Brief Information of the Cell Line and Protein
Cell Line ID: CL000006 , HEK293
Synonyms
Hek293
HEK-293
HEK/293
HEK 293
HEK;293
293
293 HEK
293 Ad5
Graham 293
Graham-293
Human Embryonic Kidney 293
Category Transformed cell line
Organism
Homo sapiens (Human)
Cellosaurus ID
CVCL_0045
Protein ID: PT01839 , Vasopressin V1a receptor
Gene Name AVPR1A
Organism Homo sapiens, Human
Protein Classification Membrane receptor
Uniprot ID P37288
Table of Molecular Bioactivities Related to the Cell Line and Protein
Cell Line ID: CL000006  Protein ID: PT01839
 
Compound ID Compound Name Compound Formula
CP0386958
4-chloro-N-(2-methylpyrazol-3-yl)benzenesulfonamide
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C10H10ClN3O2S
 3
1
EC50 = 0.1259 nM
   TI
   LI
   LO
   TS
2
IC50 > 10000 nM
   TI
   LI
   LO
   TS
3
Ki > 10000 nM
   TI
   LI
   LO
   TS
CP0393939
4-chloro-N-(2-pyridin-2-ylpyrazol-3-yl)benzenesulfonamide
   Show/Hide
C14H11ClN4O2S
 3
1
EC50 = 0.1259 nM
   TI
   LI
   LO
   TS
2
IC50 > 10000 nM
   TI
   LI
   LO
   TS
3
Ki > 10000 nM
   TI
   LI
   LO
   TS
CP0386696
N-(2-pyridin-2-ylpyrazol-3-yl)-4-(trifluoromethyl)benzenesulfonamide
   Show/Hide
C15H11F3N4O2S
 3
1
EC50 = 0.1585 nM
   TI
   LI
   LO
   TS
2
IC50 > 10000 nM
   TI
   LI
   LO
   TS
3
Ki > 10000 nM
   TI
   LI
   LO
   TS
CP0386944
N-(2-methylpyrazol-3-yl)-4-(trifluoromethyl)benzenesulfonamide
   Show/Hide
C11H10F3N3O2S
 3
1
EC50 = 0.1585 nM
   TI
   LI
   LO
   TS
2
IC50 > 10000 nM
   TI
   LI
   LO
   TS
3
Ki > 10000 nM
   TI
   LI
   LO
   TS
CP0117986
(2S)-1-[(4R,7S,10S,13S,16S,19R)-19-amino-7-(2-amino-2-oxoethyl)-10-(3-amino-3-oxopropyl)-13-[(2S)-butan-2-yl]-16-[(4-hydroxyphenyl)methyl]-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]-N-[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]pyrrolidine-2-carboxamide
   Show/Hide
C43H66N12O12S2
 6
1
EC50 = 0.18 nM
   TI
   LI
   LO
   TS
2
EC50 = 0.19 nM
   TI
   LI
   LO
   TS
3
EC50 = 10 nM
   TI
   LI
   LO
   TS
4
EC50 = 60 nM
   TI
   LI
   LO
   TS
5
IC50 > 10000 nM
   TI
   LI
   LO
   TS
6
Ki = 20 nM
   TI
   LI
   LO
   TS
CP0192572
AVP
   Show/Hide
C46H65N15O12S2
 2
1
EC50 = 0.24 nM
   TI
   LI
   LO
   TS
2
Ki = 2 nM
   TI
   LI
   LO
   TS
CP0383082
(4R,7S,10S,13S,16S,19R)-19-amino-7-(2-amino-2-oxoethyl)-N-[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]-10-(3-amino-3-oxopropyl)-13-[(2S)-butan-2-yl]-N-[(4-fluorophenyl)methyl]-16-[(4-hydroxyphenyl)methyl]-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxamide
   Show/Hide
C47H67FN12O12S2
 1
1
EC50 = 2.2 nM
   TI
   LI
   LO
   TS
CP0386874
CHEBI:59204
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C45H69N11O12S
 3
1
EC50 = 2.3 nM
   TI
   LI
   LO
   TS
2
EC50 = 41 nM
   TI
   LI
   LO
   TS
3
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0526361
(3R,6S,9S,12S,15S,18S)-18-amino-6-(2-amino-2-oxoethyl)-N-[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]-9-(3-amino-3-oxopropyl)-12-[(2S)-butan-2-yl]-N-[(4-fluorophenyl)methyl]-15-[(4-hydroxyphenyl)methyl]-5,8,11,14,17-pentaoxo-1-thia-4,7,10,13,16-pentazacycloicosane-3-carboxamide
   Show/Hide
C48H69FN12O12S
 1
1
EC50 = 4 nM
   TI
   LI
   LO
   TS
CP0452434
(2S)-N-[(2S)-5-amino-1-[(2-amino-2-oxoethyl)amino]-1-oxopentan-2-yl]-1-[(4R,7S,10S,13S,16S,19R)-19-amino-7,10-bis(2-amino-2-oxoethyl)-13-[(2S)-butan-2-yl]-16-(furan-2-ylmethyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]pyrrolidine-2-carboxamide
   Show/Hide
C39H61N13O12S2
 1
1
EC50 = 10 nM
   TI
   LI
   LO
   TS
CP0379406
(4R,7S,10S,13S,16S)-7-(2-amino-2-oxoethyl)-N-[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]-10-(3-amino-3-oxopropyl)-13-[(2S)-butan-2-yl]-N-hexyl-16-[(4-hydroxyphenyl)methyl]-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxamide
   Show/Hide
C46H73N11O12S2
 2
1
EC50 = 12 nM
   TI
   LI
   LO
   TS
2
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0379963
(4R,7S,10S,13S,16S)-7-(2-amino-2-oxoethyl)-N-[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]-10-(3-amino-3-oxopropyl)-13-[(2S)-butan-2-yl]-16-[(4-hydroxyphenyl)methyl]-6,9,12,15,18-pentaoxo-N-pentyl-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxamide
   Show/Hide
C45H71N11O12S2
 2
1
EC50 = 19 nM
   TI
   LI
   LO
   TS
2
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0374453
(2S)-N-[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]-1-[(4R,7S,10S,13S,16S)-7-(2-amino-2-oxoethyl)-10-(3-amino-3-oxopropyl)-13-[(2S)-butan-2-yl]-16-[(4-hydroxyphenyl)methyl]-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]pyrrolidine-2-carboxamide
   Show/Hide
C43H65N11O12S2
 2
1
EC50 = 21 nM
   TI
   LI
   LO
   TS
2
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0379965
(4S,7S,10S,13S,16S)-7-(2-amino-2-oxoethyl)-N-[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]-10-(3-amino-3-oxopropyl)-13-[(2S)-butan-2-yl]-16-[(4-hydroxyphenyl)methyl]-N-[(3-methylphenyl)methyl]-6,9,12,15,18-pentaoxo-1-thia-5,8,11,14,17-pentazacycloicosane-4-carboxamide
   Show/Hide
C49H71N11O12S
 2
1
EC50 = 71 nM
   TI
   LI
   LO
   TS
2
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0386943
(4R,7S,10S,13S,16S)-7-(2-amino-2-oxoethyl)-N-[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]-10-(3-amino-3-oxopropyl)-13-[(2S)-butan-2-yl]-N-cyclobutyl-16-[(4-hydroxyphenyl)methyl]-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxamide
   Show/Hide
C44H67N11O12S2
 2
1
EC50 = 85 nM
   TI
   LI
   LO
   TS
2
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0386873
(3R,6S,9S,12S,15S)-6-(2-amino-2-oxoethyl)-N-[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]-9-(3-amino-3-oxopropyl)-12-[(2S)-butan-2-yl]-15-[(4-hydroxyphenyl)methyl]-5,8,11,14,17-pentaoxo-N-pentyl-1-thia-4,7,10,13,16-pentazacycloicosane-3-carboxamide
   Show/Hide
C46H73N11O12S
 2
1
EC50 = 86 nM
   TI
   LI
   LO
   TS
2
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0483064
(2S)-N-(4-aminobutyl)-1-[(3R,6S,9S,12S,15S)-6-(2-amino-2-oxoethyl)-15-[(4-hydroxyphenyl)methyl]-5,8,11,14,17-pentaoxo-9-propan-2-yl-12-(thiophen-2-ylmethyl)-1-thia-4,7,10,13,16-pentazacycloicosane-3-carbonyl]pyrrolidine-2-carboxamide
   Show/Hide
C41H59N9O9S2
 1
1
EC50 = 650 nM
   TI
   LI
   LO
   TS
CP0374449
(4R,7S,10S,13S,16S)-7-(2-amino-2-oxoethyl)-N-[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]-10-(3-amino-3-oxopropyl)-13-[(2S)-butan-2-yl]-N-(furan-2-ylmethyl)-16-[(4-hydroxyphenyl)methyl]-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxamide
   Show/Hide
C45H65N11O13S2
 2
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
2
IC50 = 390 nM
   TI
   LI
   LO
   TS
CP0374452
(4S,7S,10S,13S,16S)-7-(2-amino-2-oxoethyl)-N-[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]-10-(3-amino-3-oxopropyl)-13-[(2S)-butan-2-yl]-16-[(4-hydroxyphenyl)methyl]-6,9,12,15,18-pentaoxo-N-pentyl-1-thia-5,8,11,14,17-pentazacycloicosane-4-carboxamide
   Show/Hide
C46H73N11O12S
 2
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
2
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0374485
(4S,7S,10S,13S,16S)-7-(2-amino-2-oxoethyl)-N-[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]-10-(3-amino-3-oxopropyl)-N,16-dibenzyl-13-[(2S)-butan-2-yl]-6,9,12,15,18-pentaoxo-1-thia-5,8,11,14,17-pentazacycloicosane-4-carboxamide
   Show/Hide
C48H69N11O11S
 2
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
2
IC50 = 1600 nM
   TI
   LI
   LO
   TS
CP0374487
(4S,7S,10S,13S,16S)-7-(2-amino-2-oxoethyl)-N-[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]-10-(3-amino-3-oxopropyl)-16-benzyl-13-[(2S)-butan-2-yl]-N-[(3-methylphenyl)methyl]-6,9,12,15,18-pentaoxo-1-thia-5,8,11,14,17-pentazacycloicosane-4-carboxamide
   Show/Hide
C49H71N11O11S
 2
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
2
IC50 = 480 nM
   TI
   LI
   LO
   TS
CP0374490
(4R,7S,10S,13S,16S)-7-(2-amino-2-oxoethyl)-N-[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]-10-(3-amino-3-oxopropyl)-13-[(2S)-butan-2-yl]-N-butyl-16-[(4-hydroxyphenyl)methyl]-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxamide
   Show/Hide
C44H69N11O12S2
 2
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
2
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0374491
