Rank |
Compound |
SMILES |
ΔG / kcal M-1 |
pIC50 |
301 |
EDJ-MED-8bb691af-6
|
|
c1ccc2c(c1)cncc2N3CCC4(C3=O)CN(Cc5c4cc(cc5)Cl)S(=O)(=O)CC6(CC6)C#N |
−6.8
± 0.8
|
4.9
± 0.6
|
302 |
VLA-UNK-e334495f-2
|
|
c1ccc2c(c1)cncc2N3CCC4(C3=O)CN(Cc5c4cc(c(c5)F)Cl)S(=O)(=O)CC6(CC6)C#N |
−6.7
± 0.6
|
4.9
± 0.5
|
303 |
EDJ-MED-40e596c8-1
|
|
CNS(=O)(=O)CN1Cc2ccc(cc2C3(C1)CCN(C3=O)c4cncc5c4cccc5)Cl |
−6.7
± 0.4
|
4.9
± 0.3
|
304 |
ALP-POS-ecbed2ba-3
|
|
CC1(CC1)CS(=O)(=O)N2Cc3ccc(cc3C4(C2)CCN(C4=O)c5cncc6c5cccc6)Cl |
−6.6
± 0.9
|
4.8
± 0.7
|
305 |
ALP-POS-477dc5b7-4
|
|
c1ccc2c(c1)cncc2N3CCC4(C3=O)CCOc5c4cc(cc5)Cl |
−6.6
± 0.3
|
4.8
± 0.2
|
306 |
VLA-UNK-3a43cd95-3
|
|
c1ccc2c(c1)cncc2N3C(=O)C[C@@]4(C3=O)CCOc5c4cc(c(c5)F)Cl |
−6.6
± 0.2
|
4.8
± 0.2
|
307 |
EDJ-MED-d4864bdc-3
|
|
c1ccc2c(c1)cncc2N3CCC4(C3=O)CCS(=O)(=O)c5c4cc(cc5)Cl |
−6.6
± 0.3
|
4.8
± 0.3
|
308 |
VLA-UNK-f2612802-2
|
|
CNC(=O)CN1C[C@]2(CCN(C2=O)c3cncc4c3cccc4)c5cc(c(cc5S1(=O)=O)F)Cl |
−6.6
± 0.5
|
4.8
± 0.4
|
309 |
JOH-MSK-1f2dff76-4
|
|
c1ccc2c(c1)cncc2N3C(=O)C[C@@]4(C3=O)CNCc5c4cc(cc5)Cl |
−6.6
± 0.4
|
4.8
± 0.3
|
310 |
EDJ-MED-468565e0-5
|
|
c1cc2cncc(c2cc1OCCN3CC(C3)(F)F)N4CCC5(C4=O)CN(Cc6c5cc(cc6)Cl)S(=O)(=O)CC7(CC7)C#N |
−6.6
± 1.0
|
4.8
± 0.7
|
311 |
VLA-UCB-05e51b3f-5
|
|
c1ccc2c(c1)cncc2N3C(=O)C[C@]4(C3=O)CCOc5c4cc(cc5)Cl |
−6.6
± 0.1
|
4.78
± 0.08
|
312 |
EDJ-MED-4138fde9-3
|
|
CNCCOc1ccc2cncc(c2c1)N3CCC4(C3=O)CN(Cc5c4cc(cc5)Cl)C6(CC6)C(=O)NC |
−6.6
± 0.4
|
4.8
± 0.3
|
313 |
DAR-DIA-6be260fc-5
|
|
c1ccc2c(c1)cncc2N3CCC4(C3=O)CCNc5c4cc(cc5)Cl |
−6.5
± 0.3
|
4.7
± 0.2
|
314 |
EDJ-MED-98c0a822-2
|
|
CNC(=O)C1(COC1)N2CC3(CCN(C3=O)c4cncc5c4cccc5)c6cc(ccc6S2(=O)=O)Cl |
