-dimethyl-cyclopropanecarbonyl]-guanidine (BMS-284640) BMS-284640 CHEMBL51879 BDBM50104844 N-[(1R,3R)-3-(2,3-Dihydro-benzofuran-4-yl)-2,2-dimethyl-cyclopropanecarbonyl]-guanidine
US20240327387, Compound BMS202 US20240043392, Compound BMS-202 CHEMBL4089730 US20230303494, Compound BMS202 US9872852, Example 202 BDBM50239947
CHEMBL106684 2'-Amino-4'-isobutyl-biphenyl-2-sulfonic acid (3,4-dimethyl-isoxazol-5-yl)-amide (BMS 187308) 2'-Amino-4'-isobutyl-biphenyl-2-sulfonic acid (3,4-dimethyl-isoxazol-5-yl)-amide BMS-187308 BDBM50068674
3,5-dichloro-2-hydroxy-N-(4-methoxy-biphenyl-3-yl)-benzenesulfonamide CHEMBL399379 BDBM50209010 US20240398737, Compound BMS-303141
BDBM16178 BMS-214662 3-benzyl-1-(1H-imidazol-5-ylmethyl)-4-(thiophen-2-ylsulfonyl)-2,3,4,5-tetrahydro-1H-1,4-benzodiazepine-7-carbonitrile 3-benzyl-1-(1H-imidazol-5-ylmethyl)-4-(thiophene-2-sulfonyl)-2,3,4,5-tetrahydro-1H-1,4-benzodiazepine-7-carbonitrile BMS 214662
BMS-377806 4-Benzoyl-1-[(4-methoxy-1Hpyrrolo[2,3-b]pyridin-3-yl)oxoacetyl]-2-(R)-methylpiperazine BMS-378806 1-((R)-4-Benzoyl-2-methyl-piperazin-1-yl)-2-(4-methoxy-1H-pyrrolo[2,3-b]pyridin-3-yl)-ethane-1,2-dione CHEMBL337301 (R)-1-(4-benzoyl-2-methylpiperazin-1-yl)-2-(4-methoxy-1H-pyrrolo[2,3-b]pyridin-3-yl)ethane-1,2-dione BDBM50133282 BMS-806
BDBM13259 N-(2,6-dimethylphenyl)-2-(pyridin-2-ylamino)-1,3-thiazole-5-carboxamide BMS-354825 2-Heteroarylamino-thiazole Analog 12d
BDBM13262 BMS-354825 2-Heteroarylamino-thiazole Analog 12g N-(2,6-dimethylphenyl)-2-(pyridazin-3-ylamino)-1,3-thiazole-5-carboxamide
BMS-354825 2-Heteroarylamino-thiazole Analog 12i 2-(pyrazin-2-ylamino)-N-(2,4,6-trimethylphenyl)-1,3-thiazole-5-carboxamide BDBM13264
5-Dimethylamino-naphthalene-1-sulfonic acid (3,4-dimethyl-isoxazol-5-yl)-amide 5-Dimethylamino-naphthalene-1-sulfonic acid (3,4-dimethyl-isoxazol-5-yl)-amide (BMS 182874) BDBM50034435 CHEMBL267458 BMS-182874 5-Dimethylamino-naphthalene-1-sulfonic acid (3,4-dimethyl-2,3-dihydro-oxazol-5-yl)-amide
2-acetamido-4-methyl-N-(2,4,6-trimethylphenyl)-1,3-thiazole-5-carboxamide BMS-354825 2-Amino-4-methyl-thiazole Analog 7c BDBM13223
BDBM13261 BMS-354825 2-Heteroarylamino-thiazole Analog 12f N-(2-chloro-6-methylphenyl)-2-(pyridazin-3-ylamino)-1,3-thiazole-5-carboxamide
BDBM13270 2-[(2,6-dimethylpyrimidin-4-yl)amino]-N-(2,4,6-trimethylphenyl)-1,3-thiazole-5-carboxamide BMS-354825 2-Heteroarylamino-thiazole Analog 12o
BMS-687453 BDBM28800 2-{[(3-{[2-(4-chlorophenyl)-5-methyl-1,3-oxazol-4-yl]methoxy}phenyl)methyl](methoxycarbonyl)amino}acetic acid
BMS345541 BMS-345541 CHEMBL471496 N-(2-aminoethyl)-3,12-dimethyl-2,5,8-triazatricyclo[7.4.0.0^{2,6}]trideca-1(13),3,5,7,9,11-hexaen-7-amine BDBM25919
N-[2'-(3,4-Dimethyl-isoxazol-5-ylsulfamoyl)-4-oxazol-2-yl-biphenyl-2-ylmethyl]-3,3-dimethyl-butyramide CHEMBL277447 BDBM50140757 BMS-207940
pyrazolo[3,4-b]pyridine deriv. BDBM5776 4-butoxy-5-[(2,6-difluoro-4-methylphenyl)carbonyl]-1H-pyrazolo[3,4-b]pyridine BMS-265246
2-{[(5-{[2-(4-chlorophenyl)-5-methyl-1,3-oxazol-4-yl]methoxy}-2-fluorophenyl)methyl](methoxycarbonyl)amino}acetic acid BDBM28802 BMS-711939
4-methyl-2-[(phenylcarbamoyl)amino]-N-(2,4,6-trimethylphenyl)-1,3-thiazole-5-carboxamide BMS-354825 2-Amino-4-methyl-thiazole Analog 8b BDBM13241
BDBM185148 (3R,4R)-4-amino-1-[[4-(3-methoxyanilino)pyrrolo[2,1-f][1,2,4]triazin-5-yl]methyl]piperidin-3-ol BMS-690514
BDBM50228465 CHEMBL238103 1-(4-benzoylpiperazin-1-yl)-2-(4,7-dimethoxy-1H-pyrrolo[2,3-c]pyridin-3-yl)ethane-1,2-dione BMS-488043
BMS-180291 3-{2-[3-(4-Pentylcarbamoyl-oxazol-2-yl)-7-oxa-bicyclo[2.2.1]hept-2-ylmethyl]-phenyl}-propionic acid CHEMBL283100 BDBM50047274
BMS-185367 CHEMBL136082 (S)-1-[(S)-3-Hydroxy-2-(naphthalene-2-sulfonylamino)-propionyl]-pyrrolidine-2-carboxylic acid (4-guanidino-butyl)-amide BDBM50107438
CHEMBL132448 BMS-354825 tert-Butoxycarbamate Analog 5e BDBM13221 tert-butyl N-{5-[(2,6-dichlorophenyl)carbamoyl]-4-methyl-1,3-thiazol-2-yl}carbamate
CHEMBL356065 (S)-1-((R)-2-Methanesulfonylamino-3-phenyl-propionyl)-pyrrolidine-2-carboxylic acid (1-carbamimidoyl-piperidin-4-ylmethyl)-amide BDBM50107463 BMS-189664
N-(2-chloro-6-methylphenyl)-2-(pyridin-2-ylamino)-1,3-thiazole-5-carboxamide BMS-354825 2-Heteroarylamino-thiazole Analog 12a BDBM13256 CHEMBL189776
BMS-564929 4-[(7R,7aS)-7-hydroxy-1,3-dioxo-hexahydro-1H-pyrrolo[1,2-a]imidazolidin-2-yl]-2-chloro-3-methylbenzonitrile BDBM18173 CHEMBL229264
(2-Chloro-6-methyl-phenyl)-[8-((S)-3-methyl-piperazin-1-yl)-2,5,9,9b-tetraaza-cyclopenta[a]naphthalen-4-yl]-amine BDBM50151366 CHEMBL189338 BMS-279700
2-N-benzene-4-methyl-5-N-(2,4,6-trimethylphenyl)-1,3-thiazole-2,5-diamido CHEMBL130719 BMS-354825 2-Amino-4-methyl-thiazole Analog 7d BDBM13224
5-N-(2-chloro-6-methylphenyl)-2-N-(2-methylcyclopropane)-1,3-thiazole-2,5-diamido BDBM13249 BMS-354825 2-Carboxamido-4-hydrido-thiazole Analog 7q
BDBM13248 5-N-(2-chloro-6-methylphenyl)-2-N-(1-methylcyclopropane)-1,3-thiazole-2,5-diamido BMS-354825 2-Carboxamido-4-hydrido-thiazole Analog 7p
N-(2-chloro-6-methylphenyl)-2-[(4,6-dimethylpyrimidin-2-yl)amino]-1,3-thiazole-5-carboxamide BDBM13269 BMS-354825 2-Heteroarylamino-thiazole Analog 12n CHEMBL186564
BMS-337197 BDBM50113230 CHEMBL64830 N-{2-[2-(3-Methoxy-4-oxazol-5-yl-phenylamino)-oxazol-5-yl]-phenyl}-N-methyl-2-morpholin-4-yl-acetamide
BMS-777607 BDBM28031 N-{4-[(2-amino-3-chloropyridin-4-yl)oxy]-3-fluorophenyl}-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide
CHEMBL489100 (R)-2-((R)-3-amino-3-(4-((2-methylquinolin-4-yl)methoxy)phenyl)-2-oxopyrrolidin-1-yl)-N-hydroxy-4-methylpentanamide BDBM50247606 BMS-561392
(2S,3R)-4-Oxo-1-[4-(6-phenyl-hexanoyl)-piperazine-1-carbonyl]-3-(2-piperidin-3-yl-ethyl)-azetidine-2-carboxylic acid BMS-354326 BDBM50144532 CHEMBL306448
BDBM50164025 BMS-316810 CHEMBL360330 Pyridine-2-sulfonic acid [6-cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinolin-3-yl]-thiophen-3-ylmethyl-amide
(2S,3S)-7-Amino-3-{[(S)-1-((R)-2-amino-3-phenyl-propionyl)-pyrrolidine-2-carbonyl]-amino}-2-hydroxy-heptanoic acid methyl ester BDBM50280253 CHEMBL41426 BMS-181316
Dapagliflozin BDBM20880 CHEMBL429910 (2S,3R,4R,5S,6R)-2-{4-chloro-3-[(4-ethoxyphenyl)methyl]phenyl}-6-(hydroxymethyl)oxane-3,4,5-triol C-aryl glucoside, 6 BMS-512148
N''-cyano-N-(4-cyanophenyl)-N'-(1,2,2-trimethylpropyl)guanidine (BMS-182264) N''-cyano-N-(4-cyanophenyl)-N'-(1,2,2-trimethylpropyl)guanidine 4-cyanoimino(1,2,2-trimethylpropylamino)methylaminobenzonitrile CHEMBL19169 BDBM50062396
4-[3-(3-{3-[4-(2-Methoxy-phenyl)-piperazin-1-yl]-propyl}-ureido)-phenyl]-2,6-dimethyl-1,4-dihydro-pyridine-3,5-dicarboxylic acid dimethyl ester BDBM50109185 BMS-189323 CHEMBL124152
