Protein Information

General Information of the Protein

Protein ID	PT00973
Protein Name	Methionine aminopeptidase 2
Secondarily Protein Name	Initiation factor 2-associated 67 kDa glycoprotein Peptidase M
Gene Name	METAP2
Secondarily Gene Name	MNPEP P67EIF2
Sequence	MAGVEEVAASGSHLNGDLDPDDREEGAASTAEEAAKKKRRKKKKSKGPSAAGEQEPDKESGASVDEVARQLERSALEDKERDEDDEDGDGDGDGATGKKKKKKKKKRGPKVQTDPPSVPICDLYPNGVFPKGQECEYPPTQDGRTAAWRTTSEEKKALDQASEEIWNDFREAAEAHRQVRKYVMSWIKPGMTMIEICEKLEDCSRKLIKENGLNAGLAFPTGCSLNNCAAHYTPNAGDTTVLQYDDICKIDFGTHISGRIIDCAFTVTFNPKYDTLLKAVKDATNTGIKCAGIDVRLCDVGEAIQEVMESYEVEIDGKTYQVKPIRNLNGHSIGQYRIHAGKTVPIVKGGEATRMEEGEVYAIETFGSTGKGVVHDDMECSHYMKNFDVGHVPIRLPRTKHLLNVINENFGTLAFCRRWLDRLGESKYLMALKNLCDLGIVDPYPPLCDIKGSYTAQFEHTILLRPTCKEVVSRGDDY Show/Hide
Organism	Homo sapiens, Human
Protein Classification	Enzyme > Protease > Metallo protease > Metallo protease MG clan > Metallo protease M24A subfamily
Function	Cotranslationally removes the N-terminal methionine from nascent proteins. The N-terminal methionine is often cleaved when the second residue in the primary sequence is small and uncharged (Met-Ala-, Cys, Gly, Pro, Ser, Thr, or Val). The catalytic activity of human METAP2 toward Met-Val peptides is consistently two orders of magnitude higher than that of METAP1, suggesting that it is responsible for processing proteins containing N-terminal Met-Val and Met-Thr sequences in vivo. Show/Hide
Uniprot ID	Primary ID: P50579 Secondarily ID: B2RDI8 B4DUX5 G3XA91 Q8NB11 Show/Hide
Ensembl ID	ENSG00000111142
HGNC ID	HGNC:16672
Subcellular Location	Cytoplasm

