General Information of the Protein
Protein ID
PT01021
Protein Name
C-C chemokine receptor type 2
Secondarily
Protein Name
Monocyte chemoattractant protein 1 receptor
Gene Name
CCR2
Secondarily
Gene Name
CMKBR2
Sequence
MLSTSRSRFIRNTNESGEEVTTFFDYDYGAPCHKFDVKQIGAQLLPPLYSLVFIFGFVGNMLVVLILINCKKLKCLTDIYLLNLAISDLLFLITLPLWAHSAANEWVFGNAMCKLFTGLYHIGYFGGIFFIILLTIDRYLAIVHAVFALKARTVTFGVVTSVITWLVAVFASVPGIIFTKCQKEDSVYVCGPYFPRGWNNFHTIMRNILGLVLPLLIMVICYSGILKTLLRCRNEKKRHRAVRVIFTIMIVYFLFWTPYNIVILLNTFQEFFGLSNCESTSQLDQATQVTETLGMTHCCINPIIYAFVGEKFRSLFHIALGCRIAPLQKPVCGGPGVRPGKNVKVTTQGLLDGRGKGKSIGRAPEASLQDKEGA
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Organism
Homo sapiens, Human
Protein Classification
Membrane receptor
>
Family A G protein-coupled receptor
>
Peptide receptor (family A GPCR)
>
Chemokine receptor
>
CC chemokine receptor
Function
Key functional receptor for CCL2 but can also bind CCL7 and CCL12 (PubMed:8146186, PubMed:8048929, PubMed:23408426). Its binding with CCL2 on monocytes and macrophages mediates chemotaxis and migration induction through the activation of the PI3K cascade, the small G protein Rac and lamellipodium protrusion (Probable). Also acts as a receptor for the beta-defensin DEFB106A/DEFB106B (PubMed:23938203). Regulates the expression of T-cell inflammatory cytokines and T-cell differentiation, promoting the differentiation of T-cells into T-helper 17 cells (Th17) during inflammation (By similarity). Facilitates the export of mature thymocytes by enhancing directional movement of thymocytes to sphingosine-1-phosphate stimulation and up-regulation of S1P1R expression; signals through the JAK-STAT pathway to regulate FOXO1 activity leading to an increased expression of S1P1R (By similarity). Plays an important role in mediating peripheral nerve injury-induced neuropathic pain (By similarity). Increases NMDA-mediated synaptic transmission in both dopamine D1 and D2 receptor-containing neurons, which may be caused by MAPK/ERK-dependent phosphorylation of GRIN2B/NMDAR2B (By similarity). Mediates the recruitment of macrophages and monocytes to the injury site following brain injury (By similarity).
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Uniprot ID
Primary ID:
P41597

Secondarily ID:
A0AVQ3
B2RMT0
O95950
Q4VBL2
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Ensembl ID
ENSG00000121807
HGNC ID
HGNC:1603
Subcellular Location
Cell membrane
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000011 , CHO
Compound ID Compound Name Compound Formula
CP0315991
(1S,3R)-N-(3,5-bis(trifluoromethyl)benzyl)-3-(3-ethyl tetrahydro-2H-pyran-4-ylamino)-1-isopropylcyclopentanecarboxamide
   Show/Hide
C25H34F6N2O2
 1
1
IC50 = 0.3 nM
   TI
   LI
   LO
   TS
CP0053417
(1S,3R)-N-(3,5-bis(trifluoromethyl)benzyl)-1-isopropyl-3-(3-(trifluoromethyl)tetrahydro-2H-pyran-4-ylamino)cyclopentanecarboxamide
   Show/Hide
C24H29F9N2O2
 2
1
IC50 = 1 nM
   TI
   LI
   LO
   TS
2
IC50 = 5.5 nM
   TI
   LI
   LO
   TS
CP0425145
(1S,3R)-1-cyclopropyl-N-{[3-fluoro-5-(trifluoromethyl)phenyl]methyl}-3-[(1S,5'R)-5'-methylspiro[indene-1,4'-piperidine]-1'-yl]cyclopentane-1-carboxamide
   Show/Hide
C31H34F4N2O
 1
1
IC50 = 1.9 nM
   TI
   LI
   LO
   TS
CP0390911
(2S)-N-{[3,5-bis(trifluoromethyl)phenyl]methyl}-2-(cyclopropylmethyl)-4-[(1R,5'R)-5'-methylspiro[indene-1,4'-piperidine]-1'-yl]butanamide
   Show/Hide
C31H34F6N2O
 2
1
IC50 = 3 nM
   TI
   LI
   LO
   TS
2
IC50 = 25 nM
   TI
   LI
   LO
   TS
CP0444505
(1S,3R)-N-{[3-fluoro-5-(trifluoromethyl)phenyl]methyl}-3-[(1S,5'R)-5'-methylspiro[indene-1,4'-piperidine]-1'-yl]-1-(propan-2-yl)cyclopentane-1-carboxamide
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C31H36F4N2O
 1
1
IC50 = 3.1 nM
   TI
   LI
   LO
   TS
CP0437369
1-ethyl-N-{[3-fluoro-5-(trifluoromethyl)phenyl]methyl}-3-[(1S,5'R)-5'-methylspiro[indene-1,4'-piperidine]-1'-yl]cyclopentane-1-carboxamide
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C30H34F4N2O
 1
1
IC50 = 3.3 nM
   TI
   LI
   LO
   TS
CP0900717
(1S,3R)-N-(3,5-bis(trifluoromethyl)benzyl)-1-isopropyl-3-(oxetan-3-ylamino)cyclopentanecarboxamide trifluoroacetate salt
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C23H27F9N2O4
 1
1
IC50 = 3.3 nM
   TI
   LI
   LO
   TS
CP0525772
(1R,3R)-N-{[3-fluoro-5-(trifluoromethyl)phenyl]methyl}-3-[(1S,5'R)-5'-methylspiro[indene-1,4'-piperidine]-1'-yl]-1-[(methylsulfanyl)methyl]cyclopentane-1-carboxamide
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C30H34F4N2OS
 1
1
IC50 = 3.5 nM
   TI
   LI
   LO
   TS
CP0428650
(1R,3R)-N-{[3-fluoro-5-(trifluoromethyl)phenyl]methyl}-1-(2-methylpropyl)-3-[(1S,5'R)-5'-methylspiro[indene-1,4'-piperidine]-1'-yl]cyclopentane-1-carboxamide
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C32H38F4N2O
 1
1
IC50 = 3.9 nM
   TI
   LI
   LO
   TS
CP0373631
(1S,3R)-N-{[3-fluoro-5-(trifluoromethyl)phenyl]methyl}-1-methyl-3-[(1S,5'R)-5'-methylspiro[indene-1,4'-piperidine]-1'-yl]cyclopentane-1-carboxamide
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C29H32F4N2O
 1
1
IC50 = 4 nM
   TI
   LI
   LO
   TS
CP0041927
(2S)-N-[3,5-bis(trifluoromethyl)benzyl]-2-cyclopropyl-4-[(1R,3R')-3'methyl-1'H-spiro[indene-1,4'-piperidin]-1'yl]butanamide
   Show/Hide
C30H32F6N2O
 2
1
IC50 = 4 nM
   TI
   LI
   LO
   TS
2
IC50 = 14 nM
   TI
   LI
   LO
   TS
CP0165577
(1S,3R)-N-(3,5-bis(trifluoromethyl)benzyl)-1-isopropyl-3-(tetrahydro-2H-pyran-4-ylamino)cyclopentanecarboxamide
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C23H30F6N2O2
 1
1
IC50 = 4.6 nM
   TI
   LI
   LO
   TS
CP0522581
N-[[3-fluoro-5-(trifluoromethyl)phenyl]methyl]-3-[(1S,3'R)-3'-methylspiro[indene-1,4'-piperidine]-1'-yl]-1-propylcyclopentane-1-carboxamide
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C31H36F4N2O
 1
1
IC50 = 5 nM
   TI
   LI
   LO
   TS
CP0522786
(1S,3R)-N-(3,5-bis(trifluoromethyl)benzyl)-1-isopropyl-3-(3-propyltetrahydro-2H-pyran-4-ylamino)cyclopentanecarboxamide
   Show/Hide
C26H36F6N2O2
 2
1
IC50 = 5.1 nM
   TI
   LI
   LO
   TS
2
IC50 = 7.8 nM
   TI
   LI
   LO
   TS
CP0425146
1-(cyclopropylmethyl)-N-{[3-fluoro-5-(trifluoromethyl)phenyl]methyl}-3-[(1S,5'R)-5'-methylspiro[indene-1,4'-piperidine]-1'-yl]cyclopentane-1-carboxamide
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C32H36F4N2O
 1
1
IC50 = 5.5 nM
   TI
   LI
   LO
   TS
CP0871032
CENICRIVIROC MESYLATE
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C42H56N4O7S2
 1
1
IC50 = 5.9 nM
   TI
   LI
   LO
   TS
CP0535185
N-[[3,5-bis(trifluoromethyl)phenyl]methyl]-1-cyclopropyl-3-[(1S,3'R)-3'-methylspiro[indene-1,4'-piperidine]-1'-yl]cyclopentane-1-carboxamide
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C32H34F6N2O
 1
1
IC50 = 6.5 nM
   TI
   LI
   LO
   TS
CP0053416
(1S,3R)-N-(3,5-bis(trifluoromethyl)benzyl)-3-(3,5-dimethyltetrahydro-2H-pyran-4-ylamino)-1-isopropylcyclopentanecarboxamide
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C25H34F6N2O2
 1
1
IC50 = 7 nM
   TI
   LI
   LO
   TS
CP0442366
(1S,3R)-N-{[3,5-bis(trifluoromethyl)phenyl]methyl}-3-[(1S,5'R)-5'-methylspiro[indene-1,4'-piperidine]-1'-yl]-1-(propan-2-yl)cyclopentane-1-carboxamide
   Show/Hide
C32H36F6N2O
 1
1
IC50 = 7.6 nM
   TI
   LI
   LO
   TS
CP0496763
(S)-N-(3,5-bis(trifluoromethyl)benzyl)-2-((3-(dimethylamino)propyl)(methyl)amino)-2-phenylacetamide
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C23H27F6N3O
 1
1
IC50 = 8 nM
   TI
   LI
   LO
   TS
CP0437367
(1R,3R)-N-{[3,5-bis(trifluoromethyl)phenyl]methyl}-1-(2-methylpropyl)-3-[(1S,5'R)-5'-methylspiro[indene-1,4'-piperidine]-1'-yl]cyclopentane-1-carboxamide
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C33H38F6N2O
 1
1
IC50 = 8 nM
   TI
   LI
   LO
   TS
CP0522580
N-[[3-fluoro-5-(trifluoromethyl)phenyl]methyl]-1-(methoxymethyl)-3-[(1S,3'R)-3'-methylspiro[indene-1,4'-piperidine]-1'-yl]cyclopentane-1-carboxamide
   Show/Hide
C30H34F4N2O2
 1
1
IC50 = 8.5 nM
   TI
   LI
   LO
   TS
CP0437368
(1S,3R)-N-{[3,5-bis(trifluoromethyl)phenyl]methyl}-1-methyl-3-[(1S,5'R)-5'-methylspiro[indene-1,4'-piperidine]-1'-yl]cyclopentane-1-carboxamide
   Show/Hide
C30H32F6N2O
 1
1
IC50 = 9 nM
   TI
   LI
   LO
   TS
CP0920191
(S)-N-(3,5-bis(trifluoromethyl)benzyl)-2-(3-(dimethylamino)propylideneamino)-2-phenylacetamide
   Show/Hide
C22H23F6N3O
 1
1
IC50 = 10 nM
   TI
   LI
   LO
   TS
CP0428649
N-[[3,5-bis(trifluoromethyl)phenyl]methyl]-1-ethyl-3-[(1S,3'R)-3'-methylspiro[indene-1,4'-piperidine]-1'-yl]cyclopentane-1-carboxamide
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C31H34F6N2O
 1
1
IC50 = 10 nM
   TI
   LI
   LO
   TS
CP0395332
(2S)-N-{[3,5-bis(trifluoromethyl)phenyl]methyl}-2-cyclobutyl-4-[(1R,5'R)-5'-methylspiro[indene-1,4'-piperidine]-1'-yl]butanamide
   Show/Hide
C31H34F6N2O
 2
1
IC50 = 11 nM
   TI
   LI
   LO
   TS
2
IC50 = 28 nM
   TI
   LI
   LO
   TS
CP0428042
