Rank |
Compound |
SMILES |
ΔG / kcal M-1 |
pIC50 |
201 |
EDJ-MED-5cd3920d-1
|
|
c1cc2cncc(c2cc1OC(F)F)N3CCC4(C3=O)CN(Cc5c4cc(cc5)Cl)S(=O)(=O)CC6(CC6)C#N |
−5.8
± 0.4
|
4.2
± 0.3
|
202 |
EDJ-MED-94fddcec-7
|
|
CS(=O)(=O)Nc1ccc2c(c1)cncc2N3CCC4(C3=O)CCS(=O)(=O)c5c4cc(cc5)Cl |
−5.8
± 0.2
|
4.2
± 0.2
|
203 |
EDJ-MED-a12e3a20-1
|
|
c1ccc2c(c1)cncc2N3CC(=O)C4(C3=O)CN(Cc5c4cc(cc5)Cl)S(=O)(=O)CC6(CC6)C#N |
−5.8
± 0.5
|
4.2
± 0.4
|
204 |
MAT-POS-853c0ffa-16
|
|
COC1(CC1)CS(=O)(=O)N2Cc3ccc(cc3C4(C2)CCN(C4=O)c5cncc6c5ccc(c6)S(=O)(=O)C)Cl |
−5.8
± 0.3
|
4.2
± 0.2
|
205 |
EDJ-MED-7e491f08-1
|
|
c1ccc2c(c1)cncc2N3CC([C@@]4(C3=O)CN(Cc5c4cc(cc5)Cl)S(=O)(=O)CC6(CC6)C#N)(F)F |
−5.8
± 0.3
|
4.2
± 0.2
|
206 |
MAT-POS-b4d6b7fc-7
|
|
CNC(=O)CN1Cc2ccc(cc2C3(C1)CCN(C3=O)c4cncc5c4ccc(c5)NS(=O)(=O)C)Cl |
−5.7
± 0.2
|
4.2
± 0.2
|
207 |
MIK-ENA-5d9157e9-1
|
|
c1ccc2c(c1)cncc2N3CC[C@@]4(C3=O)CN(Cc5c4cc(cc5)Cl)S(=O)(=O)CC6(CC6)C#N |
−5.7
± 0.3
|
4.2
± 0.2
|
208 |
EDJ-MED-94fddcec-4
|
|
c1ccc2c(c1)cncc2N3CCC4(C3=O)CCS(=O)(=O)c5c4cc(cc5)Cl |
−5.7
± 0.1
|
4.15
± 0.09
|
209 |
EDJ-MED-ede5c6cb-1
|
|
CS(=O)(=O)Nc1ccc2c(c1)cncc2N3CCC4(C3=O)CCS(=O)(=O)c5c4cc(cc5)Cl |
−5.7
± 0.2
|
4.1
± 0.1
|
210 |
ALP-POS-41e2080f-1
|
|
c1ccc2c(c1)cncc2N3CCC4(C3=O)CCS(=O)(=O)c5c4cc(cc5)Cl |
−5.7
± 0.2
|
4.1
± 0.1
|
211 |
MAT-POS-69786b79-1
|
|
CNC(=O)C1(CC1)N2Cc3ccc(cc3C4(C2)CCN(C4=O)c5cncc6c5cccc6)Cl |
−5.7
± 0.2
|
4.1
± 0.1
|
212 |
PET-UNK-94036022-3
|
|
c1ccc2c(c1)cncc2N3CC[C@@]4(C3=O)CN(Cc5c4cc(cc5)Cl)S(=O)(=O)CC6(CC6)Cl |
−5.6
± 0.3
|
4.1
± 0.2
|
213 |
EDJ-MED-b6c6ee2b-1
|
|
CNC(=O)CN1Cc2ccc(cc2C3(C1)CCN(C3=O)c4cncc5c4cc(cc5)OCCN(C)C)Cl |
−5.5
± 0.3
|
4.0
± 0.2
|
214 |
MAT-POS-853c0ffa-10
|
|