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: CL000023 , BTI-Tn-5B1-4

Cell Line Info

Compound ID	Compound Name	Compound Formula
CP0405902 Compound Info	N-[(1R)-2-[[5-chloro-6-methyl-2-(5-pyrrolidin-1-ylpyridin-2-yl)pyrimidin-4-yl]amino]-1-phenylethyl]-4-piperazin-1-ylbutanamide Show/Hide	C30H39ClN8O	1
1	EC50 = 1100 nM Bioactivity Info	TI LI LO TS
CP0380735 Compound Info	N-[(1R)-2-[[5-chloro-2-(5-fluoropyridin-2-yl)-6-methylpyrimidin-4-yl]amino]-1-phenylethyl]-4-piperazin-1-ylbutanamide Show/Hide	C26H31ClFN7O	1
1	EC50 = 1200 nM Bioactivity Info	TI LI LO TS
CP0525718 Compound Info	N-[(1R)-2-[[5-chloro-2-(5-chloropyridin-2-yl)-6-methylpyrimidin-4-yl]amino]-1-phenylethyl]-4-piperazin-1-ylbutanamide Show/Hide	C26H31Cl2N7O	1
1	EC50 = 1200 nM Bioactivity Info	TI LI LO TS
CP0525717 Compound Info	N-[(1R)-2-[[5-chloro-2-[5-(dimethylamino)pyridin-2-yl]-6-methylpyrimidin-4-yl]amino]-1-phenylethyl]-4-piperazin-1-ylbutanamide Show/Hide	C28H37ClN8O	1
1	EC50 = 1700 nM Bioactivity Info	TI LI LO TS
CP0380766 Compound Info	N-[(1R)-2-[[5-chloro-6-methyl-2-(5-nitropyridin-2-yl)pyrimidin-4-yl]amino]-1-phenylethyl]-4-piperazin-1-ylbutanamide Show/Hide	C26H31ClN8O3	1
1	EC50 = 14000 nM Bioactivity Info	TI LI LO TS
CP0560690 Compound Info	N-[(1R)-2-[[5-chloro-2-(4-methoxypyridin-2-yl)-6-methylpyrimidin-4-yl]amino]-1-phenylethyl]-4-piperazin-1-ylbutanamide Show/Hide	C27H34ClN7O2	1
1	EC50 = 14000 nM Bioactivity Info	TI LI LO TS
CP0180564 Compound Info	4-[4-[[(1R)-2-[[5-chloro-2-(5-chloropyridin-2-yl)-6-methylpyrimidin-4-yl]amino]-1-phenylethyl]amino]butyl]benzonitrile Show/Hide	C29H28Cl2N6	1
1	EC50 = 16000 nM Bioactivity Info	TI LI LO TS
CP0559150 Compound Info	N-[(1R)-2-[[5-chloro-2-(5-chloropyridin-2-yl)-6-methylpyrimidin-4-yl]amino]-1-phenylethyl]-2-phenylacetamide Show/Hide	C26H23Cl2N5O	1
1	EC50 = 28000 nM Bioactivity Info	TI LI LO TS
CP0374970 Compound Info	(1R)-N'-[5-chloro-2-(5-chloropyridin-2-yl)-6-methylpyrimidin-4-yl]-1-phenyl-N-(6-phenylhexyl)ethane-1,2-diamine Show/Hide	C30H33Cl2N5	1
1	EC50 > 30000 nM Bioactivity Info	TI LI LO TS
CP0380765 Compound Info	N-[(1R)-2-[[5-chloro-2-(5-chloropyridin-2-yl)-6-methylpyrimidin-4-yl]amino]-1-phenylethyl]-6-phenylhexanamide Show/Hide	C30H31Cl2N5O	1
1	EC50 > 30000 nM Bioactivity Info	TI LI LO TS
CP0380768 Compound Info	N-[(1R)-2-[[5-chloro-2-(6-chloropyridin-2-yl)-6-methylpyrimidin-4-yl]amino]-1-phenylethyl]-4-piperazin-1-ylbutanamide Show/Hide	C26H31Cl2N7O	1
1	EC50 > 30000 nM Bioactivity Info	TI LI LO TS
CP0432353 Compound Info	N-[(1R)-2-[[5-chloro-2-(5-chloropyridin-2-yl)-6-methylpyrimidin-4-yl]amino]-1-phenylethyl]-3-phenylpropanamide Show/Hide	C27H25Cl2N5O	1
1	EC50 > 30000 nM Bioactivity Info	TI LI LO TS
CP0491567 Compound Info	N-[(1R)-2-[[5-chloro-2-(5-chloropyridin-2-yl)-6-methylpyrimidin-4-yl]amino]-1-phenylethyl]-4-phenylbutanamide Show/Hide	C28H27Cl2N5O	1
1	EC50 > 30000 nM Bioactivity Info	TI LI LO TS
CP0508647 Compound Info	N-[(1R)-2-[[5-chloro-2-(5-chloropyridin-2-yl)-6-methylpyrimidin-4-yl]amino]-1-phenylethyl]-5-phenylpentanamide Show/Hide	C29H29Cl2N5O	1
1	EC50 > 30000 nM Bioactivity Info	TI LI LO TS
CP0508648 Compound Info	N-[(1R)-2-[[5-chloro-2-(6-methoxypyridin-2-yl)-6-methylpyrimidin-4-yl]amino]-1-phenylethyl]-4-piperazin-1-ylbutanamide Show/Hide	C27H34ClN7O2	1
1	EC50 > 30000 nM Bioactivity Info	TI LI LO TS
CP0536154 Compound Info	(1R)-N-benzyl-N'-[5-chloro-2-(5-chloropyridin-2-yl)-6-methylpyrimidin-4-yl]-1-phenylethane-1,2-diamine Show/Hide	C25H23Cl2N5	1
1	EC50 = 31000 nM Bioactivity Info	TI LI LO TS
CP0527474 Compound Info	N-[(1R)-2-[[2-(5-bromopyridin-2-yl)-5-chloro-6-methylpyrimidin-4-yl]amino]-1-phenylethyl]-4-piperazin-1-ylbutanamide Show/Hide	C26H31BrClN7O	1
1	EC50 = 53000 nM Bioactivity Info	TI LI LO TS