(4R,7S,10S,13S,16S)-7-(2-amino-2-oxoethyl)-N-[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]-10-(3-amino-3-oxopropyl)-13-[(2S)-butan-2-yl]-N-cyclopentyl-16-[(4-hydroxyphenyl)methyl]-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxamide
   Show/Hide
C45H69N11O12S2
 2
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
2
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0374493
(4R,7S,10S,13S,16S)-7-(2-amino-2-oxoethyl)-N-[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]-10-(3-amino-3-oxopropyl)-13-[(2S)-butan-2-yl]-16-[(4-hydroxyphenyl)methyl]-6,9,12,15,18-pentaoxo-N-(oxolan-2-ylmethyl)-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxamide
   Show/Hide
C45H69N11O13S2
 2
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
2
IC50 = 1500 nM
   TI
   LI
   LO
   TS
CP0374495
(4S,7S,10S,13S,16S)-7-(2-amino-2-oxoethyl)-N-[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]-10-(3-amino-3-oxopropyl)-16-benzyl-13-[(2S)-butan-2-yl]-N-butyl-6,9,12,15,18-pentaoxo-1-thia-5,8,11,14,17-pentazacycloicosane-4-carboxamide
   Show/Hide
C45H71N11O11S
 2
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
2
IC50 = 740 nM
   TI
   LI
   LO
   TS
CP0379228
(4R,7S,10S,13S,16S)-7-(2-amino-2-oxoethyl)-N-[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]-10-(3-amino-3-oxopropyl)-13-[(2S)-butan-2-yl]-16-[(4-hydroxyphenyl)methyl]-N-(3-hydroxypropyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxamide
   Show/Hide
C43H67N11O13S2
 2
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
2
IC50 = 3400 nM
   TI
   LI
   LO
   TS
CP0379229
(4R,7S,10S,13S,16S)-7-(2-amino-2-oxoethyl)-N-[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]-10-(3-amino-3-oxopropyl)-13-[(2S)-butan-2-yl]-N-[(4-fluorophenyl)methyl]-16-[(4-hydroxyphenyl)methyl]-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxamide
   Show/Hide
C47H66FN11O12S2
 2
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
2
IC50 = 880 nM
   TI
   LI
   LO
   TS
CP0379240
(4R,7S,10S,13S,16S)-7-(2-amino-2-oxoethyl)-N-[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]-10-(3-amino-3-oxopropyl)-13-[(2S)-butan-2-yl]-16-[(4-hydroxyphenyl)methyl]-N-(2-morpholin-4-ylethyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxamide
   Show/Hide
C46H72N12O13S2
 2
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
2
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0379243
(4R,7S,10S,13S,16S)-7-(2-amino-2-oxoethyl)-N-[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]-10-(3-amino-3-oxopropyl)-13-[(2S)-butan-2-yl]-16-[(4-hydroxyphenyl)methyl]-6,9,12,15,18-pentaoxo-N-(2-pyridin-2-ylethyl)-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxamide
   Show/Hide
C47H68N12O12S2
 2
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
2
IC50 = 730 nM
   TI
   LI
   LO
   TS
CP0379284
(4S,7S,10S,13S,16S)-7-(2-amino-2-oxoethyl)-N-[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]-10-(3-amino-3-oxopropyl)-16-benzyl-13-[(2S)-butan-2-yl]-6,9,12,15,18-pentaoxo-N-(2-phenylethyl)-1-thia-5,8,11,14,17-pentazacycloicosane-4-carboxamide
   Show/Hide
C49H71N11O11S
 2
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
2
IC50 = 330 nM
   TI
   LI
   LO
   TS
CP0379295
(3R,6S,9S,12S,15S)-6-(2-amino-2-oxoethyl)-N-[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]-9-(3-amino-3-oxopropyl)-12-[(2S)-butan-2-yl]-15-[(4-hydroxyphenyl)methyl]-N-[(3-methylphenyl)methyl]-5,8,11,14,17-pentaoxo-1-thia-4,7,10,13,16-pentazacycloicosane-3-carboxamide
   Show/Hide
C49H71N11O12S
 2
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
2
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0379296
(4S,7S,10S,13S,16S)-7-(2-amino-2-oxoethyl)-N-[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]-10-(3-amino-3-oxopropyl)-16-benzyl-13-[(2S)-butan-2-yl]-N-[(4-fluorophenyl)methyl]-6,9,12,15,18-pentaoxo-1-thia-5,8,11,14,17-pentazacycloicosane-4-carboxamide
   Show/Hide
C48H68FN11O11S
 2
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
2
IC50 = 1300 nM
   TI
   LI
   LO
   TS
CP0379412
(4S,7S,10S,13S,16S)-7-(2-amino-2-oxoethyl)-N-[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]-10-(3-amino-3-oxopropyl)-13-[(2S)-butan-2-yl]-16-[(4-hydroxyphenyl)methyl]-6,9,12,15,18-pentaoxo-N-(2-phenylethyl)-1-thia-5,8,11,14,17-pentazacycloicosane-4-carboxamide
   Show/Hide
C49H71N11O12S
 2
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
2
IC50 = 640 nM
   TI
   LI
   LO
   TS
CP0379415
(4R,7S,10S,13S,16S)-7-(2-amino-2-oxoethyl)-N-[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]-10-(3-amino-3-oxopropyl)-N-benzyl-13-[(2S)-butan-2-yl]-16-[(4-hydroxyphenyl)methyl]-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxamide
   Show/Hide
C47H67N11O12S2
 2
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
2
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0379417
(2S,4R)-N-[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]-1-[(3R,6S,9S,12S,15S)-6-(2-amino-2-oxoethyl)-9-(3-amino-3-oxopropyl)-12-[(2S)-butan-2-yl]-15-[(4-methoxyphenyl)methyl]-5,8,11,14,17-pentaoxo-1-thia-4,7,10,13,16-pentazacycloicosane-3-carbonyl]-4-methoxypyrrolidine-2-carboxamide
   Show/Hide
C46H71N11O13S
 2
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
2
IC50 = 1300 nM
   TI
   LI
   LO
   TS
CP0379419
(3R,6S,9S,12S,15S)-6-(2-amino-2-oxoethyl)-N-[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]-9-(3-amino-3-oxopropyl)-N-benzyl-12-[(2S)-butan-2-yl]-15-[(4-hydroxyphenyl)methyl]-5,8,11,14,17-pentaoxo-1-thia-4,7,10,13,16-pentazacycloicosane-3-carboxamide
   Show/Hide
C48H69N11O12S
 2
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
2
IC50 = 1400 nM
   TI
   LI
   LO
   TS
CP0379420
(3R,6S,9S,12S,15S)-6-(2-amino-2-oxoethyl)-N-[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]-9-(3-amino-3-oxopropyl)-12-[(2S)-butan-2-yl]-N-butyl-15-[(4-hydroxyphenyl)methyl]-5,8,11,14,17-pentaoxo-1-thia-4,7,10,13,16-pentazacycloicosane-3-carboxamide
   Show/Hide
C45H71N11O12S
 2
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
2
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0379421
(4S,7S,10S,13S,16S)-7-(2-amino-2-oxoethyl)-N-[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]-10-(3-amino-3-oxopropyl)-16-benzyl-13-[(2S)-butan-2-yl]-N-(2-methoxyethyl)-6,9,12,15,18-pentaoxo-1-thia-5,8,11,14,17-pentazacycloicosane-4-carboxamide
   Show/Hide
C44H69N11O12S
 2
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
2
IC50 = 2500 nM
   TI
   LI
   LO
   TS
CP0379484
(4R,7S,10S,13S,16S)-7-(2-amino-2-oxoethyl)-N-[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]-10-(3-amino-3-oxopropyl)-13-[(2S)-butan-2-yl]-16-[(4-hydroxyphenyl)methyl]-N-[(2-methylphenyl)methyl]-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxamide
   Show/Hide
C48H69N11O12S2
 2
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
2
IC50 = 1900 nM
   TI
   LI
   LO
   TS
CP0379486
(4R,7S,10S,13S,16S)-7-(2-amino-2-oxoethyl)-N-[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]-10-(3-amino-3-oxopropyl)-13-[(2S)-butan-2-yl]-16-[(4-hydroxyphenyl)methyl]-N-[(4-methoxyphenyl)methyl]-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxamide
   Show/Hide
C48H69N11O13S2
 2
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
2
IC50 = 970 nM
   TI
   LI
   LO
   TS
CP0379489
(4R,7S,10S,13S,16S)-7-(2-amino-2-oxoethyl)-N-[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]-10-(3-amino-3-oxopropyl)-13-[(2S)-butan-2-yl]-16-[(4-hydroxyphenyl)methyl]-6,9,12,15,18-pentaoxo-N-(2-phenylethyl)-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxamide
   Show/Hide
C48H69N11O12S2
 2
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
2
IC50 = 270 nM
   TI
   LI
   LO
   TS
CP0379490
(4R,7S,10S,13S,16S)-7-(2-amino-2-oxoethyl)-N-[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]-10-(3-amino-3-oxopropyl)-13-[(2S)-butan-2-yl]-16-[(4-hydroxyphenyl)methyl]-6,9,12,15,18-pentaoxo-N-(thiophen-2-ylmethyl)-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxamide
   Show/Hide
C45H65N11O12S3
 2
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
2
IC50 = 1200 nM
   TI
   LI
   LO
   TS
CP0379491