CN(C)CCOc1ccc2cncc(c2c1)N3CCC4(C3=O)CN(Cc5c4cc(cc5)Cl)S(=O)(=O)CC6(CC6)OC |
−5.5
± 0.4
|
4.0
± 0.3
|
215 |
BEN-BAS-c2bc0d80-3
|
|
c1ccc2c(c1)cncc2N3C(=O)C4(CCOc5c4cc(cc5)Cl)CN3 |
−5.5
± 0.2
|
4.0
± 0.1
|
216 |
EDJ-MED-b6c6ee2b-2
|
|
CNC(=O)CN1Cc2ccc(cc2C3(C1)CCN(C3=O)c4cncc5c4cc(cc5)OC)Cl |
−5.5
± 0.2
|
4.0
± 0.1
|
217 |
MAT-POS-853c0ffa-6
|
|
c1cc2c(cc1Cl)C3(CCN(C3=O)c4cncc5c4c(cc(c5)F)Cl)CN(C2)S(=O)(=O)CC6(CC6)C#N |
−5.5
± 0.4
|
4.0
± 0.3
|
218 |
ALP-POS-ecbed2ba-22
|
|
c1ccc2c(c1)cncc2N3CCC4(C3=O)CN(Cc5c4cc(cc5)Cl)S(=O)(=O)CC6(CC6)CC#N |
−5.4
± 0.4
|
4.0
± 0.3
|
219 |
MAT-POS-853c0ffa-11
|
|
CC(C)(c1ccc2cncc(c2c1)N3CCC4(C3=O)CN(Cc5c4cc(cc5)Cl)S(=O)(=O)CC6(CC6)C#N)O |
−5.4
± 0.5
|
3.9
± 0.4
|
220 |
EDJ-MED-ee81482e-4
|
|
c1cc2cncc(c2cc1OC3CCNCC3)N4CCC5(C4=O)CN(Cc6c5cc(cc6)Cl)S(=O)(=O)CC7(CC7)C#N |
−5.4
± 0.4
|
3.9
± 0.3
|
221 |
EDJ-MED-f9b78f78-4
|
|
c1ccc2c(c1)cncc2N3CCC4(C3=O)CNS(=O)(=O)c5c4cc(cc5)Cl |
−5.4
± 0.2
|
3.9
± 0.1
|
222 |
MAT-POS-853c0ffa-15
|
|
CS(=O)(=O)c1ccc2c(c1)cncc2N3CCC4(C3=O)CN(Cc5c4cc(cc5)Cl)S(=O)(=O)CC6(CC6)C#N |
−5.4
± 0.5
|
3.9
± 0.3
|
223 |
MAT-POS-38eb6498-2
|
|
CNC(=O)c1ccc2cncc(c2c1)N3CCC4(C3=O)CN(Cc5c4cc(cc5)Cl)S(=O)(=O)CC6(CC6)C#N |
−5.3
± 0.3
|
3.9
± 0.2
|
224 |
EDJ-MED-98c0a822-2
|
|
CNC(=O)C1(COC1)N2CC3(CCN(C3=O)c4cncc5c4cccc5)c6cc(ccc6S2(=O)=O)Cl |
−5.3
± 0.2
|
3.9
± 0.1
|
225 |
LUO-POS-868e8996-11
|
|
CNC(=O)CN1Cc2ccc(cc2[C@]3(C1)CCN(C3=O)c4cncc5c4cccc5)Cl |
−5.3
± 0.2
|
3.9
± 0.1
|
226 |
ALP-POS-4483ae88-1
|
|
c1ccc2c(c1)cncc2N3CCC4(C3=O)CNS(=O)(=O)c5c4cc(cc5)Cl |
−5.3
± 0.2
|
3.9
± 0.1
|
227 |
MAT-POS-853c0ffa-17
|
|
CC1(CC1)CS(=O)(=O)N2Cc3ccc(cc3C4(C2)CCN(C4=O)c5cncc6c5c(ccc6)Cl)Cl |
−5.3
± 0.2
|
3.9
± 0.2
|
228 |
EDJ-MED-8bb691af-4
|
|
CNC(=O)CN1Cc2ccc(cc2C3(C1)CCN(C3=O)c4cncc5c4cccc5)Cl |
