Ligand source activities (1 row/activity)
Ligands (move mouse cursor over ligand name to see structure) | Receptor | Activity | Chemical information | |||||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Sel. page | Common name |
GPCRdb ID |
Reference ligand |
Vendors |
Species |
Assay Type |
Activity Type |
Activity Relation |
Activity Value |
p-value (-log) |
Fold selectivity |
Tested GPCRs |
Assay Description |
Source |
Mol weight |
Rot Bonds |
H don |
H acc |
LogP |
Smiles |
DOI |
|
71461073 | 84624 | None | 1 | Human | Functional | pEC50 | = | 6 | 6.0 | - | 1 | ChEMBL | 472 | 5 | 0 | 0 | 6.5 | CC1(C)[C@H]2CC=C(C[N+](C)(C)Cc3ccc(-c4ccccc4I)cc3)[C@@H]1C2 | 10.1021/jm301240t | |||
71461074 | 84624 | None | 1 | Human | Functional | pEC50 | = | 6 | 6.0 | - | 1 | ChEMBL | 472 | 5 | 0 | 0 | 6.5 | CC1(C)[C@H]2CC=C(C[N+](C)(C)Cc3ccc(-c4ccccc4I)cc3)[C@@H]1C2 | 10.1021/jm301240t | |||
CHEMBL2181443 | 84624 | None | 1 | Human | Functional | pEC50 | = | 6 | 6.0 | - | 1 | ChEMBL | 472 | 5 | 0 | 0 | 6.5 | CC1(C)[C@H]2CC=C(C[N+](C)(C)Cc3ccc(-c4ccccc4I)cc3)[C@@H]1C2 | 10.1021/jm301240t | |||
CHEMBL2221034 | 84624 | None | 1 | Human | Functional | pEC50 | = | 6 | 6.0 | - | 1 | ChEMBL | 472 | 5 | 0 | 0 | 6.5 | CC1(C)[C@H]2CC=C(C[N+](C)(C)Cc3ccc(-c4ccccc4I)cc3)[C@@H]1C2 | 10.1021/jm301240t | |||
127032486 | 139188 | None | 0 | Human | Functional | pEC50 | = | 6.0 | 6.0 | - | 1 | ChEMBL | 744 | 16 | 3 | 6 | 6.7 | CC(C)(C)OC(=O)NCCCC[C@@H](NC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCC(=O)c1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.5b01965 | |||
CHEMBL3786631 | 139188 | None | 0 | Human | Functional | pEC50 | = | 6.0 | 6.0 | - | 1 | ChEMBL | 744 | 16 | 3 | 6 | 6.7 | CC(C)(C)OC(=O)NCCCC[C@@H](NC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCC(=O)c1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.5b01965 | |||
127030694 | 139302 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | ChEMBL | 644 | 15 | 3 | 5 | 5.2 | NCCCC[C@@H](NC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCC(=O)c1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.5b01965 | |||
CHEMBL3786670 | 139302 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | ChEMBL | 644 | 15 | 3 | 5 | 5.2 | NCCCC[C@@H](NC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCC(=O)c1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.5b01965 | |||
CHEMBL3787750 | 139302 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | ChEMBL | 644 | 15 | 3 | 5 | 5.2 | NCCCC[C@@H](NC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCC(=O)c1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.5b01965 | |||
127031313 | 139233 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | ChEMBL | 822 | 17 | 3 | 8 | 6.1 | CC(C)(C)OC(=O)N[C@@H](CCCCNC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCC(=O)c1ccc(S(C)(=O)=O)cc1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.5b01965 | |||
CHEMBL3787121 | 139233 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | ChEMBL | 822 | 17 | 3 | 8 | 6.1 | CC(C)(C)OC(=O)N[C@@H](CCCCNC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCC(=O)c1ccc(S(C)(=O)=O)cc1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.5b01965 | |||
71455657 | 84572 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | ChEMBL | 474 | 5 | 0 | 0 | 6.6 | CC1(C)[C@H]2CC[C@@H](C[N+](C)(C)Cc3ccc(-c4ccccc4I)cc3)[C@@H]1C2 | 10.1021/jm301240t | |||
CHEMBL2181446 | 84572 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | ChEMBL | 474 | 5 | 0 | 0 | 6.6 | CC1(C)[C@H]2CC[C@@H](C[N+](C)(C)Cc3ccc(-c4ccccc4I)cc3)[C@@H]1C2 | 10.1021/jm301240t | |||
CHEMBL2220411 | 84572 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | ChEMBL | 474 | 5 | 0 | 0 | 6.6 | CC1(C)[C@H]2CC[C@@H](C[N+](C)(C)Cc3ccc(-c4ccccc4I)cc3)[C@@H]1C2 | 10.1021/jm301240t | |||
71450270 | 84578 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | ChEMBL | 360 | 5 | 0 | 0 | 6.2 | Cc1ccccc1-c1ccc(C[N+](C)(C)CC2=CC[C@H]3C[C@@H]2C3(C)C)cc1 | 10.1021/jm301240t | |||
CHEMBL2181464 | 84578 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | ChEMBL | 360 | 5 | 0 | 0 | 6.2 | Cc1ccccc1-c1ccc(C[N+](C)(C)CC2=CC[C@H]3C[C@@H]2C3(C)C)cc1 | 10.1021/jm301240t | |||
CHEMBL2220445 | 84578 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | ChEMBL | 360 | 5 | 0 | 0 | 6.2 | Cc1ccccc1-c1ccc(C[N+](C)(C)CC2=CC[C@H]3C[C@@H]2C3(C)C)cc1 | 10.1021/jm301240t | |||
71459297 | 84583 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | ChEMBL | 364 | 5 | 0 | 0 | 6.1 | CC1(C)[C@H]2CC=C(C[N+](C)(C)Cc3ccc(-c4ccccc4F)cc3)[C@@H]1C2 | 10.1021/jm301240t | |||
CHEMBL2181451 | 84583 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | ChEMBL | 364 | 5 | 0 | 0 | 6.1 | CC1(C)[C@H]2CC=C(C[N+](C)(C)Cc3ccc(-c4ccccc4F)cc3)[C@@H]1C2 | 10.1021/jm301240t | |||
CHEMBL2220493 | 84583 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | ChEMBL | 364 | 5 | 0 | 0 | 6.1 | CC1(C)[C@H]2CC=C(C[N+](C)(C)Cc3ccc(-c4ccccc4F)cc3)[C@@H]1C2 | 10.1021/jm301240t | |||
71455653 | 84586 | None | 0 | Human | Functional | pEC50 | = | 4.9 | 4.9 | - | 1 | ChEMBL | 376 | 6 | 0 | 1 | 5.9 | COc1ccccc1-c1ccc(C[N+](C)(C)CC2=CC[C@H]3C[C@@H]2C3(C)C)cc1 | 10.1021/jm301240t | |||
CHEMBL2181441 | 84586 | None | 0 | Human | Functional | pEC50 | = | 4.9 | 4.9 | - | 1 | ChEMBL | 376 | 6 | 0 | 1 | 5.9 | COc1ccccc1-c1ccc(C[N+](C)(C)CC2=CC[C@H]3C[C@@H]2C3(C)C)cc1 | 10.1021/jm301240t | |||
CHEMBL2220506 | 84586 | None | 0 | Human | Functional | pEC50 | = | 4.9 | 4.9 | - | 1 | ChEMBL | 376 | 6 | 0 | 1 | 5.9 | COc1ccccc1-c1ccc(C[N+](C)(C)CC2=CC[C@H]3C[C@@H]2C3(C)C)cc1 | 10.1021/jm301240t | |||
127032747 | 139083 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | ChEMBL | 744 | 16 | 3 | 6 | 6.7 | CC(C)(C)OC(=O)NCCCC[C@H](NC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCC(=O)c1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.5b01965 | |||
CHEMBL3785515 | 139083 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | ChEMBL | 744 | 16 | 3 | 6 | 6.7 | CC(C)(C)OC(=O)NCCCC[C@H](NC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCC(=O)c1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.5b01965 | |||
71457436 | 84580 | None | 0 | Human | Functional | pEC50 | = | 5.8 | 5.8 | - | 1 | ChEMBL | 472 | 5 | 0 | 0 | 6.5 | CC1(C)[C@@H]2C=C(C[N+](C)(C)Cc3ccc(-c4ccccc4I)cc3)C[C@H]1C2 | 10.1021/jm301240t | |||
CHEMBL2181448 | 84580 | None | 0 | Human | Functional | pEC50 | = | 5.8 | 5.8 | - | 1 | ChEMBL | 472 | 5 | 0 | 0 | 6.5 | CC1(C)[C@@H]2C=C(C[N+](C)(C)Cc3ccc(-c4ccccc4I)cc3)C[C@H]1C2 | 10.1021/jm301240t | |||
CHEMBL2220478 | 84580 | None | 0 | Human | Functional | pEC50 | = | 5.8 | 5.8 | - | 1 | ChEMBL | 472 | 5 | 0 | 0 | 6.5 | CC1(C)[C@@H]2C=C(C[N+](C)(C)Cc3ccc(-c4ccccc4I)cc3)C[C@H]1C2 | 10.1021/jm301240t | |||
71452094 | 84584 | None | 0 | Human | Functional | pEC50 | = | 5.8 | 5.8 | - | 1 | ChEMBL | 380 | 5 | 0 | 0 | 6.6 | CC1(C)[C@H]2CC=C(C[N+](C)(C)Cc3ccc(-c4ccccc4Cl)cc3)[C@@H]1C2 | 10.1021/jm301240t | |||
CHEMBL2181452 | 84584 | None | 0 | Human | Functional | pEC50 | = | 5.8 | 5.8 | - | 1 | ChEMBL | 380 | 5 | 0 | 0 | 6.6 | CC1(C)[C@H]2CC=C(C[N+](C)(C)Cc3ccc(-c4ccccc4Cl)cc3)[C@@H]1C2 | 10.1021/jm301240t | |||
CHEMBL2220494 | 84584 | None | 0 | Human | Functional | pEC50 | = | 5.8 | 5.8 | - | 1 | ChEMBL | 380 | 5 | 0 | 0 | 6.6 | CC1(C)[C@H]2CC=C(C[N+](C)(C)Cc3ccc(-c4ccccc4Cl)cc3)[C@@H]1C2 | 10.1021/jm301240t | |||
71453926 | 84589 | None | 0 | Human | Functional | pEC50 | = | 5.7 | 5.7 | - | 1 | ChEMBL | 414 | 5 | 0 | 0 | 7.2 | CC1(C)[C@H]2CC=C(C[N+](C)(C)Cc3ccc(-c4c(Cl)cccc4Cl)cc3)[C@@H]1C2 | 10.1021/jm301240t | |||
CHEMBL2181460 | 84589 | None | 0 | Human | Functional | pEC50 | = | 5.7 | 5.7 | - | 1 | ChEMBL | 414 | 5 | 0 | 0 | 7.2 | CC1(C)[C@H]2CC=C(C[N+](C)(C)Cc3ccc(-c4c(Cl)cccc4Cl)cc3)[C@@H]1C2 | 10.1021/jm301240t | |||
CHEMBL2220526 | 84589 | None | 0 | Human | Functional | pEC50 | = | 5.7 | 5.7 | - | 1 | ChEMBL | 414 | 5 | 0 | 0 | 7.2 | CC1(C)[C@H]2CC=C(C[N+](C)(C)Cc3ccc(-c4c(Cl)cccc4Cl)cc3)[C@@H]1C2 | 10.1021/jm301240t | |||
127030984 | 139258 | None | 0 | Human | Functional | pEC50 | = | 5.7 | 5.7 | - | 1 | ChEMBL | 584 | 12 | 4 | 5 | 4.8 | CC(C)(C)OC(=O)N[C@@H](CCCCNC(=O)[C@@H]1Cc2ccccc2CN1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.5b01965 | |||
CHEMBL3787404 | 139258 | None | 0 | Human | Functional | pEC50 | = | 5.7 | 5.7 | - | 1 | ChEMBL | 584 | 12 | 4 | 5 | 4.8 | CC(C)(C)OC(=O)N[C@@H](CCCCNC(=O)[C@@H]1Cc2ccccc2CN1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.5b01965 | |||
127032169 | 139299 | None | 0 | Human | Functional | pEC50 | = | 5.7 | 5.7 | - | 1 | ChEMBL | 484 | 11 | 4 | 4 | 3.3 | N[C@@H](CCCCNC(=O)[C@@H]1Cc2ccccc2CN1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.5b01965 | |||
CHEMBL3787326 | 139299 | None | 0 | Human | Functional | pEC50 | = | 5.7 | 5.7 | - | 1 | ChEMBL | 484 | 11 | 4 | 4 | 3.3 | N[C@@H](CCCCNC(=O)[C@@H]1Cc2ccccc2CN1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.5b01965 | |||
CHEMBL3787718 | 139299 | None | 0 | Human | Functional | pEC50 | = | 5.7 | 5.7 | - | 1 | ChEMBL | 484 | 11 | 4 | 4 | 3.3 | N[C@@H](CCCCNC(=O)[C@@H]1Cc2ccccc2CN1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.5b01965 | |||
127032453 | 139165 | None | 0 | Human | Functional | pEC50 | = | 7.3 | 7.3 | - | 1 | ChEMBL | 804 | 18 | 3 | 8 | 6.7 | COc1ccc(C(=O)CCC(=O)N2Cc3ccccc3C[C@H]2C(=O)NCCCC[C@H](NC(=O)OC(C)(C)C)C(=O)NCC(c2ccccc2)c2ccccc2)cc1OC | 10.1021/acs.jmedchem.5b01965 | |||
CHEMBL3786459 | 139165 | None | 0 | Human | Functional | pEC50 | = | 7.3 | 7.3 | - | 1 | ChEMBL | 804 | 18 | 3 | 8 | 6.7 | COc1ccc(C(=O)CCC(=O)N2Cc3ccccc3C[C@H]2C(=O)NCCCC[C@H](NC(=O)OC(C)(C)C)C(=O)NCC(c2ccccc2)c2ccccc2)cc1OC | 10.1021/acs.jmedchem.5b01965 | |||
71462816 | 84618 | None | 0 | Human | Functional | pEC50 | = | 5.3 | 5.3 | - | 1 | ChEMBL | 414 | 5 | 0 | 0 | 7.2 | CC1(C)[C@H]2CC=C(C[N+](C)(C)Cc3ccc(-c4cc(Cl)ccc4Cl)cc3)[C@@H]1C2 | 10.1021/jm301240t | |||
CHEMBL2181459 | 84618 | None | 0 | Human | Functional | pEC50 | = | 5.3 | 5.3 | - | 1 | ChEMBL | 414 | 5 | 0 | 0 | 7.2 | CC1(C)[C@H]2CC=C(C[N+](C)(C)Cc3ccc(-c4cc(Cl)ccc4Cl)cc3)[C@@H]1C2 | 10.1021/jm301240t | |||
CHEMBL2220967 | 84618 | None | 0 | Human | Functional | pEC50 | = | 5.3 | 5.3 | - | 1 | ChEMBL | 414 | 5 | 0 | 0 | 7.2 | CC1(C)[C@H]2CC=C(C[N+](C)(C)Cc3ccc(-c4cc(Cl)ccc4Cl)cc3)[C@@H]1C2 | 10.1021/jm301240t | |||
127030991 | 139172 | None | 0 | Human | Functional | pEC50 | = | 6.3 | 6.3 | - | 1 | ChEMBL | 762 | 16 | 3 | 6 | 6.9 | CC(C)(C)OC(=O)N[C@@H](CCCCNC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCC(=O)c1ccc(F)cc1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.5b01965 | |||
CHEMBL3786522 | 139172 | None | 0 | Human | Functional | pEC50 | = | 6.3 | 6.3 | - | 1 | ChEMBL | 762 | 16 | 3 | 6 | 6.9 | CC(C)(C)OC(=O)N[C@@H](CCCCNC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCC(=O)c1ccc(F)cc1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.5b01965 | |||
71457439 | 83058 | None | 8 | Human | Functional | pEC50 | = | 6.2 | 6.2 | - | 1 | ChEMBL | 644 | 15 | 3 | 5 | 5.2 | NCCCC[C@H](NC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCC(=O)c1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.5b01965 | |||
CHEMBL2181467 | 83058 | None | 8 | Human | Functional | pEC50 | = | 6.2 | 6.2 | - | 1 | ChEMBL | 644 | 15 | 3 | 5 | 5.2 | NCCCC[C@H](NC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCC(=O)c1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.5b01965 | |||
CHEMBL3787171 | 83058 | None | 8 | Human | Functional | pEC50 | = | 6.2 | 6.2 | - | 1 | ChEMBL | 644 | 15 | 3 | 5 | 5.2 | NCCCC[C@H](NC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCC(=O)c1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.5b01965 | |||
127031312 | 139183 | None | 2 | Human | Functional | pEC50 | = | 5.2 | 5.2 | - | 1 | ChEMBL | 774 | 17 | 3 | 7 | 6.7 | COc1ccc(C(=O)CCC(=O)N2Cc3ccccc3C[C@H]2C(=O)NCCCC[C@H](NC(=O)OC(C)(C)C)C(=O)NCC(c2ccccc2)c2ccccc2)cc1 | 10.1021/acs.jmedchem.5b01965 | |||
CHEMBL3786577 | 139183 | None | 2 | Human | Functional | pEC50 | = | 5.2 | 5.2 | - | 1 | ChEMBL | 774 | 17 | 3 | 7 | 6.7 | COc1ccc(C(=O)CCC(=O)N2Cc3ccccc3C[C@H]2C(=O)NCCCC[C@H](NC(=O)OC(C)(C)C)C(=O)NCC(c2ccccc2)c2ccccc2)cc1 | 10.1021/acs.jmedchem.5b01965 | |||
71457439 | 83058 | None | 8 | Human | Functional | pEC50 | = | 6.2 | 6.2 | - | 1 | ChEMBL | 644 | 15 | 3 | 5 | 5.2 | NCCCC[C@H](NC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCC(=O)c1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/jm301240t | |||
CHEMBL2181467 | 83058 | None | 8 | Human | Functional | pEC50 | = | 6.2 | 6.2 | - | 1 | ChEMBL | 644 | 15 | 3 | 5 | 5.2 | NCCCC[C@H](NC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCC(=O)c1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/jm301240t | |||
CHEMBL3787171 | 83058 | None | 8 | Human | Functional | pEC50 | = | 6.2 | 6.2 | - | 1 | ChEMBL | 644 | 15 | 3 | 5 | 5.2 | NCCCC[C@H](NC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCC(=O)c1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/jm301240t | |||
71450266 | 84582 | None | 0 | Human | Functional | pEC50 | = | 6.2 | 6.2 | - | 1 | ChEMBL | 472 | 5 | 0 | 0 | 6.5 | CC1(C)[C@@H]2CC=C(C[N+](C)(C)Cc3ccc(-c4ccccc4I)cc3)[C@H]1C2 | 10.1021/jm301240t | |||
CHEMBL2181450 | 84582 | None | 0 | Human | Functional | pEC50 | = | 6.2 | 6.2 | - | 1 | ChEMBL | 472 | 5 | 0 | 0 | 6.5 | CC1(C)[C@@H]2CC=C(C[N+](C)(C)Cc3ccc(-c4ccccc4I)cc3)[C@H]1C2 | 10.1021/jm301240t | |||
CHEMBL2220492 | 84582 | None | 0 | Human | Functional | pEC50 | = | 6.2 | 6.2 | - | 1 | ChEMBL | 472 | 5 | 0 | 0 | 6.5 | CC1(C)[C@@H]2CC=C(C[N+](C)(C)Cc3ccc(-c4ccccc4I)cc3)[C@H]1C2 | 10.1021/jm301240t | |||
71455659 | 84588 | None | 0 | Human | Functional | pEC50 | = | 6.2 | 6.2 | - | 1 | ChEMBL | 414 | 5 | 0 | 0 | 7.2 | CC1(C)[C@H]2CC=C(C[N+](C)(C)Cc3ccc(-c4cccc(Cl)c4Cl)cc3)[C@@H]1C2 | 10.1021/jm301240t | |||
CHEMBL2181458 | 84588 | None | 0 | Human | Functional | pEC50 | = | 6.2 | 6.2 | - | 1 | ChEMBL | 414 | 5 | 0 | 0 | 7.2 | CC1(C)[C@H]2CC=C(C[N+](C)(C)Cc3ccc(-c4cccc(Cl)c4Cl)cc3)[C@@H]1C2 | 10.1021/jm301240t | |||
CHEMBL2220525 | 84588 | None | 0 | Human | Functional | pEC50 | = | 6.2 | 6.2 | - | 1 | ChEMBL | 414 | 5 | 0 | 0 | 7.2 | CC1(C)[C@H]2CC=C(C[N+](C)(C)Cc3ccc(-c4cccc(Cl)c4Cl)cc3)[C@@H]1C2 | 10.1021/jm301240t | |||
71457439 | 83058 | None | 8 | Human | Functional | pEC50 | = | 6.2 | 6.2 | - | 1 | ChEMBL | 644 | 15 | 3 | 5 | 5.2 | NCCCC[C@H](NC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCC(=O)c1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.5b01965 | |||
CHEMBL2181467 | 83058 | None | 8 | Human | Functional | pEC50 | = | 6.2 | 6.2 | - | 1 | ChEMBL | 644 | 15 | 3 | 5 | 5.2 | NCCCC[C@H](NC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCC(=O)c1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.5b01965 | |||
CHEMBL3787171 | 83058 | None | 8 | Human | Functional | pEC50 | = | 6.2 | 6.2 | - | 1 | ChEMBL | 644 | 15 | 3 | 5 | 5.2 | NCCCC[C@H](NC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCC(=O)c1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.5b01965 | |||
71459295 | 84570 | None | 1 | Human | Functional | pEC50 | = | 6.1 | 6.1 | - | 1 | ChEMBL | 424 | 5 | 0 | 0 | 6.7 | CC1(C)[C@H]2CC=C(C[N+](C)(C)Cc3ccc(-c4ccccc4Br)cc3)[C@@H]1C2 | 10.1021/jm301240t | |||
CHEMBL2181442 | 84570 | None | 1 | Human | Functional | pEC50 | = | 6.1 | 6.1 | - | 1 | ChEMBL | 424 | 5 | 0 | 0 | 6.7 | CC1(C)[C@H]2CC=C(C[N+](C)(C)Cc3ccc(-c4ccccc4Br)cc3)[C@@H]1C2 | 10.1021/jm301240t | |||
CHEMBL2220409 | 84570 | None | 1 | Human | Functional | pEC50 | = | 6.1 | 6.1 | - | 1 | ChEMBL | 424 | 5 | 0 | 0 | 6.7 | CC1(C)[C@H]2CC=C(C[N+](C)(C)Cc3ccc(-c4ccccc4Br)cc3)[C@@H]1C2 | 10.1021/jm301240t | |||
71459301 | 84577 | None | 0 | Human | Functional | pEC50 | = | 6.1 | 6.1 | - | 1 | ChEMBL | 414 | 5 | 0 | 0 | 7.2 | CC1(C)[C@H]2CC=C(C[N+](C)(C)Cc3ccc(-c4ccccc4Cl)c(Cl)c3)[C@@H]1C2 | 10.1021/jm301240t | |||
CHEMBL2181463 | 84577 | None | 0 | Human | Functional | pEC50 | = | 6.1 | 6.1 | - | 1 | ChEMBL | 414 | 5 | 0 | 0 | 7.2 | CC1(C)[C@H]2CC=C(C[N+](C)(C)Cc3ccc(-c4ccccc4Cl)c(Cl)c3)[C@@H]1C2 | 10.1021/jm301240t | |||
CHEMBL2220444 | 84577 | None | 0 | Human | Functional | pEC50 | = | 6.1 | 6.1 | - | 1 | ChEMBL | 414 | 5 | 0 | 0 | 7.2 | CC1(C)[C@H]2CC=C(C[N+](C)(C)Cc3ccc(-c4ccccc4Cl)c(Cl)c3)[C@@H]1C2 | 10.1021/jm301240t | |||
71450272 | 84579 | None | 0 | Human | Functional | pEC50 | = | 5.1 | 5.1 | - | 1 | ChEMBL | 374 | 5 | 0 | 0 | 6.5 | Cc1cccc(C)c1-c1ccc(C[N+](C)(C)CC2=CC[C@H]3C[C@@H]2C3(C)C)cc1 | 10.1021/jm301240t | |||
CHEMBL2181465 | 84579 | None | 0 | Human | Functional | pEC50 | = | 5.1 | 5.1 | - | 1 | ChEMBL | 374 | 5 | 0 | 0 | 6.5 | Cc1cccc(C)c1-c1ccc(C[N+](C)(C)CC2=CC[C@H]3C[C@@H]2C3(C)C)cc1 | 10.1021/jm301240t | |||
CHEMBL2220446 | 84579 | None | 0 | Human | Functional | pEC50 | = | 5.1 | 5.1 | - | 1 | ChEMBL | 374 | 5 | 0 | 0 | 6.5 | Cc1cccc(C)c1-c1ccc(C[N+](C)(C)CC2=CC[C@H]3C[C@@H]2C3(C)C)cc1 | 10.1021/jm301240t | |||
127032454 | 139087 | None | 0 | Human | Functional | pEC50 | = | 5.1 | 5.1 | - | 1 | ChEMBL | 730 | 16 | 3 | 5 | 7.1 | CC(C)(C)OC(=O)N[C@@H](CCCCNC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCCc1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.5b01965 | |||
CHEMBL3785564 | 139087 | None | 0 | Human | Functional | pEC50 | = | 5.1 | 5.1 | - | 1 | ChEMBL | 730 | 16 | 3 | 5 | 7.1 | CC(C)(C)OC(=O)N[C@@H](CCCCNC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCCc1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.5b01965 | |||
127032455 | 139274 | None | 0 | Human | Functional | pEC50 | = | 5.1 | 5.1 | - | 1 | ChEMBL | 716 | 15 | 3 | 5 | 6.7 | CC(C)(C)OC(=O)N[C@@H](CCCCNC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCc1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.5b01965 | |||
CHEMBL3787609 | 139274 | None | 0 | Human | Functional | pEC50 | = | 5.1 | 5.1 | - | 1 | ChEMBL | 716 | 15 | 3 | 5 | 6.7 | CC(C)(C)OC(=O)N[C@@H](CCCCNC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCc1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.5b01965 | |||
127031901 | 139300 | None | 0 | Human | Functional | pEC50 | = | 8.0 | 8.0 | - | 1 | ChEMBL | 644 | 15 | 3 | 5 | 5.2 | N[C@H](CCCCNC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCC(=O)c1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.5b01965 | |||
CHEMBL3787077 | 139300 | None | 0 | Human | Functional | pEC50 | = | 8.0 | 8.0 | - | 1 | ChEMBL | 644 | 15 | 3 | 5 | 5.2 | N[C@H](CCCCNC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCC(=O)c1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.5b01965 | |||
CHEMBL3787719 | 139300 | None | 0 | Human | Functional | pEC50 | = | 8.0 | 8.0 | - | 1 | ChEMBL | 644 | 15 | 3 | 5 | 5.2 | N[C@H](CCCCNC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCC(=O)c1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.5b01965 | |||
11569938 | 58238 | None | 0 | Human | Functional | pIC50 | = | 9.7 | 9.7 | 5 | 3 | ChEMBL | 521 | 7 | 1 | 5 | 4.8 | CCNC(=O)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4F)CC3)[C@@H](CC)C2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
CHEMBL1681882 | 58238 | None | 0 | Human | Functional | pIC50 | = | 9.7 | 9.7 | 5 | 3 | ChEMBL | 521 | 7 | 1 | 5 | 4.8 | CCNC(=O)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4F)CC3)[C@@H](CC)C2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
44592137 | 179284 | None | 5 | Human | Functional | pIC50 | = | 9.5 | 9.5 | -4 | 3 | ChEMBL | 503 | 7 | 1 | 5 | 4.7 | CCNC(=O)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4)CC3)[C@@H](CC)C2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
CHEMBL472288 | 179284 | None | 5 | Human | Functional | pIC50 | = | 9.5 | 9.5 | -4 | 3 | ChEMBL | 503 | 7 | 1 | 5 | 4.7 | CCNC(=O)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4)CC3)[C@@H](CC)C2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
45101529 | 5672 | None | 0 | Human | Functional | pIC50 | = | 9.4 | 9.4 | 1 | 5 | ChEMBL | 688 | 11 | 0 | 8 | 5.4 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc2ncccc2c(=O)n1-c1ccc(OCC(F)(F)F)cc1 | 10.1016/j.bmcl.2009.07.032 | |||
CHEMBL1077831 | 5672 | None | 0 | Human | Functional | pIC50 | = | 9.4 | 9.4 | 1 | 5 | ChEMBL | 688 | 11 | 0 | 8 | 5.4 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc2ncccc2c(=O)n1-c1ccc(OCC(F)(F)F)cc1 | 10.1016/j.bmcl.2009.07.032 | |||
44592137 | 179284 | None | 5 | Mouse | Functional | pIC50 | = | 9.3 | 9.3 | 2 | 3 | ChEMBL | 503 | 7 | 1 | 5 | 4.7 | CCNC(=O)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4)CC3)[C@@H](CC)C2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
CHEMBL472288 | 179284 | None | 5 | Mouse | Functional | pIC50 | = | 9.3 | 9.3 | 2 | 3 | ChEMBL | 503 | 7 | 1 | 5 | 4.7 | CCNC(=O)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4)CC3)[C@@H](CC)C2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
45101529 | 5672 | None | 0 | Human | Functional | pIC50 | = | 9.2 | 9.2 | 1 | 5 | ChEMBL | 688 | 11 | 0 | 8 | 5.4 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc2ncccc2c(=O)n1-c1ccc(OCC(F)(F)F)cc1 | 10.1016/j.bmcl.2009.07.032 | |||
CHEMBL1077831 | 5672 | None | 0 | Human | Functional | pIC50 | = | 9.2 | 9.2 | 1 | 5 | ChEMBL | 688 | 11 | 0 | 8 | 5.4 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc2ncccc2c(=O)n1-c1ccc(OCC(F)(F)F)cc1 | 10.1016/j.bmcl.2009.07.032 | |||
45101529 | 5672 | None | 0 | Human | Functional | pIC50 | = | 9.1 | 9.1 | 1 | 5 | ChEMBL | 688 | 11 | 0 | 8 | 5.4 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc2ncccc2c(=O)n1-c1ccc(OCC(F)(F)F)cc1 | 10.1016/j.bmcl.2009.07.032 | |||
CHEMBL1077831 | 5672 | None | 0 | Human | Functional | pIC50 | = | 9.1 | 9.1 | 1 | 5 | ChEMBL | 688 | 11 | 0 | 8 | 5.4 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc2ncccc2c(=O)n1-c1ccc(OCC(F)(F)F)cc1 | 10.1016/j.bmcl.2009.07.032 | |||
11569938 | 58238 | None | 0 | Mouse | Functional | pIC50 | = | 9.0 | 9.0 | -5 | 3 | ChEMBL | 521 | 7 | 1 | 5 | 4.8 | CCNC(=O)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4F)CC3)[C@@H](CC)C2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
CHEMBL1681882 | 58238 | None | 0 | Mouse | Functional | pIC50 | = | 9.0 | 9.0 | -5 | 3 | ChEMBL | 521 | 7 | 1 | 5 | 4.8 | CCNC(=O)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4F)CC3)[C@@H](CC)C2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
44592137 | 179284 | None | 5 | Rat | Functional | pIC50 | = | 8.9 | 8.9 | -2 | 3 | ChEMBL | 503 | 7 | 1 | 5 | 4.7 | CCNC(=O)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4)CC3)[C@@H](CC)C2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
CHEMBL472288 | 179284 | None | 5 | Rat | Functional | pIC50 | = | 8.9 | 8.9 | -2 | 3 | ChEMBL | 503 | 7 | 1 | 5 | 4.7 | CCNC(=O)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4)CC3)[C@@H](CC)C2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
89725838 | 145972 | None | 0 | Human | Functional | pIC50 | = | 8.8 | 8.8 | - | 1 | ChEMBL | 573 | 5 | 1 | 9 | 3.4 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccc(N4CCN(C)CC4)cc3[nH]2)CCN1C(=O)Cn1cccn1 | 10.1021/acs.jmedchem.2c00676 | |||
CHEMBL3917642 | 145972 | None | 0 | Human | Functional | pIC50 | = | 8.8 | 8.8 | - | 1 | ChEMBL | 573 | 5 | 1 | 9 | 3.4 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccc(N4CCN(C)CC4)cc3[nH]2)CCN1C(=O)Cn1cccn1 | 10.1021/acs.jmedchem.2c00676 | |||
71679146 | 153498 | None | 0 | Human | Functional | pIC50 | = | 8.8 | 8.8 | - | 1 | ChEMBL | 526 | 4 | 1 | 8 | 4.2 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | 10.1021/acs.jmedchem.2c00676 | |||
CHEMBL3978935 | 153498 | None | 0 | Human | Functional | pIC50 | = | 8.8 | 8.8 | - | 1 | ChEMBL | 526 | 4 | 1 | 8 | 4.2 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | 10.1021/acs.jmedchem.2c00676 | |||
11569938 | 58238 | None | 0 | Rat | Functional | pIC50 | = | 8.8 | 8.8 | -7 | 3 | ChEMBL | 521 | 7 | 1 | 5 | 4.8 | CCNC(=O)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4F)CC3)[C@@H](CC)C2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
CHEMBL1681882 | 58238 | None | 0 | Rat | Functional | pIC50 | = | 8.8 | 8.8 | -7 | 3 | ChEMBL | 521 | 7 | 1 | 5 | 4.8 | CCNC(=O)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4F)CC3)[C@@H](CC)C2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
71679146 | 153498 | None | 0 | Human | Functional | pIC50 | = | 8.8 | 8.8 | - | 1 | ChEMBL | 526 | 4 | 1 | 8 | 4.2 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL3978935 | 153498 | None | 0 | Human | Functional | pIC50 | = | 8.8 | 8.8 | - | 1 | ChEMBL | 526 | 4 | 1 | 8 | 4.2 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | 10.1021/acs.jmedchem.2c00675 | |||
168278609 | 191104 | None | 0 | Human | Functional | pIC50 | = | 8.8 | 8.8 | - | 1 | ChEMBL | 474 | 5 | 1 | 6 | 3.7 | O=C(Nc1ccccc1N1CCN(C(=O)Cn2cnc3cccnc32)CC1)c1cccc(Cl)c1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL5186472 | 191104 | None | 0 | Human | Functional | pIC50 | = | 8.8 | 8.8 | - | 1 | ChEMBL | 474 | 5 | 1 | 6 | 3.7 | O=C(Nc1ccccc1N1CCN(C(=O)Cn2cnc3cccnc32)CC1)c1cccc(Cl)c1 | 10.1021/acs.jmedchem.2c00675 | |||
117739261 | 146893 | None | 0 | Human | Functional | pIC50 | = | 8.8 | 8.8 | - | 1 | ChEMBL | 509 | 4 | 1 | 7 | 4.3 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cc(Cl)cn1 | 10.1021/acs.jmedchem.2c00676 | |||
CHEMBL3924716 | 146893 | None | 0 | Human | Functional | pIC50 | = | 8.8 | 8.8 | - | 1 | ChEMBL | 509 | 4 | 1 | 7 | 4.3 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cc(Cl)cn1 | 10.1021/acs.jmedchem.2c00676 | |||
12207 | 275 | None | 12 | Mouse | Functional | pIC50 | = | 8.8 | 8.8 | 7 | 2 | ChEMBL | 534 | 4 | 0 | 9 | 3.6 | C[C@@H]1CN(CCN1C(=O)Cn1nc(C)nc1C)c1c(c2cnc(C(F)(F)F)nc2)nc(C(F)(F)F)s1 | 10.1021/acs.jmedchem.2c00675 | |||
87056189 | 275 | None | 12 | Mouse | Functional | pIC50 | = | 8.8 | 8.8 | 7 | 2 | ChEMBL | 534 | 4 | 0 | 9 | 3.6 | C[C@@H]1CN(CCN1C(=O)Cn1nc(C)nc1C)c1c(c2cnc(C(F)(F)F)nc2)nc(C(F)(F)F)s1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL5202301 | 275 | None | 12 | Mouse | Functional | pIC50 | = | 8.8 | 8.8 | 7 | 2 | ChEMBL | 534 | 4 | 0 | 9 | 3.6 | C[C@@H]1CN(CCN1C(=O)Cn1nc(C)nc1C)c1c(c2cnc(C(F)(F)F)nc2)nc(C(F)(F)F)s1 | 10.1021/acs.jmedchem.2c00675 | |||
89725785 | 143189 | None | 0 | Human | Functional | pIC50 | = | 8.7 | 8.7 | - | 1 | ChEMBL | 486 | 5 | 1 | 8 | 3.7 | CCc1nc(-c2nc3ccccc3[nH]2)c(N2CCN(C(=O)Cn3cnc4cccnc43)[C@H](C)C2)s1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL3895485 | 143189 | None | 0 | Human | Functional | pIC50 | = | 8.7 | 8.7 | - | 1 | ChEMBL | 486 | 5 | 1 | 8 | 3.7 | CCc1nc(-c2nc3ccccc3[nH]2)c(N2CCN(C(=O)Cn3cnc4cccnc43)[C@H](C)C2)s1 | 10.1021/acs.jmedchem.2c00675 | |||
46883304 | 5665 | None | 0 | Human | Functional | pIC50 | = | 8 | 8.0 | - | 1 | ChEMBL | 639 | 10 | 0 | 7 | 6.3 | CCOc1ccc(-n2c([C@@H](C)N(C[C@H]3CCCN3C(C)C)C(=O)Cc3ccc(F)c(C(F)(F)F)c3)nc3ncccc3c2=O)cc1 | 10.1016/j.bmcl.2009.07.032 | |||
CHEMBL1077824 | 5665 | None | 0 | Human | Functional | pIC50 | = | 8 | 8.0 | - | 1 | ChEMBL | 639 | 10 | 0 | 7 | 6.3 | CCOc1ccc(-n2c([C@@H](C)N(C[C@H]3CCCN3C(C)C)C(=O)Cc3ccc(F)c(C(F)(F)F)c3)nc3ncccc3c2=O)cc1 | 10.1016/j.bmcl.2009.07.032 | |||
44453468 | 155176 | None | 0 | Human | Functional | pIC50 | = | 8 | 8.0 | 77 | 2 | ChEMBL | 571 | 9 | 1 | 6 | 6.4 | N=c1n(CC(=O)c2ccc(Cl)cc2)c2cccc(Cl)c2n1CCCN(C(=O)c1cccc2cccnc12)C1CC1 | 10.1016/j.bmcl.2008.02.049 | |||
CHEMBL401868 | 155176 | None | 0 | Human | Functional | pIC50 | = | 8 | 8.0 | 77 | 2 | ChEMBL | 571 | 9 | 1 | 6 | 6.4 | N=c1n(CC(=O)c2ccc(Cl)cc2)c2cccc(Cl)c2n1CCCN(C(=O)c1cccc2cccnc12)C1CC1 | 10.1016/j.bmcl.2008.02.049 | |||
56670465 | 64245 | None | 0 | Human | Functional | pIC50 | = | 8 | 8.0 | -1 | 2 | ChEMBL | 400 | 2 | 2 | 2 | 3.7 | CN(C)C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1808996 | 64245 | None | 0 | Human | Functional | pIC50 | = | 8 | 8.0 | -1 | 2 | ChEMBL | 400 | 2 | 2 | 2 | 3.7 | CN(C)C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1 | 10.1016/j.bmcl.2011.06.070 | |||
168287429 | 191592 | None | 0 | Human | Functional | pIC50 | = | 8 | 8.0 | - | 1 | ChEMBL | 582 | 5 | 1 | 10 | 3.1 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccc(S(C)(=O)=O)cc4[nH]3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00676 | |||
CHEMBL5193530 | 191592 | None | 0 | Human | Functional | pIC50 | = | 8 | 8.0 | - | 1 | ChEMBL | 582 | 5 | 1 | 10 | 3.1 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccc(S(C)(=O)=O)cc4[nH]3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00676 | |||
56670465 | 64245 | None | 0 | Mouse | Functional | pIC50 | = | 8 | 8.0 | 1 | 2 | ChEMBL | 400 | 2 | 2 | 2 | 3.7 | CN(C)C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1808996 | 64245 | None | 0 | Mouse | Functional | pIC50 | = | 8 | 8.0 | 1 | 2 | ChEMBL | 400 | 2 | 2 | 2 | 3.7 | CN(C)C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1 | 10.1016/j.bmcl.2011.06.070 | |||
56677273 | 64273 | None | 0 | Mouse | Functional | pIC50 | = | 8 | 8.0 | 1 | 2 | ChEMBL | 432 | 2 | 2 | 3 | 4.3 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2cccs2)C1)N1CCCC1 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1809025 | 64273 | None | 0 | Mouse | Functional | pIC50 | = | 8 | 8.0 | 1 | 2 | ChEMBL | 432 | 2 | 2 | 3 | 4.3 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2cccs2)C1)N1CCCC1 | 10.1016/j.bmcl.2011.06.070 | |||
44453232 | 95453 | None | 0 | Human | Functional | pIC50 | = | 7 | 7.0 | 12 | 2 | ChEMBL | 502 | 10 | 1 | 5 | 5.1 | CCc1cccc2c1n(CCCN(C)C(=O)Cc1ccccc1)c(=N)n2CC(=O)c1ccc(Cl)cc1 | 10.1016/j.bmcl.2008.02.049 | |||
CHEMBL256891 | 95453 | None | 0 | Human | Functional | pIC50 | = | 7 | 7.0 | 12 | 2 | ChEMBL | 502 | 10 | 1 | 5 | 5.1 | CCc1cccc2c1n(CCCN(C)C(=O)Cc1ccccc1)c(=N)n2CC(=O)c1ccc(Cl)cc1 | 10.1016/j.bmcl.2008.02.049 | |||
45482807 | 200615 | None | 0 | Human | Functional | pIC50 | = | 7 | 7.0 | - | 1 | ChEMBL | 442 | 4 | 2 | 2 | 4.8 | CCN(CC)C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccc(C)cc2)C1 | 10.1016/j.bmcl.2009.09.002 | |||
CHEMBL574831 | 200615 | None | 0 | Human | Functional | pIC50 | = | 7 | 7.0 | - | 1 | ChEMBL | 442 | 4 | 2 | 2 | 4.8 | CCN(CC)C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccc(C)cc2)C1 | 10.1016/j.bmcl.2009.09.002 | |||
45486493 | 200879 | None | 0 | Human | Functional | pIC50 | = | 7 | 7.0 | - | 1 | ChEMBL | 601 | 9 | 0 | 7 | 5.3 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc2nc(C)ccn2c1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2009.07.021 | |||
CHEMBL577108 | 200879 | None | 0 | Human | Functional | pIC50 | = | 7 | 7.0 | - | 1 | ChEMBL | 601 | 9 | 0 | 7 | 5.3 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc2nc(C)ccn2c1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2009.07.021 | |||
11296495 | 72755 | None | 22 | Human | Functional | pIC50 | = | 7 | 7.0 | - | 1 | ChEMBL | 615 | 8 | 3 | 4 | 6.1 | CCNC(=O)N1CCCN(c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2NC(=O)c2cccc(Cl)c2)CC1 | 10.1016/j.bmcl.2005.09.020 | |||
CHEMBL199839 | 72755 | None | 22 | Human | Functional | pIC50 | = | 7 | 7.0 | - | 1 | ChEMBL | 615 | 8 | 3 | 4 | 6.1 | CCNC(=O)N1CCCN(c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2NC(=O)c2cccc(Cl)c2)CC1 | 10.1016/j.bmcl.2005.09.020 | |||
44581090 | 188027 | None | 0 | Human | Functional | pIC50 | = | 6 | 6.0 | - | 1 | ChEMBL | 441 | 4 | 1 | 4 | 3.4 | O=C1CCC(c2cccnc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C(=O)N1 | 10.1016/j.bmcl.2008.07.115 | |||
CHEMBL496771 | 188027 | None | 0 | Human | Functional | pIC50 | = | 6 | 6.0 | - | 1 | ChEMBL | 441 | 4 | 1 | 4 | 3.4 | O=C1CCC(c2cccnc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C(=O)N1 | 10.1016/j.bmcl.2008.07.115 | |||
44580799 | 188211 | None | 0 | Human | Functional | pIC50 | = | 6 | 6.0 | - | 1 | ChEMBL | 456 | 4 | 2 | 4 | 3.7 | O=C1CCC(c2cccc(O)c2)(C2CCN(Cc3ccc(Br)cc3)CC2)C(=O)N1 | 10.1016/j.bmcl.2008.07.115 | |||
CHEMBL498199 | 188211 | None | 0 | Human | Functional | pIC50 | = | 6 | 6.0 | - | 1 | ChEMBL | 456 | 4 | 2 | 4 | 3.7 | O=C1CCC(c2cccc(O)c2)(C2CCN(Cc3ccc(Br)cc3)CC2)C(=O)N1 | 10.1016/j.bmcl.2008.07.115 | |||
44580878 | 188262 | None | 0 | Human | Functional | pIC50 | = | 6 | 6.0 | - | 1 | ChEMBL | 500 | 6 | 0 | 4 | 5.1 | CSCN1C(=O)CCC(c2ccccc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C1=O | 10.1016/j.bmcl.2008.07.115 | |||
CHEMBL498555 | 188262 | None | 0 | Human | Functional | pIC50 | = | 6 | 6.0 | - | 1 | ChEMBL | 500 | 6 | 0 | 4 | 5.1 | CSCN1C(=O)CCC(c2ccccc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C1=O | 10.1016/j.bmcl.2008.07.115 | |||
44570312 | 177715 | None | 0 | Mouse | Functional | pIC50 | = | 6 | 6.0 | -7 | 2 | ChEMBL | 460 | 4 | 0 | 6 | 2.7 | C[C@H]1CN(S(=O)(=O)C[C@]23CC[C@H](CC2=O)C3(C)C)CCN1c1ncc(C(F)(F)F)cn1 | 10.1016/j.bmcl.2008.11.008 | |||
CHEMBL464083 | 177715 | None | 0 | Mouse | Functional | pIC50 | = | 6 | 6.0 | -7 | 2 | ChEMBL | 460 | 4 | 0 | 6 | 2.7 | C[C@H]1CN(S(=O)(=O)C[C@]23CC[C@H](CC2=O)C3(C)C)CCN1c1ncc(C(F)(F)F)cn1 | 10.1016/j.bmcl.2008.11.008 | |||
56670455 | 64279 | None | 0 | Human | Functional | pIC50 | = | 5 | 5.0 | - | 1 | ChEMBL | 430 | 3 | 2 | 3 | 3.5 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)NCc2ccco2)C1)N1CCCC1 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1809034 | 64279 | None | 0 | Human | Functional | pIC50 | = | 5 | 5.0 | - | 1 | ChEMBL | 430 | 3 | 2 | 3 | 3.5 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)NCc2ccco2)C1)N1CCCC1 | 10.1016/j.bmcl.2011.06.070 | |||
57400629 | 69990 | None | 0 | Human | Functional | pIC50 | = | 7.0 | 7.0 | - | 1 | ChEMBL | 624 | 9 | 0 | 7 | 5.2 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc2ncccc2c(=O)n1-c1ccc(Cl)cc1 | 10.1016/j.bmcl.2011.10.120 | |||
CHEMBL1939557 | 69990 | None | 0 | Human | Functional | pIC50 | = | 7.0 | 7.0 | - | 1 | ChEMBL | 624 | 9 | 0 | 7 | 5.2 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc2ncccc2c(=O)n1-c1ccc(Cl)cc1 | 10.1016/j.bmcl.2011.10.120 | |||
168283702 | 190875 | None | 0 | Human | Functional | pIC50 | = | 6.0 | 6.0 | - | 1 | ChEMBL | 522 | 4 | 0 | 9 | 3.9 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3cnc(C(C)(C)C)nc3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL5183171 | 190875 | None | 0 | Human | Functional | pIC50 | = | 6.0 | 6.0 | - | 1 | ChEMBL | 522 | 4 | 0 | 9 | 3.9 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3cnc(C(C)(C)C)nc3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00675 | |||
168287733 | 191912 | None | 0 | Human | Functional | pIC50 | = | 7.0 | 7.0 | - | 1 | ChEMBL | 517 | 5 | 0 | 9 | 3.7 | COc1ccc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3cnc4cccnc43)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL5198351 | 191912 | None | 0 | Human | Functional | pIC50 | = | 7.0 | 7.0 | - | 1 | ChEMBL | 517 | 5 | 0 | 9 | 3.7 | COc1ccc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3cnc4cccnc43)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
89726154 | 152067 | None | 0 | Human | Functional | pIC50 | = | 6.0 | 6.0 | - | 1 | ChEMBL | 472 | 4 | 1 | 8 | 3.5 | Cc1nc(-c2nc3ccccc3[nH]2)c(N2CCN(C(=O)Cn3cnc4cccnc43)[C@H](C)C2)s1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL3966706 | 152067 | None | 0 | Human | Functional | pIC50 | = | 6.0 | 6.0 | - | 1 | ChEMBL | 472 | 4 | 1 | 8 | 3.5 | Cc1nc(-c2nc3ccccc3[nH]2)c(N2CCN(C(=O)Cn3cnc4cccnc43)[C@H](C)C2)s1 | 10.1021/acs.jmedchem.2c00675 | |||