(S)-N-(3,5-bis(trifluoromethyl)benzyl)-5-(dimethylamino)-2-phenylpentanamide
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C22H24F6N2O
 1
1
IC50 = 13 nM
   TI
   LI
   LO
   TS
CP0428698
(1R,3R)-N-{[3,5-bis(trifluoromethyl)phenyl]methyl}-3-[(1S,5'R)-5'-methylspiro[indene-1,4'-piperidine]-1'-yl]-1-[(methylsulfanyl)methyl]cyclopentane-1-carboxamide
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C31H34F6N2OS
 1
1
IC50 = 13 nM
   TI
   LI
   LO
   TS
CP0535186
N-[[3,5-bis(trifluoromethyl)phenyl]methyl]-1-(methoxymethyl)-3-[(1S,3'R)-3'-methylspiro[indene-1,4'-piperidine]-1'-yl]cyclopentane-1-carboxamide
   Show/Hide
C31H34F6N2O2
 1
1
IC50 = 15.5 nM
   TI
   LI
   LO
   TS
CP0420176
(1S,3R)-N-{[3,5-bis(trifluoromethyl)phenyl]methyl}-3-[(1S,5'R)-5'-methylspiro[indene-1,4'-piperidine]-1'-yl]-1-propylcyclopentane-1-carboxamide
   Show/Hide
C32H36F6N2O
 1
1
IC50 = 16 nM
   TI
   LI
   LO
   TS
CP0507891
US8906911, 64
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C26H35F3N4O2
 2
1
IC50 = 16.5 nM
   TI
   LI
   LO
   TS
2
Ki = 12 nM
   TI
   LI
   LO
   TS
CP0565604
US8906911, 46
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C27H35ClF3N3O3
 2
1
IC50 = 17.6 nM
   TI
   LI
   LO
   TS
2
Ki = 17 nM
   TI
   LI
   LO
   TS
CP0428169
US8906911, 63
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C26H35F3N4O2
 2
1
IC50 = 17.9 nM
   TI
   LI
   LO
   TS
2
Ki = 10 nM
   TI
   LI
   LO
   TS
CP0428648
(1R,3R)-N-{[3,5-bis(trifluoromethyl)phenyl]methyl}-1-(cyclobutylmethyl)-3-[(1S,5'R)-5'-methylspiro[indene-1,4'-piperidine]-1'-yl]cyclopentane-1-carboxamide
   Show/Hide
C34H38F6N2O
 1
1
IC50 = 19 nM
   TI
   LI
   LO
   TS
CP0518546
US8906911, 28
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C28H35F3N4O3
 2
1
IC50 = 19.8 nM
   TI
   LI
   LO
   TS
2
Ki = 32 nM
   TI
   LI
   LO
   TS
CP0427178
N-[[3,5-bis(trifluoromethyl)phenyl]methyl]-1-(cyclopropylmethyl)-3-[(1S,3'R)-3'-methylspiro[indene-1,4'-piperidine]-1'-yl]cyclopentane-1-carboxamide
   Show/Hide
C33H36F6N2O
 1
1
IC50 = 20 nM
   TI
   LI
   LO
   TS
CP0440375
(1S,3R)-N-{[3,5-bis(trifluoromethyl)phenyl]methyl}-3-[(1S,5'R)-5'-methylspiro[indene-1,4'-piperidine]-1'-yl]cyclopentane-1-carboxamide
   Show/Hide
C29H30F6N2O
 1
1
IC50 = 20 nM
   TI
   LI
   LO
   TS
CP0238399
(1S,3R)-N-(3,5-bis(trifluoromethyl)benzyl)-1-isopropyl-3-(tetrahydro-2H-thiopyran-4-ylamino)cyclopentanecarboxamide
   Show/Hide
C23H30F6N2OS
 1
1
IC50 = 22 nM
   TI
   LI
   LO
   TS
CP0496758
(S)-N-(3,5-bis(trifluoromethyl)benzyl)-2-(2-(dimethylamino)ethylthio)-2-phenylacetamide
   Show/Hide
C21H22F6N2OS
 1
1
IC50 = 25 nM
   TI
   LI
   LO
   TS
CP0562154
US8906911, 50
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C28H35F6N3O3
 2
1
IC50 = 25.9 nM
   TI
   LI
   LO
   TS
2
Ki = 78 nM
   TI
   LI
   LO
   TS
CP0373628
N-[[3-fluoro-5-(trifluoromethyl)phenyl]methyl]-1-hexyl-3-[(1S,3'R)-3'-methylspiro[indene-1,4'-piperidine]-1'-yl]cyclopentane-1-carboxamide
   Show/Hide
C34H42F4N2O
 1
1
IC50 = 27 nM
   TI
   LI
   LO
   TS
CP0666580
Dimethyl-(tetrahydro-pyran-4-yl)-{4-[(3-p-tolyl-8,9-dihydro-7H-benzocycloheptene-6-carbonyl)-amino]-benzyl}-ammonium chloride(TAK-779)
   Show/Hide
C33H39ClN2O2
 3
1
IC50 = 27 nM
   TI
   LI
   LO
   TS
2
IC50 = 28 nM
   TI
   LI
   LO
   TS
3
Ki = 4.169 nM
   TI
   LI
   LO
   TS
CP0433968
(1R,3R)-N-{[3,5-bis(trifluoromethyl)phenyl]methyl}-3-[(1S,5'R)-5'-methylspiro[indene-1,4'-piperidine]-1'-yl]-1-(methylsulfanyl)cyclopentane-1-carboxamide
   Show/Hide
C30H32F6N2OS
 1
1
IC50 = 28 nM
   TI
   LI
   LO
   TS
CP0467606
(1S,3R)-N-(3,5-bis(trifluoromethyl)benzyl)-1-isopropyl-3-(2-methyltetrahydro-2H-pyran-4-ylamino)cyclopentanecarboxamide
   Show/Hide
C24H32F6N2O2
 1
1
IC50 = 28 nM
   TI
   LI
   LO
   TS
CP0468216
US8906911, 65
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C27H37F3N4O2
 2
1
IC50 = 28 nM
   TI
   LI
   LO
   TS
2
Ki = 6 nM
   TI
   LI
   LO
   TS
CP0302119
(1S,3R)-N-(3,5-bis(trifluoromethyl)benzyl)-1-isopropyl-3-(oxepan-4-ylamino)cyclopentanecarboxamide
   Show/Hide
C24H32F6N2O2
 1
1
IC50 = 30 nM
   TI
   LI
   LO
   TS
CP0532438
1'-{2-[2-(4-fluorophenyl)-1,3-oxazol-4-yl]ethyl}-6-methyl-1,2-dihydrospiro[3,1-benzoxazine-4,4'-piperidine]-2-one
   Show/Hide
C24H24FN3O3
 1
1
IC50 = 32 nM
   TI
   LI
   LO
   TS
CP0515439
US8906911, 6
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C25H34F3N5O3
 2
1
IC50 = 32.8 nM
   TI
   LI
   LO
   TS
2
Ki = 28 nM
   TI
   LI
   LO
   TS
CP0562153
US8906911, 15
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C27H35F4N3O3
 2
1
IC50 = 34.7 nM
   TI
   LI
   LO
   TS
2
Ki = 29 nM
   TI
   LI
   LO
   TS
CP0315992
(1S,3R)-N-(3,5-bis(trifluoromethyl)benzyl)-1-isopropyl-3-(tetrahydrothiophen-3-ylamino)cyclopentanecarboxamide
   Show/Hide
C22H28F6N2OS
 1
1
IC50 = 36 nM
   TI
   LI
   LO
   TS
CP0557635
US8906911, 49
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C31H37F3N4O
 2
1
IC50 = 37 nM
   TI
   LI
   LO
   TS
2
Ki = 15 nM
   TI
   LI
   LO
   TS
CP0145835
(S)-N-(3,5-bis(trifluoromethyl)benzyl)-2-(2-(piperidin-1-yl)ethylamino)-2-(thiophen-3-yl)acetamide
   Show/Hide
C22H25F6N3OS
 1
1
IC50 = 39 nM
   TI
   LI
   LO
   TS
CP0400725
US8906911, 40
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C26H35Cl2N3O3
 2
1
IC50 = 41.5 nM
   TI
   LI
   LO
   TS
2
Ki = 38 nM
   TI
   LI
   LO
   TS
CP0468205
US8906911, 14
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C27H35F4N3O3
 2
1
IC50 = 43 nM
   TI
   LI
   LO
   TS
2
Ki = 31 nM
   TI
   LI
   LO
   TS
CP0563848
US8906911, 51
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C28H37ClF3N3O3
 2
1
IC50 = 43.3 nM
   TI
   LI
   LO
   TS
2
Ki = 21 nM
   TI
   LI
   LO
   TS
CP0538110
(2S)-N-{[3,5-bis(trifluoromethyl)phenyl]methyl}-2-(4-fluorophenyl)-4-{5'-methylspiro[indene-1,4'-piperidine]-1'-yl}butanamide
   Show/Hide
C33H31F7N2O
 1
1
IC50 = 45 nM
   TI
   LI
   LO
   TS
CP0561490
US8906911, 66
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C27H37F3N4O2
 2
1
IC50 = 45.8 nM
   TI
   LI
   LO
   TS
2
Ki = 13 nM
   TI
   LI
   LO
   TS
CP0507889
US8906911, 56
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C29H37F3N4O3
 2
1
IC50 = 46 nM
   TI
   LI
   LO
   TS
2
Ki = 32 nM
   TI
   LI
   LO
   TS
CP0516781
US8906911, 53
   Show/Hide
C29H37F3N4O3
 2
1
IC50 = 47.9 nM
   TI
   LI
   LO
   TS
2
Ki = 16 nM
   TI
   LI
   LO
   TS
CP0507888
US8906911, 47
   Show/Hide
C27H35ClN4O3
 2
1
IC50 = 49.8 nM
   TI
   LI
   LO
   TS
2
Ki = 77 nM
   TI
   LI
   LO
   TS
CP0165576
(1S,3R)-N-(3,5-bis(trifluoromethyl)benzyl)-3-(3-hydroxytetrahydro-2H-pyran-4-ylamino)-1-isopropylcyclopentanecarboxamide
   Show/Hide
C23H30F6N2O3
 1
1
IC50 = 51 nM
   TI
   LI
   LO
   TS
CP0516780
US8906911, 48
   Show/Hide
C33H37F3N4O
 2
1
IC50 = 51.8 nM
   TI
   LI
   LO
   TS
2
Ki = 8 nM
   TI
   LI
   LO
   TS
CP0518544
US8906911, 1
   Show/Hide
C26H35F3N4O3
 2
1
IC50 = 54.9 nM
   TI
   LI
   LO
   TS
2
Ki = 32 nM
   TI
   LI
   LO
   TS
CP0517169
US8906911, 39
   Show/Hide
C28H35F3N4O3
 2
1
IC50 = 55.3 nM
   TI
   LI
   LO
   TS
2
Ki = 66 nM
   TI
   LI
   LO
   TS
CP0514673
(1S,3R)-N-(3,5-bis(trifluoromethyl)benzyl)-1-isopropyl-3-(tetrahydro-2H-pyran-3-ylamino)cyclopentanecarboxamide
   Show/Hide
C23H30F6N2O2
 1
1
IC50 = 56 nM
   TI
   LI
   LO
   TS
CP0285420
(2S)-N-{[3,5-bis(trifluoromethyl)phenyl]methyl}-2-(4-fluorophenyl)-4-[(1R,5'R)-5'-methylspiro[indene-1,4'-piperidine]-1'-yl]butanamide
   Show/Hide
C33H31F7N2O
 2
1
IC50 = 59 nM
   TI
   LI
   LO
   TS
2
IC50 = 67 nM
   TI
   LI
   LO
   TS
CP0165578
(1S,3R)-N-(3,5-bis(trifluoromethyl)benzyl)-3-(cyclohexylamino)-1-isopropylcyclopentanecarboxamide
   Show/Hide
C24H32F6N2O
 1
1
IC50 = 64 nM
   TI
   LI
   LO
   TS
CP0561511
US8906911, 7
   Show/Hide
C27H37F3N4O3
 2
1
IC50 = 65.7 nM
   TI
   LI
   LO
   TS
2
Ki = 30 nM
   TI
   LI
   LO
   TS
CP0505434
(1R,3R)-N-{[3-fluoro-5-(trifluoromethyl)phenyl]methyl}-3-[(1S,5'R)-5'-methylspiro[indene-1,4'-piperidine]-1'-yl]-1-(methylsulfanyl)cyclopentane-1-carboxamide
   Show/Hide
C29H32F4N2OS
 1
1
IC50 = 67 nM
   TI
   LI
   LO
   TS
CP0390625
N-[[3,5-bis(trifluoromethyl)phenyl]methyl]-2-cyclopropyl-4-spiro[indene-1,4'-piperidine]-1'-ylbutanamide
   Show/Hide
C29H30F6N2O
 1
1
IC50 = 69 nM
   TI
   LI
   LO
   TS
CP0419277
US8906911, 18
   Show/Hide
C27H36F3N3O3
 2
1
IC50 = 76.4 nM
   TI
   LI
   LO
   TS
2
Ki = 207 nM
   TI
   LI
   LO
   TS
CP0562152
US8906911, 2
   Show/Hide
C26H35F3N4O3
 2
1
IC50 = 76.7 nM
   TI
   LI
   LO
   TS
2
Ki = 60 nM
   TI
   LI
   LO
   TS
CP0331716
(1S,3R)-N-(3,5-bis(trifluoromethyl)benzyl)-3-(2,3-dihydro-1H-inden-1-ylamino)-1-isopropylcyclopentanecarboxamide
   Show/Hide
C27H30F6N2O
 1
1
IC50 = 77 nM
   TI
   LI
   LO
   TS
CP0277808
(2S)-N-[3,5-bis(trifluoromethyl)benzyl]-2-(4-fluorophenyl)-4-(1'H-spiro[indene-1,4'-piperidin]-1'yl)butanamide
   Show/Hide
C32H29F7N2O
 1
1
IC50 = 80 nM
