| 3-[5-(5-Chloro-2-oxoindol-3-yl)-4-hydroxy-2-sulfanylidene-1,3-thiazol-3-yl]propanoic acid | IC50 | 31622.78 [1], 49000.0 [2] |
| 5-[[5-Chloro-2-(pyridin-3-ylmethylamino)pyrimidin-4-yl]amino]-1,3-dihydroindol-2-one | IC50 | 480.0 [1], 8600.0 [2] |
| (12S,14S,17E)-12-(Hydroxymethyl)-24-oxo-15,20-dioxa-2,4,5,9,11,23-hexazahexacyclo[19.7.1.13,10.111,14.04,8.022,27]hentriaconta-1(28),3(31),5,7,9,17,21(29),22(27)-octaene-7-carbonitrile | IC50 | 2.9 [1], 1995.26 [2] |
| (12S,14S,17E)-7-Chloro-12-(hydroxymethyl)-23-methyl-15,20-dioxa-2,4,5,9,11,23-hexazahexacyclo[19.7.1.13,10.111,14.04,8.022,27]hentriaconta-1(28),3(31),5,7,9,17,21(29),22(27)-octaen-24-one | IC50 | 4.9 [1], 6309.57 [2] |
| (12S,14S,17E)-23-Benzyl-7-chloro-12-(hydroxymethyl)-15,20-dioxa-2,4,5,9,11,23-hexazahexacyclo[19.7.1.13,10.111,14.04,8.022,27]hentriaconta-1(28),3(31),5,7,9,17,21(29),22(27)-octaen-24-one | IC50 | 11.0 [1], 199.53 [2] |
| (12S,14S,17E)-7-Chloro-12-(hydroxymethyl)-23-(pyridin-4-ylmethyl)-15,20-dioxa-2,4,5,9,11,23-hexazahexacyclo[19.7.1.13,10.111,14.04,8.022,27]hentriaconta-1(28),3(31),5,7,9,17,21(29),22(27)-octaen-24-one | IC50 | 9.9 [1], 398.11 [2] |
| (12S,14S,17E)-12-(Hydroxymethyl)-23-[(3-methoxyphenyl)methyl]-24-oxo-15,20-dioxa-2,4,5,9,11,23-hexazahexacyclo[19.7.1.13,10.111,14.04,8.022,27]hentriaconta-1(28),3(31),5,7,9,17,21(29),22(27)-octaene-7-carbonitrile | IC50 | 11.0 [1], 125.89 [2] |
| (12S,14S,17E)-7-Chloro-12-(hydroxymethyl)-15,20-dioxa-2,4,5,9,11,23-hexazahexacyclo[19.7.1.13,10.111,14.04,8.022,27]hentriaconta-1(28),3(31),5,7,9,17,21(29),22(27)-octaen-24-one | IC50 | 1.5 [1], 3981.07 [2] |
| (12S,14S,17E)-7-Chloro-12-(hydroxymethyl)-23-(3-morpholin-4-ylpropyl)-15,20-dioxa-2,4,5,9,11,23-hexazahexacyclo[19.7.1.13,10.111,14.04,8.022,27]hentriaconta-1(28),3(31),5,7,9,17,21(29),22(27)-octaen-24-one | IC50 | 0.87 [1], 1258.93 [2] |
| (14S)-24-Oxo-15,20-dioxa-2,4,5,9,11,23-hexazahexacyclo[19.7.1.13,10.111,14.04,8.022,27]hentriaconta-1(28),3(31),5,7,9,21(29),22(27)-heptaene-7-carbonitrile | IC50 | 24.0 [1], 15848.93 [2] |
| (12S,14S)-12-(Hydroxymethyl)-15,20-dioxa-2,4,5,9,11,23-hexazahexacyclo[19.7.1.13,10.111,14.04,8.022,27]hentriaconta-1(28),3(31),5,7,9,21(29),22(27)-heptaen-24-one | IC50 | 55.0 [1], 10000.0 [2] |
| (12S,14S,17E)-7-Chloro-12-(hydroxymethyl)-23-[(4-methylphenyl)methyl]-15,20-dioxa-2,4,5,9,11,23-hexazahexacyclo[19.7.1.13,10.111,14.04,8.022,27]hentriaconta-1(28),3(31),5,7,9,17,21(29),22(27)-octaen-24-one | IC50 | 29.0 [1], 794.33 [2] |
| (12S,14S,17E)-7-Chloro-23-(cyclopropylmethyl)-12-(hydroxymethyl)-15,20-dioxa-2,4,5,9,11,23-hexazahexacyclo[19.7.1.13,10.111,14.04,8.022,27]hentriaconta-1(28),3(31),5,7,9,17,21(29),22(27)-octaen-24-one | IC50 | 36.0 [1], 5011.87 [2] |