−5.3
± 0.2
|
3.8
± 0.1
|
229 |
MAT-POS-96396902-1
|
|
c1ccc2c(c1)cncc2N3CCC4(C3=O)CN(Cc5c4cc(cc5)Cl)Cc6nncs6 |
−5.3
± 0.2
|
3.8
± 0.1
|
230 |
ALP-POS-afe0272e-2
|
|
CNC(=O)CN1CC2(CCN(C2=O)c3cncc4c3cccc4)c5cc(c(cc5C1=O)Cl)Cl |
−5.2
± 0.2
|
3.8
± 0.1
|
231 |
MAT-POS-c7726e07-6
|
|
CNC(=O)CN1Cc2ccc(cc2[C@@]3(C1)CCN(C3=O)c4cncc5c4cccc5)Cl |
−5.2
± 0.2
|
3.8
± 0.2
|
232 |
MAT-POS-50a80394-8
|
|
CC1(CN(C(=O)C12CN(Cc3c2cc(cc3)Cl)S(=O)(=O)CC4(CC4)C#N)c5cncc6c5cccc6)C |
−5.2
± 0.4
|
3.8
± 0.3
|
233 |
MAT-POS-853c0ffa-18
|
|
CC1(CC1)CS(=O)(=O)N2Cc3ccc(cc3C4(C2)CCN(C4=O)c5cncc6c5c(cc(c6)F)Cl)Cl |
−5.1
± 0.2
|
3.7
± 0.2
|
234 |
MAT-POS-853c0ffa-8
|
|
COC1(CC1)CS(=O)(=O)N2Cc3ccc(cc3C4(C2)CCN(C4=O)c5cncc6c5c(cc(c6)F)Cl)Cl |
−5.1
± 0.3
|
3.7
± 0.2
|
235 |
MAT-POS-1d5ab790-1
|
|
c1cc2cncc(c2c(c1)Cl)N3CCC4(C3=O)CN(Cc5c4cc(cc5)Cl)S(=O)(=O)CC6(CC6)C#N |
−5.0
± 0.3
|
3.7
± 0.2
|
236 |
MAT-POS-69786b79-4
|
|
c1ccc2c(c1)cncc2N3CCC4(C3=O)CN(Cc5c4cc(cc5)Cl)CC(=O)NC6(CC6)C#N |
−5.0
± 0.3
|
3.7
± 0.2
|
237 |
ALP-POS-ecbed2ba-12
|
|
c1ccc2c(c1)cncc2N3CCC4(C3=O)CN(Cc5c4cc(cc5)Cl)CC(=O)NCC6CC6 |
−5.0
± 0.2
|
3.7
± 0.2
|
238 |
EDJ-MED-d4864bdc-3
|
|
c1ccc2c(c1)cncc2N3CCC4(C3=O)CCS(=O)(=O)c5c4cc(cc5)Cl |
−4.9
± 0.2
|
3.6
± 0.1
|
239 |
EDJ-MED-94fddcec-5
|
|
CS(=O)(=O)c1ccc2c(c1)cncc2N3CCC4(C3=O)CCS(=O)(=O)c5c4cc(cc5)Cl |
−4.9
± 0.2
|
3.5
± 0.1
|
240 |
LUO-POS-b4dec3be-1
|
|
CNC(=O)CN1Cc2ccc(cc2[C@@]3(C1)CCN(C3=O)c4cncc5c4cc(cc5)F)Cl |
−4.8
± 0.2
|
3.5
± 0.1
|
241 |
EDJ-MED-9f4ac58c-3
|
|
CS(=O)(=O)Nc1ccc2c(c1)cncc2N3CCC4(C3=O)CN(C(=O)c5c4cc(cc5)Cl)S(=O)(=O)CC6(CC6)C#N |
−4.8
± 0.5
|
3.5
± 0.3
|
242 |
PET-UNK-aa57768f-2
|
|
c1ccc2c(c1)cncc2N3CC[C@@]4(C3=O)CN(C(=O)c5c4cc(cc5)Cl)CC#N |
−4.8