   TI
   LI
   LO
   TS
CP0467334
(2R)-N-{[3,5-bis(trifluoromethyl)phenyl]methyl}-2-cyclopropyl-4-[(1R,5'R)-5'-methylspiro[indene-1,4'-piperidine]-1'-yl]butanamide
   Show/Hide
C30H32F6N2O
 1
1
IC50 = 80 nM
   TI
   LI
   LO
   TS
CP0428168
US8906911, 52
   Show/Hide
C29H37F6N3O3
 2
1
IC50 = 83.9 nM
   TI
   LI
   LO
   TS
2
Ki = 49 nM
   TI
   LI
   LO
   TS
CP0315993
(1S,3R)-N-(3,5-bis(trifluoromethyl)benzyl)-1-isopropyl-3-(tetrahydrofuran-3-ylamino)cyclopentanecarboxamide
   Show/Hide
C22H28F6N2O2
 1
1
IC50 = 85 nM
   TI
   LI
   LO
   TS
CP0532188
US8906911, 25
   Show/Hide
C27H35F4N3O3
 2
1
IC50 = 92.2 nM
   TI
   LI
   LO
   TS
2
Ki = 271 nM
   TI
   LI
   LO
   TS
CP0513407
US8906911, 30
   Show/Hide
C24H33F3N4O3S
 2
1
IC50 = 95.5 nM
   TI
   LI
   LO
   TS
2
Ki = 831 nM
   TI
   LI
   LO
   TS
CP0485249
(2S)-N-{[3,5-bis(trifluoromethyl)phenyl]methyl}-2-cyclopropyl-4-{spiro[indene-1,4'-piperidine]-1'-yl}butanamide
   Show/Hide
C29H30F6N2O
 1
1
IC50 = 98 nM
   TI
   LI
   LO
   TS
CP0517482
US8906911, 61
   Show/Hide
C26H35F3N4O2
 2
1
IC50 = 100 nM
   TI
   LI
   LO
   TS
2
Ki = 69 nM
   TI
   LI
   LO
   TS
CP0468206
US8906911, 16
   Show/Hide
C28H38F3N3O3
 2
1
IC50 = 106 nM
   TI
   LI
   LO
   TS
2
Ki = 199 nM
   TI
   LI
   LO
   TS
CP0527600
(2S)-N-{[3,5-bis(trifluoromethyl)phenyl]methyl}-2-(4-fluorophenyl)-4-[(1S,5'S)-5'-methylspiro[indene-1,4'-piperidine]-1'-yl]butanamide
   Show/Hide
C33H31F7N2O
 1
1
IC50 = 120 nM
   TI
   LI
   LO
   TS
CP0388120
(1S,3R)-N-(3,5-bis(trifluoromethyl)benzyl)-3-(3-cyclopropyltetrahydro-2H-pyran-4-ylamino)-1-isopropylcyclopentanecarboxamide
   Show/Hide
C26H34F6N2O2
 1
1
IC50 = 123 nM
   TI
   LI
   LO
   TS
CP0443065
N-[[3,5-bis(trifluoromethyl)phenyl]methyl]-4-spiro[indene-1,4'-piperidine]-1'-yl-2-(trifluoromethylsulfonylamino)butanamide
   Show/Hide
C27H26F9N3O3S
 1
1
IC50 = 125 nM
   TI
   LI
   LO
   TS
CP0386030
(R)-N-(3,5-bis(trifluoromethyl)benzyl)-2-(2-(4-phenylpiperidin-1-yl)ethyl)pentanamide
   Show/Hide
C27H32F6N2O
 1
1
IC50 = 126 nM
   TI
   LI
   LO
   TS
CP0522378
(2S)-N-[[3,5-bis(trifluoromethyl)phenyl]methyl]-2-(4-fluorophenyl)-4-[(3R,4S)-3-methyl-4-phenylpiperidin-1-yl]butan-1-amine
   Show/Hide
C31H33F7N2
 1
1
IC50 = 140 nM
   TI
   LI
   LO
   TS
CP0513440
US8906911, 5
   Show/Hide
C25H34F3N5O3
 2
1
IC50 = 140 nM
   TI
   LI
   LO
   TS
2
Ki = 104 nM
   TI
   LI
   LO
   TS
CP0468208
US8906911, 29
   Show/Hide
C27H36F3N3O4
 2
1
IC50 = 148 nM
   TI
   LI
   LO
   TS
2
Ki = 473 nM
   TI
   LI
   LO
   TS
CP0171015
(2S)-N-(3,5-bis(trifluoromethyl)benzyl)-2-(4-fluorophenyl)-4-(4-phenylpiperidin-1-yl)butanamide
   Show/Hide
C30H29F7N2O
 1
1
IC50 = 150 nM
   TI
   LI
   LO
   TS
CP0532187
US8906911, 22
   Show/Hide
C26H35F3N4O3
 2
1
IC50 = 153 nM
   TI
   LI
   LO
   TS
2
Ki = 120 nM
   TI
   LI
   LO
   TS
CP0340173
(1S,3R)-N-(3,5-bis(trifluoromethyl)benzyl)-3-(cyclopentylamino)-1-isopropylcyclopentanecarboxamide
   Show/Hide
C23H30F6N2O
 1
1
IC50 = 156 nM
   TI
   LI
   LO
   TS
CP0441645
(S)-N-(3,5-bis(trifluoromethyl)benzyl)-2-(4-fluorophenyl)-4-(4-(thiophen-3-yl)piperidin-1-yl)butanamide
   Show/Hide
C28H27F7N2OS
 1
1
IC50 = 160 nM
   TI
   LI
   LO
   TS
CP0376674
N-[[3,5-bis(trifluoromethyl)phenyl]methyl]-2-cyclohexyl-4-spiro[indene-1,4'-piperidine]-1'-ylbutanamide
   Show/Hide
C32H36F6N2O
 1
1
IC50 = 160 nM
   TI
   LI
   LO
   TS
CP0428073
N-[[3,5-bis(trifluoromethyl)phenyl]methyl]-4-[(1R,3'R)-3'-methylspiro[indene-1,4'-piperidine]-1'-yl]butanamide
   Show/Hide
C27H28F6N2O
 1
1
IC50 = 173 nM
   TI
   LI
   LO
   TS
CP0512376
(S)-N-(3,5-bis(trifluoromethyl)benzyl)-2-(4-fluorophenyl)-2-(2-(piperidin-1-yl)ethylamino)acetamide
   Show/Hide
C24H26F7N3O
 2
1
IC50 = 175 nM
   TI
   LI
   LO
   TS
2
IC50 = 180 nM
   TI
   LI
   LO
   TS
CP0481537
(1S,3R)-N-(3,5-bis(trifluoromethyl)benzyl)-3-(cycloheptylamino)-1-isopropylcyclopentanecarboxamide
   Show/Hide
C25H34F6N2O
 1
1
IC50 = 175 nM
   TI
   LI
   LO
   TS
CP0555435
US8906911, 20
   Show/Hide
C26H35ClFN3O3
 2
1
IC50 = 182 nM
   TI
   LI
   LO
   TS
2
Ki = 112 nM
   TI
   LI
   LO
   TS
CP0468412
(1S,3R)-N-(3,5-bis(trifluoromethyl)benzyl)-3-(2,3-dihydro-1H-inden-2-ylamino)-1-isopropylcyclopentanecarboxamide
   Show/Hide
C27H30F6N2O
 1
1
IC50 = 187 nM
   TI
   LI
   LO
   TS
CP0467333
(2R)-N-{[3,5-bis(trifluoromethyl)phenyl]methyl}-2-(2-{spiro[indene-1,4'-piperidine]-1'-yl}ethyl)pent-4-enamide
   Show/Hide
C29H30F6N2O
 1
1
IC50 = 193 nM
   TI
   LI
   LO
   TS
CP0282451
(1S,3R)-N-(3,5-bis(trifluoromethyl)benzyl)-3-(cyclobutylamino)-1-isopropylcyclopentanecarboxamide
   Show/Hide
C22H28F6N2O
 1
1
IC50 = 193 nM
   TI
   LI
   LO
   TS
CP0565014
US8906911, 12
   Show/Hide
C25H34F3N5O3
 2
1
IC50 = 194 nM
   TI
   LI
   LO
   TS
2
Ki = 261 nM
   TI
   LI
   LO
   TS
CP0505625
2-amino-N-[2-[[1-[(4-chlorophenyl)methyl]piperidin-4-yl]methylamino]-2-oxoethyl]-5-(trifluoromethyl)benzamide
   Show/Hide
C23H26ClF3N4O2
 1
1
IC50 = 200 nM
   TI
   LI
   LO
   TS
CP0536582
(2S)-N-{[3,5-bis(trifluoromethyl)phenyl]methyl}-3-methyl-2-(2-{spiro[indene-1,4'-piperidine]-1'-yl}ethyl)butanamide
   Show/Hide
C29H32F6N2O
 1
1
IC50 = 204 nM
   TI
   LI
   LO
   TS
CP0522282
(S)-N-(3,5-bis(trifluoromethyl)benzyl)-2-phenyl-2-(2-(piperidin-1-yl)ethylamino)acetamide
   Show/Hide
C24H27F6N3O
 2
1
IC50 = 219 nM
   TI
   LI
   LO
   TS
2
IC50 = 220 nM
   TI
   LI
   LO
   TS
CP0493802
(1S,3R)-N-(3,5-bis(trifluoromethyl)benzyl)-3-(3,3-dimethyltetrahydro-2H-pyran-4-ylamino)-1-isopropylcyclopentanecarboxamide
   Show/Hide
C25H34F6N2O2
 1
1
IC50 = 230 nM
   TI
   LI
   LO
   TS
CP0433969
N-[[3,5-bis(trifluoromethyl)phenyl]methyl]-1-hexyl-3-[(1S,3'R)-3'-methylspiro[indene-1,4'-piperidine]-1'-yl]cyclopentane-1-carboxamide
   Show/Hide
C35H42F6N2O
 1
1
IC50 = 231 nM
   TI
   LI
   LO
   TS
CP0536581
(2R)-N-{[3,5-bis(trifluoromethyl)phenyl]methyl}-2-methyl-4-{spiro[indene-1,4'-piperidine]-1'-yl}butanamide
   Show/Hide
C27H28F6N2O
 1
1
IC50 = 231 nM
   TI
   LI
   LO
   TS
CP0518545
US8906911, 19
   Show/Hide
C28H38F3N3O3
 2
1
IC50 = 233 nM
   TI
   LI
   LO
   TS
2
Ki = 306 nM
   TI
   LI
   LO
   TS
CP0459575
(1S,3R)-N-(3,5-bis(trifluoromethyl)benzyl)-1-isopropyl-3-(1,2,3,4-tetrahydronaphthalen-2-ylamino)cyclopentanecarboxamide
   Show/Hide
C28H32F6N2O
 1
1
IC50 = 239 nM
   TI
   LI
   LO
   TS
CP0541313
N-[[3,5-bis(trifluoromethyl)phenyl]methyl]-2-(methanesulfonamido)-4-spiro[indene-1,4'-piperidine]-1'-ylbutanamide
   Show/Hide
C27H29F6N3O3S
 1
1
IC50 = 244 nM
   TI
   LI
   LO
   TS
CP0453043
(S)-N-(3,5-bis(trifluoromethyl)benzyl)-2-cyclopropyl-4-(4-(4-fluorophenyl)piperidin-1-yl)butanamide
   Show/Hide
C27H29F7N2O
 1
1
IC50 = 280 nM
   TI
   LI
   LO
   TS
CP0456460
(S)-N-(3,5-bis(trifluoromethyl)benzyl)-2-cyclopropyl-4-(4-phenylpiperidin-1-yl)butanamide
   Show/Hide
C27H30F6N2O
 1
1
IC50 = 285 nM
   TI
   LI
   LO
   TS
CP0439634
2-benzyl-N-{[3,5-bis(trifluoromethyl)phenyl]methyl}-4-{spiro[indene-1,4'-piperidine]-1'-yl}butanamide
   Show/Hide
C33H32F6N2O
 1
1
IC50 = 298 nM
   TI
   LI
   LO
   TS
CP0518547
US8906911, 36
   Show/Hide
C28H35F3N4O3
 2
1
IC50 = 305 nM
   TI
   LI
   LO
   TS
2
Ki = 1060 nM
   TI
   LI
   LO
   TS
CP0468210
US8906911, 32
   Show/Hide
C26H34ClF3N4O3
 2
1
IC50 = 314 nM
   TI
   LI
   LO
   TS
2
Ki = 1060 nM
   TI
   LI
   LO
   TS
CP0496914
(2S)-N-{[3,5-bis(trifluoromethyl)phenyl]methyl}-4-{2,3-dihydrospiro[indene-1,4'-piperidine]-1'-yl}-2-(4-fluorophenyl)butanamide
   Show/Hide
C32H31F7N2O
 1
1
IC50 = 320 nM
   TI
   LI
   LO
   TS
CP0468214
US8906911, 60
   Show/Hide
C25H41N3O5
 2
1
IC50 = 328 nM
   TI
   LI
   LO
   TS
2
Ki = 552 nM
   TI
   LI
   LO
   TS
CP0428041
N-[[3,5-bis(trifluoromethyl)phenyl]methyl]-2-phenyl-2-(2-piperidin-1-ylethylamino)acetamide
   Show/Hide
C24H27F6N3O
 1
1
IC50 = 342 nM
   TI
   LI
   LO
   TS
CP0394052
(2R)-N-{[3,5-bis(trifluoromethyl)phenyl]methyl}-3-methyl-2-(2-{spiro[indene-1,4'-piperidine]-1'-yl}ethyl)butanamide
   Show/Hide
C29H32F6N2O
 1
1
IC50 = 349 nM
   TI
   LI
   LO
   TS
CP0119832
(1S,3R)-N-(3,5-bis(trifluoromethyl)benzyl)-1-isopropyl-3-((tetrahydro-2H-pyran-4-yl)methylamino)cyclopentanecarboxamide
   Show/Hide
C24H32F6N2O2
 1
1
IC50 = 362 nM
   TI
   LI
   LO
   TS
CP0466639
US8906911, 27
   Show/Hide
C25H34F3N5O3
 2
1
IC50 = 391 nM
   TI
   LI
   LO
   TS
2
Ki = 444 nM
   TI
   LI
   LO
   TS
CP0464513
(S)-N-(3,5-bis(trifluoromethyl)benzyl)-2-(2-(azepan-1-yl)ethylamino)-2-phenylacetamide
   Show/Hide
C25H29F6N3O
 1
1
IC50 = 400 nM
   TI
   LI
   LO
   TS
CP0262145
(1S,3R)-N-(3,5-bis(trifluoromethyl)benzyl)-3-(chroman-4-ylamino)-1-isopropylcyclopentanecarboxamide
   Show/Hide
C27H30F6N2O2
 1
1
IC50 = 419 nM
   TI
   LI
   LO
   TS
CP0449525
(S)-N-(3,5-bis(trifluoromethyl)benzyl)-2-(2-(dimethylamino)ethylamino)-2-(thiophen-3-yl)acetamide
   Show/Hide
C19H21F6N3OS
 1
1
IC50 = 424 nM