4-[3-(3-{3-[4-(3-Methoxy-phenyl)-piperidin-1-yl]-propyl}-ureido)-phenyl]-2,6-dimethyl-1,4-dihydro-pyridine-3,5-dicarboxylic acid dimethyl ester BMS-193885 BDBM50109122 CHEMBL324554
Aminobenzisoxazole 2g BMS-740808 Analogue 15 BDBM12688 1-(3-amino-1,2-benzoxazol-5-yl)-N-(4-{2-[(dimethylamino)methyl]phenyl}-2-fluorophenyl)-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
BDBM50280255 BMS-181412 CHEMBL539241 7-Amino-3-{[(S)-1-((R)-2-amino-3-phenyl-propionyl)-pyrrolidine-2-carbonyl]-amino}-2-hydroxy-2-methoxy-heptanoic acid methyl ester; dihydrochloride
BMS-181162 3-[(1E,3E,5E)-1-((E)-2-Carboxy-1-methyl-vinyl)-4-methyl-6-(2,6,6-trimethyl-cyclohex-1-enyl)-hexa-1,3,5-trienyl]-benzoic acid CHEMBL313583 BDBM50288286
N-{2-[6-(4-ethylpiperazin-1-yl)pyridin-3-yl]propan-2-yl}-2-fluoro-9-oxo-9,10-dihydroacridine-3-carboxamide Acridone-Based Inhibitor, 4m BDBM19289 BMS-566419
BDBM50280254 (S)-3-{[(S)-1-((R)-2-Amino-3-phenyl-propionyl)-pyrrolidine-2-carbonyl]-amino}-7-guanidino-2-hydroxy-heptanoic acid methyl ester with di TFA BMS-182060 CHEMBL290162
BMS-205603-01 Lamivudine impurity e SQ-7726 NSC-3970 BDBM50549809 CHEBI:17568 Fluorouracil specified compound c Hybar x SQ-8493 Lamivudine impurity e rs SQ-6201 Uracil Pyrod
BMS-317180 BDBM21941 Tetrazole-based compound, 2 2-{5-[(1S)-1-(2-amino-2-methylpropanamido)-2-(benzyloxy)ethyl]-1H-1,2,3,4-tetrazol-1-yl}ethyl N-(4-hydroxybutyl)carbamate CHEMBL398372
(S)-N2,N2-dimethyl-N5-((2-methylbenzofuran-5-ylamino)(2-oxo-1-(2-oxo-2-(pyrrolidin-1-yl)ethyl)azepan-3-ylamino)methylene)pyridine-2,5-dicarboxamide BDBM50328724 CHEMBL570867 BMS-344577
BDBM13260 2-(pyridin-2-ylamino)-N-(2,4,6-trimethylphenyl)-1,3-thiazole-5-carboxamide BMS-354825 2-Heteroarylamino-thiazole Analog 12e N-(2,4,6-Trimethylphenyl)-2-[(2-pyridinyl)amino]-1,3-thiazole-5-carboxamide
BDBM27879 CHEMBL401930 4-{[(2S)-2-(3-chlorophenyl)-2-hydroxyethyl]amino}-3-[4-methyl-6-(morpholin-4-yl)-1H-1,3-benzodiazol-2-yl]-1,2-dihydropyridin-2-one US10710978, Compound BMS536924 BMS-536924
CHEMBL1094165 (S)-4-(2-(3-chlorophenyl)-2-hydroxyethylamino)-3-(6-(4-(2-methoxyethyl)piperazin-1-yl)-4-methyl-1H-benzo[d]imidazol-2-yl)pyridin-2(1H)-one BDBM50318112 BMS-577098
CHEMBL231779 BMS-562247 Apixaban 1-(4-methoxyphenyl)-7-oxo-6-[4-(2-oxopiperidin-1-yl)phenyl]-1H,4H,5H,6H,7H-pyrazolo[3,4-c]pyridine-3-carboxamide US9938272, Example Apixaban BDBM19023
1-(3-amino-1,2-benzoxazol-5-yl)-6-(4-{2-[(dimethylamino)methyl]phenyl}phenyl)-3-methyl-1H,4H,5H,6H,7H-pyrazolo[3,4-c]pyridin-7-one BDBM12701 BMS-740808 Analogue 12a
2-aminothiazole deriv. BMS-357075 3-[({6-[(5-{[(5-tert-butyl-1,3-oxazol-2-yl)methyl]sulfanyl}-1,3-thiazol-2-yl)amino]pyridin-3-yl}methyl)amino]-2,2-dimethylpropan-1-ol BDBM5726
4-{[2-(4-chloro-1H-pyrazol-1-yl)ethyl]amino}-3-{6-[1-(3-fluoropropyl)piperidin-4-yl]-4-methyl-1H-1,3-benzodiazol-2-yl}-1,2-dihydropyridin-2-one BDBM27888 BMS-695735
BDBM687 BMS-186318 analog 24 tert-butyl N-[(2S,3R)-4-{[(2R,3S)-4-[4-(benzyloxy)phenyl]-3-{[(tert-butoxy)carbonyl]amino}-2-hydroxybutyl]amino}-3-hydroxy-1-phenylbutan-2-yl]carbamate
BMS-640994 (R)-2-(sec-butylamino)-N-(2-methyl-5-(methylcarbamoyl)phenyl)thiazole-5-carboxamide BDBM50236473 N-[2-methyl-5-(methylcarbamoyl)phenyl]-2-{[(1R)-1-methylpropyl]amino}-1,3-thiazole-5-carboxamide CHEMBL258202
BMS-740808 Analogue 6d 1-(3-amino-1,2-benzoxazol-5-yl)-6-(4-{2-[(methylamino)methyl]phenyl}phenyl)-3-(trifluoromethyl)-1H,4H,5H,6H,7H-pyrazolo[3,4-c]pyridin-7-one BDBM12691
CHEMBL564417 (S)-3-(4-(2-(4-(2-(2-chlorophenyl)-2-hydroxyethylamino)-2-oxo-1,2-dihydropyridin-3-yl)-7-methyl-1H-benzo[d]imidazol-5-yl)piperazin-1-yl)propanenitrile BMS-554417 BDBM50296350
tert-butyl N-[(2S,3R)-4-{[(2R,3S)-4-[3-(benzyloxy)phenyl]-3-{[(tert-butoxy)carbonyl]amino}-2-hydroxybutyl]amino}-3-hydroxy-1-phenylbutan-2-yl]carbamate BDBM688 BMS-186318 analog 25
1-(3-amino-1,2-benzoxazol-5-yl)-6-{4-[2-(piperazin-1-ylmethyl)phenyl]phenyl}-3-(trifluoromethyl)-1H,4H,5H,6H,7H-pyrazolo[3,4-c]pyridin-7-one BMS-740808 Analogue 6j BDBM12697
2-[[(tert-Butyloxy)carbonyl]-amino]-4-methyl-N-phenyl-1,3-thiazole-5-carboxamide tert-butyl N-[4-methyl-5-(phenylcarbamoyl)-1,3-thiazol-2-yl]carbamate BDBM13225 CHEMBL424450 BMS-354825 tert-Butoxycarbamate Analog 5f
BDBM12702 1-(3-amino-1,2-benzoxazol-5-yl)-3-methyl-6-{4-[2-(pyrrolidin-1-ylmethyl)phenyl]phenyl}-1H,4H,5H,6H,7H-pyrazolo[3,4-c]pyridin-7-one BMS-740808 Analogue 12b
BMS-740808 Analogue 6e 1-(3-amino-1,2-benzoxazol-5-yl)-6-{4-[2-(pyrrolidin-1-ylmethyl)phenyl]phenyl}-3-(trifluoromethyl)-1H,4H,5H,6H,7H-pyrazolo[3,4-c]pyridin-7-one BDBM12692
BMS-740808 Analogue 6i BDBM12696 1-(3-amino-1,2-benzoxazol-5-yl)-6-{4-[2-(morpholin-4-ylmethyl)phenyl]phenyl}-3-(trifluoromethyl)-1H,4H,5H,6H,7H-pyrazolo[3,4-c]pyridin-7-one
N-(2-Chloro-6-methylphenyl)-2-[(ethylcarbonyl)amino]-1,3-thiazole-5-carboxamide N-(2-chloro-6-methylphenyl)-2-propanamido-1,3-thiazole-5-carboxamide BDBM13247 BMS-354825 2-Carboxamido-4-hydrido-thiazole Analog 7o
N-[5-[[[5-(1,1-Dimethylethyl)-2-oxazolyl]methyl]thio]-2-thiazolyl]cyclohexanecarboxamide BDBM5927 BMS-387032 analog 17 N-(5-{[(5-tert-butyl-1,3-oxazol-2-yl)methyl]sulfanyl}-1,3-thiazol-2-yl)cyclohexanecarboxamide
1-(3-amino-1,2-benzoxazol-5-yl)-6-[4-(2-{[(3R)-3-hydroxypyrrolidin-1-yl]methyl}phenyl)phenyl]-3-(trifluoromethyl)-1H,4H,5H,6H,7H-pyrazolo[3,4-c]pyridin-7-one BDBM12693 BMS-740808
2-Cyclopropyl-3-[2'-(1H-tetrazol-5-yl)-biphenyl-4-ylmethoxy]-quinoline-4-carboxylic acid BMS-183920 BDBM50049201 CHEMBL305365 2-Cyclopropyl-3-[2'-(2H-tetrazol-5-yl)-biphenyl-4-yloxy]-quinoline-4-carboxylic acid
BDBM12690 1-(3-amino-1,2-benzoxazol-5-yl)-6-[4-(2-{[ethyl(methyl)amino]methyl}phenyl)phenyl]-3-(trifluoromethyl)-1H,4H,5H,6H,7H-pyrazolo[3,4-c]pyridin-7-one BMS-740808 Analogue 6c
BMS-186318 analog 28 BDBM691 tert-butyl N-[(2S,3R)-4-{[(2R,3S)-3-{[(tert-butoxy)carbonyl]amino}-2-hydroxy-4-[4-(4-methoxybutoxy)phenyl]butyl]amino}-3-hydroxy-1-phenylbutan-2-yl]carbamate
BMS-387032 analog 16 N-(5-{[(5-tert-butyl-1,3-oxazol-2-yl)methyl]sulfanyl}-1,3-thiazol-2-yl)-2-cyclohexylacetamide N-[5-[[[5-(1,1-Dimethylethyl)-2-oxazolyl]methyl]thio]-2-thiazolyl]cyclohexylmethanecarboxamide BDBM5926
BMS-740808 Analogue 17a 1-(3-amino-1,2-benzoxazol-5-yl)-7-(4-{2-[(dimethylamino)methyl]phenyl}phenyl)-3-(trifluoromethyl)-1H,6H,7H,8H-pyrazolo[3,4-c]azepin-8-one BDBM12685 bicyclic pyrazole scaffold
1-(3-amino-1,2-benzoxazol-5-yl)-6-{2-fluoro-4-[2-(pyrrolidin-1-ylmethyl)phenyl]phenyl}-3-(trifluoromethyl)-1H,4H,5H,6H,7H-pyrazolo[3,4-c]pyridin-7-one BDBM12699 BMS-740808 Analogue 7b