57393685 | 69991 | None | 0 | Human | Functional | pIC50 | = | 7.0 | 7.0 | - | 1 | ChEMBL | 624 | 9 | 0 | 7 | 5.2 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(C(F)(F)F)c(F)c1)[C@H](C)c1nc2ncccc2c(=O)n1-c1ccc(Cl)cc1 | 10.1016/j.bmcl.2011.10.120 | |||
CHEMBL1939558 | 69991 | None | 0 | Human | Functional | pIC50 | = | 7.0 | 7.0 | - | 1 | ChEMBL | 624 | 9 | 0 | 7 | 5.2 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(C(F)(F)F)c(F)c1)[C@H](C)c1nc2ncccc2c(=O)n1-c1ccc(Cl)cc1 | 10.1016/j.bmcl.2011.10.120 | |||
46891329 | 6832 | None | 0 | Human | Functional | pIC50 | = | 6.0 | 6.0 | - | 1 | ChEMBL | 425 | 7 | 1 | 5 | 3.2 | N#Cc1ccc(S(=O)(=O)N(Cc2ccc(C(=O)O)c(F)c2)Cc2ccccn2)cc1 | 10.1016/j.bmcl.2010.04.113 | |||
CHEMBL1083956 | 6832 | None | 0 | Human | Functional | pIC50 | = | 6.0 | 6.0 | - | 1 | ChEMBL | 425 | 7 | 1 | 5 | 3.2 | N#Cc1ccc(S(=O)(=O)N(Cc2ccc(C(=O)O)c(F)c2)Cc2ccccn2)cc1 | 10.1016/j.bmcl.2010.04.113 | |||
56673942 | 64275 | None | 0 | Human | Functional | pIC50 | = | 8.0 | 8.0 | 1 | 2 | ChEMBL | 432 | 2 | 2 | 2 | 4.1 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)NC2CCCCC2)C1)N1CCCC1 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1809028 | 64275 | None | 0 | Human | Functional | pIC50 | = | 8.0 | 8.0 | 1 | 2 | ChEMBL | 432 | 2 | 2 | 2 | 4.1 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)NC2CCCCC2)C1)N1CCCC1 | 10.1016/j.bmcl.2011.06.070 | |||
56673940 | 64272 | None | 0 | Mouse | Functional | pIC50 | = | 8.0 | 8.0 | 1 | 2 | ChEMBL | 432 | 2 | 2 | 3 | 4.3 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccsc2)C1)N1CCCC1 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1809024 | 64272 | None | 0 | Mouse | Functional | pIC50 | = | 8.0 | 8.0 | 1 | 2 | ChEMBL | 432 | 2 | 2 | 3 | 4.3 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccsc2)C1)N1CCCC1 | 10.1016/j.bmcl.2011.06.070 | |||
53322459 | 58192 | None | 0 | Human | Functional | pIC50 | = | 7.0 | 7.0 | - | 1 | ChEMBL | 489 | 5 | 1 | 5 | 4.5 | CNC(=O)c1cnc(N2CCN(C3CCN(C(C)c4ccc(Cl)cc4)CC3)[C@@H](C)C2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
CHEMBL1681832 | 58192 | None | 0 | Human | Functional | pIC50 | = | 7.0 | 7.0 | - | 1 | ChEMBL | 489 | 5 | 1 | 5 | 4.5 | CNC(=O)c1cnc(N2CCN(C3CCN(C(C)c4ccc(Cl)cc4)CC3)[C@@H](C)C2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
24739387 | 188263 | None | 0 | Human | Functional | pIC50 | = | 7.0 | 7.0 | 9 | 4 | ChEMBL | 454 | 4 | 0 | 2 | 5.2 | CC(=O)N1CCCC(c2ccccc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C1 | 10.1016/j.bmcl.2008.07.115 | |||
CHEMBL498556 | 188263 | None | 0 | Human | Functional | pIC50 | = | 7.0 | 7.0 | 9 | 4 | ChEMBL | 454 | 4 | 0 | 2 | 5.2 | CC(=O)N1CCCC(c2ccccc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C1 | 10.1016/j.bmcl.2008.07.115 | |||
89726171 | 143715 | None | 0 | Human | Functional | pIC50 | = | 7.0 | 7.0 | - | 1 | ChEMBL | 489 | 4 | 0 | 8 | 3.6 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3n2C)CCN1C(=O)Cn1cccn1 | 10.1021/acs.jmedchem.2c00676 | |||
CHEMBL3899775 | 143715 | None | 0 | Human | Functional | pIC50 | = | 7.0 | 7.0 | - | 1 | ChEMBL | 489 | 4 | 0 | 8 | 3.6 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3n2C)CCN1C(=O)Cn1cccn1 | 10.1021/acs.jmedchem.2c00676 | |||
56673938 | 64255 | None | 0 | Mouse | Functional | pIC50 | = | 7.0 | 7.0 | -1 | 2 | ChEMBL | 455 | 2 | 2 | 3 | 3.4 | CN1CCN(C(=O)[C@@H]2C=C3c4cccc5[nH]cc(c45)C[C@H]3N(C(=O)Nc3ccccc3)C2)CC1 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1809006 | 64255 | None | 0 | Mouse | Functional | pIC50 | = | 7.0 | 7.0 | -1 | 2 | ChEMBL | 455 | 2 | 2 | 3 | 3.4 | CN1CCN(C(=O)[C@@H]2C=C3c4cccc5[nH]cc(c45)C[C@H]3N(C(=O)Nc3ccccc3)C2)CC1 | 10.1016/j.bmcl.2011.06.070 | |||
46891327 | 6830 | None | 0 | Human | Functional | pIC50 | = | 6.0 | 6.0 | - | 1 | ChEMBL | 434 | 7 | 1 | 4 | 4.0 | O=C(O)c1ccc(CN(Cc2ccccn2)S(=O)(=O)c2ccc(Cl)cc2)cc1F | 10.1016/j.bmcl.2010.04.113 | |||
CHEMBL1083954 | 6830 | None | 0 | Human | Functional | pIC50 | = | 6.0 | 6.0 | - | 1 | ChEMBL | 434 | 7 | 1 | 4 | 4.0 | O=C(O)c1ccc(CN(Cc2ccccn2)S(=O)(=O)c2ccc(Cl)cc2)cc1F | 10.1016/j.bmcl.2010.04.113 | |||
89726281 | 148856 | None | 0 | Human | Functional | pIC50 | = | 6.0 | 6.0 | - | 1 | ChEMBL | 571 | 5 | 1 | 11 | 3.2 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccc(-n5cncn5)cc4[nH]3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00676 | |||
CHEMBL3940550 | 148856 | None | 0 | Human | Functional | pIC50 | = | 6.0 | 6.0 | - | 1 | ChEMBL | 571 | 5 | 1 | 11 | 3.2 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccc(-n5cncn5)cc4[nH]3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00676 | |||
16040696 | 94850 | None | 1 | Human | Functional | pIC50 | = | 6.9 | 6.9 | - | 1 | ChEMBL | 615 | 9 | 0 | 8 | 4.4 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc2ncccc2c(=O)n1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2009.07.032 | |||
CHEMBL253431 | 94850 | None | 1 | Human | Functional | pIC50 | = | 6.9 | 6.9 | - | 1 | ChEMBL | 615 | 9 | 0 | 8 | 4.4 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc2ncccc2c(=O)n1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2009.07.032 | |||
16040696 | 94850 | None | 1 | Human | Functional | pIC50 | = | 6.9 | 6.9 | - | 1 | ChEMBL | 615 | 9 | 0 | 8 | 4.4 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc2ncccc2c(=O)n1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2007.11.060 | |||
CHEMBL253431 | 94850 | None | 1 | Human | Functional | pIC50 | = | 6.9 | 6.9 | - | 1 | ChEMBL | 615 | 9 | 0 | 8 | 4.4 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc2ncccc2c(=O)n1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2007.11.060 | |||
16040696 | 94850 | None | 1 | Human | Functional | pIC50 | = | 6.9 | 6.9 | - | 1 | ChEMBL | 615 | 9 | 0 | 8 | 4.4 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc2ncccc2c(=O)n1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2009.07.021 | |||
CHEMBL253431 | 94850 | None | 1 | Human | Functional | pIC50 | = | 6.9 | 6.9 | - | 1 | ChEMBL | 615 | 9 | 0 | 8 | 4.4 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc2ncccc2c(=O)n1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2009.07.021 | |||
46891223 | 7276 | None | 0 | Human | Functional | pIC50 | = | 5.9 | 5.9 | - | 1 | ChEMBL | 465 | 10 | 1 | 5 | 3.6 | COc1ccc(S(=O)(=O)N(Cc2ccc(C(=O)NCC3CC3)cc2)Cc2cccnc2)cc1 | 10.1016/j.bmcl.2010.04.113 | |||
CHEMBL1085998 | 7276 | None | 0 | Human | Functional | pIC50 | = | 5.9 | 5.9 | - | 1 | ChEMBL | 465 | 10 | 1 | 5 | 3.6 | COc1ccc(S(=O)(=O)N(Cc2ccc(C(=O)NCC3CC3)cc2)Cc2cccnc2)cc1 | 10.1016/j.bmcl.2010.04.113 | |||
90480414 | 190778 | None | 0 | Human | Functional | pIC50 | = | 5.9 | 5.9 | - | 1 | ChEMBL | 495 | 5 | 0 | 9 | 3.2 | COc1ccc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3nc(C)nc3C)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL5181702 | 190778 | None | 0 | Human | Functional | pIC50 | = | 5.9 | 5.9 | - | 1 | ChEMBL | 495 | 5 | 0 | 9 | 3.2 | COc1ccc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3nc(C)nc3C)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
168287236 | 191835 | None | 0 | Human | Functional | pIC50 | = | 6.9 | 6.9 | - | 1 | ChEMBL | 550 | 6 | 0 | 10 | 3.4 | CCOc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3cnc(C(F)(F)F)n3)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL5197175 | 191835 | None | 0 | Human | Functional | pIC50 | = | 6.9 | 6.9 | - | 1 | ChEMBL | 550 | 6 | 0 | 10 | 3.4 | CCOc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3cnc(C(F)(F)F)n3)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
56660099 | 64247 | None | 0 | Human | Functional | pIC50 | = | 7.9 | 7.9 | -3 | 2 | ChEMBL | 430 | 4 | 3 | 3 | 3.1 | CN(CCO)C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1808998 | 64247 | None | 0 | Human | Functional | pIC50 | = | 7.9 | 7.9 | -3 | 2 | ChEMBL | 430 | 4 | 3 | 3 | 3.1 | CN(CCO)C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1 | 10.1016/j.bmcl.2011.06.070 | |||
56670449 | 64263 | None | 0 | Human | Functional | pIC50 | = | 7.9 | 7.9 | -1 | 2 | ChEMBL | 442 | 2 | 3 | 3 | 3.2 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CC[C@H](O)C1 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1809014 | 64263 | None | 0 | Human | Functional | pIC50 | = | 7.9 | 7.9 | -1 | 2 | ChEMBL | 442 | 2 | 3 | 3 | 3.2 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CC[C@H](O)C1 | 10.1016/j.bmcl.2011.06.070 | |||
56660101 | 64257 | None | 0 | Mouse | Functional | pIC50 | = | 7.9 | 7.9 | 1 | 3 | ChEMBL | 442 | 2 | 2 | 3 | 3.5 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CCOCC1 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1809008 | 64257 | None | 0 | Mouse | Functional | pIC50 | = | 7.9 | 7.9 | 1 | 3 | ChEMBL | 442 | 2 | 2 | 3 | 3.5 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CCOCC1 | 10.1016/j.bmcl.2011.06.070 | |||
45486525 | 201009 | None | 0 | Human | Functional | pIC50 | = | 7.9 | 7.9 | - | 1 | ChEMBL | 615 | 10 | 0 | 7 | 5.6 | CCc1nccn2c(-c3ccc(C#N)cc3)c([C@@H](C)N(CCS(=O)(=O)CC)C(=O)Cc3ccc(C(F)(F)F)c(F)c3)nc12 | 10.1016/j.bmcl.2009.07.021 | |||
CHEMBL578189 | 201009 | None | 0 | Human | Functional | pIC50 | = | 7.9 | 7.9 | - | 1 | ChEMBL | 615 | 10 | 0 | 7 | 5.6 | CCc1nccn2c(-c3ccc(C#N)cc3)c([C@@H](C)N(CCS(=O)(=O)CC)C(=O)Cc3ccc(C(F)(F)F)c(F)c3)nc12 | 10.1016/j.bmcl.2009.07.021 | |||
44593651 | 187843 | None | 0 | Human | Functional | pIC50 | = | 6.9 | 6.9 | - | 1 | ChEMBL | 476 | 4 | 1 | 3 | 4.3 | O=C1CCC(c2ccc(F)cc2F)(C2CCN(Cc3ccc(Br)cc3)CC2)C(=O)N1 | 10.1016/j.bmcl.2008.07.115 | |||
CHEMBL495531 | 187843 | None | 0 | Human | Functional | pIC50 | = | 6.9 | 6.9 | - | 1 | ChEMBL | 476 | 4 | 1 | 3 | 4.3 | O=C1CCC(c2ccc(F)cc2F)(C2CCN(Cc3ccc(Br)cc3)CC2)C(=O)N1 | 10.1016/j.bmcl.2008.07.115 | |||
15604606 | 140659 | None | 0 | Human | Functional | pIC50 | = | 6.9 | 6.9 | - | 1 | ChEMBL | 581 | 8 | 3 | 4 | 5.5 | CCNC(=O)N1CCCN(c2ccc(C(=O)NCCc3ccc(Cl)cc3)cc2NC(=O)c2cccc(Cl)c2)CC1 | 10.1016/j.bmcl.2005.09.020 | |||
CHEMBL381227 | 140659 | None | 0 | Human | Functional | pIC50 | = | 6.9 | 6.9 | - | 1 | ChEMBL | 581 | 8 | 3 | 4 | 5.5 | CCNC(=O)N1CCCN(c2ccc(C(=O)NCCc3ccc(Cl)cc3)cc2NC(=O)c2cccc(Cl)c2)CC1 | 10.1016/j.bmcl.2005.09.020 | |||
89725838 | 145972 | None | 0 | Human | Functional | pIC50 | = | 6.9 | 6.9 | - | 1 | ChEMBL | 573 | 5 | 1 | 9 | 3.4 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccc(N4CCN(C)CC4)cc3[nH]2)CCN1C(=O)Cn1cccn1 | 10.1021/acs.jmedchem.2c00676 | |||
CHEMBL3917642 | 145972 | None | 0 | Human | Functional | pIC50 | = | 6.9 | 6.9 | - | 1 | ChEMBL | 573 | 5 | 1 | 9 | 3.4 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccc(N4CCN(C)CC4)cc3[nH]2)CCN1C(=O)Cn1cccn1 | 10.1021/acs.jmedchem.2c00676 | |||
117740233 | 153750 | None | 0 | Human | Functional | pIC50 | = | 6.9 | 6.9 | - | 1 | ChEMBL | 588 | 5 | 1 | 9 | 4.5 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccc(C5CCOCC5)cc4[nH]3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00676 | |||
CHEMBL3981151 | 153750 | None | 0 | Human | Functional | pIC50 | = | 6.9 | 6.9 | - | 1 | ChEMBL | 588 | 5 | 1 | 9 | 4.5 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccc(C5CCOCC5)cc4[nH]3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00676 | |||
44570312 | 177715 | None | 0 | Human | Functional | pIC50 | = | 6.9 | 6.9 | 7 | 2 | ChEMBL | 460 | 4 | 0 | 6 | 2.7 | C[C@H]1CN(S(=O)(=O)C[C@]23CC[C@H](CC2=O)C3(C)C)CCN1c1ncc(C(F)(F)F)cn1 | 10.1016/j.bmcl.2008.11.008 | |||
CHEMBL464083 | 177715 | None | 0 | Human | Functional | pIC50 | = | 6.9 | 6.9 | 7 | 2 | ChEMBL | 460 | 4 | 0 | 6 | 2.7 | C[C@H]1CN(S(=O)(=O)C[C@]23CC[C@H](CC2=O)C3(C)C)CCN1c1ncc(C(F)(F)F)cn1 | 10.1016/j.bmcl.2008.11.008 | |||
15604608 | 72641 | None | 0 | Human | Functional | pIC50 | = | 5.9 | 5.9 | - | 1 | ChEMBL | 533 | 7 | 3 | 4 | 4.8 | CCNC(=O)N1CCCN(c2ccc(C(=O)NCc3ccccc3)cc2NC(=O)c2cccc(Cl)c2)CC1 | 10.1016/j.bmcl.2005.09.020 | |||
CHEMBL199408 | 72641 | None | 0 | Human | Functional | pIC50 | = | 5.9 | 5.9 | - | 1 | ChEMBL | 533 | 7 | 3 | 4 | 4.8 | CCNC(=O)N1CCCN(c2ccc(C(=O)NCc3ccccc3)cc2NC(=O)c2cccc(Cl)c2)CC1 | 10.1016/j.bmcl.2005.09.020 | |||
53325132 | 58216 | None | 0 | Human | Functional | pIC50 | = | 4.9 | 4.9 | - | 1 | ChEMBL | 475 | 5 | 1 | 5 | 3.9 | CNC(=O)c1cnc(N2CCC(N3CCN(Cc4ccc(Cl)cc4)C[C@@H]3C)CC2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
CHEMBL1681859 | 58216 | None | 0 | Human | Functional | pIC50 | = | 4.9 | 4.9 | - | 1 | ChEMBL | 475 | 5 | 1 | 5 | 3.9 | CNC(=O)c1cnc(N2CCC(N3CCN(Cc4ccc(Cl)cc4)C[C@@H]3C)CC2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
27307547 | 177710 | None | 0 | Mouse | Functional | pIC50 | = | 5.9 | 5.9 | -5 | 2 | ChEMBL | 445 | 4 | 0 | 5 | 2.9 | CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCN(c3ccc(C(F)(F)F)cn3)CC1)C(=O)C2 | 10.1016/j.bmcl.2008.11.008 | |||
CHEMBL464081 | 177710 | None | 0 | Mouse | Functional | pIC50 | = | 5.9 | 5.9 | -5 | 2 | ChEMBL | 445 | 4 | 0 | 5 | 2.9 | CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCN(c3ccc(C(F)(F)F)cn3)CC1)C(=O)C2 | 10.1016/j.bmcl.2008.11.008 | |||
89726625 | 152560 | None | 0 | Human | Functional | pIC50 | = | 6.9 | 6.9 | - | 1 | ChEMBL | 536 | 4 | 1 | 8 | 3.9 | C[C@@H]1CN(c2sc(Br)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL3971056 | 152560 | None | 0 | Human | Functional | pIC50 | = | 6.9 | 6.9 | - | 1 | ChEMBL | 536 | 4 | 1 | 8 | 3.9 | C[C@@H]1CN(c2sc(Br)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | 10.1021/acs.jmedchem.2c00675 | |||
44581087 | 188197 | None | 0 | Human | Functional | pIC50 | = | 5.9 | 5.9 | - | 1 | ChEMBL | 430 | 4 | 1 | 3 | 4.6 | O=C1CCC(c2ccccc2)(C2CCN(Cc3ccc(Cl)c(Cl)c3)CC2)C(=O)N1 | 10.1016/j.bmcl.2008.07.115 | |||
CHEMBL498012 | 188197 | None | 0 | Human | Functional | pIC50 | = | 5.9 | 5.9 | - | 1 | ChEMBL | 430 | 4 | 1 | 3 | 4.6 | O=C1CCC(c2ccccc2)(C2CCN(Cc3ccc(Cl)c(Cl)c3)CC2)C(=O)N1 | 10.1016/j.bmcl.2008.07.115 | |||
44580797 | 188210 | None | 0 | Human | Functional | pIC50 | = | 5.9 | 5.9 | - | 1 | ChEMBL | 581 | 6 | 2 | 6 | 2.9 | CN(C(=O)c1cccc(C2(C3CCN(Cc4ccc(Br)cc4)CC3)CCC(=O)NC2=O)c1)N1CCNCC1 | 10.1016/j.bmcl.2008.07.115 | |||
CHEMBL498198 | 188210 | None | 0 | Human | Functional | pIC50 | = | 5.9 | 5.9 | - | 1 | ChEMBL | 581 | 6 | 2 | 6 | 2.9 | CN(C(=O)c1cccc(C2(C3CCN(Cc4ccc(Br)cc4)CC3)CCC(=O)NC2=O)c1)N1CCNCC1 | 10.1016/j.bmcl.2008.07.115 | |||
44581162 | 189648 | None | 0 | Human | Functional | pIC50 | = | 5.9 | 5.9 | - | 1 | ChEMBL | 541 | 8 | 3 | 5 | 3.1 | O=C1CCC(c2cccc(C(=O)NCCCO)c2)(C2CCN(Cc3ccc(Br)cc3)CC2)C(=O)N1 | 10.1016/j.bmcl.2008.07.115 | |||
CHEMBL514259 | 189648 | None | 0 | Human | Functional | pIC50 | = | 5.9 | 5.9 | - | 1 | ChEMBL | 541 | 8 | 3 | 5 | 3.1 | O=C1CCC(c2cccc(C(=O)NCCCO)c2)(C2CCN(Cc3ccc(Br)cc3)CC2)C(=O)N1 | 10.1016/j.bmcl.2008.07.115 | |||
44581109 | 193198 | None | 0 | Human | Functional | pIC50 | = | 5.9 | 5.9 | - | 1 | ChEMBL | 458 | 4 | 1 | 3 | 4.2 | O=C1CCC(c2ccc(F)cc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C(=O)N1 | 10.1016/j.bmcl.2008.07.115 | |||
CHEMBL522551 | 193198 | None | 0 | Human | Functional | pIC50 | = | 5.9 | 5.9 | - | 1 | ChEMBL | 458 | 4 | 1 | 3 | 4.2 | O=C1CCC(c2ccc(F)cc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C(=O)N1 | 10.1016/j.bmcl.2008.07.115 | |||
45486560 | 201013 | None | 0 | Human | Functional | pIC50 | = | 6.9 | 6.9 | - | 1 | ChEMBL | 615 | 9 | 0 | 8 | 4.4 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(C(F)(F)F)c(F)c1)[C@H](C)c1nc2ncccc2c(=O)n1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2009.07.021 | |||
CHEMBL578197 | 201013 | None | 0 | Human | Functional | pIC50 | = | 6.9 | 6.9 | - | 1 | ChEMBL | 615 | 9 | 0 | 8 | 4.4 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(C(F)(F)F)c(F)c1)[C@H](C)c1nc2ncccc2c(=O)n1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2009.07.021 | |||
44253589 | 6479 | None | 0 | Human | Functional | pIC50 | = | 5.9 | 5.9 | - | 1 | ChEMBL | 473 | 7 | 1 | 5 | 4.6 | O=S(=O)(c1ccc(Cl)cc1)N(Cc1ccc(-c2nnn[nH]2)cc1)Cc1cccc(Cl)c1 | 10.1016/j.bmcl.2010.04.113 | |||
CHEMBL1082649 | 6479 | None | 0 | Human | Functional | pIC50 | = | 5.9 | 5.9 | - | 1 | ChEMBL | 473 | 7 | 1 | 5 | 4.6 | O=S(=O)(c1ccc(Cl)cc1)N(Cc1ccc(-c2nnn[nH]2)cc1)Cc1cccc(Cl)c1 | 10.1016/j.bmcl.2010.04.113 | |||
44253167 | 6636 | None | 0 | Human | Functional | pIC50 | = | 5.9 | 5.9 | - | 1 | ChEMBL | 538 | 9 | 1 | 3 | 6.3 | O=C(NCc1cccc(Cl)c1)c1ccc(CN(Cc2ccccc2)S(=O)(=O)c2ccc(Cl)cc2)cc1 | 10.1016/j.bmcl.2010.04.113 | |||
CHEMBL1083315 | 6636 | None | 0 | Human | Functional | pIC50 | = | 5.9 | 5.9 | - | 1 | ChEMBL | 538 | 9 | 1 | 3 | 6.3 | O=C(NCc1cccc(Cl)c1)c1ccc(CN(Cc2ccccc2)S(=O)(=O)c2ccc(Cl)cc2)cc1 | 10.1016/j.bmcl.2010.04.113 | |||
56673937 | 64249 | None | 0 | Rat | Functional | pIC50 | = | 7.9 | 7.9 | -2 | 3 | ChEMBL | 440 | 2 | 2 | 2 | 4.7 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CCCCC1 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1809000 | 64249 | None | 0 | Rat | Functional | pIC50 | = | 7.9 | 7.9 | -2 | 3 | ChEMBL | 440 | 2 | 2 | 2 | 4.7 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CCCCC1 | 10.1016/j.bmcl.2011.06.070 | |||
46891272 | 6425 | None | 0 | Human | Functional | pIC50 | = | 7.9 | 7.9 | - | 1 | ChEMBL | 522 | 9 | 1 | 5 | 4.8 | N#Cc1ccc(S(=O)(=O)N(Cc2ccc(C(=O)NC3(c4ccccc4)CC3)cc2)Cc2ccccn2)cc1 | 10.1016/j.bmcl.2010.04.113 | |||
CHEMBL1082388 | 6425 | None | 0 | Human | Functional | pIC50 | = | 7.9 | 7.9 | - | 1 | ChEMBL | 522 | 9 | 1 | 5 | 4.8 | N#Cc1ccc(S(=O)(=O)N(Cc2ccc(C(=O)NC3(c4ccccc4)CC3)cc2)Cc2ccccn2)cc1 | 10.1016/j.bmcl.2010.04.113 | |||
117740035 | 153942 | None | 0 | Human | Functional | pIC50 | = | 7.9 | 7.9 | - | 1 | ChEMBL | 475 | 4 | 1 | 7 | 3.6 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cccn1 | 10.1021/acs.jmedchem.2c00676 | |||
CHEMBL3982804 | 153942 | None | 0 | Human | Functional | pIC50 | = | 7.9 | 7.9 | - | 1 | ChEMBL | 475 | 4 | 1 | 7 | 3.6 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cccn1 | 10.1021/acs.jmedchem.2c00676 | |||
56660100 | 64250 | None | 0 | Mouse | Functional | pIC50 | = | 7.9 | 7.9 | 2 | 2 | ChEMBL | 454 | 2 | 2 | 2 | 5.0 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CCCCCC1 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1809001 | 64250 | None | 0 | Mouse | Functional | pIC50 | = | 7.9 | 7.9 | 2 | 2 | ChEMBL | 454 | 2 | 2 | 2 | 5.0 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CCCCCC1 | 10.1016/j.bmcl.2011.06.070 | |||
168284279 | 191651 | None | 0 | Human | Functional | pIC50 | = | 7.9 | 7.9 | - | 1 | ChEMBL | 516 | 5 | 0 | 8 | 4.3 | COc1ccc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3cnc4cccnc43)[C@H](C)C2)cc1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL5194504 | 191651 | None | 0 | Human | Functional | pIC50 | = | 7.9 | 7.9 | - | 1 | ChEMBL | 516 | 5 | 0 | 8 | 4.3 | COc1ccc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3cnc4cccnc43)[C@H](C)C2)cc1 | 10.1021/acs.jmedchem.2c00675 | |||
15604689 | 72619 | None | 0 | Human | Functional | pIC50 | = | 6.9 | 6.9 | - | 1 | ChEMBL | 587 | 8 | 3 | 5 | 5.5 | CCNC(=O)N1CCCN(c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2NC(=O)c2cccs2)CC1 | 10.1016/j.bmcl.2005.09.020 | |||
CHEMBL199321 | 72619 | None | 0 | Human | Functional | pIC50 | = | 6.9 | 6.9 | - | 1 | ChEMBL | 587 | 8 | 3 | 5 | 5.5 | CCNC(=O)N1CCCN(c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2NC(=O)c2cccs2)CC1 | 10.1016/j.bmcl.2005.09.020 | |||
44406348 | 132893 | None | 0 | Human | Functional | pIC50 | = | 4.9 | 4.9 | - | 1 | ChEMBL | 616 | 8 | 2 | 5 | 6.5 | CCOC(=O)N1CCCN(c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2NC(=O)c2cccc(Cl)c2)CC1 | 10.1016/j.bmcl.2005.09.020 | |||
CHEMBL370167 | 132893 | None | 0 | Human | Functional | pIC50 | = | 4.9 | 4.9 | - | 1 | ChEMBL | 616 | 8 | 2 | 5 | 6.5 | CCOC(=O)N1CCCN(c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2NC(=O)c2cccc(Cl)c2)CC1 | 10.1016/j.bmcl.2005.09.020 | |||
46883309 | 6180 | None | 0 | Human | Functional | pIC50 | = | 6.9 | 6.9 | - | 1 | ChEMBL | 639 | 8 | 0 | 7 | 5.5 | CCOc1ccc(-n2c([C@@H](C)N(C(=O)Cc3ccc(F)c(C(F)(F)F)c3)C3CCN(C(C)=O)CC3)nc3ncccc3c2=O)cc1 | 10.1016/j.bmcl.2009.07.032 | |||
CHEMBL1081164 | 6180 | None | 0 | Human | Functional | pIC50 | = | 6.9 | 6.9 | - | 1 | ChEMBL | 639 | 8 | 0 | 7 | 5.5 | CCOc1ccc(-n2c([C@@H](C)N(C(=O)Cc3ccc(F)c(C(F)(F)F)c3)C3CCN(C(C)=O)CC3)nc3ncccc3c2=O)cc1 | 10.1016/j.bmcl.2009.07.032 | |||
168284279 | 191651 | None | 0 | Human | Functional | pIC50 | = | 6.9 | 6.9 | - | 1 | ChEMBL | 516 | 5 | 0 | 8 | 4.3 | COc1ccc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3cnc4cccnc43)[C@H](C)C2)cc1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL5194504 | 191651 | None | 0 | Human | Functional | pIC50 | = | 6.9 | 6.9 | - | 1 | ChEMBL | 516 | 5 | 0 | 8 | 4.3 | COc1ccc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3cnc4cccnc43)[C@H](C)C2)cc1 | 10.1021/acs.jmedchem.2c00675 | |||
14479864 | 4653 | None | 0 | Human | Functional | pIC50 | = | 5.9 | 5.9 | 13 | 2 | ChEMBL | 440 | 4 | 1 | 3 | 4.0 | O=C1CCC(c2ccccc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C(=O)N1 | 10.1016/j.bmcl.2008.07.115 | |||
CHEMBL10309 | 4653 | None | 0 | Human | Functional | pIC50 | = | 5.9 | 5.9 | 13 | 2 | ChEMBL | 440 | 4 | 1 | 3 | 4.0 | O=C1CCC(c2ccccc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C(=O)N1 | 10.1016/j.bmcl.2008.07.115 | |||
117739191 | 150772 | None | 0 | Human | Functional | pIC50 | = | 6.9 | 6.9 | - | 1 | ChEMBL | 544 | 4 | 1 | 8 | 3.6 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cnc2c1CCN(C)C2 | 10.1021/acs.jmedchem.2c00676 | |||
CHEMBL3955848 | 150772 | None | 0 | Human | Functional | pIC50 | = | 6.9 | 6.9 | - | 1 | ChEMBL | 544 | 4 | 1 | 8 | 3.6 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cnc2c1CCN(C)C2 | 10.1021/acs.jmedchem.2c00676 | |||
90479878 | 190352 | None | 0 | Human | Functional | pIC50 | = | 6.9 | 6.9 | - | 1 | ChEMBL | 524 | 6 | 0 | 10 | 3.4 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3cnc(OC(C)C)nc3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL5175118 | 190352 | None | 0 | Human | Functional | pIC50 | = | 6.9 | 6.9 | - | 1 | ChEMBL | 524 | 6 | 0 | 10 | 3.4 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3cnc(OC(C)C)nc3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00675 | |||
168286976 | 191499 | None | 0 | Human | Functional | pIC50 | = | 5.9 | 5.9 | - | 1 | ChEMBL | 570 | 5 | 1 | 7 | 4.9 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)CN1C(=O)OC[C@@H]1c1ccccc1 | 10.1021/acs.jmedchem.2c00676 | |||
CHEMBL5192464 | 191499 | None | 0 | Human | Functional | pIC50 | = | 5.9 | 5.9 | - | 1 | ChEMBL | 570 | 5 | 1 | 7 | 4.9 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)CN1C(=O)OC[C@@H]1c1ccccc1 | 10.1021/acs.jmedchem.2c00676 | |||
56660100 | 64250 | None | 0 | Human | Functional | pIC50 | = | 7.9 | 7.9 | -2 | 2 | ChEMBL | 454 | 2 | 2 | 2 | 5.0 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CCCCCC1 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1809001 | 64250 | None | 0 | Human | Functional | pIC50 | = | 7.9 | 7.9 | -2 | 2 | ChEMBL | 454 | 2 | 2 | 2 | 5.0 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CCCCCC1 | 10.1016/j.bmcl.2011.06.070 | |||
56667009 | 64276 | None | 0 | Human | Functional | pIC50 | = | 7.9 | 7.9 | -1 | 2 | ChEMBL | 446 | 2 | 2 | 2 | 4.5 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)NC2CCCCCC2)C1)N1CCCC1 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1809029 | 64276 | None | 0 | Human | Functional | pIC50 | = | 7.9 | 7.9 | -1 | 2 | ChEMBL | 446 | 2 | 2 | 2 | 4.5 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)NC2CCCCCC2)C1)N1CCCC1 | 10.1016/j.bmcl.2011.06.070 | |||
11964007 | 64248 | None | 0 | Mouse | Functional | pIC50 | = | 7.9 | 7.9 | 1 | 2 | ChEMBL | 412 | 2 | 2 | 2 | 3.9 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CCC1 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1808999 | 64248 | None | 0 | Mouse | Functional | pIC50 | = | 7.9 | 7.9 | 1 | 2 | ChEMBL | 412 | 2 | 2 | 2 | 3.9 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CCC1 | 10.1016/j.bmcl.2011.06.070 | |||
71680139 | 147784 | None | 0 | Human | Functional | pIC50 | = | 7.9 | 7.9 | - | 1 | ChEMBL | 500 | 5 | 1 | 8 | 4.3 | CC(C)c1nc(-c2nc3ccccc3[nH]2)c(N2CCN(C(=O)Cn3cnc4cccnc43)[C@H](C)C2)s1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL3931920 | 147784 | None | 0 | Human | Functional | pIC50 | = | 7.9 | 7.9 | - | 1 | ChEMBL | 500 | 5 | 1 | 8 | 4.3 | CC(C)c1nc(-c2nc3ccccc3[nH]2)c(N2CCN(C(=O)Cn3cnc4cccnc43)[C@H](C)C2)s1 | 10.1021/acs.jmedchem.2c00675 | |||
90480006 | 190917 | None | 1 | Human | Functional | pIC50 | = | 7.9 | 7.9 | - | 1 | ChEMBL | 494 | 5 | 0 | 9 | 3.1 | CCc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3nc(C)nc3C)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL5183818 | 190917 | None | 1 | Human | Functional | pIC50 | = | 7.9 | 7.9 | - | 1 | ChEMBL | 494 | 5 | 0 | 9 | 3.1 | CCc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3nc(C)nc3C)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
44426723 | 86067 | None | 0 | Human | Functional | pIC50 | = | 6.9 | 6.9 | - | 1 | ChEMBL | 602 | 10 | 0 | 7 | 6.4 | CCOc1ccc(-n2c([C@@H](C)N(Cc3cccnc3)C(=O)Cc3ccc(OC(F)(F)F)cc3)nc3ccccc3c2=O)cc1 | 10.1016/j.bmcl.2009.07.032 | |||
CHEMBL230664 | 86067 | None | 0 | Human | Functional | pIC50 | = | 6.9 | 6.9 | - | 1 | ChEMBL | 602 | 10 | 0 | 7 | 6.4 | CCOc1ccc(-n2c([C@@H](C)N(Cc3cccnc3)C(=O)Cc3ccc(OC(F)(F)F)cc3)nc3ccccc3c2=O)cc1 | 10.1016/j.bmcl.2009.07.032 | |||
53323853 | 58234 | None | 0 | Human | Functional | pIC50 | = | 6.9 | 6.9 | - | 1 | ChEMBL | 519 | 6 | 1 | 7 | 3.1 | CNC(=O)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4)CC3)C(C(=O)OC)C2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
CHEMBL1681877 | 58234 | None | 0 | Human | Functional | pIC50 | = | 6.9 | 6.9 | - | 1 | ChEMBL | 519 | 6 | 1 | 7 | 3.1 | CNC(=O)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4)CC3)C(C(=O)OC)C2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
24739387 | 188263 | None | 0 | Human | Functional | pIC50 | = | 6.9 | 6.9 | 9 | 4 | ChEMBL | 454 | 4 | 0 | 2 | 5.2 | CC(=O)N1CCCC(c2ccccc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C1 | 10.1016/j.bmcl.2008.07.115 | |||
CHEMBL498556 | 188263 | None | 0 | Human | Functional | pIC50 | = | 6.9 | 6.9 | 9 | 4 | ChEMBL | 454 | 4 | 0 | 2 | 5.2 | CC(=O)N1CCCC(c2ccccc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C1 | 10.1016/j.bmcl.2008.07.115 | |||
168296640 | 192583 | None | 0 | Human | Functional | pIC50 | = | 6.9 | 6.9 | - | 1 | ChEMBL | 575 | 8 | 0 | 11 | 3.0 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2cnc(OCCN(C)C)nc2)CCN1C(=O)Cn1cnc2cccnc21 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL5208823 | 192583 | None | 0 | Human | Functional | pIC50 | = | 6.9 | 6.9 | - | 1 | ChEMBL | 575 | 8 | 0 | 11 | 3.0 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2cnc(OCCN(C)C)nc2)CCN1C(=O)Cn1cnc2cccnc21 | 10.1021/acs.jmedchem.2c00675 | |||
53325131 | 58214 | None | 0 | Human | Functional | pIC50 | = | 5.9 | 5.9 | - | 1 | ChEMBL | 587 | 7 | 1 | 5 | 4.9 | O=C(NCc1ccc(F)c(F)c1)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4)CC3)C(=O)C2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
CHEMBL1681857 | 58214 | None | 0 | Human | Functional | pIC50 | = | 5.9 | 5.9 | - | 1 | ChEMBL | 587 | 7 | 1 | 5 | 4.9 | O=C(NCc1ccc(F)c(F)c1)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4)CC3)C(=O)C2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
89726463 | 154193 | None | 0 | Human | Functional | pIC50 | = | 6.8 | 6.8 | - | 1 | ChEMBL | 542 | 4 | 2 | 8 | 3.5 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1c(=O)[nH]c2cccnc21 | 10.1021/acs.jmedchem.2c00676 | |||
CHEMBL3985006 | 154193 | None | 0 | Human | Functional | pIC50 | = | 6.8 | 6.8 | - | 1 | ChEMBL | 542 | 4 | 2 | 8 | 3.5 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1c(=O)[nH]c2cccnc21 | 10.1021/acs.jmedchem.2c00676 | |||
90480006 | 190917 | None | 1 | Human | Functional | pIC50 | = | 5.8 | 5.8 | - | 1 | ChEMBL | 494 | 5 | 0 | 9 | 3.1 | CCc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3nc(C)nc3C)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL5183818 | 190917 | None | 1 | Human | Functional | pIC50 | = | 5.8 | 5.8 | - | 1 | ChEMBL | 494 | 5 | 0 | 9 | 3.1 | CCc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3nc(C)nc3C)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
89726174 | 147207 | None | 0 | Human | Functional | pIC50 | = | 6.8 | 6.8 | - | 1 | ChEMBL | 586 | 6 | 1 | 10 | 4.2 | COc1cc2nc(-c3nc(C(F)(F)F)sc3N3CCN(C(=O)Cn4cnc5cccnc54)[C@H](C)C3)[nH]c2cc1OC | 10.1021/acs.jmedchem.2c00676 | |||
CHEMBL3927485 | 147207 | None | 0 | Human | Functional | pIC50 | = | 6.8 | 6.8 | - | 1 | ChEMBL | 586 | 6 | 1 | 10 | 4.2 | COc1cc2nc(-c3nc(C(F)(F)F)sc3N3CCN(C(=O)Cn4cnc5cccnc54)[C@H](C)C3)[nH]c2cc1OC | 10.1021/acs.jmedchem.2c00676 | |||
44581136 | 193353 | None | 0 | Human | Functional | pIC50 | = | 5.8 | 5.8 | - | 1 | ChEMBL | 474 | 4 | 1 | 3 | 4.7 | O=C1CCC(c2cccc(Cl)c2)(C2CCN(Cc3ccc(Br)cc3)CC2)C(=O)N1 | 10.1016/j.bmcl.2008.07.115 | |||
CHEMBL523748 | 193353 | None | 0 | Human | Functional | pIC50 | = | 5.8 | 5.8 | - | 1 | ChEMBL | 474 | 4 | 1 | 3 | 4.7 | O=C1CCC(c2cccc(Cl)c2)(C2CCN(Cc3ccc(Br)cc3)CC2)C(=O)N1 | 10.1016/j.bmcl.2008.07.115 | |||
44253591 | 6481 | None | 0 | Human | Functional | pIC50 | = | 5.8 | 5.8 | - | 1 | ChEMBL | 469 | 8 | 1 | 6 | 3.9 | COc1cccc(CN(Cc2ccc(-c3nnn[nH]3)cc2)S(=O)(=O)c2ccc(Cl)cc2)c1 | 10.1016/j.bmcl.2010.04.113 | |||
CHEMBL1082660 | 6481 | None | 0 | Human | Functional | pIC50 | = | 5.8 | 5.8 | - | 1 | ChEMBL | 469 | 8 | 1 | 6 | 3.9 | COc1cccc(CN(Cc2ccc(-c3nnn[nH]3)cc2)S(=O)(=O)c2ccc(Cl)cc2)c1 | 10.1016/j.bmcl.2010.04.113 | |||
168284829 | 191892 | None | 0 | Human | Functional | pIC50 | = | 5.8 | 5.8 | - | 1 | ChEMBL | 576 | 6 | 1 | 10 | 3.4 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccc(OC5COC5)cc4[nH]3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00676 | |||
CHEMBL5198121 | 191892 | None | 0 | Human | Functional | pIC50 | = | 5.8 | 5.8 | - | 1 | ChEMBL | 576 | 6 | 1 | 10 | 3.4 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccc(OC5COC5)cc4[nH]3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00676 | |||
45101529 | 5672 | None | 0 | Human | Functional | pIC50 | = | 7.8 | 7.8 | 1 | 5 | ChEMBL | 688 | 11 | 0 | 8 | 5.4 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc2ncccc2c(=O)n1-c1ccc(OCC(F)(F)F)cc1 | 10.1016/j.bmcl.2009.07.032 | |||
CHEMBL1077831 | 5672 | None | 0 | Human | Functional | pIC50 | = | 7.8 | 7.8 | 1 | 5 | ChEMBL | 688 | 11 | 0 | 8 | 5.4 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc2ncccc2c(=O)n1-c1ccc(OCC(F)(F)F)cc1 | 10.1016/j.bmcl.2009.07.032 | |||
24957182 | 153602 | None | 39 | Human | Functional | pIC50 | = | 7.8 | 7.8 | 63 | 2 | ChEMBL | 603 | 10 | 0 | 8 | 5.8 | CCOc1ccc(-n2c([C@@H](C)N(Cc3cccnc3)C(=O)Cc3ccc(OC(F)(F)F)cc3)nc3ncccc3c2=O)cc1 | 10.1016/j.bmcl.2007.11.060 | |||
CHEMBL397983 | 153602 | None | 39 | Human | Functional | pIC50 | = | 7.8 | 7.8 | 63 | 2 | ChEMBL | 603 | 10 | 0 | 8 | 5.8 | CCOc1ccc(-n2c([C@@H](C)N(Cc3cccnc3)C(=O)Cc3ccc(OC(F)(F)F)cc3)nc3ncccc3c2=O)cc1 | 10.1016/j.bmcl.2007.11.060 | |||
89726091 | 147124 | None | 0 | Human | Functional | pIC50 | = | 7.8 | 7.8 | - | 1 | ChEMBL | 572 | 5 | 1 | 8 | 4.4 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cc(C2CCN(C)CC2)cn1 | 10.1021/acs.jmedchem.2c00676 | |||
CHEMBL3926820 | 147124 | None | 0 | Human | Functional | pIC50 | = | 7.8 | 7.8 | - | 1 | ChEMBL | 572 | 5 | 1 | 8 | 4.4 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cc(C2CCN(C)CC2)cn1 | 10.1021/acs.jmedchem.2c00676 | |||
168288302 | 191478 | None | 0 | Human | Functional | pIC50 | = | 7.8 | 7.8 | - | 1 | ChEMBL | 528 | 4 | 1 | 6 | 4.5 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)CN1CCC(F)(F)CC1 | 10.1021/acs.jmedchem.2c00676 | |||
CHEMBL5192187 | 191478 | None | 0 | Human | Functional | pIC50 | = | 7.8 | 7.8 | - | 1 | ChEMBL | 528 | 4 | 1 | 6 | 4.5 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)CN1CCC(F)(F)CC1 | 10.1021/acs.jmedchem.2c00676 | |||
24957182 | 153602 | None | 39 | Human | Functional | pIC50 | = | 7.8 | 7.8 | 63 | 2 | ChEMBL | 603 | 10 | 0 | 8 | 5.8 | CCOc1ccc(-n2c([C@@H](C)N(Cc3cccnc3)C(=O)Cc3ccc(OC(F)(F)F)cc3)nc3ncccc3c2=O)cc1 | 10.1016/j.bmcl.2007.03.106 | |||
CHEMBL397983 | 153602 | None | 39 | Human | Functional | pIC50 | = | 7.8 | 7.8 | 63 | 2 | ChEMBL | 603 | 10 | 0 | 8 | 5.8 | CCOc1ccc(-n2c([C@@H](C)N(Cc3cccnc3)C(=O)Cc3ccc(OC(F)(F)F)cc3)nc3ncccc3c2=O)cc1 | 10.1016/j.bmcl.2007.03.106 | |||
24739386 | 187884 | None | 0 | Human | Functional | pIC50 | = | 6.8 | 6.8 | - | 1 | ChEMBL | 440 | 5 | 0 | 2 | 4.9 | O=CN1CCCC(c2ccccc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C1 | 10.1016/j.bmcl.2008.07.115 | |||
CHEMBL495752 | 187884 | None | 0 | Human | Functional | pIC50 | = | 6.8 | 6.8 | - | 1 | ChEMBL | 440 | 5 | 0 | 2 | 4.9 | O=CN1CCCC(c2ccccc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C1 | 10.1016/j.bmcl.2008.07.115 | |||
89726765 | 149355 | None | 0 | Human | Functional | pIC50 | = | 6.8 | 6.8 | - | 1 | ChEMBL | 533 | 7 | 0 | 9 | 3.8 | COCCn1c(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3cccn3)[C@H](C)C2)nc2ccccc21 | 10.1021/acs.jmedchem.2c00676 | |||
CHEMBL3944489 | 149355 | None | 0 | Human | Functional | pIC50 | = | 6.8 | 6.8 | - | 1 | ChEMBL | 533 | 7 | 0 | 9 | 3.8 | COCCn1c(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3cccn3)[C@H](C)C2)nc2ccccc21 | 10.1021/acs.jmedchem.2c00676 | |||
44581134 | 188004 | None | 0 | Human | Functional | pIC50 | = | 5.8 | 5.8 | - | 1 | ChEMBL | 470 | 5 | 1 | 4 | 4.0 | COc1cccc(C2(C3CCN(Cc4ccc(Br)cc4)CC3)CCC(=O)NC2=O)c1 | 10.1016/j.bmcl.2008.07.115 | |||
CHEMBL496570 | 188004 | None | 0 | Human | Functional | pIC50 | = | 5.8 | 5.8 | - | 1 | ChEMBL | 470 | 5 | 1 | 4 | 4.0 | COc1cccc(C2(C3CCN(Cc4ccc(Br)cc4)CC3)CCC(=O)NC2=O)c1 | 10.1016/j.bmcl.2008.07.115 | |||
46891537 | 6416 | None | 0 | Human | Functional | pIC50 | = | 6.8 | 6.8 | - | 1 | ChEMBL | 475 | 7 | 1 | 5 | 4.2 | O=S(=O)(c1ccc(Cl)cc1)N(Cc1ccc(-c2nnn[nH]2)c(F)c1)Cc1ccccc1F | 10.1016/j.bmcl.2010.04.113 | |||
CHEMBL1082360 | 6416 | None | 0 | Human | Functional | pIC50 | = | 6.8 | 6.8 | - | 1 | ChEMBL | 475 | 7 | 1 | 5 | 4.2 | O=S(=O)(c1ccc(Cl)cc1)N(Cc1ccc(-c2nnn[nH]2)c(F)c1)Cc1ccccc1F | 10.1016/j.bmcl.2010.04.113 | |||
46891536 | 7176 | None | 0 | Human | Functional | pIC50 | = | 6.8 | 6.8 | - | 1 | ChEMBL | 454 | 8 | 1 | 7 | 2.8 | COc1ccc(S(=O)(=O)N(Cc2ccc(-c3nnn[nH]3)c(F)c2)Cc2ccccn2)cc1 | 10.1016/j.bmcl.2010.04.113 | |||
CHEMBL1085508 | 7176 | None | 0 | Human | Functional | pIC50 | = | 6.8 | 6.8 | - | 1 | ChEMBL | 454 | 8 | 1 | 7 | 2.8 | COc1ccc(S(=O)(=O)N(Cc2ccc(-c3nnn[nH]3)c(F)c2)Cc2ccccn2)cc1 | 10.1016/j.bmcl.2010.04.113 | |||
44569942 | 176810 | None | 0 | Human | Functional | pIC50 | = | 6.8 | 6.8 | - | 1 | ChEMBL | 447 | 4 | 1 | 5 | 2.7 | CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCN(c3ccc(C(F)(F)F)cn3)CC1)C(O)C2 | 10.1016/j.bmcl.2008.11.008 | |||
CHEMBL459950 | 176810 | None | 0 | Human | Functional | pIC50 | = | 6.8 | 6.8 | - | 1 | ChEMBL | 447 | 4 | 1 | 5 | 2.7 | CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCN(c3ccc(C(F)(F)F)cn3)CC1)C(O)C2 | 10.1016/j.bmcl.2008.11.008 | |||