   TI
   LI
   LO
   TS
CP0390994
(2S)-N-{[3,5-bis(trifluoromethyl)phenyl]methyl}-4-[(1R,3'R)-3'-ethylspiro[indene-1,4'-piperidine]-1'-yl]-2-(4-fluorophenyl)butanamide
   Show/Hide
C34H33F7N2O
 1
1
IC50 = 437 nM
   TI
   LI
   LO
   TS
CP0422297
(2S)-N-{[3,5-bis(trifluoromethyl)phenyl]methyl}-4-{5'-ethylspiro[indene-1,4'-piperidine]-1'-yl}-2-(4-fluorophenyl)butanamide
   Show/Hide
C34H33F7N2O
 1
1
IC50 = 440 nM
   TI
   LI
   LO
   TS
CP0468215
US8906911, 62
   Show/Hide
C26H35F3N4O2
 1
1
IC50 = 445 nM
   TI
   LI
   LO
   TS
CP0556819
US8906911, 9
   Show/Hide
C32H37F3N4O3
 1
1
IC50 = 470 nM
   TI
   LI
   LO
   TS
CP0532437
N-[[3,5-bis(trifluoromethyl)phenyl]methyl]-2-phenyl-2-(2-pyrrolidin-1-ylethylamino)acetamide
   Show/Hide
C23H25F6N3O
 1
1
IC50 = 521 nM
   TI
   LI
   LO
   TS
CP0507890
US8906911, 57
   Show/Hide
C29H37F3N4O3
 1
1
IC50 = 521 nM
   TI
   LI
   LO
   TS
CP0528177
N-[1-[[3,5-bis(trifluoromethyl)phenyl]methylamino]-1-oxo-4-spiro[indene-1,4'-piperidine]-1'-ylbutan-2-yl]-2-oxoimidazolidine-4-carboxamide
   Show/Hide
C30H31F6N5O3
 1
1
IC50 = 525 nM
   TI
   LI
   LO
   TS
CP0563261
US8906911, 13
   Show/Hide
C25H34F3N5O3
 2
1
IC50 = 525 nM
   TI
   LI
   LO
   TS
2
Ki = 593 nM
   TI
   LI
   LO
   TS
CP0480387
N-[[3,5-bis(trifluoromethyl)phenyl]methyl]-4-spiro[indene-1,4'-piperidine]-1'-ylbutanamide
   Show/Hide
C26H26F6N2O
 1
1
IC50 = 570 nM
   TI
   LI
   LO
   TS
CP0542432
N-[[3,5-bis(trifluoromethyl)phenyl]methyl]-2-(2-morpholin-4-ylethylamino)-2-phenylacetamide
   Show/Hide
C23H25F6N3O2
 1
1
IC50 = 575 nM
   TI
   LI
   LO
   TS
CP0511038
N-[[3,5-bis(trifluoromethyl)phenyl]methyl]-2-[2-(dimethylamino)ethylamino]-2-(furan-2-yl)acetamide
   Show/Hide
C19H21F6N3O2
 1
1
IC50 = 592 nM
   TI
   LI
   LO
   TS
CP0468207
US8906911, 26
   Show/Hide
C26H35F3N4O3
 2
1
IC50 = 598 nM
   TI
   LI
   LO
   TS
2
Ki = 792 nM
   TI
   LI
   LO
   TS
CP0501984
(2S)-N-{[3,5-bis(trifluoromethyl)phenyl]methyl}-2-methyl-4-{spiro[indene-1,4'-piperidine]-1'-yl}butanamide
   Show/Hide
C27H28F6N2O
 1
1
IC50 = 605 nM
   TI
   LI
   LO
   TS
CP0388118
(1S,3R)-3-(1,1-Dioxo-hexahydro-1lambda*6*-thiopyran-4-ylamino)-1-isopropyl-cyclopentanecarboxylic acid 3,5-bis-trifluoromethyl-benzylamide
   Show/Hide
C23H30F6N2O3S
 1
1
IC50 = 631 nM
   TI
   LI
   LO
   TS
CP0390923
(R)-N-(3,5-bis(trifluoromethyl)benzyl)-2-(2-(4-phenylpiperidin-1-yl)ethyl)pent-4-enamide
   Show/Hide
C27H30F6N2O
 1
1
IC50 = 642 nM
   TI
   LI
   LO
   TS
CP0500007
2-(1-acetylpiperidin-3-yl)-N-{[3,5-bis(trifluoromethyl)phenyl]methyl}-4-{spiro[indene-1,4'-piperidine]-1'-yl}butanamide
   Show/Hide
C33H37F6N3O2
 1
1
IC50 = 660 nM
   TI
   LI
   LO
   TS
CP0464560
N-[[3,5-bis(trifluoromethyl)phenyl]methyl]-2-[2-(diethylamino)ethylamino]-2-phenylacetamide
   Show/Hide
C23H27F6N3O
 1
1
IC50 = 678 nM
   TI
   LI
   LO
   TS
CP0496915
(2S)-N-[[3,5-bis(trifluoromethyl)phenyl]methyl]-2-(4-fluorophenyl)-4-[(3S,4S)-3-methyl-4-phenylpiperidin-1-yl]butan-1-amine
   Show/Hide
C31H33F7N2
 1
1
IC50 = 700 nM
   TI
   LI
   LO
   TS
CP0167324
(S)-N-(3,5-bis(trifluoromethyl)benzyl)-2-(2-(dimethylamino)ethylamino)-2-(4-fluorophenyl)acetamide
   Show/Hide
C21H22F7N3O
 2
1
IC50 = 720 nM
   TI
   LI
   LO
   TS
2
IC50 = 770 nM
   TI
   LI
   LO
   TS
CP0464512
(S)-N-(3,5-bis(trifluoromethyl)benzyl)-2-(2-(4-methylpiperidin-1-yl)ethylamino)-2-phenylacetamide
   Show/Hide
C25H29F6N3O
 1
1
IC50 = 756 nM
   TI
   LI
   LO
   TS
CP0204218
(1S,3R)-N-(3,5-bis(trifluoromethyl)benzyl)-3-(3-hydroxy-3-(trifluoromethyl)tetrahydro-2H-pyran-4-ylamino)-1-isopropylcyclopentanecarboxamide
   Show/Hide
C24H29F9N2O3
 1
1
IC50 = 765 nM
   TI
   LI
   LO
   TS
CP0515959
(2S)-N-(3,5-bis(trifluoromethyl)benzyl)-2-(4-fluorophenyl)-4-(3-methyl-4-phenylpiperazin-1-yl)butanamide
   Show/Hide
C30H30F7N3O
 1
1
IC50 = 780 nM
   TI
   LI
   LO
   TS
CP0536583
N-[[3,5-bis(trifluoromethyl)phenyl]methyl]-2-(1-methylsulfonylpiperidin-3-yl)-4-spiro[indene-1,4'-piperidine]-1'-ylbutanamide
   Show/Hide
C32H37F6N3O3S
 1
1
IC50 = 783 nM
   TI
   LI
   LO
   TS
CP0541314
methyl N-[1-[[3,5-bis(trifluoromethyl)phenyl]methylamino]-1-oxo-4-spiro[indene-1,4'-piperidine]-1'-ylbutan-2-yl]carbamate
   Show/Hide
C28H29F6N3O3
 1
1
IC50 = 805 nM
   TI
   LI
   LO
   TS
CP0564955
US8906911, 42
   Show/Hide
C28H35F3N4O3
 1
1
IC50 = 812 nM
   TI
   LI
   LO
   TS
CP0461573
US8906911, 21
   Show/Hide
C26H34F4N4O3
 1
1
IC50 = 821 nM
   TI
   LI
   LO
   TS
CP0501138
(S)-N-(3,5-bis(trifluoromethyl)benzyl)-2-phenyl-2-(2-(4-phenylpiperidin-1-yl)ethylamino)acetamide
   Show/Hide
C30H31F6N3O
 2
1
IC50 = 822 nM
   TI
   LI
   LO
   TS
2
IC50 = 830 nM
   TI
   LI
   LO
   TS
CP0516783
US8906911, 59
   Show/Hide
C24H31F3N4O2
 1
1
IC50 = 830 nM
   TI
   LI
   LO
   TS
CP0542431
(2S)-N-(3,5-bis(trifluoromethyl)benzyl)-2-(2-(2-methylpiperidin-1-yl)ethylamino)-2-phenylacetamide
   Show/Hide
C25H29F6N3O
 1
1
IC50 = 838 nM
   TI
   LI
   LO
   TS
CP0524406
(S)-N-(3,5-bis(trifluoromethyl)benzyl)-2-(2-(dimethylamino)ethylamino)-2-(thiophen-2-yl)acetamide
   Show/Hide
C19H21F6N3OS
 1
1
IC50 = 865 nM
   TI
   LI
   LO
   TS
CP0441644
(R)-N-(3,5-bis(trifluoromethyl)benzyl)-2-(4-fluorophenyl)-4-(4-phenylpiperidin-1-yl)butanamide
   Show/Hide
C30H29F7N2O
 1
1
IC50 = 930 nM
   TI
   LI
   LO
   TS
CP0442885
(S)-N-(3,5-bis(trifluoromethyl)benzyl)-2-(2-(dimethylamino)ethylamino)-2-phenylacetamide
   Show/Hide
C21H23F6N3O
 1
1
IC50 = 1000 nM
   TI
   LI
   LO
   TS
CP0464517
(S)-N-(3,5-bis(trifluoromethyl)benzyl)-2-(4-fluorophenyl)-5-(piperidin-1-yl)pentanamide
   Show/Hide
C25H27F7N2O
 1
1
IC50 = 1000 nM
   TI
   LI
   LO
   TS
CP0468209
US8906911, 31
   Show/Hide
C28H38F3N3O4
 1
1
IC50 = 1020 nM
   TI
   LI
   LO
   TS
CP0522377
(R)-N-(3,5-bis(trifluoromethyl)benzyl)-2-(4-fluorophenyl)-2-methyl-4-(4-phenylpiperidin-1-yl)butan-1-amine
   Show/Hide
C31H33F7N2
 1
1
IC50 = 1070 nM
   TI
   LI
   LO
   TS
CP0464518
(S)-N-(3,5-bis(trifluoromethyl)benzyl)-2-(4-fluorophenyl)-5-(4-phenylpiperidin-1-yl)pentanamide
   Show/Hide
C31H31F7N2O
 1
1
IC50 = 1100 nM
   TI
   LI
   LO
   TS
CP0501957
(S)-N-(3,5-bis(trifluoromethyl)benzyl)-2-(4-fluorophenyl)-4-(piperidin-1-yl)butanamide
   Show/Hide
C24H25F7N2O
 1
1
IC50 = 1100 nM
   TI
   LI
   LO
   TS
CP0563074
US8906911, 23
   Show/Hide
C28H38F3N3O3
 1
1
IC50 = 1110 nM
   TI
   LI
   LO
   TS
CP0565601
US8906911, 17
   Show/Hide
C27H35F4N3O3
 1
1
IC50 = 1290 nM
   TI
   LI
   LO
   TS
CP0563855
US8906911, 24
   Show/Hide
C28H38F3N3O3
 1
1
IC50 = 1390 nM
   TI
   LI
   LO
   TS
CP0466641
US8906911, 55
   Show/Hide
C29H37F6N3O3
 1
1
IC50 = 1410 nM
   TI
   LI
   LO
   TS
CP0555433
US8906911, 11
   Show/Hide
C27H37F3N4O3
 1
1
IC50 = 1470 nM
   TI
   LI
   LO
   TS
CP0464561
N-[[3,5-bis(trifluoromethyl)phenyl]methyl]-2-[2-(dimethylamino)ethylamino]-2-phenylacetamide
   Show/Hide
C21H23F6N3O
 1
1
IC50 = 1477 nM
   TI
   LI
   LO
   TS
CP0551302
(2S)-N-(3,5-bis(trifluoromethyl)benzyl)-2-(4-fluorophenyl)-4-(4-phenylpiperidin-1-yl)pentan-1-amine
   Show/Hide
C31H33F7N2
 1
1
IC50 = 1500 nM
   TI
   LI
   LO
   TS
CP0466640
US8906911, 43
   Show/Hide
C28H35F6N3O3
 1
1
IC50 = 1520 nM
   TI
   LI
   LO
   TS
CP0419276
US8906911, 10
   Show/Hide
C32H37F3N4O3
 1
1
IC50 = 1600 nM
   TI
   LI
   LO
   TS
CP0468211
US8906911, 37
   Show/Hide
C28H35F3N4O3
 1
1
IC50 = 1600 nM
   TI
   LI
   LO
   TS
CP0468212
US8906911, 38
   Show/Hide
C27H37F3N4O3
 1
1
IC50 = 1600 nM
   TI
   LI
   LO
   TS
CP0468213
US8906911, 44
   Show/Hide
C27H35ClN4O3
 1
1
IC50 = 1600 nM
   TI
   LI
   LO
   TS
CP0565603
US8906911, 45
   Show/Hide
C28H35F3N4O3
 1
1
IC50 = 2200 nM
   TI
   LI
   LO
   TS
CP0555431
US8906911, 3
   Show/Hide
C26H35F3N4O3
 1
1
IC50 = 2500 nM
   TI
   LI
   LO
   TS
CP0428167
US8906911, 34
   Show/Hide
C26H35F3N4O3
 1
1
IC50 = 2780 nM
   TI
   LI
   LO
   TS
CP0516782
US8906911, 54
   Show/Hide
C29H37F3N4O3
 1
1
IC50 = 2780 nM
   TI
   LI
   LO
   TS
CP0556910
US8906911, 58
   Show/Hide
C28H37ClN4O3
 1
1
IC50 = 2780 nM
   TI
   LI
   LO
   TS
CP0563856
US8906911, 35
   Show/Hide
C25H35ClN4O3
 1
1
IC50 = 2780 nM
   TI
   LI
   LO
   TS
CP0649585
1-butyl-3-(2-methylpropyl)-9-(6-phenylhexyl)-1,4,9-triazaspiro-[5.5]undeca-2,5-dione hydrochloride
   Show/Hide
C28H46ClN3O2
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0662025
(3R)-3-cyclohexylmethyl-9-(6-phenylhexyl)-1-propyl-1,4,9-triazaspiro[5.5]undeca-2,5-dione hydrochloride
   Show/Hide
C30H48ClN3O2
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0878092
(3S)-3-(2-methylpropyl)-9-(6-phenylhexyl)-1-propyl-1,4,9-triazaspiro[5.5]undeca-2,5-dione hydrochloride
   Show/Hide
C27H44ClN3O2
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0651200
9-(1,4-benzodioxane-6-yl)-1-butyl-3-(2-methylpropyl)-1,4,9-triazaspiro[5.5]undeca-2,5-dione hydrochloride
   Show/Hide
C25H38ClN3O4