2-(3-furoylamino)-N-mesityl-4-methyl-1,3-thiazole-5-carboxamide 2-N-(furan-3-)-4-methyl-5-N-(2,4,6-trimethylphenyl)-1,3-thiazole-2,5-diamido BMS-354825 2-Amino-4-methyl-thiazole Analog 7g BDBM13233
BDBM12686 BMS-740808 Analogue 17b bicyclic pyrazole scaffold 1-(3-amino-1,2-benzoxazol-5-yl)-7-(4-{2-[(dimethylamino)methyl]phenyl}-2-fluorophenyl)-3-(trifluoromethyl)-1H,6H,7H,8H-pyrazolo[3,4-c]azepin-8-one
BDBM12689 bicyclic pyrazole scaffold 1-(3-amino-1,2-benzoxazol-5-yl)-6-(4-{2-[(diethylamino)methyl]phenyl}phenyl)-3-(trifluoromethyl)-1H,4H,5H,6H,7H-pyrazolo[3,4-c]pyridin-7-one BMS-740808 Analogue 6b
BDBM13229 tert-butyl N-{5-[(2,4-dimethylphenyl)carbamoyl]-4-methyl-1,3-thiazol-2-yl}carbamate BMS-354825 tert-Butoxycarbamate Analog 5j 2-[[(tert-Butyloxy)carbonyl]-amino]-4-methyl-N-(2,4-dimethylphenyl)-1,3-thiazole-5-carboxamide
BDBM13258 N-(2-chloro-6-methylphenyl)-2-(pyridin-4-ylamino)-1,3-thiazole-5-carboxamide N-(2-Chloro-6-methylphenyl)-2-[(4-pyridinyl)amino]-1,3-thiazole-5-carboxamide BMS-354825 2-Heteroarylamino-thiazole Analog 12c CHEMBL360810
BMS-186318 analog 27 tert-butyl N-[(2S,3R)-4-{[(2R,3S)-4-[4-(1,3-benzoxazol-2-ylmethoxy)phenyl]-3-{[(tert-butoxy)carbonyl]amino}-2-hydroxybutyl]amino}-3-hydroxy-1-phenylbutan-2-yl]carbamate BDBM690
BMS-354825 2-Amino-4-methyl-thiazole Analog 8e 2-[[(Benzylamino)carbonyl]-amino]-4-methyl-N-(2,4,6-trimethylphenyl)-1,3-thiazole-5-carboxamide 2-[(benzylcarbamoyl)amino]-4-methyl-N-(2,4,6-trimethylphenyl)-1,3-thiazole-5-carboxamide BDBM13244
BMS-354825 2-Carboxamido-4-hydrido-thiazole Analog 7v N-(2-Chloro-6-methylphenyl)-2-[(cyclobutylcarbonyl)amino]-1,3-thiazole-5-carboxamide 5-N-(2-chloro-6-methylphenyl)-2-N-cyclobutane-1,3-thiazole-2,5-diamido BDBM13254
BMS-477118 (1S,3S,5S)-2-[(2S)-2-amino-2-(3-hydroxyadamantan-1-yl)acetyl]-2-azabicyclo[3.1.0]hexane-3-carbonitrile; 2,2,2-trifluoroacetic acid BDBM11542 (S)-3-Hydroxyadamantylglycine-L-cis-4,5-methanoprolinenitrile TFA salt Saxagliptin
BMS-477118 analogue Saxagliptin Analogue 23 (S)-Adamantylglycine-L-cis-4,5-methanoprolinenitrile TFA salt (1S,3S,5S)-2-[(2S)-2-(adamantan-1-yl)-2-aminoacetyl]-2-azabicyclo[3.1.0]hexane-3-carbonitrile; 2,2,2-trifluoroacetic acid BDBM11541
BMS-740808 Analogue 6h 1-(3-amino-1,2-benzoxazol-5-yl)-6-(4-{2-[(4-hydroxypiperidin-1-yl)methyl]phenyl}phenyl)-3-(trifluoromethyl)-1H,4H,5H,6H,7H-pyrazolo[3,4-c]pyridin-7-one BDBM12695
BMS-740808 Analogue 6k 1-(3-amino-1,2-benzoxazol-5-yl)-6-(4-{2-[(4-methylpiperazin-1-yl)methyl]phenyl}phenyl)-3-(trifluoromethyl)-1H,4H,5H,6H,7H-pyrazolo[3,4-c]pyridin-7-one BDBM12698
N-(2-Chloro-6-methylphenyl)-2-[(3-pyridinyl)amino]-1,3-thiazole-5-carboxamide BDBM13257 CHEMBL189675 N-(2-chloro-6-methylphenyl)-2-(pyridin-3-ylamino)-1,3-thiazole-5-carboxamide BMS-354825 2-Heteroarylamino-thiazole Analog 12b
N-(2-Chloro-6-methylphenyl)-2-[(cyclopentylcarbonyl)amino]-1,3-thiazole-5-carboxamide 5-N-(2-chloro-6-methylphenyl)-2-N-cyclopentane-1,3-thiazole-2,5-diamido BMS-354825 2-Carboxamido-4-hydrido-thiazole Analog 7w BDBM13255
N-[5-((R)-2-{[Bis-(4-difluoromethoxy-phenyl)-methyl]-amino}-1-hydroxy-ethyl)-2-hydroxy-phenyl]-methanesulfonamide (R)-N-(5-(2-(bis(4-(difluoromethoxy)phenyl)methylamino)-1-hydroxyethyl)-2-hydroxyphenyl)methanesulfonamide CHEMBL320915 BMS-194449 BDBM50106794
sodium (3R,5S,6E)-7-[4-(4-fluorophenyl)-2-[methyl(1-methyl-1H-1,2,4-triazol-5-yl)amino]-6-(propan-2-yl)pyrimidin-5-yl]-3,5-dihydroxyhept-6-enoate BMS-644950 triazole compound, 1b BDBM22163
1-(3-amino-1,2-benzoxazol-5-yl)-6-(4-{2-[(dimethylamino)methyl]phenyl}-2-fluorophenyl)-3-(trifluoromethyl)-1H,4H,5H,6H,7H-pyrazolo[3,4-c]pyridin-7-one bicyclic pyrazole scaffold BMS-740808 Analogue 7a BDBM12682
1-(3-amino-1,2-benzoxazol-5-yl)-7-(4-{2-[(dimethylamino)methyl]phenyl}phenyl)-3-(trifluoromethyl)-1H,4H,5H,6H,7H,8H-pyrazolo[3,4-c]azepin-8-one BMS-740808 Analogue 16a BDBM12683 bicyclic pyrazole scaffolds
2-[[(Butylamino)-carbonyl]amino]-4-methyl-N-(2,4,6-trimethylphenyl)-1,3-thiazole-5-carboxamide CHEMBL131346 BMS-354825 2-Amino-4-methyl-thiazole Analog 8c 2-[(butylcarbamoyl)amino]-4-methyl-N-(2,4,6-trimethylphenyl)-1,3-thiazole-5-carboxamide BDBM13242
BDBM13240 4-methyl-2-[(methylcarbamoyl)amino]-N-(2,4,6-trimethylphenyl)-1,3-thiazole-5-carboxamide 2-[[(Methylamino)-carbonyl]amino]-4-methyl-N-(2,4,6-trimethylphenyl)-1,3-thiazole-5-carboxamide BMS-354825 2-Amino-4-methyl-thiazole Analog 8a CHEMBL338159
BDBM13250 2-N-benzene-5-N-(2-chloro-6-methylphenyl)-1,3-thiazole-2,5-diamido BMS-354825 2-Carboxamido-4-hydrido-thiazole Analog 7r N-(2-Chloro-6-methylphenyl)-2-[(phenylcarbonyl)amino]-1,3-thiazole-5-carboxamide CHEMBL131393
BMS-354825 2-Amino-4-methyl-thiazole Analog 7e 2-[[(tert-Butyl)carbonyl]-amino]-4-methyl-N-(2,4,6-trimethylphenyl)-1,3-thiazole-5-carboxamide 2-(2,2-dimethylpropanamido)-4-methyl-N-(2,4,6-trimethylphenyl)-1,3-thiazole-5-carboxamide BDBM13231
BMS-354825 tert-Butoxycarbamate Analog 5a tert-butyl N-{4-methyl-5-[(2,4,6-trimethylphenyl)carbamoyl]-1,3-thiazol-2-yl}carbamate 2-[[(tert-Butyloxy)carbonyl]-amino]-4-methyl-N-(2,4,6-trimethylphenyl)-1,3-thiazole-5-carboxamide BDBM13217 CHEMBL66109
BMS-354825 tert-Butoxycarbamate Analog 5c CHEMBL129454 BDBM13219 tert-butyl N-{5-[(2,6-dimethylphenyl)carbamoyl]-4-methyl-1,3-thiazol-2-yl}carbamate 2-[[(tert-Butyloxy)carbonyl]-amino]-4-methyl-N-(2,6-dimethylphenyl)-1,3-thiazole-5-carboxamide
BMS-740808 Analogue 12c BDBM12703 1-(3-amino-1,2-benzoxazol-5-yl)-6-[4-(2-{[(3R)-3-hydroxypyrrolidin-1-yl]methyl}phenyl)phenyl]-3-methyl-1H,4H,5H,6H,7H-pyrazolo[3,4-c]pyridin-7-one
BMS-740808 Analogue 6g 1-(3-amino-1,2-benzoxazol-5-yl)-6-[4-(2-{[(3S)-3-hydroxypyrrolidin-1-yl]methyl}phenyl)phenyl]-3-(trifluoromethyl)-1H,4H,5H,6H,7H-pyrazolo[3,4-c]pyridin-7-one BDBM12694
CHEMBL128568 tert-butyl N-{4-methyl-5-[(2-methylphenyl)carbamoyl]-1,3-thiazol-2-yl}carbamate BDBM13226 2-[[(tert-Butyloxy)carbonyl]-amino]-4-methyl-N-(2-methylphenyl)-1,3-thiazole-5-carboxamide BMS-354825 tert-Butoxycarbamate Analog 5g
CHEMBL131577 BMS-354825 2-Carboxamido-4-hydrido-thiazole Analog 7n BDBM13246 N-(2-chloro-6-methylphenyl)-2-[(cyclopropylcarbonyl)amino]-1,3-thiazole-5-carboxamide 5-N-(2-chloro-6-methylphenyl)-2-N-cyclopropane-1,3-thiazole-2,5-diamido
CHEMBL131661 2-N-(furan-2-)-4-methyl-5-N-(2,4,6-trimethylphenyl)-1,3-thiazole-2,5-diamido BMS-354825 2-Amino-4-methyl-thiazole Analog 7f 2-(2-furoylamino)-N-mesityl-4-methyl-1,3-thiazole-5-carboxamide BDBM13232
N-(5-{[(5-tert-butyl-1,3-oxazol-2-yl)methyl]sulfanyl}-1,3-thiazol-2-yl)pyrrolidine-2-carboxamide (+/-)-N-[5-[[[5-(1,1-Dimethylethyl)-2-oxazolyl]methyl]thio]-2-thiazolyl]-2-pyrrolidinecarboxamide BDBM5928 BMS-387032 analog 18