44570549 | 178478 | None | 0 | Human | Functional | pIC50 | = | 6.8 | 6.8 | 15 | 2 | ChEMBL | 459 | 4 | 0 | 5 | 3.3 | C[C@H]1CN(S(=O)(=O)C[C@]23CC[C@H](CC2=O)C3(C)C)CCN1c1ccc(C(F)(F)F)cn1 | 10.1016/j.bmcl.2008.11.008 | |||
CHEMBL465283 | 178478 | None | 0 | Human | Functional | pIC50 | = | 6.8 | 6.8 | 15 | 2 | ChEMBL | 459 | 4 | 0 | 5 | 3.3 | C[C@H]1CN(S(=O)(=O)C[C@]23CC[C@H](CC2=O)C3(C)C)CCN1c1ccc(C(F)(F)F)cn1 | 10.1016/j.bmcl.2008.11.008 | |||
44570385 | 183171 | None | 0 | Human | Functional | pIC50 | = | 6.8 | 6.8 | 5 | 2 | ChEMBL | 463 | 4 | 0 | 5 | 3.1 | CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCN(c3ncc(C(F)(F)F)cc3F)CC1)C(=O)C2 | 10.1016/j.bmcl.2008.11.008 | |||
CHEMBL479426 | 183171 | None | 0 | Human | Functional | pIC50 | = | 6.8 | 6.8 | 5 | 2 | ChEMBL | 463 | 4 | 0 | 5 | 3.1 | CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCN(c3ncc(C(F)(F)F)cc3F)CC1)C(=O)C2 | 10.1016/j.bmcl.2008.11.008 | |||
44570219 | 184010 | None | 0 | Human | Functional | pIC50 | = | 6.8 | 6.8 | 3 | 2 | ChEMBL | 461 | 4 | 1 | 5 | 3.1 | C[C@H]1CN(S(=O)(=O)C[C@]23CC[C@H](CC2O)C3(C)C)CCN1c1ccc(C(F)(F)F)cn1 | 10.1016/j.bmcl.2008.11.008 | |||
CHEMBL481197 | 184010 | None | 0 | Human | Functional | pIC50 | = | 6.8 | 6.8 | 3 | 2 | ChEMBL | 461 | 4 | 1 | 5 | 3.1 | C[C@H]1CN(S(=O)(=O)C[C@]23CC[C@H](CC2O)C3(C)C)CCN1c1ccc(C(F)(F)F)cn1 | 10.1016/j.bmcl.2008.11.008 | |||
44570272 | 177690 | None | 0 | Mouse | Functional | pIC50 | = | 6.8 | 6.8 | -3 | 2 | ChEMBL | 479 | 4 | 1 | 5 | 3.3 | C[C@H]1CN(S(=O)(=O)C[C@]23CC[C@H](CC2O)C3(C)C)CCN1c1ncc(C(F)(F)F)cc1F | 10.1016/j.bmcl.2008.11.008 | |||
CHEMBL464064 | 177690 | None | 0 | Mouse | Functional | pIC50 | = | 6.8 | 6.8 | -3 | 2 | ChEMBL | 479 | 4 | 1 | 5 | 3.3 | C[C@H]1CN(S(=O)(=O)C[C@]23CC[C@H](CC2O)C3(C)C)CCN1c1ncc(C(F)(F)F)cc1F | 10.1016/j.bmcl.2008.11.008 | |||
44580960 | 188268 | None | 0 | Human | Functional | pIC50 | = | 5.8 | 5.8 | - | 1 | ChEMBL | 426 | 4 | 1 | 2 | 4.5 | O=C1NCCCC1(c1ccccc1)C1CCN(Cc2ccc(Br)cc2)CC1 | 10.1016/j.bmcl.2008.07.115 | |||
CHEMBL498620 | 188268 | None | 0 | Human | Functional | pIC50 | = | 5.8 | 5.8 | - | 1 | ChEMBL | 426 | 4 | 1 | 2 | 4.5 | O=C1NCCCC1(c1ccccc1)C1CCN(Cc2ccc(Br)cc2)CC1 | 10.1016/j.bmcl.2008.07.115 | |||
44569941 | 176675 | None | 0 | Human | Functional | pIC50 | = | 5.8 | 5.8 | - | 1 | ChEMBL | 445 | 4 | 0 | 5 | 2.9 | CC1(C)[C@@H]2CC[C@]1(CS(=O)(=O)N1CCN(c3ccc(C(F)(F)F)cn3)CC1)C(=O)C2 | 10.1016/j.bmcl.2008.11.008 | |||
CHEMBL459742 | 176675 | None | 0 | Human | Functional | pIC50 | = | 5.8 | 5.8 | - | 1 | ChEMBL | 445 | 4 | 0 | 5 | 2.9 | CC1(C)[C@@H]2CC[C@]1(CS(=O)(=O)N1CCN(c3ccc(C(F)(F)F)cn3)CC1)C(=O)C2 | 10.1016/j.bmcl.2008.11.008 | |||
44570341 | 189980 | None | 0 | Human | Functional | pIC50 | = | 5.8 | 5.8 | - | 1 | ChEMBL | 455 | 4 | 0 | 5 | 2.7 | CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCN(c3ccc(Br)cn3)CC1)C(=O)C2 | 10.1016/j.bmcl.2008.11.008 | |||
CHEMBL516872 | 189980 | None | 0 | Human | Functional | pIC50 | = | 5.8 | 5.8 | - | 1 | ChEMBL | 455 | 4 | 0 | 5 | 2.7 | CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCN(c3ccc(Br)cn3)CC1)C(=O)C2 | 10.1016/j.bmcl.2008.11.008 | |||
44570273 | 177691 | None | 0 | Mouse | Functional | pIC50 | = | 5.8 | 5.8 | -25 | 2 | ChEMBL | 479 | 4 | 1 | 5 | 3.3 | C[C@H]1CN(S(=O)(=O)C[C@]23CC[C@H](C[C@H]2O)C3(C)C)CCN1c1ncc(C(F)(F)F)cc1F | 10.1016/j.bmcl.2008.11.008 | |||
CHEMBL464065 | 177691 | None | 0 | Mouse | Functional | pIC50 | = | 5.8 | 5.8 | -25 | 2 | ChEMBL | 479 | 4 | 1 | 5 | 3.3 | C[C@H]1CN(S(=O)(=O)C[C@]23CC[C@H](C[C@H]2O)C3(C)C)CCN1c1ncc(C(F)(F)F)cc1F | 10.1016/j.bmcl.2008.11.008 | |||
44570274 | 177839 | None | 0 | Mouse | Functional | pIC50 | = | 5.8 | 5.8 | -39 | 2 | ChEMBL | 521 | 4 | 0 | 6 | 3.6 | C[C@H]1CN(S(=O)(=O)C[C@]23CC[C@H](CC24OCCO4)C3(C)C)CCN1c1ncc(C(F)(F)F)cc1F | 10.1016/j.bmcl.2008.11.008 | |||
CHEMBL464244 | 177839 | None | 0 | Mouse | Functional | pIC50 | = | 5.8 | 5.8 | -39 | 2 | ChEMBL | 521 | 4 | 0 | 6 | 3.6 | C[C@H]1CN(S(=O)(=O)C[C@]23CC[C@H](CC24OCCO4)C3(C)C)CCN1c1ncc(C(F)(F)F)cc1F | 10.1016/j.bmcl.2008.11.008 | |||
44570629 | 183932 | None | 0 | Human | Functional | pIC50 | = | 4.8 | 4.8 | - | 1 | ChEMBL | 459 | 5 | 1 | 5 | 3.4 | CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)NC1CCN(c3ccc(C(F)(F)F)cn3)CC1)C(=O)C2 | 10.1016/j.bmcl.2008.11.008 | |||
CHEMBL480601 | 183932 | None | 0 | Human | Functional | pIC50 | = | 4.8 | 4.8 | - | 1 | ChEMBL | 459 | 5 | 1 | 5 | 3.4 | CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)NC1CCN(c3ccc(C(F)(F)F)cn3)CC1)C(=O)C2 | 10.1016/j.bmcl.2008.11.008 | |||
44570515 | 190049 | None | 0 | Human | Functional | pIC50 | = | 4.8 | 4.8 | - | 1 | ChEMBL | 427 | 4 | 0 | 5 | 3.1 | CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCN(c3cc4ccccc4cn3)CC1)C(=O)C2 | 10.1016/j.bmcl.2008.11.008 | |||
CHEMBL517024 | 190049 | None | 0 | Human | Functional | pIC50 | = | 4.8 | 4.8 | - | 1 | ChEMBL | 427 | 4 | 0 | 5 | 3.1 | CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCN(c3cc4ccccc4cn3)CC1)C(=O)C2 | 10.1016/j.bmcl.2008.11.008 | |||
45101497 | 58207 | None | 0 | Human | Functional | pIC50 | = | 7.8 | 7.8 | - | 1 | ChEMBL | 619 | 7 | 1 | 5 | 6.8 | C[C@H]1CN(c2ncc(C(=O)NCc3ccc(Cl)c(Cl)c3)cc2Cl)CCN1C1CCN(Cc2ccc(Cl)cc2)CC1 | 10.1016/j.bmcl.2010.12.114 | |||
CHEMBL1681850 | 58207 | None | 0 | Human | Functional | pIC50 | = | 7.8 | 7.8 | - | 1 | ChEMBL | 619 | 7 | 1 | 5 | 6.8 | C[C@H]1CN(c2ncc(C(=O)NCc3ccc(Cl)c(Cl)c3)cc2Cl)CCN1C1CCN(Cc2ccc(Cl)cc2)CC1 | 10.1016/j.bmcl.2010.12.114 | |||
56660101 | 64257 | None | 0 | Human | Functional | pIC50 | = | 7.8 | 7.8 | -1 | 3 | ChEMBL | 442 | 2 | 2 | 3 | 3.5 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CCOCC1 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1809008 | 64257 | None | 0 | Human | Functional | pIC50 | = | 7.8 | 7.8 | -1 | 3 | ChEMBL | 442 | 2 | 2 | 3 | 3.5 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CCOCC1 | 10.1016/j.bmcl.2011.06.070 | |||
56667007 | 64264 | None | 0 | Mouse | Functional | pIC50 | = | 7.8 | 7.8 | 1 | 2 | ChEMBL | 444 | 2 | 2 | 2 | 4.4 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2F)C1)N1CCCC1 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1809015 | 64264 | None | 0 | Mouse | Functional | pIC50 | = | 7.8 | 7.8 | 1 | 2 | ChEMBL | 444 | 2 | 2 | 2 | 4.4 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2F)C1)N1CCCC1 | 10.1016/j.bmcl.2011.06.070 | |||
56667009 | 64276 | None | 0 | Mouse | Functional | pIC50 | = | 7.8 | 7.8 | 1 | 2 | ChEMBL | 446 | 2 | 2 | 2 | 4.5 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)NC2CCCCCC2)C1)N1CCCC1 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1809029 | 64276 | None | 0 | Mouse | Functional | pIC50 | = | 7.8 | 7.8 | 1 | 2 | ChEMBL | 446 | 2 | 2 | 2 | 4.5 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)NC2CCCCCC2)C1)N1CCCC1 | 10.1016/j.bmcl.2011.06.070 | |||
46883310 | 5670 | None | 0 | Human | Functional | pIC50 | = | 6.8 | 6.8 | - | 1 | ChEMBL | 598 | 8 | 0 | 7 | 5.6 | CCOc1ccc(-n2c([C@@H](C)N(C(=O)Cc3ccc(F)c(C(F)(F)F)c3)C3CCOCC3)nc3ncccc3c2=O)cc1 | 10.1016/j.bmcl.2009.07.032 | |||
CHEMBL1077829 | 5670 | None | 0 | Human | Functional | pIC50 | = | 6.8 | 6.8 | - | 1 | ChEMBL | 598 | 8 | 0 | 7 | 5.6 | CCOc1ccc(-n2c([C@@H](C)N(C(=O)Cc3ccc(F)c(C(F)(F)F)c3)C3CCOCC3)nc3ncccc3c2=O)cc1 | 10.1016/j.bmcl.2009.07.032 | |||
168280397 | 191389 | None | 0 | Human | Functional | pIC50 | = | 6.8 | 6.8 | - | 1 | ChEMBL | 495 | 6 | 0 | 9 | 3.3 | CCOc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3nccc3C)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL5190681 | 191389 | None | 0 | Human | Functional | pIC50 | = | 6.8 | 6.8 | - | 1 | ChEMBL | 495 | 6 | 0 | 9 | 3.3 | CCOc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3nccc3C)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
168288472 | 191828 | None | 0 | Human | Functional | pIC50 | = | 6.8 | 6.8 | - | 1 | ChEMBL | 502 | 4 | 0 | 9 | 3.4 | Cc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3cnc4cccnc43)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL5197065 | 191828 | None | 0 | Human | Functional | pIC50 | = | 6.8 | 6.8 | - | 1 | ChEMBL | 502 | 4 | 0 | 9 | 3.4 | Cc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3cnc4cccnc43)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
89726091 | 147124 | None | 0 | Human | Functional | pIC50 | = | 5.8 | 5.8 | - | 1 | ChEMBL | 572 | 5 | 1 | 8 | 4.4 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cc(C2CCN(C)CC2)cn1 | 10.1021/acs.jmedchem.2c00676 | |||
CHEMBL3926820 | 147124 | None | 0 | Human | Functional | pIC50 | = | 5.8 | 5.8 | - | 1 | ChEMBL | 572 | 5 | 1 | 8 | 4.4 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cc(C2CCN(C)CC2)cn1 | 10.1021/acs.jmedchem.2c00676 | |||
46883297 | 5658 | None | 0 | Human | Functional | pIC50 | = | 7.8 | 7.8 | - | 1 | ChEMBL | 654 | 9 | 0 | 6 | 7.6 | CCOc1ccc(-n2c([C@@H](C)N(Cc3cccnc3)C(=O)Cc3cc(C(F)(F)F)cc(C(F)(F)F)c3)nc3ccccc3c2=O)cc1 | 10.1016/j.bmcl.2009.07.032 | |||
CHEMBL1077817 | 5658 | None | 0 | Human | Functional | pIC50 | = | 7.8 | 7.8 | - | 1 | ChEMBL | 654 | 9 | 0 | 6 | 7.6 | CCOc1ccc(-n2c([C@@H](C)N(Cc3cccnc3)C(=O)Cc3cc(C(F)(F)F)cc(C(F)(F)F)c3)nc3ccccc3c2=O)cc1 | 10.1016/j.bmcl.2009.07.032 | |||
53318510 | 58193 | None | 0 | Human | Functional | pIC50 | = | 7.8 | 7.8 | - | 1 | ChEMBL | 509 | 5 | 1 | 5 | 4.6 | CNC(=O)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4Cl)CC3)[C@@H](C)C2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
CHEMBL1681833 | 58193 | None | 0 | Human | Functional | pIC50 | = | 7.8 | 7.8 | - | 1 | ChEMBL | 509 | 5 | 1 | 5 | 4.6 | CNC(=O)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4Cl)CC3)[C@@H](C)C2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
45486526 | 200066 | None | 0 | Human | Functional | pIC50 | = | 7.8 | 7.8 | - | 1 | ChEMBL | 627 | 10 | 0 | 7 | 5.9 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(C(F)(F)F)c(F)c1)[C@H](C)c1nc2c(C3CC3)nccn2c1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2009.07.021 | |||
CHEMBL570665 | 200066 | None | 0 | Human | Functional | pIC50 | = | 7.8 | 7.8 | - | 1 | ChEMBL | 627 | 10 | 0 | 7 | 5.9 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(C(F)(F)F)c(F)c1)[C@H](C)c1nc2c(C3CC3)nccn2c1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2009.07.021 | |||
44581135 | 188005 | None | 0 | Human | Functional | pIC50 | = | 6.8 | 6.8 | - | 1 | ChEMBL | 550 | 6 | 2 | 6 | 3.3 | COc1ccc(S(=O)(=O)O)cc1C1(C2CCN(Cc3ccc(Br)cc3)CC2)CCC(=O)NC1=O | 10.1016/j.bmcl.2008.07.115 | |||
CHEMBL496571 | 188005 | None | 0 | Human | Functional | pIC50 | = | 6.8 | 6.8 | - | 1 | ChEMBL | 550 | 6 | 2 | 6 | 3.3 | COc1ccc(S(=O)(=O)O)cc1C1(C2CCN(Cc3ccc(Br)cc3)CC2)CCC(=O)NC1=O | 10.1016/j.bmcl.2008.07.115 | |||
56670456 | 64281 | None | 0 | Human | Functional | pIC50 | = | 6.8 | 6.8 | - | 1 | ChEMBL | 425 | 3 | 1 | 2 | 3.8 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Cc2ccccc2)C1)N1CCCC1 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1809036 | 64281 | None | 0 | Human | Functional | pIC50 | = | 6.8 | 6.8 | - | 1 | ChEMBL | 425 | 3 | 1 | 2 | 3.8 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Cc2ccccc2)C1)N1CCCC1 | 10.1016/j.bmcl.2011.06.070 | |||
15604607 | 133504 | None | 0 | Human | Functional | pIC50 | = | 6.8 | 6.8 | - | 1 | ChEMBL | 611 | 9 | 3 | 5 | 5.5 | CCNC(=O)N1CCCN(c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2NC(=O)c2cccc(OC)c2)CC1 | 10.1016/j.bmcl.2005.09.020 | |||
CHEMBL370591 | 133504 | None | 0 | Human | Functional | pIC50 | = | 6.8 | 6.8 | - | 1 | ChEMBL | 611 | 9 | 3 | 5 | 5.5 | CCNC(=O)N1CCCN(c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2NC(=O)c2cccc(OC)c2)CC1 | 10.1016/j.bmcl.2005.09.020 | |||
89726443 | 150962 | None | 0 | Human | Functional | pIC50 | = | 6.8 | 6.8 | - | 1 | ChEMBL | 488 | 5 | 2 | 9 | 2.7 | C[C@@H]1CN(c2sc(CO)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL3957343 | 150962 | None | 0 | Human | Functional | pIC50 | = | 6.8 | 6.8 | - | 1 | ChEMBL | 488 | 5 | 2 | 9 | 2.7 | C[C@@H]1CN(c2sc(CO)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | 10.1021/acs.jmedchem.2c00675 | |||
90480455 | 191382 | None | 0 | Human | Functional | pIC50 | = | 6.8 | 6.8 | - | 1 | ChEMBL | 510 | 6 | 0 | 10 | 3.0 | CCOc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3nc(C)nc3C)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL5190588 | 191382 | None | 0 | Human | Functional | pIC50 | = | 6.8 | 6.8 | - | 1 | ChEMBL | 510 | 6 | 0 | 10 | 3.0 | CCOc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3nc(C)nc3C)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
56667005 | 64253 | None | 0 | Mouse | Functional | pIC50 | = | 5.8 | 5.8 | -2 | 2 | ChEMBL | 441 | 2 | 3 | 3 | 3.1 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CCNCC1 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1809004 | 64253 | None | 0 | Mouse | Functional | pIC50 | = | 5.8 | 5.8 | -2 | 2 | ChEMBL | 441 | 2 | 3 | 3 | 3.1 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CCNCC1 | 10.1016/j.bmcl.2011.06.070 | |||
168271845 | 190659 | None | 0 | Human | Functional | pIC50 | = | 6.8 | 6.8 | - | 1 | ChEMBL | 475 | 5 | 1 | 7 | 3.1 | O=C(Nc1ncccc1N1CCN(C(=O)Cn2cnc3cccnc32)CC1)c1cccc(Cl)c1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL5179925 | 190659 | None | 0 | Human | Functional | pIC50 | = | 6.8 | 6.8 | - | 1 | ChEMBL | 475 | 5 | 1 | 7 | 3.1 | O=C(Nc1ncccc1N1CCN(C(=O)Cn2cnc3cccnc32)CC1)c1cccc(Cl)c1 | 10.1021/acs.jmedchem.2c00675 | |||
168273430 | 190794 | None | 0 | Human | Functional | pIC50 | = | 6.8 | 6.8 | - | 1 | ChEMBL | 518 | 5 | 0 | 10 | 3.1 | COc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3cnc4cccnc43)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL5181928 | 190794 | None | 0 | Human | Functional | pIC50 | = | 6.8 | 6.8 | - | 1 | ChEMBL | 518 | 5 | 0 | 10 | 3.1 | COc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3cnc4cccnc43)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
53326388 | 58195 | None | 0 | Human | Functional | pIC50 | = | 7.8 | 7.8 | - | 1 | ChEMBL | 493 | 5 | 1 | 5 | 4.1 | CNC(=O)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4F)CC3)[C@@H](C)C2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
CHEMBL1681835 | 58195 | None | 0 | Human | Functional | pIC50 | = | 7.8 | 7.8 | - | 1 | ChEMBL | 493 | 5 | 1 | 5 | 4.1 | CNC(=O)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4F)CC3)[C@@H](C)C2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
45482789 | 201381 | None | 0 | Human | Functional | pIC50 | = | 7.8 | 7.8 | 1 | 14 | ChEMBL | 428 | 4 | 2 | 2 | 4.5 | CCN(CC)C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1 | 10.1016/j.bmcl.2009.09.002 | |||
CHEMBL584554 | 201381 | None | 0 | Human | Functional | pIC50 | = | 7.8 | 7.8 | 1 | 14 | ChEMBL | 428 | 4 | 2 | 2 | 4.5 | CCN(CC)C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1 | 10.1016/j.bmcl.2009.09.002 | |||
45482789 | 201381 | None | 0 | Human | Functional | pIC50 | = | 7.8 | 7.8 | 1 | 14 | ChEMBL | 428 | 4 | 2 | 2 | 4.5 | CCN(CC)C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL584554 | 201381 | None | 0 | Human | Functional | pIC50 | = | 7.8 | 7.8 | 1 | 14 | ChEMBL | 428 | 4 | 2 | 2 | 4.5 | CCN(CC)C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1 | 10.1016/j.bmcl.2011.06.070 | |||
90480414 | 190778 | None | 0 | Human | Functional | pIC50 | = | 7.8 | 7.8 | - | 1 | ChEMBL | 495 | 5 | 0 | 9 | 3.2 | COc1ccc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3nc(C)nc3C)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL5181702 | 190778 | None | 0 | Human | Functional | pIC50 | = | 7.8 | 7.8 | - | 1 | ChEMBL | 495 | 5 | 0 | 9 | 3.2 | COc1ccc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3nc(C)nc3C)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
45486561 | 200109 | None | 0 | Human | Functional | pIC50 | = | 7.8 | 7.8 | - | 1 | ChEMBL | 645 | 10 | 0 | 9 | 4.4 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(C(F)(F)F)c(F)c1)[C@H](C)c1nc2nc(OC)ccc2c(=O)n1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2009.07.021 | |||
CHEMBL570919 | 200109 | None | 0 | Human | Functional | pIC50 | = | 7.8 | 7.8 | - | 1 | ChEMBL | 645 | 10 | 0 | 9 | 4.4 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(C(F)(F)F)c(F)c1)[C@H](C)c1nc2nc(OC)ccc2c(=O)n1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2009.07.021 | |||
45486522 | 200983 | None | 0 | Human | Functional | pIC50 | = | 7.8 | 7.8 | - | 1 | ChEMBL | 617 | 10 | 0 | 8 | 5.0 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(C(F)(F)F)c(F)c1)C(C)c1nc2c(OC)nccn2c1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2009.07.021 | |||
CHEMBL577973 | 200983 | None | 0 | Human | Functional | pIC50 | = | 7.8 | 7.8 | - | 1 | ChEMBL | 617 | 10 | 0 | 8 | 5.0 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(C(F)(F)F)c(F)c1)C(C)c1nc2c(OC)nccn2c1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2009.07.021 | |||
45379650 | 201011 | None | 0 | Human | Functional | pIC50 | = | 7.7 | 7.7 | 1 | 2 | ChEMBL | 653 | 8 | 0 | 7 | 6.3 | C[C@H](c1nc2c(C3CC3)nccn2c1-c1ccc(C#N)cc1)N(CC1CCS(=O)(=O)CC1)C(=O)Cc1ccc(C(F)(F)F)c(F)c1 | 10.1016/j.bmcl.2009.07.021 | |||
CHEMBL578192 | 201011 | None | 0 | Human | Functional | pIC50 | = | 7.7 | 7.7 | 1 | 2 | ChEMBL | 653 | 8 | 0 | 7 | 6.3 | C[C@H](c1nc2c(C3CC3)nccn2c1-c1ccc(C#N)cc1)N(CC1CCS(=O)(=O)CC1)C(=O)Cc1ccc(C(F)(F)F)c(F)c1 | 10.1016/j.bmcl.2009.07.021 | |||
44580903 | 187945 | None | 0 | Human | Functional | pIC50 | = | 6.8 | 6.8 | - | 1 | ChEMBL | 466 | 5 | 0 | 3 | 5.0 | O=C1CC1N1CCCC(c2ccccc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C1 | 10.1016/j.bmcl.2008.07.115 | |||
CHEMBL496176 | 187945 | None | 0 | Human | Functional | pIC50 | = | 6.8 | 6.8 | - | 1 | ChEMBL | 466 | 5 | 0 | 3 | 5.0 | O=C1CC1N1CCCC(c2ccccc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C1 | 10.1016/j.bmcl.2008.07.115 | |||
46890724 | 7295 | None | 0 | Human | Functional | pIC50 | = | 6.7 | 6.7 | - | 1 | ChEMBL | 482 | 7 | 0 | 3 | 6.4 | O=S(=O)(c1ccc(Cl)cc1)N(Cc1ccc(-c2cccc(Cl)c2)cc1)Cc1ccccn1 | 10.1016/j.bmcl.2010.04.113 | |||
CHEMBL1086040 | 7295 | None | 0 | Human | Functional | pIC50 | = | 6.7 | 6.7 | - | 1 | ChEMBL | 482 | 7 | 0 | 3 | 6.4 | O=S(=O)(c1ccc(Cl)cc1)N(Cc1ccc(-c2cccc(Cl)c2)cc1)Cc1ccccn1 | 10.1016/j.bmcl.2010.04.113 | |||
56660098 | 64246 | None | 0 | Human | Functional | pIC50 | = | 6.7 | 6.7 | 1 | 2 | ChEMBL | 488 | 8 | 2 | 4 | 3.8 | COCCN(CCOC)C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1808997 | 64246 | None | 0 | Human | Functional | pIC50 | = | 6.7 | 6.7 | 1 | 2 | ChEMBL | 488 | 8 | 2 | 4 | 3.8 | COCCN(CCOC)C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1 | 10.1016/j.bmcl.2011.06.070 | |||
56673431 | 63954 | None | 0 | Rat | Functional | pIC50 | = | 7.7 | 7.7 | -63 | 3 | ChEMBL | 426 | 2 | 2 | 2 | 4.3 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CCCC1 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1806523 | 63954 | None | 0 | Rat | Functional | pIC50 | = | 7.7 | 7.7 | -63 | 3 | ChEMBL | 426 | 2 | 2 | 2 | 4.3 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CCCC1 | 10.1016/j.bmcl.2011.06.070 | |||
56670449 | 64263 | None | 0 | Mouse | Functional | pIC50 | = | 7.7 | 7.7 | 1 | 2 | ChEMBL | 442 | 2 | 3 | 3 | 3.2 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CC[C@H](O)C1 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1809014 | 64263 | None | 0 | Mouse | Functional | pIC50 | = | 7.7 | 7.7 | 1 | 2 | ChEMBL | 442 | 2 | 3 | 3 | 3.2 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CC[C@H](O)C1 | 10.1016/j.bmcl.2011.06.070 | |||
90479919 | 191483 | None | 0 | Human | Functional | pIC50 | = | 7.7 | 7.7 | - | 1 | ChEMBL | 480 | 4 | 0 | 9 | 2.9 | Cc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3nc(C)nc3C)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL5192208 | 191483 | None | 0 | Human | Functional | pIC50 | = | 7.7 | 7.7 | - | 1 | ChEMBL | 480 | 4 | 0 | 9 | 2.9 | Cc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3nc(C)nc3C)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
44406319 | 74179 | None | 0 | Human | Functional | pIC50 | = | 6.7 | 6.7 | - | 1 | ChEMBL | 581 | 8 | 3 | 4 | 5.5 | CCNC(=O)N1CCCN(c2ccc(C(=O)NCCc3ccccc3Cl)cc2NC(=O)c2cccc(Cl)c2)CC1 | 10.1016/j.bmcl.2005.09.020 | |||
CHEMBL202289 | 74179 | None | 0 | Human | Functional | pIC50 | = | 6.7 | 6.7 | - | 1 | ChEMBL | 581 | 8 | 3 | 4 | 5.5 | CCNC(=O)N1CCCN(c2ccc(C(=O)NCCc3ccccc3Cl)cc2NC(=O)c2cccc(Cl)c2)CC1 | 10.1016/j.bmcl.2005.09.020 | |||
117740035 | 153942 | None | 0 | Human | Functional | pIC50 | = | 6.7 | 6.7 | - | 1 | ChEMBL | 475 | 4 | 1 | 7 | 3.6 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cccn1 | 10.1021/acs.jmedchem.2c00676 | |||
CHEMBL3982804 | 153942 | None | 0 | Human | Functional | pIC50 | = | 6.7 | 6.7 | - | 1 | ChEMBL | 475 | 4 | 1 | 7 | 3.6 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cccn1 | 10.1021/acs.jmedchem.2c00676 | |||
46891078 | 6637 | None | 0 | Human | Functional | pIC50 | = | 6.7 | 6.7 | - | 1 | ChEMBL | 510 | 9 | 1 | 4 | 5.7 | O=C(NCc1cccs1)c1ccc(CN(Cc2ccccc2)S(=O)(=O)c2ccc(Cl)cc2)cc1 | 10.1016/j.bmcl.2010.04.113 | |||
CHEMBL1083316 | 6637 | None | 0 | Human | Functional | pIC50 | = | 6.7 | 6.7 | - | 1 | ChEMBL | 510 | 9 | 1 | 4 | 5.7 | O=C(NCc1cccs1)c1ccc(CN(Cc2ccccc2)S(=O)(=O)c2ccc(Cl)cc2)cc1 | 10.1016/j.bmcl.2010.04.113 | |||
46700871 | 7177 | None | 0 | Human | Functional | pIC50 | = | 6.7 | 6.7 | - | 1 | ChEMBL | 466 | 7 | 1 | 6 | 3.4 | N#Cc1ccc(S(=O)(=O)N(Cc2ccc(-c3nnn[nH]3)c(F)c2)Cc2ccccc2F)cc1 | 10.1016/j.bmcl.2010.04.113 | |||
CHEMBL1085509 | 7177 | None | 0 | Human | Functional | pIC50 | = | 6.7 | 6.7 | - | 1 | ChEMBL | 466 | 7 | 1 | 6 | 3.4 | N#Cc1ccc(S(=O)(=O)N(Cc2ccc(-c3nnn[nH]3)c(F)c2)Cc2ccccc2F)cc1 | 10.1016/j.bmcl.2010.04.113 | |||
45482814 | 200746 | None | 0 | Human | Functional | pIC50 | = | 5.7 | 5.7 | - | 1 | ChEMBL | 430 | 4 | 2 | 2 | 4.6 | CCN(CC)C(=O)[C@@H]1CC2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1 | 10.1016/j.bmcl.2009.09.002 | |||
CHEMBL575890 | 200746 | None | 0 | Human | Functional | pIC50 | = | 5.7 | 5.7 | - | 1 | ChEMBL | 430 | 4 | 2 | 2 | 4.6 | CCN(CC)C(=O)[C@@H]1CC2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1 | 10.1016/j.bmcl.2009.09.002 | |||
53318512 | 58199 | None | 0 | Human | Functional | pIC50 | = | 5.7 | 5.7 | - | 1 | ChEMBL | 447 | 5 | 1 | 6 | 3.3 | CNC(=O)c1cnc(N2CCN(C3CCN(Cc4cccs4)CC3)[C@@H](C)C2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
CHEMBL1681840 | 58199 | None | 0 | Human | Functional | pIC50 | = | 5.7 | 5.7 | - | 1 | ChEMBL | 447 | 5 | 1 | 6 | 3.3 | CNC(=O)c1cnc(N2CCN(C3CCN(Cc4cccs4)CC3)[C@@H](C)C2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
44253169 | 6818 | None | 0 | Human | Functional | pIC50 | = | 5.7 | 5.7 | - | 1 | ChEMBL | 468 | 9 | 1 | 3 | 4.9 | O=C(NCC1CC1)c1ccc(CN(Cc2ccccc2)S(=O)(=O)c2ccc(Cl)cc2)cc1 | 10.1016/j.bmcl.2010.04.113 | |||
CHEMBL1083929 | 6818 | None | 0 | Human | Functional | pIC50 | = | 5.7 | 5.7 | - | 1 | ChEMBL | 468 | 9 | 1 | 3 | 4.9 | O=C(NCC1CC1)c1ccc(CN(Cc2ccccc2)S(=O)(=O)c2ccc(Cl)cc2)cc1 | 10.1016/j.bmcl.2010.04.113 | |||
44569944 | 176811 | None | 0 | Human | Functional | pIC50 | = | 6.7 | 6.7 | - | 1 | ChEMBL | 461 | 4 | 1 | 5 | 3.1 | CC1(O)C[C@H]2CC[C@]1(CS(=O)(=O)N1CCN(c3ccc(C(F)(F)F)cn3)CC1)C2(C)C | 10.1016/j.bmcl.2008.11.008 | |||
CHEMBL459951 | 176811 | None | 0 | Human | Functional | pIC50 | = | 6.7 | 6.7 | - | 1 | ChEMBL | 461 | 4 | 1 | 5 | 3.1 | CC1(O)C[C@H]2CC[C@]1(CS(=O)(=O)N1CCN(c3ccc(C(F)(F)F)cn3)CC1)C2(C)C | 10.1016/j.bmcl.2008.11.008 | |||
44570029 | 178833 | None | 0 | Human | Functional | pIC50 | = | 6.7 | 6.7 | - | 1 | ChEMBL | 489 | 4 | 0 | 6 | 3.1 | CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCN(c3ccc(C(F)(F)F)cn3)CC1)C1(C2)OCCO1 | 10.1016/j.bmcl.2008.11.008 | |||
CHEMBL468468 | 178833 | None | 0 | Human | Functional | pIC50 | = | 6.7 | 6.7 | - | 1 | ChEMBL | 489 | 4 | 0 | 6 | 3.1 | CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCN(c3ccc(C(F)(F)F)cn3)CC1)C1(C2)OCCO1 | 10.1016/j.bmcl.2008.11.008 | |||
25265835 | 177833 | None | 0 | Mouse | Functional | pIC50 | = | 6.7 | 6.7 | -6 | 2 | ChEMBL | 479 | 4 | 1 | 5 | 3.3 | C[C@H]1CN(S(=O)(=O)C[C@]23CC[C@H](C[C@@H]2O)C3(C)C)CCN1c1ncc(C(F)(F)F)cc1F | 10.1016/j.bmcl.2008.11.008 | |||
CHEMBL464234 | 177833 | None | 0 | Mouse | Functional | pIC50 | = | 6.7 | 6.7 | -6 | 2 | ChEMBL | 479 | 4 | 1 | 5 | 3.3 | C[C@H]1CN(S(=O)(=O)C[C@]23CC[C@H](C[C@@H]2O)C3(C)C)CCN1c1ncc(C(F)(F)F)cc1F | 10.1016/j.bmcl.2008.11.008 | |||
44570220 | 184011 | None | 0 | Mouse | Functional | pIC50 | = | 6.7 | 6.7 | -6 | 2 | ChEMBL | 461 | 4 | 1 | 5 | 3.1 | C[C@H]1CN(S(=O)(=O)C[C@]23CC[C@H](C[C@@H]2O)C3(C)C)CCN1c1ccc(C(F)(F)F)cn1 | 10.1016/j.bmcl.2008.11.008 | |||
CHEMBL481198 | 184011 | None | 0 | Mouse | Functional | pIC50 | = | 6.7 | 6.7 | -6 | 2 | ChEMBL | 461 | 4 | 1 | 5 | 3.1 | C[C@H]1CN(S(=O)(=O)C[C@]23CC[C@H](C[C@@H]2O)C3(C)C)CCN1c1ccc(C(F)(F)F)cn1 | 10.1016/j.bmcl.2008.11.008 | |||
44570470 | 183934 | None | 0 | Human | Functional | pIC50 | = | 5.7 | 5.7 | - | 1 | ChEMBL | 462 | 4 | 0 | 4 | 3.7 | CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCN(c3ccc(C(F)(F)F)cc3F)CC1)C(=O)C2 | 10.1016/j.bmcl.2008.11.008 | |||
CHEMBL480608 | 183934 | None | 0 | Human | Functional | pIC50 | = | 5.7 | 5.7 | - | 1 | ChEMBL | 462 | 4 | 0 | 4 | 3.7 | CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCN(c3ccc(C(F)(F)F)cc3F)CC1)C(=O)C2 | 10.1016/j.bmcl.2008.11.008 | |||
44570141 | 184180 | None | 0 | Human | Functional | pIC50 | = | 5.7 | 5.7 | - | 1 | ChEMBL | 488 | 5 | 1 | 5 | 2.9 | CC(=O)NC1C[C@H]2CC[C@]1(CS(=O)(=O)N1CCN(c3ccc(C(F)(F)F)cn3)CC1)C2(C)C | 10.1016/j.bmcl.2008.11.008 | |||
CHEMBL482370 | 184180 | None | 0 | Human | Functional | pIC50 | = | 5.7 | 5.7 | - | 1 | ChEMBL | 488 | 5 | 1 | 5 | 2.9 | CC(=O)NC1C[C@H]2CC[C@]1(CS(=O)(=O)N1CCN(c3ccc(C(F)(F)F)cn3)CC1)C2(C)C | 10.1016/j.bmcl.2008.11.008 | |||
56673944 | 64284 | None | 0 | Human | Functional | pIC50 | = | 8.7 | 8.7 | 1 | 3 | ChEMBL | 497 | 5 | 1 | 4 | 4.3 | CN(C)CCn1cc2c3c(cccc31)C1=C[C@@H](C(=O)N3CCCC3)CN(C(=O)Nc3ccccc3)[C@@H]1C2 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1809039 | 64284 | None | 0 | Human | Functional | pIC50 | = | 8.7 | 8.7 | 1 | 3 | ChEMBL | 497 | 5 | 1 | 4 | 4.3 | CN(C)CCn1cc2c3c(cccc31)C1=C[C@@H](C(=O)N3CCCC3)CN(C(=O)Nc3ccccc3)[C@@H]1C2 | 10.1016/j.bmcl.2011.06.070 | |||
89725952 | 145568 | None | 0 | Human | Functional | pIC50 | = | 8.7 | 8.7 | - | 1 | ChEMBL | 601 | 5 | 1 | 9 | 4.5 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccc(C5CCN(C)CC5)cc4[nH]3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00676 | |||
CHEMBL3914555 | 145568 | None | 0 | Human | Functional | pIC50 | = | 8.7 | 8.7 | - | 1 | ChEMBL | 601 | 5 | 1 | 9 | 4.5 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccc(C5CCN(C)CC5)cc4[nH]3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00676 | |||
56680570 | 64252 | None | 0 | Mouse | Functional | pIC50 | = | 8.7 | 8.7 | 3 | 2 | ChEMBL | 438 | 2 | 2 | 2 | 4.8 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1C=CCCC1 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1809003 | 64252 | None | 0 | Mouse | Functional | pIC50 | = | 8.7 | 8.7 | 3 | 2 | ChEMBL | 438 | 2 | 2 | 2 | 4.8 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1C=CCCC1 | 10.1016/j.bmcl.2011.06.070 | |||
56663560 | 64265 | None | 0 | Mouse | Functional | pIC50 | = | 8.7 | 8.7 | 1 | 2 | ChEMBL | 444 | 2 | 2 | 2 | 4.4 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2cccc(F)c2)C1)N1CCCC1 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1809016 | 64265 | None | 0 | Mouse | Functional | pIC50 | = | 8.7 | 8.7 | 1 | 2 | ChEMBL | 444 | 2 | 2 | 2 | 4.4 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2cccc(F)c2)C1)N1CCCC1 | 10.1016/j.bmcl.2011.06.070 | |||
56673944 | 64284 | None | 0 | Mouse | Functional | pIC50 | = | 8.7 | 8.7 | -1 | 3 | ChEMBL | 497 | 5 | 1 | 4 | 4.3 | CN(C)CCn1cc2c3c(cccc31)C1=C[C@@H](C(=O)N3CCCC3)CN(C(=O)Nc3ccccc3)[C@@H]1C2 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1809039 | 64284 | None | 0 | Mouse | Functional | pIC50 | = | 8.7 | 8.7 | -1 | 3 | ChEMBL | 497 | 5 | 1 | 4 | 4.3 | CN(C)CCn1cc2c3c(cccc31)C1=C[C@@H](C(=O)N3CCCC3)CN(C(=O)Nc3ccccc3)[C@@H]1C2 | 10.1016/j.bmcl.2011.06.070 | |||
56673945 | 64285 | None | 0 | Mouse | Functional | pIC50 | = | 8.7 | 8.7 | 1 | 3 | ChEMBL | 523 | 5 | 1 | 4 | 4.8 | O=C([C@@H]1C=C2c3cccc4c3c(cn4CCN3CCCC3)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CCCC1 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1809040 | 64285 | None | 0 | Mouse | Functional | pIC50 | = | 8.7 | 8.7 | 1 | 3 | ChEMBL | 523 | 5 | 1 | 4 | 4.8 | O=C([C@@H]1C=C2c3cccc4c3c(cn4CCN3CCCC3)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CCCC1 | 10.1016/j.bmcl.2011.06.070 | |||
168270807 | 190156 | None | 0 | Human | Functional | pIC50 | = | 8.7 | 8.7 | - | 1 | ChEMBL | 532 | 6 | 0 | 10 | 3.5 | CCOc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3cnc4cccnc43)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL5172053 | 190156 | None | 0 | Human | Functional | pIC50 | = | 8.7 | 8.7 | - | 1 | ChEMBL | 532 | 6 | 0 | 10 | 3.5 | CCOc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3cnc4cccnc43)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
168282215 | 191054 | None | 0 | Human | Functional | pIC50 | = | 8.7 | 8.7 | - | 1 | ChEMBL | 531 | 6 | 0 | 9 | 4.1 | CCOc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3cnc4ccccc43)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL5185762 | 191054 | None | 0 | Human | Functional | pIC50 | = | 8.7 | 8.7 | - | 1 | ChEMBL | 531 | 6 | 0 | 9 | 4.1 | CCOc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3cnc4ccccc43)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
168280397 | 191389 | None | 0 | Human | Functional | pIC50 | = | 8.7 | 8.7 | - | 1 | ChEMBL | 495 | 6 | 0 | 9 | 3.3 | CCOc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3nccc3C)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL5190681 | 191389 | None | 0 | Human | Functional | pIC50 | = | 8.7 | 8.7 | - | 1 | ChEMBL | 495 | 6 | 0 | 9 | 3.3 | CCOc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3nccc3C)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
117739802 | 152013 | None | 0 | Human | Functional | pIC50 | = | 8.7 | 8.7 | - | 1 | ChEMBL | 586 | 7 | 2 | 10 | 3.6 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3cc(OCCO)ccc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | 10.1021/acs.jmedchem.2c00676 | |||
CHEMBL3966250 | 152013 | None | 0 | Human | Functional | pIC50 | = | 8.7 | 8.7 | - | 1 | ChEMBL | 586 | 7 | 2 | 10 | 3.6 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3cc(OCCO)ccc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | 10.1021/acs.jmedchem.2c00676 | |||
89726497 | 153195 | None | 0 | Human | Functional | pIC50 | = | 8.7 | 8.7 | - | 1 | ChEMBL | 587 | 5 | 2 | 9 | 4.1 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccc(C5CCNCC5)cc4[nH]3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00676 | |||
CHEMBL3976317 | 153195 | None | 0 | Human | Functional | pIC50 | = | 8.7 | 8.7 | - | 1 | ChEMBL | 587 | 5 | 2 | 9 | 4.1 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccc(C5CCNCC5)cc4[nH]3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00676 | |||
53322509 | 58225 | None | 0 | Human | Functional | pIC50 | = | 8.6 | 8.6 | - | 1 | ChEMBL | 489 | 6 | 1 | 5 | 4.3 | CCNC(=O)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4)CC3)[C@@H](C)C2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
CHEMBL1681868 | 58225 | None | 0 | Human | Functional | pIC50 | = | 8.6 | 8.6 | - | 1 | ChEMBL | 489 | 6 | 1 | 5 | 4.3 | CCNC(=O)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4)CC3)[C@@H](C)C2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
168281055 | 191110 | None | 0 | Human | Functional | pIC50 | = | 8.6 | 8.6 | - | 1 | ChEMBL | 509 | 6 | 0 | 9 | 3.6 | CCOc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3nc(C)cc3C)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL5186627 | 191110 | None | 0 | Human | Functional | pIC50 | = | 8.6 | 8.6 | - | 1 | ChEMBL | 509 | 6 | 0 | 9 | 3.6 | CCOc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3nc(C)cc3C)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
53317276 | 58227 | None | 0 | Human | Functional | pIC50 | = | 8.6 | 8.6 | - | 1 | ChEMBL | 557 | 7 | 1 | 5 | 5.9 | C[C@H]1CN(c2ncc(C(=O)NCC3CCCCC3)cc2Cl)CCN1C1CCN(Cc2ccc(Cl)cc2)CC1 | 10.1016/j.bmcl.2010.12.114 | |||
CHEMBL1681870 | 58227 | None | 0 | Human | Functional | pIC50 | = | 8.6 | 8.6 | - | 1 | ChEMBL | 557 | 7 | 1 | 5 | 5.9 | C[C@H]1CN(c2ncc(C(=O)NCC3CCCCC3)cc2Cl)CCN1C1CCN(Cc2ccc(Cl)cc2)CC1 | 10.1016/j.bmcl.2010.12.114 | |||
89726129 | 153640 | None | 4 | Human | Functional | pIC50 | = | 8.6 | 8.6 | 1288 | 2 | ChEMBL | 586 | 5 | 1 | 11 | 4.0 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccc(-c5noc(C)n5)cc4[nH]3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00676 | |||
CHEMBL3980161 | 153640 | None | 4 | Human | Functional | pIC50 | = | 8.6 | 8.6 | 1288 | 2 | ChEMBL | 586 | 5 | 1 | 11 | 4.0 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccc(-c5noc(C)n5)cc4[nH]3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00676 | |||
89726463 | 154193 | None | 0 | Human | Functional | pIC50 | = | 8.6 | 8.6 | - | 1 | ChEMBL | 542 | 4 | 2 | 8 | 3.5 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1c(=O)[nH]c2cccnc21 | 10.1021/acs.jmedchem.2c00676 | |||
CHEMBL3985006 | 154193 | None | 0 | Human | Functional | pIC50 | = | 8.6 | 8.6 | - | 1 | ChEMBL | 542 | 4 | 2 | 8 | 3.5 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1c(=O)[nH]c2cccnc21 | 10.1021/acs.jmedchem.2c00676 | |||
12207 | 275 | None | 12 | Human | Functional | pIC50 | = | 8.6 | 8.6 | -7 | 2 | ChEMBL | 534 | 4 | 0 | 9 | 3.6 | C[C@@H]1CN(CCN1C(=O)Cn1nc(C)nc1C)c1c(c2cnc(C(F)(F)F)nc2)nc(C(F)(F)F)s1 | 10.1021/acs.jmedchem.2c00675 | |||
87056189 | 275 | None | 12 | Human | Functional | pIC50 | = | 8.6 | 8.6 | -7 | 2 | ChEMBL | 534 | 4 | 0 | 9 | 3.6 | C[C@@H]1CN(CCN1C(=O)Cn1nc(C)nc1C)c1c(c2cnc(C(F)(F)F)nc2)nc(C(F)(F)F)s1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL5202301 | 275 | None | 12 | Human | Functional | pIC50 | = | 8.6 | 8.6 | -7 | 2 | ChEMBL | 534 | 4 | 0 | 9 | 3.6 | C[C@@H]1CN(CCN1C(=O)Cn1nc(C)nc1C)c1c(c2cnc(C(F)(F)F)nc2)nc(C(F)(F)F)s1 | 10.1021/acs.jmedchem.2c00675 | |||
117739228 | 145460 | None | 0 | Human | Functional | pIC50 | = | 8.6 | 8.6 | - | 1 | ChEMBL | 546 | 6 | 1 | 8 | 4.0 | Cc1nn(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccccc4[nH]3)C[C@H]2C)cc1CN(C)C | 10.1021/acs.jmedchem.2c00676 | |||
CHEMBL3913741 | 145460 | None | 0 | Human | Functional | pIC50 | = | 8.6 | 8.6 | - | 1 | ChEMBL | 546 | 6 | 1 | 8 | 4.0 | Cc1nn(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccccc4[nH]3)C[C@H]2C)cc1CN(C)C | 10.1021/acs.jmedchem.2c00676 | |||
12207 | 275 | None | 12 | Human | Functional | pIC50 | = | 8.6 | 8.6 | -7 | 2 | ChEMBL | 534 | 4 | 0 | 9 | 3.6 | C[C@@H]1CN(CCN1C(=O)Cn1nc(C)nc1C)c1c(c2cnc(C(F)(F)F)nc2)nc(C(F)(F)F)s1 | 10.1021/acs.jmedchem.2c00675 | |||