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0657856
(+/-)-1-butyl-3-(cyclohexylmethyl)-9-(4-phenoxybenzyl)-1,4,9-triazaspiro[5.5]undecane-2,5-dione hydrochloride
   Show/Hide
C32H44ClN3O3
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0662064
9-(1,4-benzodioxane-6-yl)-1-butyl-3-cyclohexyl-1,4,9-triazaspiro-[5.5]undeca-2,5-dione hydrochloride
   Show/Hide
C28H42ClN3O4
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0662079
(3S)-3-cyclohexylmethyl-9-(6-phenylhexyl)-1-propyl-1,4,9-triazaspiro[5.5]undeca-2,5-dione hydrochloride
   Show/Hide
C30H48ClN3O2
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0720738
(+/-)-1-butyl-3-isobutyl-9-(4-phenoxybenzyl)-1,4,9-triazaspiro[5.5]undecane-2,5-dione hydrochloride
   Show/Hide
C29H40ClN3O3
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0837909
9-(4-allyloxyphenylmethyl)-1-butyl-3-cyclohexyl-1,4,9-triazaspiro[5.5]undeca-2,5-dione hydrochloride
   Show/Hide
C29H44ClN3O3
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0878091
(3R)-3-(2-methylpropyl)-9-(6-phenylhexyl)-1-propyl-1,4,9-triazaspiro[5.5]undeca-2,5-dione hydrochloride
   Show/Hide
C27H44ClN3O2
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0449524
4-(5,6-dichloro-1H-benzo[d]imidazol-2-yl)-N-methyl-N-(2-(piperidin-1-yl)ethyl)benzenamine
   Show/Hide
C21H24Cl2N4
 1
1
IC50 = 13400 nM
   TI
   LI
   LO
   TS
CP0419274
US8906911, 8
   Show/Hide
C27H37F3N4O3
 1
1
IC50 = 14430 nM
   TI
   LI
   LO
   TS
CP0400726
US8906911, 41
   Show/Hide
C27H37F3N4O3
 1
1
IC50 = 25000 nM
   TI
   LI
   LO
   TS
CP0428166
US8906911, 33
   Show/Hide
C26H35F3N4O3
 1
1
IC50 = 25000 nM
   TI
   LI
   LO
   TS
CP0515438
US8906911, 4
   Show/Hide
C26H35F3N4O3
 1
1
IC50 = 25000 nM
   TI
   LI
   LO
   TS
CP0466642
US8906911, Compound B
   Show/Hide
C25H34F3N3O2
 1
1
IC50 = 28000 nM
   TI
   LI
   LO
   TS
CP0651215
9-benzyl-1-butyl-3-(2-methylpropyl)-1,4,9-triazaspiro[5.5]-undeca-2,5-dione hydrochloride
   Show/Hide
C23H36ClN3O2
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0856132
(3S)-1,9-dibenzyl-3-(2-methylpropyl)-1,4,9-triazaspiro[5.5]-undeca-2,5-dione hydrochloride
   Show/Hide
C26H34ClN3O2
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0651202
1-butyl-3-cyclohexylmethyl-9-(4-methoxyphenylmethyl)-1,4,9-triazaspiro[5.5]undeca-2,5-dione hydrochloride
   Show/Hide
C27H42ClN3O3
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0699196
3-(2-methylpropyl)-9-(4-phenoxyphenylmethyl)-1-propyl-1,4,9-triazaspiro[5.5]undeca-2,5-dione hydrochloride
   Show/Hide
C28H38ClN3O3
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0850182
(3R)-1,9-dibenzyl-3-(2-methylpropyl)-1,4,9-triazaspiro[5.5]-undeca-2,5-dione hydrochloride
   Show/Hide
C26H34ClN3O2
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0462820
US8906911, Compound A
   Show/Hide
C26H36F3N3O2
 1
1
IC50 > 50000 nM
   TI
   LI
   LO
   TS
CP0129722
2-[5-chloro-3-[(3,4-dichlorophenyl)sulfonylamino]pyridin-2-yl]oxybenzoic acid
   Show/Hide
C18H11Cl3N2O5S
 1
1
Ki = 1.259 nM
   TI
   LI
   LO
   TS
CP0497113
3-[5-chloro-3-[(3,4-dichlorophenyl)sulfonylamino]pyridin-2-yl]oxybenzoic acid
   Show/Hide
C18H11Cl3N2O5S
 1
1
Ki = 1.585 nM
   TI
   LI
   LO
   TS
CP0502322
2-[5-chloro-3-[(3,4-dichlorophenyl)sulfonylamino]pyridin-2-yl]oxy-6-fluorobenzoic acid
   Show/Hide
C18H10Cl3FN2O5S
 1
1
Ki = 1.995 nM
   TI
   LI
   LO
   TS
CP0496030
4-[4-chloro-2-[[4-chloro-3-(trifluoromethyl)phenyl]sulfonylamino]phenoxy]-N-(2-pyrrolidin-1-ylethyl)benzamide
   Show/Hide
C26H24Cl2F3N3O4S
 1
1
Ki = 2 nM
   TI
   LI
   LO
   TS
CP0221913
4-[5-chloro-3-[[4-chloro-3-(trifluoromethyl)phenyl]sulfonylamino]pyridin-2-yl]oxy-N-(2-piperidin-1-ylethyl)benzamide
   Show/Hide
C26H25Cl2F3N4O4S
 1
1
Ki = 3 nM
   TI
   LI
   LO
   TS
CP0116928
2-[4-chloro-2-[(3,4-dichlorophenyl)sulfonylamino]phenoxy]benzoic acid
   Show/Hide
C19H12Cl3NO5S
 1
1
Ki = 3.162 nM
   TI
   LI
   LO
   TS
CP0427754
4-[5-chloro-3-[(3,4-dichlorophenyl)sulfonylamino]pyridin-2-yl]oxybenzoic acid
   Show/Hide
C18H11Cl3N2O5S
 1
1
Ki = 3.162 nM
   TI
   LI
   LO
   TS
CP0391753
4-[4-chloro-2-[[4-chloro-3-(trifluoromethyl)phenyl]sulfonylamino]-5-methoxyphenoxy]-N-(2-pyrrolidin-1-ylethyl)benzamide
   Show/Hide
C27H26Cl2F3N3O5S
 1
1
Ki = 4 nM
   TI
   LI
   LO
   TS
CP0502323
2-[4-chloro-2-[(5-chlorothiophen-2-yl)sulfonylamino]phenoxy]benzoic acid
   Show/Hide
C17H11Cl2NO5S2
 1
1
Ki = 5.012 nM
   TI
   LI
   LO
   TS
CP0094565
4-[4-chloro-2-[[4-chloro-3-(trifluoromethyl)phenyl]sulfonylamino]phenoxy]-3-methoxy-N-(2-pyrrolidin-1-ylethyl)benzamide
   Show/Hide
C27H26Cl2F3N3O5S
 1
1
Ki = 6 nM
   TI
   LI
   LO
   TS
CP0430764
2-[4-chloro-2-[(3-chlorophenyl)sulfonylamino]phenoxy]benzoic acid
   Show/Hide
C19H13Cl2NO5S
 1
1
Ki = 7.943 nM
   TI
   LI
   LO
   TS
CP0401059
4-[4-chloro-2-[[4-chloro-3-(trifluoromethyl)phenyl]sulfonylamino]phenoxy]-3-methyl-N-(2-pyrrolidin-1-ylethyl)benzamide
   Show/Hide
C27H26Cl2F3N3O4S
 1
1
Ki = 8 nM
   TI
   LI
   LO
   TS
CP0461434
4-[4-chloro-2-[[4-chloro-3-(trifluoromethyl)phenyl]sulfonylamino]-5-methylphenoxy]-N-(2-pyrrolidin-1-ylethyl)benzamide
   Show/Hide
C27H26Cl2F3N3O4S
 1
1
Ki = 8 nM
   TI
   LI
   LO
   TS
CP0039269
3,4-dichloro-N-[5-chloro-2-(2-methylpyridin-3-yl)oxypyridin-3-yl]benzenesulfonamide
   Show/Hide
C17H12Cl3N3O3S
 2
1
Ki = 10 nM
   TI
   LI
   LO
   TS
2
Ki = 1259 nM
   TI
   LI
   LO
   TS
CP0373790
5-[5-chloro-3-[(3,4-dichlorophenyl)sulfonylamino]pyridin-2-yl]oxypyridine-3-carboxylic acid
   Show/Hide
C17H10Cl3N3O5S
 1
1
Ki = 10 nM
   TI
   LI
   LO
   TS
CP0461432
4-[4-chloro-2-[[4-chloro-3-(trifluoromethyl)phenyl]sulfonylamino]-5-methoxyphenoxy]-N-(2-piperidin-1-ylethyl)benzamide
   Show/Hide
C28H28Cl2F3N3O5S
 1
1
Ki = 10 nM
   TI
   LI
   LO
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CP0517819
4-[4-chloro-2-[[4-chloro-3-(trifluoromethyl)phenyl]sulfonylamino]phenoxy]-N-(2-piperidin-1-ylethyl)benzamide
   Show/Hide
C27H26Cl2F3N3O4S
 1
1
Ki = 10 nM
   TI
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   TS
CP0228770
3,4-dichloro-N-[5-chloro-2-(5-chloropyridin-3-yl)oxypyridin-3-yl]benzenesulfonamide
   Show/Hide
C16H9Cl4N3O3S
 1
1
Ki = 12.59 nM
   TI
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   TS
CP0273839
4-[5-chloro-3-[(3,4-dichlorophenyl)sulfonylamino]pyridin-2-yl]oxy-N-(2-piperidin-1-ylethyl)benzamide
   Show/Hide
C25H25Cl3N4O4S
 2
1
Ki = 13 nM
   TI
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   TS
2
Ki = 20 nM
   TI
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CP0298012
4-[5-chloro-3-[(3,4-dichlorophenyl)sulfonylamino]pyridin-2-yl]oxy-N-(2-pyrrolidin-1-ylethyl)benzamide
   Show/Hide
C24H23Cl3N4O4S
 2
1
Ki = 13 nM
   TI
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2
Ki = 63 nM
   TI
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CP0401900
3,4-dichloro-N-[5-chloro-2-(6-cyanopyridin-3-yl)oxypyridin-3-yl]benzenesulfonamide
   Show/Hide
C17H9Cl3N4O3S
 1
1
Ki = 15.85 nM
   TI
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CP0390963
4-[4-chloro-2-[[4-chloro-3-(trifluoromethyl)phenyl]sulfonylamino]-5-methylphenoxy]-N-(2-piperidin-1-ylethyl)benzamide
   Show/Hide
C28H28Cl2F3N3O4S
 1
1
Ki = 16 nM
   TI
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CP0226249
3,4-dichloro-N-(5-chloro-2-pyridin-3-yloxypyridin-3-yl)benzenesulfonamide
   Show/Hide
C16H10Cl3N3O3S
 1
1
Ki = 19.95 nM
   TI
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CP0387732
2-[4-chloro-2-[(4-chlorophenyl)sulfonylamino]phenoxy]benzoic acid
   Show/Hide
C19H13Cl2NO5S
 1
1
Ki = 19.95 nM
   TI
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CP0400865
4-[4-chloro-2-[[4-chloro-3-(trifluoromethyl)phenyl]sulfonylamino]phenoxy]-3-methyl-N-(2-piperidin-1-ylethyl)benzamide
   Show/Hide
C28H28Cl2F3N3O4S
 1
1
Ki = 25 nM
   TI
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CP0400866
4-[4-chloro-2-[[4-chloro-3-(trifluoromethyl)phenyl]sulfonylamino]phenoxy]-3-methoxy-N-(2-piperidin-1-ylethyl)benzamide
   Show/Hide
C28H28Cl2F3N3O5S
 1
1
Ki = 25 nM
   TI
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   TS
CP0125371
2-[5-chloro-3-[(3,4-dichlorophenyl)sulfonylamino]pyridin-2-yl]oxy-N-(2-hydroxyethyl)benzamide
   Show/Hide
C20H16Cl3N3O5S
 1
1
Ki = 25.12 nM
   TI
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   TS
CP0863194
3-p-Tolyl-8,9-dihydro-7H-benzocycloheptene-6-carboxylic acid (4-{[methyl-(tetrahydro-pyran-4-yl)-amino]-methyl}-phenyl)-amide
   Show/Hide
C32H36N2O2
 1
1
Ki = 28.84 nM
   TI
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CP0390615
1-(3,4-dichlorobenzyl)-5-hydroxy-1H-indole-2-carboxylic acid
   Show/Hide
C16H11Cl2NO3
 1
1
Ki = 29 nM
   TI
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CP0416381
2-[3-[(3,4-dichlorophenyl)sulfonylamino]pyridin-2-yl]oxybenzoic acid
   Show/Hide
C18H12Cl2N2O5S
 1
1
Ki = 31.62 nM
   TI