CP0394881 Compound Info	(1R)-N'-[5-chloro-2-(5-chloropyridin-2-yl)-6-methylpyrimidin-4-yl]-1-phenyl-N-(4-phenylbutyl)ethane-1,2-diamine Show/Hide	C28H29Cl2N5	1
1	EC50 > 100000 nM Bioactivity Info	TI LI LO TS
CP0515315 Compound Info	(1R)-N'-[5-chloro-2-(5-chloropyridin-2-yl)-6-methylpyrimidin-4-yl]-1-phenyl-N-(5-phenylpentyl)ethane-1,2-diamine Show/Hide	C29H31Cl2N5	1
1	EC50 > 100000 nM Bioactivity Info	TI LI LO TS
CP0515316 Compound Info	(1R)-N'-[5-chloro-2-(5-chloropyridin-2-yl)-6-methylpyrimidin-4-yl]-1-phenyl-N-(2-phenylethyl)ethane-1,2-diamine Show/Hide	C26H25Cl2N5	1
1	EC50 > 100000 nM Bioactivity Info	TI LI LO TS
CP0527473 Compound Info	(1R)-N'-[5-chloro-2-(5-chloropyridin-2-yl)-6-methylpyrimidin-4-yl]-1-phenyl-N-(4-pyrrol-1-ylbutyl)ethane-1,2-diamine Show/Hide	C26H28Cl2N6	1
1	EC50 > 100000 nM Bioactivity Info	TI LI LO TS
CP0057298 Compound Info	5-chloro-6-methyl-N-(2-phenylethyl)-2-pyridin-2-ylpyrimidin-4-amine Show/Hide	C18H17ClN4	1
1	IC50 = 9000 nM Bioactivity Info	TI LI LO TS
CP0563103 Compound Info	N-[(1R)-2-[(5-chloro-6-methyl-2-pyridin-2-ylpyrimidin-4-yl)amino]-1-phenylethyl]-2-piperazin-1-ylethanesulfonamide Show/Hide	C24H30ClN7O2S	1
1	IC50 = 9400 nM Bioactivity Info	TI LI LO TS
CP0508649 Compound Info	N-benzyl-5-chloro-N,6-dimethyl-2-pyridin-2-ylpyrimidin-4-amine Show/Hide	C18H17ClN4	1
1	IC50 = 13000 nM Bioactivity Info	TI LI LO TS
CP0397165 Compound Info	5-chloro-N,6-dimethyl-2-pyridin-2-ylpyrimidin-4-amine Show/Hide	C11H11ClN4	1
1	IC50 = 14000 nM Bioactivity Info	TI LI LO TS
CP0394883 Compound Info	N-[(1R)-2-[(5-chloro-6-methyl-2-pyridin-2-ylpyrimidin-4-yl)amino]-1-phenylethyl]-3-piperazin-1-ylpropanamide Show/Hide	C25H30ClN7O	1
1	IC50 = 22000 nM Bioactivity Info	TI LI LO TS
CP0508651 Compound Info	5-fluoro-6-methyl-N-(2-phenylethyl)-2-pyridin-2-ylpyrimidin-4-amine Show/Hide	C18H17FN4	1
1	IC50 = 62000 nM Bioactivity Info	TI LI LO TS
CP0432354 Compound Info	N-[(1R)-2-[(5-chloro-6-methyl-2-pyridin-2-ylpyrimidin-4-yl)amino]-1-phenylethyl]-2-[4-(2-hydroxyethyl)piperazin-1-yl]ethanesulfonamide Show/Hide	C26H34ClN7O3S	1
1	IC50 = 95000 nM Bioactivity Info	TI LI LO TS
CP0110262 Compound Info	N'-(5-chloro-6-methyl-2-pyridin-2-ylpyrimidin-4-yl)-N-[5-(trifluoromethyl)pyridin-2-yl]ethane-1,2-diamine Show/Hide	C18H16ClF3N6	1
1	IC50 > 100000 nM Bioactivity Info	TI LI LO TS
CP0380769 Compound Info	N'-(5-chloro-6-methyl-2-pyridin-2-ylpyrimidin-4-yl)-N-[6-(trifluoromethyl)pyridin-2-yl]ethane-1,2-diamine Show/Hide	C18H16ClF3N6	1
1	IC50 > 100000 nM Bioactivity Info	TI LI LO TS
CP0380770 Compound Info	6-methyl-N-(2-phenylethyl)-2-pyridin-2-ylpyrimidin-4-amine Show/Hide	C18H18N4	1
1	IC50 > 100000 nM Bioactivity Info	TI LI LO TS
CP0397166 Compound Info	N-benzyl-5-chloro-6-methyl-2-pyridin-3-ylpyrimidin-4-amine Show/Hide	C17H15ClN4	1
1	IC50 > 100000 nM Bioactivity Info	TI LI LO TS
CP0508650 Compound Info	4-benzylsulfanyl-5-chloro-6-methyl-2-pyridin-2-ylpyrimidine Show/Hide	C17H14ClN3S	1
1	IC50 > 100000 nM Bioactivity Info	TI LI LO TS
CP0525367 Compound Info	5-chloro-N-[1-[3-chloro-5-(trifluoromethyl)pyridin-2-yl]piperidin-4-yl]-6-methyl-2-pyridin-2-ylpyrimidin-4-amine Show/Hide	C21H19Cl2F3N6	1
1	IC50 > 100000 nM Bioactivity Info	TI LI LO TS
CP0529612 Compound Info	5-chloro-4-methyl-6-(2-phenylethylsulfanyl)-2-pyridin-2-ylpyrimidine Show/Hide	C18H16ClN3S	1
1	IC50 > 100000 nM Bioactivity Info	TI LI LO TS
CP0559151 Compound Info	5,6-dimethyl-N-(2-phenylethyl)-2-pyridin-2-ylpyrimidin-4-amine Show/Hide	C19H20N4	1
1	IC50 > 100000 nM Bioactivity Info	TI LI LO TS
CP0563104 Compound Info	2-[4-(5-chloro-6-methyl-2-pyridin-2-ylpyrimidin-4-yl)piperazin-1-yl]ethanol Show/Hide	C16H20ClN5O	1
1	IC50 > 100000 nM Bioactivity Info	TI LI LO TS