N-[5-[[[5-(1,1-Dimethylethyl)-2-oxazolyl]methyl]thio]-2-thiazolyl]-4-piperidinecarboxamide BDBM5931 N-(5-{[(5-tert-butyl-1,3-oxazol-2-yl)methyl]sulfanyl}-1,3-thiazol-2-yl)piperidine-4-carboxamide CHEMBL296468 BMS-387072 cid_3025986
benzyl N-{4-methyl-5-[(2,4,6-trimethylphenyl)carbamoyl]-1,3-thiazol-2-yl}carbamate BMS-354825 2-Amino-4-methyl-thiazole Analog 7b 2-[[(Benzyloxy)carbonyl]-amino]-4-methyl-N-(2,4,6-trimethylphenyl)-1,3-thiazole-5-carboxamide BDBM13230
(S)-2-(1,1-Dimethylprop-1-yl)glycine-L-cis-4,5-methanoprolinenitrile TFA salt BMS-477118 BDBM11533 (1S,3S,5S)-2-[(2S)-2-amino-3,3-dimethylpentanoyl]-2-azabicyclo[3.1.0]hexane-3-carbonitrile; 2,2,2-trifluoroacetic acid Saxagliptin Analogue 10a
1-(3-amino-1,2-benzoxazol-5-yl)-7-(4-{2-[(dimethylamino)methyl]phenyl}-2-fluorophenyl)-3-(trifluoromethyl)-1H,4H,5H,6H,7H,8H-pyrazolo[3,4-c]azepin-8-one BMS-740808 Analogue 16b BDBM12684 bicyclic pyrazole scaffold
2-[(tert-butylcarbamoyl)amino]-4-methyl-N-(2,4,6-trimethylphenyl)-1,3-thiazole-5-carboxamide BMS-354825 2-Amino-4-methyl-thiazole Analog 8d 2-[[(tert-Butylamino)carbonyl]-amino]-4-methyl-N-(2,4,6-trimethylphenyl)-1,3-thiazole-5-carboxamide BDBM13243
BDBM13251 BMS-354825 2-Carboxamido-4-hydrido-thiazole Analog 7s 5-N-(2-chloro-6-methylphenyl)-2-N-(thiophene-2-)-1,3-thiazole-2,5-diamido N-(2-Chloro-6-methylphenyl)-2-[(2-thienylcarbonyl)amino]-1,3-thiazole-5-carboxamide
BDBM689 BMS-186318 analog 26 tert-butyl N-[(2S,3R)-4-{[(2R,3S)-4-{4-[3-(1,3-benzoxazol-2-yl)propoxy]phenyl}-3-{[(tert-butoxy)carbonyl]amino}-2-hydroxybutyl]amino}-3-hydroxy-1-phenylbutan-2-yl]carbamate
BMS-186318 analog 29 BDBM692 tert-butyl N-[(2S,3R)-4-{[(2R,3S)-3-{[(tert-butoxy)carbonyl]amino}-2-hydroxy-4-{4-[3-(morpholin-4-yl)propoxy]phenyl}butyl]amino}-3-hydroxy-1-phenylbutan-2-yl]carbamate
BMS-354825 2-Amino-4-methyl-thiazole Analog 7h 4-methyl-2-N-(thiophene-3-)-5-N-(2,4,6-trimethylphenyl)-1,3-thiazole-2,5-diamido BDBM13234 N-mesityl-4-methyl-2-[(thien-3-ylcarbonyl)amino]-1,3-thiazole-5-carboxamide
BMS-354825 2-Carboxamido-4-hydrido-thiazole Analog 7t N-(2-Chloro-6-methylphenyl)-2-[(3-thienylcarbonyl)amino]-1,3-thiazole-5-carboxamide 5-N-(2-chloro-6-methylphenyl)-2-N-(thiophene-3-)-1,3-thiazole-2,5-diamido BDBM13252
BMS-387032 analog 13 3-amino-N-(5-{[(5-tert-butyl-1,3-oxazol-2-yl)methyl]sulfanyl}-1,3-thiazol-2-yl)propanamide BDBM5923 N-[5-[[[5-(1,1-Dimethylethyl)-2-oxazolyl]methyl]thio]-2-thiazolyl]-2-aminoethanecarboxamide Hydrochloride
BMS-387032 analog 14 N-(5-{[(5-tert-butyl-1,3-oxazol-2-yl)methyl]sulfanyl}-1,3-thiazol-2-yl)-2-phenylacetamide BDBM5924 N-[5-[[[5-(1,1-Dimethylethyl)-2-oxazolyl]methyl]thio]-2-thiazolyl]phenylmethanecarboxamide Trifluoroacetic Acid Salt
BMS-477118 (S)-3,5-Dihydroxyadamantylglycine-L-cis-4,5-methanoprolinenitrile TFA salt Saxagliptin analogue 28 (1S,3S,5S)-2-[(2S)-2-amino-2-(3,5-dihydroxyadamantan-1-yl)acetyl]-2-azabicyclo[3.1.0]hexane-3-carbonitrile; 2,2,2-trifluoroacetic acid BDBM11543
BMS-477118 BDBM11544 (S)-3-Fluoroadamantylglycine-L-cis-4,5-methanoprolinenitrile TFA salt Saxagliptin analogue 30 (1S,3S,5S)-2-[(2S)-2-amino-2-(3-fluoroadamantan-1-yl)acetyl]-2-azabicyclo[3.1.0]hexane-3-carbonitrile; 2,2,2-trifluoroacetic acid
CHEMBL128589 BMS-354825 2-Amino-4-methyl-thiazole Analog 7a methyl N-{4-methyl-5-[(2,4,6-trimethylphenyl)carbamoyl]-1,3-thiazol-2-yl}carbamate 2-[[(Methoxy)carbonyl]-amino]-4-methyl-N-(2,4,6-trimethylphenyl)-1,3-thiazole-5-carboxamide BDBM13222
CHEMBL297570 (+/-)-N-[5-[[[5-(1,1-Dimethylethyl)-2-oxazolyl]methyl]thio]-2-thiazolyl]-3-piperidinecarboxamide BDBM5929 N-(5-{[(5-tert-butyl-1,3-oxazol-2-yl)methyl]sulfanyl}-1,3-thiazol-2-yl)piperidine-3-carboxamide BMS-387032 analog 19
dihydropyrazolo[4,3-d]pyrimidinone 24a BDBM12687 BMS-740808 Analogue 18 1-(3-amino-1,2-benzoxazol-5-yl)-6-(4-{2-[(dimethylamino)methyl]phenyl}phenyl)-3-(trifluoromethyl)-1H,4H,5H,6H,7H-pyrazolo[4,3-d]pyrimidin-7-one
(1S,3S,5S)-2-[(2S)-2-amino-3,3-diethylpentanoyl]-2-azabicyclo[3.1.0]hexane-3-carbonitrile; 2,2,2-trifluoroacetic acid BMS-477118 analogue BDBM11534 Saxagliptin Analogue 10b (S)-2-(1,1-Diethylprop-1-yl)glycine-L-cis-4,5-methanoprolinenitrile TFA salt
1-(3-amino-1,2-benzoxazol-5-yl)-6-(4-{2-[(dimethylamino)methyl]phenyl}phenyl)-3-(trifluoromethyl)-1H,4H,5H,6H,7H-pyrazolo[3,4-c]pyridin-7-one dihydropyrazolopyridinone analogue 9 bicyclic pyrazole scaffold BMS-740808 Analogue 6a BDBM12681
1-(3-amino-1,2-benzoxazol-5-yl)-6-[2-fluoro-4-(2-{[(3R)-3-hydroxypyrrolidin-1-yl]methyl}phenyl)phenyl]-3-methyl-1H,4H,5H,6H,7H-pyrazolo[3,4-c]pyridin-7-one BMS-740808 Analogue 12d BDBM12704
BDBM11529 Saxagliptin Analogue 8d (1S,3S,5S)-2-[(2S)-2-amino-2-(1-ethenylcyclopentyl)acetyl]-2-azabicyclo[3.1.0]hexane-3-carbonitrile; 2,2,2-trifluoroacetic acid BMS-477118 analogue (S)-2-(1-Ethenylcyclopent-1-yl)glycine-L-cis-4,5-methanoprolinenitrile
BDBM12700 1-(3-amino-1,2-benzoxazol-5-yl)-6-[2-fluoro-4-(2-{[(3R)-3-hydroxypyrrolidin-1-yl]methyl}phenyl)phenyl]-3-(trifluoromethyl)-1H,4H,5H,6H,7H-pyrazolo[3,4-c]pyridin-7-one BMS-740808 Analogue 7c
BMS-354825 2-Carboxamido-4-hydrido-thiazole Analog 7u N-(2-Chloro-6-methylphenyl)-2-[(2-furanylcarbonyl)amino]-1,3-thiazole-5-carboxamide 5-N-(2-chloro-6-methylphenyl)-2-N-(furan-2-)-1,3-thiazole-2,5-diamido CHEMBL128070 BDBM13253
N-(2-chloro-6-methylphenyl)-2-[(3,5-dimethylpyrazin-2-yl)amino]-1,3-thiazole-5-carboxamide BMS-354825 2-Heteroarylamino-thiazole Analog 12h N-(2-Chloro-6-methylphenyl)-2-[(3,5-dimethyl-2-pyrazinyl)-amino]-1,3-thiazole-5-carboxamide BDBM13263
N-[5-[[[5-(1,1-Dimethylethyl)-2-oxazolyl]methyl]thio]-2-thiazolyl]-4-methylpiperidinecarboxamide BDBM5930 BMS-387032 analog 20 N-(5-{[(5-tert-butyl-1,3-oxazol-2-yl)methyl]sulfanyl}-1,3-thiazol-2-yl)-2-(piperidin-4-yl)acetamide
hydroxy-1-(phenylmethyl)propyl]carbamic Acid, 1,1-Dimethylethyl Ester BMS-186318 analog 23 BDBM686 [1S-[1R*,2S*(2S*,3R*)]]-[3-[[3-[[(1,10-Dimethylethoxy)carbonyl]amino]-2-hydroxy-4-[4-[[(4-morpholinyl-carbonyl)oxy]methyl]phenyl]butyl]amino]-2-
tert-butyl N-[(2S,3R)-4-{[(2R,3S)-3-{[(tert-butoxy)carbonyl]amino}-2-hydroxy-4-{4-[3-(3-oxomorpholin-4-yl)propoxy]phenyl}butyl]amino}-3-hydroxy-1-phenylbutan-2-yl]carbamate BDBM693 BMS-186318 analog 30
(1S,3S,5S)-2-[(2S)-2-amino-2-[1-(1,2-dihydroxyethyl)cyclopentyl]acetyl]-2-azabicyclo[3.1.0]hexane-3-carbonitrile Saxagliptin Analogue 18d (2S)-2-[1-(1,2-Dihydroxyethyl)cyclopent-1-yl]glycine-L-cis-4,5-methanoprolinenitrile BMS-477118 analogue BDBM11540
N-(2-Chloro-6-methylphenyl)-2-[(4-methyl-2-pyridinyl)amino]-1,3-thiazole-5-carboxamide BMS-354825 2-Heteroarylamino-thiazole Analog 12k CHEMBL186568 BDBM13266 N-(2-chloro-6-methylphenyl)-2-[(4-methylpyridin-2-yl)amino]-1,3-thiazole-5-carboxamide