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CP0506133
2-[2-[(4-chlorophenyl)sulfonylamino]-6-fluoro-4-(trifluoromethyl)phenoxy]benzoic acid
   Show/Hide
C20H12ClF4NO5S
 1
1
Ki = 31.62 nM
   TI
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CP0430766
2-[2-[(4-chlorophenyl)sulfonylamino]-4-fluorophenoxy]benzoic acid
   Show/Hide
C19H13ClFNO5S
 1
1
Ki = 39.81 nM
   TI
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CP0275299
4-[5-chloro-3-[(3,4-dichlorophenyl)sulfonylamino]pyridin-2-yl]oxy-N-(2-piperazin-1-ylethyl)benzamide
   Show/Hide
C24H24Cl3N5O4S
 2
1
Ki = 40 nM
   TI
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2
Ki = 251 nM
   TI
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CP0104462
(E)-3-(3,4-Dichloro-phenyl)-N-{5-[4-(5-hydroxy-1H-indol-3-yl)-piperidin-1-yl]-pentyl}-acrylamide
   Show/Hide
C27H31Cl2N3O2
 2
1
Ki = 50 nM
   TI
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2
Ki = 50.12 nM
   TI
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CP0471020
2-[4-[(3,4-dichlorophenyl)sulfonylamino]pyridin-3-yl]oxybenzoic acid
   Show/Hide
C18H12Cl2N2O5S
 1
1
Ki = 50.12 nM
   TI
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CP0488745
3,4-dichloro-N-[5-cyano-2-(2-methylpyridin-3-yl)oxypyridin-3-yl]benzenesulfonamide
   Show/Hide
C18H12Cl2N4O3S
 1
1
Ki = 50.12 nM
   TI
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CP0387506
4-[4-chloro-2-[(3,4-dichlorophenyl)sulfonylamino]phenoxy]-N-(2-piperidin-1-ylethyl)benzamide
   Show/Hide
C26H26Cl3N3O4S
 1
1
Ki = 63 nM
   TI
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CP0390739
4-[4-chloro-2-[[4-chloro-3-(trifluoromethyl)phenyl]sulfonylamino]phenoxy]-N-[2-(3,3-difluoropyrrolidin-1-yl)ethyl]benzamide
   Show/Hide
C26H22Cl2F5N3O4S
 1
1
Ki = 63 nM
   TI
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CP0516419
2-[2-[(4-chlorophenyl)sulfonylamino]-4-cyanophenoxy]benzoic acid
   Show/Hide
C20H13ClN2O5S
 1
1
Ki = 63.1 nM
   TI
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CP0323451
3-[5-chloro-3-[(3,4-dichlorophenyl)sulfonylamino]pyridin-2-yl]oxy-N-(2-piperidin-1-ylethyl)benzamide
   Show/Hide
C25H25Cl3N4O4S
 2
1
Ki = 79 nM
   TI
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2
Ki = 1259 nM
   TI
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CP0314740
3-[5-chloro-3-[(3,4-dichlorophenyl)sulfonylamino]pyridin-2-yl]oxy-N-(2-pyrrolidin-1-ylethyl)benzamide
   Show/Hide
C24H23Cl3N4O4S
 2
1
Ki = 100 nM
   TI
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2
Ki = 1000 nM
   TI
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CP0387734
2-[2-[(4-chlorophenyl)sulfonylamino]-4-(trifluoromethyl)phenoxy]-6-fluorobenzoic acid
   Show/Hide
C20H12ClF4NO5S
 1
1
Ki = 125.89 nM
   TI
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CP0473576
2-[2-(benzenesulfonamido)-4-chlorophenoxy]benzoic acid
   Show/Hide
C19H14ClNO5S
 1
1
Ki = 158.49 nM
   TI
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CP0493533
3,4-dichloro-N-(5-chloro-2-pyridazin-3-yloxypyridin-3-yl)benzenesulfonamide
   Show/Hide
C15H9Cl3N4O3S
 1
1
Ki = 199.53 nM
   TI
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CP0209406
3-[5-chloro-3-[(3,4-dichlorophenyl)sulfonylamino]pyridin-2-yl]oxy-N-(2-piperazin-1-ylethyl)benzamide
   Show/Hide
C24H24Cl3N5O4S
 2
1
Ki = 200 nM
   TI
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2
Ki = 2511 nM
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CP0250469
6-methyl-1'-[2-(5-methyl-2-phenyl-1,3-oxazol-4-yl)ethyl]spiro[1,4-dihydro-2H-benzo[d][1,3]oxazine-4,4'-(hexahydropyridine)]-2-one
   Show/Hide
C25H27N3O3
 1
1
Ki = 208.93 nM
   TI
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CP0416380
2-[2-[(4-chlorophenyl)sulfonylamino]phenoxy]benzoic acid
   Show/Hide
C19H14ClNO5S
 1
1
Ki = 251.19 nM
   TI
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CP0185499
(R)-N-(2-(1-(2,4-dimethylbenzyl)pyrrolidin-3-ylamino)-2-oxoethyl)-3-(trifluoromethyl)benzamide
   Show/Hide
C23H26F3N3O2
 1
1
Ki = 288.4 nM
   TI
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CP0416382
2-[4-chloro-2-(methanesulfonamido)phenoxy]benzoic acid
   Show/Hide
C14H12ClNO5S
 1
1
Ki = 398.11 nM
   TI
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CP0438745
2-[2-chloro-6-[(4-chlorophenyl)sulfonylamino]phenoxy]benzoic acid
   Show/Hide
C19H13Cl2NO5S
 1
1
Ki = 398.11 nM
   TI
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CP0499946
2-[5-[(3,4-dichlorophenyl)sulfonylamino]pyrimidin-4-yl]oxybenzoic acid
   Show/Hide
C17H11Cl2N3O5S
 1
1
Ki = 398.11 nM
   TI
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CP0464608
2-[2-[(4-chlorophenyl)sulfonylamino]-5-methylphenoxy]benzoic acid
   Show/Hide
C20H16ClNO5S
 1
1
Ki = 630.96 nM
   TI
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CP0209407
2-[5-chloro-3-[(3,4-dichlorophenyl)sulfonylamino]pyridin-2-yl]oxy-N-(2-pyrrolidin-1-ylethyl)benzamide
   Show/Hide
C24H23Cl3N4O4S
 2
1
Ki = 631 nM
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2
Ki = 2512 nM
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CP0298013
2-[5-chloro-3-[(3,4-dichlorophenyl)sulfonylamino]pyridin-2-yl]oxy-N-(2-piperidin-1-ylethyl)benzamide
   Show/Hide
C25H25Cl3N4O4S
 2
1
Ki = 794 nM
   TI
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2
Ki = 1585 nM
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CP0502324
2-[2-[(4-chlorophenyl)sulfonylamino]-4-(trifluoromethyl)phenoxy]benzoic acid
   Show/Hide
C20H13ClF3NO5S
 1
1
Ki = 794.33 nM
   TI
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CP0514942
2-[3-[(3,4-dichlorophenyl)sulfonylamino]pyrazin-2-yl]oxybenzoic acid
   Show/Hide
C17H11Cl2N3O5S
 1
1
Ki = 794.33 nM
   TI
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CP0471061
2-[2-[(4-chlorophenyl)sulfonylamino]-4-methylsulfonylphenoxy]benzoic acid
   Show/Hide
C20H16ClNO7S2
 1
1
Ki > 3162.28 nM
   TI
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CP0516417
2-[2-[(4-chlorophenyl)sulfonylamino]-3-fluorophenoxy]benzoic acid
   Show/Hide
C19H13ClFNO5S
 1
1
Ki > 3162.28 nM
   TI
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CP0516418
2-[2-[(4-chlorophenyl)sulfonylamino]-6-methylphenoxy]benzoic acid
   Show/Hide
C20H16ClNO5S
 1
1
Ki > 3162.28 nM
   TI
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Biochemical Assays
Compound ID Compound Name Compound Formula
CP0066063
N-[2-[[(1S,2R,4R)-2-(benzenesulfonylmethyl)-4-[methyl(propan-2-yl)amino]cyclohexyl]amino]-2-oxoethyl]-3-(trifluoromethyl)benzamide
   Show/Hide
C27H34F3N3O4S
 2
1 IC50 = 0.8 nM
2 IC50 = 1.3 nM
CP0059668
N-[(3S)-1-[(1S,2R,4R)-2-(benzenesulfonylmethyl)-4-[methyl(propan-2-yl)amino]cyclohexyl]-2-oxopyrrolidin-3-yl]-3-(trifluoromethyl)benzamide
   Show/Hide
C29H36F3N3O4S
 1
1 IC50 = 1 nM
CP0154997
N-[(1R,2S,5R)-5-[methyl(propan-2-yl)amino]-2-[(3S)-2-oxo-3-[[6-(trifluoromethyl)quinazolin-4-yl]amino]pyrrolidin-1-yl]cyclohexyl]acetamide
   Show/Hide
C25H33F3N6O2
 1
1 IC50 = 1.1 nM
CP0099584
N-[2-[[2-[[(1S,3S,4R)-4-amino-3-(benzenesulfonylmethyl)cyclohexyl]amino]-2-oxoethyl]carbamoyl]-4-(trifluoromethyl)phenyl]azetidine-1-carboxamide
   Show/Hide
C27H32F3N5O5S
 1
1 IC50 = 1.4 nM
CP0315991
(1S,3R)-N-(3,5-bis(trifluoromethyl)benzyl)-3-(3-ethyl tetrahydro-2H-pyran-4-ylamino)-1-isopropylcyclopentanecarboxamide
   Show/Hide
C25H34F6N2O2
 1
1 IC50 = 1.5 nM
CP0522786
(1S,3R)-N-(3,5-bis(trifluoromethyl)benzyl)-1-isopropyl-3-(3-propyltetrahydro-2H-pyran-4-ylamino)cyclopentanecarboxamide
   Show/Hide
C26H36F6N2O2
 1
1 IC50 = 2.999 nM
CP0035313
(S,E)-2-(4-(1H-indol-3-yl)piperidin-1-yl)-2-(1-(3-(3,4,5-trifluorophenyl)acryloyl)piperidin-4-yl)acetic acid
   Show/Hide
C29H30F3N3O3
 1
1 IC50 = 4 nM
CP0514673
(1S,3R)-N-(3,5-bis(trifluoromethyl)benzyl)-1-isopropyl-3-(tetrahydro-2H-pyran-3-ylamino)cyclopentanecarboxamide
   Show/Hide
C23H30F6N2O2
 1
1 IC50 = 4.603 nM
CP0204218
(1S,3R)-N-(3,5-bis(trifluoromethyl)benzyl)-3-(3-hydroxy-3-(trifluoromethyl)tetrahydro-2H-pyran-4-ylamino)-1-isopropylcyclopentanecarboxamide
   Show/Hide
C24H29F9N2O3
 1
1 IC50 = 5.495 nM
CP0053417
(1S,3R)-N-(3,5-bis(trifluoromethyl)benzyl)-1-isopropyl-3-(3-(trifluoromethyl)tetrahydro-2H-pyran-4-ylamino)cyclopentanecarboxamide
   Show/Hide
C24H29F9N2O2
 1
1 IC50 = 5.998 nM
CP0126803
2-(3-isopropylureido)-N-(2-((1S,2R)-2-(4-(methylthio)benzamido)cyclohexylamino)-2-oxoethyl)-5-(trifluoromethyl)benzamide
   Show/Hide
C28H34F3N5O4S
 1
1 IC50 = 7.5 nM
CP0388120
(1S,3R)-N-(3,5-bis(trifluoromethyl)benzyl)-3-(3-cyclopropyltetrahydro-2H-pyran-4-ylamino)-1-isopropylcyclopentanecarboxamide
   Show/Hide
C26H34F6N2O2
 1
1 IC50 = 7.798 nM
CP0051245
(S)-N-(2-(3-(2,4-dimethylbenzylamino)-1-(tert-butylamino)-1-oxopropan-2-ylamino)-2-oxoethyl)-2-amino-5-(trifluoromethyl)benzamide
   Show/Hide
C26H34F3N5O3
 1
1 IC50 = 11 nM
CP0202246