(3R,6S,9S,12S,15S)-6-(2-amino-2-oxoethyl)-N-[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]-9-(3-amino-3-oxopropyl)-12-[(2S)-butan-2-yl]-15-[(4-hydroxyphenyl)methyl]-N-(2-methoxyethyl)-5,8,11,14,17-pentaoxo-1-thia-4,7,10,13,16-pentazacycloicosane-3-carboxamide
   Show/Hide
C44H69N11O13S
 2
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
2
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0379492
(4S,7S,10S,13S,16S)-7-(2-amino-2-oxoethyl)-N-[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]-10-(3-amino-3-oxopropyl)-13-[(2S)-butan-2-yl]-16-[(4-hydroxyphenyl)methyl]-N-(3-hydroxypropyl)-6,9,12,15,18-pentaoxo-1-thia-5,8,11,14,17-pentazacycloicosane-4-carboxamide
   Show/Hide
C44H69N11O13S
 2
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
2
IC50 = 1800 nM
   TI
   LI
   LO
   TS
CP0379493
(3R,6S,9S,12S,15S)-6-(2-amino-2-oxoethyl)-N-[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]-9-(3-amino-3-oxopropyl)-12-[(2S)-butan-2-yl]-15-[(4-hydroxyphenyl)methyl]-5,8,11,14,17-pentaoxo-N-(thiophen-2-ylmethyl)-1-thia-4,7,10,13,16-pentazacycloicosane-3-carboxamide
   Show/Hide
C46H67N11O12S2
 2
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
2
IC50 = 2100 nM
   TI
   LI
   LO
   TS
CP0379964
(4R,7S,10S,13S,16S)-7-(2-amino-2-oxoethyl)-N-[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]-10-(3-amino-3-oxopropyl)-13-[(2S)-butan-2-yl]-16-[(4-hydroxyphenyl)methyl]-6,9,12,15,18-pentaoxo-N-(pyridin-2-ylmethyl)-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxamide
   Show/Hide
C46H66N12O12S2
 2
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
2
IC50 = 2200 nM
   TI
   LI
   LO
   TS
CP0379976
(4R,7S,10S,13S,16S)-7-(2-amino-2-oxoethyl)-N-[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]-10-(3-amino-3-oxopropyl)-13-[(2S)-butan-2-yl]-16-[(4-hydroxyphenyl)methyl]-N-[(4-methylphenyl)methyl]-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxamide
   Show/Hide
C48H69N11O12S2
 2
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
2
IC50 = 1400 nM
   TI
   LI
   LO
   TS
CP0379977
(4R,7S,10S,13S,16S)-7-(2-amino-2-oxoethyl)-N-[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]-10-(3-amino-3-oxopropyl)-13-[(2S)-butan-2-yl]-16-[(4-hydroxyphenyl)methyl]-6,9,12,15,18-pentaoxo-N-(pyridin-4-ylmethyl)-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxamide
   Show/Hide
C46H66N12O12S2
 2
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
2
IC50 = 3200 nM
   TI
   LI
   LO
   TS
CP0379978
(4S,7S,10S,13S,16S)-7-(2-amino-2-oxoethyl)-N-[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]-10-(3-amino-3-oxopropyl)-16-benzyl-13-[(2S)-butan-2-yl]-6,9,12,15,18-pentaoxo-N-pentyl-1-thia-5,8,11,14,17-pentazacycloicosane-4-carboxamide
   Show/Hide
C46H73N11O11S
 2
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
2
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0379979
(4S,7S,10S,13S,16S)-7-(2-amino-2-oxoethyl)-N-[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]-10-(3-amino-3-oxopropyl)-13-[(2S)-butan-2-yl]-N-[(4-fluorophenyl)methyl]-16-[(4-hydroxyphenyl)methyl]-6,9,12,15,18-pentaoxo-1-thia-5,8,11,14,17-pentazacycloicosane-4-carboxamide
   Show/Hide
C48H68FN11O12S
 2
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
2
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0381388
(4S,7S,10S,13S,16S)-7-(2-amino-2-oxoethyl)-N-[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]-10-(3-amino-3-oxopropyl)-N-benzyl-13-[(2S)-butan-2-yl]-16-[(4-hydroxyphenyl)methyl]-6,9,12,15,18-pentaoxo-1-thia-5,8,11,14,17-pentazacycloicosane-4-carboxamide
   Show/Hide
C48H69N11O12S
 2
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
2
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0381390
(4S,7S,10S,13S,16S)-7-(2-amino-2-oxoethyl)-N-[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]-10-(3-amino-3-oxopropyl)-13-[(2S)-butan-2-yl]-16-[(4-hydroxyphenyl)methyl]-6,9,12,15,18-pentaoxo-N-(thiophen-2-ylmethyl)-1-thia-5,8,11,14,17-pentazacycloicosane-4-carboxamide
   Show/Hide
C46H67N11O12S2
 2
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
2
IC50 = 380 nM
   TI
   LI
   LO
   TS
CP0381413
(4S,7S,10S,13S,16S)-7-(2-amino-2-oxoethyl)-N-[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]-10-(3-amino-3-oxopropyl)-16-benzyl-13-[(2S)-butan-2-yl]-N-(3-hydroxypropyl)-6,9,12,15,18-pentaoxo-1-thia-5,8,11,14,17-pentazacycloicosane-4-carboxamide
   Show/Hide
C44H69N11O12S
 2
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
2
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0381555
(4R,7S,10S,13S,16S)-7-(2-amino-2-oxoethyl)-N-[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]-10-(3-amino-3-oxopropyl)-13-[(2S)-butan-2-yl]-N-(cyclopropylmethyl)-16-[(4-hydroxyphenyl)methyl]-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxamide
   Show/Hide
C44H67N11O12S2
 2
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
2
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0386854
(4S,7S,10S,13S,16S)-7-(2-amino-2-oxoethyl)-N-[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]-10-(3-amino-3-oxopropyl)-16-benzyl-13-[(2S)-butan-2-yl]-6,9,12,15,18-pentaoxo-N-(thiophen-2-ylmethyl)-1-thia-5,8,11,14,17-pentazacycloicosane-4-carboxamide
   Show/Hide
C46H67N11O11S2
 2
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
2
IC50 = 1200 nM
   TI
   LI
   LO
   TS
CP0386875
(4R,7S,10S,13S,16S)-7-(2-amino-2-oxoethyl)-N-[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]-10-(3-amino-3-oxopropyl)-13-[(2S)-butan-2-yl]-16-[(4-hydroxyphenyl)methyl]-N-(2-methoxyethyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxamide
   Show/Hide
C43H67N11O13S2
 2
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
2
IC50 = 1800 nM
   TI
   LI
   LO
   TS
CP0386942
(3R,6S,9S,12S,15S)-6-(2-amino-2-oxoethyl)-N-[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]-9-(3-amino-3-oxopropyl)-12-[(2S)-butan-2-yl]-15-[(4-hydroxyphenyl)methyl]-5,8,11,14,17-pentaoxo-N-(2-phenylethyl)-1-thia-4,7,10,13,16-pentazacycloicosane-3-carboxamide
   Show/Hide
C49H71N11O12S
 2
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
2
IC50 = 490 nM
   TI
   LI
   LO
   TS
CP0389135
(4R,7S,10S,13S,16S)-7-(2-amino-2-oxoethyl)-N-[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]-10-(3-amino-3-oxopropyl)-13-[(2S)-butan-2-yl]-16-[(4-hydroxyphenyl)methyl]-6,9,12,15,18-pentaoxo-N-(pyridin-3-ylmethyl)-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxamide
   Show/Hide
C46H66N12O12S2
 2
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
2
IC50 = 1300 nM
   TI
   LI
   LO
   TS
CP0400333
(4S,7S,10S,13S,16S)-7-(2-amino-2-oxoethyl)-N-[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]-10-(3-amino-3-oxopropyl)-13-[(2S)-butan-2-yl]-N-butyl-16-[(4-hydroxyphenyl)methyl]-6,9,12,15,18-pentaoxo-1-thia-5,8,11,14,17-pentazacycloicosane-4-carboxamide
   Show/Hide
C45H71N11O12S
 2
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
2
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0400335
(4R,7S,10S,13S,16S)-7-(2-amino-2-oxoethyl)-N-[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]-10-(3-amino-3-oxopropyl)-13-[(2S)-butan-2-yl]-N-cyclohexyl-16-[(4-hydroxyphenyl)methyl]-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxamide
   Show/Hide
C46H71N11O12S2
 2
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
2
IC50 = 2000 nM
   TI
   LI
   LO
   TS
CP0410445
(4R,7S,10S,13S,16S)-7-(2-amino-2-oxoethyl)-N-[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]-10-(3-amino-3-oxopropyl)-13-[(2S)-butan-2-yl]-16-[(4-hydroxyphenyl)methyl]-6,9,12,15,18-pentaoxo-N-(2-pyrrolidin-2-ylethyl)-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxamide
   Show/Hide
C46H72N12O12S2
 2
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
2
IC50 = 1300 nM
   TI
   LI
   LO
   TS
CP0410446
(3R,6S,9S,12S,15S)-6-(2-amino-2-oxoethyl)-N-[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]-9-(3-amino-3-oxopropyl)-15-benzyl-12-[(2S)-butan-2-yl]-N-butyl-5,8,11,14,17-pentaoxo-1-thia-4,7,10,13,16-pentazacycloicosane-3-carboxamide
   Show/Hide
C45H71N11O11S
 2
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
2
IC50 = 300 nM
   TI
   LI
   LO
   TS
CP0411518
(4R,7S,10S,13S,16S)-7-(2-amino-2-oxoethyl)-N-[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]-10-(3-amino-3-oxopropyl)-13-[(2S)-butan-2-yl]-16-[(4-hydroxyphenyl)methyl]-N-[(3-methylphenyl)methyl]-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxamide
   Show/Hide
C48H69N11O12S2
 2
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
2
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0418736
(4R,7S,10S,13S,16S)-7-(2-amino-2-oxoethyl)-N-[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]-10-(3-amino-3-oxopropyl)-13-[(2S)-butan-2-yl]-16-[(4-hydroxyphenyl)methyl]-6,9,12,15,18-pentaoxo-N-(2-thiophen-2-ylethyl)-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxamide
   Show/Hide
C46H67N11O12S3
 2
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
2
IC50 = 280 nM
   TI
   LI
   LO
   TS
CP0425942
(3R,6S,9S,12S,15S)-6-(2-amino-2-oxoethyl)-N-[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]-9-(3-amino-3-oxopropyl)-15-benzyl-12-[(2S)-butan-2-yl]-N-(2-methoxyethyl)-5,8,11,14,17-pentaoxo-1-thia-4,7,10,13,16-pentazacycloicosane-3-carboxamide
   Show/Hide
C44H69N11O12S
 2
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
2
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0425948
(4R,7S,10S,13S,16S)-7-(2-amino-2-oxoethyl)-N-[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]-10-(3-amino-3-oxopropyl)-13-[(2S)-butan-2-yl]-16-[(4-hydroxyphenyl)methyl]-6,9,12,15,18-pentaoxo-N-(2-pyridin-4-ylethyl)-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxamide
   Show/Hide
C47H68N12O12S2
 2
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
2
IC50 = 350 nM
   TI
   LI
   LO
   TS
CP0459759
(4R,7S,10S,13S,16S)-7-(2-amino-2-oxoethyl)-N-[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]-10-(3-amino-3-oxopropyl)-13-[(2S)-butan-2-yl]-N-cyclopropyl-16-[(4-hydroxyphenyl)methyl]-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxamide
   Show/Hide
C43H65N11O12S2
 2
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
2
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0480508
(4S,7S,10S,13S,16S)-7-(2-amino-2-oxoethyl)-N-[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]-10-(3-amino-3-oxopropyl)-13-[(2S)-butan-2-yl]-16-[(4-hydroxyphenyl)methyl]-N-(2-methoxyethyl)-6,9,12,15,18-pentaoxo-1-thia-5,8,11,14,17-pentazacycloicosane-4-carboxamide
   Show/Hide
C44H69N11O13S
 2
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
2
IC50 = 990 nM
   TI
   LI
   LO
   TS
CP0219136
4-[(3,5-dihydroxyphenyl)methyl]-N-[[2-methyl-4-(1-methyl-4,10-dihydropyrazolo[4,3-c][1,5]benzodiazepine-5-carbonyl)phenyl]methyl]piperazine-1-carboxamide
   Show/Hide
C32H35N7O4
 6
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
2
IC50 = 7 nM
   TI
   LI
   LO
   TS
3
IC50 = 613 nM
   TI
   LI
   LO
   TS
4
Ki = 12.5 nM
   TI
   LI
   LO
   TS
5
Ki = 27 nM
   TI
   LI
   LO
   TS
6
Ki = 113 nM
   TI
   LI
   LO
   TS
CP0385080
7-[4-[(3,5-dimethoxyphenyl)methyl]piperazin-1-yl]-1-(1-methyl-4,10-dihydropyrazolo[4,3-c][1,5]benzodiazepin-5-yl)heptan-1-one
   Show/Hide
C31H42N6O3
 4
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
2
IC50 > 10000 nM
   TI
   LI
   LO
   TS
3
Ki = 194.7 nM
   TI
   LI
   LO
   TS
4
Ki = 195 nM
   TI
   LI
   LO
   TS
CP0385081
5-[4-[(3,5-dimethoxyphenyl)methyl]piperazin-1-yl]-1-(1-methyl-4,10-dihydropyrazolo[4,3-c][1,5]benzodiazepin-5-yl)pentan-1-one
   Show/Hide
C29H38N6O3
 3
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
2
IC50 > 10000 nM
   TI
   LI
   LO
   TS
3
Ki = 409 nM
   TI
   LI
   LO
   TS
CP0385082
5-[4-[(3,5-dihydroxyphenyl)methyl]piperazin-1-yl]-1-(1-methyl-4,10-dihydropyrazolo[4,3-c][1,5]benzodiazepin-5-yl)pentan-1-one
   Show/Hide
C27H34N6O3
 3
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
2
IC50 > 10000 nM
   TI
   LI
   LO
   TS
3
Ki = 466 nM
   TI
   LI
   LO
   TS
CP0385371
8-[4-[(3,5-dihydroxyphenyl)methyl]piperazin-1-yl]-1-(1-methyl-4,10-dihydropyrazolo[4,3-c][1,5]benzodiazepin-5-yl)octan-1-one
   Show/Hide
C30H40N6O3
 4
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
2
IC50 = 4667 nM
   TI
   LI
   LO
   TS
3
Ki = 64 nM
   TI
   LI
   LO
   TS
4
Ki = 64.1 nM
   TI
   LI
   LO
   TS
CP0385372
4-[(3,5-dimethoxyphenyl)methyl]-N-[[2-methyl-4-(1-methyl-4,10-dihydropyrazolo[4,3-c][1,5]benzodiazepine-5-carbonyl)phenyl]methyl]piperazine-1-carboxamide
   Show/Hide
C34H39N7O4
 3
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
2
IC50 = 1113 nM
   TI
   LI
   LO
   TS
3
Ki = 62 nM
   TI
   LI
   LO
   TS
CP0385374
8-[4-[(3,5-dimethoxyphenyl)methyl]piperazin-1-yl]-1-(1-methyl-4,10-dihydropyrazolo[4,3-c][1,5]benzodiazepin-5-yl)octan-1-one
   Show/Hide
C32H44N6O3
 3
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
2
IC50 = 7674 nM
   TI
   LI
   LO
   TS
3
Ki = 248 nM
   TI
   LI
   LO
   TS
CP0401206
6-[4-[(3,5-dihydroxyphenyl)methyl]piperazin-1-yl]-1-(1-methyl-4,10-dihydropyrazolo[4,3-c][1,5]benzodiazepin-5-yl)hexan-1-one
   Show/Hide
C28H36N6O3
 3
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
2
IC50 > 10000 nM
   TI
   LI
   LO
   TS
3
Ki = 449 nM
   TI
   LI
   LO
   TS
CP0417316
7-[4-[(3,5-dihydroxyphenyl)methyl]piperazin-1-yl]-1-(1-methyl-4,10-dihydropyrazolo[4,3-c][1,5]benzodiazepin-5-yl)heptan-1-one
   Show/Hide
C29H38N6O3
 3
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
2
IC50 > 10000 nM
   TI
   LI
   LO
   TS
3
Ki = 130 nM
   TI
   LI
   LO
   TS
CP0417317
6-[4-[(3,5-dimethoxyphenyl)methyl]piperazin-1-yl]-1-(1-methyl-4,10-dihydropyrazolo[4,3-c][1,5]benzodiazepin-5-yl)hexan-1-one
   Show/Hide
C30H40N6O3
 3
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
2
IC50 = 8203 nM
   TI
   LI
   LO
   TS
3
Ki = 266 nM
   TI
   LI
   LO
   TS
CP0389627
2-[4-[4-[(3,5-dimethoxyphenyl)methyl]piperazin-1-yl]phenyl]-1-(1-methyl-4,10-dihydropyrazolo[4,3-c][1,5]benzodiazepin-5-yl)ethanone
   Show/Hide
C32H36N6O3
 3
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
2
IC50 > 10000 nM
   TI
   LI
   LO
   TS
3
Ki = 1910 nM
   TI
   LI
   LO
   TS
CP0393045
3-[2-[4-[(3,5-dihydroxyphenyl)methyl]piperazin-1-yl]phenyl]-1-(1-methyl-4,10-dihydropyrazolo[4,3-c][1,5]benzodiazepin-5-yl)propan-1-one
   Show/Hide
C31H34N6O3
 3
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
2
IC50 > 10000 nM
   TI
   LI
   LO
   TS
3
Ki = 250.7 nM
   TI
   LI
   LO
   TS
CP0393183
2-[3-[4-[(3,5-dihydroxyphenyl)methyl]piperazin-1-yl]phenyl]-1-(1-methyl-4,10-dihydropyrazolo[4,3-c][1,5]benzodiazepin-5-yl)ethanone
   Show/Hide
C30H32N6O3
 3
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
2
IC50 > 10000 nM
   TI
   LI
   LO
   TS
3
Ki = 642.8 nM
   TI
   LI
   LO
   TS
CP0393185
2-[4-[4-[(3,5-dihydroxyphenyl)methyl]piperazin-1-yl]phenyl]-1-(1-methyl-4,10-dihydropyrazolo[4,3-c][1,5]benzodiazepin-5-yl)ethanone
   Show/Hide
C30H32N6O3
 3
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
2
IC50 > 10000 nM
   TI
   LI
   LO
   TS
3
Ki = 795.1 nM
   TI
   LI
   LO
   TS
CP0393186
3-[4-[4-[(3,5-dihydroxyphenyl)methyl]piperazin-1-yl]phenyl]-1-(1-methyl-4,10-dihydropyrazolo[4,3-c][1,5]benzodiazepin-5-yl)propan-1-one
   Show/Hide
C31H34N6O3
 3
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
2
IC50 > 10000 nM
   TI
   LI
   LO
   TS
3
Ki = 1756 nM
   TI
   LI
   LO
   TS
CP0409109
2-[3-[4-[(3,5-dimethoxyphenyl)methyl]piperazin-1-yl]phenyl]-1-(1-methyl-4,10-dihydropyrazolo[4,3-c][1,5]benzodiazepin-5-yl)ethanone
   Show/Hide
C32H36N6O3
 3
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
2
IC50 > 10000 nM
   TI
   LI
   LO
   TS
3
Ki = 2095 nM
   TI
   LI
   LO
   TS
CP0430543
2-[2-[4-[(3,5-dimethoxyphenyl)methyl]piperazin-1-yl]phenyl]-1-(1-methyl-4,10-dihydropyrazolo[4,3-c][1,5]benzodiazepin-5-yl)ethanone
   Show/Hide
C32H36N6O3
 3
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
2
IC50 > 10000 nM
   TI
   LI
   LO
   TS
3
Ki = 6807 nM
   TI
   LI
   LO
   TS
CP0430544
2-[2-[4-[(3,5-dihydroxyphenyl)methyl]piperazin-1-yl]phenyl]-1-(1-methyl-4,10-dihydropyrazolo[4,3-c][1,5]benzodiazepin-5-yl)ethanone
   Show/Hide
C30H32N6O3
 3
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
2
IC50 > 10000 nM
   TI
   LI
   LO
   TS
3
Ki = 1938 nM
   TI
   LI
   LO
   TS
CP0456589
3-[4-[4-[(3,5-dimethoxyphenyl)methyl]piperazin-1-yl]phenyl]-1-(1-methyl-4,10-dihydropyrazolo[4,3-c][1,5]benzodiazepin-5-yl)propan-1-one
   Show/Hide
C33H38N6O3
 3