N-(2-chloro-6-methylphenyl)-2-[(2,6-dimethylpyrimidin-4-yl)amino]-1,3-thiazole-5-carboxamide BMS-354825 2-Heteroarylamino-thiazole Analog 12m BDBM13268 CHEMBL364623 N-(2-Chloro-6-methylphenyl)-2-[(2,6-dimethyl-4-pyrimidinyl)-amino]-1,3-thiazole-5-carboxamide
N-(2-chloro-6-methylphenyl)-2-[(4,6-dimethylpyridin-2-yl)amino]-1,3-thiazole-5-carboxamide BMS-354825 2-Heteroarylamino-thiazole Analog 12l N-(2-Chloro-6-methylphenyl)-2-[(4,6-dimethyl-2-pyridinyl)-amino]-1,3-thiazole-5-carboxamide BDBM13267 CHEMBL188478
N-(2-chloro-6-methylphenyl)-2-[(6-methylpyridin-2-yl)amino]-1,3-thiazole-5-carboxamide BMS-354825 2-Heteroarylamino-thiazole Analog 12j N-(2-Chloro-6-methylphenyl)-2-[(6-methyl-2-pyridinyl)amino]-1,3-thiazole-5-carboxamide BDBM13265 CHEMBL365505
N-(5-{(R)-2-[(R)-1-(4-Difluoromethoxy-phenyl)-2-phenyl-ethylamino]-1-hydroxy-ethyl}-2-hydroxy-phenyl)-methanesulfonamide BDBM50106829 BMS-196085 CHEMBL322862 N-(5-((R)-2-((R)-1-(4-(difluoromethoxy)phenyl)-2-phenylethylamino)-1-hydroxyethyl)-2-hydroxyphenyl)methanesulfonamide
N-(5-{[(5-tert-butyl-1,3-oxazol-2-yl)methyl]sulfanyl}-1,3-thiazol-2-yl)-1-methanesulfonylpiperidine-4-carboxamide BMS-387032 analog 24 BDBM5934 N-[5-[[[5-(1,1-Dimethylethyl)-2-oxazolyl]methyl]thio]-2-thiazolyl]-(N-methylsulfonyl)-4-piperidinecarboxamide
N-(5-{[(5-tert-butyl-1,3-oxazol-2-yl)methyl]sulfanyl}-1,3-thiazol-2-yl)-1-methylpiperidine-4-carboxamide BMS-387032 analog 22 BDBM5932 1-Methyl-N-[5-[[[5-(1,1-dimethylethyl)-2-oxazolyl]methyl]thio]-2-thiazolyl]-4-piperidinecarboxamide
(1S,3S,5S)-2-[(2S)-2-amino-2-(1-ethylcyclopentyl)acetyl]-2-azabicyclo[3.1.0]hexane-3-carbonitrile; 2,2,2-trifluoroacetic acid BMS-477118 analogue BDBM11535 Saxagliptin Analogue 10d (S)-2-(1-Ethylcyclopent-1-yl)-l-glycine-L-cis-4,5-methanoprolinenitrile TFA salt
2-[[(n-Butylamino)carbonyl]-amino]-4-methyl-N-(2-chloro-6-methylphenyl)-1,3-thiazole-5-carboxamide 2-[(butylcarbamoyl)amino]-N-(2-chloro-6-methylphenyl)-4-methyl-1,3-thiazole-5-carboxamide BMS-354825 2-Amino-4-methyl-thiazole Analog 8f BDBM13245 CHEMBL130160
2-[[(tert-Butyloxy)carbonyl]-amino]-4-methyl-N-(4-bromo-2,6-dimethylphenyl)-1,3-thiazole-5-carboxamide CHEMBL340322 tert-butyl N-{5-[(4-bromo-2,6-dimethylphenyl)carbamoyl]-4-methyl-1,3-thiazol-2-yl}carbamate BMS-354825 tert-Butoxycarbamate Analog 5d BDBM13220
5-N-(2-chloro-6-methylphenyl)-2-N-(furan-2-)-4-methyl-1,3-thiazole-2,5-diamido BMS-354825 2-Amino-4-methyl-thiazole Analog 7k CHEMBL127500 N-(2-chloro-6-methylphenyl)-2-(2-furoylamino)-4-methyl-1,3-thiazole-5-carboxamide BDBM13237
5-N-(2-chloro-6-methylphenyl)-2-N-cyclopropane-4-methyl-1,3-thiazole-2,5-diamido CHEMBL128377 2-[[(Cyclopropyl)carbonyl]-amino]-4-methyl-N-(2-chloro-6-methylphenyl)-1,3-thiazole-5-carboxamide BDBM13239 BMS-354825 2-Amino-4-methyl-thiazole Analog 7m
BDBM11528 Saxagliptin Analogue 8c BMS-477118 analogue (1S,3S,5S)-2-[(2S)-2-amino-2-(1-ethenylcyclobutyl)acetyl]-2-azabicyclo[3.1.0]hexane-3-carbonitrile; 2,2,2-trifluoroacetic acid (S)-2-(1-Ethenylcyclobut-1-yl)glycine-L-cis-4,5-methanoprolinenitrile TFA salt
BDBM13228 CHEMBL132399 BMS-354825 tert-Butoxycarbamate Analog 5i tert-butyl N-{5-[(2-methoxy-6-methylphenyl)carbamoyl]-4-methyl-1,3-thiazol-2-yl}carbamate 2-[[(tert-Butyloxy)carbonyl]-amino]-4-methyl-N-(2-methoxy-6-methylphenyl)-1,3-thiazole-5-carboxamide
BDBM13238 2-N-benzene-5-N-(2-chloro-6-methylphenyl)-4-methyl-1,3-thiazole-2,5-diamido 2-[(Benzoyl)-amino]-4-methyl-N-(2-chloro-6-methylphenyl)-1,3-thiazole-5-carboxamide BMS-354825 2-Amino-4-methyl-thiazole Analog 7l CHEMBL337985
BMS-387032 analog 15 N-[5-[[[5-tert-Butyl-2-oxazolyl]methyl]thio]-2-thiazolyl]benzamide BDBM5683 2-amino-5-thio-substituted thiazole 31 N-(5-{[(5-tert-butyl-1,3-oxazol-2-yl)methyl]sulfanyl}-1,3-thiazol-2-yl)benzamide
BMS-387032 analog 26 4-amino-N-(5-{[(5-tert-butyl-1,3-oxazol-2-yl)methyl]sulfanyl}-1,3-thiazol-2-yl)cyclohexane-1-carboxamide cis-4-Amino-N-[5-[[[5-(1,1-dimethylethyl)-2-oxazolyl]methyl]thio]-2-thiazolyl]cyclohexanecarboxamide Hydrochloride BDBM5936
BMS-387032 analog 27 4-amino-N-(5-{[(5-tert-butyl-1,3-oxazol-2-yl)methyl]sulfanyl}-1,3-thiazol-2-yl)cyclohexane-1-carboxamide trans-4-Amino-N-[5-[[[5-(1,1-dimethylethyl)-2-oxazolyl]methyl]thio]-2-thiazolyl]cyclohexanecarboxamide Hydrochloride BDBM5937
BMS-477118 analogue Saxagliptin Analogue 8f BDBM11531 (1S,3S,5S)-2-[(2S)-2-amino-2-(1-ethenylcycloheptyl)acetyl]-2-azabicyclo[3.1.0]hexane-3-carbonitrile; 2,2,2-trifluoroacetic acid (S)-2-(1-Ethenylcyclohept-1-yl)glycine-L-cis-4,5-methanoprolinenitrile TFA salt
CABOZANTINIB US12304898, Example Cabozantinib Cometriq US10227329, Compound Cabozantinib US20240174674, Compound Cabozantinib Cabometyx US10202365, Compound Cabozantinib CHEBI:72317 US12338253, Compound Cabozantinib US10464902, Cabozantinib BDBM50021574 BMS-907351 US11279688, Compound Cabozantinib cabozantinib s-malate US10183928, Cabozantinib XL-184 US10273211, Compound Cabozantinib US10774070, Compound Cabozantinib
CHEMBL189649 N-(2-Chloro-6-methylphenyl)-2-(6-morpholinopyrimidin-4-ylamino)-1,3-thiazole-5-carboxamide N-(2-chloro-6-methylphenyl)-2-{[6-(morpholin-4-yl)pyrimidin-4-yl]amino}-1,3-thiazole-5-carboxamide BMS-354825 2-Heteroarylamino-thiazole Analog 12s BDBM13274
CHEMBL334333 tert-butyl N-{5-[(2-chloro-6-methylphenyl)carbamoyl]-4-methyl-1,3-thiazol-2-yl}carbamate BMS-354825 tert-Butoxycarbamate Analog 5b BDBM13218 2-[[(tert-Butyloxy)carbonyl]-amino]-4-methyl-N-(2-chloro-6-methylphenyl)-1,3-thiazole-5-carboxamide
Saxagliptin Analogue 8e (S)-2-(1-Ethenylcyclohex-1-yl)glycine-L-cis-4,5-methanoprolinenitrile TFA salt BMS-477118 analogue BDBM11530 (1S,3S,5S)-2-[(2S)-2-amino-2-(1-ethenylcyclohexyl)acetyl]-2-azabicyclo[3.1.0]hexane-3-carbonitrile; 2,2,2-trifluoroacetic acid
(1S,3S,5S)-2-[(2S)-2-amino-3,3-dimethylpent-4-enoyl]-2-azabicyclo[3.1.0]hexane-3-carbonitrile; 2,2,2-trifluoroacetic acid BMS-477118 analogue BDBM11525 Saxagliptin Analogue 8a (S)-2-(1,1-Dimethylprop-2-en-1-yl)glycine-L-cis-4,5-methanoprolinenitrile TFA salt
(S)-2-(4-Ethenyltetrahydropyran-4-yl)glycine-L-cis-4,5-methanoprolinenitrile TFA salt BMS-477118 analogue Saxagliptin Analogue 8g (1S,3S,5S)-2-[(2S)-2-amino-2-(4-ethenyloxan-4-yl)acetyl]-2-azabicyclo[3.1.0]hexane-3-carbonitrile; 2,2,2-trifluoroacetic acid BDBM11532
(S)-2-(4-Ethyltetrahydropyran-4-yl)glycine-L-cis-4,5-methanoprolinenitrile TFA salt BMS-477118 analogue BDBM11536 Saxagliptin Analogue 10g (1S,3S,5S)-2-[(2S)-2-amino-2-(4-ethyloxan-4-yl)acetyl]-2-azabicyclo[3.1.0]hexane-3-carbonitrile; 2,2,2-trifluoroacetic acid