(S)-N-(2-(3-(2,4-dimethylbenzylamino)-1-(tert-butylamino)-1-oxopropan-2-ylamino)-2-oxoethyl)-2-(ethylamino)-5-(trifluoromethyl)benzamide
   Show/Hide
C28H38F3N5O3
 1
1 IC50 = 13 nM
CP0185497
(S)-1-(2-((2-(3-(2,4-dimethylbenzylamino)-1-(tert-butylamino)-1-oxopropan-2-ylamino)-2-oxoethyl)carbamoyl)-4-(trifluoromethyl)phenyl)-3-isopropylurea
   Show/Hide
C30H41F3N6O4
 1
1 IC50 = 15 nM
CP0185499
(R)-N-(2-(1-(2,4-dimethylbenzyl)pyrrolidin-3-ylamino)-2-oxoethyl)-3-(trifluoromethyl)benzamide
   Show/Hide
C23H26F3N3O2
 1
1 IC50 = 17 nM
CP0136162
(S)-N-(2-(3-(2,4-dimethylbenzylamino)-1-(tert-butylamino)-1-oxopropan-2-ylamino)-2-oxoethyl)-3-(ethylamino)-5-(trifluoromethyl)benzamide
   Show/Hide
C28H38F3N5O3
 1
1 IC50 = 19 nM
CP0528311
(S)-N-(2-(3-(2,4-dimethylbenzylamino)-1-(tert-butylamino)-1-oxopropan-2-ylamino)-2-oxoethyl)-2-(benzylamino)-5-(trifluoromethyl)benzamide
   Show/Hide
C33H40F3N5O3
 1
1 IC50 = 19 nM
CP0160834
(S)-N-(2-(3-(4-bromo-2-methylbenzylamino)-1-(tert-butylamino)-1-oxopropan-2-ylamino)-2-oxoethyl)-2-amino-3-(trifluoromethyl)benzamide
   Show/Hide
C25H31BrF3N5O3
 1
1 IC50 = 20 nM
CP0315992
(1S,3R)-N-(3,5-bis(trifluoromethyl)benzyl)-1-isopropyl-3-(tetrahydrothiophen-3-ylamino)cyclopentanecarboxamide
   Show/Hide
C22H28F6N2OS
 1
1 IC50 = 21.98 nM
CP0199851
(S)-N-(2-(3-(2,4-dimethylbenzylamino)-1-(tert-butylamino)-1-oxopropan-2-ylamino)-2-oxoethyl)-3-amino-5-(trifluoromethyl)benzamide
   Show/Hide
C26H34F3N5O3
 1
1 IC50 = 23 nM
CP0144619
[(2R,3aR,6aR)-2-[[(3R,4R)-3-methoxyoxan-4-yl]amino]-2,3,4,5,6,6a-hexahydro-1H-pentalen-3a-yl]-[3-(trifluoromethyl)-7,8-dihydro-5H-1,6-naphthyridin-6-yl]methanone
   Show/Hide
C24H32F3N3O3
 2
1 IC50 = 24 nM
2 IC50 = 61 nM
CP0666580
Dimethyl-(tetrahydro-pyran-4-yl)-{4-[(3-p-tolyl-8,9-dihydro-7H-benzocycloheptene-6-carbonyl)-amino]-benzyl}-ammonium chloride(TAK-779)
   Show/Hide
C33H39ClN2O2
 1
1 IC50 = 27 nM
CP0493802
(1S,3R)-N-(3,5-bis(trifluoromethyl)benzyl)-3-(3,3-dimethyltetrahydro-2H-pyran-4-ylamino)-1-isopropylcyclopentanecarboxamide
   Show/Hide
C25H34F6N2O2
 1
1 IC50 = 27.99 nM
CP0302119
(1S,3R)-N-(3,5-bis(trifluoromethyl)benzyl)-1-isopropyl-3-(oxepan-4-ylamino)cyclopentanecarboxamide
   Show/Hide
C24H32F6N2O2
 1
1 IC50 = 29.99 nM
CP0085708
(E)-1-[(3aR,5R,6aR)-5-[(3-methoxyoxan-4-yl)amino]-3a-[3-(trifluoromethyl)-7,8-dihydro-5H-1,6-naphthyridine-6-carbonyl]-1,3,4,5,6,6a-hexahydrocyclopenta[c]pyrrol-2-yl]-3-phenylprop-2-en-1-one
   Show/Hide
C32H37F3N4O4
 1
1 IC50 = 30 nM
CP0085738
2-(oxan-4-yl)ethyl (3aR,5R,6aR)-5-[(3-methoxyoxan-4-yl)amino]-3a-[3-(trifluoromethyl)-7,8-dihydro-5H-1,6-naphthyridine-6-carbonyl]-1,3,4,5,6,6a-hexahydrocyclopenta[c]pyrrole-2-carboxylate
   Show/Hide
C31H43F3N4O6
 1
1 IC50 = 31 nM
CP0219341
oxan-4-ylmethyl (3aR,5R,6aR)-5-[(3-methoxyoxan-4-yl)amino]-3a-[3-(trifluoromethyl)-7,8-dihydro-5H-1,6-naphthyridine-6-carbonyl]-1,3,4,5,6,6a-hexahydrocyclopenta[c]pyrrole-2-carboxylate
   Show/Hide
C30H41F3N4O6
 1
1 IC50 = 32 nM
CP0134117
2-pyrrolidin-1-ylethyl (3aR,5R,6aR)-5-[(3-methoxyoxan-4-yl)amino]-3a-[3-(trifluoromethyl)-7,8-dihydro-5H-1,6-naphthyridine-6-carbonyl]-1,3,4,5,6,6a-hexahydrocyclopenta[c]pyrrole-2-carboxylate
   Show/Hide
C30H42F3N5O5
 1
1 IC50 = 33 nM
CP0069631
2-methylpropyl (3aR,5R,6aR)-5-[(3-methoxyoxan-4-yl)amino]-3a-[3-(trifluoromethyl)-7,8-dihydro-5H-1,6-naphthyridine-6-carbonyl]-1,3,4,5,6,6a-hexahydrocyclopenta[c]pyrrole-2-carboxylate
   Show/Hide
C28H39F3N4O5
 1
1 IC50 = 35 nM
CP0238399
(1S,3R)-N-(3,5-bis(trifluoromethyl)benzyl)-1-isopropyl-3-(tetrahydro-2H-thiopyran-4-ylamino)cyclopentanecarboxamide
   Show/Hide
C23H30F6N2OS
 1
1 IC50 = 35.97 nM
CP0208642
(S)-N-(2-(3-(2,4-dimethylbenzylamino)-1-amino-1-oxopropan-2-ylamino)-2-oxoethyl)-2-amino-3-(trifluoromethyl)benzamide
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C22H26F3N5O3
 1
1 IC50 = 37 nM
CP0326435
(3aR,5R,6aR)-N'-cyano-5-[(3-methoxyoxan-4-yl)amino]-3a-[3-(trifluoromethyl)-7,8-dihydro-5H-1,6-naphthyridine-6-carbonyl]-1,3,4,5,6,6a-hexahydrocyclopenta[c]pyrrole-2-carboximidamide
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C25H32F3N7O3
 1
1 IC50 = 37 nM
CP0258415
2-morpholin-4-ylethyl (3aR,5R,6aR)-5-[(3-methoxyoxan-4-yl)amino]-3a-[3-(trifluoromethyl)-7,8-dihydro-5H-1,6-naphthyridine-6-carbonyl]-1,3,4,5,6,6a-hexahydrocyclopenta[c]pyrrole-2-carboxylate
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C30H42F3N5O6
 1
1 IC50 = 41 nM
CP0134118
2-acetamidoethyl (3aR,5R,6aR)-5-[(3-methoxyoxan-4-yl)amino]-3a-[3-(trifluoromethyl)-7,8-dihydro-5H-1,6-naphthyridine-6-carbonyl]-1,3,4,5,6,6a-hexahydrocyclopenta[c]pyrrole-2-carboxylate
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C28H38F3N5O6
 1
1 IC50 = 45 nM
CP0201872
(S)-N-(2-(3-(2,4-dimethylbenzylamino)-1-(tert-butylamino)-1-oxopropan-2-ylamino)-2-oxoethyl)-3-(trifluoromethyl)benzamide
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C26H33F3N4O3
 1
1 IC50 = 48 nM
CP0165577
(1S,3R)-N-(3,5-bis(trifluoromethyl)benzyl)-1-isopropyl-3-(tetrahydro-2H-pyran-4-ylamino)cyclopentanecarboxamide
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C23H30F6N2O2
 1
1 IC50 = 55.98 nM
CP0069637
(3aR,5R,6aR)-N-benzyl-5-[(3-methoxyoxan-4-yl)amino]-3a-[3-(trifluoromethyl)-7,8-dihydro-5H-1,6-naphthyridine-6-carbonyl]-1,3,4,5,6,6a-hexahydrocyclopenta[c]pyrrole-2-carboxamide
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C31H38F3N5O4
 1
1 IC50 = 57 nM
CP0155510
2,2-dimethylpropyl (3aR,5R,6aR)-5-[(3-methoxyoxan-4-yl)amino]-3a-[3-(trifluoromethyl)-7,8-dihydro-5H-1,6-naphthyridine-6-carbonyl]-1,3,4,5,6,6a-hexahydrocyclopenta[c]pyrrole-2-carboxylate
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C29H41F3N4O5
 1
1 IC50 = 59 nM
CP0176443
[(3aR,5R,6aR)-5-[(3-methoxyoxan-4-yl)amino]-2-phenyl-1,3,4,5,6,6a-hexahydrocyclopenta[c]pyrrol-3a-yl]-[3-(trifluoromethyl)-7,8-dihydro-5H-1,6-naphthyridin-6-yl]methanone
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C29H35F3N4O3
 1
1 IC50 = 62 nM
CP0165578
(1S,3R)-N-(3,5-bis(trifluoromethyl)benzyl)-3-(cyclohexylamino)-1-isopropylcyclopentanecarboxamide
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C24H32F6N2O
 1
1 IC50 = 63.97 nM
CP0069632
(3aR,5R,6aR)-5-[(3-methoxyoxan-4-yl)amino]-3a-[3-(trifluoromethyl)-7,8-dihydro-5H-1,6-naphthyridine-6-carbonyl]-1,3,4,5,6,6a-hexahydrocyclopenta[c]pyrrole-2-carboxamide
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C24H32F3N5O4
 1
1 IC50 = 64 nM
CP0215141
(S)-N-(2-(3-(2,4-dimethylbenzylamino)-1-amino-1-oxopropan-2-ylamino)-2-oxoethyl)-3-(trifluoromethyl)benzamide
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C22H25F3N4O3
 1
1 IC50 = 66 nM
CP0085707
(E)-1-[(3aR,5R,6aR)-5-[(3-methoxyoxan-4-yl)amino]-3a-[3-(trifluoromethyl)-7,8-dihydro-5H-1,6-naphthyridine-6-carbonyl]-1,3,4,5,6,6a-hexahydrocyclopenta[c]pyrrol-2-yl]-4,4-dimethylpent-2-en-1-one
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C30H41F3N4O4
 1
1 IC50 = 68 nM
CP0331716
(1S,3R)-N-(3,5-bis(trifluoromethyl)benzyl)-3-(2,3-dihydro-1H-inden-1-ylamino)-1-isopropylcyclopentanecarboxamide
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C27H30F6N2O
 1
1 IC50 = 76.91 nM
CP0176444
(3aR,5R,6aR)-5-[(3-methoxyoxan-4-yl)amino]-N-methyl-3a-[3-(trifluoromethyl)-7,8-dihydro-5H-1,6-naphthyridine-6-carbonyl]-1,3,4,5,6,6a-hexahydrocyclopenta[c]pyrrole-2-carboxamide
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C25H34F3N5O4
 1
1 IC50 = 77 nM
CP0167981
N-[2-[[(1S,3S,4R)-3-(benzenesulfonylmethyl)-4-[methyl(propan-2-yl)amino]cyclohexyl]amino]-2-oxoethyl]-3-(trifluoromethyl)benzamide
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C27H34F3N3O4S
 1
1 IC50 = 79 nM
CP0317447
2-methoxyethyl (3aR,5R,6aR)-5-[(3-methoxyoxan-4-yl)amino]-3a-[3-(trifluoromethyl)-7,8-dihydro-5H-1,6-naphthyridine-6-carbonyl]-1,3,4,5,6,6a-hexahydrocyclopenta[c]pyrrole-2-carboxylate
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C27H37F3N4O6
 1
1 IC50 = 82 nM
CP0315993
(1S,3R)-N-(3,5-bis(trifluoromethyl)benzyl)-1-isopropyl-3-(tetrahydrofuran-3-ylamino)cyclopentanecarboxamide
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C22H28F6N2O2
 1
1 IC50 = 84.92 nM
CP0202906
1-[(3aR,5R,6aR)-5-[(3-methoxyoxan-4-yl)amino]-3a-[3-(trifluoromethyl)-7,8-dihydro-5H-1,6-naphthyridine-6-carbonyl]-1,3,4,5,6,6a-hexahydrocyclopenta[c]pyrrol-2-yl]-3-cyclopropylprop-2-yn-1-one
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C29H35F3N4O4
 1
1 IC50 = 87 nM
CP0176445
1-[(3aR,5R,6aR)-5-[(3-methoxyoxan-4-yl)amino]-3a-[3-(trifluoromethyl)-7,8-dihydro-5H-1,6-naphthyridine-6-carbonyl]-1,3,4,5,6,6a-hexahydrocyclopenta[c]pyrrol-2-yl]-3-phenylpropan-1-one
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C32H39F3N4O4
 1
1 IC50 = 110 nM
CP0339382
benzyl (3aR,5R,6aR)-5-[(3-methoxyoxan-4-yl)amino]-3a-[3-(trifluoromethyl)-7,8-dihydro-5H-1,6-naphthyridine-6-carbonyl]-1,3,4,5,6,6a-hexahydrocyclopenta[c]pyrrole-2-carboxylate
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C31H37F3N4O5
 1