± 0.1
|
3.47
± 0.09
|
243 |
MAT-POS-853c0ffa-13
|
|
c1cc2cncc(c2cc1F)N3CCC4(C3=O)CN(Cc5c4cc(cc5)Cl)S(=O)(=O)CC6(CC6)C#N |
−4.7
± 0.3
|
3.5
± 0.2
|
244 |
MAT-POS-38eb6498-5
|
|
CNC(=O)CN1Cc2ccc(cc2C3(C1)CCN(C3=O)c4cncc5c4cc(cc5)C(=O)NC)Cl |
−4.7
± 0.2
|
3.4
± 0.2
|
245 |
PET-UNK-94036022-13
|
|
C=C1C(=O)C2(CN(Cc3c2cc(cc3)Cl)S(=O)(=O)CC4(CC4)C#N)C(=O)N1c5cncc6c5cccc6 |
−4.6
± 0.4
|
3.4
± 0.3
|
246 |
EDJ-MED-8bb691af-6
|
|
c1ccc2c(c1)cncc2N3CCC4(C3=O)CN(Cc5c4cc(cc5)Cl)S(=O)(=O)CC6(CC6)C#N |
−4.6
± 0.3
|
3.3
± 0.2
|
247 |
ALP-POS-afe0272e-1
|
|
CNC(=O)CN1Cc2cc(c(cc2C3(C1)CCN(C3=O)c4cncc5c4cccc5)Cl)Cl |
−4.5
± 0.2
|
3.3
± 0.1
|
248 |
MAT-POS-69786b79-3
|
|
CC1(CC1)NC(=O)CN2Cc3ccc(cc3C4(C2)CCN(C4=O)c5cncc6c5cccc6)Cl |
−4.5
± 0.3
|
3.3
± 0.2
|
249 |
ALP-POS-ecbed2ba-10
|
|
COC1CN(C1)S(=O)(=O)N2Cc3ccc(cc3C4(C2)CCN(C4=O)c5cncc6c5cccc6)Cl |
−4.5
± 0.5
|
3.3
± 0.4
|
250 |
ALP-POS-ecbed2ba-5
|
|
c1ccc2c(c1)cncc2N3CCC4(C3=O)CN(Cc5c4cc(cc5)Cl)S(=O)(=O)CC6CS(=O)(=O)C6 |
−4.4
± 0.8
|
3.2
± 0.6
|
251 |
MAT-POS-b4d6b7fc-5
|
|
CNC(=O)CN1Cc2ccc(cc2C3(C1)CCN(C3=O)c4cncc5c4cc(cc5)F)Cl |
−4.4
± 0.2
|
3.2
± 0.1
|
252 |
EDJ-MED-d7486dd1-1
|
|
Cc1cc(cc2c1c(cnc2)N3CCC4(C3)CCOc5c4cc(cc5)Cl)S(=O)(=O)C |
−4.40
± 0.08
|
3.21
± 0.06
|
253 |
MAT-POS-853c0ffa-5
|
|
c1cc2cncc(c2c(c1)Cl)N3CCC4(C3=O)CN(Cc5c4cc(cc5)Cl)S(=O)(=O)CC6(CC6)C#N |
−4.4
± 0.7
|
3.2
± 0.5
|
254 |
EDJ-MED-a6bab6fb-1
|
|
Cc1cccc2c1c(cnc2)N3CCC4(C3)CCOc5c4cc(cc5)Cl |
−4.17
± 0.07
|
3.04
± 0.05
|
255 |
EDJ-MED-94fddcec-6
|
|
CN(c1ccc2c(c1)cncc2N3CCC4(C3=O)CCS(=O)(=O)c5c4cc(cc5)Cl)S(=O)(=O)C |
−4.2
± 0.2
|
3.0
± 0.2
|
256 |
ALP-POS-ecbed2ba-14
|
|
c1ccc2c(c1)cncc2N3CCC4(C3=O)CN(Cc5c4cc(cc5)Cl)CC(=O)NCC#N |
−4.1
± 0.2
|
3.0
± 0.2
|
257 |