87056189 | 275 | None | 12 | Human | Functional | pIC50 | = | 8.6 | 8.6 | -7 | 2 | ChEMBL | 534 | 4 | 0 | 9 | 3.6 | C[C@@H]1CN(CCN1C(=O)Cn1nc(C)nc1C)c1c(c2cnc(C(F)(F)F)nc2)nc(C(F)(F)F)s1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL5202301 | 275 | None | 12 | Human | Functional | pIC50 | = | 8.6 | 8.6 | -7 | 2 | ChEMBL | 534 | 4 | 0 | 9 | 3.6 | C[C@@H]1CN(CCN1C(=O)Cn1nc(C)nc1C)c1c(c2cnc(C(F)(F)F)nc2)nc(C(F)(F)F)s1 | 10.1021/acs.jmedchem.2c00675 | |||
89726538 | 152825 | None | 0 | Human | Functional | pIC50 | = | 8.6 | 8.6 | - | 1 | ChEMBL | 560 | 4 | 1 | 8 | 4.8 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3cc(Cl)ccc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | 10.1021/acs.jmedchem.2c00676 | |||
CHEMBL3973196 | 152825 | None | 0 | Human | Functional | pIC50 | = | 8.6 | 8.6 | - | 1 | ChEMBL | 560 | 4 | 1 | 8 | 4.8 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3cc(Cl)ccc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | 10.1021/acs.jmedchem.2c00676 | |||
89726625 | 152560 | None | 0 | Human | Functional | pIC50 | = | 8.6 | 8.6 | - | 1 | ChEMBL | 536 | 4 | 1 | 8 | 3.9 | C[C@@H]1CN(c2sc(Br)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL3971056 | 152560 | None | 0 | Human | Functional | pIC50 | = | 8.6 | 8.6 | - | 1 | ChEMBL | 536 | 4 | 1 | 8 | 3.9 | C[C@@H]1CN(c2sc(Br)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | 10.1021/acs.jmedchem.2c00675 | |||
45784923 | 5660 | None | 21 | Human | Functional | pIC50 | = | 7.7 | 7.7 | - | 1 | ChEMBL | 605 | 9 | 0 | 7 | 6.1 | CCOc1ccc(-n2c([C@@H](C)N(Cc3cccnc3)C(=O)Cc3ccc(F)c(C(F)(F)F)c3)nc3ncccc3c2=O)cc1 | 10.1016/j.bmcl.2009.07.032 | |||
CHEMBL1077819 | 5660 | None | 21 | Human | Functional | pIC50 | = | 7.7 | 7.7 | - | 1 | ChEMBL | 605 | 9 | 0 | 7 | 6.1 | CCOc1ccc(-n2c([C@@H](C)N(Cc3cccnc3)C(=O)Cc3ccc(F)c(C(F)(F)F)c3)nc3ncccc3c2=O)cc1 | 10.1016/j.bmcl.2009.07.032 | |||
46883306 | 5667 | None | 0 | Human | Functional | pIC50 | = | 7.7 | 7.7 | - | 1 | ChEMBL | 597 | 9 | 1 | 7 | 5.2 | CCOc1ccc(-n2c([C@@H](C)N(C[C@H]3CCCN3)C(=O)Cc3ccc(F)c(C(F)(F)F)c3)nc3ncccc3c2=O)cc1 | 10.1016/j.bmcl.2009.07.032 | |||
CHEMBL1077826 | 5667 | None | 0 | Human | Functional | pIC50 | = | 7.7 | 7.7 | - | 1 | ChEMBL | 597 | 9 | 1 | 7 | 5.2 | CCOc1ccc(-n2c([C@@H](C)N(C[C@H]3CCCN3)C(=O)Cc3ccc(F)c(C(F)(F)F)c3)nc3ncccc3c2=O)cc1 | 10.1016/j.bmcl.2009.07.032 | |||
46883307 | 5668 | None | 0 | Human | Functional | pIC50 | = | 7.7 | 7.7 | - | 1 | ChEMBL | 625 | 9 | 0 | 7 | 5.8 | CCOc1ccc(-n2c([C@@H](C)N(CC3CCN(C)CC3)C(=O)Cc3ccc(F)c(C(F)(F)F)c3)nc3ncccc3c2=O)cc1 | 10.1016/j.bmcl.2009.07.032 | |||
CHEMBL1077827 | 5668 | None | 0 | Human | Functional | pIC50 | = | 7.7 | 7.7 | - | 1 | ChEMBL | 625 | 9 | 0 | 7 | 5.8 | CCOc1ccc(-n2c([C@@H](C)N(CC3CCN(C)CC3)C(=O)Cc3ccc(F)c(C(F)(F)F)c3)nc3ncccc3c2=O)cc1 | 10.1016/j.bmcl.2009.07.032 | |||
44455870 | 155604 | None | 0 | Human | Functional | pIC50 | = | 7.7 | 7.7 | - | 1 | ChEMBL | 604 | 9 | 0 | 6 | 6.7 | CCOc1ccc(-n2c([C@@H](C)N(Cc3cccnc3)C(=O)Cc3ccc(F)c(C(F)(F)F)c3)nc3ccccc3c2=O)cc1 | 10.1016/j.bmcl.2009.07.032 | |||
CHEMBL404201 | 155604 | None | 0 | Human | Functional | pIC50 | = | 7.7 | 7.7 | - | 1 | ChEMBL | 604 | 9 | 0 | 6 | 6.7 | CCOc1ccc(-n2c([C@@H](C)N(Cc3cccnc3)C(=O)Cc3ccc(F)c(C(F)(F)F)c3)nc3ccccc3c2=O)cc1 | 10.1016/j.bmcl.2009.07.032 | |||
53319881 | 58223 | None | 0 | Human | Functional | pIC50 | = | 7.7 | 7.7 | - | 1 | ChEMBL | 501 | 6 | 1 | 5 | 4.9 | C[C@H]1CN(c2ncc(NC(=O)C3CC3)cc2Cl)CCN1C1CCN(Cc2ccc(Cl)cc2)CC1 | 10.1016/j.bmcl.2010.12.114 | |||
CHEMBL1681866 | 58223 | None | 0 | Human | Functional | pIC50 | = | 7.7 | 7.7 | - | 1 | ChEMBL | 501 | 6 | 1 | 5 | 4.9 | C[C@H]1CN(c2ncc(NC(=O)C3CC3)cc2Cl)CCN1C1CCN(Cc2ccc(Cl)cc2)CC1 | 10.1016/j.bmcl.2010.12.114 | |||
44453616 | 95218 | None | 0 | Human | Functional | pIC50 | = | 7.7 | 7.7 | 8 | 2 | ChEMBL | 495 | 8 | 1 | 6 | 4.7 | CN(CCCn1c(=N)n(CC(=O)c2ccc(Cl)cc2)c2cccc(Cl)c21)C(=O)c1ccccn1 | 10.1016/j.bmcl.2008.02.049 | |||
CHEMBL255798 | 95218 | None | 0 | Human | Functional | pIC50 | = | 7.7 | 7.7 | 8 | 2 | ChEMBL | 495 | 8 | 1 | 6 | 4.7 | CN(CCCn1c(=N)n(CC(=O)c2ccc(Cl)cc2)c2cccc(Cl)c21)C(=O)c1ccccn1 | 10.1016/j.bmcl.2008.02.049 | |||
44453558 | 95486 | None | 0 | Human | Functional | pIC50 | = | 7.7 | 7.7 | 3 | 2 | ChEMBL | 571 | 6 | 1 | 6 | 6.2 | N=c1n(CC(=O)c2ccc(Cl)cc2)c2cccc(Cl)c2n1C[C@@H]1CCCN(C(=O)c2cccc3cccnc23)C1 | 10.1016/j.bmcl.2008.02.049 | |||
CHEMBL257038 | 95486 | None | 0 | Human | Functional | pIC50 | = | 7.7 | 7.7 | 3 | 2 | ChEMBL | 571 | 6 | 1 | 6 | 6.2 | N=c1n(CC(=O)c2ccc(Cl)cc2)c2cccc(Cl)c2n1C[C@@H]1CCCN(C(=O)c2cccc3cccnc23)C1 | 10.1016/j.bmcl.2008.02.049 | |||
44453583 | 97975 | None | 0 | Human | Functional | pIC50 | = | 7.7 | 7.7 | 4 | 2 | ChEMBL | 571 | 6 | 1 | 6 | 6.2 | N=c1n(CC(=O)c2ccc(Cl)cc2)c2cccc(Cl)c2n1CC1CCCN(C(=O)c2cccc3cccnc23)C1 | 10.1016/j.bmcl.2008.02.049 | |||
CHEMBL272522 | 97975 | None | 0 | Human | Functional | pIC50 | = | 7.7 | 7.7 | 4 | 2 | ChEMBL | 571 | 6 | 1 | 6 | 6.2 | N=c1n(CC(=O)c2ccc(Cl)cc2)c2cccc(Cl)c2n1CC1CCCN(C(=O)c2cccc3cccnc23)C1 | 10.1016/j.bmcl.2008.02.049 | |||
44453640 | 97988 | None | 0 | Human | Functional | pIC50 | = | 7.7 | 7.7 | 4 | 2 | ChEMBL | 524 | 9 | 1 | 6 | 5.3 | COc1ccccc1C(=O)N(C)CCCn1c(=N)n(CC(=O)c2ccc(Cl)cc2)c2cccc(Cl)c21 | 10.1016/j.bmcl.2008.02.049 | |||
CHEMBL272558 | 97988 | None | 0 | Human | Functional | pIC50 | = | 7.7 | 7.7 | 4 | 2 | ChEMBL | 524 | 9 | 1 | 6 | 5.3 | COc1ccccc1C(=O)N(C)CCCn1c(=N)n(CC(=O)c2ccc(Cl)cc2)c2cccc(Cl)c21 | 10.1016/j.bmcl.2008.02.049 | |||
44453470 | 155405 | None | 0 | Human | Functional | pIC50 | = | 7.7 | 7.7 | 3 | 2 | ChEMBL | 571 | 7 | 1 | 6 | 6.4 | N=c1n(CC(=O)c2ccc(Cl)cc2)c2cccc(Cl)c2n1CC[C@@H]1CCCN1C(=O)c1cccc2cccnc12 | 10.1016/j.bmcl.2008.02.049 | |||
CHEMBL403040 | 155405 | None | 0 | Human | Functional | pIC50 | = | 7.7 | 7.7 | 3 | 2 | ChEMBL | 571 | 7 | 1 | 6 | 6.4 | N=c1n(CC(=O)c2ccc(Cl)cc2)c2cccc(Cl)c2n1CC[C@@H]1CCCN1C(=O)c1cccc2cccnc12 | 10.1016/j.bmcl.2008.02.049 | |||
44453530 | 155443 | None | 0 | Human | Functional | pIC50 | = | 7.7 | 7.7 | 3 | 2 | ChEMBL | 571 | 6 | 1 | 6 | 6.2 | N=c1n(CC(=O)c2ccc(Cl)cc2)c2cccc(Cl)c2n1C[C@H]1CCCN(C(=O)c2cccc3cccnc23)C1 | 10.1016/j.bmcl.2008.02.049 | |||
CHEMBL403290 | 155443 | None | 0 | Human | Functional | pIC50 | = | 7.7 | 7.7 | 3 | 2 | ChEMBL | 571 | 6 | 1 | 6 | 6.2 | N=c1n(CC(=O)c2ccc(Cl)cc2)c2cccc(Cl)c2n1C[C@H]1CCCN(C(=O)c2cccc3cccnc23)C1 | 10.1016/j.bmcl.2008.02.049 | |||
44453643 | 158957 | None | 0 | Human | Functional | pIC50 | = | 7.7 | 7.7 | 10 | 2 | ChEMBL | 494 | 8 | 1 | 5 | 5.3 | CN(CCCn1c(=N)n(CC(=O)c2ccc(Cl)cc2)c2cccc(Cl)c21)C(=O)c1ccccc1 | 10.1016/j.bmcl.2008.02.049 | |||
CHEMBL409499 | 158957 | None | 0 | Human | Functional | pIC50 | = | 7.7 | 7.7 | 10 | 2 | ChEMBL | 494 | 8 | 1 | 5 | 5.3 | CN(CCCn1c(=N)n(CC(=O)c2ccc(Cl)cc2)c2cccc(Cl)c21)C(=O)c1ccccc1 | 10.1016/j.bmcl.2008.02.049 | |||
44453585 | 166576 | None | 0 | Human | Functional | pIC50 | = | 7.7 | 7.7 | 2 | 2 | ChEMBL | 545 | 8 | 1 | 6 | 5.8 | CN(CCCn1c(=N)n(CC(=O)c2ccc(Cl)cc2)c2cccc(Cl)c21)C(=O)c1cccc2cccnc12 | 10.1016/j.bmcl.2008.02.049 | |||
CHEMBL427833 | 166576 | None | 0 | Human | Functional | pIC50 | = | 7.7 | 7.7 | 2 | 2 | ChEMBL | 545 | 8 | 1 | 6 | 5.8 | CN(CCCn1c(=N)n(CC(=O)c2ccc(Cl)cc2)c2cccc(Cl)c21)C(=O)c1cccc2cccnc12 | 10.1016/j.bmcl.2008.02.049 | |||
56667007 | 64264 | None | 0 | Human | Functional | pIC50 | = | 7.7 | 7.7 | -1 | 2 | ChEMBL | 444 | 2 | 2 | 2 | 4.4 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2F)C1)N1CCCC1 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1809015 | 64264 | None | 0 | Human | Functional | pIC50 | = | 7.7 | 7.7 | -1 | 2 | ChEMBL | 444 | 2 | 2 | 2 | 4.4 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2F)C1)N1CCCC1 | 10.1016/j.bmcl.2011.06.070 | |||
168270807 | 190156 | None | 0 | Human | Functional | pIC50 | = | 7.7 | 7.7 | - | 1 | ChEMBL | 532 | 6 | 0 | 10 | 3.5 | CCOc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3cnc4cccnc43)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL5172053 | 190156 | None | 0 | Human | Functional | pIC50 | = | 7.7 | 7.7 | - | 1 | ChEMBL | 532 | 6 | 0 | 10 | 3.5 | CCOc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3cnc4cccnc43)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
45484739 | 199754 | None | 0 | Human | Functional | pIC50 | = | 7.7 | 7.7 | - | 1 | ChEMBL | 558 | 9 | 1 | 7 | 4.2 | N#Cc1ccc(CN2CCC(N3CCN(c4ncc(C(=O)NCCOc5ccccc5)cc4Cl)CC3)CC2)cc1 | 10.1016/j.bmcl.2009.07.020 | |||
CHEMBL568676 | 199754 | None | 0 | Human | Functional | pIC50 | = | 7.7 | 7.7 | - | 1 | ChEMBL | 558 | 9 | 1 | 7 | 4.2 | N#Cc1ccc(CN2CCC(N3CCN(c4ncc(C(=O)NCCOc5ccccc5)cc4Cl)CC3)CC2)cc1 | 10.1016/j.bmcl.2009.07.020 | |||
11296495 | 72755 | None | 22 | Human | Functional | pIC50 | = | 7.7 | 7.7 | - | 1 | ChEMBL | 615 | 8 | 3 | 4 | 6.1 | CCNC(=O)N1CCCN(c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2NC(=O)c2cccc(Cl)c2)CC1 | 10.1016/j.bmcl.2005.09.020 | |||
CHEMBL199839 | 72755 | None | 22 | Human | Functional | pIC50 | = | 7.7 | 7.7 | - | 1 | ChEMBL | 615 | 8 | 3 | 4 | 6.1 | CCNC(=O)N1CCCN(c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2NC(=O)c2cccc(Cl)c2)CC1 | 10.1016/j.bmcl.2005.09.020 | |||
44453364 | 160678 | None | 0 | Human | Functional | pIC50 | = | 6.7 | 6.7 | - | 1 | ChEMBL | 460 | 8 | 1 | 5 | 4.5 | CN(Cc1ccccc1)C(=O)CCn1c(=N)n(CC(=O)c2ccc(Cl)cc2)c2ccccc21 | 10.1016/j.bmcl.2008.02.049 | |||
CHEMBL411273 | 160678 | None | 0 | Human | Functional | pIC50 | = | 6.7 | 6.7 | - | 1 | ChEMBL | 460 | 8 | 1 | 5 | 4.5 | CN(Cc1ccccc1)C(=O)CCn1c(=N)n(CC(=O)c2ccc(Cl)cc2)c2ccccc21 | 10.1016/j.bmcl.2008.02.049 | |||
44253168 | 7343 | None | 0 | Human | Functional | pIC50 | = | 6.7 | 6.7 | - | 1 | ChEMBL | 469 | 9 | 1 | 4 | 4.3 | O=C(NCC1CC1)c1ccc(CN(Cc2ccccn2)S(=O)(=O)c2ccc(Cl)cc2)cc1 | 10.1016/j.bmcl.2010.04.113 | |||
CHEMBL1086236 | 7343 | None | 0 | Human | Functional | pIC50 | = | 6.7 | 6.7 | - | 1 | ChEMBL | 469 | 9 | 1 | 4 | 4.3 | O=C(NCC1CC1)c1ccc(CN(Cc2ccccn2)S(=O)(=O)c2ccc(Cl)cc2)cc1 | 10.1016/j.bmcl.2010.04.113 | |||
56667006 | 64261 | None | 0 | Human | Functional | pIC50 | = | 6.7 | 6.7 | -2 | 2 | ChEMBL | 472 | 2 | 4 | 4 | 2.6 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CC[C@@H](O)[C@@H](O)C1 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1809012 | 64261 | None | 0 | Human | Functional | pIC50 | = | 6.7 | 6.7 | -2 | 2 | ChEMBL | 472 | 2 | 4 | 4 | 2.6 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CC[C@@H](O)[C@@H](O)C1 | 10.1016/j.bmcl.2011.06.070 | |||
44406196 | 72721 | None | 0 | Human | Functional | pIC50 | = | 6.7 | 6.7 | - | 1 | ChEMBL | 599 | 8 | 3 | 4 | 5.6 | CCNC(=O)N1CCCN(c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2NC(=O)c2ccc(F)cc2)CC1 | 10.1016/j.bmcl.2005.09.020 | |||
CHEMBL199698 | 72721 | None | 0 | Human | Functional | pIC50 | = | 6.7 | 6.7 | - | 1 | ChEMBL | 599 | 8 | 3 | 4 | 5.6 | CCNC(=O)N1CCCN(c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2NC(=O)c2ccc(F)cc2)CC1 | 10.1016/j.bmcl.2005.09.020 | |||
44580860 | 188110 | None | 0 | Human | Functional | pIC50 | = | 5.7 | 5.7 | - | 1 | ChEMBL | 498 | 7 | 0 | 4 | 4.4 | COCCN1C(=O)CCC(c2ccccc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C1=O | 10.1016/j.bmcl.2008.07.115 | |||
CHEMBL497396 | 188110 | None | 0 | Human | Functional | pIC50 | = | 5.7 | 5.7 | - | 1 | ChEMBL | 498 | 7 | 0 | 4 | 4.4 | COCCN1C(=O)CCC(c2ccccc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C1=O | 10.1016/j.bmcl.2008.07.115 | |||
46890727 | 7142 | None | 0 | Human | Functional | pIC50 | = | 6.7 | 6.7 | - | 1 | ChEMBL | 507 | 9 | 0 | 5 | 5.6 | O=[N+]([O-])c1cccc(Cc2ccc(CN(Cc3ccccn3)S(=O)(=O)c3ccc(Cl)cc3)cc2)c1 | 10.1016/j.bmcl.2010.04.113 | |||
CHEMBL1085327 | 7142 | None | 0 | Human | Functional | pIC50 | = | 6.7 | 6.7 | - | 1 | ChEMBL | 507 | 9 | 0 | 5 | 5.6 | O=[N+]([O-])c1cccc(Cc2ccc(CN(Cc3ccccn3)S(=O)(=O)c3ccc(Cl)cc3)cc2)c1 | 10.1016/j.bmcl.2010.04.113 | |||
53318514 | 58204 | None | 0 | Human | Functional | pIC50 | = | 6.7 | 6.7 | - | 1 | ChEMBL | 489 | 4 | 1 | 5 | 3.6 | CNC(=O)c1cnc(N2CCN(C3CCN(C(=O)c4ccc(Cl)cc4)CC3)[C@@H](C)C2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
CHEMBL1681845 | 58204 | None | 0 | Human | Functional | pIC50 | = | 6.7 | 6.7 | - | 1 | ChEMBL | 489 | 4 | 1 | 5 | 3.6 | CNC(=O)c1cnc(N2CCN(C3CCN(C(=O)c4ccc(Cl)cc4)CC3)[C@@H](C)C2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
24739388 | 187917 | None | 0 | Human | Functional | pIC50 | = | 6.7 | 6.7 | - | 1 | ChEMBL | 491 | 5 | 1 | 3 | 3.9 | NS(=O)(=O)N1CCCC(c2ccccc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C1 | 10.1016/j.bmcl.2008.07.115 | |||
CHEMBL495940 | 187917 | None | 0 | Human | Functional | pIC50 | = | 6.7 | 6.7 | - | 1 | ChEMBL | 491 | 5 | 1 | 3 | 3.9 | NS(=O)(=O)N1CCCC(c2ccccc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C1 | 10.1016/j.bmcl.2008.07.115 | |||
168293706 | 192273 | None | 0 | Human | Functional | pIC50 | = | 5.7 | 5.7 | - | 1 | ChEMBL | 519 | 5 | 2 | 8 | 3.3 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1ccc(C(=O)O)n1 | 10.1021/acs.jmedchem.2c00676 | |||
CHEMBL5203982 | 192273 | None | 0 | Human | Functional | pIC50 | = | 5.7 | 5.7 | - | 1 | ChEMBL | 519 | 5 | 2 | 8 | 3.3 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1ccc(C(=O)O)n1 | 10.1021/acs.jmedchem.2c00676 | |||
44406362 | 135815 | None | 0 | Human | Functional | pIC50 | = | 5.7 | 5.7 | - | 1 | ChEMBL | 497 | 7 | 3 | 4 | 4.0 | CCNC(=O)N1CCCN(c2ccc(C(=O)NCC3CC3)cc2NC(=O)c2cccc(Cl)c2)CC1 | 10.1016/j.bmcl.2005.09.020 | |||
CHEMBL373008 | 135815 | None | 0 | Human | Functional | pIC50 | = | 5.7 | 5.7 | - | 1 | ChEMBL | 497 | 7 | 3 | 4 | 4.0 | CCNC(=O)N1CCCN(c2ccc(C(=O)NCC3CC3)cc2NC(=O)c2cccc(Cl)c2)CC1 | 10.1016/j.bmcl.2005.09.020 | |||
46890726 | 7354 | None | 0 | Human | Functional | pIC50 | = | 6.7 | 6.7 | - | 1 | ChEMBL | 462 | 8 | 0 | 3 | 5.7 | O=S(=O)(c1ccc(Cl)cc1)N(Cc1ccc(Cc2ccccc2)cc1)Cc1ccccn1 | 10.1016/j.bmcl.2010.04.113 | |||
CHEMBL1086280 | 7354 | None | 0 | Human | Functional | pIC50 | = | 6.7 | 6.7 | - | 1 | ChEMBL | 462 | 8 | 0 | 3 | 5.7 | O=S(=O)(c1ccc(Cl)cc1)N(Cc1ccc(Cc2ccccc2)cc1)Cc1ccccn1 | 10.1016/j.bmcl.2010.04.113 | |||
56673939 | 64258 | None | 0 | Human | Functional | pIC50 | = | 6.7 | 6.7 | - | 1 | ChEMBL | 470 | 2 | 2 | 3 | 4.3 | CC1CN(C(=O)[C@@H]2C=C3c4cccc5[nH]cc(c45)C[C@H]3N(C(=O)Nc3ccccc3)C2)CC(C)O1 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1809009 | 64258 | None | 0 | Human | Functional | pIC50 | = | 6.7 | 6.7 | - | 1 | ChEMBL | 470 | 2 | 2 | 3 | 4.3 | CC1CN(C(=O)[C@@H]2C=C3c4cccc5[nH]cc(c45)C[C@H]3N(C(=O)Nc3ccccc3)C2)CC(C)O1 | 10.1016/j.bmcl.2011.06.070 | |||
15604776 | 133674 | None | 0 | Human | Functional | pIC50 | = | 5.7 | 5.7 | - | 1 | ChEMBL | 485 | 6 | 3 | 4 | 4.0 | CCNC(=O)N1CCCN(c2ccc(C(=O)NC(C)C)cc2NC(=O)c2cccc(Cl)c2)CC1 | 10.1016/j.bmcl.2005.09.020 | |||
CHEMBL371298 | 133674 | None | 0 | Human | Functional | pIC50 | = | 5.7 | 5.7 | - | 1 | ChEMBL | 485 | 6 | 3 | 4 | 4.0 | CCNC(=O)N1CCCN(c2ccc(C(=O)NC(C)C)cc2NC(=O)c2cccc(Cl)c2)CC1 | 10.1016/j.bmcl.2005.09.020 | |||
46883311 | 5671 | None | 0 | Human | Functional | pIC50 | = | 7.7 | 7.7 | - | 1 | ChEMBL | 634 | 11 | 0 | 8 | 4.9 | CCOc1ccc(-n2c([C@@H](C)N(CCS(=O)(=O)CC)C(=O)Cc3ccc(F)c(C(F)(F)F)c3)nc3ncccc3c2=O)cc1 | 10.1016/j.bmcl.2009.07.032 | |||
CHEMBL1077830 | 5671 | None | 0 | Human | Functional | pIC50 | = | 7.7 | 7.7 | - | 1 | ChEMBL | 634 | 11 | 0 | 8 | 4.9 | CCOc1ccc(-n2c([C@@H](C)N(CCS(=O)(=O)CC)C(=O)Cc3ccc(F)c(C(F)(F)F)c3)nc3ncccc3c2=O)cc1 | 10.1016/j.bmcl.2009.07.032 | |||
53317277 | 58228 | None | 0 | Human | Functional | pIC50 | = | 7.7 | 7.7 | - | 1 | ChEMBL | 573 | 6 | 1 | 5 | 6.1 | C[C@H]1CN(c2ncc(C(=O)Nc3ccc(F)c(F)c3)cc2Cl)CCN1C1CCN(Cc2ccc(Cl)cc2)CC1 | 10.1016/j.bmcl.2010.12.114 | |||
CHEMBL1681871 | 58228 | None | 0 | Human | Functional | pIC50 | = | 7.7 | 7.7 | - | 1 | ChEMBL | 573 | 6 | 1 | 5 | 6.1 | C[C@H]1CN(c2ncc(C(=O)Nc3ccc(F)c(F)c3)cc2Cl)CCN1C1CCN(Cc2ccc(Cl)cc2)CC1 | 10.1016/j.bmcl.2010.12.114 | |||
56663559 | 64262 | None | 0 | Human | Functional | pIC50 | = | 7.7 | 7.7 | - | 1 | ChEMBL | 442 | 2 | 3 | 3 | 3.2 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CC[C@@H](O)C1 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1809013 | 64262 | None | 0 | Human | Functional | pIC50 | = | 7.7 | 7.7 | - | 1 | ChEMBL | 442 | 2 | 3 | 3 | 3.2 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CC[C@@H](O)C1 | 10.1016/j.bmcl.2011.06.070 | |||
45486533 | 200094 | None | 0 | Human | Functional | pIC50 | = | 7.7 | 7.7 | - | 1 | ChEMBL | 635 | 8 | 0 | 7 | 6.1 | C[C@H](c1nc2c(C3CC3)nccn2c1-c1ccc(C#N)cc1)N(CC1CCS(=O)(=O)CC1)C(=O)Cc1ccc(C(F)(F)F)cc1 | 10.1016/j.bmcl.2009.07.021 | |||
CHEMBL570858 | 200094 | None | 0 | Human | Functional | pIC50 | = | 7.7 | 7.7 | - | 1 | ChEMBL | 635 | 8 | 0 | 7 | 6.1 | C[C@H](c1nc2c(C3CC3)nccn2c1-c1ccc(C#N)cc1)N(CC1CCS(=O)(=O)CC1)C(=O)Cc1ccc(C(F)(F)F)cc1 | 10.1016/j.bmcl.2009.07.021 | |||
45486556 | 200130 | None | 0 | Human | Functional | pIC50 | = | 7.7 | 7.7 | - | 1 | ChEMBL | 645 | 10 | 0 | 9 | 4.4 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc2nc(OC)ccc2c(=O)n1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2009.07.021 | |||
CHEMBL571081 | 200130 | None | 0 | Human | Functional | pIC50 | = | 7.7 | 7.7 | - | 1 | ChEMBL | 645 | 10 | 0 | 9 | 4.4 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc2nc(OC)ccc2c(=O)n1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2009.07.021 | |||
46883298 | 5659 | None | 0 | Human | Functional | pIC50 | = | 6.7 | 6.7 | - | 1 | ChEMBL | 620 | 10 | 0 | 7 | 6.6 | CCOc1ccc(-n2c([C@@H](C)N(Cc3cccnc3)C(=O)Cc3ccc(OC(F)(F)F)c(F)c3)nc3ccccc3c2=O)cc1 | 10.1016/j.bmcl.2009.07.032 | |||
CHEMBL1077818 | 5659 | None | 0 | Human | Functional | pIC50 | = | 6.7 | 6.7 | - | 1 | ChEMBL | 620 | 10 | 0 | 7 | 6.6 | CCOc1ccc(-n2c([C@@H](C)N(Cc3cccnc3)C(=O)Cc3ccc(OC(F)(F)F)c(F)c3)nc3ccccc3c2=O)cc1 | 10.1016/j.bmcl.2009.07.032 | |||
53326434 | 58209 | None | 0 | Human | Functional | pIC50 | = | 6.7 | 6.7 | - | 1 | ChEMBL | 619 | 7 | 1 | 5 | 6.8 | C[C@@H]1CN(C2CCN(Cc3ccc(Cl)cc3)CC2)CCN1c1ncc(C(=O)NCc2ccc(Cl)c(Cl)c2)cc1Cl | 10.1016/j.bmcl.2010.12.114 | |||
CHEMBL1681852 | 58209 | None | 0 | Human | Functional | pIC50 | = | 6.7 | 6.7 | - | 1 | ChEMBL | 619 | 7 | 1 | 5 | 6.8 | C[C@@H]1CN(C2CCN(Cc3ccc(Cl)cc3)CC2)CCN1c1ncc(C(=O)NCc2ccc(Cl)c(Cl)c2)cc1Cl | 10.1016/j.bmcl.2010.12.114 | |||
168290369 | 192025 | None | 0 | Human | Functional | pIC50 | = | 6.7 | 6.7 | - | 1 | ChEMBL | 607 | 5 | 1 | 10 | 3.6 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccc(N5CCOCC5)c(F)c4[nH]3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00676 | |||
CHEMBL5200180 | 192025 | None | 0 | Human | Functional | pIC50 | = | 6.7 | 6.7 | - | 1 | ChEMBL | 607 | 5 | 1 | 10 | 3.6 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccc(N5CCOCC5)c(F)c4[nH]3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00676 | |||
56670454 | 64278 | None | 0 | Human | Functional | pIC50 | = | 5.7 | 5.7 | - | 1 | ChEMBL | 440 | 3 | 2 | 2 | 3.9 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)NCc2ccccc2)C1)N1CCCC1 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1809033 | 64278 | None | 0 | Human | Functional | pIC50 | = | 5.7 | 5.7 | - | 1 | ChEMBL | 440 | 3 | 2 | 2 | 3.9 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)NCc2ccccc2)C1)N1CCCC1 | 10.1016/j.bmcl.2011.06.070 | |||
12207 | 275 | None | 12 | Human | Functional | pIC50 | = | 6.7 | 6.7 | -7 | 2 | ChEMBL | 534 | 4 | 0 | 9 | 3.6 | C[C@@H]1CN(CCN1C(=O)Cn1nc(C)nc1C)c1c(c2cnc(C(F)(F)F)nc2)nc(C(F)(F)F)s1 | 10.1021/acs.jmedchem.2c00675 | |||
87056189 | 275 | None | 12 | Human | Functional | pIC50 | = | 6.7 | 6.7 | -7 | 2 | ChEMBL | 534 | 4 | 0 | 9 | 3.6 | C[C@@H]1CN(CCN1C(=O)Cn1nc(C)nc1C)c1c(c2cnc(C(F)(F)F)nc2)nc(C(F)(F)F)s1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL5202301 | 275 | None | 12 | Human | Functional | pIC50 | = | 6.7 | 6.7 | -7 | 2 | ChEMBL | 534 | 4 | 0 | 9 | 3.6 | C[C@@H]1CN(CCN1C(=O)Cn1nc(C)nc1C)c1c(c2cnc(C(F)(F)F)nc2)nc(C(F)(F)F)s1 | 10.1021/acs.jmedchem.2c00675 | |||
34747495 | 6817 | None | 0 | Human | Functional | pIC50 | = | 5.6 | 5.6 | - | 1 | ChEMBL | 498 | 9 | 1 | 4 | 4.6 | O=C(NC[C@@H]1CCCO1)c1ccc(CN(Cc2ccccc2)S(=O)(=O)c2ccc(Cl)cc2)cc1 | 10.1016/j.bmcl.2010.04.113 | |||
CHEMBL1083928 | 6817 | None | 0 | Human | Functional | pIC50 | = | 5.6 | 5.6 | - | 1 | ChEMBL | 498 | 9 | 1 | 4 | 4.6 | O=C(NC[C@@H]1CCCO1)c1ccc(CN(Cc2ccccc2)S(=O)(=O)c2ccc(Cl)cc2)cc1 | 10.1016/j.bmcl.2010.04.113 | |||
46883300 | 5661 | None | 0 | Human | Functional | pIC50 | = | 7.6 | 7.6 | - | 1 | ChEMBL | 605 | 9 | 0 | 7 | 6.1 | CCOc1ccc(-n2c([C@@H](C)N(Cc3cccnc3)C(=O)Cc3ccc(F)c(C(F)(F)F)c3)nc3cnccc3c2=O)cc1 | 10.1016/j.bmcl.2009.07.032 | |||
CHEMBL1077820 | 5661 | None | 0 | Human | Functional | pIC50 | = | 7.6 | 7.6 | - | 1 | ChEMBL | 605 | 9 | 0 | 7 | 6.1 | CCOc1ccc(-n2c([C@@H](C)N(Cc3cccnc3)C(=O)Cc3ccc(F)c(C(F)(F)F)c3)nc3cnccc3c2=O)cc1 | 10.1016/j.bmcl.2009.07.032 | |||
53321187 | 58239 | None | 0 | Human | Functional | pIC50 | = | 7.6 | 7.6 | - | 1 | ChEMBL | 517 | 7 | 1 | 5 | 4.9 | CCNC(=O)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4)CC3)[C@@H](C(C)C)C2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
CHEMBL1681883 | 58239 | None | 0 | Human | Functional | pIC50 | = | 7.6 | 7.6 | - | 1 | ChEMBL | 517 | 7 | 1 | 5 | 4.9 | CCNC(=O)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4)CC3)[C@@H](C(C)C)C2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
117739351 | 148559 | None | 0 | Human | Functional | pIC50 | = | 7.6 | 7.6 | - | 1 | ChEMBL | 536 | 4 | 1 | 6 | 5.5 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cc1cccc2cccnc12 | 10.1021/acs.jmedchem.2c00676 | |||
CHEMBL3938074 | 148559 | None | 0 | Human | Functional | pIC50 | = | 7.6 | 7.6 | - | 1 | ChEMBL | 536 | 4 | 1 | 6 | 5.5 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cc1cccc2cccnc12 | 10.1021/acs.jmedchem.2c00676 | |||
168273685 | 190500 | None | 0 | Human | Functional | pIC50 | = | 7.6 | 7.6 | - | 1 | ChEMBL | 531 | 6 | 0 | 9 | 4.1 | CCOc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3ccc4cnccc43)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL5177520 | 190500 | None | 0 | Human | Functional | pIC50 | = | 7.6 | 7.6 | - | 1 | ChEMBL | 531 | 6 | 0 | 9 | 4.1 | CCOc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3ccc4cnccc43)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
44453295 | 97771 | None | 0 | Human | Functional | pIC50 | = | 5.6 | 5.6 | - | 1 | ChEMBL | 446 | 7 | 1 | 5 | 4.2 | CN(CCn1c(=N)n(CC(=O)c2ccc(Cl)cc2)c2ccccc21)C(=O)c1ccccc1 | 10.1016/j.bmcl.2008.02.049 | |||
CHEMBL271459 | 97771 | None | 0 | Human | Functional | pIC50 | = | 5.6 | 5.6 | - | 1 | ChEMBL | 446 | 7 | 1 | 5 | 4.2 | CN(CCn1c(=N)n(CC(=O)c2ccc(Cl)cc2)c2ccccc21)C(=O)c1ccccc1 | 10.1016/j.bmcl.2008.02.049 | |||
24739387 | 188263 | None | 0 | Human | Functional | pIC50 | = | 5.6 | 5.6 | 9 | 4 | ChEMBL | 454 | 4 | 0 | 2 | 5.2 | CC(=O)N1CCCC(c2ccccc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C1 | 10.1016/j.bmcl.2008.07.115 | |||
CHEMBL498556 | 188263 | None | 0 | Human | Functional | pIC50 | = | 5.6 | 5.6 | 9 | 4 | ChEMBL | 454 | 4 | 0 | 2 | 5.2 | CC(=O)N1CCCC(c2ccccc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C1 | 10.1016/j.bmcl.2008.07.115 | |||
46891424 | 6807 | None | 0 | Human | Functional | pIC50 | = | 6.6 | 6.6 | - | 1 | ChEMBL | 431 | 7 | 1 | 7 | 2.5 | N#Cc1ccc(S(=O)(=O)N(Cc2ccc(-c3nnn[nH]3)cc2)Cc2ccccn2)cc1 | 10.1016/j.bmcl.2010.04.113 | |||
CHEMBL1083913 | 6807 | None | 0 | Human | Functional | pIC50 | = | 6.6 | 6.6 | - | 1 | ChEMBL | 431 | 7 | 1 | 7 | 2.5 | N#Cc1ccc(S(=O)(=O)N(Cc2ccc(-c3nnn[nH]3)cc2)Cc2ccccn2)cc1 | 10.1016/j.bmcl.2010.04.113 | |||
46891538 | 6417 | None | 0 | Human | Functional | pIC50 | = | 6.6 | 6.6 | - | 1 | ChEMBL | 448 | 7 | 1 | 6 | 3.3 | N#Cc1ccc(S(=O)(=O)N(Cc2ccc(-c3nnn[nH]3)cc2)Cc2ccccc2F)cc1 | 10.1016/j.bmcl.2010.04.113 | |||
CHEMBL1082361 | 6417 | None | 0 | Human | Functional | pIC50 | = | 6.6 | 6.6 | - | 1 | ChEMBL | 448 | 7 | 1 | 6 | 3.3 | N#Cc1ccc(S(=O)(=O)N(Cc2ccc(-c3nnn[nH]3)cc2)Cc2ccccc2F)cc1 | 10.1016/j.bmcl.2010.04.113 | |||
89726522 | 149533 | None | 0 | Human | Functional | pIC50 | = | 5.6 | 5.6 | - | 1 | ChEMBL | 515 | 6 | 1 | 9 | 3.2 | C[C@@H]1CN(c2sc(CN(C)C)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL3945976 | 149533 | None | 0 | Human | Functional | pIC50 | = | 5.6 | 5.6 | - | 1 | ChEMBL | 515 | 6 | 1 | 9 | 3.2 | C[C@@H]1CN(c2sc(CN(C)C)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | 10.1021/acs.jmedchem.2c00675 | |||
117739568 | 144815 | None | 0 | Human | Functional | pIC50 | = | 6.6 | 6.6 | - | 1 | ChEMBL | 504 | 4 | 1 | 8 | 3.7 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccccc4[nH]3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00676 | |||
CHEMBL3908818 | 144815 | None | 0 | Human | Functional | pIC50 | = | 6.6 | 6.6 | - | 1 | ChEMBL | 504 | 4 | 1 | 8 | 3.7 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccccc4[nH]3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00676 | |||
46891145 | 7235 | None | 0 | Human | Functional | pIC50 | = | 6.6 | 6.6 | - | 1 | ChEMBL | 530 | 9 | 1 | 3 | 6.2 | O=C(NC1(c2ccccc2)CC1)c1ccc(CN(Cc2ccccc2)S(=O)(=O)c2ccc(Cl)cc2)cc1 | 10.1016/j.bmcl.2010.04.113 | |||
CHEMBL1085740 | 7235 | None | 0 | Human | Functional | pIC50 | = | 6.6 | 6.6 | - | 1 | ChEMBL | 530 | 9 | 1 | 3 | 6.2 | O=C(NC1(c2ccccc2)CC1)c1ccc(CN(Cc2ccccc2)S(=O)(=O)c2ccc(Cl)cc2)cc1 | 10.1016/j.bmcl.2010.04.113 | |||
89726129 | 153640 | None | 4 | Human | Functional | pIC50 | = | 6.6 | 6.6 | 1288 | 2 | ChEMBL | 586 | 5 | 1 | 11 | 4.0 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccc(-c5noc(C)n5)cc4[nH]3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00676 | |||
CHEMBL3980161 | 153640 | None | 4 | Human | Functional | pIC50 | = | 6.6 | 6.6 | 1288 | 2 | ChEMBL | 586 | 5 | 1 | 11 | 4.0 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccc(-c5noc(C)n5)cc4[nH]3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00676 | |||
168269773 | 190170 | None | 0 | Human | Functional | pIC50 | = | 7.6 | 7.6 | - | 1 | ChEMBL | 546 | 6 | 0 | 8 | 3.6 | CCOc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)CN3C(=O)Cc4ccccc43)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL5172352 | 190170 | None | 0 | Human | Functional | pIC50 | = | 7.6 | 7.6 | - | 1 | ChEMBL | 546 | 6 | 0 | 8 | 3.6 | CCOc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)CN3C(=O)Cc4ccccc43)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
24957182 | 153602 | None | 39 | Human | Functional | pIC50 | = | 6.6 | 6.6 | 63 | 2 | ChEMBL | 603 | 10 | 0 | 8 | 5.8 | CCOc1ccc(-n2c([C@@H](C)N(Cc3cccnc3)C(=O)Cc3ccc(OC(F)(F)F)cc3)nc3ncccc3c2=O)cc1 | 10.1016/j.bmcl.2009.07.032 | |||
CHEMBL397983 | 153602 | None | 39 | Human | Functional | pIC50 | = | 6.6 | 6.6 | 63 | 2 | ChEMBL | 603 | 10 | 0 | 8 | 5.8 | CCOc1ccc(-n2c([C@@H](C)N(Cc3cccnc3)C(=O)Cc3ccc(OC(F)(F)F)cc3)nc3ncccc3c2=O)cc1 | 10.1016/j.bmcl.2009.07.032 | |||
71525884 | 132872 | None | 0 | Human | Functional | pIC50 | = | 6.6 | 6.6 | -41 | 4 | ChEMBL | 523 | 8 | 3 | 10 | 2.6 | COC(=O)[C@H]1CCCN1C(=O)c1cccc(Nc2c(N[C@@H](c3ccc(C)o3)C3(C)COC3)c(=O)c2=O)c1O | nan | |||
CHEMBL3701188 | 132872 | None | 0 | Human | Functional | pIC50 | = | 6.6 | 6.6 | -41 | 4 | ChEMBL | 523 | 8 | 3 | 10 | 2.6 | COC(=O)[C@H]1CCCN1C(=O)c1cccc(Nc2c(N[C@@H](c3ccc(C)o3)C3(C)COC3)c(=O)c2=O)c1O | nan | |||
15604938 | 132863 | None | 0 | Human | Functional | pIC50 | = | 6.6 | 6.6 | - | 1 | ChEMBL | 617 | 8 | 3 | 4 | 5.7 | CCNC(=O)N1CCCN(c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2NC(=O)c2cc(F)cc(F)c2)CC1 | 10.1016/j.bmcl.2005.09.020 | |||
CHEMBL370064 | 132863 | None | 0 | Human | Functional | pIC50 | = | 6.6 | 6.6 | - | 1 | ChEMBL | 617 | 8 | 3 | 4 | 5.7 | CCNC(=O)N1CCCN(c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2NC(=O)c2cc(F)cc(F)c2)CC1 | 10.1016/j.bmcl.2005.09.020 | |||
15560447 | 193378 | None | 5 | Human | Functional | pIC50 | = | 5.6 | 5.6 | - | 1 | ChEMBL | 376 | 4 | 1 | 3 | 3.6 | Cc1ccc(CN2CCC(C3(c4ccccc4)CCC(=O)NC3=O)CC2)cc1 | 10.1016/j.bmcl.2008.07.115 | |||
CHEMBL523900 | 193378 | None | 5 | Human | Functional | pIC50 | = | 5.6 | 5.6 | - | 1 | ChEMBL | 376 | 4 | 1 | 3 | 3.6 | Cc1ccc(CN2CCC(C3(c4ccccc4)CCC(=O)NC3=O)CC2)cc1 | 10.1016/j.bmcl.2008.07.115 | |||
168288302 | 191478 | None | 0 | Human | Functional | pIC50 | = | 5.6 | 5.6 | - | 1 | ChEMBL | 528 | 4 | 1 | 6 | 4.5 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)CN1CCC(F)(F)CC1 | 10.1021/acs.jmedchem.2c00676 | |||
CHEMBL5192187 | 191478 | None | 0 | Human | Functional | pIC50 | = | 5.6 | 5.6 | - | 1 | ChEMBL | 528 | 4 | 1 | 6 | 4.5 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)CN1CCC(F)(F)CC1 | 10.1021/acs.jmedchem.2c00676 | |||
44253170 | 7236 | None | 0 | Human | Functional | pIC50 | = | 5.6 | 5.6 | - | 1 | ChEMBL | 563 | 11 | 1 | 5 | 5.6 | O=C(NCCc1cccc([N+](=O)[O-])c1)c1ccc(CN(Cc2ccccc2)S(=O)(=O)c2ccc(Cl)cc2)cc1 | 10.1016/j.bmcl.2010.04.113 | |||
CHEMBL1085741 | 7236 | None | 0 | Human | Functional | pIC50 | = | 5.6 | 5.6 | - | 1 | ChEMBL | 563 | 11 | 1 | 5 | 5.6 | O=C(NCCc1cccc([N+](=O)[O-])c1)c1ccc(CN(Cc2ccccc2)S(=O)(=O)c2ccc(Cl)cc2)cc1 | 10.1016/j.bmcl.2010.04.113 | |||
117739438 | 143937 | None | 0 | Human | Functional | pIC50 | = | 5.6 | 5.6 | - | 1 | ChEMBL | 491 | 4 | 1 | 8 | 3.7 | Cc1nnc(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccccc4[nH]3)C[C@H]2C)o1 | 10.1021/acs.jmedchem.2c00676 | |||
CHEMBL3901607 | 143937 | None | 0 | Human | Functional | pIC50 | = | 5.6 | 5.6 | - | 1 | ChEMBL | 491 | 4 | 1 | 8 | 3.7 | Cc1nnc(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccccc4[nH]3)C[C@H]2C)o1 | 10.1021/acs.jmedchem.2c00676 | |||
44237762 | 6642 | None | 0 | Human | Functional | pIC50 | = | 7.6 | 7.6 | - | 1 | ChEMBL | 531 | 9 | 1 | 4 | 5.5 | O=C(NC1(c2ccccc2)CC1)c1ccc(CN(Cc2ccccn2)S(=O)(=O)c2ccc(Cl)cc2)cc1 | 10.1016/j.bmcl.2010.04.113 | |||
CHEMBL1083335 | 6642 | None | 0 | Human | Functional | pIC50 | = | 7.6 | 7.6 | - | 1 | ChEMBL | 531 | 9 | 1 | 4 | 5.5 | O=C(NC1(c2ccccc2)CC1)c1ccc(CN(Cc2ccccn2)S(=O)(=O)c2ccc(Cl)cc2)cc1 | 10.1016/j.bmcl.2010.04.113 | |||
90479922 | 190733 | None | 0 | Human | Functional | pIC50 | = | 7.6 | 7.6 | - | 1 | ChEMBL | 496 | 5 | 0 | 10 | 2.6 | COc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3nc(C)nc3C)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL5181086 | 190733 | None | 0 | Human | Functional | pIC50 | = | 7.6 | 7.6 | - | 1 | ChEMBL | 496 | 5 | 0 | 10 | 2.6 | COc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3nc(C)nc3C)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
45486531 | 200770 | None | 0 | Human | Functional | pIC50 | = | 7.6 | 7.6 | - | 1 | ChEMBL | 653 | 8 | 0 | 7 | 6.3 | C[C@H](c1nc2c(C3CC3)nccn2c1-c1ccc(C#N)cc1)N(CC1CCS(=O)(=O)CC1)C(=O)Cc1ccc(F)c(C(F)(F)F)c1 | 10.1016/j.bmcl.2009.07.021 | |||
CHEMBL576097 | 200770 | None | 0 | Human | Functional | pIC50 | = | 7.6 | 7.6 | - | 1 | ChEMBL | 653 | 8 | 0 | 7 | 6.3 | C[C@H](c1nc2c(C3CC3)nccn2c1-c1ccc(C#N)cc1)N(CC1CCS(=O)(=O)CC1)C(=O)Cc1ccc(F)c(C(F)(F)F)c1 | 10.1016/j.bmcl.2009.07.021 | |||
24739889 | 188946 | None | 0 | Human | Functional | pIC50 | = | 6.6 | 6.6 | - | 1 | ChEMBL | 455 | 4 | 1 | 2 | 4.8 | NC(=O)N1CCCC(c2ccccc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C1 | 10.1016/j.bmcl.2008.07.115 | |||
CHEMBL506627 | 188946 | None | 0 | Human | Functional | pIC50 | = | 6.6 | 6.6 | - | 1 | ChEMBL | 455 | 4 | 1 | 2 | 4.8 | NC(=O)N1CCCC(c2ccccc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C1 | 10.1016/j.bmcl.2008.07.115 | |||
44406274 | 135316 | None | 0 | Human | Functional | pIC50 | = | 6.6 | 6.6 | - | 1 | ChEMBL | 567 | 7 | 3 | 4 | 5.4 | CCNC(=O)N1CCCN(c2ccc(C(=O)NCc3ccc(Cl)cc3)cc2NC(=O)c2cccc(Cl)c2)CC1 | 10.1016/j.bmcl.2005.09.020 | |||
CHEMBL372528 | 135316 | None | 0 | Human | Functional | pIC50 | = | 6.6 | 6.6 | - | 1 | ChEMBL | 567 | 7 | 3 | 4 | 5.4 | CCNC(=O)N1CCCN(c2ccc(C(=O)NCc3ccc(Cl)cc3)cc2NC(=O)c2cccc(Cl)c2)CC1 | 10.1016/j.bmcl.2005.09.020 | |||
15605073 | 135336 | None | 0 | Human | Functional | pIC50 | = | 6.6 | 6.6 | - | 1 | ChEMBL | 582 | 8 | 3 | 5 | 4.9 | CCNC(=O)N1CCCN(c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2NC(=O)c2ccncc2)CC1 | 10.1016/j.bmcl.2005.09.020 | |||
CHEMBL372595 | 135336 | None | 0 | Human | Functional | pIC50 | = | 6.6 | 6.6 | - | 1 | ChEMBL | 582 | 8 | 3 | 5 | 4.9 | CCNC(=O)N1CCCN(c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2NC(=O)c2ccncc2)CC1 | 10.1016/j.bmcl.2005.09.020 | |||
44453439 | 97701 | None | 1 | Human | Functional | pIC50 | = | 5.6 | 5.6 | - | 1 | ChEMBL | 385 | 7 | 1 | 6 | 3.4 | CCOC(=O)CCn1c(=N)n(CC(=O)c2ccc(Cl)cc2)c2ccccc21 | 10.1016/j.bmcl.2008.02.049 | |||
CHEMBL271081 | 97701 | None | 1 | Human | Functional | pIC50 | = | 5.6 | 5.6 | - | 1 | ChEMBL | 385 | 7 | 1 | 6 | 3.4 | CCOC(=O)CCn1c(=N)n(CC(=O)c2ccc(Cl)cc2)c2ccccc21 | 10.1016/j.bmcl.2008.02.049 | |||
117739261 | 146893 | None | 0 | Human | Functional | pIC50 | = | 6.6 | 6.6 | - | 1 | ChEMBL | 509 | 4 | 1 | 7 | 4.3 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cc(Cl)cn1 | 10.1021/acs.jmedchem.2c00676 | |||
CHEMBL3924716 | 146893 | None | 0 | Human | Functional | pIC50 | = | 6.6 | 6.6 | - | 1 | ChEMBL | 509 | 4 | 1 | 7 | 4.3 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cc(Cl)cn1 | 10.1021/acs.jmedchem.2c00676 | |||
27307547 | 177710 | None | 0 | Human | Functional | pIC50 | = | 6.6 | 6.6 | 5 | 2 | ChEMBL | 445 | 4 | 0 | 5 | 2.9 | CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCN(c3ccc(C(F)(F)F)cn3)CC1)C(=O)C2 | 10.1016/j.bmcl.2008.11.008 | |||
CHEMBL464081 | 177710 | None | 0 | Human | Functional | pIC50 | = | 6.6 | 6.6 | 5 | 2 | ChEMBL | 445 | 4 | 0 | 5 | 2.9 | CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCN(c3ccc(C(F)(F)F)cn3)CC1)C(=O)C2 | 10.1016/j.bmcl.2008.11.008 | |||
44570431 | 184088 | None | 0 | Human | Functional | pIC50 | = | 6.6 | 6.6 | - | 1 | ChEMBL | 479 | 4 | 0 | 5 | 3.6 | CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCN(c3ccc(C(F)(F)F)c(Cl)n3)CC1)C(=O)C2 | 10.1016/j.bmcl.2008.11.008 | |||
CHEMBL481780 | 184088 | None | 0 | Human | Functional | pIC50 | = | 6.6 | 6.6 | - | 1 | ChEMBL | 479 | 4 | 0 | 5 | 3.6 | CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCN(c3ccc(C(F)(F)F)c(Cl)n3)CC1)C(=O)C2 | 10.1016/j.bmcl.2008.11.008 | |||
44581088 | 188001 | None | 0 | Human | Functional | pIC50 | = | 5.6 | 5.6 | - | 1 | ChEMBL | 464 | 4 | 1 | 3 | 4.9 | O=C1CCC(c2ccccc2)(C2CCN(Cc3ccc(Cl)c(C(F)(F)F)c3)CC2)C(=O)N1 | 10.1016/j.bmcl.2008.07.115 | |||
CHEMBL496563 | 188001 | None | 0 | Human | Functional | pIC50 | = | 5.6 | 5.6 | - | 1 | ChEMBL | 464 | 4 | 1 | 3 | 4.9 | O=C1CCC(c2ccccc2)(C2CCN(Cc3ccc(Cl)c(C(F)(F)F)c3)CC2)C(=O)N1 | 10.1016/j.bmcl.2008.07.115 | |||
44580857 | 188080 | None | 0 | Human | Functional | pIC50 | = | 5.6 | 5.6 | - | 1 | ChEMBL | 468 | 5 | 0 | 3 | 4.8 | CCN1C(=O)CCC(c2ccccc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C1=O | 10.1016/j.bmcl.2008.07.115 | |||
CHEMBL497189 | 188080 | None | 0 | Human | Functional | pIC50 | = | 5.6 | 5.6 | - | 1 | ChEMBL | 468 | 5 | 0 | 3 | 4.8 | CCN1C(=O)CCC(c2ccccc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C1=O | 10.1016/j.bmcl.2008.07.115 | |||