| (12S,14S)-12-(Hydroxymethyl)-24-oxo-15,20-dioxa-2,4,5,9,11,23-hexazahexacyclo[19.7.1.13,10.111,14.04,8.022,27]hentriaconta-1(28),3(31),5,7,9,21(29),22(27)-heptaene-7-carbonitrile | IC50 | 2.4 [1], 6309.57 [2] |
| (12S,14S,17E)-7-Chloro-23-[(3,3-difluorocyclobutyl)methyl]-12-(hydroxymethyl)-15,20-dioxa-2,4,5,9,11,23-hexazahexacyclo[19.7.1.13,10.111,14.04,8.022,27]hentriaconta-1(28),3(31),5,7,9,17,21(29),22(27)-octaen-24-one | IC50 | 5.0 [1], 501.19 [2] |
| (12S,14S,17E)-7-Chloro-12-(hydroxymethyl)-23-[(3-methoxyphenyl)methyl]-15,20-dioxa-2,4,5,9,11,23-hexazahexacyclo[19.7.1.13,10.111,14.04,8.022,27]hentriaconta-1(28),3(31),5,7,9,17,21(29),22(27)-octaen-24-one | IC50 | 12.0 [1], 100.0 [2] |
| 2-[(12S,14S,17E)-7-Chloro-23-[(3,3-difluorocyclobutyl)methyl]-24-oxo-15,20-dioxa-2,4,5,9,11,23-hexazahexacyclo[19.7.1.13,10.111,14.04,8.022,27]hentriaconta-1(28),3(31),5,7,9,17,21(29),22(27)-octaen-12-yl]acetic acid | IC50 | 16.0 [1], 3162.28 [2] |
| (12S,14S)-7-Chloro-12-(hydroxymethyl)-15,20-dioxa-2,4,5,9,11,23-hexazahexacyclo[19.7.1.13,10.111,14.04,8.022,27]hentriaconta-1(28),3(31),5,7,9,21(29),22(27)-heptaen-24-one | IC50 | 3.3 [1], 3981.07 [2] |
| (12S,14S,17E)-7-Chloro-12-(hydroxymethyl)-23-[(2-methylphenyl)methyl]-15,20-dioxa-2,4,5,9,11,23-hexazahexacyclo[19.7.1.13,10.111,14.04,8.022,27]hentriaconta-1(28),3(31),5,7,9,17,21(29),22(27)-octaen-24-one | IC50 | 13.0 [1], 79.43 [2] |
| 2-[5-(5-Bromo-2-oxoindol-3-yl)-4-hydroxy-2-sulfanylidene-1,3-thiazol-3-yl]butanedioic acid | IC50 | 212000.0 [1] |
| (2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-Acetamido-4-methylpentanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-hydroxybutanoyl]amino]-3-carboxypropanoyl]amino]-3-methylpentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-4-methylsulfanylbutanoyl]amino]-3-hydroxypropanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-5-carbamimidamidopentanoyl]amino]-3-methylbutanoyl]pyrrolidine-2-carboxylic acid | IC50 | 1.0 [1] |
| 1-[2-(1H-Indol-3-yl)ethyl]-3-[3-[(4-methylpiperazin-1-yl)methyl]-1-(2-morpholin-4-yl-2-oxoethyl)indol-6-yl]thiourea | IC50 | 27000.0 [1] |
| 2-[(2S)-1-[3-Cyano-7-[(2-oxo-3,4-dihydro-1H-quinolin-6-yl)amino]pyrazolo[1,5-a]pyrimidin-5-yl]pyrrolidin-2-yl]acetic acid | IC50 | 350.0 [1] |
| 2-[6-[2-(1H-Indol-3-yl)ethylcarbamothioylamino]-3-[(4-methylpiperazin-1-yl)methyl]indol-1-yl]-N-propan-2-ylacetamide | IC50 | 142000.0 [1] |
| 2-[(12S,14S,17E)-7-Cyano-24-oxo-15,20-dioxa-2,4,5,9,11,23-hexazahexacyclo[19.7.1.13,10.111,14.04,8.022,27]hentriaconta-1(28),3(31),5,7,9,17,21(29),22(27)-octaen-12-yl]acetic acid | IC50 | 1.7 [1] |
| (5S,8E)-6,11-Dioxa-2,17,19,20,24-pentazapentacyclo[16.6.1.12,5.112,16.019,23]heptacosa-1(24),8,12,14,16(26),18(25),20,22-octaene-22-carbonitrile | IC50 | 2300.0 [1] |
| N-[4-[3-Cyano-7-(cyclopropylamino)pyrazolo[1,5-a]pyrimidin-5-yl]-2-[(3R)-3-(dimethylamino)pyrrolidin-1-yl]phenyl]acetamide | IC50 | 61000.0 [1] |