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
2
IC50 > 10000 nM
   TI
   LI
   LO
   TS
3
Ki = 6250 nM
   TI
   LI
   LO
   TS
CP0456590
3-[2-[4-[(3,5-dimethoxyphenyl)methyl]piperazin-1-yl]phenyl]-1-(1-methyl-4,10-dihydropyrazolo[4,3-c][1,5]benzodiazepin-5-yl)propan-1-one
   Show/Hide
C33H38N6O3
 3
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
2
IC50 > 10000 nM
   TI
   LI
   LO
   TS
3
Ki = 1062 nM
   TI
   LI
   LO
   TS
CP0474748
3-[3-[4-[(3,5-dimethoxyphenyl)methyl]piperazin-1-yl]phenyl]-1-(1-methyl-4,10-dihydropyrazolo[4,3-c][1,5]benzodiazepin-5-yl)propan-1-one
   Show/Hide
C33H38N6O3
 3
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
2
IC50 > 10000 nM
   TI
   LI
   LO
   TS
3
Ki = 3343 nM
   TI
   LI
   LO
   TS
CP0474750
3-[3-[4-[(3,5-dihydroxyphenyl)methyl]piperazin-1-yl]phenyl]-1-(1-methyl-4,10-dihydropyrazolo[4,3-c][1,5]benzodiazepin-5-yl)propan-1-one
   Show/Hide
C31H34N6O3
 3
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
2
IC50 > 10000 nM
   TI
   LI
   LO
   TS
3
Ki = 874.1 nM
   TI
   LI
   LO
   TS
CP0426671
[4-[[(4R,7S,10S,13S,16S,19R)-7-(2-amino-2-oxoethyl)-4-[(2S)-2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]carbamoyl]pyrrolidine-1-carbonyl]-10-(3-amino-3-oxopropyl)-13-[(2S)-butan-2-yl]-19-(hexadecanoylamino)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicos-16-yl]methyl]phenyl] N-tetradecylcarbamate
   Show/Hide
C74H125N13O14S2
 1
1
EC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0528500
[4-[[(4R,7S,10S,13S,16S,19R)-7-(2-amino-2-oxoethyl)-4-[(2S)-2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]carbamoyl]pyrrolidine-1-carbonyl]-10-(3-amino-3-oxopropyl)-13-[(2S)-butan-2-yl]-19-(hexadecanoylamino)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicos-16-yl]methyl]phenyl] N-hexadecylcarbamate
   Show/Hide
C76H129N13O14S2
 1
1
EC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0548027
[4-[[(4R,7S,10S,13S,16S,19R)-7-(2-amino-2-oxoethyl)-4-[(2S)-2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]carbamoyl]pyrrolidine-1-carbonyl]-10-(3-amino-3-oxopropyl)-13-[(2S)-butan-2-yl]-19-(hexadecanoylamino)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicos-16-yl]methyl]phenyl] pentadecyl carbonate
   Show/Hide
C75H126N12O15S2
 1
1
EC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0548028
[4-[[(4R,7S,10S,13S,16S,19R)-7-(2-amino-2-oxoethyl)-4-[(2S)-2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]carbamoyl]pyrrolidine-1-carbonyl]-10-(3-amino-3-oxopropyl)-13-[(2S)-butan-2-yl]-19-(hexadecanoylamino)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicos-16-yl]methyl]phenyl] tetradecyl carbonate
   Show/Hide
C74H124N12O15S2
 1
1
EC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0548029
[4-[[(4R,7S,10S,13S,16S,19R)-7-(2-amino-2-oxoethyl)-4-[(2S)-2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]carbamoyl]pyrrolidine-1-carbonyl]-10-(3-amino-3-oxopropyl)-13-[(2S)-butan-2-yl]-19-(hexadecanoylamino)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicos-16-yl]methyl]phenyl] N-pentadecylcarbamate
   Show/Hide
C75H127N13O14S2
 1
1
EC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0550985
[4-[[(4R,7S,10S,13S,16S,19R)-7-(2-amino-2-oxoethyl)-4-[(2S)-2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]carbamoyl]pyrrolidine-1-carbonyl]-10-(3-amino-3-oxopropyl)-13-[(2S)-butan-2-yl]-19-(hexadecanoylamino)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicos-16-yl]methyl]phenyl] hexadecyl carbonate
   Show/Hide
C76H128N12O15S2
 1
1
EC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0374494
(3R,6S,9S,12S,15S)-6-(2-amino-2-oxoethyl)-N-[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]-9-(3-amino-3-oxopropyl)-12-[(2S)-butan-2-yl]-15-[(4-hydroxyphenyl)methyl]-N-(3-hydroxypropyl)-5,8,11,14,17-pentaoxo-1-thia-4,7,10,13,16-pentazacycloicosane-3-carboxamide
   Show/Hide
C44H69N11O13S
 2
1
EC50 > 10 nM
   TI
   LI
   LO
   TS
2
IC50 = 1400 nM
   TI
   LI
   LO
   TS
CP0379418
(3R,6S,9S,12S,15S)-6-(2-amino-2-oxoethyl)-N-[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]-9-(3-amino-3-oxopropyl)-12-[(2S)-butan-2-yl]-N-[(4-fluorophenyl)methyl]-15-[(4-hydroxyphenyl)methyl]-5,8,11,14,17-pentaoxo-1-thia-4,7,10,13,16-pentazacycloicosane-3-carboxamide
   Show/Hide
C48H68FN11O12S
 2
1
EC50 > 10 nM
   TI
   LI
   LO
   TS
2
IC50 = 1200 nM
   TI
   LI
   LO
   TS
CP0487989
(3R,6S,9S,12S,15S,18S)-18-amino-6-(2-amino-2-oxoethyl)-N-[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]-9-(3-amino-3-oxopropyl)-12-[(2S)-butan-2-yl]-15-[(4-hydroxyphenyl)methyl]-N-(3-hydroxypropyl)-5,8,11,14,17-pentaoxo-1-thia-4,7,10,13,16-pentazacycloicosane-3-carboxamide
   Show/Hide
C44H70N12O13S
 1
1
EC50 > 10 nM
   TI
   LI
   LO
   TS
CP0526362
(4R,7S,10S,13S,16S,19R)-19-amino-7-(2-amino-2-oxoethyl)-N-[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]-10-(3-amino-3-oxopropyl)-13-[(2S)-butan-2-yl]-16-[(4-hydroxyphenyl)methyl]-N-(3-hydroxypropyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxamide
   Show/Hide
C43H68N12O13S2
 1
1
EC50 > 10 nM
   TI
   LI
   LO
   TS
CP0410443
(2S,4S)-N-[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]-1-[(3R,6S,9S,12S,15S)-6-(2-amino-2-oxoethyl)-9-(3-amino-3-oxopropyl)-12-[(2S)-butan-2-yl]-15-[(4-ethoxyphenyl)methyl]-5,8,11,14,17-pentaoxo-1-thia-4,7,10,13,16-pentazacycloicosane-3-carbonyl]-4-methoxypyrrolidine-2-carboxamide
   Show/Hide
C47H73N11O13S
 2
1
EC50 > 100 nM
   TI
   LI
   LO
   TS
2
IC50 = 55 nM
   TI
   LI
   LO
   TS
CP0375555
(2S)-N-[(2S)-4-amino-1-[(2-amino-2-oxoethyl)amino]-1-oxobutan-2-yl]-1-[(4R,7S,10S,13S,16S,19R)-19-amino-7-(2-amino-2-oxoethyl)-10-(3-amino-3-oxopropyl)-16-(1-benzothiophen-3-ylmethyl)-13-[(2S)-butan-2-yl]-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]pyrrolidine-2-carboxamide
   Show/Hide
C43H63N13O11S3
 1
1
EC50 > 1000 nM
   TI
   LI
   LO
   TS
CP0388466
(2S)-N-[(2S)-4-amino-1-[(2-amino-2-oxoethyl)amino]-1-oxobutan-2-yl]-1-[(4R,7S,10S,13S,16S,19R)-19-amino-7-(2-amino-2-oxoethyl)-10-(3-amino-3-oxopropyl)-13-[(2S)-butan-2-yl]-16-methyl-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]pyrrolidine-2-carboxamide
   Show/Hide
C35H59N13O11S2
 1
1
EC50 > 1000 nM
   TI
   LI
   LO
   TS
CP0374451
(3R,6S,9S,12S,15S)-6-(2-amino-2-oxoethyl)-N-[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]-9-(3-amino-3-oxopropyl)-12-[(2S)-butan-2-yl]-15-[(4-methoxyphenyl)methyl]-5,8,11,14,17-pentaoxo-1-thia-4,7,10,13,16-pentazacycloicosane-3-carboxamide
   Show/Hide
C42H65N11O12S
 2
1
EC50 > 1000 nM
   TI
   LI
   LO
   TS
2
IC50 = 1400 nM
   TI
   LI
   LO
   TS
CP0379414
(2S,4S)-N-[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]-1-[(3R,6S,9S,12S,15S)-6-(2-amino-2-oxoethyl)-9-(3-amino-3-oxopropyl)-12-[(2S)-butan-2-yl]-15-[(4-ethoxyphenyl)methyl]-5,8,11,14,17-pentaoxo-1-thia-4,7,10,13,16-pentazacycloicosane-3-carbonyl]-4-hydroxypyrrolidine-2-carboxamide
   Show/Hide
C46H71N11O13S
 2
1
EC50 > 1000 nM
   TI
   LI
   LO
   TS
2
IC50 = 17 nM
   TI
   LI
   LO
   TS
CP0379479
(S)-1-((4R,7S,10S,13S,16S)-7-(2-amino-2-oxoethyl)-10-(3-amino-3-oxopropyl)-13-benzyl-16-(4-hydroxybenzyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentaazacycloicosane-4-carbonyl)-N-((R)-1-(2-amino-2-oxoethylamino)-5-guanidino-1-oxopentan-2-yl)pyrrolidine-2-carboxamide
   Show/Hide
C46H64N14O12S2
 1
1
EC50 > 1000 nM
   TI
   LI
   LO
   TS
CP0381414
(2S,4R)-N-[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]-1-[(3R,6S,9S,12S,15S)-6-(2-amino-2-oxoethyl)-9-(3-amino-3-oxopropyl)-12-[(2S)-butan-2-yl]-15-[(4-methoxyphenyl)methyl]-5,8,11,14,17-pentaoxo-1-thia-4,7,10,13,16-pentazacycloicosane-3-carbonyl]-4-methylsulfanylpyrrolidine-2-carboxamide
   Show/Hide
C46H71N11O12S2
 2
1
EC50 > 1000 nM
   TI
   LI
   LO
   TS
2
IC50 = 670 nM
   TI
   LI
   LO
   TS
CP0464288
(4R)-N-[2-(dimethylamino)ethyl]-1-({4-[(2-phenylbenzene)amido]phenyl}carbonyl)-1,2,3,5-tetrahydrospiro[1-benzazepine-4,1'-cyclopentan]-2'-ene-3'-carboxamide
   Show/Hide
C39H40N4O3
 2
1
IC50 = 2 nM
   TI
   LI
   LO
   TS
2
IC50 = 45 nM
   TI
   LI
   LO
   TS
CP0124484
3'N-(2-dimethylaminoethyl)-1-[4-(2-phenylphenylcarboxamido)benzoyl]spiro[2,3,4,5-tetrahydro-1H-benzo[b]azepine-4,1'-(2'-cyclopentene)]-3'-carboxamide