Cell Line ID: CL000006 , HEK293

Cell Line Info

Cell Line ID: CL000156 , HT-1080

Cell Line Info

Cell Line ID: CL000749 , HUVEC-C

Cell Line Info

Cell Line ID: CL000013 , Sf9

Cell Line Info

Biochemical Assays

Compound ID	Compound Name	Compound Formula
CP0443513 Compound Info	(3S)-1-[4-methyl-5-[6-(trifluoromethyl)-1H-indazol-4-yl]pyrimidin-2-yl]pyrrolidin-3-ol Show/Hide	C17H16F3N5O	1
1	IC50 = 7 nM
CP0067292 Compound Info	2-benzenesulfonamido-5,6,7,8-tetrahydronaphthalene-1-carboxylic acid Show/Hide	C17H17NO4S	4
1	IC50 = 9 nM
2	IC50 = 10 nM
3	IC50 = 3300 nM
4	IC50 = 4200 nM
CP0700243 Compound Info	2-[({2-[(1Z)-3-(diethylamino)-1-propenyl]-4-fluorophenyl}-sulfonyl)amino]-5,6,7,8-tetrahydro-1-naphthalenecarboxylic acid Show/Hide	C24H29FN2O4S	2
1	IC50 = 11 nM
2	IC50 = 79 nM
CP0196254 Compound Info	2-[(2-{[4-(dimethylamino)butyl]amino}benzene)sulfonamido]-5,6,7,8-tetrahydronaphthalene-1-carboxylic acid Show/Hide	C23H31N3O4S	3
1	IC50 = 12 nM
2	IC50 = 12.02 nM
3	IC50 = 630 nM
CP0215398 Compound Info	2-({2-[(1Z)-3-(diethylamino)prop-1-en-1-yl]benzene}sulfonamido)-5,6,7,8-tetrahydronaphthalene-1-carboxylic acid Show/Hide	C24H30N2O4S	2
1	IC50 = 12 nM
2	IC50 = 130 nM
CP0034767 Compound Info	2-({2-[(3-aminopropyl)amino]benzene}sulfonamido)-5,6,7,8-tetrahydronaphthalene-1-carboxylic acid Show/Hide	C20H25N3O4S	3
1	IC50 = 12.88 nM
2	IC50 = 13 nM
3	IC50 = 360 nM
CP0199544 Compound Info	2-[(2-{[3-(dimethylamino)propyl]amino}benzene)sulfonamido]-5,6,7,8-tetrahydronaphthalene-1-carboxylic acid Show/Hide	C22H29N3O4S	3
1	IC50 = 14 nM
2	IC50 = 14.13 nM
3	IC50 = 470 nM
CP0036761 Compound Info	2-[(2-{[(1-methylpiperidin-4-yl)methyl]amino}benzene)sulfonamido]-5,6,7,8-tetrahydronaphthalene-1-carboxylic acid Show/Hide	C24H31N3O4S	3
1	IC50 = 15 nM
2	IC50 = 15.14 nM
3	IC50 = 1200 nM
CP0360729 Compound Info	2-({2-[(1Z)-4-(diethylamino)but-1-en-1-yl]benzene}sulfonamido)-5,6,7,8-tetrahydronaphthalene-1-carboxylic acid Show/Hide	C25H32N2O4S	2
1	IC50 = 16 nM
2	IC50 = 470 nM
CP0096345 Compound Info	2-({2-[(piperidin-4-ylmethyl)amino]benzene}sulfonamido)-5,6,7,8-tetrahydronaphthalene-1-carboxylic acid Show/Hide	C23H29N3O4S	3
1	IC50 = 16.98 nM
2	IC50 = 17 nM
3	IC50 = 1200 nM
CP0277819 Compound Info	2-[(2-{[3-(pyrrolidin-1-yl)propyl]amino}benzene)sulfonamido]-5,6,7,8-tetrahydronaphthalene-1-carboxylic acid Show/Hide	C24H31N3O4S	3
1	IC50 = 16.98 nM
2	IC50 = 17 nM
3	IC50 = 490 nM
CP0286441 Compound Info	2-[(2-{[2-(1-methylpyrrolidin-2-yl)ethyl]amino}benzene)sulfonamido]-5,6,7,8-tetrahydronaphthalene-1-carboxylic acid Show/Hide	C24H31N3O4S	3
1	IC50 = 16.98 nM
2	IC50 = 17 nM
3	IC50 = 560 nM
CP0199496 Compound Info	2-{[2-({2-[(dimethylamino)methyl]-2-methylpropyl}amino)benzene]sulfonamido}-5,6,7,8-tetrahydronaphthalene-1-carboxylic acid Show/Hide	C24H33N3O4S	3
1	IC50 = 18 nM
2	IC50 = 18.2 nM
3	IC50 = 780 nM
CP0215394 Compound Info	2-({2-[4-(diethylamino)butyl]benzene}sulfonamido)-5,6,7,8-tetrahydronaphthalene-1-carboxylic acid Show/Hide	C25H34N2O4S	2
1	IC50 <= 19 nM
2	IC50 = 1000 nM
CP0192620 Compound Info	2-[(2-{[3-(piperidin-1-yl)propyl]amino}benzene)sulfonamido]-5,6,7,8-tetrahydronaphthalene-1-carboxylic acid Show/Hide	C25H33N3O4S	3