44580823 | 192746 | None | 0 | Human | Functional | pIC50 | = | 5.6 | 5.6 | - | 1 | ChEMBL | 454 | 4 | 0 | 3 | 4.4 | CN1C(=O)CCC(c2ccccc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C1=O | 10.1016/j.bmcl.2008.07.115 | |||
CHEMBL521707 | 192746 | None | 0 | Human | Functional | pIC50 | = | 5.6 | 5.6 | - | 1 | ChEMBL | 454 | 4 | 0 | 3 | 4.4 | CN1C(=O)CCC(c2ccccc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C1=O | 10.1016/j.bmcl.2008.07.115 | |||
44570549 | 178478 | None | 0 | Mouse | Functional | pIC50 | = | 5.6 | 5.6 | -15 | 2 | ChEMBL | 459 | 4 | 0 | 5 | 3.3 | C[C@H]1CN(S(=O)(=O)C[C@]23CC[C@H](CC2=O)C3(C)C)CCN1c1ccc(C(F)(F)F)cn1 | 10.1016/j.bmcl.2008.11.008 | |||
CHEMBL465283 | 178478 | None | 0 | Mouse | Functional | pIC50 | = | 5.6 | 5.6 | -15 | 2 | ChEMBL | 459 | 4 | 0 | 5 | 3.3 | C[C@H]1CN(S(=O)(=O)C[C@]23CC[C@H](CC2=O)C3(C)C)CCN1c1ccc(C(F)(F)F)cn1 | 10.1016/j.bmcl.2008.11.008 | |||
44570311 | 177713 | None | 0 | Human | Functional | pIC50 | = | 4.6 | 4.6 | - | 1 | ChEMBL | 445 | 4 | 0 | 5 | 2.9 | CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCN(c3cc(C(F)(F)F)ccn3)CC1)C(=O)C2 | 10.1016/j.bmcl.2008.11.008 | |||
CHEMBL464082 | 177713 | None | 0 | Human | Functional | pIC50 | = | 4.6 | 4.6 | - | 1 | ChEMBL | 445 | 4 | 0 | 5 | 2.9 | CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCN(c3cc(C(F)(F)F)ccn3)CC1)C(=O)C2 | 10.1016/j.bmcl.2008.11.008 | |||
44570340 | 178484 | None | 0 | Human | Functional | pIC50 | = | 4.6 | 4.6 | - | 1 | ChEMBL | 445 | 4 | 0 | 5 | 2.9 | CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCN(c3cccc(C(F)(F)F)n3)CC1)C(=O)C2 | 10.1016/j.bmcl.2008.11.008 | |||
CHEMBL465303 | 178484 | None | 0 | Human | Functional | pIC50 | = | 4.6 | 4.6 | - | 1 | ChEMBL | 445 | 4 | 0 | 5 | 2.9 | CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCN(c3cccc(C(F)(F)F)n3)CC1)C(=O)C2 | 10.1016/j.bmcl.2008.11.008 | |||
57400677 | 69994 | None | 0 | Human | Functional | pIC50 | = | 6.6 | 6.6 | - | 1 | ChEMBL | 608 | 9 | 0 | 7 | 4.6 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc2ncccc2c(=O)n1-c1ccc(F)cc1 | 10.1016/j.bmcl.2011.10.120 | |||
CHEMBL1939561 | 69994 | None | 0 | Human | Functional | pIC50 | = | 6.6 | 6.6 | - | 1 | ChEMBL | 608 | 9 | 0 | 7 | 4.6 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc2ncccc2c(=O)n1-c1ccc(F)cc1 | 10.1016/j.bmcl.2011.10.120 | |||
46891477 | 6633 | None | 0 | Human | Functional | pIC50 | = | 6.6 | 6.6 | - | 1 | ChEMBL | 501 | 8 | 1 | 8 | 3.6 | CC(C)(C)c1nc(CCN(Cc2ccc(-c3nnn[nH]3)cc2)S(=O)(=O)c2ccc(Cl)cc2)no1 | 10.1016/j.bmcl.2010.04.113 | |||
CHEMBL1083310 | 6633 | None | 0 | Human | Functional | pIC50 | = | 6.6 | 6.6 | - | 1 | ChEMBL | 501 | 8 | 1 | 8 | 3.6 | CC(C)(C)c1nc(CCN(Cc2ccc(-c3nnn[nH]3)cc2)S(=O)(=O)c2ccc(Cl)cc2)no1 | 10.1016/j.bmcl.2010.04.113 | |||
44253590 | 6560 | None | 0 | Human | Functional | pIC50 | = | 5.6 | 5.6 | - | 1 | ChEMBL | 457 | 7 | 1 | 5 | 4.1 | O=S(=O)(c1ccc(Cl)cc1)N(Cc1ccc(F)cc1)Cc1ccc(-c2nnn[nH]2)cc1 | 10.1016/j.bmcl.2010.04.113 | |||
CHEMBL1082995 | 6560 | None | 0 | Human | Functional | pIC50 | = | 5.6 | 5.6 | - | 1 | ChEMBL | 457 | 7 | 1 | 5 | 4.1 | O=S(=O)(c1ccc(Cl)cc1)N(Cc1ccc(F)cc1)Cc1ccc(-c2nnn[nH]2)cc1 | 10.1016/j.bmcl.2010.04.113 | |||
90480457 | 191736 | None | 0 | Human | Functional | pIC50 | = | 6.6 | 6.6 | - | 1 | ChEMBL | 508 | 6 | 0 | 9 | 3.5 | CCCc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3nc(C)nc3C)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL5195689 | 191736 | None | 0 | Human | Functional | pIC50 | = | 6.6 | 6.6 | - | 1 | ChEMBL | 508 | 6 | 0 | 9 | 3.5 | CCCc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3nc(C)nc3C)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
53325134 | 58232 | None | 0 | Human | Functional | pIC50 | = | 6.6 | 6.6 | - | 1 | ChEMBL | 517 | 7 | 1 | 5 | 4.9 | CNC(=O)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4)CC3)[C@@H](CC(C)C)C2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
CHEMBL1681875 | 58232 | None | 0 | Human | Functional | pIC50 | = | 6.6 | 6.6 | - | 1 | ChEMBL | 517 | 7 | 1 | 5 | 4.9 | CNC(=O)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4)CC3)[C@@H](CC(C)C)C2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
53322506 | 58213 | None | 0 | Human | Functional | pIC50 | = | 7.6 | 7.6 | - | 1 | ChEMBL | 619 | 7 | 1 | 5 | 6.8 | CC1(N2CCN(c3ncc(C(=O)NCc4ccc(Cl)c(Cl)c4)cc3Cl)CC2)CCN(Cc2ccc(Cl)cc2)CC1 | 10.1016/j.bmcl.2010.12.114 | |||
CHEMBL1681856 | 58213 | None | 0 | Human | Functional | pIC50 | = | 7.6 | 7.6 | - | 1 | ChEMBL | 619 | 7 | 1 | 5 | 6.8 | CC1(N2CCN(c3ncc(C(=O)NCc4ccc(Cl)c(Cl)c4)cc3Cl)CC2)CCN(Cc2ccc(Cl)cc2)CC1 | 10.1016/j.bmcl.2010.12.114 | |||
56670451 | 64268 | None | 0 | Human | Functional | pIC50 | = | 7.6 | 7.6 | -1 | 2 | ChEMBL | 456 | 3 | 2 | 3 | 4.3 | COc1cccc(NC(=O)N2C[C@H](C(=O)N3CCCC3)C=C3c4cccc5[nH]cc(c45)C[C@H]32)c1 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1809019 | 64268 | None | 0 | Human | Functional | pIC50 | = | 7.6 | 7.6 | -1 | 2 | ChEMBL | 456 | 3 | 2 | 3 | 4.3 | COc1cccc(NC(=O)N2C[C@H](C(=O)N3CCCC3)C=C3c4cccc5[nH]cc(c45)C[C@H]32)c1 | 10.1016/j.bmcl.2011.06.070 | |||
53322505 | 58210 | None | 0 | Human | Functional | pIC50 | = | 5.6 | 5.6 | - | 1 | ChEMBL | 553 | 7 | 1 | 5 | 5.1 | CC1CN(C2CCN(Cc3ccc(Cl)cc3)CC2)CCN1c1ccc(C(=O)NCc2ccc(F)c(F)c2)cn1 | 10.1016/j.bmcl.2010.12.114 | |||
CHEMBL1681853 | 58210 | None | 0 | Human | Functional | pIC50 | = | 5.6 | 5.6 | - | 1 | ChEMBL | 553 | 7 | 1 | 5 | 5.1 | CC1CN(C2CCN(Cc3ccc(Cl)cc3)CC2)CCN1c1ccc(C(=O)NCc2ccc(F)c(F)c2)cn1 | 10.1016/j.bmcl.2010.12.114 | |||
168289637 | 191585 | None | 0 | Human | Functional | pIC50 | = | 6.6 | 6.6 | - | 1 | ChEMBL | 515 | 6 | 0 | 9 | 3.6 | CCOc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3cc(Cl)cn3)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL5193432 | 191585 | None | 0 | Human | Functional | pIC50 | = | 6.6 | 6.6 | - | 1 | ChEMBL | 515 | 6 | 0 | 9 | 3.6 | CCOc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3cc(Cl)cn3)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
45482849 | 201303 | None | 2 | Human | Functional | pIC50 | = | 7.6 | 7.6 | - | 1 | ChEMBL | 442 | 4 | 2 | 2 | 4.8 | CCN(CC)C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2C)C1 | 10.1016/j.bmcl.2009.09.002 | |||
CHEMBL583761 | 201303 | None | 2 | Human | Functional | pIC50 | = | 7.6 | 7.6 | - | 1 | ChEMBL | 442 | 4 | 2 | 2 | 4.8 | CCN(CC)C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2C)C1 | 10.1016/j.bmcl.2009.09.002 | |||
53318562 | 58218 | None | 0 | Human | Functional | pIC50 | = | 6.6 | 6.6 | - | 1 | ChEMBL | 475 | 5 | 1 | 5 | 3.8 | CNC(=O)c1cnc(N2CCC(N3CCN(Cc4ccc(Cl)cc4)CC3)C(C)C2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
CHEMBL1681861 | 58218 | None | 0 | Human | Functional | pIC50 | = | 6.6 | 6.6 | - | 1 | ChEMBL | 475 | 5 | 1 | 5 | 3.8 | CNC(=O)c1cnc(N2CCC(N3CCN(Cc4ccc(Cl)cc4)CC3)C(C)C2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
56677270 | 64256 | None | 0 | Human | Functional | pIC50 | = | 6.5 | 6.5 | - | 1 | ChEMBL | 483 | 2 | 2 | 3 | 3.3 | CC(=O)N1CCN(C(=O)[C@@H]2C=C3c4cccc5[nH]cc(c45)C[C@H]3N(C(=O)Nc3ccccc3)C2)CC1 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1809007 | 64256 | None | 0 | Human | Functional | pIC50 | = | 6.5 | 6.5 | - | 1 | ChEMBL | 483 | 2 | 2 | 3 | 3.3 | CC(=O)N1CCN(C(=O)[C@@H]2C=C3c4cccc5[nH]cc(c45)C[C@H]3N(C(=O)Nc3ccccc3)C2)CC1 | 10.1016/j.bmcl.2011.06.070 | |||
53326850 | 58203 | None | 0 | Human | Functional | pIC50 | = | 7.5 | 7.5 | - | 1 | ChEMBL | 501 | 4 | 1 | 5 | 4.4 | CNC(=O)c1cnc(N2CCN(C3CCN(C4CCc5cc(Cl)ccc54)CC3)[C@@H](C)C2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
CHEMBL1681844 | 58203 | None | 0 | Human | Functional | pIC50 | = | 7.5 | 7.5 | - | 1 | ChEMBL | 501 | 4 | 1 | 5 | 4.4 | CNC(=O)c1cnc(N2CCN(C3CCN(C4CCc5cc(Cl)ccc54)CC3)[C@@H](C)C2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
24739888 | 187944 | None | 0 | Human | Functional | pIC50 | = | 6.5 | 6.5 | - | 1 | ChEMBL | 468 | 5 | 0 | 2 | 5.6 | CCC(=O)N1CCCC(c2ccccc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C1 | 10.1016/j.bmcl.2008.07.115 | |||
CHEMBL496175 | 187944 | None | 0 | Human | Functional | pIC50 | = | 6.5 | 6.5 | - | 1 | ChEMBL | 468 | 5 | 0 | 2 | 5.6 | CCC(=O)N1CCCC(c2ccccc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C1 | 10.1016/j.bmcl.2008.07.115 | |||
15605137 | 135317 | None | 0 | Human | Functional | pIC50 | = | 6.5 | 6.5 | - | 1 | ChEMBL | 617 | 8 | 3 | 4 | 5.7 | CCNC(=O)N1CCCN(c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2NC(=O)c2ccc(F)c(F)c2)CC1 | 10.1016/j.bmcl.2005.09.020 | |||
CHEMBL372529 | 135317 | None | 0 | Human | Functional | pIC50 | = | 6.5 | 6.5 | - | 1 | ChEMBL | 617 | 8 | 3 | 4 | 5.7 | CCNC(=O)N1CCCN(c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2NC(=O)c2ccc(F)c(F)c2)CC1 | 10.1016/j.bmcl.2005.09.020 | |||
57400628 | 69989 | None | 0 | Human | Functional | pIC50 | = | 6.5 | 6.5 | - | 1 | ChEMBL | 608 | 9 | 0 | 7 | 4.6 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(C(F)(F)F)c(F)c1)[C@H](C)c1nc2ncccc2c(=O)n1-c1ccc(F)cc1 | 10.1016/j.bmcl.2011.10.120 | |||
CHEMBL1939556 | 69989 | None | 0 | Human | Functional | pIC50 | = | 6.5 | 6.5 | - | 1 | ChEMBL | 608 | 9 | 0 | 7 | 4.6 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(C(F)(F)F)c(F)c1)[C@H](C)c1nc2ncccc2c(=O)n1-c1ccc(F)cc1 | 10.1016/j.bmcl.2011.10.120 | |||
2396278 | 6426 | None | 21 | Human | Functional | pIC50 | = | 5.5 | 5.5 | -7 | 2 | ChEMBL | 415 | 7 | 1 | 3 | 4.4 | O=C(O)c1ccc(CN(Cc2ccccc2)S(=O)(=O)c2ccc(Cl)cc2)cc1 | 10.1016/j.bmcl.2010.04.113 | |||
CHEMBL1082389 | 6426 | None | 21 | Human | Functional | pIC50 | = | 5.5 | 5.5 | -7 | 2 | ChEMBL | 415 | 7 | 1 | 3 | 4.4 | O=C(O)c1ccc(CN(Cc2ccccc2)S(=O)(=O)c2ccc(Cl)cc2)cc1 | 10.1016/j.bmcl.2010.04.113 | |||
53324231 | 58231 | None | 0 | Human | Functional | pIC50 | = | 8.5 | 8.5 | - | 1 | ChEMBL | 489 | 6 | 1 | 5 | 4.3 | CC[C@H]1CN(c2ncc(C(=O)NC)cc2Cl)CCN1C1CCN(Cc2ccc(Cl)cc2)CC1 | 10.1016/j.bmcl.2010.12.114 | |||
CHEMBL1681874 | 58231 | None | 0 | Human | Functional | pIC50 | = | 8.5 | 8.5 | - | 1 | ChEMBL | 489 | 6 | 1 | 5 | 4.3 | CC[C@H]1CN(c2ncc(C(=O)NC)cc2Cl)CCN1C1CCN(Cc2ccc(Cl)cc2)CC1 | 10.1016/j.bmcl.2010.12.114 | |||
56663557 | 64251 | None | 0 | Human | Functional | pIC50 | = | 8.5 | 8.5 | -2 | 2 | ChEMBL | 424 | 2 | 2 | 2 | 4.0 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CC=CC1 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1809002 | 64251 | None | 0 | Human | Functional | pIC50 | = | 8.5 | 8.5 | -2 | 2 | ChEMBL | 424 | 2 | 2 | 2 | 4.0 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CC=CC1 | 10.1016/j.bmcl.2011.06.070 | |||
56663560 | 64265 | None | 0 | Human | Functional | pIC50 | = | 8.5 | 8.5 | -1 | 2 | ChEMBL | 444 | 2 | 2 | 2 | 4.4 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2cccc(F)c2)C1)N1CCCC1 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1809016 | 64265 | None | 0 | Human | Functional | pIC50 | = | 8.5 | 8.5 | -1 | 2 | ChEMBL | 444 | 2 | 2 | 2 | 4.4 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2cccc(F)c2)C1)N1CCCC1 | 10.1016/j.bmcl.2011.06.070 | |||
56673945 | 64285 | None | 0 | Human | Functional | pIC50 | = | 8.5 | 8.5 | -1 | 3 | ChEMBL | 523 | 5 | 1 | 4 | 4.8 | O=C([C@@H]1C=C2c3cccc4c3c(cn4CCN3CCCC3)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CCCC1 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1809040 | 64285 | None | 0 | Human | Functional | pIC50 | = | 8.5 | 8.5 | -1 | 3 | ChEMBL | 523 | 5 | 1 | 4 | 4.8 | O=C([C@@H]1C=C2c3cccc4c3c(cn4CCN3CCCC3)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CCCC1 | 10.1016/j.bmcl.2011.06.070 | |||
56663557 | 64251 | None | 0 | Mouse | Functional | pIC50 | = | 8.5 | 8.5 | 2 | 2 | ChEMBL | 424 | 2 | 2 | 2 | 4.0 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CC=CC1 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1809002 | 64251 | None | 0 | Mouse | Functional | pIC50 | = | 8.5 | 8.5 | 2 | 2 | ChEMBL | 424 | 2 | 2 | 2 | 4.0 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CC=CC1 | 10.1016/j.bmcl.2011.06.070 | |||
56660102 | 64286 | None | 0 | Mouse | Functional | pIC50 | = | 8.5 | 8.5 | 1 | 3 | ChEMBL | 537 | 5 | 1 | 4 | 5.2 | O=C([C@@H]1C=C2c3cccc4c3c(cn4CCN3CCCCC3)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CCCC1 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1809041 | 64286 | None | 0 | Mouse | Functional | pIC50 | = | 8.5 | 8.5 | 1 | 3 | ChEMBL | 537 | 5 | 1 | 4 | 5.2 | O=C([C@@H]1C=C2c3cccc4c3c(cn4CCN3CCCCC3)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CCCC1 | 10.1016/j.bmcl.2011.06.070 | |||
56663562 | 64287 | None | 0 | Mouse | Functional | pIC50 | = | 8.5 | 8.5 | 1 | 3 | ChEMBL | 552 | 5 | 1 | 5 | 4.0 | CN1CCN(CCn2cc3c4c(cccc42)C2=C[C@@H](C(=O)N4CCCC4)CN(C(=O)Nc4ccccc4)[C@@H]2C3)CC1 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1809042 | 64287 | None | 0 | Mouse | Functional | pIC50 | = | 8.5 | 8.5 | 1 | 3 | ChEMBL | 552 | 5 | 1 | 5 | 4.0 | CN1CCN(CCn2cc3c4c(cccc42)C2=C[C@@H](C(=O)N4CCCC4)CN(C(=O)Nc4ccccc4)[C@@H]2C3)CC1 | 10.1016/j.bmcl.2011.06.070 | |||
168269773 | 190170 | None | 0 | Human | Functional | pIC50 | = | 8.5 | 8.5 | - | 1 | ChEMBL | 546 | 6 | 0 | 8 | 3.6 | CCOc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)CN3C(=O)Cc4ccccc43)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL5172352 | 190170 | None | 0 | Human | Functional | pIC50 | = | 8.5 | 8.5 | - | 1 | ChEMBL | 546 | 6 | 0 | 8 | 3.6 | CCOc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)CN3C(=O)Cc4ccccc43)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
89726440 | 142782 | None | 0 | Human | Functional | pIC50 | = | 8.5 | 8.5 | - | 1 | ChEMBL | 522 | 4 | 1 | 8 | 3.8 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4c(F)cccc4[nH]3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00676 | |||
CHEMBL3892103 | 142782 | None | 0 | Human | Functional | pIC50 | = | 8.5 | 8.5 | - | 1 | ChEMBL | 522 | 4 | 1 | 8 | 3.8 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4c(F)cccc4[nH]3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00676 | |||
168272767 | 190661 | None | 0 | Human | Functional | pIC50 | = | 8.5 | 8.5 | - | 1 | ChEMBL | 518 | 4 | 1 | 8 | 4.0 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4cccc(C)c4[nH]3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00676 | |||
CHEMBL5179941 | 190661 | None | 0 | Human | Functional | pIC50 | = | 8.5 | 8.5 | - | 1 | ChEMBL | 518 | 4 | 1 | 8 | 4.0 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4cccc(C)c4[nH]3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00676 | |||
168284045 | 191365 | None | 0 | Human | Functional | pIC50 | = | 8.5 | 8.5 | - | 1 | ChEMBL | 607 | 5 | 1 | 10 | 3.6 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4cc(N5CCOCC5)cc(F)c4[nH]3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00676 | |||
CHEMBL5190291 | 191365 | None | 0 | Human | Functional | pIC50 | = | 8.5 | 8.5 | - | 1 | ChEMBL | 607 | 5 | 1 | 10 | 3.6 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4cc(N5CCOCC5)cc(F)c4[nH]3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00676 | |||
168279606 | 191087 | None | 0 | Human | Functional | pIC50 | = | 8.5 | 8.5 | - | 1 | ChEMBL | 495 | 6 | 0 | 9 | 3.3 | CCOc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3ccc(C)n3)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL5186167 | 191087 | None | 0 | Human | Functional | pIC50 | = | 8.5 | 8.5 | - | 1 | ChEMBL | 495 | 6 | 0 | 9 | 3.3 | CCOc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3ccc(C)n3)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
117739568 | 144815 | None | 0 | Human | Functional | pIC50 | = | 8.5 | 8.5 | - | 1 | ChEMBL | 504 | 4 | 1 | 8 | 3.7 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccccc4[nH]3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00676 | |||
CHEMBL3908818 | 144815 | None | 0 | Human | Functional | pIC50 | = | 8.5 | 8.5 | - | 1 | ChEMBL | 504 | 4 | 1 | 8 | 3.7 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccccc4[nH]3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00676 | |||
89726174 | 147207 | None | 0 | Human | Functional | pIC50 | = | 8.5 | 8.5 | - | 1 | ChEMBL | 586 | 6 | 1 | 10 | 4.2 | COc1cc2nc(-c3nc(C(F)(F)F)sc3N3CCN(C(=O)Cn4cnc5cccnc54)[C@H](C)C3)[nH]c2cc1OC | 10.1021/acs.jmedchem.2c00676 | |||
CHEMBL3927485 | 147207 | None | 0 | Human | Functional | pIC50 | = | 8.5 | 8.5 | - | 1 | ChEMBL | 586 | 6 | 1 | 10 | 4.2 | COc1cc2nc(-c3nc(C(F)(F)F)sc3N3CCN(C(=O)Cn4cnc5cccnc54)[C@H](C)C3)[nH]c2cc1OC | 10.1021/acs.jmedchem.2c00676 | |||
117740233 | 153750 | None | 0 | Human | Functional | pIC50 | = | 8.5 | 8.5 | - | 1 | ChEMBL | 588 | 5 | 1 | 9 | 4.5 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccc(C5CCOCC5)cc4[nH]3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00676 | |||
CHEMBL3981151 | 153750 | None | 0 | Human | Functional | pIC50 | = | 8.5 | 8.5 | - | 1 | ChEMBL | 588 | 5 | 1 | 9 | 4.5 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccc(C5CCOCC5)cc4[nH]3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00676 | |||
168276987 | 190482 | None | 0 | Human | Functional | pIC50 | = | 8.5 | 8.5 | - | 1 | ChEMBL | 530 | 6 | 0 | 9 | 4.1 | CCCc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3cnc4cccnc43)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL5177288 | 190482 | None | 0 | Human | Functional | pIC50 | = | 8.5 | 8.5 | - | 1 | ChEMBL | 530 | 6 | 0 | 9 | 4.1 | CCCc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3cnc4cccnc43)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
168290539 | 192031 | None | 0 | Human | Functional | pIC50 | = | 8.5 | 8.5 | - | 1 | ChEMBL | 548 | 6 | 0 | 10 | 3.7 | CCOc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3c(=O)oc4ccccc43)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL5200240 | 192031 | None | 0 | Human | Functional | pIC50 | = | 8.5 | 8.5 | - | 1 | ChEMBL | 548 | 6 | 0 | 10 | 3.7 | CCOc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3c(=O)oc4ccccc43)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
12207 | 275 | None | 12 | Human | Functional | pIC50 | = | 8.5 | 8.5 | -7 | 2 | ChEMBL | 534 | 4 | 0 | 9 | 3.6 | C[C@@H]1CN(CCN1C(=O)Cn1nc(C)nc1C)c1c(c2cnc(C(F)(F)F)nc2)nc(C(F)(F)F)s1 | 10.1021/acs.jmedchem.2c00675 | |||
87056189 | 275 | None | 12 | Human | Functional | pIC50 | = | 8.5 | 8.5 | -7 | 2 | ChEMBL | 534 | 4 | 0 | 9 | 3.6 | C[C@@H]1CN(CCN1C(=O)Cn1nc(C)nc1C)c1c(c2cnc(C(F)(F)F)nc2)nc(C(F)(F)F)s1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL5202301 | 275 | None | 12 | Human | Functional | pIC50 | = | 8.5 | 8.5 | -7 | 2 | ChEMBL | 534 | 4 | 0 | 9 | 3.6 | C[C@@H]1CN(CCN1C(=O)Cn1nc(C)nc1C)c1c(c2cnc(C(F)(F)F)nc2)nc(C(F)(F)F)s1 | 10.1021/acs.jmedchem.2c00675 | |||
90479878 | 190352 | None | 0 | Human | Functional | pIC50 | = | 8.5 | 8.5 | - | 1 | ChEMBL | 524 | 6 | 0 | 10 | 3.4 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3cnc(OC(C)C)nc3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL5175118 | 190352 | None | 0 | Human | Functional | pIC50 | = | 8.5 | 8.5 | - | 1 | ChEMBL | 524 | 6 | 0 | 10 | 3.4 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3cnc(OC(C)C)nc3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00675 | |||
90479923 | 192379 | None | 0 | Human | Functional | pIC50 | = | 8.5 | 8.5 | - | 1 | ChEMBL | 506 | 5 | 0 | 9 | 3.4 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3cnc(C4CC4)nc3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL5205683 | 192379 | None | 0 | Human | Functional | pIC50 | = | 8.5 | 8.5 | - | 1 | ChEMBL | 506 | 5 | 0 | 9 | 3.4 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3cnc(C4CC4)nc3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00675 | |||
90479958 | 192439 | None | 0 | Human | Functional | pIC50 | = | 8.5 | 8.5 | - | 1 | ChEMBL | 535 | 5 | 0 | 10 | 3.2 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3cnc(N4CCCC4)nc3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL5206539 | 192439 | None | 0 | Human | Functional | pIC50 | = | 8.5 | 8.5 | - | 1 | ChEMBL | 535 | 5 | 0 | 10 | 3.2 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3cnc(N4CCCC4)nc3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00675 | |||
117739191 | 150772 | None | 0 | Human | Functional | pIC50 | = | 8.4 | 8.4 | - | 1 | ChEMBL | 544 | 4 | 1 | 8 | 3.6 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cnc2c1CCN(C)C2 | 10.1021/acs.jmedchem.2c00676 | |||
CHEMBL3955848 | 150772 | None | 0 | Human | Functional | pIC50 | = | 8.4 | 8.4 | - | 1 | ChEMBL | 544 | 4 | 1 | 8 | 3.6 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cnc2c1CCN(C)C2 | 10.1021/acs.jmedchem.2c00676 | |||
168282969 | 190934 | None | 0 | Human | Functional | pIC50 | = | 8.4 | 8.4 | - | 1 | ChEMBL | 610 | 5 | 1 | 9 | 5.1 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccc(OC(F)(F)F)cc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | 10.1021/acs.jmedchem.2c00676 | |||
CHEMBL5183995 | 190934 | None | 0 | Human | Functional | pIC50 | = | 8.4 | 8.4 | - | 1 | ChEMBL | 610 | 5 | 1 | 9 | 5.1 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccc(OC(F)(F)F)cc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | 10.1021/acs.jmedchem.2c00676 | |||
168290369 | 192025 | None | 0 | Human | Functional | pIC50 | = | 8.4 | 8.4 | - | 1 | ChEMBL | 607 | 5 | 1 | 10 | 3.6 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccc(N5CCOCC5)c(F)c4[nH]3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00676 | |||
CHEMBL5200180 | 192025 | None | 0 | Human | Functional | pIC50 | = | 8.4 | 8.4 | - | 1 | ChEMBL | 607 | 5 | 1 | 10 | 3.6 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccc(N5CCOCC5)c(F)c4[nH]3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00676 | |||
168273685 | 190500 | None | 0 | Human | Functional | pIC50 | = | 8.4 | 8.4 | - | 1 | ChEMBL | 531 | 6 | 0 | 9 | 4.1 | CCOc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3ccc4cnccc43)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL5177520 | 190500 | None | 0 | Human | Functional | pIC50 | = | 8.4 | 8.4 | - | 1 | ChEMBL | 531 | 6 | 0 | 9 | 4.1 | CCOc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3ccc4cnccc43)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
168288472 | 191828 | None | 0 | Human | Functional | pIC50 | = | 8.4 | 8.4 | - | 1 | ChEMBL | 502 | 4 | 0 | 9 | 3.4 | Cc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3cnc4cccnc43)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL5197065 | 191828 | None | 0 | Human | Functional | pIC50 | = | 8.4 | 8.4 | - | 1 | ChEMBL | 502 | 4 | 0 | 9 | 3.4 | Cc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3cnc4cccnc43)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
12207 | 275 | None | 12 | Human | Functional | pIC50 | = | 8.4 | 8.4 | -7 | 2 | ChEMBL | 534 | 4 | 0 | 9 | 3.6 | C[C@@H]1CN(CCN1C(=O)Cn1nc(C)nc1C)c1c(c2cnc(C(F)(F)F)nc2)nc(C(F)(F)F)s1 | 10.1021/acs.jmedchem.2c00675 | |||
87056189 | 275 | None | 12 | Human | Functional | pIC50 | = | 8.4 | 8.4 | -7 | 2 | ChEMBL | 534 | 4 | 0 | 9 | 3.6 | C[C@@H]1CN(CCN1C(=O)Cn1nc(C)nc1C)c1c(c2cnc(C(F)(F)F)nc2)nc(C(F)(F)F)s1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL5202301 | 275 | None | 12 | Human | Functional | pIC50 | = | 8.4 | 8.4 | -7 | 2 | ChEMBL | 534 | 4 | 0 | 9 | 3.6 | C[C@@H]1CN(CCN1C(=O)Cn1nc(C)nc1C)c1c(c2cnc(C(F)(F)F)nc2)nc(C(F)(F)F)s1 | 10.1021/acs.jmedchem.2c00675 | |||
89726335 | 153857 | None | 0 | Human | Functional | pIC50 | = | 8.4 | 8.4 | - | 1 | ChEMBL | 575 | 6 | 2 | 10 | 3.0 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccc(OC5CNC5)cc4[nH]3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00676 | |||
CHEMBL3982035 | 153857 | None | 0 | Human | Functional | pIC50 | = | 8.4 | 8.4 | - | 1 | ChEMBL | 575 | 6 | 2 | 10 | 3.0 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccc(OC5CNC5)cc4[nH]3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00676 | |||
168269369 | 190027 | None | 0 | Human | Functional | pIC50 | = | 8.4 | 8.4 | - | 1 | ChEMBL | 531 | 6 | 0 | 9 | 4.1 | CCOc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3ccc4cccnc43)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL5169888 | 190027 | None | 0 | Human | Functional | pIC50 | = | 8.4 | 8.4 | - | 1 | ChEMBL | 531 | 6 | 0 | 9 | 4.1 | CCOc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3ccc4cccnc43)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
168273430 | 190794 | None | 0 | Human | Functional | pIC50 | = | 8.4 | 8.4 | - | 1 | ChEMBL | 518 | 5 | 0 | 10 | 3.1 | COc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3cnc4cccnc43)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL5181928 | 190794 | None | 0 | Human | Functional | pIC50 | = | 8.4 | 8.4 | - | 1 | ChEMBL | 518 | 5 | 0 | 10 | 3.1 | COc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3cnc4cccnc43)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
168282319 | 191182 | None | 0 | Human | Functional | pIC50 | = | 8.4 | 8.4 | - | 1 | ChEMBL | 549 | 6 | 0 | 9 | 4.0 | CCOc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3ccc(C(F)(F)F)n3)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL5187464 | 191182 | None | 0 | Human | Functional | pIC50 | = | 8.4 | 8.4 | - | 1 | ChEMBL | 549 | 6 | 0 | 9 | 4.0 | CCOc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3ccc(C(F)(F)F)n3)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
168287236 | 191835 | None | 0 | Human | Functional | pIC50 | = | 8.4 | 8.4 | - | 1 | ChEMBL | 550 | 6 | 0 | 10 | 3.4 | CCOc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3cnc(C(F)(F)F)n3)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL5197175 | 191835 | None | 0 | Human | Functional | pIC50 | = | 8.4 | 8.4 | - | 1 | ChEMBL | 550 | 6 | 0 | 10 | 3.4 | CCOc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3cnc(C(F)(F)F)n3)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
168286207 | 191625 | None | 0 | Human | Functional | pIC50 | = | 8.4 | 8.4 | - | 1 | ChEMBL | 538 | 4 | 2 | 9 | 3.5 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccc(O)c(F)c4[nH]3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00676 | |||
CHEMBL5193975 | 191625 | None | 0 | Human | Functional | pIC50 | = | 8.4 | 8.4 | - | 1 | ChEMBL | 538 | 4 | 2 | 9 | 3.5 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccc(O)c(F)c4[nH]3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00676 | |||
71680140 | 145940 | None | 0 | Human | Functional | pIC50 | = | 8.4 | 8.4 | - | 1 | ChEMBL | 472 | 5 | 1 | 8 | 3.6 | CC[C@@H]1CN(c2scnc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL3917322 | 145940 | None | 0 | Human | Functional | pIC50 | = | 8.4 | 8.4 | - | 1 | ChEMBL | 472 | 5 | 1 | 8 | 3.6 | CC[C@@H]1CN(c2scnc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | 10.1021/acs.jmedchem.2c00675 | |||
24739554 | 188169 | None | 0 | Human | Functional | pIC50 | = | 7.5 | 7.5 | 64 | 2 | ChEMBL | 531 | 5 | 1 | 2 | 6.9 | O=C(Nc1ccccc1)N1CCCC(c2ccccc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C1 | 10.1016/j.bmcl.2008.07.115 | |||
CHEMBL497799 | 188169 | None | 0 | Human | Functional | pIC50 | = | 7.5 | 7.5 | 64 | 2 | ChEMBL | 531 | 5 | 1 | 2 | 6.9 | O=C(Nc1ccccc1)N1CCCC(c2ccccc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C1 | 10.1016/j.bmcl.2008.07.115 | |||
45482789 | 201381 | None | 0 | Mouse | Functional | pIC50 | = | 7.5 | 7.5 | -1 | 14 | ChEMBL | 428 | 4 | 2 | 2 | 4.5 | CCN(CC)C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1 | 10.1016/j.bmcl.2009.09.002 | |||
CHEMBL584554 | 201381 | None | 0 | Mouse | Functional | pIC50 | = | 7.5 | 7.5 | -1 | 14 | ChEMBL | 428 | 4 | 2 | 2 | 4.5 | CCN(CC)C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1 | 10.1016/j.bmcl.2009.09.002 | |||
45482789 | 201381 | None | 0 | Mouse | Functional | pIC50 | = | 7.5 | 7.5 | -1 | 14 | ChEMBL | 428 | 4 | 2 | 2 | 4.5 | CCN(CC)C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL584554 | 201381 | None | 0 | Mouse | Functional | pIC50 | = | 7.5 | 7.5 | -1 | 14 | ChEMBL | 428 | 4 | 2 | 2 | 4.5 | CCN(CC)C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1 | 10.1016/j.bmcl.2011.06.070 | |||
71679792 | 146935 | None | 0 | Human | Functional | pIC50 | = | 7.5 | 7.5 | - | 1 | ChEMBL | 444 | 4 | 1 | 8 | 2.8 | O=C(Cn1cnc2cccnc21)N1CCN(c2scnc2-c2nc3ccccc3[nH]2)CC1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL3925131 | 146935 | None | 0 | Human | Functional | pIC50 | = | 7.5 | 7.5 | - | 1 | ChEMBL | 444 | 4 | 1 | 8 | 2.8 | O=C(Cn1cnc2cccnc21)N1CCN(c2scnc2-c2nc3ccccc3[nH]2)CC1 | 10.1021/acs.jmedchem.2c00675 | |||
45486555 | 200129 | None | 0 | Human | Functional | pIC50 | = | 7.5 | 7.5 | - | 1 | ChEMBL | 629 | 9 | 0 | 8 | 4.7 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc2nc(C)ccc2c(=O)n1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2009.07.021 | |||
CHEMBL571080 | 200129 | None | 0 | Human | Functional | pIC50 | = | 7.5 | 7.5 | - | 1 | ChEMBL | 629 | 9 | 0 | 8 | 4.7 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc2nc(C)ccc2c(=O)n1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2009.07.021 | |||
17754758 | 97516 | None | 0 | Human | Functional | pIC50 | = | 6.5 | 6.5 | 4 | 2 | ChEMBL | 494 | 8 | 1 | 5 | 4.8 | CN(CCn1c(=N)n(CC(=O)c2ccc(Cl)cc2)c2cccc(Cl)c21)C(=O)Cc1ccccc1 | 10.1016/j.bmcl.2008.02.049 | |||
CHEMBL270166 | 97516 | None | 0 | Human | Functional | pIC50 | = | 6.5 | 6.5 | 4 | 2 | ChEMBL | 494 | 8 | 1 | 5 | 4.8 | CN(CCn1c(=N)n(CC(=O)c2ccc(Cl)cc2)c2cccc(Cl)c21)C(=O)Cc1ccccc1 | 10.1016/j.bmcl.2008.02.049 | |||
15604774 | 72686 | None | 0 | Human | Functional | pIC50 | = | 6.5 | 6.5 | - | 1 | ChEMBL | 581 | 8 | 3 | 4 | 5.5 | CCNC(=O)N1CCCN(c2ccc(C(=O)NCCc3cccc(Cl)c3)cc2NC(=O)c2cccc(Cl)c2)CC1 | 10.1016/j.bmcl.2005.09.020 | |||
CHEMBL199563 | 72686 | None | 0 | Human | Functional | pIC50 | = | 6.5 | 6.5 | - | 1 | ChEMBL | 581 | 8 | 3 | 4 | 5.5 | CCNC(=O)N1CCCN(c2ccc(C(=O)NCCc3cccc(Cl)c3)cc2NC(=O)c2cccc(Cl)c2)CC1 | 10.1016/j.bmcl.2005.09.020 | |||
168284045 | 191365 | None | 0 | Human | Functional | pIC50 | = | 6.5 | 6.5 | - | 1 | ChEMBL | 607 | 5 | 1 | 10 | 3.6 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4cc(N5CCOCC5)cc(F)c4[nH]3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00676 | |||
CHEMBL5190291 | 191365 | None | 0 | Human | Functional | pIC50 | = | 6.5 | 6.5 | - | 1 | ChEMBL | 607 | 5 | 1 | 10 | 3.6 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4cc(N5CCOCC5)cc(F)c4[nH]3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00676 | |||
89726497 | 153195 | None | 0 | Human | Functional | pIC50 | = | 6.5 | 6.5 | - | 1 | ChEMBL | 587 | 5 | 2 | 9 | 4.1 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccc(C5CCNCC5)cc4[nH]3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00676 | |||
CHEMBL3976317 | 153195 | None | 0 | Human | Functional | pIC50 | = | 6.5 | 6.5 | - | 1 | ChEMBL | 587 | 5 | 2 | 9 | 4.1 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccc(C5CCNCC5)cc4[nH]3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00676 | |||
53317274 | 58212 | None | 0 | Human | Functional | pIC50 | = | 7.5 | 7.5 | - | 1 | ChEMBL | 475 | 5 | 1 | 5 | 3.9 | CNC(=O)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4)C(C)C3)CC2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
CHEMBL1681855 | 58212 | None | 0 | Human | Functional | pIC50 | = | 7.5 | 7.5 | - | 1 | ChEMBL | 475 | 5 | 1 | 5 | 3.9 | CNC(=O)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4)C(C)C3)CC2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
117739438 | 143937 | None | 0 | Human | Functional | pIC50 | = | 7.5 | 7.5 | - | 1 | ChEMBL | 491 | 4 | 1 | 8 | 3.7 | Cc1nnc(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccccc4[nH]3)C[C@H]2C)o1 | 10.1021/acs.jmedchem.2c00676 | |||
CHEMBL3901607 | 143937 | None | 0 | Human | Functional | pIC50 | = | 7.5 | 7.5 | - | 1 | ChEMBL | 491 | 4 | 1 | 8 | 3.7 | Cc1nnc(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccccc4[nH]3)C[C@H]2C)o1 | 10.1021/acs.jmedchem.2c00676 | |||
56673942 | 64275 | None | 0 | Mouse | Functional | pIC50 | = | 7.5 | 7.5 | -1 | 2 | ChEMBL | 432 | 2 | 2 | 2 | 4.1 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)NC2CCCCC2)C1)N1CCCC1 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1809028 | 64275 | None | 0 | Mouse | Functional | pIC50 | = | 7.5 | 7.5 | -1 | 2 | ChEMBL | 432 | 2 | 2 | 2 | 4.1 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)NC2CCCCC2)C1)N1CCCC1 | 10.1016/j.bmcl.2011.06.070 | |||
71679146 | 153498 | None | 0 | Human | Functional | pIC50 | = | 7.5 | 7.5 | - | 1 | ChEMBL | 526 | 4 | 1 | 8 | 4.2 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL3978935 | 153498 | None | 0 | Human | Functional | pIC50 | = | 7.5 | 7.5 | - | 1 | ChEMBL | 526 | 4 | 1 | 8 | 4.2 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | 10.1021/acs.jmedchem.2c00675 | |||
25265835 | 177833 | None | 0 | Human | Functional | pIC50 | = | 7.5 | 7.5 | 6 | 2 | ChEMBL | 479 | 4 | 1 | 5 | 3.3 | C[C@H]1CN(S(=O)(=O)C[C@]23CC[C@H](C[C@@H]2O)C3(C)C)CCN1c1ncc(C(F)(F)F)cc1F | 10.1016/j.bmcl.2008.11.008 | |||
CHEMBL464234 | 177833 | None | 0 | Human | Functional | pIC50 | = | 7.5 | 7.5 | 6 | 2 | ChEMBL | 479 | 4 | 1 | 5 | 3.3 | C[C@H]1CN(S(=O)(=O)C[C@]23CC[C@H](C[C@@H]2O)C3(C)C)CCN1c1ncc(C(F)(F)F)cc1F | 10.1016/j.bmcl.2008.11.008 | |||
44570220 | 184011 | None | 0 | Human | Functional | pIC50 | = | 7.5 | 7.5 | 6 | 2 | ChEMBL | 461 | 4 | 1 | 5 | 3.1 | C[C@H]1CN(S(=O)(=O)C[C@]23CC[C@H](C[C@@H]2O)C3(C)C)CCN1c1ccc(C(F)(F)F)cn1 | 10.1016/j.bmcl.2008.11.008 | |||
CHEMBL481198 | 184011 | None | 0 | Human | Functional | pIC50 | = | 7.5 | 7.5 | 6 | 2 | ChEMBL | 461 | 4 | 1 | 5 | 3.1 | C[C@H]1CN(S(=O)(=O)C[C@]23CC[C@H](C[C@@H]2O)C3(C)C)CCN1c1ccc(C(F)(F)F)cn1 | 10.1016/j.bmcl.2008.11.008 | |||
53321186 | 58236 | None | 0 | Human | Functional | pIC50 | = | 5.5 | 5.5 | - | 1 | ChEMBL | 505 | 7 | 1 | 6 | 3.6 | CNC(=O)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4)CC3)C(COC)C2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
CHEMBL1681879 | 58236 | None | 0 | Human | Functional | pIC50 | = | 5.5 | 5.5 | - | 1 | ChEMBL | 505 | 7 | 1 | 6 | 3.6 | CNC(=O)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4)CC3)C(COC)C2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
44406261 | 140882 | None | 0 | Human | Functional | pIC50 | = | 5.5 | 5.5 | - | 1 | ChEMBL | 582 | 8 | 3 | 5 | 4.9 | CCNC(=O)N1CCCN(c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2NC(=O)c2cccnc2)CC1 | 10.1016/j.bmcl.2005.09.020 | |||
CHEMBL381877 | 140882 | None | 0 | Human | Functional | pIC50 | = | 5.5 | 5.5 | - | 1 | ChEMBL | 582 | 8 | 3 | 5 | 4.9 | CCNC(=O)N1CCCN(c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2NC(=O)c2cccnc2)CC1 | 10.1016/j.bmcl.2005.09.020 | |||
44570516 | 178282 | None | 0 | Human | Functional | pIC50 | = | 6.5 | 6.5 | - | 1 | ChEMBL | 459 | 4 | 0 | 5 | 3.3 | CC1CN(S(=O)(=O)C[C@]23CC[C@H](CC2=O)C3(C)C)CCN1c1ccc(C(F)(F)F)cn1 | 10.1016/j.bmcl.2008.11.008 | |||
CHEMBL464922 | 178282 | None | 0 | Human | Functional | pIC50 | = | 6.5 | 6.5 | - | 1 | ChEMBL | 459 | 4 | 0 | 5 | 3.3 | CC1CN(S(=O)(=O)C[C@]23CC[C@H](CC2=O)C3(C)C)CCN1c1ccc(C(F)(F)F)cn1 | 10.1016/j.bmcl.2008.11.008 | |||
44570221 | 178510 | None | 0 | Human | Functional | pIC50 | = | 6.5 | 6.5 | 1 | 2 | ChEMBL | 461 | 4 | 1 | 5 | 3.1 | C[C@H]1CN(S(=O)(=O)C[C@]23CC[C@H](C[C@H]2O)C3(C)C)CCN1c1ccc(C(F)(F)F)cn1 | 10.1016/j.bmcl.2008.11.008 | |||