(S)-2-[1-(Hydroxymethyl)cyclohex-1-yl]glycine-L-cis-4,5-methanoprolinenitrile TFA Salt BDBM11539 BMS-477118 analogue (1S,3S,5S)-2-[(2S)-2-amino-2-[1-(hydroxymethyl)cyclohexyl]acetyl]-2-azabicyclo[3.1.0]hexane-3-carbonitrile; 2,2,2-trifluoroacetic acid Saxagliptin Analogue 16e
2-[[(tert-Butyloxy)carbonyl]-amino]-4-methyl-N-(2-isopropyl6-methylphenyl)-1,3-thiazole-5-carboxamide CHEMBL336330 BDBM13227 BMS-354825 tert-Butoxycarbamate Analog 5h tert-butyl N-(4-methyl-5-{[2-methyl-6-(propan-2-yl)phenyl]carbamoyl}-1,3-thiazol-2-yl)carbamate
BDBM11527 BMS-477118 analogue Saxagliptin Analogue 8b (1S,3S,5S)-2-[(2S)-2-amino-3,3-diethylpent-4-enoyl]-2-azabicyclo[3.1.0]hexane-3-carbonitrile; 2,2,2-trifluoroacetic acid (S)-2-(1,1-Diethylprop-2-en-1-yl)glycine-L-cis-4,5-methanoprolinenitrile TFA salt
BDBM11537 BMS-477118 analogue (1S,3S,5S)-2-[(2S)-2-amino-2-[1-(hydroxymethyl)cyclobutyl]acetyl]-2-azabicyclo[3.1.0]hexane-3-carbonitrile; 2,2,2-trifluoroacetic acid (S)-2-[1-(Hydroxymethyl)cyclobut-1-yl]glycine-L-cis-4,5-methanoprolinenitrile TFA Salt Saxagliptin Analogue 16c
BDBM11538 BMS-477118 analogue (S)-2-[1-(Hydroxymethyl)cyclopent-1-yl]glycine-L-cis-4,5-methanoprolinenitrile TFA Salt (1S,3S,5S)-2-[(2S)-2-amino-2-[1-(hydroxymethyl)cyclopentyl]acetyl]-2-azabicyclo[3.1.0]hexane-3-carbonitrile; 2,2,2-trifluoroacetic acid Saxagliptin Analogue 16d
BDBM13271 N-(2-Chloro-6-methylphenyl)-2-(6-(2-hydroxyethylamino)pyridin-2-ylamino)-1,3-thiazole-5-carboxamide BMS-354825 2-Heteroarylamino-thiazole Analog 12p N-(2-chloro-6-methylphenyl)-2-({6-[(2-hydroxyethyl)amino]pyridin-2-yl}amino)-1,3-thiazole-5-carboxamide
BDBM5660 BMS-387032 analog 12 2-aminothiazole 2 N-(5-{[(5-tert-butyl-1,3-oxazol-2-yl)methyl]sulfanyl}-1,3-thiazol-2-yl)acetamide 2-amino-5-thio-substituted thiazole 25 N-[5-[[(5-tert-Butyl-2-oxazolyl)methyl]thio]-2-thiazolyl]acetamide
BMS-354825 2-Amino-4-methyl-thiazole Analog 7i BDBM13235 N-(2-chloro-6-methylphenyl)-4-methyl-2-[(thien-3-ylcarbonyl)amino]-1,3-thiazole-5-carboxamide 5-N-(2-chloro-6-methylphenyl)-4-methyl-2-N-(thiophene-3-)-1,3-thiazole-2,5-diamido
BMS-387032 analog 23 BDBM5933 N-[5-[[[5-(1,1-Dimethylethyl)-2-oxazolyl]methyl]thio]-2-thiazolyl]-1-(2-hydroxyethyl)-4-piperidinecarboxamide N-(5-{[(5-tert-butyl-1,3-oxazol-2-yl)methyl]sulfanyl}-1,3-thiazol-2-yl)-1-(2-hydroxyethyl)piperidine-4-carboxamide
BMS-387032 analog 25 tert-butyl 4-[(5-{[(5-tert-butyl-1,3-oxazol-2-yl)methyl]sulfanyl}-1,3-thiazol-2-yl)carbamoyl]piperidine-1-carboxylate BDBM5935 N-[5-[[[5-(1,1-Dimethylethyl)-2-oxazolyl]methyl]thio]-2-thiazolyl]-(N-tert-butoxycarbonyl)-4-piperidinecarboxamide
BMS-477118 (1S,3S,5S)-2-[(S)-2-amino-2-(3-hydroxy-adamantan-1-yl)-acetyl]-2-aza-bicyclo[3.1.0]hexane-3-carbonitrile BDBM50225074 SAXAGLIPTIN (1S,6S)-2-(2-adamantan-1-yl-2-amino-acetyl)-2-aza-bicyclo[3.1.0]hexane-3-carbonitrile CHEMBL385517
N-(2-chloro-6-methylphenyl)-4-methyl-2-[(thien-2-ylcarbonyl)amino]-1,3-thiazole-5-carboxamide BMS-354825 2-Amino-4-methyl-thiazole Analog 7j BDBM13236 5-N-(2-chloro-6-methylphenyl)-4-methyl-2-N-(thiophene-2-)-1,3-thiazole-2,5-diamido
4'-Oxazol-2-yl-biphenyl-2-sulfonic acid (3,4-dimethyl-isoxazol-5-yl)-amide CHEMBL24461 BMS-193884 BDBM50091105 4''-Oxazol-2-yl-biphenyl-2-sulfonic acid (3,4-dimethyl-isoxazol-5-yl)-amide 4'-Oxazol-2-yl-biphenyl-2-sulfonicacid(3,4-dimethyl-isoxazol-5-yl)-amide
BDBM13272 BMS-354825 2-Heteroarylamino-thiazole Analog 12q N-(2-chloro-6-methylphenyl)-2-[(6-{[3-(morpholin-4-yl)propyl]amino}pyridin-2-yl)amino]-1,3-thiazole-5-carboxamide N-(2-Chloro-6-methylphenyl)-2-(6-(3-morpholinopropylamino)pyridin-2-ylamino)-1,3-thiazole-5-carboxamide
N-(2-Chloro-6-methylphenyl)-2-(6-(2-hydroxyethylamino)-2-methylpyrimidin-4-ylamino)-1,3-thiazole-5-carboxamide BMS-354825 2-Heteroarylamino-thiazole Analog 12v N-(2-chloro-6-methylphenyl)-2-({6-[(2-hydroxyethyl)amino]-2-methylpyrimidin-4-yl}amino)-1,3-thiazole-5-carboxamide BDBM13277
N-(2-chloro-6-methylphenyl)-2-{[2-methyl-6-(morpholin-4-yl)pyrimidin-4-yl]amino}-1,3-thiazole-5-carboxamide N-(2-Chloro-6-methylphenyl)-2-(2-methyl-6-morpholinopyrimidin-4-ylamino)-1,3-thiazole-5-carboxamide BMS-354825 2-Heteroarylamino-thiazole Analog 12t BDBM13275
(4S,7S,10aS)-4-((S)-2-mercapto-3-phenylpropanamido)-5-oxo-octahydro-2H-pyrido[2,1-b][1,3]thiazepine-7-carboxylic acid CHEMBL289556 OMAPATRILAT BMS-186716 (4S,6S,9aS)-6-((S)-2-Mercapto-3-phenyl-propionylamino)-5-oxo-octahydro-9-thia-4a-aza-benzocycloheptene-4-carboxylic acid BDBM50073120
2-butyl-3-{[2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl}-1,3-diazaspiro[4.4]non-1-en-4-one CHEMBL1513 BDBM50042235 IRBESARTAN BMS 186295 2-butyl-3-{[2'-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl}-1,3-diazaspiro[4.4]non-1-en-4-one
(R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan-2-ol CHEMBL377300 (R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5-methylpyrrolo[1,2-f][1,2,4]triazin-6-yloxy)propan-2-ol BMS-540215 BDBM50184807
9-(4-{4-[(4''-Trifluoromethyl-biphenyl-2-carbonyl)-amino]-piperidin-1-yl}-butyl)-9H-fluorene-9-carboxylic acid (2,2,2-trifluoro-ethyl)-amide CHEMBL354541 9-(4-{4-[(4'-Trifluoromethyl-biphenyl-2-carbonyl)-amino]-piperidin-1-yl}-butyl)-9H-fluorene-9-carboxylic acid (2,2,2-trifluoro-ethyl)-amide BDBM50098320 BMS-201038 LOMITAPIDE
BMS-354825 2-Heteroarylamino-thiazole Analog 12w N-(2-chloro-6-methylphenyl)-2-({6-[4-(hydroxymethyl)piperidin-1-yl]-2-methylpyrimidin-4-yl}amino)-1,3-thiazole-5-carboxamide N-(2-Chloro-6-methylphenyl)-2-(6-(4-(hydroxymethyl)piperidin-1-yl)-2-methylpyrimidin-4-ylamino)-1,3-thiazole-5-carboxamide BDBM13278
N-(2-Chloro-6-methylphenyl)-2-(2-methyl-6-(3-morpholinopropyl)-pyrimidin-4-ylamino)-1,3-thiazole-5-carboxamide BMS-354825 2-Heteroarylamino-thiazole Analog 12u BDBM13276 N-(2-chloro-6-methylphenyl)-2-[(2-methyl-6-{[3-(morpholin-4-yl)propyl]amino}pyrimidin-4-yl)amino]-1,3-thiazole-5-carboxamide
BDBM13273 N-(2-chloro-6-methylphenyl)-2-[(6-{[3-(1H-imidazol-1-yl)propyl]amino}pyridin-2-yl)amino]-1,3-thiazole-5-carboxamide 2-(6-(3-(1H-Imidazol-1-yl)propylamino)pyridin-2-ylamino)-N-(2-chloro-6-methylphenyl)-1,3-thiazole-5-carboxamide BMS-354825 2-Heteroarylamino-thiazole Analog 12r
1-Methyl-1H-imidazole-4-sulfonic Acid Benzyl-[6-cyano1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydroquinolin-3-yl]amide CHEMBL182888 tetrahydroquinoline (THQ)-based inhibitor 4e N-benzyl-N-{6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl}-1-methyl-1H-imidazole-4-sulfonamide BDBM13323 BMS-339941
CHEMBL558198 Razaxaban BMS-561389 BDBM12676 1-(3-Aminobenzisoxazol-5-yl)-3-trifluoromethyl-N-[2-fluoro-4-[(2-dimethylaminomethyl)imidazol-1-yl]phenyl]-1H-pyrazole-5-carboxyamide Hydrochloride Salt CHEMBL206335 DPC 906 1-(3-amino-1,2-benzoxazol-5-yl)-N-(4-{2-[(dimethylamino)methyl]-1H-imidazol-1-yl}-2-fluorophenyl)-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