| 7-(Cyclopropylamino)-5-pyrrolidin-1-ylpyrazolo[1,5-a]pyrimidine-3-carbonitrile | IC50 | 99000.0 [1] |
| 7-Anilino-5-pyrrolidin-1-ylpyrazolo[1,5-a]pyrimidine-3-carbonitrile | IC50 | 100000.0 [1] |
| 5-[(2R)-2-(Hydroxymethyl)pyrrolidin-1-yl]-7-[(2-oxo-3,4-dihydro-1H-quinolin-6-yl)amino]pyrazolo[1,5-a]pyrimidine-3-carbonitrile | IC50 | 590.0 [1] |
| (3S,5S,8E)-3-(Hydroxymethyl)-6,11-dioxa-2,17,19,20,24-pentazapentacyclo[16.6.1.12,5.112,16.019,23]heptacosa-1(24),8,12,14,16(26),18(25),20,22-octaene-22-carbonitrile | IC50 | 390.0 [1] |
| (15R)-17,25-Dioxo-21-oxa-2,4,5,9,11,18,24-heptazahexacyclo[20.7.1.13,10.04,8.011,15.023,28]hentriaconta-1(29),3(31),5,7,9,22(30),23(28)-heptaene-7-carbonitrile | IC50 | 210.0 [1] |
| 2-[(4Z)-4-(5-Bromo-2-oxo-1H-indol-3-ylidene)-2-sulfanylidene-1,3-thiazolidin-3-yl]butanedioic acid | IC50 | 212000.0 [1] |
| 2-[(2S)-1-[3-Cyano-7-(cyclopropylamino)pyrazolo[1,5-a]pyrimidin-5-yl]pyrrolidin-2-yl]acetic acid | IC50 | 64000.0 [1] |
| 7-Anilino-5-[(2S)-2-(hydroxymethyl)pyrrolidin-1-yl]pyrazolo[1,5-a]pyrimidine-3-carbonitrile | IC50 | 24000.0 [1] |
| (2R)-1-[3-Cyano-7-(cyclopropylamino)pyrazolo[1,5-a]pyrimidin-5-yl]pyrrolidine-2-carboxylic acid | IC50 | 45000.0 [1] |
| (3R,5S,8E)-3-(Hydroxymethyl)-6,11-dioxa-2,17,19,20,24-pentazapentacyclo[16.6.1.12,5.112,16.019,23]heptacosa-1(24),8,12,14,16(26),18(25),20,22-octaene-22-carbonitrile | IC50 | 10000.0 [1] |
| 5-[(2S)-2-(Hydroxymethyl)pyrrolidin-1-yl]-7-[(2-oxo-3,4-dihydro-1H-quinolin-6-yl)amino]pyrazolo[1,5-a]pyrimidine-3-carbonitrile | IC50 | 370.0 [1] |
| (5S,8E,27R)-27-(Hydroxymethyl)-6,11-dioxa-2,17,19,20,24-pentazapentacyclo[16.6.1.12,5.112,16.019,23]heptacosa-1(24),8,12,14,16(26),18(25),20,22-octaene-22-carbonitrile | IC50 | 8200.0 [1] |
| 7-(Cyclopropylamino)pyrazolo[1,5-a]pyrimidine-3-carbonitrile | IC50 | 99000.0 [1] |
| (14S,17E)-24-Oxo-15,20-dioxa-2,4,5,9,11,23-hexazahexacyclo[19.7.1.13,10.111,14.04,8.022,27]hentriaconta-1(28),3(31),5,7,9,17,21(29),22(27)-octaene-7-carbonitrile | IC50 | 15.0 [1] |
| 7-[(2-Oxo-3,4-dihydro-1H-quinolin-6-yl)amino]-5-pyrrolidin-1-ylpyrazolo[1,5-a]pyrimidine-3-carbonitrile | IC50 | 2900.0 [1] |
| 1-[2-(1H-Indol-3-yl)ethyl]-3-[1-[2-(2-methylmorpholin-4-yl)-2-oxoethyl]-3-[(4-methylpiperazin-1-yl)methyl]indol-6-yl]thiourea | IC50 | 62000.0 [1] |
| 2-[[2-[6-[2-(1H-Indol-3-yl)ethylcarbamothioylamino]-3-[(4-methylpiperazin-1-yl)methyl]indol-1-yl]acetyl]amino]acetic acid | IC50 | 112000.0 [1] |
| 1-[2-(1H-Indol-3-yl)ethyl]-3-[3-[(4-methylpiperazin-1-yl)methyl]-1-(2-oxo-2-piperidin-1-ylethyl)indol-6-yl]thiourea | IC50 | 34000.0 [1] |
| Methyl 2-[6-[2-(1H-indol-3-yl)ethylcarbamothioylamino]-3-[(4-methylpiperazin-1-yl)methyl]indol-1-yl]acetate | IC50 | 80000.0 [1] |
| 2-[[2-[6-[2-(1H-Indol-3-yl)ethylcarbamothioylamino]indol-1-yl]acetyl]amino]acetic acid | IC50 | 170000.0 [1] |