CHEMBL465918 | 178510 | None | 0 | Human | Functional | pIC50 | = | 6.5 | 6.5 | 1 | 2 | ChEMBL | 461 | 4 | 1 | 5 | 3.1 | C[C@H]1CN(S(=O)(=O)C[C@]23CC[C@H](C[C@H]2O)C3(C)C)CCN1c1ccc(C(F)(F)F)cn1 | 10.1016/j.bmcl.2008.11.008 | |||
44570471 | 183511 | None | 0 | Human | Functional | pIC50 | = | 6.5 | 6.5 | - | 1 | ChEMBL | 446 | 4 | 0 | 6 | 2.3 | CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCN(c3ncc(C(F)(F)F)cn3)CC1)C(=O)C2 | 10.1016/j.bmcl.2008.11.008 | |||
CHEMBL479828 | 183511 | None | 0 | Human | Functional | pIC50 | = | 6.5 | 6.5 | - | 1 | ChEMBL | 446 | 4 | 0 | 6 | 2.3 | CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCN(c3ncc(C(F)(F)F)cn3)CC1)C(=O)C2 | 10.1016/j.bmcl.2008.11.008 | |||
44570432 | 183978 | None | 0 | Human | Functional | pIC50 | = | 6.5 | 6.5 | - | 1 | ChEMBL | 513 | 4 | 0 | 5 | 4.3 | CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCN(c3nc(Cl)c(C(F)(F)F)cc3Cl)CC1)C(=O)C2 | 10.1016/j.bmcl.2008.11.008 | |||
CHEMBL480996 | 183978 | None | 0 | Human | Functional | pIC50 | = | 6.5 | 6.5 | - | 1 | ChEMBL | 513 | 4 | 0 | 5 | 4.3 | CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCN(c3nc(Cl)c(C(F)(F)F)cc3Cl)CC1)C(=O)C2 | 10.1016/j.bmcl.2008.11.008 | |||
44570218 | 184009 | None | 0 | Human | Functional | pIC50 | = | 6.5 | 6.5 | 19 | 2 | ChEMBL | 493 | 5 | 1 | 6 | 2.4 | CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCN(c3ncc(C(F)(F)F)cc3F)[C@H](CO)C1)C(=O)C2 | 10.1016/j.bmcl.2008.11.008 | |||
CHEMBL481196 | 184009 | None | 0 | Human | Functional | pIC50 | = | 6.5 | 6.5 | 19 | 2 | ChEMBL | 493 | 5 | 1 | 6 | 2.4 | CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCN(c3ncc(C(F)(F)F)cc3F)[C@H](CO)C1)C(=O)C2 | 10.1016/j.bmcl.2008.11.008 | |||
44581160 | 175209 | None | 0 | Human | Functional | pIC50 | = | 5.5 | 5.5 | - | 1 | ChEMBL | 483 | 5 | 2 | 4 | 3.1 | NC(=O)c1cccc(C2(C3CCN(Cc4ccc(Br)cc4)CC3)CCC(=O)NC2=O)c1 | 10.1016/j.bmcl.2008.07.115 | |||
CHEMBL456904 | 175209 | None | 0 | Human | Functional | pIC50 | = | 5.5 | 5.5 | - | 1 | ChEMBL | 483 | 5 | 2 | 4 | 3.1 | NC(=O)c1cccc(C2(C3CCN(Cc4ccc(Br)cc4)CC3)CCC(=O)NC2=O)c1 | 10.1016/j.bmcl.2008.07.115 | |||
44581161 | 175210 | None | 0 | Human | Functional | pIC50 | = | 5.5 | 5.5 | - | 1 | ChEMBL | 497 | 5 | 2 | 4 | 3.4 | CNC(=O)c1cccc(C2(C3CCN(Cc4ccc(Br)cc4)CC3)CCC(=O)NC2=O)c1 | 10.1016/j.bmcl.2008.07.115 | |||
CHEMBL456905 | 175210 | None | 0 | Human | Functional | pIC50 | = | 5.5 | 5.5 | - | 1 | ChEMBL | 497 | 5 | 2 | 4 | 3.4 | CNC(=O)c1cccc(C2(C3CCN(Cc4ccc(Br)cc4)CC3)CCC(=O)NC2=O)c1 | 10.1016/j.bmcl.2008.07.115 | |||
44581070 | 193446 | None | 0 | Human | Functional | pIC50 | = | 5.5 | 5.5 | - | 1 | ChEMBL | 430 | 4 | 1 | 3 | 4.6 | O=C1CCC(c2ccccc2)(C2CCN(Cc3ccc(Cl)cc3Cl)CC2)C(=O)N1 | 10.1016/j.bmcl.2008.07.115 | |||
CHEMBL524627 | 193446 | None | 0 | Human | Functional | pIC50 | = | 5.5 | 5.5 | - | 1 | ChEMBL | 430 | 4 | 1 | 3 | 4.6 | O=C1CCC(c2ccccc2)(C2CCN(Cc3ccc(Cl)cc3Cl)CC2)C(=O)N1 | 10.1016/j.bmcl.2008.07.115 | |||
16214851 | 183170 | None | 0 | Human | Functional | pIC50 | = | 5.5 | 5.5 | - | 1 | ChEMBL | 490 | 5 | 0 | 7 | 2.9 | CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCN(c3ncc(C(F)(F)F)cc3[N+](=O)[O-])CC1)C(=O)C2 | 10.1016/j.bmcl.2008.11.008 | |||
CHEMBL479425 | 183170 | None | 0 | Human | Functional | pIC50 | = | 5.5 | 5.5 | - | 1 | ChEMBL | 490 | 5 | 0 | 7 | 2.9 | CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCN(c3ncc(C(F)(F)F)cc3[N+](=O)[O-])CC1)C(=O)C2 | 10.1016/j.bmcl.2008.11.008 | |||
44570628 | 191643 | None | 0 | Human | Functional | pIC50 | = | 4.5 | 4.5 | - | 1 | ChEMBL | 459 | 5 | 1 | 5 | 3.7 | CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC(Nc3ccc(C(F)(F)F)cn3)CC1)C(=O)C2 | 10.1016/j.bmcl.2008.11.008 | |||
CHEMBL519434 | 191643 | None | 0 | Human | Functional | pIC50 | = | 4.5 | 4.5 | - | 1 | ChEMBL | 459 | 5 | 1 | 5 | 3.7 | CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC(Nc3ccc(C(F)(F)F)cn3)CC1)C(=O)C2 | 10.1016/j.bmcl.2008.11.008 | |||
45101498 | 58200 | None | 0 | Human | Functional | pIC50 | = | 7.5 | 7.5 | - | 1 | ChEMBL | 475 | 5 | 1 | 5 | 3.9 | CNC(=O)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4)CC3)[C@@H](C)C2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
CHEMBL1681841 | 58200 | None | 0 | Human | Functional | pIC50 | = | 7.5 | 7.5 | - | 1 | ChEMBL | 475 | 5 | 1 | 5 | 3.9 | CNC(=O)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4)CC3)[C@@H](C)C2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
53319882 | 58240 | None | 0 | Human | Functional | pIC50 | = | 7.5 | 7.5 | - | 1 | ChEMBL | 533 | 7 | 1 | 5 | 4.8 | CCNC(=O)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4F)CC3)C(C3CC3)C2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
CHEMBL1681884 | 58240 | None | 0 | Human | Functional | pIC50 | = | 7.5 | 7.5 | - | 1 | ChEMBL | 533 | 7 | 1 | 5 | 4.8 | CCNC(=O)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4F)CC3)C(C3CC3)C2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
24739555 | 187885 | None | 0 | Human | Functional | pIC50 | = | 6.5 | 6.5 | - | 1 | ChEMBL | 484 | 5 | 0 | 3 | 5.9 | CCOC(=O)N1CCCC(c2ccccc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C1 | 10.1016/j.bmcl.2008.07.115 | |||
CHEMBL495753 | 187885 | None | 0 | Human | Functional | pIC50 | = | 6.5 | 6.5 | - | 1 | ChEMBL | 484 | 5 | 0 | 3 | 5.9 | CCOC(=O)N1CCCC(c2ccccc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C1 | 10.1016/j.bmcl.2008.07.115 | |||
44580798 | 193536 | None | 0 | Human | Functional | pIC50 | = | 6.5 | 6.5 | - | 1 | ChEMBL | 455 | 4 | 2 | 4 | 3.6 | Nc1cccc(C2(C3CCN(Cc4ccc(Br)cc4)CC3)CCC(=O)NC2=O)c1 | 10.1016/j.bmcl.2008.07.115 | |||
CHEMBL526097 | 193536 | None | 0 | Human | Functional | pIC50 | = | 6.5 | 6.5 | - | 1 | ChEMBL | 455 | 4 | 2 | 4 | 3.6 | Nc1cccc(C2(C3CCN(Cc4ccc(Br)cc4)CC3)CCC(=O)NC2=O)c1 | 10.1016/j.bmcl.2008.07.115 | |||
15604934 | 73013 | None | 0 | Human | Functional | pIC50 | = | 6.5 | 6.5 | - | 1 | ChEMBL | 565 | 8 | 3 | 4 | 4.9 | CCNC(=O)N1CCCN(c2ccc(C(=O)NCCc3ccc(F)cc3)cc2NC(=O)c2cccc(Cl)c2)CC1 | 10.1016/j.bmcl.2005.09.020 | |||
CHEMBL200759 | 73013 | None | 0 | Human | Functional | pIC50 | = | 6.5 | 6.5 | - | 1 | ChEMBL | 565 | 8 | 3 | 4 | 4.9 | CCNC(=O)N1CCCN(c2ccc(C(=O)NCCc3ccc(F)cc3)cc2NC(=O)c2cccc(Cl)c2)CC1 | 10.1016/j.bmcl.2005.09.020 | |||
89726440 | 142782 | None | 0 | Human | Functional | pIC50 | = | 6.5 | 6.5 | - | 1 | ChEMBL | 522 | 4 | 1 | 8 | 3.8 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4c(F)cccc4[nH]3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00676 | |||
CHEMBL3892103 | 142782 | None | 0 | Human | Functional | pIC50 | = | 6.5 | 6.5 | - | 1 | ChEMBL | 522 | 4 | 1 | 8 | 3.8 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4c(F)cccc4[nH]3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00676 | |||
168286958 | 191476 | None | 0 | Human | Functional | pIC50 | = | 6.5 | 6.5 | - | 1 | ChEMBL | 562 | 8 | 0 | 11 | 3.1 | COCCOc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3cnc4cccnc43)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL5192156 | 191476 | None | 0 | Human | Functional | pIC50 | = | 6.5 | 6.5 | - | 1 | ChEMBL | 562 | 8 | 0 | 11 | 3.1 | COCCOc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3cnc4cccnc43)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
168276987 | 190482 | None | 0 | Human | Functional | pIC50 | = | 7.5 | 7.5 | - | 1 | ChEMBL | 530 | 6 | 0 | 9 | 4.1 | CCCc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3cnc4cccnc43)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL5177288 | 190482 | None | 0 | Human | Functional | pIC50 | = | 7.5 | 7.5 | - | 1 | ChEMBL | 530 | 6 | 0 | 9 | 4.1 | CCCc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3cnc4cccnc43)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
24957182 | 153602 | None | 39 | Human | Functional | pIC50 | = | 6.5 | 6.5 | 63 | 2 | ChEMBL | 603 | 10 | 0 | 8 | 5.8 | CCOc1ccc(-n2c([C@@H](C)N(Cc3cccnc3)C(=O)Cc3ccc(OC(F)(F)F)cc3)nc3ncccc3c2=O)cc1 | 10.1016/j.bmcl.2008.07.115 | |||
CHEMBL397983 | 153602 | None | 39 | Human | Functional | pIC50 | = | 6.5 | 6.5 | 63 | 2 | ChEMBL | 603 | 10 | 0 | 8 | 5.8 | CCOc1ccc(-n2c([C@@H](C)N(Cc3cccnc3)C(=O)Cc3ccc(OC(F)(F)F)cc3)nc3ncccc3c2=O)cc1 | 10.1016/j.bmcl.2008.07.115 | |||
44593651 | 187843 | None | 0 | Human | Functional | pIC50 | = | 6.5 | 6.5 | - | 1 | ChEMBL | 476 | 4 | 1 | 3 | 4.3 | O=C1CCC(c2ccc(F)cc2F)(C2CCN(Cc3ccc(Br)cc3)CC2)C(=O)N1 | 10.1016/j.bmcl.2008.07.115 | |||
CHEMBL495531 | 187843 | None | 0 | Human | Functional | pIC50 | = | 6.5 | 6.5 | - | 1 | ChEMBL | 476 | 4 | 1 | 3 | 4.3 | O=C1CCC(c2ccc(F)cc2F)(C2CCN(Cc3ccc(Br)cc3)CC2)C(=O)N1 | 10.1016/j.bmcl.2008.07.115 | |||
117739228 | 145460 | None | 0 | Human | Functional | pIC50 | = | 6.5 | 6.5 | - | 1 | ChEMBL | 546 | 6 | 1 | 8 | 4.0 | Cc1nn(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccccc4[nH]3)C[C@H]2C)cc1CN(C)C | 10.1021/acs.jmedchem.2c00676 | |||
CHEMBL3913741 | 145460 | None | 0 | Human | Functional | pIC50 | = | 6.5 | 6.5 | - | 1 | ChEMBL | 546 | 6 | 1 | 8 | 4.0 | Cc1nn(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccccc4[nH]3)C[C@H]2C)cc1CN(C)C | 10.1021/acs.jmedchem.2c00676 | |||
71525425 | 132880 | None | 0 | Human | Functional | pIC50 | = | 5.5 | 5.5 | -977 | 5 | ChEMBL | 509 | 8 | 3 | 9 | 2.7 | Cc1ccc(C(Nc2c(Nc3ccc(Cl)c(S(=O)(=O)N(C)C)c3O)c(=O)c2=O)C2(C)COC2)o1 | nan | |||
CHEMBL3701196 | 132880 | None | 0 | Human | Functional | pIC50 | = | 5.5 | 5.5 | -977 | 5 | ChEMBL | 509 | 8 | 3 | 9 | 2.7 | Cc1ccc(C(Nc2c(Nc3ccc(Cl)c(S(=O)(=O)N(C)C)c3O)c(=O)c2=O)C2(C)COC2)o1 | nan | |||
168282969 | 190934 | None | 0 | Human | Functional | pIC50 | = | 6.5 | 6.5 | - | 1 | ChEMBL | 610 | 5 | 1 | 9 | 5.1 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccc(OC(F)(F)F)cc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | 10.1021/acs.jmedchem.2c00676 | |||
CHEMBL5183995 | 190934 | None | 0 | Human | Functional | pIC50 | = | 6.5 | 6.5 | - | 1 | ChEMBL | 610 | 5 | 1 | 9 | 5.1 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccc(OC(F)(F)F)cc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | 10.1021/acs.jmedchem.2c00676 | |||
168280503 | 190871 | None | 0 | Human | Functional | pIC50 | = | 5.5 | 5.5 | - | 1 | ChEMBL | 508 | 5 | 1 | 7 | 3.5 | COC1CCN(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccccc4[nH]3)C[C@H]2C)C1 | 10.1021/acs.jmedchem.2c00676 | |||
CHEMBL5183078 | 190871 | None | 0 | Human | Functional | pIC50 | = | 5.5 | 5.5 | - | 1 | ChEMBL | 508 | 5 | 1 | 7 | 3.5 | COC1CCN(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccccc4[nH]3)C[C@H]2C)C1 | 10.1021/acs.jmedchem.2c00676 | |||
46890725 | 7296 | None | 0 | Human | Functional | pIC50 | = | 6.5 | 6.5 | - | 1 | ChEMBL | 466 | 7 | 0 | 3 | 5.9 | O=S(=O)(c1ccc(Cl)cc1)N(Cc1ccc(-c2cccc(F)c2)cc1)Cc1ccccn1 | 10.1016/j.bmcl.2010.04.113 | |||
CHEMBL1086041 | 7296 | None | 0 | Human | Functional | pIC50 | = | 6.5 | 6.5 | - | 1 | ChEMBL | 466 | 7 | 0 | 3 | 5.9 | O=S(=O)(c1ccc(Cl)cc1)N(Cc1ccc(-c2cccc(F)c2)cc1)Cc1ccccn1 | 10.1016/j.bmcl.2010.04.113 | |||
45486530 | 200769 | None | 0 | Human | Functional | pIC50 | = | 7.5 | 7.5 | - | 1 | ChEMBL | 651 | 9 | 0 | 8 | 6.0 | C[C@H](c1nc2c(C3CC3)nccn2c1-c1ccc(C#N)cc1)N(CC1CCS(=O)(=O)CC1)C(=O)Cc1ccc(OC(F)(F)F)cc1 | 10.1016/j.bmcl.2009.07.021 | |||
CHEMBL576096 | 200769 | None | 0 | Human | Functional | pIC50 | = | 7.5 | 7.5 | - | 1 | ChEMBL | 651 | 9 | 0 | 8 | 6.0 | C[C@H](c1nc2c(C3CC3)nccn2c1-c1ccc(C#N)cc1)N(CC1CCS(=O)(=O)CC1)C(=O)Cc1ccc(OC(F)(F)F)cc1 | 10.1016/j.bmcl.2009.07.021 | |||
24774715 | 193173 | None | 0 | Human | Functional | pIC50 | = | 6.5 | 6.5 | - | 1 | ChEMBL | 414 | 4 | 1 | 3 | 4.1 | O=C1CCC(c2ccccc2)(C2CCN(Cc3ccc(Cl)c(F)c3)CC2)C(=O)N1 | 10.1016/j.bmcl.2008.07.115 | |||
CHEMBL522399 | 193173 | None | 0 | Human | Functional | pIC50 | = | 6.5 | 6.5 | - | 1 | ChEMBL | 414 | 4 | 1 | 3 | 4.1 | O=C1CCC(c2ccccc2)(C2CCN(Cc3ccc(Cl)c(F)c3)CC2)C(=O)N1 | 10.1016/j.bmcl.2008.07.115 | |||
15604859 | 73961 | None | 0 | Human | Functional | pIC50 | = | 6.5 | 6.5 | - | 1 | ChEMBL | 565 | 8 | 3 | 4 | 4.9 | CCNC(=O)N1CCCN(c2ccc(C(=O)NCCc3ccccc3F)cc2NC(=O)c2cccc(Cl)c2)CC1 | 10.1016/j.bmcl.2005.09.020 | |||
CHEMBL202086 | 73961 | None | 0 | Human | Functional | pIC50 | = | 6.5 | 6.5 | - | 1 | ChEMBL | 565 | 8 | 3 | 4 | 4.9 | CCNC(=O)N1CCCN(c2ccc(C(=O)NCCc3ccccc3F)cc2NC(=O)c2cccc(Cl)c2)CC1 | 10.1016/j.bmcl.2005.09.020 | |||
15605071 | 73981 | None | 0 | Human | Functional | pIC50 | = | 6.5 | 6.5 | - | 1 | ChEMBL | 565 | 8 | 3 | 4 | 4.9 | CCNC(=O)N1CCCN(c2ccc(C(=O)NCCc3cccc(F)c3)cc2NC(=O)c2cccc(Cl)c2)CC1 | 10.1016/j.bmcl.2005.09.020 | |||
CHEMBL202136 | 73981 | None | 0 | Human | Functional | pIC50 | = | 6.5 | 6.5 | - | 1 | ChEMBL | 565 | 8 | 3 | 4 | 4.9 | CCNC(=O)N1CCCN(c2ccc(C(=O)NCCc3cccc(F)c3)cc2NC(=O)c2cccc(Cl)c2)CC1 | 10.1016/j.bmcl.2005.09.020 | |||
44453362 | 97533 | None | 0 | Human | Functional | pIC50 | = | 5.5 | 5.5 | - | 1 | ChEMBL | 384 | 6 | 1 | 5 | 2.9 | CC(=O)N(C)CCn1c(=N)n(CC(=O)c2ccc(Cl)cc2)c2ccccc21 | 10.1016/j.bmcl.2008.02.049 | |||
CHEMBL270222 | 97533 | None | 0 | Human | Functional | pIC50 | = | 5.5 | 5.5 | - | 1 | ChEMBL | 384 | 6 | 1 | 5 | 2.9 | CC(=O)N(C)CCn1c(=N)n(CC(=O)c2ccc(Cl)cc2)c2ccccc21 | 10.1016/j.bmcl.2008.02.049 | |||
44253727 | 7125 | None | 0 | Human | Functional | pIC50 | = | 6.5 | 6.5 | - | 1 | ChEMBL | 500 | 10 | 1 | 4 | 5.0 | COc1ccc(S(=O)(=O)N(Cc2ccccc2)Cc2ccc(C(=O)NCc3ccccc3)cc2)cc1 | 10.1016/j.bmcl.2010.04.113 | |||
CHEMBL1085258 | 7125 | None | 0 | Human | Functional | pIC50 | = | 6.5 | 6.5 | - | 1 | ChEMBL | 500 | 10 | 1 | 4 | 5.0 | COc1ccc(S(=O)(=O)N(Cc2ccccc2)Cc2ccc(C(=O)NCc3ccccc3)cc2)cc1 | 10.1016/j.bmcl.2010.04.113 | |||
90479923 | 192379 | None | 0 | Human | Functional | pIC50 | = | 6.5 | 6.5 | - | 1 | ChEMBL | 506 | 5 | 0 | 9 | 3.4 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3cnc(C4CC4)nc3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL5205683 | 192379 | None | 0 | Human | Functional | pIC50 | = | 6.5 | 6.5 | - | 1 | ChEMBL | 506 | 5 | 0 | 9 | 3.4 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3cnc(C4CC4)nc3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00675 | |||
53326850 | 58203 | None | 0 | Human | Functional | pIC50 | = | 7.5 | 7.5 | - | 1 | ChEMBL | 501 | 4 | 1 | 5 | 4.4 | CNC(=O)c1cnc(N2CCN(C3CCN(C4CCc5cc(Cl)ccc54)CC3)[C@@H](C)C2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
CHEMBL1681844 | 58203 | None | 0 | Human | Functional | pIC50 | = | 7.5 | 7.5 | - | 1 | ChEMBL | 501 | 4 | 1 | 5 | 4.4 | CNC(=O)c1cnc(N2CCN(C3CCN(C4CCc5cc(Cl)ccc54)CC3)[C@@H](C)C2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
11599725 | 201066 | None | 0 | Human | Functional | pIC50 | = | 7.5 | 7.5 | - | 1 | ChEMBL | 605 | 7 | 1 | 5 | 6.4 | O=C(NCc1ccc(Cl)c(Cl)c1)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4)CC3)CC2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
CHEMBL578779 | 201066 | None | 0 | Human | Functional | pIC50 | = | 7.5 | 7.5 | - | 1 | ChEMBL | 605 | 7 | 1 | 5 | 6.4 | O=C(NCc1ccc(Cl)c(Cl)c1)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4)CC3)CC2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
9938326 | 168815 | None | 0 | Human | Functional | pIC50 | = | 6.5 | 6.5 | - | 1 | ChEMBL | 586 | 9 | 0 | 6 | 6.5 | CCOc1ccc(-n2c([C@@H](C)N(Cc3cccnc3)C(=O)Cc3ccc(C(F)(F)F)cc3)nc3ccccc3c2=O)cc1 | 10.1016/j.bmcl.2009.07.032 | |||
CHEMBL436826 | 168815 | None | 0 | Human | Functional | pIC50 | = | 6.5 | 6.5 | - | 1 | ChEMBL | 586 | 9 | 0 | 6 | 6.5 | CCOc1ccc(-n2c([C@@H](C)N(Cc3cccnc3)C(=O)Cc3ccc(C(F)(F)F)cc3)nc3ccccc3c2=O)cc1 | 10.1016/j.bmcl.2009.07.032 | |||
703050 | 169282 | None | 6 | Human | Functional | pIC50 | = | 5.5 | 5.5 | - | 1 | ChEMBL | 313 | 4 | 1 | 4 | 3.5 | CCn1c(=N)n(CC(=O)c2ccc(Cl)cc2)c2ccccc21 | 10.1016/j.bmcl.2008.02.049 | |||
CHEMBL440586 | 169282 | None | 6 | Human | Functional | pIC50 | = | 5.5 | 5.5 | - | 1 | ChEMBL | 313 | 4 | 1 | 4 | 3.5 | CCn1c(=N)n(CC(=O)c2ccc(Cl)cc2)c2ccccc21 | 10.1016/j.bmcl.2008.02.049 | |||
89726171 | 143715 | None | 0 | Human | Functional | pIC50 | = | 5.5 | 5.5 | - | 1 | ChEMBL | 489 | 4 | 0 | 8 | 3.6 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3n2C)CCN1C(=O)Cn1cccn1 | 10.1021/acs.jmedchem.2c00676 | |||
CHEMBL3899775 | 143715 | None | 0 | Human | Functional | pIC50 | = | 5.5 | 5.5 | - | 1 | ChEMBL | 489 | 4 | 0 | 8 | 3.6 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3n2C)CCN1C(=O)Cn1cccn1 | 10.1021/acs.jmedchem.2c00676 | |||
24957182 | 153602 | None | 39 | Human | Functional | pIC50 | = | 7.4 | 7.4 | 63 | 2 | ChEMBL | 603 | 10 | 0 | 8 | 5.8 | CCOc1ccc(-n2c([C@@H](C)N(Cc3cccnc3)C(=O)Cc3ccc(OC(F)(F)F)cc3)nc3ncccc3c2=O)cc1 | 10.1016/j.bmcl.2007.11.060 | |||
CHEMBL397983 | 153602 | None | 39 | Human | Functional | pIC50 | = | 7.4 | 7.4 | 63 | 2 | ChEMBL | 603 | 10 | 0 | 8 | 5.8 | CCOc1ccc(-n2c([C@@H](C)N(Cc3cccnc3)C(=O)Cc3ccc(OC(F)(F)F)cc3)nc3ncccc3c2=O)cc1 | 10.1016/j.bmcl.2007.11.060 | |||
45486532 | 200771 | None | 0 | Human | Functional | pIC50 | = | 7.4 | 7.4 | - | 1 | ChEMBL | 635 | 8 | 0 | 7 | 6.1 | C[C@H](c1nc2c(C3CC3)nccn2c1-c1ccc(C#N)cc1)N(CC1CCS(=O)(=O)CC1)C(=O)Cc1cccc(C(F)(F)F)c1 | 10.1016/j.bmcl.2009.07.021 | |||
CHEMBL576098 | 200771 | None | 0 | Human | Functional | pIC50 | = | 7.4 | 7.4 | - | 1 | ChEMBL | 635 | 8 | 0 | 7 | 6.1 | C[C@H](c1nc2c(C3CC3)nccn2c1-c1ccc(C#N)cc1)N(CC1CCS(=O)(=O)CC1)C(=O)Cc1cccc(C(F)(F)F)c1 | 10.1016/j.bmcl.2009.07.021 | |||
24957182 | 153602 | None | 39 | Human | Functional | pIC50 | = | 7.4 | 7.4 | 63 | 2 | ChEMBL | 603 | 10 | 0 | 8 | 5.8 | CCOc1ccc(-n2c([C@@H](C)N(Cc3cccnc3)C(=O)Cc3ccc(OC(F)(F)F)cc3)nc3ncccc3c2=O)cc1 | 10.1016/j.bmcl.2007.03.106 | |||
CHEMBL397983 | 153602 | None | 39 | Human | Functional | pIC50 | = | 7.4 | 7.4 | 63 | 2 | ChEMBL | 603 | 10 | 0 | 8 | 5.8 | CCOc1ccc(-n2c([C@@H](C)N(Cc3cccnc3)C(=O)Cc3ccc(OC(F)(F)F)cc3)nc3ncccc3c2=O)cc1 | 10.1016/j.bmcl.2007.03.106 | |||
46891224 | 7346 | None | 0 | Human | Functional | pIC50 | = | 6.4 | 6.4 | - | 1 | ChEMBL | 460 | 9 | 1 | 5 | 3.5 | N#Cc1ccc(S(=O)(=O)N(Cc2ccc(C(=O)NCC3CC3)cc2)Cc2ccccn2)cc1 | 10.1016/j.bmcl.2010.04.113 | |||
CHEMBL1086241 | 7346 | None | 0 | Human | Functional | pIC50 | = | 6.4 | 6.4 | - | 1 | ChEMBL | 460 | 9 | 1 | 5 | 3.5 | N#Cc1ccc(S(=O)(=O)N(Cc2ccc(C(=O)NCC3CC3)cc2)Cc2ccccn2)cc1 | 10.1016/j.bmcl.2010.04.113 | |||
168286976 | 191499 | None | 0 | Human | Functional | pIC50 | = | 6.4 | 6.4 | - | 1 | ChEMBL | 570 | 5 | 1 | 7 | 4.9 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)CN1C(=O)OC[C@@H]1c1ccccc1 | 10.1021/acs.jmedchem.2c00676 | |||
CHEMBL5192464 | 191499 | None | 0 | Human | Functional | pIC50 | = | 6.4 | 6.4 | - | 1 | ChEMBL | 570 | 5 | 1 | 7 | 4.9 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)CN1C(=O)OC[C@@H]1c1ccccc1 | 10.1021/acs.jmedchem.2c00676 | |||
44581110 | 192745 | None | 0 | Human | Functional | pIC50 | = | 5.4 | 5.4 | - | 1 | ChEMBL | 470 | 5 | 1 | 4 | 4.0 | COc1ccc(C2(C3CCN(Cc4ccc(Br)cc4)CC3)CCC(=O)NC2=O)cc1 | 10.1016/j.bmcl.2008.07.115 | |||
CHEMBL521704 | 192745 | None | 0 | Human | Functional | pIC50 | = | 5.4 | 5.4 | - | 1 | ChEMBL | 470 | 5 | 1 | 4 | 4.0 | COc1ccc(C2(C3CCN(Cc4ccc(Br)cc4)CC3)CCC(=O)NC2=O)cc1 | 10.1016/j.bmcl.2008.07.115 | |||
89726199 | 153527 | None | 0 | Human | Functional | pIC50 | = | 6.4 | 6.4 | - | 1 | ChEMBL | 589 | 5 | 1 | 10 | 3.5 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccc(N5CCOCC5)cc4[nH]3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00676 | |||
CHEMBL3979234 | 153527 | None | 0 | Human | Functional | pIC50 | = | 6.4 | 6.4 | - | 1 | ChEMBL | 589 | 5 | 1 | 10 | 3.5 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccc(N5CCOCC5)cc4[nH]3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00676 | |||
57402420 | 69987 | None | 0 | Human | Functional | pIC50 | = | 7.4 | 7.4 | - | 1 | ChEMBL | 641 | 7 | 0 | 8 | 4.8 | C[C@H](c1nc2ncccc2c(=O)n1-c1ccc(C#N)cc1)N(CC1CCS(=O)(=O)CC1)C(=O)Cc1ccc(C(F)(F)F)c(F)c1 | 10.1016/j.bmcl.2011.10.120 | |||
CHEMBL1939554 | 69987 | None | 0 | Human | Functional | pIC50 | = | 7.4 | 7.4 | - | 1 | ChEMBL | 641 | 7 | 0 | 8 | 4.8 | C[C@H](c1nc2ncccc2c(=O)n1-c1ccc(C#N)cc1)N(CC1CCS(=O)(=O)CC1)C(=O)Cc1ccc(C(F)(F)F)c(F)c1 | 10.1016/j.bmcl.2011.10.120 | |||
16416811 | 191931 | None | 7 | Human | Functional | pIC50 | = | 6.4 | 6.4 | - | 1 | ChEMBL | 415 | 5 | 1 | 6 | 3.7 | Cn1c(CN2CCN(c3ccccc3NC(=O)c3ccco3)CC2)nc2ccccc21 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL5198731 | 191931 | None | 7 | Human | Functional | pIC50 | = | 6.4 | 6.4 | - | 1 | ChEMBL | 415 | 5 | 1 | 6 | 3.7 | Cn1c(CN2CCN(c3ccccc3NC(=O)c3ccco3)CC2)nc2ccccc21 | 10.1021/acs.jmedchem.2c00675 | |||
168272767 | 190661 | None | 0 | Human | Functional | pIC50 | = | 6.4 | 6.4 | - | 1 | ChEMBL | 518 | 4 | 1 | 8 | 4.0 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4cccc(C)c4[nH]3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00676 | |||
CHEMBL5179941 | 190661 | None | 0 | Human | Functional | pIC50 | = | 6.4 | 6.4 | - | 1 | ChEMBL | 518 | 4 | 1 | 8 | 4.0 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4cccc(C)c4[nH]3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00676 | |||
89726538 | 152825 | None | 0 | Human | Functional | pIC50 | = | 7.4 | 7.4 | - | 1 | ChEMBL | 560 | 4 | 1 | 8 | 4.8 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3cc(Cl)ccc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | 10.1021/acs.jmedchem.2c00676 | |||
CHEMBL3973196 | 152825 | None | 0 | Human | Functional | pIC50 | = | 7.4 | 7.4 | - | 1 | ChEMBL | 560 | 4 | 1 | 8 | 4.8 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3cc(Cl)ccc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | 10.1021/acs.jmedchem.2c00676 | |||
57394143 | 69872 | None | 0 | Human | Functional | pIC50 | = | 7.4 | 7.4 | - | 1 | ChEMBL | 641 | 7 | 0 | 8 | 4.8 | C[C@H](c1nc2ncccc2c(=O)n1-c1ccc(C#N)cc1)N(CC1CCS(=O)(=O)CC1)C(=O)Cc1ccc(F)c(C(F)(F)F)c1 | 10.1016/j.bmcl.2011.10.120 | |||
CHEMBL1938408 | 69872 | None | 0 | Human | Functional | pIC50 | = | 7.4 | 7.4 | - | 1 | ChEMBL | 641 | 7 | 0 | 8 | 4.8 | C[C@H](c1nc2ncccc2c(=O)n1-c1ccc(C#N)cc1)N(CC1CCS(=O)(=O)CC1)C(=O)Cc1ccc(F)c(C(F)(F)F)c1 | 10.1016/j.bmcl.2011.10.120 | |||
53319879 | 58208 | None | 0 | Human | Functional | pIC50 | = | 7.4 | 7.4 | - | 1 | ChEMBL | 619 | 7 | 1 | 5 | 6.8 | C[C@H]1CN(C2CCN(Cc3ccc(Cl)cc3)CC2)CCN1c1ncc(C(=O)NCc2ccc(Cl)c(Cl)c2)cc1Cl | 10.1016/j.bmcl.2010.12.114 | |||
CHEMBL1681851 | 58208 | None | 0 | Human | Functional | pIC50 | = | 7.4 | 7.4 | - | 1 | ChEMBL | 619 | 7 | 1 | 5 | 6.8 | C[C@H]1CN(C2CCN(Cc3ccc(Cl)cc3)CC2)CCN1c1ncc(C(=O)NCc2ccc(Cl)c(Cl)c2)cc1Cl | 10.1016/j.bmcl.2010.12.114 | |||
53321184 | 58224 | None | 0 | Human | Functional | pIC50 | = | 7.4 | 7.4 | - | 1 | ChEMBL | 461 | 5 | 1 | 5 | 3.7 | C[C@H]1CN(c2ncc(C(N)=O)cc2Cl)CCN1C1CCN(Cc2ccc(Cl)cc2)CC1 | 10.1016/j.bmcl.2010.12.114 | |||
CHEMBL1681867 | 58224 | None | 0 | Human | Functional | pIC50 | = | 7.4 | 7.4 | - | 1 | ChEMBL | 461 | 5 | 1 | 5 | 3.7 | C[C@H]1CN(c2ncc(C(N)=O)cc2Cl)CCN1C1CCN(Cc2ccc(Cl)cc2)CC1 | 10.1016/j.bmcl.2010.12.114 | |||
44570274 | 177839 | None | 0 | Human | Functional | pIC50 | = | 7.4 | 7.4 | 39 | 2 | ChEMBL | 521 | 4 | 0 | 6 | 3.6 | C[C@H]1CN(S(=O)(=O)C[C@]23CC[C@H](CC24OCCO4)C3(C)C)CCN1c1ncc(C(F)(F)F)cc1F | 10.1016/j.bmcl.2008.11.008 | |||
CHEMBL464244 | 177839 | None | 0 | Human | Functional | pIC50 | = | 7.4 | 7.4 | 39 | 2 | ChEMBL | 521 | 4 | 0 | 6 | 3.6 | C[C@H]1CN(S(=O)(=O)C[C@]23CC[C@H](CC24OCCO4)C3(C)C)CCN1c1ncc(C(F)(F)F)cc1F | 10.1016/j.bmcl.2008.11.008 | |||
44570595 | 178499 | None | 0 | Human | Functional | pIC50 | = | 6.4 | 6.4 | - | 1 | ChEMBL | 475 | 5 | 1 | 6 | 2.3 | CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCN(c3ccc(C(F)(F)F)cn3)C(CO)C1)C(=O)C2 | 10.1016/j.bmcl.2008.11.008 | |||
CHEMBL465637 | 178499 | None | 0 | Human | Functional | pIC50 | = | 6.4 | 6.4 | - | 1 | ChEMBL | 475 | 5 | 1 | 6 | 2.3 | CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCN(c3ccc(C(F)(F)F)cn3)C(CO)C1)C(=O)C2 | 10.1016/j.bmcl.2008.11.008 | |||
44570430 | 184087 | None | 0 | Human | Functional | pIC50 | = | 6.4 | 6.4 | - | 1 | ChEMBL | 479 | 4 | 0 | 5 | 3.6 | CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCN(c3ncc(C(F)(F)F)cc3Cl)CC1)C(=O)C2 | 10.1016/j.bmcl.2008.11.008 | |||
CHEMBL481779 | 184087 | None | 0 | Human | Functional | pIC50 | = | 6.4 | 6.4 | - | 1 | ChEMBL | 479 | 4 | 0 | 5 | 3.6 | CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCN(c3ncc(C(F)(F)F)cc3Cl)CC1)C(=O)C2 | 10.1016/j.bmcl.2008.11.008 | |||
56673431 | 63954 | None | 0 | Human | Functional | pIC50 | = | 8.4 | 8.4 | -6 | 3 | ChEMBL | 426 | 2 | 2 | 2 | 4.3 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CCCC1 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1806523 | 63954 | None | 0 | Human | Functional | pIC50 | = | 8.4 | 8.4 | -6 | 3 | ChEMBL | 426 | 2 | 2 | 2 | 4.3 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CCCC1 | 10.1016/j.bmcl.2011.06.070 | |||
56680570 | 64252 | None | 0 | Human | Functional | pIC50 | = | 8.4 | 8.4 | -3 | 2 | ChEMBL | 438 | 2 | 2 | 2 | 4.8 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1C=CCCC1 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1809003 | 64252 | None | 0 | Human | Functional | pIC50 | = | 8.4 | 8.4 | -3 | 2 | ChEMBL | 438 | 2 | 2 | 2 | 4.8 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1C=CCCC1 | 10.1016/j.bmcl.2011.06.070 | |||
56677271 | 64266 | None | 0 | Human | Functional | pIC50 | = | 8.4 | 8.4 | -1 | 2 | ChEMBL | 444 | 2 | 2 | 2 | 4.4 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccc(F)cc2)C1)N1CCCC1 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1809017 | 64266 | None | 0 | Human | Functional | pIC50 | = | 8.4 | 8.4 | -1 | 2 | ChEMBL | 444 | 2 | 2 | 2 | 4.4 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccc(F)cc2)C1)N1CCCC1 | 10.1016/j.bmcl.2011.06.070 | |||
56673431 | 63954 | None | 0 | Mouse | Functional | pIC50 | = | 8.4 | 8.4 | 6 | 3 | ChEMBL | 426 | 2 | 2 | 2 | 4.3 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CCCC1 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1806523 | 63954 | None | 0 | Mouse | Functional | pIC50 | = | 8.4 | 8.4 | 6 | 3 | ChEMBL | 426 | 2 | 2 | 2 | 4.3 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CCCC1 | 10.1016/j.bmcl.2011.06.070 | |||
56677271 | 64266 | None | 0 | Mouse | Functional | pIC50 | = | 8.4 | 8.4 | 1 | 2 | ChEMBL | 444 | 2 | 2 | 2 | 4.4 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccc(F)cc2)C1)N1CCCC1 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1809017 | 64266 | None | 0 | Mouse | Functional | pIC50 | = | 8.4 | 8.4 | 1 | 2 | ChEMBL | 444 | 2 | 2 | 2 | 4.4 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccc(F)cc2)C1)N1CCCC1 | 10.1016/j.bmcl.2011.06.070 | |||
56680574 | 64283 | None | 0 | Mouse | Functional | pIC50 | = | 8.4 | 8.4 | 1 | 3 | ChEMBL | 470 | 4 | 2 | 4 | 3.7 | O=C([C@@H]1C=C2c3cccc4c3c(cn4CCO)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CCCC1 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1809038 | 64283 | None | 0 | Mouse | Functional | pIC50 | = | 8.4 | 8.4 | 1 | 3 | ChEMBL | 470 | 4 | 2 | 4 | 3.7 | O=C([C@@H]1C=C2c3cccc4c3c(cn4CCO)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CCCC1 | 10.1016/j.bmcl.2011.06.070 | |||
90479960 | 192231 | None | 0 | Human | Functional | pIC50 | = | 8.4 | 8.4 | - | 1 | ChEMBL | 536 | 6 | 0 | 10 | 3.5 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3cnc(OC4CCC4)nc3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL5203452 | 192231 | None | 0 | Human | Functional | pIC50 | = | 8.4 | 8.4 | - | 1 | ChEMBL | 536 | 6 | 0 | 10 | 3.5 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3cnc(OC4CCC4)nc3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00675 | |||
168285354 | 191596 | None | 0 | Human | Functional | pIC50 | = | 8.4 | 8.4 | - | 1 | ChEMBL | 532 | 6 | 0 | 10 | 3.5 | CCOc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3ncc4cccnc43)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL5193608 | 191596 | None | 0 | Human | Functional | pIC50 | = | 8.4 | 8.4 | - | 1 | ChEMBL | 532 | 6 | 0 | 10 | 3.5 | CCOc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3ncc4cccnc43)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
168287733 | 191912 | None | 0 | Human | Functional | pIC50 | = | 8.4 | 8.4 | - | 1 | ChEMBL | 517 | 5 | 0 | 9 | 3.7 | COc1ccc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3cnc4cccnc43)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL5198351 | 191912 | None | 0 | Human | Functional | pIC50 | = | 8.4 | 8.4 | - | 1 | ChEMBL | 517 | 5 | 0 | 9 | 3.7 | COc1ccc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3cnc4cccnc43)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
168282516 | 190932 | None | 0 | Human | Functional | pIC50 | = | 8.4 | 8.4 | - | 1 | ChEMBL | 475 | 5 | 1 | 7 | 3.1 | O=C(Nc1cccnc1N1CCN(C(=O)Cn2cnc3cccnc32)CC1)c1cccc(Cl)c1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL5183980 | 190932 | None | 0 | Human | Functional | pIC50 | = | 8.4 | 8.4 | - | 1 | ChEMBL | 475 | 5 | 1 | 7 | 3.1 | O=C(Nc1cccnc1N1CCN(C(=O)Cn2cnc3cccnc32)CC1)c1cccc(Cl)c1 | 10.1021/acs.jmedchem.2c00675 | |||
90480049 | 192137 | None | 0 | Human | Functional | pIC50 | = | 8.4 | 8.4 | - | 1 | ChEMBL | 533 | 4 | 0 | 8 | 4.2 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3ccc(C(F)(F)F)nc3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL5201967 | 192137 | None | 0 | Human | Functional | pIC50 | = | 8.4 | 8.4 | - | 1 | ChEMBL | 533 | 4 | 0 | 8 | 4.2 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3ccc(C(F)(F)F)nc3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00675 | |||
168279505 | 190879 | None | 0 | Human | Functional | pIC50 | = | 8.4 | 8.4 | - | 1 | ChEMBL | 437 | 4 | 1 | 6 | 3.3 | O=C(Cn1cnc2cccnc21)N1CCN(c2ccccc2-c2nc3ccccc3[nH]2)CC1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL5183256 | 190879 | None | 0 | Human | Functional | pIC50 | = | 8.4 | 8.4 | - | 1 | ChEMBL | 437 | 4 | 1 | 6 | 3.3 | O=C(Cn1cnc2cccnc21)N1CCN(c2ccccc2-c2nc3ccccc3[nH]2)CC1 | 10.1021/acs.jmedchem.2c00675 | |||
90480457 | 191736 | None | 0 | Human | Functional | pIC50 | = | 8.4 | 8.4 | - | 1 | ChEMBL | 508 | 6 | 0 | 9 | 3.5 | CCCc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3nc(C)nc3C)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL5195689 | 191736 | None | 0 | Human | Functional | pIC50 | = | 8.4 | 8.4 | - | 1 | ChEMBL | 508 | 6 | 0 | 9 | 3.5 | CCCc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3nc(C)nc3C)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
89726228 | 150040 | None | 0 | Human | Functional | pIC50 | = | 8.3 | 8.3 | - | 1 | ChEMBL | 556 | 5 | 2 | 9 | 3.7 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccc(CO)cc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | 10.1021/acs.jmedchem.2c00676 | |||
CHEMBL3949824 | 150040 | None | 0 | Human | Functional | pIC50 | = | 8.3 | 8.3 | - | 1 | ChEMBL | 556 | 5 | 2 | 9 | 3.7 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccc(CO)cc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | 10.1021/acs.jmedchem.2c00676 | |||
168286958 | 191476 | None | 0 | Human | Functional | pIC50 | = | 8.3 | 8.3 | - | 1 | ChEMBL | 562 | 8 | 0 | 11 | 3.1 | COCCOc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3cnc4cccnc43)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL5192156 | 191476 | None | 0 | Human | Functional | pIC50 | = | 8.3 | 8.3 | - | 1 | ChEMBL | 562 | 8 | 0 | 11 | 3.1 | COCCOc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3cnc4cccnc43)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
53322504 | 58205 | None | 0 | Human | Functional | pIC50 | = | 7.4 | 7.4 | 2 | 3 | ChEMBL | 573 | 7 | 1 | 5 | 5.4 | O=C(NCc1ccc(F)c(F)c1)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4)CC3)CC2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
CHEMBL1681848 | 58205 | None | 0 | Human | Functional | pIC50 | = | 7.4 | 7.4 | 2 | 3 | ChEMBL | 573 | 7 | 1 | 5 | 5.4 | O=C(NCc1ccc(F)c(F)c1)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4)CC3)CC2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
44453168 | 95357 | None | 0 | Human | Functional | pIC50 | = | 7.4 | 7.4 | 20 | 2 | ChEMBL | 544 | 8 | 1 | 5 | 6.4 | CN(CCCn1c(=N)n(CC(=O)c2ccc(Cl)cc2)c2cccc(Cl)c21)C(=O)c1ccc2ccccc2c1 | 10.1016/j.bmcl.2008.02.049 | |||
CHEMBL256457 | 95357 | None | 0 | Human | Functional | pIC50 | = | 7.4 | 7.4 | 20 | 2 | ChEMBL | 544 | 8 | 1 | 5 | 6.4 | CN(CCCn1c(=N)n(CC(=O)c2ccc(Cl)cc2)c2cccc(Cl)c21)C(=O)c1ccc2ccccc2c1 | 10.1016/j.bmcl.2008.02.049 | |||
56667006 | 64261 | None | 0 | Mouse | Functional | pIC50 | = | 7.4 | 7.4 | 2 | 2 | ChEMBL | 472 | 2 | 4 | 4 | 2.6 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CC[C@@H](O)[C@@H](O)C1 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1809012 | 64261 | None | 0 | Mouse | Functional | pIC50 | = | 7.4 | 7.4 | 2 | 2 | ChEMBL | 472 | 2 | 4 | 4 | 2.6 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CC[C@@H](O)[C@@H](O)C1 | 10.1016/j.bmcl.2011.06.070 | |||
44453266 | 95485 | None | 0 | Human | Functional | pIC50 | = | 6.4 | 6.4 | - | 1 | ChEMBL | 522 | 10 | 1 | 5 | 5.6 | CN(CCCCn1c(=N)n(CC(=O)c2ccc(Cl)cc2)c2cccc(Cl)c21)C(=O)Cc1ccccc1 | 10.1016/j.bmcl.2008.02.049 | |||
CHEMBL257031 | 95485 | None | 0 | Human | Functional | pIC50 | = | 6.4 | 6.4 | - | 1 | ChEMBL | 522 | 10 | 1 | 5 | 5.6 | CN(CCCCn1c(=N)n(CC(=O)c2ccc(Cl)cc2)c2cccc(Cl)c21)C(=O)Cc1ccccc1 | 10.1016/j.bmcl.2008.02.049 | |||
44453201 | 155687 | None | 0 | Human | Functional | pIC50 | = | 6.4 | 6.4 | - | 1 | ChEMBL | 474 | 7 | 1 | 5 | 5.0 | CN(CCCn1c(=N)n(CC(=O)c2ccc(Cl)cc2)c2cccc(Cl)c21)C(=O)C(C)(C)C | 10.1016/j.bmcl.2008.02.049 | |||
CHEMBL404517 | 155687 | None | 0 | Human | Functional | pIC50 | = | 6.4 | 6.4 | - | 1 | ChEMBL | 474 | 7 | 1 | 5 | 5.0 | CN(CCCn1c(=N)n(CC(=O)c2ccc(Cl)cc2)c2cccc(Cl)c21)C(=O)C(C)(C)C | 10.1016/j.bmcl.2008.02.049 | |||
44454824 | 95175 | None | 0 | Human | Functional | pIC50 | = | 6.4 | 6.4 | - | 1 | ChEMBL | 341 | 5 | 1 | 4 | 3.9 | CCCc1cccc2c1n(C)c(=N)n2CC(=O)c1ccc(Cl)cc1 | 10.1016/j.bmcl.2008.01.074 | |||
CHEMBL255546 | 95175 | None | 0 | Human | Functional | pIC50 | = | 6.4 | 6.4 | - | 1 | ChEMBL | 341 | 5 | 1 | 4 | 3.9 | CCCc1cccc2c1n(C)c(=N)n2CC(=O)c1ccc(Cl)cc1 | 10.1016/j.bmcl.2008.01.074 | |||
25032779 | 154708 | None | 0 | Human | Functional | pIC50 | = | 7.4 | 7.4 | - | 1 | ChEMBL | 614 | 9 | 0 | 7 | 5.0 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc2ccccn2c(=O)c1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2007.11.060 | |||
CHEMBL399285 | 154708 | None | 0 | Human | Functional | pIC50 | = | 7.4 | 7.4 | - | 1 | ChEMBL | 614 | 9 | 0 | 7 | 5.0 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc2ccccn2c(=O)c1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2007.11.060 | |||
168280503 | 190871 | None | 0 | Human | Functional | pIC50 | = | 7.4 | 7.4 | - | 1 | ChEMBL | 508 | 5 | 1 | 7 | 3.5 | COC1CCN(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccccc4[nH]3)C[C@H]2C)C1 | 10.1021/acs.jmedchem.2c00676 | |||
CHEMBL5183078 | 190871 | None | 0 | Human | Functional | pIC50 | = | 7.4 | 7.4 | - | 1 | ChEMBL | 508 | 5 | 1 | 7 | 3.5 | COC1CCN(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccccc4[nH]3)C[C@H]2C)C1 | 10.1021/acs.jmedchem.2c00676 | |||