1-((2R,3S)-4-((S)-3-(4-fluorobenzyl)piperidin-1-yl)-3-hydroxybutan-2-yl)-3-(3-(1-methyl-1H-tetrazol-5-yl)phenyl)urea CHEMBL399495 BDBM50231358 BMS-639623 1-{(1R,2S)-3-[(S)-3-(4-Fluoro-benzyl)-piperidin-1-yl]-2-hydroxy-1-methyl-propyl}-3-[3-(1-methyl-1H-tetrazol-5-yl)-phenyl]-urea
BDBM678 3-{4-[(2S,3R)-2-{[(tert-butoxy)carbonyl]amino}-4-{[(2R,3S)-3-{[(tert-butoxy)carbonyl]amino}-2-hydroxy-4-phenylbutyl]amino}-3-hydroxybutyl]phenoxy}propanoic acid BMS-186318 analog 15 [1S-[1R*,2S*(2S*,3R*)]]-[4-[4-(Carboxymethoxy)phenyl]-3-[[3-[[(1,1-dimethylethoxy)carbonyl]amino]-2-hydroxy-1-(phenylmethyl)propyl)carbamic Acid, 1,1-Dimethylethyl Ester
BMS-186318 analog 1 [(S,R)-3-[[(R,S)-3-[[(1,1-Dimethylethoxy)carbonyl]amino]-2-hydroxy-4-phenylbutyl]amino]-2-hydroxy-1-(phenylmethyl)propyl]carbamic Acid, 1,1-Dimethylethyl Ester tert-butyl N-[(2S,3R)-4-{[(2R,3S)-3-{[(tert-butoxy)carbonyl]amino}-2-hydroxy-4-phenylbutyl]amino}-3-hydroxy-1-phenylbutan-2-yl]carbamate BDBM914 Aminodiol deriv. 9a
BMS-387032 analog 2 BDBM5668 N-[5-[[[5-tert-Butyl-2-oxazolyl]methyl]thio]-2-thiazolyl]-4-[[[bis(hydroxymethyl)methyl]amino]methyl]benzeneacetamide Hydrochloride Salt N-(5-{[(5-tert-butyl-1,3-oxazol-2-yl)methyl]sulfanyl}-1,3-thiazol-2-yl)-2-(4-{[(1,3-dihydroxypropan-2-yl)amino]methyl}phenyl)acetamide 2-amino-5-thio-substituted thiazole 45
CHEMBL183536 BDBM13319 BMS-386914 tert-butyl 2-({6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl}(1-methyl-1H-imidazole-4-)sulfonamido)acetate [[6-Cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydroquinolin-3-yl]-(1-methyl-1H-imidazole-4-sulfonyl)amino]-acetic Acid tert-Butyl Ester tetrahydroquinoline (THQ)-based inhibitor 4a
BDBM665 BMS-186318 analog 2 [1S-[1R*,2S*(2S*,3R*)]]-[3-[[3-[[(1,1-Dimethylethoxy)-carbonyl]amino]-2-hydroxy-4-phenylbutyl]amino]-2-hydroxy-1-(4-pyridinylmethyl)propyl]carbamic Acid, 1,1-Dimethylethyl Ester tert-butyl N-[(2S,3R)-4-{[(2R,3S)-3-{[(tert-butoxy)carbonyl]amino}-2-hydroxy-4-(pyridin-4-yl)butyl]amino}-3-hydroxy-1-phenylbutan-2-yl]carbamate
BDBM666 BMS-186318 analog 3 [1S-[1R*,2S*(2S*,3R*)]]-[3-[[3-[[(1,1-Dimethylethoxy)-carbonyl]amino]-2-hydroxy-4-phenylbutyl]amino]-2-hydroxy-1-(6-quinolinylmethyl)propyl]carbamic Acid, 1,1-Dimethylethyl Ester tert-butyl N-[(2S,3R)-4-{[(2R,3S)-3-{[(tert-butoxy)carbonyl]amino}-2-hydroxy-4-(quinolin-6-yl)butyl]amino}-3-hydroxy-1-phenylbutan-2-yl]carbamate
BDBM668 [1S-[1R*,2S*(2S*,3R*)]]-[3-[[3-[[(1,1-Dimethylethoxy)-carbonyl]amino]-2-hydroxy-4-(3-hydroxyphenyl)butyl]-amino]-2-hydroxy-1-(phenylmethyl)propyl]carbamic Acid, 1,1-Dimethylethyl Ester BMS-186318 analog 5 tert-butyl N-[(2S,3R)-4-{[(2R,3S)-3-{[(tert-butoxy)carbonyl]amino}-2-hydroxy-4-(3-hydroxyphenyl)butyl]amino}-3-hydroxy-1-phenylbutan-2-yl]carbamate
BDBM669 BMS-186318 analog 6 tert-butyl N-[(2S,3R)-4-{[(2R,3S)-3-{[(tert-butoxy)carbonyl]amino}-2-hydroxy-4-(2-hydroxyphenyl)butyl]amino}-3-hydroxy-1-phenylbutan-2-yl]carbamate [1S-[1R*,2S*(2S*,3R*)]]-[3-[[3-[[(1,1-Dimethylethoxy)-carbonyl]amino]-2-hydroxy-4-(2-hydroxyphenyl)butyl]amino]-2-hydroxy-1-(phenylmethyl)propyl]carbamic Acid, 1,1-Dimethylethyl Ester
BMS-186318 analog 4 (1S-(1R*,2S*(2S,3R*)))-[3-[[3-[[(1,1-Dimethylethoxy)carbonyl]amino]-2-hydroxy-4-(4-hydroxyphenyl)butyl]amino]-2-hydroxy-1-(phenylmethyl)propyl]carbamic Acid, 1,1-Dimethylethyl Ester BDBM918 tert-butyl N-[(2S,3R)-4-{[(2R,3S)-3-{[(tert-butoxy)carbonyl]amino}-2-hydroxy-4-(4-hydroxyphenyl)butyl]amino}-3-hydroxy-1-phenylbutan-2-yl]carbamate Aminodiol deriv. 15b
CHEMBL181102 N-{6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1,2,3,4-tetrahydroquinolin-3-yl}-1-methyl-N-(2-methylprop-2-en-1-yl)-1H-imidazole-4-sulfonamide BMS-388891 tetrahydroquinoline (THQ)-based inhibitor 4b 1-Methyl-1H-imidazole-4-sulfonic Acid [6-Cyano-1-(3-methyl-3H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydroquinolin-3-yl]-(2-methylallyl)amide BDBM13320
BDBM676 BMS-186318 analog 13 tert-butyl N-[(2S,3R)-4-{[(2R,3S)-3-{[(tert-butoxy)carbonyl]amino}-2-hydroxy-4-[4-(2-hydroxypropoxy)phenyl]butyl]amino}-3-hydroxy-1-phenylbutan-2-yl]carbamate [1S-[1R*, 2S*(2S*, 3R*)]-[3-[[3-[[(1,1-Dimethylethoxy)-carbonyl]amino]-2-hydroxy-4-[4-(2-hydroxypropoxy)phenyl]butyl]amino]-2-hydroxy-1-(phenylmethyl)propyl]carbamic Acid, 1,1-Dimethyl Ester
BDBM679 BMS-186318 analog 16 tert-butyl N-[(2S,3R)-4-{[(2R,3S)-3-{[(tert-butoxy)carbonyl]amino}-4-(4-{2-[(dimethylcarbamoyl)oxy]ethoxy}phenyl)-2-hydroxybutyl]amino}-3-hydroxy-1-phenylbutan-2-yl]carbamate [1S-[1R*,2S*(2S*,3R*)]]-[3-[[4-[4-[2-[[(Dimethylamino)-carbonyl]oxy]ethoxy]phenyl]-3-[[(1,1-dimethylethoxy)-carbonyl]amino]-2-hydroxybutyl]amino]-2-hydroxy-1-(phenylmethyl)propyl]carbamic Acid
BMS-186318 analog 12 [1S-[1R*,2S*(2S*,3R*)]]-[3-[[3-[[(1,1-Dimethylethoxy)-carbonyl]amino]-2-hydroxy-4-[4-(2-methoxyethoxy)phenyl]butyl]amino]-2-hydroxy-1-(phenylmethyl)propyl]carbamic Acid, 1,1-Dimethylethyl Ester BDBM675 tert-butyl N-[(2S,3R)-4-{[(2R,3S)-3-{[(tert-butoxy)carbonyl]amino}-2-hydroxy-4-[4-(2-methoxyethoxy)phenyl]butyl]amino}-3-hydroxy-1-phenylbutan-2-yl]carbamate
[1S-[1R*,2S*(2S*,3R*)]]-[3-[[3-[[(1,1-Dimethylethoxy)-carbonyl]amino]-2-hydroxy-4-[4-(2-hydroxyethoxy)phenyl]butyl]amino]-2-hydroxy-1-(phenylmethyl)propyl]carbamic Acid, 1,1-Dimethylethyl Ester BMS-186318 analog 11 BDBM674 tert-butyl N-[(2S,3R)-4-{[(2R,3S)-3-{[(tert-butoxy)carbonyl]amino}-2-hydroxy-4-[4-(2-hydroxyethoxy)phenyl]butyl]amino}-3-hydroxy-1-phenylbutan-2-yl]carbamate
4'-(2-Butyl-4-oxo-1,3-diaza-spiro[4.4]non-1-en-3-ylmethyl)-2'-(3,3-dimethyl-2-oxo-pyrrolidin-1-ylmethyl)-biphenyl-2-sulfonic acid (3,4-dimethyl-isoxazol-5-yl)-amide CHEMBL11706 BDBM50117910 BMS-248360 4''-(2-Butyl-4-oxo-1,3-diaza-spiro[4.4]non-1-en-3-ylmethyl)-2''-(3,3-dimethyl-2-oxo-pyrrolidin-1-ylmethyl)-biphenyl-2-sulfonic acid (3,4-dimethyl-isoxazol-5-yl)-amide
BMS-186318 analog 21 [1S-[1R*,2S*(2S*,3R*)]]-[3-[[3-[[(1,1-Dimethylethoxy)-carbonyl]amino]-2-hydroxy-4-[4-[2-(4-morpholinyl)ethoxy]-phenyl]butyl]amino]-2-hydroxy-1- tert-butyl N-[(2S,3R)-4-{[(2R,3S)-3-{[(tert-butoxy)carbonyl]amino}-2-hydroxy-4-{4-[2-(morpholin-4-yl)ethoxy]phenyl}butyl]amino}-3-hydroxy-1-phenylbutan-2-yl]carbamate (phenylmethyl)propyl]carbamic Acid, 1,1-Dimethylethyl Ester BDBM684
BMS-186318 analog 8 BDBM671 tert-butyl N-[(2S,3R)-4-{[(2R,3S)-3-{[(tert-butoxy)carbonyl]amino}-2-hydroxy-4-{4-[2-(pyridin-2-yl)ethoxy]phenyl}butyl]amino}-3-hydroxy-1-phenylbutan-2-yl]carbamate [1S-[1R*,2S*(2S*,3R*)]]-[3-[[3-[[(1,1-Dimethylethoxy)-carbonyl]amino]-2-hydroxy-4-(4-[2-(2-pyridinyl)ethoxy]phenyl]butyl]amino]-2-hydroxy-1-(phenylmethyl)propyl]carbamic Acid, 1,1-Dimethylethyl Ester