−6.4
± 0.5
|
4.7
± 0.4
|
315 |
EDJ-MED-accc2c4d-1
|
|
c1ccc2c(c1)cncc2N3CCC4(C3=O)CN(Cc5c4cc(cc5)Cl)S(=O)(=O)CCC#N |
−6.4
± 0.8
|
4.7
± 0.6
|
316 |
MAT-POS-853c0ffa-6
|
|
c1cc2c(cc1Cl)C3(CCN(C3=O)c4cncc5c4c(cc(c5)F)Cl)CN(C2)S(=O)(=O)CC6(CC6)C#N |
−6.4
± 0.1
|
4.64
± 0.10
|
317 |
LUO-POS-e1dab717-19
|
|
c1ccc2c(c1)cncc2N3CCC4(C3=O)CN(Cc5c4cc(cc5)Cl)CC(=O)O |
−6.4
± 0.3
|
4.6
± 0.2
|
318 |
EDJ-MED-159244ea-1
|
|
c1ccc2c(c1)cncc2N3CC[C@]4(C3=O)CCOc5c4cc(cc5)Cl |
−6.2
± 0.3
|
4.5
± 0.2
|
319 |
ALP-POS-ecbed2ba-20
|
|
c1ccc2c(c1)cncc2N3CCC4(C3=O)CN(Cc5c4cc(cc5)Cl)S(=O)(=O)N6CCC6 |
−6
± 1
|
4.5
± 0.7
|
320 |
EDJ-MED-accc2c4d-3
|
|
c1ccc2c(c1)cncc2N3CCC4(C3=O)CN(Cc5c4cc(cc5)Cl)S(=O)(=O)CC#N |
−6.2
± 0.7
|
4.5
± 0.5
|
321 |
LUO-POS-868e8996-10
|
|
c1ccc2c(c1)cncc2N3C(=O)C[C@]4(C3=O)CN(Cc5c4cc(cc5)Cl)S(=O)(=O)CC6(CC6)C#N |
−6.2
± 0.1
|
4.51
± 0.10
|
322 |
EDJ-MED-ede5c6cb-2
|
|
c1cc2c(cc1NS(=O)(=O)C3CC3)cncc2N4CCC5(C4=O)CCS(=O)(=O)c6c5cc(cc6)Cl |
−6.2
± 0.4
|
4.5
± 0.3
|
323 |
EDJ-MED-7587a9ee-3
|
|
CS(=O)(=O)N1Cc2ccc(cc2C3(C1)CCN(C3=O)c4cncc5c4cccc5)Cl |
−6.2
± 0.8
|
4.5
± 0.5
|
324 |
ALP-POS-ecbed2ba-6
|
|
COC1(CC1)CS(=O)(=O)N2Cc3ccc(cc3C4(C2)CCN(C4=O)c5cncc6c5cccc6)Cl |
−6.2
± 0.7
|
4.5
± 0.5
|
325 |
MIK-ENA-0547b12c-1
|
|
CC[C@@H]1CN(C(=O)[C@@]12CN(Cc3c2cc(cc3)Cl)S(=O)(=O)CC4(CC4)C#N)c5cncc6c5cccc6 |
−6.2
± 0.9
|
4.5
± 0.6
|
326 |
VLA-UNK-5d8210f0-5
|
|
CNC(=O)CN1Cc2ccc(cc2C3(C1C(F)F)CCN(C3=O)c4cncc5c4cccc5)Cl |
−6.1
± 0.4
|
4.4
± 0.3
|
327 |
EDJ-MED-dfa1d800-2
|
|
CNC(=O)C1(CC1)N2CC3(CCN(C3=O)c4cncc5c4cc(cc5)OCCN6CCOCC6)c7cc(ccc7C2=O)Cl |
−6.1
± 0.3
|
4.4
± 0.2
|
328 |
LUO-POS-868e8996-7
|
|
CNC(=O)CN1C[C@@]2(CC(=O)N(C2=O)c3cncc4c3cccc4)c5cc(ccc5C1=O)Cl |