1	IC50 = 19.95 nM
2	IC50 = 20 nM
3	IC50 = 1200 nM
CP0319796 Compound Info	2-({2-[(1-benzylpiperidin-4-yl)amino]benzene}sulfonamido)-5,6,7,8-tetrahydronaphthalene-1-carboxylic acid Show/Hide	C29H33N3O4S	2
1	IC50 = 20 nM
2	IC50 <= 4500 nM
CP0145817 Compound Info	2-[(2-{[2-(pyrrolidin-2-yl)ethyl]amino}benzene)sulfonamido]-5,6,7,8-tetrahydronaphthalene-1-carboxylic acid Show/Hide	C23H29N3O4S	3
1	IC50 = 21.88 nM
2	IC50 = 22 nM
3	IC50 = 550 nM
CP0108229 Compound Info	2-[(2-{[3-(diethylamino)propyl]amino}benzene)sulfonamido]-5,6,7,8-tetrahydronaphthalene-1-carboxylic acid Show/Hide	C24H33N3O4S	3
1	IC50 = 25 nM
2	IC50 = 181.97 nM
3	IC50 = 950 nM
CP0215395 Compound Info	2-({2-[(1E)-4-(diethylamino)but-1-en-1-yl]benzene}sulfonamido)-5,6,7,8-tetrahydronaphthalene-1-carboxylic acid Show/Hide	C25H32N2O4S	2
1	IC50 = 25 nM
2	IC50 = 700 nM
CP0186448 Compound Info	2-[(2-{[3-(4-methylpiperazin-1-yl)propyl]amino}benzene)sulfonamido]-5,6,7,8-tetrahydronaphthalene-1-carboxylic acid Show/Hide	C25H34N4O4S	3
1	IC50 = 25.7 nM
2	IC50 = 26 nM
3	IC50 = 2100 nM
CP0810981 Compound Info	2-[({2-[(1E)-3-(diethylamino)-1-propenyl]phenyl}sulfonyl)-amino]-5,6,7,8-tetrahydro-1-naphthalenecarboxylic acid Show/Hide	C22H26N2O4S	2
1	IC50 = 27 nM
2	IC50 = 410 nM
CP0277100 Compound Info	2-({2-[(1Z)-5-(diethylamino)pent-1-en-1-yl]benzene}sulfonamido)-5,6,7,8-tetrahydronaphthalene-1-carboxylic acid Show/Hide	C26H34N2O4S	2
1	IC50 = 28 nM
2	IC50 = 1300 nM
CP0045276 Compound Info	2-{[2-({2-[bis(propan-2-yl)amino]ethyl}amino)benzene]sulfonamido}-5,6,7,8-tetrahydronaphthalene-1-carboxylic acid Show/Hide	C25H35N3O4S	3
1	IC50 = 30.9 nM
2	IC50 = 31 nM
3	IC50 = 410 nM
CP0096344 Compound Info	2-[(2-{[2-(diethylamino)ethyl]amino}benzene)sulfonamido]-5,6,7,8-tetrahydronaphthalene-1-carboxylic acid Show/Hide	C23H31N3O4S	3
1	IC50 = 30.9 nM
2	IC50 = 31 nM
3	IC50 = 480 nM
CP0160675 Compound Info	2-[(2-{[2-(diethylamino)ethyl]carbamoyl}benzene)sulfonamido]-5,6,7,8-tetrahydronaphthalene-1-carboxylic acid Show/Hide	C24H31N3O5S	2
1	IC50 = 31 nM
2	IC50 = 160 nM
CP0215439 Compound Info	2-({2-[4-(piperidin-1-yl)butanamido]benzene}sulfonamido)-5,6,7,8-tetrahydronaphthalene-1-carboxylic acid Show/Hide	C26H33N3O5S	2
1	IC50 = 32 nM
2	IC50 = 210 nM
CP0145542 Compound Info	2-({2-[(pyrrolidin-3-ylmethyl)amino]benzene}sulfonamido)-5,6,7,8-tetrahydronaphthalene-1-carboxylic acid Show/Hide	C22H27N3O4S	3
1	IC50 = 33.88 nM
2	IC50 = 34 nM
3	IC50 = 790 nM
CP0757715 Compound Info	5-[(S)-3-(3-Chloro-5-fluoro-benzylcarbamoyl)-3-hydroxy-2-oxopyrrolidin-1-yl]-1H-indole-2-carboxylic Acid (3-Amino-propyl)-amide Show/Hide	C24H25ClFN5O4	1
1	IC50 = 34 nM
CP0075383 Compound Info	2-({2-[(piperidin-3-ylmethyl)amino]benzene}sulfonamido)-5,6,7,8-tetrahydronaphthalene-1-carboxylic acid Show/Hide	C23H29N3O4S	3
1	IC50 = 34.67 nM
2	IC50 = 35 nM
3	IC50 = 1600 nM
CP0215410 Compound Info	2-[(2-{[2-(diethylamino)ethane]sulfinyl}benzene)sulfonamido]-5,6,7,8-tetrahydronaphthalene-1-carboxylic acid Show/Hide	C23H30N2O5S2	2
1	IC50 = 39 nM
2	IC50 = 190 nM