1 IC50 = 118 nM
CP0165576
(1S,3R)-N-(3,5-bis(trifluoromethyl)benzyl)-3-(3-hydroxytetrahydro-2H-pyran-4-ylamino)-1-isopropylcyclopentanecarboxamide
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C23H30F6N2O3
 1
1 IC50 = 123.03 nM
CP0340173
(1S,3R)-N-(3,5-bis(trifluoromethyl)benzyl)-3-(cyclopentylamino)-1-isopropylcyclopentanecarboxamide
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C23H30F6N2O
 1
1 IC50 = 155.96 nM
CP0481537
(1S,3R)-N-(3,5-bis(trifluoromethyl)benzyl)-3-(cycloheptylamino)-1-isopropylcyclopentanecarboxamide
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C25H34F6N2O
 1
1 IC50 = 174.98 nM
CP0277402
(R)-N-(2-(1-(4-chlorobenzyl)pyrrolidin-3-ylamino)-2-oxoethyl)-3-(trifluoromethyl)benzamide
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C21H21ClF3N3O2
 1
1 IC50 = 180 nM
CP0459575
(1S,3R)-N-(3,5-bis(trifluoromethyl)benzyl)-1-isopropyl-3-(1,2,3,4-tetrahydronaphthalen-2-ylamino)cyclopentanecarboxamide
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C28H32F6N2O
 1
1 IC50 = 187.07 nM
CP0282451
(1S,3R)-N-(3,5-bis(trifluoromethyl)benzyl)-3-(cyclobutylamino)-1-isopropylcyclopentanecarboxamide
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C22H28F6N2O
 1
1 IC50 = 193.2 nM
CP0053416
(1S,3R)-N-(3,5-bis(trifluoromethyl)benzyl)-3-(3,5-dimethyltetrahydro-2H-pyran-4-ylamino)-1-isopropylcyclopentanecarboxamide
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C25H34F6N2O2
 1
1 IC50 = 230.14 nM
CP0155511
[(3aR,5R,6aR)-5-[(3-methoxyoxan-4-yl)amino]-2-methyl-1,3,4,5,6,6a-hexahydrocyclopenta[c]pyrrol-3a-yl]-[3-(trifluoromethyl)-7,8-dihydro-5H-1,6-naphthyridin-6-yl]methanone
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C24H33F3N4O3
 1
1 IC50 = 300 nM
CP0119832
(1S,3R)-N-(3,5-bis(trifluoromethyl)benzyl)-1-isopropyl-3-((tetrahydro-2H-pyran-4-yl)methylamino)cyclopentanecarboxamide
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C24H32F6N2O2
 1
1 IC50 = 362.24 nM
CP0346051
1-[(3aR,5R,6aR)-5-[(3-methoxyoxan-4-yl)amino]-3a-[3-(trifluoromethyl)-7,8-dihydro-5H-1,6-naphthyridine-6-carbonyl]-1,3,4,5,6,6a-hexahydrocyclopenta[c]pyrrol-2-yl]ethanone
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C25H33F3N4O4
 1
1 IC50 = 395 nM
CP0258416
methyl (3aR,5R,6aR)-5-[(3-methoxyoxan-4-yl)amino]-3a-[3-(trifluoromethyl)-7,8-dihydro-5H-1,6-naphthyridine-6-carbonyl]-1,3,4,5,6,6a-hexahydrocyclopenta[c]pyrrole-2-carboxylate
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C25H33F3N4O5
 1
1 IC50 = 410 nM
CP0347344
(3aR,5R,6aR)-5-[(3-methoxyoxan-4-yl)amino]-N-propan-2-yl-3a-[3-(trifluoromethyl)-7,8-dihydro-5H-1,6-naphthyridine-6-carbonyl]-1,3,4,5,6,6a-hexahydrocyclopenta[c]pyrrole-2-carboxamide
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C27H38F3N5O4
 1
1 IC50 = 410 nM
CP0262145
(1S,3R)-N-(3,5-bis(trifluoromethyl)benzyl)-3-(chroman-4-ylamino)-1-isopropylcyclopentanecarboxamide
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C27H30F6N2O2
 1
1 IC50 = 418.79 nM
CP0154057
phenyl (3aR,5R,6aR)-5-[(3-methoxyoxan-4-yl)amino]-3a-[3-(trifluoromethyl)-7,8-dihydro-5H-1,6-naphthyridine-6-carbonyl]-1,3,4,5,6,6a-hexahydrocyclopenta[c]pyrrole-2-carboxylate
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C30H35F3N4O5
 1
1 IC50 = 560 nM
CP0133098
N-[2-[[(2R)-1-[(4-chlorophenyl)methyl]pyrrolidin-2-yl]methylamino]-2-oxoethyl]-3-(trifluoromethyl)benzamide
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C22H23ClF3N3O2
 1
1 IC50 = 570 nM
CP0388118
(1S,3R)-3-(1,1-Dioxo-hexahydro-1lambda*6*-thiopyran-4-ylamino)-1-isopropyl-cyclopentanecarboxylic acid 3,5-bis-trifluoromethyl-benzylamide
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C23H30F6N2O3S
 1
1 IC50 = 630.96 nM
CP0330247
N-[2-[[1-[(4-chlorophenyl)methyl]piperidin-3-yl]amino]-2-oxoethyl]-3-(trifluoromethyl)benzamide
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C22H23ClF3N3O2
 1
1 IC50 = 660 nM
CP0133099
N-[2-[[1-[(4-chlorophenyl)methyl]piperidin-4-yl]methylamino]-2-oxoethyl]-3-(trifluoromethyl)benzamide
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C23H25ClF3N3O2
 1
1 IC50 = 700 nM
CP0277285
3-{1-Hydroxy-3-[4-(4-methanesulfonyl-benzyl)-[1,4]diazepan-1-yl]-1-phenyl-propyl}-phenol
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C28H34N2O4S
 1
1 IC50 = 710 nM
CP0467606
(1S,3R)-N-(3,5-bis(trifluoromethyl)benzyl)-1-isopropyl-3-(2-methyltetrahydro-2H-pyran-4-ylamino)cyclopentanecarboxamide
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C24H32F6N2O2
 1
1 IC50 = 765.6 nM
CP0069634
[(3aR,5R,6aR)-5-[(3-methoxyoxan-4-yl)amino]-2,3,4,5,6,6a-hexahydro-1H-cyclopenta[c]pyrrol-3a-yl]-[3-(trifluoromethyl)-7,8-dihydro-5H-1,6-naphthyridin-6-yl]methanone
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C23H31F3N4O3
 1
1 IC50 = 780 nM
CP0298935
N-[2-[[(3S)-1-[(4-chlorophenyl)methyl]pyrrolidin-3-yl]amino]-2-oxoethyl]-3-(trifluoromethyl)benzamide
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C21H21ClF3N3O2
 1
1 IC50 = 1200 nM
CP0717334
N-({[1-(4-Chloro-benzyl)-pyrrolidin-2-ylmethyl]-carbamoyl}-methyl)-3-trifluoromethyl-benzamide
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C22H23ClF3N3O2
 1
1 IC50 = 3100 nM
CP0254041
4-Methyl-thiophene-2-carboxylic acid N''-{2-[4-(4-chloro-benzyl)-[1,4]diazepan-1-yl]-acetyl}-hydrazide
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C20H25ClN4O2S
 1
1 IC50 = 7400 nM
CP0649585
1-butyl-3-(2-methylpropyl)-9-(6-phenylhexyl)-1,4,9-triazaspiro-[5.5]undeca-2,5-dione hydrochloride
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C28H46ClN3O2
 1
1 IC50 > 10000 nM
CP0651200
9-(1,4-benzodioxane-6-yl)-1-butyl-3-(2-methylpropyl)-1,4,9-triazaspiro[5.5]undeca-2,5-dione hydrochloride
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C25H38ClN3O4
 1
1 IC50 > 10000 nM
CP0657856
(+/-)-1-butyl-3-(cyclohexylmethyl)-9-(4-phenoxybenzyl)-1,4,9-triazaspiro[5.5]undecane-2,5-dione hydrochloride
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C32H44ClN3O3
 1
1 IC50 > 10000 nM
CP0662064
9-(1,4-benzodioxane-6-yl)-1-butyl-3-cyclohexyl-1,4,9-triazaspiro-[5.5]undeca-2,5-dione hydrochloride
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C28H42ClN3O4
 1
1 IC50 > 10000 nM
CP0720738
(+/-)-1-butyl-3-isobutyl-9-(4-phenoxybenzyl)-1,4,9-triazaspiro[5.5]undecane-2,5-dione hydrochloride
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C29H40ClN3O3
 1
1 IC50 > 10000 nM
CP0837909
9-(4-allyloxyphenylmethyl)-1-butyl-3-cyclohexyl-1,4,9-triazaspiro[5.5]undeca-2,5-dione hydrochloride
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C29H44ClN3O3
 1
1 IC50 > 10000 nM
CP0651202
1-butyl-3-cyclohexylmethyl-9-(4-methoxyphenylmethyl)-1,4,9-triazaspiro[5.5]undeca-2,5-dione hydrochloride
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C27H42ClN3O3
 1
1 IC50 > 30000 nM
CP0699196
3-(2-methylpropyl)-9-(4-phenoxyphenylmethyl)-1-propyl-1,4,9-triazaspiro[5.5]undeca-2,5-dione hydrochloride
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C28H38ClN3O3
 1
1 IC50 > 30000 nM
CP0149803
3,4-dichloro-N-[5-chloro-2-(triazol-1-ylmethyl)phenyl]benzenesulfonamide
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C15H11Cl3N4O2S
 1
1 Ki = 10 nM
CP0045327
(E)-3-(3,4-Dichloro-phenyl)-N-{4-[(R)-3-((2S,7aS)-5-hydroxy-1H-indol-3-yl)-8-aza-bicyclo[3.2.1]oct-8-ylmethyl]-cyclohexyl}-acrylamide
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C31H35Cl2N3O2
 1
1 Ki = 40 nM
CP0104462
(E)-3-(3,4-Dichloro-phenyl)-N-{5-[4-(5-hydroxy-1H-indol-3-yl)-piperidin-1-yl]-pentyl}-acrylamide
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C27H31Cl2N3O2
 1
1 Ki = 50 nM
Clinical Information about the Protein
Target 1 ( C-C chemokine receptor type 2 (CCR2) )
Target Type Clinical trial Target
Disease 7 Target-related Diseases  7
1 Diabetic nephropathy [ICD-11: GB61.Z]
2 Human immunodeficiency virus infection [ICD-11: 1C62]
3 Multiple sclerosis [ICD-11: 8A40]
4 Diabetic retinopathy [ICD-11: 9B71.0]
5 Chronic obstructive pulmonary disease [ICD-11: CA22]
6 Arteriosclerosis [ICD-11: BD40]
7 Inflammation [ICD-11: 1A00-CA43.1]
Clinical Trial Drug(s) 5 Clinical Trial Drugs  5
1 BMS-813160 Phase 2
Diabetic nephropathy
2 CCX-140 Phase 2
Diabetic nephropathy
3 Cenicriviroc Phase 2
Human immunodeficiency virus infection
4 MK-0812 Phase 2
Multiple sclerosis
5 Aminoguanidine Phase 1
Diabetic retinopathy
Discontinued Drug(s) 3 Discontinued Drugs  3
1 CCX915 Discontinued in Phase 1
Multiple sclerosis
2 INCB3344 Terminated
Arteriosclerosis
3 SB-282241 Terminated
Inflammation
Investigative Drug(s) 1 Investigative Drug  1
1 BMS-A Investigative
Inflammation
Preclinical Drug(s) 1 Preclinical Drug  1
1 RS-504393 Preclinical
Chronic obstructive pulmonary disease
Similar Protein(s) and Bioactivity Statistics
50% Identity
Protein ID Protein Name Protein Organism
PT04128 C-C chemokine receptor type 2 Mus musculus, Mouse
PT04757 C-C chemokine receptor type 2 Rattus norvegicus, Rat