   Show/Hide
C39H40N4O3
 1
1
IC50 = 4 nM
   TI
   LI
   LO
   TS
CP0280289
3'N-(3-dimethylaminopropyl)-1-[4-(5-fluoro-2-methylphenylcarboxamido)benzoyl]spiro[2,3,4,5-tetrahydro-1H-benzo[b]azepine-4,1'-(2'-cyclopentene)]-3'-carboxamide
   Show/Hide
C35H39FN4O3
 1
1
IC50 = 4 nM
   TI
   LI
   LO
   TS
CP0454321
(4R)-1-({4-[(2-chloro-5-fluorobenzene)amido]-3-methoxyphenyl}carbonyl)-1,2,3,5-tetrahydrospiro[1-benzazepine-4,1'-cyclopentan]-2'-ene-3'-carboxylic acid
   Show/Hide
C30H26ClFN2O5
 2
1
IC50 = 5 nM
   TI
   LI
   LO
   TS
2
IC50 = 38 nM
   TI
   LI
   LO
   TS
CP0281438
3'N-(2-hydroxyethyl)-1-[4-(2-phenylphenylcarboxamido)benzoyl]spiro[2,3,4,5-tetrahydro-1H-benzo[b]azepine-4,1'-(2'-cyclopentene)]-3'-carboxamide
   Show/Hide
C37H35N3O4
 1
1
IC50 = 5 nM
   TI
   LI
   LO
   TS
CP0444371
(4R)-1-({4-[(2-chloro-5-fluorobenzene)amido]-3-ethoxyphenyl}carbonyl)-1,2,3,5-tetrahydrospiro[1-benzazepine-4,1'-cyclopentan]-2'-ene-3'-carboxylic acid
   Show/Hide
C31H28ClFN2O5
 2
1
IC50 = 8 nM
   TI
   LI
   LO
   TS
2
IC50 = 50 nM
   TI
   LI
   LO
   TS
CP0078819
(2S)-N-{2-Methyl-4-[(1-methyl-4,10-dihydropyrazolo[3,4-b]-[1,5]benzodiazepin-5(1H)-yl)carbonyl]benzyl}-2-[(4-methyl-1,4-diazepan-1-yl)carbonothioyl]pyrrolidine-1-carboxamide
   Show/Hide
C32H40N8O2S
 2
1
IC50 = 8 nM
   TI
   LI
   LO
   TS
2
Ki = 196 nM
   TI
   LI
   LO
   TS
CP0454096
N-[4-[1'-(hydroxymethyl)spiro[3,5-dihydro-2H-1-benzazepine-4,3'-cyclopentene]-1-carbonyl]phenyl]-2-phenylbenzamide
   Show/Hide
C35H32N2O3
 1
1
IC50 = 9 nM
   TI
   LI
   LO
   TS
CP0410989
1-[2-(dimethylamino)-2-sulfanylideneethyl]-3-[[2-methyl-4-(1-methyl-4,10-dihydropyrazolo[4,3-c][1,5]benzodiazepine-5-carbonyl)phenyl]methyl]urea
   Show/Hide
C25H29N7O2S
 2
1
IC50 = 9 nM
   TI
   LI
   LO
   TS
2
Ki = 82 nM
   TI
   LI
   LO
   TS
CP0464259
(4R)-1-({4-[(2-chloro-5-fluorobenzene)amido]phenyl}carbonyl)-1,2,3,5-tetrahydrospiro[1-benzazepine-4,1'-cyclopentan]-2'-ene-3'-carboxylic acid
   Show/Hide
C29H24ClFN2O4
 2
1
IC50 = 13 nM
   TI
   LI
   LO
   TS
2
IC50 = 380 nM
   TI
   LI
   LO
   TS
CP0464750
methyl 1-[4-[(2-fluorobenzoyl)amino]benzoyl]spiro[3,5-dihydro-2H-1-benzazepine-4,3'-cyclopentene]-1'-carboxylate
   Show/Hide
C30H27FN2O4
 2
1
IC50 = 15 nM
   TI
   LI
   LO
   TS
2
IC50 = 130 nM
   TI
   LI
   LO
   TS
CP0489317
N-[4-[1'-(methylaminomethyl)spiro[3,5-dihydro-2H-1-benzazepine-4,3'-cyclopentene]-1-carbonyl]phenyl]-2-phenylbenzamide
   Show/Hide
C36H35N3O2
 2
1
IC50 = 18 nM
   TI
   LI
   LO
   TS
2
IC50 = 630 nM
   TI
   LI
   LO
   TS
CP0461665
1-({4-[(2-chloro-5-fluorobenzene)amido]-3-methoxyphenyl}carbonyl)-1,2,3,5-tetrahydrospiro[1-benzazepine-4,1'-cyclopentan]-2'-ene-3'-carboxylic acid
   Show/Hide
C30H26ClFN2O5
 2
1
IC50 = 19 nM
   TI
   LI
   LO
   TS
2
IC50 = 89 nM
   TI
   LI
   LO
   TS
CP0433271
1-({4-[(2-phenylbenzene)amido]phenyl}carbonyl)-1,2,3,5-tetrahydrospiro[1-benzazepine-4,1'-cyclopentan]-2'-ene-3'-carboxylic acid
   Show/Hide
C35H30N2O4
 2
1
IC50 = 20 nM
   TI
   LI
   LO
   TS
2
IC50 = 37 nM
   TI
   LI
   LO
   TS
CP0501743
(4R)-1-({4-[(2-chloro-5-fluorobenzene)amido]-3-methoxyphenyl}carbonyl)-N-sulfamoyl-1,2,3,5-tetrahydrospiro[1-benzazepine-4,1'-cyclopentan]-2'-ene-3'-carboxamide
   Show/Hide
C30H28ClFN4O6S
 1
1
IC50 = 27 nM
   TI
   LI
   LO
   TS
CP0154509
3'N-(3-dimethylaminopropyl)-1-[4-(2-phenylphenylcarboxamido)benzoyl]spiro[2,3,4,5-tetrahydro-1H-benzo[b]azepine-4,1'-(2'-cyclopentene)]-3'-carboxamide
   Show/Hide
C40H42N4O3
 1
1
IC50 = 29 nM
   TI
   LI
   LO
   TS
CP0304035
3'N-(2-tetrahydro-1H-1-pyrrolylethyl)-1-[4-(5-fluoro-2-methylphenylcarboxamido)benzoyl]spiro[2,3,4,5-tetrahydro-1H-benzo[b]azepine-4,1'-(2'-cyclopentene)]-3'-carboxamide
   Show/Hide
C36H39FN4O3
 1
1
IC50 = 29 nM
   TI
   LI
   LO
   TS
CP0461696
1-({4-[(2-chloro-5-fluorobenzene)amido]phenyl}carbonyl)-1,2,3,5-tetrahydrospiro[1-benzazepine-4,1'-cyclopentan]-2'-ene-3'-carboxylic acid
   Show/Hide
C29H24ClFN2O4
 2
1
IC50 = 32 nM
   TI
   LI
   LO
   TS
2
IC50 = 780 nM
   TI
   LI
   LO
   TS
CP0461695
methyl 1-[4-[(2-chloro-5-fluorobenzoyl)amino]benzoyl]spiro[3,5-dihydro-2H-1-benzazepine-4,3'-cyclopentene]-1'-carboxylate
   Show/Hide
C30H26ClFN2O4
 2
1
IC50 = 40 nM
   TI
   LI
   LO
   TS
2
IC50 = 190 nM
   TI
   LI
   LO
   TS
CP0154510
(4S)-N-[2-(dimethylamino)ethyl]-1-[4-[(2-phenylbenzoyl)amino]benzoyl]spiro[3,5-dihydro-2H-1-benzazepine-4,3'-cyclopentene]-1'-carboxamide
   Show/Hide
C39H40N4O3
 1
1
IC50 = 45 nM
   TI
   LI
   LO
   TS
CP0042892
3'N-(2-hexahydro-1-pyridinylethyl)-1-[4-(5-fluoro-2-methylphenylcarboxamido)benzoyl]spiro[2,3,4,5-tetrahydro-1H-benzo[b]azepine-4,1'-(2'-cyclopentene)]-3'-carboxamide
   Show/Hide
C37H41FN4O3
 2
1
IC50 = 48 nM
   TI
   LI
   LO
   TS
2
IC50 = 71 nM
   TI
   LI
   LO
   TS
CP0410990
N,N-dimethyl-2-[[2-methyl-4-(1-methyl-4,10-dihydropyrazolo[4,3-c][1,5]benzodiazepine-5-carbonyl)phenyl]methylcarbamoylamino]acetamide
   Show/Hide
C25H29N7O3
 2
1
IC50 = 50 nM
   TI
   LI
   LO
   TS
2
Ki > 1000 nM
   TI
   LI
   LO
   TS
CP0454322
2-chloro-5-fluoro-N-(2-methoxy-4-{[(4R)-3'-(1H-1,2,3,4-tetrazol-5-yl)-1,2,3,5-tetrahydrospiro[1-benzazepine-4,1'-cyclopentan]-2'-en-1-yl]carbonyl}phenyl)benzamide
   Show/Hide
C30H26ClFN6O3
 1
1
IC50 = 63 nM
   TI
   LI
   LO
   TS
CP0056752
3'N-(2-dimethylaminoethyl)-1-[4-(5-fluoro-2-methylphenylcarboxamido)benzoyl]spiro[2,3,4,5-tetrahydro-1H-benzo[b]azepine-4,1'-(2'-cyclopentene)]-3'-carboxamide
   Show/Hide
C34H37FN4O3
 1
1
IC50 = 65 nM
   TI
   LI
   LO
   TS
CP0041307
(4R)-N-[2-(dimethylamino)ethyl]-1-[4-[(2-fluorobenzoyl)amino]benzoyl]spiro[3,5-dihydro-2H-1-benzazepine-4,3'-cyclopentene]-1'-carboxamide
   Show/Hide
C33H35FN4O3
 1
1
IC50 = 78 nM
   TI
   LI
   LO
   TS
CP0154159
2-[1-[4-(2-phenylphenylcarboxamido)benzoyl]spiro[2,3,4,5-tetrahydro-1H-benzo[b]azepine-4,1'-(2'-cyclopentene)]-3-ylcarboxamido]acetic acid
   Show/Hide
C37H33N3O5
 1
1
IC50 = 78 nM
   TI
   LI
   LO
   TS
CP0438918
2-chloro-5-fluoro-N-(4-{[(4R)-3'-(1H-imidazol-2-yl)-1,2,3,5-tetrahydrospiro[1-benzazepine-4,1'-cyclopentan]-2'-en-1-yl]carbonyl}-2-methoxyphenyl)benzamide
   Show/Hide
C32H28ClFN4O3
 1
1
IC50 = 95 nM
   TI
   LI
   LO
   TS
CP0387124
(2S)-2-N,2-N-dimethyl-1-N-[[2-methyl-4-(1-methyl-4,10-dihydropyrazolo[4,3-c][1,5]benzodiazepine-5-carbonyl)phenyl]methyl]pyrrolidine-1,2-dicarboxamide
   Show/Hide
C28H33N7O3
 2
1
IC50 = 95 nM
   TI
   LI
   LO
   TS
2
Ki > 1000 nM
   TI
   LI
   LO
   TS
CP0197121
3'N-(2-hydroxyethyl)-1-[4-(2-fluorophenylcarboxamido)benzoyl]spiro[2,3,4,5-tetrahydro-1H-benzo[b]azepine-4,1'-(2'-cyclopentene)]-3'-carboxamide
   Show/Hide
C31H30FN3O4
 1
1
IC50 = 99 nM
   TI
   LI
   LO
   TS
CP0393052
N-[3-chloro-4-[1'-(hydroxymethyl)spiro[3,5-dihydro-2H-1-benzazepine-4,3'-cyclopentene]-1-carbonyl]phenyl]-5-fluoro-2-methylbenzamide
   Show/Hide
C30H28ClFN2O3
 1
1
IC50 = 100 nM
   TI
   LI
   LO
   TS
CP0454098
1-({4-[(2-fluorobenzene)amido]phenyl}carbonyl)-1,2,3,5-tetrahydrospiro[1-benzazepine-4,1'-cyclopentan]-2'-ene-3'-carboxylic acid
   Show/Hide
C29H25FN2O4
 1
1
IC50 = 100 nM
   TI
   LI
   LO
   TS
CP0405331
(2S)-2-(dimethylcarbamothioyl)-N-[[2-methyl-4-(1-methyl-4,10-dihydropyrazolo[4,3-c][1,5]benzodiazepine-5-carbonyl)phenyl]methyl]pyrrolidine-1-carboxamide
   Show/Hide
C28H33N7O2S
 2
1
IC50 = 100 nM
   TI
   LI
   LO
   TS
2
Ki = 1253 nM
   TI
   LI
   LO
   TS
CP0387123
methyl 2-[[2-methyl-4-(1-methyl-4,10-dihydropyrazolo[4,3-c][1,5]benzodiazepine-5-carbonyl)phenyl]methylcarbamoylamino]acetate
   Show/Hide
C24H26N6O4
 2
1
IC50 = 110 nM
   TI
   LI
   LO
   TS
2
Ki > 1000 nM
   TI
   LI
   LO
   TS
CP0194057
3'N-(2-dimethylaminoethyl)-1-[4-(2-fluorophenylcarboxamido)benzoyl]spiro[2,3,4,5-tetrahydro-1H-benzo[b]azepine-4,1'-(2'-cyclopentene)]-3'-carboxamide
   Show/Hide
C33H35FN4O3
 1
1
IC50 = 126 nM
   TI
   LI
   LO
   TS
CP0289902
methyl 2-[[1-[4-[(5-fluoro-2-methylbenzoyl)amino]benzoyl]spiro[3,5-dihydro-2H-1-benzazepine-4,3'-cyclopentene]-1'-carbonyl]amino]acetate
   Show/Hide
C33H32FN3O5
 1
1
IC50 = 135 nM
   TI
   LI
   LO
   TS
CP0040044
3-chloro-4-(10,11-dihydro-5H-benzo[e]pyrrolo[1,2-a][1,4]diazepin-10-ylcarbonyl)-1-(5-fluoro-2-methylphenylcarboxamido)benzene