15604937 | 141155 | None | 0 | Human | Functional | pIC50 | = | 6.4 | 6.4 | - | 1 | ChEMBL | 607 | 10 | 3 | 6 | 4.8 | CCNC(=O)N1CCCN(c2ccc(C(=O)NCCc3ccc(OC)c(OC)c3)cc2NC(=O)c2cccc(Cl)c2)CC1 | 10.1016/j.bmcl.2005.09.020 | |||
CHEMBL382502 | 141155 | None | 0 | Human | Functional | pIC50 | = | 6.4 | 6.4 | - | 1 | ChEMBL | 607 | 10 | 3 | 6 | 4.8 | CCNC(=O)N1CCCN(c2ccc(C(=O)NCCc3ccc(OC)c(OC)c3)cc2NC(=O)c2cccc(Cl)c2)CC1 | 10.1016/j.bmcl.2005.09.020 | |||
89726224 | 143657 | None | 0 | Human | Functional | pIC50 | = | 5.4 | 5.4 | - | 1 | ChEMBL | 444 | 4 | 1 | 8 | 2.8 | O=C(Cn1cnc2cccnc21)N1CCN(c2ncsc2-c2nc3ccccc3[nH]2)CC1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL3899217 | 143657 | None | 0 | Human | Functional | pIC50 | = | 5.4 | 5.4 | - | 1 | ChEMBL | 444 | 4 | 1 | 8 | 2.8 | O=C(Cn1cnc2cccnc21)N1CCN(c2ncsc2-c2nc3ccccc3[nH]2)CC1 | 10.1021/acs.jmedchem.2c00675 | |||
168286207 | 191625 | None | 0 | Human | Functional | pIC50 | = | 6.4 | 6.4 | - | 1 | ChEMBL | 538 | 4 | 2 | 9 | 3.5 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccc(O)c(F)c4[nH]3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00676 | |||
CHEMBL5193975 | 191625 | None | 0 | Human | Functional | pIC50 | = | 6.4 | 6.4 | - | 1 | ChEMBL | 538 | 4 | 2 | 9 | 3.5 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccc(O)c(F)c4[nH]3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00676 | |||
44581069 | 188171 | None | 0 | Human | Functional | pIC50 | = | 5.4 | 5.4 | - | 1 | ChEMBL | 392 | 5 | 1 | 4 | 3.3 | COc1ccc(CN2CCC(C3(c4ccccc4)CCC(=O)NC3=O)CC2)cc1 | 10.1016/j.bmcl.2008.07.115 | |||
CHEMBL497809 | 188171 | None | 0 | Human | Functional | pIC50 | = | 5.4 | 5.4 | - | 1 | ChEMBL | 392 | 5 | 1 | 4 | 3.3 | COc1ccc(CN2CCC(C3(c4ccccc4)CCC(=O)NC3=O)CC2)cc1 | 10.1016/j.bmcl.2008.07.115 | |||
56660098 | 64246 | None | 0 | Mouse | Functional | pIC50 | = | 6.4 | 6.4 | -1 | 2 | ChEMBL | 488 | 8 | 2 | 4 | 3.8 | COCCN(CCOC)C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1808997 | 64246 | None | 0 | Mouse | Functional | pIC50 | = | 6.4 | 6.4 | -1 | 2 | ChEMBL | 488 | 8 | 2 | 4 | 3.8 | COCCN(CCOC)C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1 | 10.1016/j.bmcl.2011.06.070 | |||
45486524 | 201008 | None | 0 | Human | Functional | pIC50 | = | 7.4 | 7.4 | - | 1 | ChEMBL | 601 | 9 | 0 | 7 | 5.3 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(C(F)(F)F)c(F)c1)[C@H](C)c1nc2c(C)nccn2c1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2009.07.021 | |||
CHEMBL578188 | 201008 | None | 0 | Human | Functional | pIC50 | = | 7.4 | 7.4 | - | 1 | ChEMBL | 601 | 9 | 0 | 7 | 5.3 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(C(F)(F)F)c(F)c1)[C@H](C)c1nc2c(C)nccn2c1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2009.07.021 | |||
46891478 | 6469 | None | 0 | Human | Functional | pIC50 | = | 6.4 | 6.4 | - | 1 | ChEMBL | 458 | 7 | 1 | 6 | 3.4 | O=S(=O)(c1ccc(Cl)cc1)N(Cc1ccc(-c2nnn[nH]2)c(F)c1)Cc1ccccn1 | 10.1016/j.bmcl.2010.04.113 | |||
CHEMBL1082623 | 6469 | None | 0 | Human | Functional | pIC50 | = | 6.4 | 6.4 | - | 1 | ChEMBL | 458 | 7 | 1 | 6 | 3.4 | O=S(=O)(c1ccc(Cl)cc1)N(Cc1ccc(-c2nnn[nH]2)c(F)c1)Cc1ccccn1 | 10.1016/j.bmcl.2010.04.113 | |||
56834986 | 69992 | None | 0 | Human | Functional | pIC50 | = | 7.4 | 7.4 | 19 | 2 | ChEMBL | 650 | 7 | 0 | 7 | 5.5 | C[C@H](c1nc2ncccc2c(=O)n1-c1ccc(Cl)cc1)N(CC1CCS(=O)(=O)CC1)C(=O)Cc1ccc(F)c(C(F)(F)F)c1 | 10.1016/j.bmcl.2011.10.120 | |||
CHEMBL1939559 | 69992 | None | 0 | Human | Functional | pIC50 | = | 7.4 | 7.4 | 19 | 2 | ChEMBL | 650 | 7 | 0 | 7 | 5.5 | C[C@H](c1nc2ncccc2c(=O)n1-c1ccc(Cl)cc1)N(CC1CCS(=O)(=O)CC1)C(=O)Cc1ccc(F)c(C(F)(F)F)c1 | 10.1016/j.bmcl.2011.10.120 | |||
45482795 | 201350 | None | 0 | Human | Functional | pIC50 | = | 7.4 | 7.4 | - | 1 | ChEMBL | 442 | 4 | 2 | 2 | 4.8 | CCN(CC)C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2cccc(C)c2)C1 | 10.1016/j.bmcl.2009.09.002 | |||
CHEMBL584356 | 201350 | None | 0 | Human | Functional | pIC50 | = | 7.4 | 7.4 | - | 1 | ChEMBL | 442 | 4 | 2 | 2 | 4.8 | CCN(CC)C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2cccc(C)c2)C1 | 10.1016/j.bmcl.2009.09.002 | |||
45484739 | 199754 | None | 0 | Human | Functional | pIC50 | = | 7.4 | 7.4 | - | 1 | ChEMBL | 558 | 9 | 1 | 7 | 4.2 | N#Cc1ccc(CN2CCC(N3CCN(c4ncc(C(=O)NCCOc5ccccc5)cc4Cl)CC3)CC2)cc1 | 10.1016/j.bmcl.2009.07.020 | |||
CHEMBL568676 | 199754 | None | 0 | Human | Functional | pIC50 | = | 7.4 | 7.4 | - | 1 | ChEMBL | 558 | 9 | 1 | 7 | 4.2 | N#Cc1ccc(CN2CCC(N3CCN(c4ncc(C(=O)NCCOc5ccccc5)cc4Cl)CC3)CC2)cc1 | 10.1016/j.bmcl.2009.07.020 | |||
45486528 | 200093 | None | 0 | Human | Functional | pIC50 | = | 7.4 | 7.4 | - | 1 | ChEMBL | 630 | 10 | 0 | 8 | 5.1 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(C(F)(F)F)c(F)c1)C(C)c1nc2c(N(C)C)nccn2c1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2009.07.021 | |||
CHEMBL570857 | 200093 | None | 0 | Human | Functional | pIC50 | = | 7.4 | 7.4 | - | 1 | ChEMBL | 630 | 10 | 0 | 8 | 5.1 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(C(F)(F)F)c(F)c1)C(C)c1nc2c(N(C)C)nccn2c1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2009.07.021 | |||
46883289 | 5649 | None | 0 | Human | Functional | pIC50 | = | 6.4 | 6.4 | - | 1 | ChEMBL | 576 | 9 | 0 | 8 | 5.2 | CCOc1ccc(-n2c([C@@H](C)N(Cc3cccnc3)C(=O)Cn3cnc(C(F)(F)F)c3)nc3ccccc3c2=O)cc1 | 10.1016/j.bmcl.2009.07.032 | |||
CHEMBL1077809 | 5649 | None | 0 | Human | Functional | pIC50 | = | 6.4 | 6.4 | - | 1 | ChEMBL | 576 | 9 | 0 | 8 | 5.2 | CCOc1ccc(-n2c([C@@H](C)N(Cc3cccnc3)C(=O)Cn3cnc(C(F)(F)F)c3)nc3ccccc3c2=O)cc1 | 10.1016/j.bmcl.2009.07.032 | |||
45485420 | 200042 | None | 0 | Human | Functional | pIC50 | = | 5.4 | 5.4 | - | 1 | ChEMBL | 605 | 7 | 1 | 5 | 6.4 | O=C(NCc1ccc(Cl)c(Cl)c1)c1cnc(N2CCC(N3CCN(Cc4ccc(Cl)cc4)CC3)CC2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
CHEMBL570509 | 200042 | None | 0 | Human | Functional | pIC50 | = | 5.4 | 5.4 | - | 1 | ChEMBL | 605 | 7 | 1 | 5 | 6.4 | O=C(NCc1ccc(Cl)c(Cl)c1)c1cnc(N2CCC(N3CCN(Cc4ccc(Cl)cc4)CC3)CC2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
56667005 | 64253 | None | 0 | Human | Functional | pIC50 | = | 6.3 | 6.3 | 2 | 2 | ChEMBL | 441 | 2 | 3 | 3 | 3.1 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CCNCC1 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1809004 | 64253 | None | 0 | Human | Functional | pIC50 | = | 6.3 | 6.3 | 2 | 2 | ChEMBL | 441 | 2 | 3 | 3 | 3.1 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CCNCC1 | 10.1016/j.bmcl.2011.06.070 | |||
197750 | 98353 | None | 0 | Human | Functional | pIC50 | = | 5.3 | 5.3 | - | 1 | ChEMBL | 380 | 4 | 1 | 3 | 3.4 | O=C1CCC(c2ccccc2)(C2CCN(Cc3ccc(F)cc3)CC2)C(=O)N1 | 10.1016/j.bmcl.2008.07.115 | |||
CHEMBL274817 | 98353 | None | 0 | Human | Functional | pIC50 | = | 5.3 | 5.3 | - | 1 | ChEMBL | 380 | 4 | 1 | 3 | 3.4 | O=C1CCC(c2ccccc2)(C2CCN(Cc3ccc(F)cc3)CC2)C(=O)N1 | 10.1016/j.bmcl.2008.07.115 | |||
45486560 | 201013 | None | 0 | Human | Functional | pIC50 | = | 7.3 | 7.3 | - | 1 | ChEMBL | 615 | 9 | 0 | 8 | 4.4 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(C(F)(F)F)c(F)c1)[C@H](C)c1nc2ncccc2c(=O)n1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2011.10.120 | |||
CHEMBL578197 | 201013 | None | 0 | Human | Functional | pIC50 | = | 7.3 | 7.3 | - | 1 | ChEMBL | 615 | 9 | 0 | 8 | 4.4 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(C(F)(F)F)c(F)c1)[C@H](C)c1nc2ncccc2c(=O)n1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2011.10.120 | |||
168269369 | 190027 | None | 0 | Human | Functional | pIC50 | = | 7.3 | 7.3 | - | 1 | ChEMBL | 531 | 6 | 0 | 9 | 4.1 | CCOc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3ccc4cccnc43)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL5169888 | 190027 | None | 0 | Human | Functional | pIC50 | = | 7.3 | 7.3 | - | 1 | ChEMBL | 531 | 6 | 0 | 9 | 4.1 | CCOc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3ccc4cccnc43)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
44253450 | 6478 | None | 0 | Human | Functional | pIC50 | = | 6.3 | 6.3 | - | 1 | ChEMBL | 457 | 7 | 1 | 5 | 4.1 | O=S(=O)(c1ccc(Cl)cc1)N(Cc1ccc(-c2nnn[nH]2)cc1)Cc1ccccc1F | 10.1016/j.bmcl.2010.04.113 | |||
CHEMBL1082648 | 6478 | None | 0 | Human | Functional | pIC50 | = | 6.3 | 6.3 | - | 1 | ChEMBL | 457 | 7 | 1 | 5 | 4.1 | O=S(=O)(c1ccc(Cl)cc1)N(Cc1ccc(-c2nnn[nH]2)cc1)Cc1ccccc1F | 10.1016/j.bmcl.2010.04.113 | |||
44447091 | 94752 | None | 0 | Human | Functional | pIC50 | = | 7.3 | 7.3 | - | 1 | ChEMBL | 598 | 9 | 0 | 6 | 5.9 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc2ncccc2cc1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2007.11.060 | |||
CHEMBL252819 | 94752 | None | 0 | Human | Functional | pIC50 | = | 7.3 | 7.3 | - | 1 | ChEMBL | 598 | 9 | 0 | 6 | 5.9 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc2ncccc2cc1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2007.11.060 | |||
168295351 | 192352 | None | 0 | Human | Functional | pIC50 | = | 5.3 | 5.3 | - | 1 | ChEMBL | 439 | 4 | 1 | 8 | 2.1 | O=C(Cn1cnc2cccnc21)N1CCN(c2nnccc2-c2nc3ccccc3[nH]2)CC1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL5205299 | 192352 | None | 0 | Human | Functional | pIC50 | = | 5.3 | 5.3 | - | 1 | ChEMBL | 439 | 4 | 1 | 8 | 2.1 | O=C(Cn1cnc2cccnc21)N1CCN(c2nnccc2-c2nc3ccccc3[nH]2)CC1 | 10.1021/acs.jmedchem.2c00675 | |||
168282215 | 191054 | None | 0 | Human | Functional | pIC50 | = | 7.3 | 7.3 | - | 1 | ChEMBL | 531 | 6 | 0 | 9 | 4.1 | CCOc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3cnc4ccccc43)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL5185762 | 191054 | None | 0 | Human | Functional | pIC50 | = | 7.3 | 7.3 | - | 1 | ChEMBL | 531 | 6 | 0 | 9 | 4.1 | CCOc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3cnc4ccccc43)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
15605012 | 140377 | None | 0 | Human | Functional | pIC50 | = | 6.3 | 6.3 | - | 1 | ChEMBL | 587 | 8 | 3 | 5 | 5.5 | CCNC(=O)N1CCCN(c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2NC(=O)c2ccsc2)CC1 | 10.1016/j.bmcl.2005.09.020 | |||
CHEMBL380594 | 140377 | None | 0 | Human | Functional | pIC50 | = | 6.3 | 6.3 | - | 1 | ChEMBL | 587 | 8 | 3 | 5 | 5.5 | CCNC(=O)N1CCCN(c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2NC(=O)c2ccsc2)CC1 | 10.1016/j.bmcl.2005.09.020 | |||
44253446 | 6477 | None | 0 | Human | Functional | pIC50 | = | 6.3 | 6.3 | - | 1 | ChEMBL | 440 | 7 | 1 | 6 | 3.3 | O=S(=O)(c1ccc(Cl)cc1)N(Cc1ccc(-c2nnn[nH]2)cc1)Cc1ccccn1 | 10.1016/j.bmcl.2010.04.113 | |||
CHEMBL1082641 | 6477 | None | 0 | Human | Functional | pIC50 | = | 6.3 | 6.3 | - | 1 | ChEMBL | 440 | 7 | 1 | 6 | 3.3 | O=S(=O)(c1ccc(Cl)cc1)N(Cc1ccc(-c2nnn[nH]2)cc1)Cc1ccccn1 | 10.1016/j.bmcl.2010.04.113 | |||
168274591 | 190472 | None | 0 | Human | Functional | pIC50 | = | 6.3 | 6.3 | - | 1 | ChEMBL | 438 | 4 | 1 | 7 | 2.7 | O=C(Cn1cnc2cccnc21)N1CCN(c2ncccc2-c2nc3ccccc3[nH]2)CC1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL5177124 | 190472 | None | 0 | Human | Functional | pIC50 | = | 6.3 | 6.3 | - | 1 | ChEMBL | 438 | 4 | 1 | 7 | 2.7 | O=C(Cn1cnc2cccnc21)N1CCN(c2ncccc2-c2nc3ccccc3[nH]2)CC1 | 10.1021/acs.jmedchem.2c00675 | |||
46883308 | 5669 | None | 0 | Human | Functional | pIC50 | = | 8.3 | 8.3 | - | 1 | ChEMBL | 639 | 9 | 0 | 7 | 6.3 | CCOc1ccc(-n2c([C@@H](C)N(C(=O)Cc3ccc(F)c(C(F)(F)F)c3)C3CCN(C(C)C)CC3)nc3ncccc3c2=O)cc1 | 10.1016/j.bmcl.2009.07.032 | |||
CHEMBL1077828 | 5669 | None | 0 | Human | Functional | pIC50 | = | 8.3 | 8.3 | - | 1 | ChEMBL | 639 | 9 | 0 | 7 | 6.3 | CCOc1ccc(-n2c([C@@H](C)N(C(=O)Cc3ccc(F)c(C(F)(F)F)c3)C3CCN(C(C)C)CC3)nc3ncccc3c2=O)cc1 | 10.1016/j.bmcl.2009.07.032 | |||
53322459 | 58192 | None | 0 | Human | Functional | pIC50 | = | 8.3 | 8.3 | - | 1 | ChEMBL | 489 | 5 | 1 | 5 | 4.5 | CNC(=O)c1cnc(N2CCN(C3CCN(C(C)c4ccc(Cl)cc4)CC3)[C@@H](C)C2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
CHEMBL1681832 | 58192 | None | 0 | Human | Functional | pIC50 | = | 8.3 | 8.3 | - | 1 | ChEMBL | 489 | 5 | 1 | 5 | 4.5 | CNC(=O)c1cnc(N2CCN(C3CCN(C(C)c4ccc(Cl)cc4)CC3)[C@@H](C)C2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
53321185 | 58226 | None | 0 | Human | Functional | pIC50 | = | 8.3 | 8.3 | - | 1 | ChEMBL | 503 | 6 | 1 | 5 | 4.7 | CC(C)NC(=O)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4)CC3)[C@@H](C)C2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
CHEMBL1681869 | 58226 | None | 0 | Human | Functional | pIC50 | = | 8.3 | 8.3 | - | 1 | ChEMBL | 503 | 6 | 1 | 5 | 4.7 | CC(C)NC(=O)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4)CC3)[C@@H](C)C2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
24957182 | 153602 | None | 39 | Human | Functional | pIC50 | = | 8.3 | 8.3 | 63 | 2 | ChEMBL | 603 | 10 | 0 | 8 | 5.8 | CCOc1ccc(-n2c([C@@H](C)N(Cc3cccnc3)C(=O)Cc3ccc(OC(F)(F)F)cc3)nc3ncccc3c2=O)cc1 | 10.1016/j.bmcl.2007.03.106 | |||
CHEMBL397983 | 153602 | None | 39 | Human | Functional | pIC50 | = | 8.3 | 8.3 | 63 | 2 | ChEMBL | 603 | 10 | 0 | 8 | 5.8 | CCOc1ccc(-n2c([C@@H](C)N(Cc3cccnc3)C(=O)Cc3ccc(OC(F)(F)F)cc3)nc3ncccc3c2=O)cc1 | 10.1016/j.bmcl.2007.03.106 | |||
56673937 | 64249 | None | 0 | Human | Functional | pIC50 | = | 8.3 | 8.3 | -5 | 3 | ChEMBL | 440 | 2 | 2 | 2 | 4.7 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CCCCC1 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1809000 | 64249 | None | 0 | Human | Functional | pIC50 | = | 8.3 | 8.3 | -5 | 3 | ChEMBL | 440 | 2 | 2 | 2 | 4.7 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CCCCC1 | 10.1016/j.bmcl.2011.06.070 | |||
56670448 | 64260 | None | 0 | Human | Functional | pIC50 | = | 8.3 | 8.3 | -3 | 3 | ChEMBL | 456 | 2 | 3 | 3 | 3.6 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CCC(O)CC1 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1809011 | 64260 | None | 0 | Human | Functional | pIC50 | = | 8.3 | 8.3 | -3 | 3 | ChEMBL | 456 | 2 | 3 | 3 | 3.6 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CCC(O)CC1 | 10.1016/j.bmcl.2011.06.070 | |||
56680574 | 64283 | None | 0 | Human | Functional | pIC50 | = | 8.3 | 8.3 | -1 | 3 | ChEMBL | 470 | 4 | 2 | 4 | 3.7 | O=C([C@@H]1C=C2c3cccc4c3c(cn4CCO)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CCCC1 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1809038 | 64283 | None | 0 | Human | Functional | pIC50 | = | 8.3 | 8.3 | -1 | 3 | ChEMBL | 470 | 4 | 2 | 4 | 3.7 | O=C([C@@H]1C=C2c3cccc4c3c(cn4CCO)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CCCC1 | 10.1016/j.bmcl.2011.06.070 | |||
56660102 | 64286 | None | 0 | Human | Functional | pIC50 | = | 8.3 | 8.3 | -1 | 3 | ChEMBL | 537 | 5 | 1 | 4 | 5.2 | O=C([C@@H]1C=C2c3cccc4c3c(cn4CCN3CCCCC3)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CCCC1 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1809041 | 64286 | None | 0 | Human | Functional | pIC50 | = | 8.3 | 8.3 | -1 | 3 | ChEMBL | 537 | 5 | 1 | 4 | 5.2 | O=C([C@@H]1C=C2c3cccc4c3c(cn4CCN3CCCCC3)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CCCC1 | 10.1016/j.bmcl.2011.06.070 | |||
56663562 | 64287 | None | 0 | Human | Functional | pIC50 | = | 8.3 | 8.3 | -1 | 3 | ChEMBL | 552 | 5 | 1 | 5 | 4.0 | CN1CCN(CCn2cc3c4c(cccc42)C2=C[C@@H](C(=O)N4CCCC4)CN(C(=O)Nc4ccccc4)[C@@H]2C3)CC1 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1809042 | 64287 | None | 0 | Human | Functional | pIC50 | = | 8.3 | 8.3 | -1 | 3 | ChEMBL | 552 | 5 | 1 | 5 | 4.0 | CN1CCN(CCn2cc3c4c(cccc42)C2=C[C@@H](C(=O)N4CCCC4)CN(C(=O)Nc4ccccc4)[C@@H]2C3)CC1 | 10.1016/j.bmcl.2011.06.070 | |||
56663563 | 64288 | None | 0 | Mouse | Functional | pIC50 | = | 8.3 | 8.3 | 2 | 3 | ChEMBL | 539 | 5 | 1 | 5 | 4.1 | O=C([C@@H]1C=C2c3cccc4c3c(cn4CCN3CCOCC3)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CCCC1 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1809043 | 64288 | None | 0 | Mouse | Functional | pIC50 | = | 8.3 | 8.3 | 2 | 3 | ChEMBL | 539 | 5 | 1 | 5 | 4.1 | O=C([C@@H]1C=C2c3cccc4c3c(cn4CCN3CCOCC3)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CCCC1 | 10.1016/j.bmcl.2011.06.070 | |||
168289637 | 191585 | None | 0 | Human | Functional | pIC50 | = | 8.3 | 8.3 | - | 1 | ChEMBL | 515 | 6 | 0 | 9 | 3.6 | CCOc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3cc(Cl)cn3)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL5193432 | 191585 | None | 0 | Human | Functional | pIC50 | = | 8.3 | 8.3 | - | 1 | ChEMBL | 515 | 6 | 0 | 9 | 3.6 | CCOc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3cc(Cl)cn3)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
89726199 | 153527 | None | 0 | Human | Functional | pIC50 | = | 8.2 | 8.2 | - | 1 | ChEMBL | 589 | 5 | 1 | 10 | 3.5 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccc(N5CCOCC5)cc4[nH]3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00676 | |||
CHEMBL3979234 | 153527 | None | 0 | Human | Functional | pIC50 | = | 8.2 | 8.2 | - | 1 | ChEMBL | 589 | 5 | 1 | 10 | 3.5 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccc(N5CCOCC5)cc4[nH]3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00676 | |||
89726281 | 148856 | None | 0 | Human | Functional | pIC50 | = | 8.2 | 8.2 | - | 1 | ChEMBL | 571 | 5 | 1 | 11 | 3.2 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccc(-n5cncn5)cc4[nH]3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00676 | |||
CHEMBL3940550 | 148856 | None | 0 | Human | Functional | pIC50 | = | 8.2 | 8.2 | - | 1 | ChEMBL | 571 | 5 | 1 | 11 | 3.2 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccc(-n5cncn5)cc4[nH]3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00676 | |||
71679630 | 146051 | None | 0 | Human | Functional | pIC50 | = | 8.2 | 8.2 | - | 1 | ChEMBL | 458 | 4 | 1 | 8 | 3.2 | C[C@@H]1CN(c2scnc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL3918205 | 146051 | None | 0 | Human | Functional | pIC50 | = | 8.2 | 8.2 | - | 1 | ChEMBL | 458 | 4 | 1 | 8 | 3.2 | C[C@@H]1CN(c2scnc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | 10.1021/acs.jmedchem.2c00675 | |||
89726522 | 149533 | None | 0 | Human | Functional | pIC50 | = | 7.3 | 7.3 | - | 1 | ChEMBL | 515 | 6 | 1 | 9 | 3.2 | C[C@@H]1CN(c2sc(CN(C)C)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL3945976 | 149533 | None | 0 | Human | Functional | pIC50 | = | 7.3 | 7.3 | - | 1 | ChEMBL | 515 | 6 | 1 | 9 | 3.2 | C[C@@H]1CN(c2sc(CN(C)C)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | 10.1021/acs.jmedchem.2c00675 | |||
15605074 | 141323 | None | 0 | Human | Functional | pIC50 | = | 7.3 | 7.3 | - | 1 | ChEMBL | 643 | 10 | 3 | 4 | 6.9 | CCCCNC(=O)N1CCCN(c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2NC(=O)c2cccc(Cl)c2)CC1 | 10.1016/j.bmcl.2005.09.020 | |||
CHEMBL382938 | 141323 | None | 0 | Human | Functional | pIC50 | = | 7.3 | 7.3 | - | 1 | ChEMBL | 643 | 10 | 3 | 4 | 6.9 | CCCCNC(=O)N1CCCN(c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2NC(=O)c2cccc(Cl)c2)CC1 | 10.1016/j.bmcl.2005.09.020 | |||
44570272 | 177690 | None | 0 | Human | Functional | pIC50 | = | 7.3 | 7.3 | 3 | 2 | ChEMBL | 479 | 4 | 1 | 5 | 3.3 | C[C@H]1CN(S(=O)(=O)C[C@]23CC[C@H](CC2O)C3(C)C)CCN1c1ncc(C(F)(F)F)cc1F | 10.1016/j.bmcl.2008.11.008 | |||
CHEMBL464064 | 177690 | None | 0 | Human | Functional | pIC50 | = | 7.3 | 7.3 | 3 | 2 | ChEMBL | 479 | 4 | 1 | 5 | 3.3 | C[C@H]1CN(S(=O)(=O)C[C@]23CC[C@H](CC2O)C3(C)C)CCN1c1ncc(C(F)(F)F)cc1F | 10.1016/j.bmcl.2008.11.008 | |||
46883290 | 5651 | None | 0 | Human | Functional | pIC50 | = | 6.3 | 6.3 | - | 1 | ChEMBL | 587 | 9 | 0 | 7 | 5.9 | CCOc1ccc(-n2c([C@@H](C)N(Cc3cccnc3)C(=O)Cc3ccc(C(F)(F)F)cn3)nc3ccccc3c2=O)cc1 | 10.1016/j.bmcl.2009.07.032 | |||
CHEMBL1077810 | 5651 | None | 0 | Human | Functional | pIC50 | = | 6.3 | 6.3 | - | 1 | ChEMBL | 587 | 9 | 0 | 7 | 5.9 | CCOc1ccc(-n2c([C@@H](C)N(Cc3cccnc3)C(=O)Cc3ccc(C(F)(F)F)cn3)nc3ccccc3c2=O)cc1 | 10.1016/j.bmcl.2009.07.032 | |||
4324393 | 70372 | None | 5 | Human | Functional | pIC50 | = | 6.3 | 6.3 | - | 1 | ChEMBL | 508 | 14 | 0 | 5 | 6.1 | CCCCCCCCCC(=O)N(CCN(C)C)C(C)c1nc2ccccc2c(=O)n1-c1ccc(F)cc1 | 10.1016/j.bmcl.2007.03.106 | |||
CHEMBL194494 | 70372 | None | 5 | Human | Functional | pIC50 | = | 6.3 | 6.3 | - | 1 | ChEMBL | 508 | 14 | 0 | 5 | 6.1 | CCCCCCCCCC(=O)N(CCN(C)C)C(C)c1nc2ccccc2c(=O)n1-c1ccc(F)cc1 | 10.1016/j.bmcl.2007.03.106 | |||
44581089 | 188002 | None | 0 | Human | Functional | pIC50 | = | 6.3 | 6.3 | - | 1 | ChEMBL | 441 | 4 | 1 | 4 | 3.4 | O=C1CCC(c2ccccn2)(C2CCN(Cc3ccc(Br)cc3)CC2)C(=O)N1 | 10.1016/j.bmcl.2008.07.115 | |||
CHEMBL496564 | 188002 | None | 0 | Human | Functional | pIC50 | = | 6.3 | 6.3 | - | 1 | ChEMBL | 441 | 4 | 1 | 4 | 3.4 | O=C1CCC(c2ccccn2)(C2CCN(Cc3ccc(Br)cc3)CC2)C(=O)N1 | 10.1016/j.bmcl.2008.07.115 | |||
44580939 | 193330 | None | 0 | Human | Functional | pIC50 | = | 6.3 | 6.3 | - | 1 | ChEMBL | 426 | 4 | 1 | 2 | 4.5 | O=C1CCC(c2ccccc2)(C2CCN(Cc3ccc(Br)cc3)CC2)CN1 | 10.1016/j.bmcl.2008.07.115 | |||
CHEMBL523568 | 193330 | None | 0 | Human | Functional | pIC50 | = | 6.3 | 6.3 | - | 1 | ChEMBL | 426 | 4 | 1 | 2 | 4.5 | O=C1CCC(c2ccccc2)(C2CCN(Cc3ccc(Br)cc3)CC2)CN1 | 10.1016/j.bmcl.2008.07.115 | |||
44454895 | 95396 | None | 1 | Human | Functional | pIC50 | = | 5.3 | 5.3 | - | 1 | ChEMBL | 313 | 3 | 1 | 4 | 3.3 | Cc1ccc2c(c1)n(C)c(=N)n2CC(=O)c1ccc(Cl)cc1 | 10.1016/j.bmcl.2008.01.074 | |||
CHEMBL256647 | 95396 | None | 1 | Human | Functional | pIC50 | = | 5.3 | 5.3 | - | 1 | ChEMBL | 313 | 3 | 1 | 4 | 3.3 | Cc1ccc2c(c1)n(C)c(=N)n2CC(=O)c1ccc(Cl)cc1 | 10.1016/j.bmcl.2008.01.074 | |||
44570181 | 183176 | None | 0 | Human | Functional | pIC50 | = | 6.3 | 6.3 | - | 1 | ChEMBL | 477 | 4 | 0 | 5 | 3.5 | C[C@@H]1CN(S(=O)(=O)C[C@]23CC[C@H](CC2=O)C3(C)C)CCN1c1ncc(C(F)(F)F)cc1F | 10.1016/j.bmcl.2008.11.008 | |||
CHEMBL479430 | 183176 | None | 0 | Human | Functional | pIC50 | = | 6.3 | 6.3 | - | 1 | ChEMBL | 477 | 4 | 0 | 5 | 3.5 | C[C@@H]1CN(S(=O)(=O)C[C@]23CC[C@H](CC2=O)C3(C)C)CCN1c1ncc(C(F)(F)F)cc1F | 10.1016/j.bmcl.2008.11.008 | |||
44570550 | 190426 | None | 0 | Human | Functional | pIC50 | = | 6.3 | 6.3 | - | 1 | ChEMBL | 459 | 4 | 0 | 5 | 3.3 | C[C@@H]1CN(S(=O)(=O)C[C@]23CC[C@H](CC2=O)C3(C)C)CCN1c1ccc(C(F)(F)F)cn1 | 10.1016/j.bmcl.2008.11.008 | |||
CHEMBL517623 | 190426 | None | 0 | Human | Functional | pIC50 | = | 6.3 | 6.3 | - | 1 | ChEMBL | 459 | 4 | 0 | 5 | 3.3 | C[C@@H]1CN(S(=O)(=O)C[C@]23CC[C@H](CC2=O)C3(C)C)CCN1c1ccc(C(F)(F)F)cn1 | 10.1016/j.bmcl.2008.11.008 | |||
44570180 | 183654 | None | 0 | Mouse | Functional | pIC50 | = | 6.3 | 6.3 | -6 | 2 | ChEMBL | 477 | 4 | 0 | 5 | 3.5 | C[C@H]1CN(S(=O)(=O)C[C@]23CC[C@H](CC2=O)C3(C)C)CCN1c1ncc(C(F)(F)F)cc1F | 10.1016/j.bmcl.2008.11.008 | |||
CHEMBL480016 | 183654 | None | 0 | Mouse | Functional | pIC50 | = | 6.3 | 6.3 | -6 | 2 | ChEMBL | 477 | 4 | 0 | 5 | 3.5 | C[C@H]1CN(S(=O)(=O)C[C@]23CC[C@H](CC2=O)C3(C)C)CCN1c1ncc(C(F)(F)F)cc1F | 10.1016/j.bmcl.2008.11.008 | |||
44581137 | 188028 | None | 0 | Human | Functional | pIC50 | = | 5.3 | 5.3 | - | 1 | ChEMBL | 484 | 5 | 2 | 4 | 3.7 | O=C1CCC(c2ccc(C(=O)O)cc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C(=O)N1 | 10.1016/j.bmcl.2008.07.115 | |||
CHEMBL496780 | 188028 | None | 0 | Human | Functional | pIC50 | = | 5.3 | 5.3 | - | 1 | ChEMBL | 484 | 5 | 2 | 4 | 3.7 | O=C1CCC(c2ccc(C(=O)O)cc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C(=O)N1 | 10.1016/j.bmcl.2008.07.115 | |||
44580859 | 188109 | None | 0 | Human | Functional | pIC50 | = | 5.3 | 5.3 | - | 1 | ChEMBL | 482 | 5 | 0 | 3 | 5.2 | CC(C)N1C(=O)CCC(c2ccccc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C1=O | 10.1016/j.bmcl.2008.07.115 | |||
CHEMBL497395 | 188109 | None | 0 | Human | Functional | pIC50 | = | 5.3 | 5.3 | - | 1 | ChEMBL | 482 | 5 | 0 | 3 | 5.2 | CC(C)N1C(=O)CCC(c2ccccc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C1=O | 10.1016/j.bmcl.2008.07.115 | |||
44580858 | 193425 | None | 0 | Human | Functional | pIC50 | = | 5.3 | 5.3 | - | 1 | ChEMBL | 482 | 6 | 0 | 3 | 5.2 | CCCN1C(=O)CCC(c2ccccc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C1=O | 10.1016/j.bmcl.2008.07.115 | |||
CHEMBL524265 | 193425 | None | 0 | Human | Functional | pIC50 | = | 5.3 | 5.3 | - | 1 | ChEMBL | 482 | 6 | 0 | 3 | 5.2 | CCCN1C(=O)CCC(c2ccccc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C1=O | 10.1016/j.bmcl.2008.07.115 | |||
44570473 | 191198 | None | 0 | Human | Functional | pIC50 | = | 5.3 | 5.3 | - | 1 | ChEMBL | 446 | 4 | 0 | 6 | 2.3 | CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCN(c3ccc(C(F)(F)F)nn3)CC1)C(=O)C2 | 10.1016/j.bmcl.2008.11.008 | |||
CHEMBL518767 | 191198 | None | 0 | Human | Functional | pIC50 | = | 5.3 | 5.3 | - | 1 | ChEMBL | 446 | 4 | 0 | 6 | 2.3 | CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCN(c3ccc(C(F)(F)F)nn3)CC1)C(=O)C2 | 10.1016/j.bmcl.2008.11.008 | |||
117739351 | 148559 | None | 0 | Human | Functional | pIC50 | = | 6.3 | 6.3 | - | 1 | ChEMBL | 536 | 4 | 1 | 6 | 5.5 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cc1cccc2cccnc12 | 10.1021/acs.jmedchem.2c00676 | |||
CHEMBL3938074 | 148559 | None | 0 | Human | Functional | pIC50 | = | 6.3 | 6.3 | - | 1 | ChEMBL | 536 | 4 | 1 | 6 | 5.5 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cc1cccc2cccnc12 | 10.1021/acs.jmedchem.2c00676 | |||
90480413 | 192543 | None | 0 | Human | Functional | pIC50 | = | 6.3 | 6.3 | - | 1 | ChEMBL | 509 | 6 | 0 | 9 | 3.6 | CCOc1ccc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3nc(C)nc3C)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL5208280 | 192543 | None | 0 | Human | Functional | pIC50 | = | 6.3 | 6.3 | - | 1 | ChEMBL | 509 | 6 | 0 | 9 | 3.6 | CCOc1ccc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3nc(C)nc3C)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
45482843 | 200576 | None | 0 | Human | Functional | pIC50 | = | 6.3 | 6.3 | - | 1 | ChEMBL | 518 | 6 | 1 | 3 | 6.0 | CCN(CC)C(=O)[C@@H]1C=C2c3cccc4c3c(cn4Cc3ccccc3)C[C@H]2N(C(=O)Nc2ccccc2)C1 | 10.1016/j.bmcl.2009.09.002 | |||
CHEMBL574596 | 200576 | None | 0 | Human | Functional | pIC50 | = | 6.3 | 6.3 | - | 1 | ChEMBL | 518 | 6 | 1 | 3 | 6.0 | CCN(CC)C(=O)[C@@H]1C=C2c3cccc4c3c(cn4Cc3ccccc3)C[C@H]2N(C(=O)Nc2ccccc2)C1 | 10.1016/j.bmcl.2009.09.002 | |||
44253726 | 7347 | None | 0 | Human | Functional | pIC50 | = | 6.3 | 6.3 | - | 1 | ChEMBL | 486 | 9 | 1 | 3 | 5.0 | O=C(NCC1CC1)c1ccc(CN(Cc2ccccc2F)S(=O)(=O)c2ccc(Cl)cc2)cc1 | 10.1016/j.bmcl.2010.04.113 | |||
CHEMBL1086242 | 7347 | None | 0 | Human | Functional | pIC50 | = | 6.3 | 6.3 | - | 1 | ChEMBL | 486 | 9 | 1 | 3 | 5.0 | O=C(NCC1CC1)c1ccc(CN(Cc2ccccc2F)S(=O)(=O)c2ccc(Cl)cc2)cc1 | 10.1016/j.bmcl.2010.04.113 | |||
15605075 | 72756 | None | 0 | Human | Functional | pIC50 | = | 6.3 | 6.3 | - | 1 | ChEMBL | 547 | 8 | 3 | 4 | 4.8 | CCNC(=O)N1CCCN(c2ccc(C(=O)NCCc3ccccc3)cc2NC(=O)c2cccc(Cl)c2)CC1 | 10.1016/j.bmcl.2005.09.020 | |||
CHEMBL199847 | 72756 | None | 0 | Human | Functional | pIC50 | = | 6.3 | 6.3 | - | 1 | ChEMBL | 547 | 8 | 3 | 4 | 4.8 | CCNC(=O)N1CCCN(c2ccc(C(=O)NCCc3ccccc3)cc2NC(=O)c2cccc(Cl)c2)CC1 | 10.1016/j.bmcl.2005.09.020 | |||
46891328 | 6831 | None | 0 | Human | Functional | pIC50 | = | 6.3 | 6.3 | - | 1 | ChEMBL | 451 | 7 | 1 | 3 | 4.7 | O=C(O)c1ccc(CN(Cc2ccccc2F)S(=O)(=O)c2ccc(Cl)cc2)cc1F | 10.1016/j.bmcl.2010.04.113 | |||
CHEMBL1083955 | 6831 | None | 0 | Human | Functional | pIC50 | = | 6.3 | 6.3 | - | 1 | ChEMBL | 451 | 7 | 1 | 3 | 4.7 | O=C(O)c1ccc(CN(Cc2ccccc2F)S(=O)(=O)c2ccc(Cl)cc2)cc1F | 10.1016/j.bmcl.2010.04.113 | |||
53317275 | 58219 | None | 0 | Human | Functional | pIC50 | = | 6.3 | 6.3 | - | 1 | ChEMBL | 460 | 5 | 0 | 5 | 4.8 | CC(=O)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4)CC3)[C@@H](C)C2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
CHEMBL1681862 | 58219 | None | 0 | Human | Functional | pIC50 | = | 6.3 | 6.3 | - | 1 | ChEMBL | 460 | 5 | 0 | 5 | 4.8 | CC(=O)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4)CC3)[C@@H](C)C2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
44447095 | 154967 | None | 0 | Human | Functional | pIC50 | = | 6.3 | 6.3 | - | 1 | ChEMBL | 586 | 9 | 0 | 6 | 5.6 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc2ccccc2n1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2007.11.060 | |||
CHEMBL400719 | 154967 | None | 0 | Human | Functional | pIC50 | = | 6.3 | 6.3 | - | 1 | ChEMBL | 586 | 9 | 0 | 6 | 5.6 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc2ccccc2n1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2007.11.060 | |||
90479958 | 192439 | None | 0 | Human | Functional | pIC50 | = | 6.3 | 6.3 | - | 1 | ChEMBL | 535 | 5 | 0 | 10 | 3.2 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3cnc(N4CCCC4)nc3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL5206539 | 192439 | None | 0 | Human | Functional | pIC50 | = | 6.3 | 6.3 | - | 1 | ChEMBL | 535 | 5 | 0 | 10 | 3.2 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3cnc(N4CCCC4)nc3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00675 | |||
56663561 | 64282 | None | 0 | Human | Functional | pIC50 | = | 7.3 | 7.3 | -1 | 2 | ChEMBL | 526 | 5 | 1 | 5 | 4.7 | CC(C)OC(=O)Cn1cc2c3c(cccc31)C1=C[C@@H](C(=O)N3CCCC3)CN(C(=O)Nc3ccccc3)[C@@H]1C2 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1809037 | 64282 | None | 0 | Human | Functional | pIC50 | = | 7.3 | 7.3 | -1 | 2 | ChEMBL | 526 | 5 | 1 | 5 | 4.7 | CC(C)OC(=O)Cn1cc2c3c(cccc31)C1=C[C@@H](C(=O)N3CCCC3)CN(C(=O)Nc3ccccc3)[C@@H]1C2 | 10.1016/j.bmcl.2011.06.070 | |||
56663561 | 64282 | None | 0 | Mouse | Functional | pIC50 | = | 7.3 | 7.3 | 1 | 2 | ChEMBL | 526 | 5 | 1 | 5 | 4.7 | CC(C)OC(=O)Cn1cc2c3c(cccc31)C1=C[C@@H](C(=O)N3CCCC3)CN(C(=O)Nc3ccccc3)[C@@H]1C2 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1809037 | 64282 | None | 0 | Mouse | Functional | pIC50 | = | 7.3 | 7.3 | 1 | 2 | ChEMBL | 526 | 5 | 1 | 5 | 4.7 | CC(C)OC(=O)Cn1cc2c3c(cccc31)C1=C[C@@H](C(=O)N3CCCC3)CN(C(=O)Nc3ccccc3)[C@@H]1C2 | 10.1016/j.bmcl.2011.06.070 | |||
89726367 | 147175 | None | 0 | Human | Functional | pIC50 | = | 7.3 | 7.3 | - | 1 | ChEMBL | 514 | 5 | 1 | 9 | 3.3 | C[C@@H]1CN(c2sc(C3COC3)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL3927250 | 147175 | None | 0 | Human | Functional | pIC50 | = | 7.3 | 7.3 | - | 1 | ChEMBL | 514 | 5 | 1 | 9 | 3.3 | C[C@@H]1CN(c2sc(C3COC3)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | 10.1021/acs.jmedchem.2c00675 | |||
56663558 | 64259 | None | 0 | Mouse | Functional | pIC50 | = | 6.3 | 6.3 | -3 | 2 | ChEMBL | 490 | 2 | 2 | 4 | 2.9 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CCS(=O)(=O)CC1 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1809010 | 64259 | None | 0 | Mouse | Functional | pIC50 | = | 6.3 | 6.3 | -3 | 2 | ChEMBL | 490 | 2 | 2 | 4 | 2.9 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CCS(=O)(=O)CC1 | 10.1016/j.bmcl.2011.06.070 | |||
6143230 | 7191 | None | 0 | Human | Functional | pIC50 | = | 6.3 | 6.3 | - | 1 | ChEMBL | 588 | 10 | 2 | 5 | 5.8 | CC(=O)Nc1cccc(/C(C)=N\NC(=O)c2ccc(CN(Cc3ccccc3)S(=O)(=O)c3ccc(Cl)cc3)cc2)c1 | 10.1016/j.bmcl.2010.04.113 | |||
CHEMBL1085565 | 7191 | None | 0 | Human | Functional | pIC50 | = | 6.3 | 6.3 | - | 1 | ChEMBL | 588 | 10 | 2 | 5 | 5.8 | CC(=O)Nc1cccc(/C(C)=N\NC(=O)c2ccc(CN(Cc3ccccc3)S(=O)(=O)c3ccc(Cl)cc3)cc2)c1 | 10.1016/j.bmcl.2010.04.113 | |||
46891425 | 6879 | None | 0 | Human | Functional | pIC50 | = | 6.3 | 6.3 | - | 1 | ChEMBL | 450 | 9 | 1 | 7 | 3.1 | CCOc1ccc(S(=O)(=O)N(Cc2ccc(-c3nnn[nH]3)cc2)Cc2ccccn2)cc1 | 10.1016/j.bmcl.2010.04.113 | |||
CHEMBL1084198 | 6879 | None | 0 | Human | Functional | pIC50 | = | 6.3 | 6.3 | - | 1 | ChEMBL | 450 | 9 | 1 | 7 | 3.1 | CCOc1ccc(S(=O)(=O)N(Cc2ccc(-c3nnn[nH]3)cc2)Cc2ccccn2)cc1 | 10.1016/j.bmcl.2010.04.113 | |||
56680572 | 64271 | None | 0 | Human | Functional | pIC50 | = | 5.3 | 5.3 | - | 1 | ChEMBL | 483 | 4 | 2 | 3 | 4.3 | CN(C)Cc1ccc(NC(=O)N2C[C@H](C(=O)N3CCCC3)C=C3c4cccc5[nH]cc(c45)C[C@H]32)cc1 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1809023 | 64271 | None | 0 | Human | Functional | pIC50 | = | 5.3 | 5.3 | - | 1 | ChEMBL | 483 | 4 | 2 | 3 | 4.3 | CN(C)Cc1ccc(NC(=O)N2C[C@H](C(=O)N3CCCC3)C=C3c4cccc5[nH]cc(c45)C[C@H]32)cc1 | 10.1016/j.bmcl.2011.06.070 | |||
44137674 | 69993 | None | 0 | Human | Functional | pIC50 | = | 7.3 | 7.3 | - | 1 | ChEMBL | 650 | 7 | 0 | 7 | 5.5 | C[C@H](c1nc2ncccc2c(=O)n1-c1ccc(Cl)cc1)N(CC1CCS(=O)(=O)CC1)C(=O)Cc1ccc(C(F)(F)F)c(F)c1 | 10.1016/j.bmcl.2011.10.120 | |||
CHEMBL1939560 | 69993 | None | 0 | Human | Functional | pIC50 | = | 7.3 | 7.3 | - | 1 | ChEMBL | 650 | 7 | 0 | 7 | 5.5 | C[C@H](c1nc2ncccc2c(=O)n1-c1ccc(Cl)cc1)N(CC1CCS(=O)(=O)CC1)C(=O)Cc1ccc(C(F)(F)F)c(F)c1 | 10.1016/j.bmcl.2011.10.120 | |||
168285354 | 191596 | None | 0 | Human | Functional | pIC50 | = | 7.3 | 7.3 | - | 1 | ChEMBL | 532 | 6 | 0 | 10 | 3.5 | CCOc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3ncc4cccnc43)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL5193608 | 191596 | None | 0 | Human | Functional | pIC50 | = | 7.3 | 7.3 | - | 1 | ChEMBL | 532 | 6 | 0 | 10 | 3.5 | CCOc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3ncc4cccnc43)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
168293706 | 192273 | None | 0 | Human | Functional | pIC50 | = | 5.3 | 5.3 | - | 1 | ChEMBL | 519 | 5 | 2 | 8 | 3.3 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1ccc(C(=O)O)n1 | 10.1021/acs.jmedchem.2c00676 | |||
CHEMBL5203982 | 192273 | None | 0 | Human | Functional | pIC50 | = | 5.3 | 5.3 | - | 1 | ChEMBL | 519 | 5 | 2 | 8 | 3.3 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1ccc(C(=O)O)n1 | 10.1021/acs.jmedchem.2c00676 | |||
90479922 | 190733 | None | 0 | Human | Functional | pIC50 | = | 6.3 | 6.3 | - | 1 | ChEMBL | 496 | 5 | 0 | 10 | 2.6 | COc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3nc(C)nc3C)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL5181086 | 190733 | None | 0 | Human | Functional | pIC50 | = | 6.3 | 6.3 | - | 1 | ChEMBL | 496 | 5 | 0 | 10 | 2.6 | COc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3nc(C)nc3C)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
44253594 | 6949 | None | 0 | Human | Functional | pIC50 | = | 5.3 | 5.3 | - | 1 | ChEMBL | 518 | 10 | 1 | 4 | 5.1 | O=C(NCC1CC1)c1ccc(CN(Cc2ccccc2)S(=O)(=O)c2ccc(OC(F)(F)F)cc2)cc1 | 10.1016/j.bmcl.2010.04.113 | |||
CHEMBL1084505 | 6949 | None | 0 | Human | Functional | pIC50 | = | 5.3 | 5.3 | - | 1 | ChEMBL | 518 | 10 | 1 | 4 | 5.1 | O=C(NCC1CC1)c1ccc(CN(Cc2ccccc2)S(=O)(=O)c2ccc(OC(F)(F)F)cc2)cc1 | 10.1016/j.bmcl.2010.04.113 | |||
45484656 | 199288 | None | 0 | Human | Functional | pIC50 | = | 6.3 | 6.3 | - | 1 | ChEMBL | 461 | 5 | 1 | 5 | 3.5 | CNC(=O)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4)CC3)CC2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
CHEMBL565761 | 199288 | None | 0 | Human | Functional | pIC50 | = | 6.3 | 6.3 | - | 1 | ChEMBL | 461 | 5 | 1 | 5 | 3.5 | CNC(=O)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4)CC3)CC2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
45482808 | 201022 | None | 0 | Human | Functional | pIC50 | = | 6.3 | 6.3 | - | 1 | ChEMBL | 518 | 7 | 2 | 5 | 4.5 | CCN(CC)C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2cc(OC)c(OC)c(OC)c2)C1 | 10.1016/j.bmcl.2009.09.002 | |||
CHEMBL578231 | 201022 | None | 0 | Human | Functional | pIC50 | = | 6.3 | 6.3 | - | 1 | ChEMBL | 518 | 7 | 2 | 5 | 4.5 | CCN(CC)C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2cc(OC)c(OC)c(OC)c2)C1 | 10.1016/j.bmcl.2009.09.002 | |||