MAT-POS-c7726e07-5
|
|
CNC(=O)CN1Cc2ccc(cc2[C@]3(C1)CCN(C3=O)c4cncc5c4cccc5)Cl |
−4.1
± 0.3
|
3.0
± 0.2
|
258 |
LUO-POS-b4dec3be-2
|
|
CNC(=O)CN1Cc2ccc(cc2[C@]3(C1)CCN(C3=O)c4cncc5c4cc(cc5)F)Cl |
−4.1
± 0.2
|
3.0
± 0.2
|
259 |
EDJ-MED-8bb691af-7
|
|
CNC(=O)CN1CC2(CCN(C2)c3cncc4c3cccc4)c5cc(ccc5C1=O)Cl |
−4.0
± 0.1
|
2.89
± 0.08
|
260 |
EDJ-MED-e78d5f1a-1
|
|
c1cc2cncc(c2c(c1)Cl)N3CCC4(C3)CCOc5c4cc(cc5)Cl |
−3.93
± 0.08
|
2.87
± 0.06
|
261 |
LUO-POS-868e8996-12
|
|
CNC(=O)CN1Cc2ccc(cc2[C@@]3(C1)CCN(C3=O)c4cncc5c4cccc5)Cl |
−3.8
± 0.2
|
2.8
± 0.1
|
262 |
EDJ-MED-159244ea-2
|
|
c1ccc2c(c1)cncc2N3CC[C@@]4(C3)CCOc5c4cc(cc5)Cl |
−3.76
± 0.08
|
2.74
± 0.06
|
263 |
MAT-POS-b4d6b7fc-6
|
|
CNC(=O)CN1Cc2ccc(cc2C3(C1)CCN(C3=O)c4cncc5c4c(ccc5)Cl)Cl |
−3.6
± 0.2
|
2.7
± 0.1
|
264 |
MAT-POS-983b399a-2
|
|
c1ccc2c(c1)cncc2N3CCC4(C3)CCOc5c4cc(cc5)Cl |
−3.63
± 0.07
|
2.65
± 0.05
|
265 |
EDJ-MED-8bb691af-2
|
|
c1ccc2c(c1)cncc2N3CCC4(C3)CN(Cc5c4cc(cc5)Cl)S(=O)(=O)CC6(CC6)C#N |
−3.6
± 0.2
|
2.6
± 0.2
|
266 |
EDJ-MED-f3cfbbb5-1
|
|
Cc1cccc2c1c(cnc2)N3CCC4(C3)COCc5c4cc(cc5)Cl |
−3.59
± 0.07
|
2.62
± 0.05
|
267 |
MAT-POS-1d5ab790-2
|
|
CNC(=O)CN1Cc2ccc(cc2C3(C1)CCN(C3=O)c4cncc5c4c(ccc5)Cl)Cl |
−3.4
± 0.2
|
2.5
± 0.2
|
268 |
LUO-POS-eaf50f21-1
|
|
c1ccc2c(c1)cncc2N3C(=O)C4(CN(Cc5c4cc(cc5)Cl)S(=O)(=O)CC6(CC6)C#N)N=C3N |
−3.4
± 0.4
|
2.5
± 0.3
|
269 |
EDJ-MED-3656d29d-1
|
|
Cc1cccc2c1c(cnc2)N3CCC4(C3)CN(Cc5c4cc(cc5)Cl)CC(=O)NC |
−3.1
± 0.1
|
2.29
± 0.08
|
270 |
EDJ-MED-8bb691af-1
|
|
CNC(=O)CN1Cc2ccc(cc2C3(C1)CCN(C3)c4cncc5c4cccc5)Cl |
−3.1
± 0.1
|
2.29
± 0.09
|
271 |
PET-UNK-94036022-6
|
|
C=C1C(=O)[C@]2(CN(Cc3c2cc(cc3)Cl)S(=O)(=O)CC4(CC4)C#N)C(=O)N1c5cncc6c5cccc6 |
−3.1
± 0.3
|
2.3
± 0.2
|
272 |
EDG-MED-00af8776-1