CP0232986 Compound Info	5-[(3S)-3-[(3-chloro-5-fluorophenyl)methylcarbamoyl]-3-hydroxy-2-oxopyrrolidin-1-yl]-N-ethyl-1H-indole-2-carboxamide Show/Hide	C23H22ClFN4O4	1
1	IC50 = 41 nM
CP0173606 Compound Info	2-{[2-({[3-(piperidin-1-yl)propyl]carbamoyl}amino)benzene]sulfonamido}-5,6,7,8-tetrahydronaphthalene-1-carboxylic acid Show/Hide	C26H34N4O5S	2
1	IC50 = 42 nM
2	IC50 = 410 nM
CP0215440 Compound Info	2-({2-[4-(pyrrolidin-1-yl)butanamido]benzene}sulfonamido)-5,6,7,8-tetrahydronaphthalene-1-carboxylic acid Show/Hide	C25H31N3O5S	2
1	IC50 = 42 nM
2	IC50 = 210 nM
CP0215911 Compound Info	2-[(2-{[3-(diethylamino)propyl]sulfanyl}benzene)sulfonamido]-5,6,7,8-tetrahydronaphthalene-1-carboxylic acid Show/Hide	C24H32N2O4S2	2
1	IC50 = 43 nM
2	IC50 = 1200 nM
CP0185598 Compound Info	2-[(2-{[4-(diethylamino)butyl]carbamoyl}benzene)sulfonamido]-5,6,7,8-tetrahydronaphthalene-1-carboxylic acid Show/Hide	C26H35N3O5S	2
1	IC50 = 44 nM
2	IC50 = 410 nM
CP0556579 Compound Info	(3S)-3-hydroxy-2-oxo-1-(2-oxo-3,4-dihydro-1H-quinolin-6-yl)-N-[(2,3,5-trifluorophenyl)methyl]pyrrolidine-3-carboxamide Show/Hide	C21H18F3N3O4	1
1	IC50 = 44 nM
CP0075373 Compound Info	2-{[2-({[1-(propan-2-yl)piperidin-4-yl]methyl}amino)benzene]sulfonamido}-5,6,7,8-tetrahydronaphthalene-1-carboxylic acid Show/Hide	C26H35N3O4S	3
1	IC50 = 45.71 nM
2	IC50 = 46 nM
3	IC50 = 3600 nM
CP0290647 Compound Info	2-[(2-{[2-(dimethylamino)ethyl]amino}benzene)sulfonamido]-5,6,7,8-tetrahydronaphthalene-1-carboxylic acid Show/Hide	C21H27N3O4S	3
1	IC50 = 47.86 nM
2	IC50 <= 48 nM
3	IC50 = 560 nM
CP0320158 Compound Info	2-{[2-({[2-(diethylamino)ethoxy]carbonyl}amino)benzene]sulfonamido}-5,6,7,8-tetrahydronaphthalene-1-carboxylic acid Show/Hide	C24H31N3O6S	2
1	IC50 = 51 nM
2	IC50 = 490 nM
CP0350677 Compound Info	(3S)-N-[(2,3-difluorophenyl)methyl]-3-hydroxy-2-oxo-1-(2-oxo-3,4-dihydro-1H-quinolin-6-yl)pyrrolidine-3-carboxamide Show/Hide	C21H19F2N3O4	1
1	IC50 = 52 nM
CP0556757 Compound Info	(3S)-N-[(3,5-difluorophenyl)methyl]-3-hydroxy-2-oxo-1-(2-oxo-3,4-dihydro-1H-quinolin-6-yl)pyrrolidine-3-carboxamide Show/Hide	C21H19F2N3O4	1
1	IC50 = 52 nM
CP0239916 Compound Info	(3S)-N-[(3-chloro-2-fluorophenyl)methyl]-3-hydroxy-2-oxo-1-(2-oxo-3,4-dihydro-1H-quinolin-6-yl)pyrrolidine-3-carboxamide Show/Hide	C21H19ClFN3O4	1
1	IC50 = 53 nM
CP0355582 Compound Info	(3S)-N-[(3,5-difluorophenyl)methyl]-3-hydroxy-1-(1H-indol-5-yl)-2-oxopyrrolidine-3-carboxamide Show/Hide	C20H17F2N3O3	1
1	IC50 = 54 nM
CP0215409 Compound Info	2-[(2-{[2-(diethylamino)ethane]sulfinyl}-4-fluorobenzene)sulfonamido]-5,6,7,8-tetrahydronaphthalene-1-carboxylic acid Show/Hide	C23H29FN2O5S2	2
1	IC50 = 55 nM
2	IC50 = 230 nM
CP0288414 Compound Info	2-{[2-({[3-(morpholin-4-yl)propyl]carbamoyl}amino)benzene]sulfonamido}-5,6,7,8-tetrahydronaphthalene-1-carboxylic acid Show/Hide	C25H32N4O6S	2
1	IC50 = 55 nM
2	IC50 = 680 nM
CP0058397 Compound Info	5-nitro-8-quinolinol Show/Hide	C9H6N2O3	1
1	IC50 = 55 nM
CP0368892 Compound Info	(3S)-N-[(3-chloro-2,5-difluorophenyl)methyl]-3-hydroxy-2-oxo-1-(2-oxo-3,4-dihydro-1H-quinolin-6-yl)pyrrolidine-3-carboxamide Show/Hide	C21H18ClF2N3O4	1
1	IC50 = 58 nM