−6.0
± 0.1
|
4.34
± 0.09
|
329 |
MAT-POS-50a80394-3
|
|
CC(C)C1CN(C(=O)C12CN(Cc3c2cc(cc3)Cl)S(=O)(=O)CC4(CC4)C#N)c5cncc6c5cccc6 |
−5.9
± 0.8
|
4.3
± 0.6
|
330 |
ALP-POS-ecbed2ba-19
|
|
CN(CCO)S(=O)(=O)N1Cc2ccc(cc2C3(C1)CCN(C3=O)c4cncc5c4cccc5)Cl |
−6
± 1
|
4.3
± 0.8
|
331 |
MAT-POS-853c0ffa-14
|
|
COC1(CC1)CS(=O)(=O)N2Cc3ccc(cc3C4(C2)CCN(C4=O)c5cncc6c5cc(cc6)F)Cl |
−5.8
± 0.9
|
4.3
± 0.7
|
332 |
PET-UNK-94036022-9
|
|
C#CC1(CC1)CS(=O)(=O)N2Cc3ccc(cc3C4(C2)CCN(C4=O)c5cncc6c5cccc6)Cl |
−5.8
± 0.8
|
4.2
± 0.6
|
333 |
JOH-MSK-1f2dff76-3
|
|
c1ccc2c(c1)cncc2N3C(=O)C[C@]4(C3=O)CNCc5c4cc(cc5)Cl |
−5.7
± 0.4
|
4.2
± 0.3
|
334 |
EDJ-MED-5cd3920d-2
|
|
c1cc2cncc(c2cc1C(F)F)N3CCC4(C3=O)CN(Cc5c4cc(cc5)Cl)S(=O)(=O)CC6(CC6)C#N |
−5.7
± 0.8
|
4.1
± 0.6
|
335 |
EDJ-MED-468565e0-1
|
|
c1cc2cncc(c2cc1OCCN3CCCC3)N4CCC5(C4=O)CN(Cc6c5cc(cc6)Cl)S(=O)(=O)CC7(CC7)C#N |
−5.5
± 0.8
|
4.0
± 0.6
|
336 |
PET-UNK-94036022-10
|
|
c1ccc2c(c1)cncc2N3CCC4(C3=O)CN(Cc5c4cc(cc5)Cl)S(=O)(=O)CC6(CC6)Cl |
−5.4
± 0.8
|
4.0
± 0.6
|
337 |
MIK-ENA-edcfce18-1
|
|
CC[C@@H]1CN(C(=O)[C@]12CN(Cc3c2cc(cc3)Cl)S(=O)(=O)CC4(CC4)C#N)c5cncc6c5cccc6 |
−5.4
± 0.5
|
4.0
± 0.4
|
338 |
ALP-POS-ecbed2ba-5
|
|
c1ccc2c(c1)cncc2N3CCC4(C3=O)CN(Cc5c4cc(cc5)Cl)S(=O)(=O)CC6CS(=O)(=O)C6 |
−5.3
± 0.9
|
3.9
± 0.7
|
339 |
PET-UNK-94036022-12
|
|
c1ccc2c(c1)cncc2N3C(=O)CC4(C3=O)CN(Cc5c4cc(cc5)Cl)S(=O)(=O)CC6(CC6)Cl |
−5.3
± 0.9
|
3.9
± 0.7
|
340 |
EDJ-MED-dfa1d800-4
|
|
CNC(=O)C1(CC1)N2CC3(CCN(C3=O)c4cncc5c4cc(cc5)OCCN6CCC(CC6)(F)F)c7cc(ccc7C2=O)Cl |
−5.3
± 0.4
|
3.8
± 0.3
|
341 |
MIK-ENA-2c0ad173-1
|
|
C[C@@H]1CN(C(=O)[C@@]12CN(Cc3c2cc(cc3)Cl)S(=O)(=O)CC4(CC4)C#N)c5cncc6c5cccc6 |