|
|
c1ccc2c(c1)cncc2N3C=NC4(C3=O)CN(Cc5c4cc(cc5)Cl)S(=O)(=O)CC6(CC6)C#N |
−2.9
± 0.4
|
2.1
± 0.3
|
273 |
ALP-POS-ecbed2ba-8
|
|
c1ccc2c(c1)cncc2N3CCC4(C3=O)CN(Cc5c4cc(cc5)Cl)S(=O)(=O)CC6(CCC6)C#N |
−2.8
± 0.5
|
2.1
± 0.4
|
274 |
EDJ-MED-98c0a822-1
|
|
CNC(=O)C1(CCC1)N2CC3(CCN(C3=O)c4cncc5c4cccc5)c6cc(ccc6S2(=O)=O)Cl |
−2.6
± 0.3
|
1.9
± 0.2
|
275 |
PET-UNK-94036022-7
|
|
CNC(=O)CN1Cc2ccc(cc2[C@]3(C1)C(=O)C(=C)N(C3=O)c4cncc5c4cccc5)Cl |
−2.3
± 0.2
|
1.7
± 0.2
|
276 |
EDG-MED-0c930815-1
|
|
c1ccc2c(c1)cncc2N3C=NC4(C3=O)CN(Cc5c4cc(cc5)Cl)S(=O)(=O)CC6(CC6)C#N |
−1.5
± 0.3
|
1.1
± 0.2
|
277 |
PET-UNK-94036022-14
|
|
CNC(=O)CN1Cc2ccc(cc2C3(C1)C(=O)C(=C)N(C3=O)c4cncc5c4cccc5)Cl |
−1.4
± 0.3
|
1.0
± 0.2
|
278 |
EDJ-MED-976a33d5-3
|
|
CNC(=O)C1(CC1)N2CC3(CCN(C3=O)c4cncc5c4cccc5)c6cc(ccc6S2(=O)=O)Cl |
−1.2
± 0.5
|
0.9
± 0.4
|
279 |
EDG-MED-b6bce001-1
|
|
c1ccc2c(c1)cncc2N3C=NC4(C3=O)CN(Cc5c4cc(cc5)Cl)S(=O)(=O)CC6(CC6)C#N |
−1.2
± 0.3
|
0.8
± 0.2
|
280 |
EDJ-MED-fd8ed875-1
|
|
CNC(=O)CN1CC2(c3cc(ccc3C1=O)Cl)C(=O)N(C=N2)c4cncc5c4cccc5 |
−0.8
± 0.2
|
0.6
± 0.1
|
281 |
LUO-POS-b5068a05-1
|
|
CN(C)NC1=NC2(CN(Cc3c2cc(cc3)Cl)S(=O)(=O)CC4(CC4)C#N)C(=O)N1c5cncc6c5cccc6 |
−0.8
± 0.3
|
0.6
± 0.2
|
282 |
EDJ-MED-fd8ed875-2
|
|
CNC(=O)C1(CC1)N2CC3(c4cc(ccc4C2=O)Cl)C(=O)N(C=N3)c5cncc6c5cccc6 |
−0.6
± 0.2
|
0.4
± 0.1
|
283 |
LUO-POS-eaf50f21-3
|
|
CC(=O)NC1=NC2(CN(Cc3c2cc(cc3)Cl)S(=O)(=O)CC4(CC4)C#N)C(=O)N1c5cncc6c5cccc6 |
0.2
± 0.5
|
−0.1
± 0.3
|
284 |
EDG-MED-b6bce001-2
|
|
CC1=NC2(CN(Cc3c2cc(cc3)Cl)S(=O)(=O)CC4(CC4)C#N)C(=O)N1c5cncc6c5cccc6 |
0.2
± 0.6
|
−0.1
± 0.5
|
285 |
LUO-POS-eaf50f21-4
|
|
CN(C)C1=NC2(CN(Cc3c2cc(cc3)Cl)S(=O)(=O)CC4(CC4)C#N)C(=O)N1c5cncc6c5cccc6 |
1.4
± 0.4
|
−1.0
± 0.3
|