CP0371533 Compound Info	(3S)-N-[(3-chloro-5-fluorophenyl)methyl]-3-hydroxy-1-(1H-indol-5-yl)-2-oxopyrrolidine-3-carboxamide Show/Hide	C20H17ClFN3O3	1
1	IC50 = 59 nM
CP0302325 Compound Info	2-{[2-({2-[1-(propan-2-yl)pyrrolidin-2-yl]ethyl}amino)benzene]sulfonamido}-5,6,7,8-tetrahydronaphthalene-1-carboxylic acid Show/Hide	C26H35N3O4S	3
1	IC50 = 61.66 nM
2	IC50 = 62 nM
3	IC50 = 680 nM
CP0368739 Compound Info	(3S)-3-hydroxy-2-oxo-1-(2-oxo-3,4-dihydro-1H-quinolin-6-yl)-N-[(2,3,6-trifluorophenyl)methyl]pyrrolidine-3-carboxamide Show/Hide	C21H18F3N3O4	1
1	IC50 = 62 nM
CP0371532 Compound Info	(3S)-N-[(3-chloro-5-fluorophenyl)methyl]-3-hydroxy-2-oxo-1-(1H-pyrrolo[2,3-b]pyridin-5-yl)pyrrolidine-3-carboxamide Show/Hide	C19H16ClFN4O3	1
1	IC50 = 63 nM
CP0143027 Compound Info	(3S)-N-[(3-chloro-5-fluorophenyl)methyl]-3-hydroxy-1-(1H-indazol-5-yl)-2-oxopyrrolidine-3-carboxamide Show/Hide	C19H16ClFN4O3	1
1	IC50 = 64 nM
CP0274865 Compound Info	2-[(2-{[5-(diethylamino)pentan-2-yl]carbamoyl}-4-fluorobenzene)sulfonamido]-5,6,7,8-tetrahydronaphthalene-1-carboxylic acid Show/Hide	C27H36FN3O5S	2
1	IC50 = 67 nM
2	IC50 <= 340 nM
CP0254865 Compound Info	2-[(2-{[2-(pyrrolidin-1-yl)ethyl]amino}benzene)sulfonamido]-5,6,7,8-tetrahydronaphthalene-1-carboxylic acid Show/Hide	C23H29N3O4S	3
1	IC50 = 69 nM
2	IC50 = 69.18 nM
3	IC50 = 1500 nM
CP0274940 Compound Info	2-{[2-({2-[1-(1-methylpiperidin-4-yl)pyrrolidin-2-yl]ethyl}amino)benzene]sulfonamido}-5,6,7,8-tetrahydronaphthalene-1-carboxylic acid Show/Hide	C29H40N4O4S	3
1	IC50 = 70 nM
2	IC50 = 70.79 nM
3	IC50 = 420 nM
CP0232985 Compound Info	(3S)-N-[(3-chloro-5-fluorophenyl)methyl]-3-hydroxy-1-[3-(methanesulfonamido)phenyl]-2-oxopyrrolidine-3-carboxamide Show/Hide	C19H19ClFN3O5S	1
1	IC50 = 71 nM
CP0083036 Compound Info	2-{[2-({[2-(1-methylpyrrolidin-2-yl)ethyl]carbamoyl}amino)benzene]sulfonamido}-5,6,7,8-tetrahydronaphthalene-1-carboxylic acid Show/Hide	C25H32N4O5S	2
1	IC50 = 72 nM
2	IC50 = 500 nM
CP0164309 Compound Info	(3S)-N-[(3-chloro-5-fluorophenyl)methyl]-3-hydroxy-2-oxo-1-(2-oxo-3,4-dihydro-1H-quinolin-6-yl)pyrrolidine-3-carboxamide Show/Hide	C21H19ClFN3O4	3
1	IC50 = 74 nM
2	IC50 = 75 nM
3	IC50 = 160 nM
CP0477267 Compound Info	(3S)-N-[(3-chloro-5-fluorophenyl)methyl]-1-(3-chloro-1H-pyrrolo[2,3-b]pyridin-5-yl)-3-hydroxy-2-oxopyrrolidine-3-carboxamide Show/Hide	C19H15Cl2FN4O3	1
1	IC50 = 74 nM
CP0244234 Compound Info	(3S)-N-[(3-chloro-5-fluorophenyl)methyl]-3-hydroxy-1-(1-methyl-2-oxo-3,4-dihydroquinolin-6-yl)-2-oxopyrrolidine-3-carboxamide Show/Hide	C22H21ClFN3O4	1
1	IC50 = 79 nM
CP0239917 Compound Info	US10005756, Compound A75 Show/Hide	C19H16F2N4O3	1
1	IC50 = 80 nM
CP0757713 Compound Info	(S)-3-Hydroxy-2-oxo-1-(1H-pyrrolo[2,3-b]pyridin-5-yl)-pyrrolidine-3-carboxylic Acid 3,5-Difluoro-benzylamide Show/Hide	C19H16F2N4O3	1
1	IC50 = 87 nM
CP0274882 Compound Info	2-({2-[(1,2,2,6,6-pentamethylpiperidin-4-yl)amino]benzene}sulfonamido)-5,6,7,8-tetrahydronaphthalene-1-carboxylic acid Show/Hide	C27H37N3O4S	2
1	IC50 = 91 nM
2	IC50 <= 4600 nM
CP0355581 Compound Info	US10005756, Compound A79 Show/Hide	C19H15ClF2N4O3	1