   Show/Hide
C27H21ClFN3O2
 2
1
IC50 = 150 nM
   TI
   LI
   LO
   TS
2
IC50 > 5000 nM
   TI
   LI
   LO
   TS
CP0105811
3'N-(2-tetrahydro-1H-1-pyrrolylethyl)-1-[4-(2-fluorophenylcarboxamido)benzoyl]spiro[2,3,4,5-tetrahydro-1H-benzo[b]azepine-4,1'-(2'-cyclopentene)]-3'-carboxamide
   Show/Hide
C35H37FN4O3
 1
1
IC50 = 155 nM
   TI
   LI
   LO
   TS
CP0279457
4-{2-[1-[4-(2-fluorophenylcarboxamido)benzoyl]spiro[2,3,4,5-tetrahydro-1H-benzo[b]azepine-4,1'-(2'-cyclopentene)]-3-ylcarboxamido]ethyl}-1,4-oxazinane
   Show/Hide
C35H37FN4O4
 1
1
IC50 = 227 nM
   TI
   LI
   LO
   TS
CP0433272
2-chloro-N-(4-{[(4R)-3'-(4,5-dihydro-1H-imidazol-2-yl)-1,2,3,5-tetrahydrospiro[1-benzazepine-4,1'-cyclopentan]-2'-en-1-yl]carbonyl}-2-methoxyphenyl)-5-fluorobenzamide
   Show/Hide
C32H30ClFN4O3
 1
1
IC50 = 320 nM
   TI
   LI
   LO
   TS
CP0440682
2-[5-[(1S,5R)-1-(2-chloro-4-fluorophenyl)-3-azabicyclo[3.1.0]hexan-3-yl]-4-(6-methoxypyridin-3-yl)-1,2,4-triazol-3-yl]acetonitrile
   Show/Hide
C21H18ClFN6O
 1
1
IC50 = 769 nM
   TI
   LI
   LO
   TS
CP0455169
(1S,5R)-3-[4-(1,3-benzodioxol-5-yl)-5-(methoxymethyl)-1,2,4-triazol-3-yl]-1-(2-chloro-4-fluorophenyl)-3-azabicyclo[3.1.0]hexane
   Show/Hide
C22H20ClFN4O3
 1
1
IC50 = 810 nM
   TI
   LI
   LO
   TS
CP0440684
(1S,5R)-1-(2-chloro-4-fluorophenyl)-3-[5-(2-fluoroethoxymethyl)-4-(6-methoxypyridin-3-yl)-1,2,4-triazol-3-yl]-3-azabicyclo[3.1.0]hexane
   Show/Hide
C22H22ClF2N5O2
 1
1
IC50 = 819 nM
   TI
   LI
   LO
   TS
CP0304375
3'N-(2-hexahydro-1-pyridinylethyl)-1-[4-(2-fluorophenylcarboxamido)benzoyl]spiro[2,3,4,5-tetrahydro-1H-benzo[b]azepine-4,1'-(2'-cyclopentene)]-3'-carboxamide
   Show/Hide
C36H39FN4O3
 1
1
IC50 = 950 nM
   TI
   LI
   LO
   TS
CP0467938
(1S,5R)-1-(2-chloro-4-fluorophenyl)-3-[5-(ethoxymethyl)-4-(6-methoxypyridin-3-yl)-1,2,4-triazol-3-yl]-3-azabicyclo[3.1.0]hexane
   Show/Hide
C22H23ClFN5O2
 1
1
IC50 = 1757 nM
   TI
   LI
   LO
   TS
CP0467939
(1S,5R)-1-(2-chloro-4-fluorophenyl)-3-[5-(difluoromethyl)-4-(6-methoxypyridin-3-yl)-1,2,4-triazol-3-yl]-3-azabicyclo[3.1.0]hexane
   Show/Hide
C20H17ClF3N5O
 1
1
IC50 = 1867 nM
   TI
   LI
   LO
   TS
CP0467937
(1S,5R)-1-(2-chloro-4-fluorophenyl)-3-[4-(6-methoxypyridin-3-yl)-5-[[(3R)-oxolan-3-yl]oxymethyl]-1,2,4-triazol-3-yl]-3-azabicyclo[3.1.0]hexane
   Show/Hide
C24H25ClFN5O3
 1
1
IC50 = 1979 nM
   TI
   LI
   LO
   TS
CP0169179
(1S,5R)-1-(2-chloro-4-fluorophenyl)-3-[5-(methoxymethyl)-4-(6-methoxypyridin-3-yl)-1,2,4-triazol-3-yl]-3-azabicyclo[3.1.0]hexane
   Show/Hide
C21H21ClFN5O2
 1
1
IC50 = 2885 nM
   TI
   LI
   LO
   TS
CP0479500
(1S,5R)-1-(2-chloro-3-fluorophenyl)-3-[5-(methoxymethyl)-4-(6-methoxypyridin-3-yl)-1,2,4-triazol-3-yl]-3-azabicyclo[3.1.0]hexane
   Show/Hide
C21H21ClFN5O2
 1
1
IC50 = 3811 nM
   TI
   LI
   LO
   TS
CP0440685
(1S,5R)-1-(2-chloro-4-fluorophenyl)-3-[4-(6-methoxypyridin-3-yl)-5-(oxan-4-yloxymethyl)-1,2,4-triazol-3-yl]-3-azabicyclo[3.1.0]hexane
   Show/Hide
C25H27ClFN5O3
 1
1
IC50 = 4697 nM
   TI
   LI
   LO
   TS
CP0534259
(1S,5R)-1-(2-chloro-4-fluorophenyl)-3-[4-(6-methoxypyridin-3-yl)-5-[[(3S)-oxolan-3-yl]oxymethyl]-1,2,4-triazol-3-yl]-3-azabicyclo[3.1.0]hexane
   Show/Hide
C24H25ClFN5O3
 1
1
IC50 = 7520 nM
   TI
   LI
   LO
   TS
CP0431543
(1S,5R)-1-(2-chloro-4-fluorophenyl)-3-[5-cyclopropyl-4-(6-methoxypyridin-3-yl)-1,2,4-triazol-3-yl]-3-azabicyclo[3.1.0]hexane
   Show/Hide
C22H21ClFN5O
 1
1
IC50 = 10970 nM
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CP0433270
1-({4-[(5-fluoro-2-methylbenzene)amido]-2-methoxyphenyl}carbonyl)-1,2,3,5-tetrahydrospiro[1-benzazepine-4,1'-cyclopentan]-2'-ene-3'-carboxylic acid
   Show/Hide
C31H29FN2O5
 1
1
IC50 = 11600 nM
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CP0400285
2-[(1E,3E,5Z)-5-[3-[4-[2-[3-[4-[(4-chlorophenyl)-[2-[(2-hydroxy-1H-indol-3-yl)diazenyl]-2-oxoethyl]sulfamoyl]phenyl]propanoylamino]ethylamino]-4-oxobutyl]-1-ethyl-3-methyl-5-sulfoindol-2-ylidene]penta-1,3-dienyl]-1-ethyl-3,3-dimethylindol-1-ium-6-sulfonate
   Show/Hide
C59H63ClN8O12S3
 1
1
Kd = 19.7 nM
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CP0400286
CHEMBL3416749
   Show/Hide
C54H48ClN7O12S
 1
1
Kd = 61 nM
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CP0847936
2-(5-(3-(1-(5-(3-(2-chloro-4-fluorophenoxy)azetidin-1-yl)-4-(6-methoxypyridinium-3-yl)-4H-1,2,4-triazol-3-yl)-15-oxo-2,5,8,11-tetraoxa-14-azaoctadecan-18-yl)-1-ethyl-3-methyl-5-sulfoindolin-2-ylidene)penta-1,3-dienyl)-1-ethyl-3,3-dimethyl-3H-indolium-6-sulfonate 2,2,2-trifluoroacetate
   Show/Hide
C60H71ClF4N8O15S2
 1
1
Kd > 1000 nM
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CP0847937
2-(5-(3-(1-(5-(3-(2-chloro-4-fluorophenoxy)azetidin-1-yl)-4-(6-methoxypyridinium-3-yl)-4H-1,2,4-triazol-3-yl)-27-oxo-2,5,8,11,14,17,20,23-octaoxa-26-azatriacontan-30-yl)-1-ethyl-3-methyl-5-sulfoindolin-2-ylidene)penta-1,3-dienyl)-1-ethyl-3,3-dimethyl-3H-indolium-6-sulfonate 2,2,2-trifluoroacetate
   Show/Hide
C68H87ClF4N8O19S2
 1
1
Kd > 1000 nM
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CP0859026
5-(3-(34-(3-carboxy-4-(3-oxo-3H-xanthen-9-yl)phenyl)-27,34-dioxo-2,5,8,11,14,17,20,23-octaoxa-26,33-diazatetratriacontyl)-5-(3-(2-chloro-4-fluorophenoxy)azetidin-1-yl)-4H-1,2,4-triazol-4-yl)-2-methoxypyridinium 2,2,2-trifluoroacetate
   Show/Hide
C63H72ClF4N7O19
 1
1
Kd > 1000 nM
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CP0859027
5-(3-(22-(3-carboxy-4-(3-oxo-3H-xanthen-9-yl)phenyl)-15,22-dioxo-2,5,8,11-tetraoxa-14,21-diazadocosyl)-5-(3-(2-chloro-4-fluorophenoxy)azetidin-1-yl)-4H-1,2,4-triazol-4-yl)-2-methoxypyridinium 2,2,2-trifluoroacetate
   Show/Hide
C55H56ClF4N7O15
 1
1
Kd > 1000 nM
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CP0419751
2-[6-chloro-3-(spiro[1H-2-benzofuran-3,4'-piperidine]-1'-carbonyl)indol-1-yl]-N,N-dimethylacetamide
   Show/Hide
C25H26ClN3O3
 1
1
Ki = 0.5 nM
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CP0244529
[6-chloro-1-[2-(dimethylamino)ethyl]indol-3-yl]-spiro[1H-2-benzofuran-3,4'-piperidine]-1'-ylmethanone
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C25H28ClN3O2
 1
1
Ki = 1 nM
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CP0379184
2-[6-chloro-3-(spiro[1H-2-benzofuran-3,4'-piperidine]-1'-carbonyl)indol-1-yl]-1-(4-methylpiperazin-1-yl)ethanone
   Show/Hide
C28H31ClN4O3
 1
1
Ki = 1 nM
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CP0441648
[6-chloro-1-[[(2S)-1-methylpyrrolidin-2-yl]methyl]indol-3-yl]-spiro[1H-2-benzofuran-3,4'-piperidine]-1'-ylmethanone
   Show/Hide
C27H30ClN3O2
 1
1
Ki = 1 nM
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CP0474312
N-[4-[(5R)-5-hydroxy-2,3,4,5-tetrahydro-1-benzazepine-1-carbonyl]phenyl]-2-methylbenzamide
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C25H24N2O3
 1
1
Ki = 1.03 nM
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CP0379185
[6-chloro-1-[[(2S)-pyrrolidin-2-yl]methyl]indol-3-yl]-spiro[1H-2-benzofuran-3,4'-piperidine]-1'-ylmethanone
   Show/Hide
C26H28ClN3O2
 1
1
Ki = 1.4 nM
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CP0548474
N-[4-(5-hydroxy-2,3,4,5-tetrahydro-1-benzazepine-1-carbonyl)phenyl]-2-methylbenzamide
   Show/Hide
C25H24N2O3
 1
1
Ki = 1.58 nM
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CP0474311
N-[4-[(5S)-5-hydroxy-2,3,4,5-tetrahydro-1-benzazepine-1-carbonyl]phenyl]-2-methylbenzamide
   Show/Hide
C25H24N2O3
 1
1
Ki = 1.85 nM
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CP0246508
(1-benzyl-2-methylindol-3-yl)-spiro[1H-2-benzofuran-3,4'-piperidine]-1'-ylmethanone
   Show/Hide
C29H28N2O2
 1
1
Ki = 2 nM
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CP0379179
2-[6-chloro-3-(spiro[1H-2-benzofuran-3,4'-piperidine]-1'-carbonyl)indol-1-yl]-N-[2-(dimethylamino)ethyl]acetamide
   Show/Hide
C27H31ClN4O3
 1
1
Ki = 2 nM
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CP0573811
N-[4-[(5S)-5-hydroxy-6-methyl-2,3,4,5-tetrahydro-1-benzazepine-1-carbonyl]phenyl]-2-methylbenzamide
   Show/Hide
C26H26N2O3
 1
1
Ki = 2.06 nM
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CP0543049
N-[4-[(5R)-5-hydroxy-9-methyl-2,3,4,5-tetrahydro-1-benzazepine-1-carbonyl]phenyl]-2-methylbenzamide
   Show/Hide
C26H26N2O3
 1
1