−5.2
± 0.7
|
3.8
± 0.5
|
342 |
EDJ-MED-f9b78f78-4
|
|
c1ccc2c(c1)cncc2N3CCC4(C3=O)CNS(=O)(=O)c5c4cc(cc5)Cl |
−5.1
± 0.4
|
3.7
± 0.3
|
343 |
MAT-POS-853c0ffa-21
|
|
CC1(CC1)CS(=O)(=O)N2Cc3ccc(cc3C4(C2)CCN(C4=O)c5cncc6c5cc(cc6)F)Cl |
−5.1
± 0.8
|
3.7
± 0.6
|
344 |
EDJ-MED-4138fde9-2
|
|
c1cc2cncc(c2cc1OCCNCC(F)(F)F)N3CCC4(C3=O)CN(Cc5c4cc(cc5)Cl)S(=O)(=O)CC6(CC6)C#N |
−5.1
± 1.0
|
3.7
± 0.7
|
345 |
ALP-POS-ecbed2ba-18
|
|
CCN(C)S(=O)(=O)N1Cc2ccc(cc2C3(C1)CCN(C3=O)c4cncc5c4cccc5)Cl |
−5.1
± 0.9
|
3.7
± 0.7
|
346 |
EDJ-MED-3707c4bc-1
|
|
CC(C)CS(=O)(=O)N1Cc2ccc(cc2C3(C1)CCN(C3=O)c4cncc5c4cccc5)Cl |
−5.0
± 0.9
|
3.6
± 0.7
|
347 |
MIC-UNK-c85ea37c-2
|
|
CCC(=O)Nc1ccc(cc1)C2CN(C(=O)C23CN(Cc4c3cc(cc4)Cl)S(=O)(=O)CC5(CC5)C#N)c6cncc7c6cccc7 |
−5.0
± 0.9
|
3.6
± 0.6
|
348 |
LUO-POS-e1dab717-16
|
|
CC1(CC2(CN(Cc3c2cc(cc3)Cl)S(=O)(=O)CC4(CC4)C#N)C(=O)N1c5cncc6c5cccc6)C |
−5.0
± 1.0
|
3.6
± 0.7
|
349 |
MAT-POS-40ad851a-1
|
|
CN1CCCC1COc2ccc3cncc(c3c2)N4CCC5(C4=O)CN(Cc6c5cc(cc6)Cl)S(=O)(=O)CC7(CC7)C#N |
−4.9
± 0.7
|
3.6
± 0.5
|
350 |
EDJ-MED-976a33d5-3
|
|
CNC(=O)C1(CC1)N2CC3(CCN(C3=O)c4cncc5c4cccc5)c6cc(ccc6S2(=O)=O)Cl |
−4.9
± 0.9
|
3.6
± 0.6
|
351 |
ALP-POS-ecbed2ba-17
|
|
CN(CC#N)S(=O)(=O)N1Cc2ccc(cc2C3(C1)CCN(C3=O)c4cncc5c4cccc5)Cl |
−4.9
± 0.8
|
3.6
± 0.5
|
352 |
MIC-UNK-c85ea37c-3
|
|
CN(C)c1ccc(cc1)C2CN(C(=O)C23CN(Cc4c3cc(cc4)Cl)S(=O)(=O)CC5(CC5)C#N)c6cncc7c6cccc7 |
−4.8
± 0.7
|
3.5
± 0.5
|
353 |
ALP-POS-ecbed2ba-11
|
|
c1ccc2c(c1)cncc2N3CCC4(C3=O)CN(Cc5c4cc(cc5)Cl)S(=O)(=O)CC6(CCOCC6)C#N |
−4.7
± 0.9
|
3.4
± 0.7
|
354 |
ALP-POS-ecbed2ba-10
|
|
COC1CN(C1)S(=O)(=O)N2Cc3ccc(cc3C4(C2)CCN(C4=O)c5cncc6c5cccc6)Cl |
−4.6
± 0.8
|