CHEMBL450668 (R)-4-(8-Fluoro-2-oxo-1,2-dihydroquinazolin-3(4H)-yl)-N-(3-(7-methyl-1H-indazol-5-yl)-1-oxo-1-(4-(piperidin-1-yl)piperidin-1-yl)propan-2-yl)piperidine-1-carboxamide BDBM50268484 BMS-694153 (R)-N-(1-(1,4'-bipiperidin-1'-yl)-3-(7-methyl-1H-indazol-5-yl)-1-oxopropan-2-yl)-4-(8-fluoro-2-oxo-1,2-dihydroquinazolin-3(4H)-yl)piperidine-1-carboxamide
[1S-[1R*,2S*(2S*,3R*)]]-[3-[[3[[(1,1-Dimethylethoxy)-carbonyl]amino]-2-hydroxy-4-[4-(2-hydroxy-2-methylpropoxy)phenyl]butyl]amino]-2-hydroxy-1- BDBM677 BMS-186318 analog 14 tert-butyl N-[(2S,3R)-4-{[(2R,3S)-3-{[(tert-butoxy)carbonyl]amino}-2-hydroxy-4-[4-(2-hydroxy-2-methylpropoxy)phenyl]butyl]amino}-3-hydroxy-1-phenylbutan-2-yl]carbamate (phenylmethyl)propyl]carbamic Acid, 1,1-Dimethylethyl Ester
hydroxy-1-(phenylmethyl)propyl]carbamic Acid, 1,1-Dimethylethy Ester [1S-[1R*,2S*(2S*,3R*)]]-[3-[[3-[[(1,1-Dimethylethoamino]-2-hydroxy-4-[4-[3-(4-morpholinyl)-3-oxopropyl]xy)-carbonyl]phenyl]butyl]amino]-2- tert-butyl N-[(2S,3R)-4-{[(2R,3S)-3-{[(tert-butoxy)carbonyl]amino}-2-hydroxy-4-{4-[3-(morpholin-4-yl)-3-oxopropyl]phenyl}butyl]amino}-3-hydroxy-1-phenylbutan-2-yl]carbamate BMS-186318 analog 20 BDBM683
tert-butyl N-[(2S,3R)-4-{[(2R,3S)-3-{[(tert-butoxy)carbonyl]amino}-2-hydroxy-4-{4-[2-(morpholin-4-yl)-2-oxoethoxy]phenyl}butyl]amino}-3-hydroxy-1-phenylbutan-2-yl]carbamate BDBM682 hydroxy-1-(phenylmethyl)]propyl]carbamic Acid, 1,1-Dimethylethyl Ester [1S-[1R*,2S*(2S*,3R*)]]-[3-[[3-[[(1,1-Dimethylethoxy)-carbonyl]amino]-2-hydroxy-4-[4-[2-(4-morpholinyl)-2-oxoethoxyphenyl]butyl]amino]-2- BMS-186318 analog 19
tert-butyl N-[(2S,3R)-4-{[(2R,3S)-3-{[(tert-butoxy)carbonyl]amino}-2-hydroxy-4-{4-[2-(pyridin-3-yloxy)ethoxy]phenyl}butyl]amino}-3-hydroxy-1-phenylbutan-2-yl]carbamate BMS-186318 analog 9 (phenylmethyl)propyl]carbamic Acid, 1,1-Dimethylethyl Ester BDBM672 [1S-[1R*,2S*(2S*, 3R*)]]-[3-[[3-[[(1,1-Dimethylethoxy)carbonyl]amino]-2-hydroxy-4-[4-[2-(3-pyridinyloxy)ethoxy]phenyl]butyl]amino]-2-hydroxy-1-
tert-butyl N-[(2S,3R)-4-{[(2R,3S)-3-{[(tert-butoxy)carbonyl]amino}-2-hydroxy-4-{4-[2-oxo-2-(piperidin-1-yl)ethoxy]phenyl}butyl]amino}-3-hydroxy-1-phenylbutan-2-yl]carbamate BMS-186318 analog 22 BDBM685 [1S-[1R*,2S*(2S*,3R*)]]-[3-[[3-[[(1,1-Dimethylethoxy)-carbonyl]amino]-2-hydroxy-4-[4-(2-piperidinylethoxy)-phenyl]butyl]amino]-2-hydroxy-1-(phenylmethyl)propyl]carbamic Acid, 1,1-Dimethylethyl Ester
(2S,3R)-3-(1-Carbamimidoyl-piperidin-3-ylmethyl)-4-oxo-1-[4-(5-phenyl-pentanoyl)-piperazine-1-carbonyl]-azetidine-2-carboxylic acid BMS-363131 BDBM50120387 CHEMBL303437 (2S,3R)-3-((R)-1-Carbamimidoyl-piperidin-3-ylmethyl)-4-oxo-1-[4-(6-phenyl-hexanoyl)-piperazine-1-carbonyl]-azetidine-2-carboxylic acid (2S,3R)-3-(1-Carbamimidoyl-piperidin-3-ylmethyl)-4-oxo-1-[4-((R)-6-phenyl-hexanoyl)-piperazine-1-carbonyl]-azetidine-2-carboxylic acid
(S)-2-cyano-1-(2-methylbenzofuran-5-yl)-3-(2-oxo-1-(2-oxo-2-(pyrrolidin-1-yl)ethylazepan-3-yl)guanidine BDBM50296258 (S)-2-cyano-1-(2-methylbenzofuran-5-yl)-3-(2-oxo-1-(2-oxo-2-(pyrrolidin-1-yl)ethyl)azepan-3-yl)guanidine 1-cyano-2-(2-methyl-1-benzofuran-5-yl)-3-[(3S)-2-oxo-1-(2-oxo-2-pyrrolidin-1-ylethyl)azepan-3-yl]guanidine BMS-269223 CHEMBL551991
BMS-186318 analog 17 (phenylmethyl)propyl]carbamic Acid, 1,1-Dimethylethylethyl Ester [1S-[1R*,2S*(2S*,3R*)]]-[3-[[3-[[(1,1-Dimethylethoxy)-carbonyl]amino]-2-hydroxy-4-[4-[2-(2-oxo-3-oxazolidinyl)-ethoxy]phenyl]butyl]amino]-2-hydroxy-1- tert-butyl N-[(2S,3R)-4-{[(2R,3S)-3-{[(tert-butoxy)carbonyl]amino}-2-hydroxy-4-{4-[2-(2-oxo-1,3-oxazolidin-3-yl)ethoxy]phenyl}butyl]amino}-3-hydroxy-1-phenylbutan-2-yl]carbamate BDBM680
[1S-[1R*,2S*(2S*,3R*)]]-[3-[[3-[[(1,1-Dimethylethoxy)carbonyl]amino]-2-hydroxy-4-[4-[2-(1H-imidazol-1-yl)ethoxy]phenyl]butyl]amino]-2-hydroxy-1-(phenylmethyl)propyl]carbamic Acid, 1,1-Dimethylethyl Es tert-butyl N-[(2S,3R)-4-{[(2R,3S)-3-{[(tert-butoxy)carbonyl]amino}-2-hydroxy-4-{4-[2-(1H-imidazol-1-yl)ethoxy]phenyl}butyl]amino}-3-hydroxy-1-phenylbutan-2-yl]carbamate BMS-186318 analog 7 BDBM670
tert-butyl N-[(2S,3R)-4-{[(2R,3S)-3-{[(tert-butoxy)carbonyl]amino}-2-hydroxy-4-{4-[2-hydroxy-2-(pyridin-3-yl)ethoxy]phenyl}butyl]amino}-3-hydroxy-1-phenylbutan-2-yl]carbamate [1S-[1R*,2S*(2S*,3R*)]]-[3-[[3-[[(1,1-Dimethylethoxy)-carbonyl]amino]-2-hydroxy-4-[4-[2-hydroxy-2-(3-pyridinyl)ethoxy]phenyl]butyl]amino]-2-hydroxy-1- BMS-186318 analog 10 (phenylmethyl)propyl]carbamic Acid, 1,1-Dimethylethyl Ester BDBM673
BDBM50120368 BMS-262084 (2S,3R)-1-(4-tert-Butylcarbamoyl-piperazine-1-carbonyl)-3-(3-guanidino-propyl)-4-oxo-azetidine-2-carboxylic acid (R)-1-(4-tert-Butylcarbamoyl-piperazine-1-carbonyl)-3-(3-guanidino-propyl)-4-oxo-azetidine-2-carboxylic acid (3S,4R)-1-(4-tert-Butylcarbamoyl-piperazine-1-carbonyl)-3-(3-guanidino-propyl)-4-oxo-azetidine-2-carboxylic acid 1-(4-tert-Butylcarbamoyl-piperazine-1-carbonyl)-3-(3-guanidino-propyl)-4-oxo-azetidine-2-carboxylic acid CHEMBL71037
BMS-186318 analog 18 hydroxy-1-(phenylmethyl)propyl]carbamic Acid, 1,1-Dimethylethyl Ester tert-butyl N-[(2S,3R)-4-{[(2R,3S)-3-{[(tert-butoxy)carbonyl]amino}-2-hydroxy-4-{4-[2-(3-methyl-2-oxoimidazolidin-1-yl)ethoxy]phenyl}butyl]amino}-3-hydroxy-1-phenylbutan-2-yl]carbamate BDBM681 [1S-[1R*,2S*(2S*,3R*)]]-[3-[[3-[[(1,1-Dimethylethoxy)-carbonyl]amino]-2-hydroxy-4-[4-[2-(3-methyl-2-oxo-1-imidazolidinyl)ethoxy]phenyl]butyl]amino]-2-
CGP 73547 methyl N-[(1S)-1-[[(2S,3S)-3-hydroxy-4-[[[(2S)-2-(methoxycarbonylamino)-3,3-dimethyl-butanoyl]amino]-[(4-pyridin-2-ylphenyl)methyl]amino]-1-phenyl-butan-2-yl]carbamoyl]-2,2-dimethyl-propyl]carbamate US10806794, Compound Atazanavir US11938127, Compound atazanavir Atazanavir BDBM13934 Latazanavir BMS 232632 CHEMBL1163 methyl N-[(1S)-1-{[(2S,3S)-3-hydroxy-4-[(2S)-2-[(methoxycarbonyl)amino]-3,3-dimethyl-N'-{[4-(pyridin-2-yl)phenyl]methyl}butanehydrazido]-1-phenylbutan-2-yl]carbamoyl}-2,2-dimethylpropyl]carbamate
3-Benzyl-1-(3H-imidazol-4-ylmethyl)-4-(thiophene-2-sulfonyl)-2,3,4,5-tetrahydro-1H-benzo[e][1,4]diazepine-7-carbonitrile (R)-3-Benzyl-1-(3H-imidazol-4-ylmethyl)-4-(thiophene-2-sulfonyl)-2,3,4,5-tetrahydro-1H-benzo[e][1,4]diazepine-7-carbonitrile CHEMBL351706 BMS-214662 (R)-3-Benzyl-1-(1H-imidazol-4-ylmethyl)-4-(thiophene-2-sulfonyl)-2,3,4,5-tetrahydro-1H-benzo[e][1,4]diazepine-7-carbonitrile 3-BENZYL-1-(1H-IMIDAZOL-4-YLMETHYL)-4-(THIEN-2-YLSULFONYL)-2,3,4,5-TETRAHYDRO-1H-1,4-BENZODIAZEPINE-7-CARBONITRILE BDBM50092365 (R)-1-((1H-imidazol-5-yl)methyl)-3-benzyl-4-(thiophen-2-ylsulfonyl)-2,3,4,5-tetrahydro-1H-benzo[e][1,4]diazepine-7-carbonitrile