Ki = 2.84 nM
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CP0379178
[6-chloro-1-(1-methylpiperidin-4-yl)indol-3-yl]-spiro[1H-2-benzofuran-3,4'-piperidine]-1'-ylmethanone
   Show/Hide
C27H30ClN3O2
 1
1
Ki = 4 nM
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CP0441646
(6-chloro-1H-indol-3-yl)-spiro[1H-2-benzofuran-3,4'-piperidine]-1'-ylmethanone
   Show/Hide
C21H19ClN2O2
 1
1
Ki = 4 nM
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CP0521728
N-[4-[(5S)-5-hydroxy-9-methyl-2,3,4,5-tetrahydro-1-benzazepine-1-carbonyl]phenyl]-2-methylbenzamide
   Show/Hide
C26H26N2O3
 1
1
Ki = 4.68 nM
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CP0379183
(6-chloro-1H-indol-3-yl)-spiro[5H-furo[3,4-b]pyridine-7,4'-piperidine]-1'-ylmethanone
   Show/Hide
C20H18ClN3O2
 1
1
Ki = 5 nM
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CP0433525
1'-(6-chloro-1H-indole-3-carbonyl)spiro[2-benzofuran-3,4'-piperidine]-1-one
   Show/Hide
C21H17ClN2O3
 1
1
Ki = 5 nM
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CP0548473
N-[4-(5-hydroxy-9-methyl-2,3,4,5-tetrahydro-1-benzazepine-1-carbonyl)phenyl]-2-methylbenzamide
   Show/Hide
C26H26N2O3
 1
1
Ki = 6.26 nM
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CP0521729
N-[4-(5-hydroxy-6-methyl-2,3,4,5-tetrahydro-1-benzazepine-1-carbonyl)phenyl]-2-methylbenzamide
   Show/Hide
C26H26N2O3
 1
1
Ki = 6.75 nM
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CP0379180
3-[1-(6-chloro-1H-indole-3-carbonyl)piperidin-4-yl]-1H-benzimidazol-2-one
   Show/Hide
C21H19ClN4O2
 1
1
Ki = 8 nM
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CP0499768
(6-chloro-1H-indol-3-yl)-spiro[1H-furo[3,4-c]pyridine-3,4'-piperidine]-1'-ylmethanone
   Show/Hide
C20H18ClN3O2
 1
1
Ki = 9 nM
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CP0419749
(6-chloro-1H-indol-3-yl)-spiro[2H-1-benzofuran-3,4'-piperidine]-1'-ylmethanone
   Show/Hide
C21H19ClN2O2
 1
1
Ki = 16 nM
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CP0196743
1N-{4-[6-chloro-16-methyl-(12S)-2,10-diazatetracyclo[11.2.1.02,12.04,9]hexadeca-4(9),5,7-trien-10-ylcarbonyl]phenyl}-2-(4-methylphenyl)benzamide
   Show/Hide
C35H32ClN3O2
 1
1
Ki = 23 nM
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CP0498957
(6-chloro-1H-indol-3-yl)-(4-phenylpiperidin-1-yl)methanone
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C20H19ClN2O
 1
1
Ki = 23 nM
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CP0398079
(6-chloro-1H-indol-3-yl)-(2,2-dioxospiro[1H-2-benzothiophene-3,4'-piperidine]-1'-yl)methanone
   Show/Hide
C21H19ClN2O3S
 1
1
Ki = 24 nM
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CP0379181
(6-chloro-1H-indol-3-yl)-spiro[1,2-dihydroindole-3,4'-piperidine]-1'-ylmethanone
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C21H20ClN3O
 1
1
Ki = 27 nM
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CP0430562
(2S)-N-[(2S)-1-[(2-amino-2-oxoethyl)amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-1-[(5R,8S,11S,14S,17S)-8-(2-amino-2-oxoethyl)-11-(3-amino-3-oxopropyl)-14-[(2S)-butan-2-yl]-17-[(4-hydroxyphenyl)methyl]-7,10,13,16,19-pentaoxo-3,22-dithia-6,9,12,15,18-pentazabicyclo[22.4.0]octacosa-1(28),24,26-triene-5-carbonyl]pyrrolidine-2-carboxamide
   Show/Hide
C51H74N14O12S2
 1
1
Ki = 30 nM
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CP0379186
1'-(6-chloro-1H-indole-3-carbonyl)spiro[1H-3,1-benzoxazine-4,4'-piperidine]-2-one
   Show/Hide
C21H18ClN3O3
 1
1
Ki = 32 nM
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CP0419752
1H-indol-3-yl(spiro[1H-2-benzofuran-3,4'-piperidine]-1'-yl)methanone
   Show/Hide
C21H20N2O2
 1
1
Ki = 32 nM
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CP0379182
(6-chloro-1H-indol-3-yl)-spiro[7H-furo[3,4-b]pyridine-5,4'-piperidine]-1'-ylmethanone
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C20H18ClN3O2
 1
1
Ki = 39 nM
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CP0206403
1N-{4-[6-chloro-16-methyl-(12S)-2,10-diazatetracyclo[11.2.1.02,12.04,9]hexadeca-4(9),5,7-trien-10-ylcarbonyl]phenyl}-2-trifluoromethylbenzamide
   Show/Hide
C29H25ClF3N3O2
 1
1
Ki = 40 nM
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CP0386760
(2S)-N-[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]-1-[(5R,8S,11S,14S,17S)-8-(2-amino-2-oxoethyl)-11-(3-amino-3-oxopropyl)-14-[(2S)-butan-2-yl]-17-[(4-hydroxyphenyl)methyl]-7,10,13,16,19-pentaoxo-3,22-dithia-6,9,12,15,18-pentazabicyclo[22.4.0]octacosa-1(28),24,26-triene-5-carbonyl]pyrrolidine-2-carboxamide
   Show/Hide
C51H73N11O12S2
 1
1
Ki = 69 nM
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CP0543048
N-[4-[(5R)-5-hydroxy-6-methyl-2,3,4,5-tetrahydro-1-benzazepine-1-carbonyl]phenyl]-2-methylbenzamide
   Show/Hide
C26H26N2O3
 1
1
Ki = 78 nM
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CP0308266
(2-ethoxynaphthalen-1-yl)-spiro[1H-2-benzofuran-3,4'-piperidine]-1'-ylmethanone
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C25H25NO3
 1
1
Ki = 81 nM
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CP0433526
(6-chloro-1H-indol-3-yl)-[4-(2-chlorophenyl)piperazin-1-yl]methanone
   Show/Hide
C19H17Cl2N3O
 1
1
Ki = 118 nM
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CP0106503
3-chloro-4-[16-methyl-(12S)-2,10-diazatetracyclo[11.2.1.02,12.04,9]hexadeca-4(9),5,7-trien-10-ylcarbonyl]-1-(2-phenylphenylcarboxamido)benzene
   Show/Hide
C34H30ClN3O2
 1
1
Ki = 130 nM
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CP0219489
1N-{4-[6-chloro-16-methyl-(12S)-2,10-diazatetracyclo[11.2.1.02,12.04,9]hexadeca-4(9),5,7-trien-10-ylcarbonyl]phenyl}-2-chlorobenzamide
   Show/Hide
C28H25Cl2N3O2
 1
1
Ki = 130 nM
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CP0219211
(4-benzyl-4-hydroxypiperidin-1-yl)-(1-benzyl-2-methylindol-3-yl)methanone
   Show/Hide
C29H30N2O2
 1
1
Ki = 295 nM
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CP0062116
1N-{4-[6-chloro-16-ethyl-(12S)-2,10-diazatetracyclo[11.2.1.02,12.04,9]hexadeca-4(9),5,7-trien-10-ylcarbonyl]phenyl}-2-chlorobenzamide
   Show/Hide
C29H27Cl2N3O2
 1
1
Ki = 620 nM
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CP0365138
2-Methyl-N-[4-(2,3,4,5-tetrahydro-benzo[b][1,4]diazepine-1-carbonyl)-phenyl]-benzamide
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C24H23N3O2
 1
1
Ki = 890 nM
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CP0387328
(2S)-N-[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]-1-[(5R,8S,11S,14S,17S)-8-(2-amino-2-oxoethyl)-11-(3-amino-3-oxopropyl)-14-[(2S)-butan-2-yl]-17-[(4-hydroxyphenyl)methyl]-7,10,13,16,19-pentaoxo-3,22-dithia-6,9,12,15,18-pentazabicyclo[22.3.1]octacosa-1(27),24(28),25-triene-5-carbonyl]pyrrolidine-2-carboxamide
   Show/Hide
C51H73N11O12S2
 1
1
Ki = 1681 nM
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CP0476263
(2S)-N-[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]-1-[(4R,7S,10S,13S,16S)-7-(2-amino-2-oxoethyl)-10-(3-amino-3-oxopropyl)-13-[(2S)-butan-2-yl]-16-[(4-hydroxyphenyl)methyl]-6,9,12,15,18-pentaoxo-2,21-dithia-5,8,11,14,17-pentazabicyclo[21.2.2]heptacosa-1(25),23,26-triene-4-carbonyl]pyrrolidine-2-carboxamide
   Show/Hide
C50H71N11O12S2
 1
1
Ki = 1954 nM
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CP0104567
1N-{4-[6-chloro-16-methyl-(12S)-2,10-diazatetracyclo[11.2.1.02,12.04,9]hexadeca-4(9),5,7-trien-10-ylcarbonyl]phenyl}-2-fluorobenzamide
   Show/Hide
C28H25ClFN3O2
 1
1
Ki = 2600 nM
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CP0106713
(4-benzyl-4-hydroxypiperidin-1-yl)-(2-ethoxynaphthalen-1-yl)methanone
   Show/Hide
C25H27NO3
 1
1
Ki = 2830 nM
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CP0441650
[3-(4-benzyl-4-hydroxypiperidine-1-carbonyl)-2-methylindol-1-yl]-phenylmethanone
   Show/Hide
C29H28N2O3
 1
1
Ki = 3900 nM
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CP0433529
[1-(benzenesulfonyl)-2-methylindol-3-yl]-(4-benzyl-4-hydroxypiperidin-1-yl)methanone
   Show/Hide
C28H28N2O4S
 1
1
Ki = 4990 nM
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CP0379188
(4-benzyl-4-hydroxypiperidin-1-yl)-naphthalen-1-ylmethanone
   Show/Hide
C23H23NO2
 1
1
Ki = 6620 nM
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