3.3
± 0.6
|
355 |
ALP-POS-ecbed2ba-13
|
|
CC(C)(CS(=O)(=O)N1Cc2ccc(cc2C3(C1)CCN(C3=O)c4cncc5c4cccc5)Cl)C#N |
−4.4
± 0.9
|
3.2
± 0.7
|
356 |
EDJ-MED-3707c4bc-2
|
|
CC(C)(C)CS(=O)(=O)N1Cc2ccc(cc2C3(C1)CCN(C3=O)c4cncc5c4cccc5)Cl |
−4.4
± 0.7
|
3.2
± 0.5
|
357 |
MIC-UNK-257d841f-1
|
|
c1ccc2c(c1)cncc2N3CC(C4(C3=O)CN(Cc5c4cc(cc5)Cl)S(=O)(=O)CC6(CC6)C#N)C7CC7 |
−4.3
± 0.8
|
3.1
± 0.6
|
358 |
EDJ-MED-ee81482e-4
|
|
c1cc2cncc(c2cc1OC3CCNCC3)N4CCC5(C4=O)CN(Cc6c5cc(cc6)Cl)S(=O)(=O)CC7(CC7)C#N |
−4
± 1
|
3.1
± 0.7
|
359 |
MIK-ENA-17e27e9c-1
|
|
C[C@H]1CN(C(=O)[C@@]12CN(Cc3c2cc(cc3)Cl)S(=O)(=O)CC4(CC4)C#N)c5cncc6c5cccc6 |
−4.2
± 0.6
|
3.1
± 0.4
|
360 |
MAT-POS-50a80394-8
|
|
CC1(CN(C(=O)C12CN(Cc3c2cc(cc3)Cl)S(=O)(=O)CC4(CC4)C#N)c5cncc6c5cccc6)C |
−4.0
± 0.9
|
2.9
± 0.7
|
361 |
LUO-POS-ed2cfb03-2
|
|
CNS(=O)(=O)N1Cc2ccc(cc2C3(C1)CCN(C3=O)c4cncc5c4cccc5)Cl |
−4.0
± 0.8
|
2.9
± 0.6
|
362 |
MAT-POS-50a80394-1
|
|
CC1CN(C(=O)C12CN(Cc3c2cc(cc3)Cl)S(=O)(=O)CC4(CC4)C#N)c5cncc6c5cccc6 |
−3.8
± 0.6
|
2.8
± 0.4
|
363 |
ALP-POS-ecbed2ba-21
|
|
CN(CCOC)S(=O)(=O)N1Cc2ccc(cc2C3(C1)CCN(C3=O)c4cncc5c4cccc5)Cl |
−3.7
± 0.9
|
2.7
± 0.6
|
364 |
MIK-ENA-8063e9dc-1
|
|
CN(C)CCOc1ccc2cncc(c2c1)N3CC[C@]4(C3=O)CN(Cc5c4cc(cc5)Cl)S(=O)(=O)CC6(CC6)C#N |
−3.7
± 0.9
|
2.7
± 0.6
|
365 |
EDJ-MED-4138fde9-7
|
|
CN1CC(C1)(CS(=O)(=O)N2Cc3ccc(cc3C4(C2)CCN(C4=O)c5cncc6c5cccc6)Cl)C#N |
−3.6
± 0.8
|
2.7
± 0.6
|
366 |
MAT-POS-40ad851a-4
|
|
CN(C)CCCOc1ccc2cncc(c2c1)N3CCC4(C3=O)CN(Cc5c4cc(cc5)Cl)S(=O)(=O)CC6(CC6)C#N |
−3.5
± 0.9
|
2.5
± 0.7
|
367 |
ALP-POS-ecbed2ba-22
|
|
c1ccc2c(c1)cncc2N3CCC4(C3=O)CN(Cc5c4cc(cc5)Cl)S(=O)(=O)CC6(CC6)CC#N |
−3.5
± 0.8
|
2.5
± 0.6
|
368 |