1	IC50 = 92 nM
CP0098551 Compound Info	(3S)-N-[(2,6-difluorophenyl)methyl]-3-hydroxy-2-oxo-1-(2-oxo-3,4-dihydro-1H-quinolin-6-yl)pyrrolidine-3-carboxamide Show/Hide	C21H19F2N3O4	1
1	IC50 = 94 nM
CP0344007 Compound Info	(3S)-N-[(3-chloro-5-fluorophenyl)methyl]-1-(8-fluoro-2-oxo-3,4-dihydro-1H-quinolin-6-yl)-3-hydroxy-2-oxopyrrolidine-3-carboxamide Show/Hide	C21H18ClF2N3O4	1
1	IC50 = 95 nM
CP0350678 Compound Info	(3S)-N-[(3-chloro-5-fluorophenyl)methyl]-3-hydroxy-1-(2-methyl-1H-indol-5-yl)-2-oxopyrrolidine-3-carboxamide Show/Hide	C21H19ClFN3O3	1
1	IC50 = 100 nM
CP0098549 Compound Info	(3S)-N-[(2-chloro-5-fluorophenyl)methyl]-3-hydroxy-2-oxo-1-(2-oxo-3,4-dihydro-1H-quinolin-6-yl)pyrrolidine-3-carboxamide Show/Hide	C21H19ClFN3O4	1
1	IC50 = 110 nM
CP0556578 Compound Info	(3S)-N-[(2-chloro-6-fluorophenyl)methyl]-3-hydroxy-2-oxo-1-(2-oxo-3,4-dihydro-1H-quinolin-6-yl)pyrrolidine-3-carboxamide Show/Hide	C21H19ClFN3O4	1
1	IC50 = 110 nM
CP0098552 Compound Info	(3S)-3-hydroxy-2-oxo-1-(2-oxo-3,4-dihydro-1H-quinolin-6-yl)-N-[(3,4,5-trifluorophenyl)methyl]pyrrolidine-3-carboxamide Show/Hide	C21H18F3N3O4	1
1	IC50 = 120 nM
CP0306040 Compound Info	2-[(2-{[5-(diethylamino)pentan-2-yl]amino}benzene)sulfonamido]-5,6,7,8-tetrahydronaphthalene-1-carboxylic acid Show/Hide	C26H37N3O4S	2
1	IC50 = 130 nM
2	IC50 = 66000 nM
CP0556580 Compound Info	(3S)-N-[(3-chloro-2,4-difluorophenyl)methyl]-3-hydroxy-2-oxo-1-(2-oxo-3,4-dihydro-1H-quinolin-6-yl)pyrrolidine-3-carboxamide Show/Hide	C21H18ClF2N3O4	1
1	IC50 = 160 nM
CP0296999 Compound Info	2-[(2-{[5-(diethylamino)pentan-2-yl]carbamoyl}benzene)sulfonamido]-5,6,7,8-tetrahydronaphthalene-1-carboxylic acid Show/Hide	C27H37N3O5S	2
1	IC50 = 170 nM
2	IC50 = 1000 nM
CP0215405 Compound Info	2-({2-[2-(1-methylpyrrolidin-2-yl)ethoxy]benzene}sulfonamido)-5,6,7,8-tetrahydronaphthalene-1-carboxylic acid Show/Hide	C24H30N2O5S	2
1	IC50 = 430 nM
2	IC50 = 8200 nM
CP0056176 Compound Info	5-chloranylquinolin-8-ol Show/Hide	C9H6ClNO	1
1	IC50 = 1270 nM
CP0068732 Compound Info	8-quinolinol Show/Hide	C9H7NO	1
1	IC50 = 2030 nM
CP0057298 Compound Info	5-chloro-6-methyl-N-(2-phenylethyl)-2-pyridin-2-ylpyrimidin-4-amine Show/Hide	C18H17ClN4	1
1	IC50 = 7000 nM
CP0032544 Compound Info	(3R)-1-[4-methyl-5-[6-(trifluoromethyl)-1H-indazol-4-yl]pyrimidin-2-yl]pyrrolidin-3-ol Show/Hide	C17H16F3N5O	2
1	IC50 ~ 7 nM
2	IC50 ~ 31 nM
CP0057786 Compound Info	2-Methyl-quinolin-8-ol Show/Hide	C10H9NO	1
1	IC50 > 15000 nM

Clinical Information about the Protein

Target 1 ( Methionine aminopeptidase 2 (METAP2) )

Target Type	Clinical trial Target
Disease	3 Target-related Diseases				3
1	Type 2 diabetes [ICD-11: 5A11]
2	Solid tumour/cancer [ICD-11: 2A00-2F9Z]
3	Autoimmune diabetes [ICD-11: 5A10]
Clinical Trial Drug(s)	3 Clinical Trial Drugs				3
1	ZGN-1061	Drug Info	Phase 2	Type 2 diabetes
2	Beloranib	Drug Info	Phase 3	Solid tumour/cancer
3	PPI-2458	Drug Info	Phase 1	Autoimmune diabetes
Discontinued Drug(s)	1 Discontinued Drug				1
1	TNP-470	Drug Info	Discontinued in Phase 2	Solid tumour/cancer

Cite

About MolBiC

Correspondence

Prof. Feng ZHU

Prof. Leo, Lianyi Han