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
|
2.5
± 0.7
|
369 |
ALP-POS-ecbed2ba-9
|
|
c1ccc2c(c1)cncc2N3CCC4(C3=O)CN(Cc5c4cc(cc5)Cl)S(=O)(=O)N6CC(C6)C#N |
−3
± 1
|
2.4
± 0.8
|
370 |
EDJ-MED-468565e0-2
|
|
c1cc2cncc(c2cc1OCCN3CCOCC3)N4CCC5(C4=O)CN(Cc6c5cc(cc6)Cl)S(=O)(=O)CC7(CC7)C#N |
−3.0
± 0.6
|
2.2
± 0.5
|
371 |
LUO-POS-d1147590-1
|
|
CN1CCC(CC1)Oc2ccc3cncc(c3c2)N4CCC5(C4=O)CN(Cc6c5cc(cc6)Cl)S(=O)(=O)CC7(CC7)C#N |
−2.9
± 1.0
|
2.1
± 0.7
|
372 |
LUO-POS-f7b1afe6-2
|
|
CC1(CN(C(=O)C12CN(Cc3c2cc(cc3)Cl)S(=O)(=O)CC4(CC4)C#N)c5cncc6c5cccc6)C |
−3
± 1
|
1.9
± 0.8
|
373 |
MAT-POS-40ad851a-2
|
|
CCN(C)CCOc1ccc2cncc(c2c1)N3CCC4(C3=O)CN(Cc5c4cc(cc5)Cl)S(=O)(=O)CC6(CC6)C#N |
−2.3
± 0.7
|
1.6
± 0.5
|
374 |
EDJ-MED-468565e0-3
|
|
c1cc2cncc(c2cc1OCCN3CCS(=O)(=O)CC3)N4CCC5(C4=O)CN(Cc6c5cc(cc6)Cl)S(=O)(=O)CC7(CC7)C#N |
−2.2
± 0.7
|
1.6
± 0.5
|
375 |
EDJ-MED-ee81482e-3
|
|
CN(C)CC(COc1ccc2cncc(c2c1)N3CCC4(C3=O)CN(Cc5c4cc(cc5)Cl)S(=O)(=O)CC6(CC6)C#N)O |
−2.0
± 0.8
|
1.5
± 0.6
|
376 |
MAT-POS-1a788f51-4
|
|
CC(C)(C)NCCOc1ccc2cncc(c2c1)N3CCC4(C3=O)CN(Cc5c4cc(cc5)Cl)S(=O)(=O)CC6(CC6)C#N |
−1.8
± 1.0
|
1.3
± 0.7
|
377 |
MAT-POS-40ad851a-5
|
|
c1cc2cncc(c2cc1OCCCN3CCCC3)N4CCC5(C4=O)CN(Cc6c5cc(cc6)Cl)S(=O)(=O)CC7(CC7)C#N |
−1.4
± 0.7
|
1.0
± 0.5
|
378 |
MAT-POS-40ad851a-3
|
|
CCN(CC)CCOc1ccc2cncc(c2c1)N3CCC4(C3=O)CN(Cc5c4cc(cc5)Cl)S(=O)(=O)CC6(CC6)C#N |
−1.0
± 1.0
|
0.7
± 0.7
|
379 |
PET-UNK-94036022-13
|
|
C=C1C(=O)C2(CN(Cc3c2cc(cc3)Cl)S(=O)(=O)CC4(CC4)C#N)C(=O)N1c5cncc6c5cccc6 |
0.5
± 0.9
|
−0.3
± 0.7
|
380 |
EDJ-MED-468565e0-4
|
|
c1cc2cncc(c2cc1OCCN3CCC(CC3)(F)F)N4CCC5(C4=O)CN(Cc6c5cc(cc6)Cl)S(=O)(=O)CC7(CC7)C#N |
0.5
± 0.5
|
−0.4
± 0.4
|