45486521 | 200982 | None | 0 | Human | Functional | pIC50 | = | 7.2 | 7.2 | - | 1 | ChEMBL | 621 | 9 | 0 | 7 | 5.6 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(C(F)(F)F)c(F)c1)C(C)c1nc2c(Cl)nccn2c1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2009.07.021 | |||
CHEMBL577972 | 200982 | None | 0 | Human | Functional | pIC50 | = | 7.2 | 7.2 | - | 1 | ChEMBL | 621 | 9 | 0 | 7 | 5.6 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(C(F)(F)F)c(F)c1)C(C)c1nc2c(Cl)nccn2c1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2009.07.021 | |||
90479919 | 191483 | None | 0 | Human | Functional | pIC50 | = | 6.2 | 6.2 | - | 1 | ChEMBL | 480 | 4 | 0 | 9 | 2.9 | Cc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3nc(C)nc3C)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL5192208 | 191483 | None | 0 | Human | Functional | pIC50 | = | 6.2 | 6.2 | - | 1 | ChEMBL | 480 | 4 | 0 | 9 | 2.9 | Cc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3nc(C)nc3C)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
9938965 | 5673 | None | 2 | Human | Functional | pIC50 | = | 7.2 | 7.2 | - | 1 | ChEMBL | 619 | 10 | 0 | 8 | 5.0 | CCOc1ccc(-n2c([C@@H](C)N(Cc3ccc[n+]([O-])c3)C(=O)Cc3ccc(OC(F)(F)F)cc3)nc3ncccc3c2=O)cc1 | 10.1016/j.bmcl.2009.07.032 | |||
CHEMBL1077832 | 5673 | None | 2 | Human | Functional | pIC50 | = | 7.2 | 7.2 | - | 1 | ChEMBL | 619 | 10 | 0 | 8 | 5.0 | CCOc1ccc(-n2c([C@@H](C)N(Cc3ccc[n+]([O-])c3)C(=O)Cc3ccc(OC(F)(F)F)cc3)nc3ncccc3c2=O)cc1 | 10.1016/j.bmcl.2009.07.032 | |||
53318513 | 58202 | None | 0 | Human | Functional | pIC50 | = | 7.2 | 7.2 | - | 1 | ChEMBL | 493 | 5 | 1 | 5 | 4.1 | CNC(=O)c1cnc(N2CCN(C3CCN(Cc4ccc(F)cc4Cl)CC3)[C@@H](C)C2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
CHEMBL1681843 | 58202 | None | 0 | Human | Functional | pIC50 | = | 7.2 | 7.2 | - | 1 | ChEMBL | 493 | 5 | 1 | 5 | 4.1 | CNC(=O)c1cnc(N2CCN(C3CCN(Cc4ccc(F)cc4Cl)CC3)[C@@H](C)C2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
89726335 | 153857 | None | 0 | Human | Functional | pIC50 | = | 6.2 | 6.2 | - | 1 | ChEMBL | 575 | 6 | 2 | 10 | 3.0 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccc(OC5CNC5)cc4[nH]3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00676 | |||
CHEMBL3982035 | 153857 | None | 0 | Human | Functional | pIC50 | = | 6.2 | 6.2 | - | 1 | ChEMBL | 575 | 6 | 2 | 10 | 3.0 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccc(OC5CNC5)cc4[nH]3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00676 | |||
46883303 | 5664 | None | 0 | Human | Functional | pIC50 | = | 7.2 | 7.2 | - | 1 | ChEMBL | 609 | 9 | 0 | 8 | 6.0 | CCOc1ccc(-n2c([C@@H](C)N(Cc3cc(C)no3)C(=O)Cc3ccc(F)c(C(F)(F)F)c3)nc3ncccc3c2=O)cc1 | 10.1016/j.bmcl.2009.07.032 | |||
CHEMBL1077823 | 5664 | None | 0 | Human | Functional | pIC50 | = | 7.2 | 7.2 | - | 1 | ChEMBL | 609 | 9 | 0 | 8 | 6.0 | CCOc1ccc(-n2c([C@@H](C)N(Cc3cc(C)no3)C(=O)Cc3ccc(F)c(C(F)(F)F)c3)nc3ncccc3c2=O)cc1 | 10.1016/j.bmcl.2009.07.032 | |||
15605007 | 72991 | None | 0 | Human | Functional | pIC50 | = | 6.2 | 6.2 | - | 1 | ChEMBL | 599 | 8 | 3 | 4 | 5.6 | CCNC(=O)N1CCCN(c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2NC(=O)c2ccccc2F)CC1 | 10.1016/j.bmcl.2005.09.020 | |||
CHEMBL200665 | 72991 | None | 0 | Human | Functional | pIC50 | = | 6.2 | 6.2 | - | 1 | ChEMBL | 599 | 8 | 3 | 4 | 5.6 | CCNC(=O)N1CCCN(c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2NC(=O)c2ccccc2F)CC1 | 10.1016/j.bmcl.2005.09.020 | |||
71680139 | 147784 | None | 0 | Human | Functional | pIC50 | = | 6.2 | 6.2 | - | 1 | ChEMBL | 500 | 5 | 1 | 8 | 4.3 | CC(C)c1nc(-c2nc3ccccc3[nH]2)c(N2CCN(C(=O)Cn3cnc4cccnc43)[C@H](C)C2)s1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL3931920 | 147784 | None | 0 | Human | Functional | pIC50 | = | 6.2 | 6.2 | - | 1 | ChEMBL | 500 | 5 | 1 | 8 | 4.3 | CC(C)c1nc(-c2nc3ccccc3[nH]2)c(N2CCN(C(=O)Cn3cnc4cccnc43)[C@H](C)C2)s1 | 10.1021/acs.jmedchem.2c00675 | |||
53318560 | 58206 | None | 0 | Human | Functional | pIC50 | = | 8.2 | 8.2 | -1 | 3 | ChEMBL | 587 | 7 | 1 | 5 | 5.8 | C[C@H]1CN(c2ncc(C(=O)NCc3ccc(F)c(F)c3)cc2Cl)CCN1C1CCN(Cc2ccc(Cl)cc2)CC1 | 10.1016/j.bmcl.2010.12.114 | |||
CHEMBL1681849 | 58206 | None | 0 | Human | Functional | pIC50 | = | 8.2 | 8.2 | -1 | 3 | ChEMBL | 587 | 7 | 1 | 5 | 5.8 | C[C@H]1CN(c2ncc(C(=O)NCc3ccc(F)c(F)c3)cc2Cl)CCN1C1CCN(Cc2ccc(Cl)cc2)CC1 | 10.1016/j.bmcl.2010.12.114 | |||
89726090 | 144174 | None | 0 | Human | Functional | pIC50 | = | 8.2 | 8.2 | - | 1 | ChEMBL | 572 | 4 | 1 | 8 | 4.7 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4c(C(F)(F)F)cccc4[nH]3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00676 | |||
CHEMBL3903412 | 144174 | None | 0 | Human | Functional | pIC50 | = | 8.2 | 8.2 | - | 1 | ChEMBL | 572 | 4 | 1 | 8 | 4.7 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4c(C(F)(F)F)cccc4[nH]3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00676 | |||
56673937 | 64249 | None | 0 | Mouse | Functional | pIC50 | = | 8.2 | 8.2 | 2 | 3 | ChEMBL | 440 | 2 | 2 | 2 | 4.7 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CCCCC1 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1809000 | 64249 | None | 0 | Mouse | Functional | pIC50 | = | 8.2 | 8.2 | 2 | 3 | ChEMBL | 440 | 2 | 2 | 2 | 4.7 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CCCCC1 | 10.1016/j.bmcl.2011.06.070 | |||
117740323 | 152487 | None | 0 | Human | Functional | pIC50 | = | 8.2 | 8.2 | - | 1 | ChEMBL | 500 | 4 | 1 | 6 | 4.7 | Cc1ccc(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccccc4[nH]3)C[C@H]2C)cn1 | 10.1021/acs.jmedchem.2c00676 | |||
CHEMBL3970456 | 152487 | None | 0 | Human | Functional | pIC50 | = | 8.2 | 8.2 | - | 1 | ChEMBL | 500 | 4 | 1 | 6 | 4.7 | Cc1ccc(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccccc4[nH]3)C[C@H]2C)cn1 | 10.1021/acs.jmedchem.2c00676 | |||
53318560 | 58206 | None | 0 | Mouse | Functional | pIC50 | = | 8.2 | 8.2 | 1 | 3 | ChEMBL | 587 | 7 | 1 | 5 | 5.8 | C[C@H]1CN(c2ncc(C(=O)NCc3ccc(F)c(F)c3)cc2Cl)CCN1C1CCN(Cc2ccc(Cl)cc2)CC1 | 10.1016/j.bmcl.2010.12.114 | |||
CHEMBL1681849 | 58206 | None | 0 | Mouse | Functional | pIC50 | = | 8.2 | 8.2 | 1 | 3 | ChEMBL | 587 | 7 | 1 | 5 | 5.8 | C[C@H]1CN(c2ncc(C(=O)NCc3ccc(F)c(F)c3)cc2Cl)CCN1C1CCN(Cc2ccc(Cl)cc2)CC1 | 10.1016/j.bmcl.2010.12.114 | |||
168296640 | 192583 | None | 0 | Human | Functional | pIC50 | = | 8.2 | 8.2 | - | 1 | ChEMBL | 575 | 8 | 0 | 11 | 3.0 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2cnc(OCCN(C)C)nc2)CCN1C(=O)Cn1cnc2cccnc21 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL5208823 | 192583 | None | 0 | Human | Functional | pIC50 | = | 8.2 | 8.2 | - | 1 | ChEMBL | 575 | 8 | 0 | 11 | 3.0 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2cnc(OCCN(C)C)nc2)CCN1C(=O)Cn1cnc2cccnc21 | 10.1021/acs.jmedchem.2c00675 | |||
168272582 | 190470 | None | 0 | Human | Functional | pIC50 | = | 8.2 | 8.2 | - | 1 | ChEMBL | 481 | 6 | 0 | 9 | 3.0 | CCOc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3cccn3)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL5177069 | 190470 | None | 0 | Human | Functional | pIC50 | = | 8.2 | 8.2 | - | 1 | ChEMBL | 481 | 6 | 0 | 9 | 3.0 | CCOc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3cccn3)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
57402421 | 69988 | None | 0 | Human | Functional | pIC50 | = | 7.2 | 7.2 | - | 1 | ChEMBL | 638 | 8 | 0 | 8 | 5.1 | C[C@H](c1nc2ccccn2c(=O)c1-c1ccc(C#N)cc1)N(CC1CCS(=O)(=O)CC1)C(=O)Cc1ccc(OC(F)(F)F)cc1 | 10.1016/j.bmcl.2011.10.120 | |||
CHEMBL1939555 | 69988 | None | 0 | Human | Functional | pIC50 | = | 7.2 | 7.2 | - | 1 | ChEMBL | 638 | 8 | 0 | 8 | 5.1 | C[C@H](c1nc2ccccn2c(=O)c1-c1ccc(C#N)cc1)N(CC1CCS(=O)(=O)CC1)C(=O)Cc1ccc(OC(F)(F)F)cc1 | 10.1016/j.bmcl.2011.10.120 | |||
44593651 | 187843 | None | 0 | Human | Functional | pIC50 | = | 7.2 | 7.2 | - | 1 | ChEMBL | 476 | 4 | 1 | 3 | 4.3 | O=C1CCC(c2ccc(F)cc2F)(C2CCN(Cc3ccc(Br)cc3)CC2)C(=O)N1 | 10.1016/j.bmcl.2008.07.115 | |||
CHEMBL495531 | 187843 | None | 0 | Human | Functional | pIC50 | = | 7.2 | 7.2 | - | 1 | ChEMBL | 476 | 4 | 1 | 3 | 4.3 | O=C1CCC(c2ccc(F)cc2F)(C2CCN(Cc3ccc(Br)cc3)CC2)C(=O)N1 | 10.1016/j.bmcl.2008.07.115 | |||
24739886 | 187975 | None | 0 | Human | Functional | pIC50 | = | 7.2 | 7.2 | 12 | 4 | ChEMBL | 469 | 6 | 1 | 3 | 4.2 | NC(=O)CN1CCCC(c2ccccc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C1 | 10.1016/j.bmcl.2008.07.115 | |||
CHEMBL496376 | 187975 | None | 0 | Human | Functional | pIC50 | = | 7.2 | 7.2 | 12 | 4 | ChEMBL | 469 | 6 | 1 | 3 | 4.2 | NC(=O)CN1CCCC(c2ccccc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C1 | 10.1016/j.bmcl.2008.07.115 | |||
24739554 | 188169 | None | 0 | Human | Functional | pIC50 | = | 7.2 | 7.2 | 64 | 2 | ChEMBL | 531 | 5 | 1 | 2 | 6.9 | O=C(Nc1ccccc1)N1CCCC(c2ccccc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C1 | 10.1016/j.bmcl.2008.07.115 | |||
CHEMBL497799 | 188169 | None | 0 | Human | Functional | pIC50 | = | 7.2 | 7.2 | 64 | 2 | ChEMBL | 531 | 5 | 1 | 2 | 6.9 | O=C(Nc1ccccc1)N1CCCC(c2ccccc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C1 | 10.1016/j.bmcl.2008.07.115 | |||
45482836 | 200419 | None | 0 | Human | Functional | pIC50 | = | 7.2 | 7.2 | - | 1 | ChEMBL | 442 | 4 | 1 | 3 | 4.5 | CCN(CC)C(=O)[C@@H]1C=C2c3cccc4c3c(cn4C)C[C@H]2N(C(=O)Nc2ccccc2)C1 | 10.1016/j.bmcl.2009.09.002 | |||
CHEMBL573468 | 200419 | None | 0 | Human | Functional | pIC50 | = | 7.2 | 7.2 | - | 1 | ChEMBL | 442 | 4 | 1 | 3 | 4.5 | CCN(CC)C(=O)[C@@H]1C=C2c3cccc4c3c(cn4C)C[C@H]2N(C(=O)Nc2ccccc2)C1 | 10.1016/j.bmcl.2009.09.002 | |||
56670450 | 64267 | None | 0 | Human | Functional | pIC50 | = | 7.2 | 7.2 | - | 1 | ChEMBL | 456 | 3 | 2 | 3 | 4.3 | COc1ccccc1NC(=O)N1C[C@H](C(=O)N2CCCC2)C=C2c3cccc4[nH]cc(c34)C[C@H]21 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1809018 | 64267 | None | 0 | Human | Functional | pIC50 | = | 7.2 | 7.2 | - | 1 | ChEMBL | 456 | 3 | 2 | 3 | 4.3 | COc1ccccc1NC(=O)N1C[C@H](C(=O)N2CCCC2)C=C2c3cccc4[nH]cc(c34)C[C@H]21 | 10.1016/j.bmcl.2011.06.070 | |||
15604935 | 72615 | None | 0 | Human | Functional | pIC50 | = | 7.2 | 7.2 | - | 1 | ChEMBL | 629 | 9 | 3 | 4 | 6.5 | CCCNC(=O)N1CCCN(c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2NC(=O)c2cccc(Cl)c2)CC1 | 10.1016/j.bmcl.2005.09.020 | |||
CHEMBL199301 | 72615 | None | 0 | Human | Functional | pIC50 | = | 7.2 | 7.2 | - | 1 | ChEMBL | 629 | 9 | 3 | 4 | 6.5 | CCCNC(=O)N1CCCN(c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2NC(=O)c2cccc(Cl)c2)CC1 | 10.1016/j.bmcl.2005.09.020 | |||
15604604 | 72640 | None | 0 | Human | Functional | pIC50 | = | 7.2 | 7.2 | - | 1 | ChEMBL | 629 | 8 | 3 | 4 | 6.5 | CC(C)NC(=O)N1CCCN(c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2NC(=O)c2cccc(Cl)c2)CC1 | 10.1016/j.bmcl.2005.09.020 | |||
CHEMBL199406 | 72640 | None | 0 | Human | Functional | pIC50 | = | 7.2 | 7.2 | - | 1 | ChEMBL | 629 | 8 | 3 | 4 | 6.5 | CC(C)NC(=O)N1CCCN(c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2NC(=O)c2cccc(Cl)c2)CC1 | 10.1016/j.bmcl.2005.09.020 | |||
11296495 | 72755 | None | 22 | Human | Functional | pIC50 | = | 7.2 | 7.2 | - | 1 | ChEMBL | 615 | 8 | 3 | 4 | 6.1 | CCNC(=O)N1CCCN(c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2NC(=O)c2cccc(Cl)c2)CC1 | 10.1016/j.bmcl.2005.09.020 | |||
CHEMBL199839 | 72755 | None | 22 | Human | Functional | pIC50 | = | 7.2 | 7.2 | - | 1 | ChEMBL | 615 | 8 | 3 | 4 | 6.1 | CCNC(=O)N1CCCN(c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2NC(=O)c2cccc(Cl)c2)CC1 | 10.1016/j.bmcl.2005.09.020 | |||
15604856 | 133660 | None | 0 | Human | Functional | pIC50 | = | 7.2 | 7.2 | - | 1 | ChEMBL | 599 | 8 | 3 | 4 | 5.6 | CCNC(=O)N1CCCN(c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2NC(=O)c2cccc(F)c2)CC1 | 10.1016/j.bmcl.2005.09.020 | |||
CHEMBL371240 | 133660 | None | 0 | Human | Functional | pIC50 | = | 7.2 | 7.2 | - | 1 | ChEMBL | 599 | 8 | 3 | 4 | 5.6 | CCNC(=O)N1CCCN(c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2NC(=O)c2cccc(F)c2)CC1 | 10.1016/j.bmcl.2005.09.020 | |||
71680140 | 145940 | None | 0 | Human | Functional | pIC50 | = | 6.2 | 6.2 | - | 1 | ChEMBL | 472 | 5 | 1 | 8 | 3.6 | CC[C@@H]1CN(c2scnc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL3917322 | 145940 | None | 0 | Human | Functional | pIC50 | = | 6.2 | 6.2 | - | 1 | ChEMBL | 472 | 5 | 1 | 8 | 3.6 | CC[C@@H]1CN(c2scnc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | 10.1021/acs.jmedchem.2c00675 | |||
90480049 | 192137 | None | 0 | Human | Functional | pIC50 | = | 6.2 | 6.2 | - | 1 | ChEMBL | 533 | 4 | 0 | 8 | 4.2 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3ccc(C(F)(F)F)nc3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL5201967 | 192137 | None | 0 | Human | Functional | pIC50 | = | 6.2 | 6.2 | - | 1 | ChEMBL | 533 | 4 | 0 | 8 | 4.2 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3ccc(C(F)(F)F)nc3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00675 | |||
14479864 | 4653 | None | 0 | Human | Functional | pIC50 | = | 6.2 | 6.2 | 13 | 2 | ChEMBL | 440 | 4 | 1 | 3 | 4.0 | O=C1CCC(c2ccccc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C(=O)N1 | 10.1016/j.bmcl.2008.07.115 | |||
CHEMBL10309 | 4653 | None | 0 | Human | Functional | pIC50 | = | 6.2 | 6.2 | 13 | 2 | ChEMBL | 440 | 4 | 1 | 3 | 4.0 | O=C1CCC(c2ccccc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C(=O)N1 | 10.1016/j.bmcl.2008.07.115 | |||
56677274 | 64280 | None | 0 | Human | Functional | pIC50 | = | 5.2 | 5.2 | - | 1 | ChEMBL | 411 | 2 | 1 | 2 | 3.9 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)c2ccccc2)C1)N1CCCC1 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1809035 | 64280 | None | 0 | Human | Functional | pIC50 | = | 5.2 | 5.2 | - | 1 | ChEMBL | 411 | 2 | 1 | 2 | 3.9 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)c2ccccc2)C1)N1CCCC1 | 10.1016/j.bmcl.2011.06.070 | |||
45482819 | 200647 | None | 0 | Human | Functional | pIC50 | = | 7.2 | 7.2 | - | 1 | ChEMBL | 429 | 4 | 2 | 3 | 3.9 | CCN(CC)C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccn2)C1 | 10.1016/j.bmcl.2009.09.002 | |||
CHEMBL575049 | 200647 | None | 0 | Human | Functional | pIC50 | = | 7.2 | 7.2 | - | 1 | ChEMBL | 429 | 4 | 2 | 3 | 3.9 | CCN(CC)C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccn2)C1 | 10.1016/j.bmcl.2009.09.002 | |||
56670452 | 64270 | None | 0 | Human | Functional | pIC50 | = | 5.2 | 5.2 | - | 1 | ChEMBL | 483 | 4 | 2 | 3 | 4.3 | CN(C)Cc1cccc(NC(=O)N2C[C@H](C(=O)N3CCCC3)C=C3c4cccc5[nH]cc(c45)C[C@H]32)c1 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1809022 | 64270 | None | 0 | Human | Functional | pIC50 | = | 5.2 | 5.2 | - | 1 | ChEMBL | 483 | 4 | 2 | 3 | 4.3 | CN(C)Cc1cccc(NC(=O)N2C[C@H](C(=O)N3CCCC3)C=C3c4cccc5[nH]cc(c45)C[C@H]32)c1 | 10.1016/j.bmcl.2011.06.070 | |||
89726367 | 147175 | None | 0 | Human | Functional | pIC50 | = | 5.2 | 5.2 | - | 1 | ChEMBL | 514 | 5 | 1 | 9 | 3.3 | C[C@@H]1CN(c2sc(C3COC3)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL3927250 | 147175 | None | 0 | Human | Functional | pIC50 | = | 5.2 | 5.2 | - | 1 | ChEMBL | 514 | 5 | 1 | 9 | 3.3 | C[C@@H]1CN(c2sc(C3COC3)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | 10.1021/acs.jmedchem.2c00675 | |||
168271575 | 190303 | None | 0 | Human | Functional | pIC50 | = | 6.2 | 6.2 | - | 1 | ChEMBL | 580 | 5 | 2 | 9 | 4.0 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccc(C(C)(C)O)c(F)c4[nH]3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00676 | |||
CHEMBL5174313 | 190303 | None | 0 | Human | Functional | pIC50 | = | 6.2 | 6.2 | - | 1 | ChEMBL | 580 | 5 | 2 | 9 | 4.0 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccc(C(C)(C)O)c(F)c4[nH]3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00676 | |||
53322460 | 58194 | None | 0 | Human | Functional | pIC50 | = | 7.2 | 7.2 | - | 1 | ChEMBL | 419 | 3 | 1 | 5 | 2.6 | CNC(=O)c1cnc(N2CCN(C3CCN(C(F)(F)F)CC3)[C@@H](C)C2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
CHEMBL1681834 | 58194 | None | 0 | Human | Functional | pIC50 | = | 7.2 | 7.2 | - | 1 | ChEMBL | 419 | 3 | 1 | 5 | 2.6 | CNC(=O)c1cnc(N2CCN(C3CCN(C(F)(F)F)CC3)[C@@H](C)C2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
44570273 | 177691 | None | 0 | Human | Functional | pIC50 | = | 7.2 | 7.2 | 25 | 2 | ChEMBL | 479 | 4 | 1 | 5 | 3.3 | C[C@H]1CN(S(=O)(=O)C[C@]23CC[C@H](C[C@H]2O)C3(C)C)CCN1c1ncc(C(F)(F)F)cc1F | 10.1016/j.bmcl.2008.11.008 | |||
CHEMBL464065 | 177691 | None | 0 | Human | Functional | pIC50 | = | 7.2 | 7.2 | 25 | 2 | ChEMBL | 479 | 4 | 1 | 5 | 3.3 | C[C@H]1CN(S(=O)(=O)C[C@]23CC[C@H](C[C@H]2O)C3(C)C)CCN1c1ncc(C(F)(F)F)cc1F | 10.1016/j.bmcl.2008.11.008 | |||
53322511 | 58230 | None | 0 | Human | Functional | pIC50 | = | 6.2 | 6.2 | - | 1 | ChEMBL | 501 | 5 | 0 | 5 | 4.4 | C[C@H]1CN(c2ncc(C(=O)N3CCC3)cc2Cl)CCN1C1CCN(Cc2ccc(Cl)cc2)CC1 | 10.1016/j.bmcl.2010.12.114 | |||
CHEMBL1681873 | 58230 | None | 0 | Human | Functional | pIC50 | = | 6.2 | 6.2 | - | 1 | ChEMBL | 501 | 5 | 0 | 5 | 4.4 | C[C@H]1CN(c2ncc(C(=O)N3CCC3)cc2Cl)CCN1C1CCN(Cc2ccc(Cl)cc2)CC1 | 10.1016/j.bmcl.2010.12.114 | |||
44581159 | 175899 | None | 0 | Human | Functional | pIC50 | = | 6.2 | 6.2 | - | 1 | ChEMBL | 484 | 5 | 2 | 4 | 3.7 | O=C1CCC(c2cccc(C(=O)O)c2)(C2CCN(Cc3ccc(Br)cc3)CC2)C(=O)N1 | 10.1016/j.bmcl.2008.07.115 | |||
CHEMBL458422 | 175899 | None | 0 | Human | Functional | pIC50 | = | 6.2 | 6.2 | - | 1 | ChEMBL | 484 | 5 | 2 | 4 | 3.7 | O=C1CCC(c2cccc(C(=O)O)c2)(C2CCN(Cc3ccc(Br)cc3)CC2)C(=O)N1 | 10.1016/j.bmcl.2008.07.115 | |||
44581108 | 187882 | None | 0 | Human | Functional | pIC50 | = | 6.2 | 6.2 | - | 1 | ChEMBL | 441 | 4 | 1 | 4 | 3.4 | O=C1CCC(c2ccncc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C(=O)N1 | 10.1016/j.bmcl.2008.07.115 | |||
CHEMBL495748 | 187882 | None | 0 | Human | Functional | pIC50 | = | 6.2 | 6.2 | - | 1 | ChEMBL | 441 | 4 | 1 | 4 | 3.4 | O=C1CCC(c2ccncc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C(=O)N1 | 10.1016/j.bmcl.2008.07.115 | |||
44570517 | 178284 | None | 0 | Human | Functional | pIC50 | = | 6.2 | 6.2 | - | 1 | ChEMBL | 459 | 4 | 0 | 5 | 3.3 | CC1CN(c2ccc(C(F)(F)F)cn2)CCN1S(=O)(=O)C[C@]12CC[C@H](CC1=O)C2(C)C | 10.1016/j.bmcl.2008.11.008 | |||
CHEMBL464923 | 178284 | None | 0 | Human | Functional | pIC50 | = | 6.2 | 6.2 | - | 1 | ChEMBL | 459 | 4 | 0 | 5 | 3.3 | CC1CN(c2ccc(C(F)(F)F)cn2)CCN1S(=O)(=O)C[C@]12CC[C@H](CC1=O)C2(C)C | 10.1016/j.bmcl.2008.11.008 | |||
44570472 | 183513 | None | 0 | Human | Functional | pIC50 | = | 6.2 | 6.2 | - | 1 | ChEMBL | 456 | 4 | 0 | 6 | 2.1 | CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCN(c3ncc(Br)cn3)CC1)C(=O)C2 | 10.1016/j.bmcl.2008.11.008 | |||
CHEMBL479829 | 183513 | None | 0 | Human | Functional | pIC50 | = | 6.2 | 6.2 | - | 1 | ChEMBL | 456 | 4 | 0 | 6 | 2.1 | CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCN(c3ncc(Br)cn3)CC1)C(=O)C2 | 10.1016/j.bmcl.2008.11.008 | |||
44570142 | 184086 | None | 0 | Human | Functional | pIC50 | = | 6.2 | 6.2 | - | 1 | ChEMBL | 524 | 6 | 1 | 6 | 2.3 | CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCN(c3ccc(C(F)(F)F)cn3)CC1)C(NS(C)(=O)=O)C2 | 10.1016/j.bmcl.2008.11.008 | |||
CHEMBL481776 | 184086 | None | 0 | Human | Functional | pIC50 | = | 6.2 | 6.2 | - | 1 | ChEMBL | 524 | 6 | 1 | 6 | 2.3 | CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCN(c3ccc(C(F)(F)F)cn3)CC1)C(NS(C)(=O)=O)C2 | 10.1016/j.bmcl.2008.11.008 | |||
44570596 | 190969 | None | 0 | Human | Functional | pIC50 | = | 6.2 | 6.2 | - | 1 | ChEMBL | 473 | 5 | 0 | 5 | 3.7 | CCC1CN(S(=O)(=O)C[C@]23CC[C@H](CC2=O)C3(C)C)CCN1c1ccc(C(F)(F)F)cn1 | 10.1016/j.bmcl.2008.11.008 | |||
CHEMBL518459 | 190969 | None | 0 | Human | Functional | pIC50 | = | 6.2 | 6.2 | - | 1 | ChEMBL | 473 | 5 | 0 | 5 | 3.7 | CCC1CN(S(=O)(=O)C[C@]23CC[C@H](CC2=O)C3(C)C)CCN1c1ccc(C(F)(F)F)cn1 | 10.1016/j.bmcl.2008.11.008 | |||
44570221 | 178510 | None | 0 | Mouse | Functional | pIC50 | = | 6.2 | 6.2 | -1 | 2 | ChEMBL | 461 | 4 | 1 | 5 | 3.1 | C[C@H]1CN(S(=O)(=O)C[C@]23CC[C@H](C[C@H]2O)C3(C)C)CCN1c1ccc(C(F)(F)F)cn1 | 10.1016/j.bmcl.2008.11.008 | |||
CHEMBL465918 | 178510 | None | 0 | Mouse | Functional | pIC50 | = | 6.2 | 6.2 | -1 | 2 | ChEMBL | 461 | 4 | 1 | 5 | 3.1 | C[C@H]1CN(S(=O)(=O)C[C@]23CC[C@H](C[C@H]2O)C3(C)C)CCN1c1ccc(C(F)(F)F)cn1 | 10.1016/j.bmcl.2008.11.008 | |||
44570219 | 184010 | None | 0 | Mouse | Functional | pIC50 | = | 6.2 | 6.2 | -3 | 2 | ChEMBL | 461 | 4 | 1 | 5 | 3.1 | C[C@H]1CN(S(=O)(=O)C[C@]23CC[C@H](CC2O)C3(C)C)CCN1c1ccc(C(F)(F)F)cn1 | 10.1016/j.bmcl.2008.11.008 | |||
CHEMBL481197 | 184010 | None | 0 | Mouse | Functional | pIC50 | = | 6.2 | 6.2 | -3 | 2 | ChEMBL | 461 | 4 | 1 | 5 | 3.1 | C[C@H]1CN(S(=O)(=O)C[C@]23CC[C@H](CC2O)C3(C)C)CCN1c1ccc(C(F)(F)F)cn1 | 10.1016/j.bmcl.2008.11.008 | |||
44570547 | 178477 | None | 0 | Human | Functional | pIC50 | = | 5.2 | 5.2 | - | 1 | ChEMBL | 473 | 4 | 0 | 5 | 3.7 | C[C@H]1CN(S(=O)(=O)C[C@]23CC[C@H](CC2=O)C3(C)C)[C@H](C)CN1c1ccc(C(F)(F)F)cn1 | 10.1016/j.bmcl.2008.11.008 | |||
CHEMBL465282 | 178477 | None | 0 | Human | Functional | pIC50 | = | 5.2 | 5.2 | - | 1 | ChEMBL | 473 | 4 | 0 | 5 | 3.7 | C[C@H]1CN(S(=O)(=O)C[C@]23CC[C@H](CC2=O)C3(C)C)[C@H](C)CN1c1ccc(C(F)(F)F)cn1 | 10.1016/j.bmcl.2008.11.008 | |||
44570627 | 183931 | None | 0 | Human | Functional | pIC50 | = | 5.2 | 5.2 | - | 1 | ChEMBL | 459 | 4 | 0 | 5 | 3.3 | CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCCN(c3ccc(C(F)(F)F)cn3)CC1)C(=O)C2 | 10.1016/j.bmcl.2008.11.008 | |||
CHEMBL480600 | 183931 | None | 0 | Human | Functional | pIC50 | = | 5.2 | 5.2 | - | 1 | ChEMBL | 459 | 4 | 0 | 5 | 3.3 | CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCCN(c3ccc(C(F)(F)F)cn3)CC1)C(=O)C2 | 10.1016/j.bmcl.2008.11.008 | |||
44570218 | 184009 | None | 0 | Mouse | Functional | pIC50 | = | 5.2 | 5.2 | -19 | 2 | ChEMBL | 493 | 5 | 1 | 6 | 2.4 | CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCN(c3ncc(C(F)(F)F)cc3F)[C@H](CO)C1)C(=O)C2 | 10.1016/j.bmcl.2008.11.008 | |||
CHEMBL481196 | 184009 | None | 0 | Mouse | Functional | pIC50 | = | 5.2 | 5.2 | -19 | 2 | ChEMBL | 493 | 5 | 1 | 6 | 2.4 | CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCN(c3ncc(C(F)(F)F)cc3F)[C@H](CO)C1)C(=O)C2 | 10.1016/j.bmcl.2008.11.008 | |||
24739554 | 188169 | None | 0 | Human | Functional | pIC50 | = | 5.2 | 5.2 | 64 | 2 | ChEMBL | 531 | 5 | 1 | 2 | 6.9 | O=C(Nc1ccccc1)N1CCCC(c2ccccc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C1 | 10.1016/j.bmcl.2008.07.115 | |||
CHEMBL497799 | 188169 | None | 0 | Human | Functional | pIC50 | = | 5.2 | 5.2 | 64 | 2 | ChEMBL | 531 | 5 | 1 | 2 | 6.9 | O=C(Nc1ccccc1)N1CCCC(c2ccccc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C1 | 10.1016/j.bmcl.2008.07.115 | |||
53319880 | 58211 | None | 0 | Human | Functional | pIC50 | = | 7.2 | 7.2 | - | 1 | ChEMBL | 475 | 5 | 1 | 5 | 3.8 | CNC(=O)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4)CC3C)CC2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
CHEMBL1681854 | 58211 | None | 0 | Human | Functional | pIC50 | = | 7.2 | 7.2 | - | 1 | ChEMBL | 475 | 5 | 1 | 5 | 3.8 | CNC(=O)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4)CC3C)CC2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
15605618 | 72231 | None | 0 | Human | Functional | pIC50 | = | 6.2 | 6.2 | - | 1 | ChEMBL | 571 | 8 | 3 | 5 | 5.1 | CCNC(=O)N1CCCN(c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2NC(=O)c2ccco2)CC1 | 10.1016/j.bmcl.2005.09.020 | |||
CHEMBL198076 | 72231 | None | 0 | Human | Functional | pIC50 | = | 6.2 | 6.2 | - | 1 | ChEMBL | 571 | 8 | 3 | 5 | 5.1 | CCNC(=O)N1CCCN(c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2NC(=O)c2ccco2)CC1 | 10.1016/j.bmcl.2005.09.020 | |||
44447097 | 154971 | None | 0 | Human | Functional | pIC50 | = | 6.2 | 6.2 | - | 1 | ChEMBL | 587 | 9 | 0 | 7 | 5.0 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc2ncccn2c1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2007.11.060 | |||
CHEMBL400736 | 154971 | None | 0 | Human | Functional | pIC50 | = | 6.2 | 6.2 | - | 1 | ChEMBL | 587 | 9 | 0 | 7 | 5.0 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc2ncccn2c1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2007.11.060 | |||
44447097 | 154971 | None | 0 | Human | Functional | pIC50 | = | 6.2 | 6.2 | - | 1 | ChEMBL | 587 | 9 | 0 | 7 | 5.0 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc2ncccn2c1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2009.07.021 | |||
CHEMBL400736 | 154971 | None | 0 | Human | Functional | pIC50 | = | 6.2 | 6.2 | - | 1 | ChEMBL | 587 | 9 | 0 | 7 | 5.0 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc2ncccn2c1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2009.07.021 | |||
46891273 | 6714 | None | 0 | Human | Functional | pIC50 | = | 5.2 | 5.2 | - | 1 | ChEMBL | 411 | 8 | 1 | 4 | 3.8 | COc1ccc(S(=O)(=O)N(Cc2ccccc2)Cc2ccc(C(=O)O)cc2)cc1 | 10.1016/j.bmcl.2010.04.113 | |||
CHEMBL1083645 | 6714 | None | 0 | Human | Functional | pIC50 | = | 5.2 | 5.2 | - | 1 | ChEMBL | 411 | 8 | 1 | 4 | 3.8 | COc1ccc(S(=O)(=O)N(Cc2ccccc2)Cc2ccc(C(=O)O)cc2)cc1 | 10.1016/j.bmcl.2010.04.113 | |||
45482823 | 200395 | None | 0 | Human | Functional | pIC50 | = | 7.2 | 7.2 | - | 1 | ChEMBL | 429 | 4 | 2 | 3 | 3.9 | CCN(CC)C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2cccnc2)C1 | 10.1016/j.bmcl.2009.09.002 | |||
CHEMBL573232 | 200395 | None | 0 | Human | Functional | pIC50 | = | 7.2 | 7.2 | - | 1 | ChEMBL | 429 | 4 | 2 | 3 | 3.9 | CCN(CC)C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2cccnc2)C1 | 10.1016/j.bmcl.2009.09.002 | |||
56663558 | 64259 | None | 0 | Human | Functional | pIC50 | = | 7.2 | 7.2 | 3 | 2 | ChEMBL | 490 | 2 | 2 | 4 | 2.9 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CCS(=O)(=O)CC1 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1809010 | 64259 | None | 0 | Human | Functional | pIC50 | = | 7.2 | 7.2 | 3 | 2 | ChEMBL | 490 | 2 | 2 | 4 | 2.9 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CCS(=O)(=O)CC1 | 10.1016/j.bmcl.2011.06.070 | |||
71680142 | 143133 | None | 0 | Human | Functional | pIC50 | = | 7.2 | 7.2 | - | 1 | ChEMBL | 458 | 4 | 1 | 8 | 3.2 | C[C@H]1CN(c2scnc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL3894991 | 143133 | None | 0 | Human | Functional | pIC50 | = | 7.2 | 7.2 | - | 1 | ChEMBL | 458 | 4 | 1 | 8 | 3.2 | C[C@H]1CN(c2scnc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | 10.1021/acs.jmedchem.2c00675 | |||
44253448 | 7179 | None | 0 | Human | Functional | pIC50 | = | 6.2 | 6.2 | - | 1 | ChEMBL | 478 | 11 | 1 | 4 | 4.6 | CCOc1ccc(S(=O)(=O)N(Cc2ccccc2)Cc2ccc(C(=O)NCC3CC3)cc2)cc1 | 10.1016/j.bmcl.2010.04.113 | |||
CHEMBL1085517 | 7179 | None | 0 | Human | Functional | pIC50 | = | 6.2 | 6.2 | - | 1 | ChEMBL | 478 | 11 | 1 | 4 | 4.6 | CCOc1ccc(S(=O)(=O)N(Cc2ccccc2)Cc2ccc(C(=O)NCC3CC3)cc2)cc1 | 10.1016/j.bmcl.2010.04.113 | |||
168284829 | 191892 | None | 0 | Human | Functional | pIC50 | = | 7.2 | 7.2 | - | 1 | ChEMBL | 576 | 6 | 1 | 10 | 3.4 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccc(OC5COC5)cc4[nH]3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00676 | |||
CHEMBL5198121 | 191892 | None | 0 | Human | Functional | pIC50 | = | 7.2 | 7.2 | - | 1 | ChEMBL | 576 | 6 | 1 | 10 | 3.4 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccc(OC5COC5)cc4[nH]3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00676 | |||
45482800 | 200378 | None | 0 | Human | Functional | pIC50 | = | 5.2 | 5.2 | - | 1 | ChEMBL | 429 | 4 | 2 | 3 | 3.9 | CCN(CC)C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccncc2)C1 | 10.1016/j.bmcl.2009.09.002 | |||
CHEMBL573022 | 200378 | None | 0 | Human | Functional | pIC50 | = | 5.2 | 5.2 | - | 1 | ChEMBL | 429 | 4 | 2 | 3 | 3.9 | CCN(CC)C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccncc2)C1 | 10.1016/j.bmcl.2009.09.002 | |||
89726765 | 149355 | None | 0 | Human | Functional | pIC50 | = | 5.2 | 5.2 | - | 1 | ChEMBL | 533 | 7 | 0 | 9 | 3.8 | COCCn1c(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3cccn3)[C@H](C)C2)nc2ccccc21 | 10.1021/acs.jmedchem.2c00676 | |||
CHEMBL3944489 | 149355 | None | 0 | Human | Functional | pIC50 | = | 5.2 | 5.2 | - | 1 | ChEMBL | 533 | 7 | 0 | 9 | 3.8 | COCCn1c(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3cccn3)[C@H](C)C2)nc2ccccc21 | 10.1021/acs.jmedchem.2c00676 | |||
44580902 | 187943 | None | 0 | Human | Functional | pIC50 | = | 6.2 | 6.2 | - | 1 | ChEMBL | 508 | 4 | 0 | 2 | 5.8 | O=C(N1CCCC(c2ccccc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C1)C(F)(F)F | 10.1016/j.bmcl.2008.07.115 | |||
CHEMBL496171 | 187943 | None | 0 | Human | Functional | pIC50 | = | 6.2 | 6.2 | - | 1 | ChEMBL | 508 | 4 | 0 | 2 | 5.8 | O=C(N1CCCC(c2ccccc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C1)C(F)(F)F | 10.1016/j.bmcl.2008.07.115 | |||
44253449 | 6401 | None | 0 | Human | Functional | pIC50 | = | 6.2 | 6.2 | - | 1 | ChEMBL | 456 | 7 | 1 | 7 | 3.9 | O=S(=O)(c1ccc(Cl)cc1)N(Cc1ccc(-c2nnc(O)o2)cc1)Cc1ccccn1 | 10.1016/j.bmcl.2010.04.113 | |||
CHEMBL1082320 | 6401 | None | 0 | Human | Functional | pIC50 | = | 6.2 | 6.2 | - | 1 | ChEMBL | 456 | 7 | 1 | 7 | 3.9 | O=S(=O)(c1ccc(Cl)cc1)N(Cc1ccc(-c2nnc(O)o2)cc1)Cc1ccccn1 | 10.1016/j.bmcl.2010.04.113 | |||
44253447 | 7341 | None | 0 | Human | Functional | pIC50 | = | 6.2 | 6.2 | - | 1 | ChEMBL | 464 | 10 | 1 | 4 | 4.2 | COc1ccc(S(=O)(=O)N(Cc2ccccc2)Cc2ccc(C(=O)NCC3CC3)cc2)cc1 | 10.1016/j.bmcl.2010.04.113 | |||
CHEMBL1086232 | 7341 | None | 0 | Human | Functional | pIC50 | = | 6.2 | 6.2 | - | 1 | ChEMBL | 464 | 10 | 1 | 4 | 4.2 | COc1ccc(S(=O)(=O)N(Cc2ccccc2)Cc2ccc(C(=O)NCC3CC3)cc2)cc1 | 10.1016/j.bmcl.2010.04.113 | |||
56673940 | 64272 | None | 0 | Human | Functional | pIC50 | = | 8.2 | 8.2 | -1 | 2 | ChEMBL | 432 | 2 | 2 | 3 | 4.3 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccsc2)C1)N1CCCC1 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1809024 | 64272 | None | 0 | Human | Functional | pIC50 | = | 8.2 | 8.2 | -1 | 2 | ChEMBL | 432 | 2 | 2 | 3 | 4.3 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccsc2)C1)N1CCCC1 | 10.1016/j.bmcl.2011.06.070 | |||
90480455 | 191382 | None | 0 | Human | Functional | pIC50 | = | 8.2 | 8.2 | - | 1 | ChEMBL | 510 | 6 | 0 | 10 | 3.0 | CCOc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3nc(C)nc3C)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL5190588 | 191382 | None | 0 | Human | Functional | pIC50 | = | 8.2 | 8.2 | - | 1 | ChEMBL | 510 | 6 | 0 | 10 | 3.0 | CCOc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3nc(C)nc3C)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
45486523 | 201007 | None | 0 | Human | Functional | pIC50 | = | 8.2 | 8.2 | - | 1 | ChEMBL | 617 | 10 | 0 | 8 | 5.0 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(C(F)(F)F)c(F)c1)[C@H](C)c1nc2c(OC)nccn2c1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2009.07.021 | |||
CHEMBL578187 | 201007 | None | 0 | Human | Functional | pIC50 | = | 8.2 | 8.2 | - | 1 | ChEMBL | 617 | 10 | 0 | 8 | 5.0 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(C(F)(F)F)c(F)c1)[C@H](C)c1nc2c(OC)nccn2c1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2009.07.021 | |||
44453267 | 95181 | None | 0 | Human | Functional | pIC50 | = | 7.2 | 7.2 | 9 | 2 | ChEMBL | 508 | 9 | 1 | 5 | 5.2 | CN(CCCn1c(=N)n(CC(=O)c2ccc(Cl)cc2)c2cccc(Cl)c21)C(=O)Cc1ccccc1 | 10.1016/j.bmcl.2008.02.049 | |||
CHEMBL255583 | 95181 | None | 0 | Human | Functional | pIC50 | = | 7.2 | 7.2 | 9 | 2 | ChEMBL | 508 | 9 | 1 | 5 | 5.2 | CN(CCCn1c(=N)n(CC(=O)c2ccc(Cl)cc2)c2cccc(Cl)c21)C(=O)Cc1ccccc1 | 10.1016/j.bmcl.2008.02.049 | |||
17754488 | 95619 | None | 0 | Human | Functional | pIC50 | = | 7.2 | 7.2 | - | 1 | ChEMBL | 327 | 4 | 1 | 4 | 3.6 | CCc1cccc2c1n(C)c(=N)n2CC(=O)c1ccc(Cl)cc1 | 10.1016/j.bmcl.2008.01.074 | |||
CHEMBL257663 | 95619 | None | 0 | Human | Functional | pIC50 | = | 7.2 | 7.2 | - | 1 | ChEMBL | 327 | 4 | 1 | 4 | 3.6 | CCc1cccc2c1n(C)c(=N)n2CC(=O)c1ccc(Cl)cc1 | 10.1016/j.bmcl.2008.01.074 | |||
71679146 | 153498 | None | 0 | Human | Functional | pIC50 | = | 7.2 | 7.2 | - | 1 | ChEMBL | 526 | 4 | 1 | 8 | 4.2 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | 10.1021/acs.jmedchem.2c00676 | |||
CHEMBL3978935 | 153498 | None | 0 | Human | Functional | pIC50 | = | 7.2 | 7.2 | - | 1 | ChEMBL | 526 | 4 | 1 | 8 | 4.2 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | 10.1021/acs.jmedchem.2c00676 | |||
168279606 | 191087 | None | 0 | Human | Functional | pIC50 | = | 7.2 | 7.2 | - | 1 | ChEMBL | 495 | 6 | 0 | 9 | 3.3 | CCOc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3ccc(C)n3)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL5186167 | 191087 | None | 0 | Human | Functional | pIC50 | = | 7.2 | 7.2 | - | 1 | ChEMBL | 495 | 6 | 0 | 9 | 3.3 | CCOc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3ccc(C)n3)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
15605197 | 72141 | None | 0 | Human | Functional | pIC50 | = | 7.2 | 7.2 | - | 1 | ChEMBL | 581 | 8 | 3 | 4 | 5.5 | CCNC(=O)N1CCCN(c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2NC(=O)c2ccccc2)CC1 | 10.1016/j.bmcl.2005.09.020 | |||
CHEMBL197818 | 72141 | None | 0 | Human | Functional | pIC50 | = | 7.2 | 7.2 | - | 1 | ChEMBL | 581 | 8 | 3 | 4 | 5.5 | CCNC(=O)N1CCCN(c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2NC(=O)c2ccccc2)CC1 | 10.1016/j.bmcl.2005.09.020 | |||
71525974 | 133389 | None | 0 | Human | Functional | pIC50 | = | 6.2 | 6.2 | -489 | 4 | ChEMBL | 439 | 7 | 3 | 8 | 2.5 | Cc1ccc([C@H](Nc2c(Nc3cccc(C(=O)N(C)C)c3O)c(=O)c2=O)C2(C)COC2)o1 | nan | |||
CHEMBL3704570 | 133389 | None | 0 | Human | Functional | pIC50 | = | 6.2 | 6.2 | -489 | 4 | ChEMBL | 439 | 7 | 3 | 8 | 2.5 | Cc1ccc([C@H](Nc2c(Nc3cccc(C(=O)N(C)C)c3O)c(=O)c2=O)C2(C)COC2)o1 | nan | |||
15604688 | 72288 | None | 0 | Human | Functional | pIC50 | = | 6.2 | 6.2 | - | 1 | ChEMBL | 615 | 8 | 3 | 4 | 6.1 | CCNC(=O)N1CCCN(c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2NC(=O)c2ccccc2Cl)CC1 | 10.1016/j.bmcl.2005.09.020 | |||
CHEMBL198237 | 72288 | None | 0 | Human | Functional | pIC50 | = | 6.2 | 6.2 | - | 1 | ChEMBL | 615 | 8 | 3 | 4 | 6.1 | CCNC(=O)N1CCCN(c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2NC(=O)c2ccccc2Cl)CC1 | 10.1016/j.bmcl.2005.09.020 | |||
53318561 | 58215 | None | 0 | Human | Functional | pIC50 | = | 5.2 | 5.2 | - | 1 | ChEMBL | 489 | 5 | 1 | 5 | 3.5 | CNC(=O)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4)C(=O)C3)[C@@H](C)C2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
CHEMBL1681858 | 58215 | None | 0 | Human | Functional | pIC50 | = | 5.2 | 5.2 | - | 1 | ChEMBL | 489 | 5 | 1 | 5 | 3.5 | CNC(=O)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4)C(=O)C3)[C@@H](C)C2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
56680588 | 64244 | None | 0 | Human | Functional | pIC50 | = | 7.2 | 7.2 | -1 | 2 | ChEMBL | 400 | 3 | 3 | 2 | 3.8 | CCNC(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1808995 | 64244 | None | 0 | Human | Functional | pIC50 | = | 7.2 | 7.2 | -1 | 2 | ChEMBL | 400 | 3 | 3 | 2 | 3.8 | CCNC(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1 | 10.1016/j.bmcl.2011.06.070 | |||
44447090 | 94942 | None | 0 | Human | Functional | pIC50 | = | 7.1 | 7.1 | - | 1 | ChEMBL | 597 | 9 | 0 | 5 | 6.5 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc2ccccc2cc1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2007.11.060 | |||
CHEMBL254083 | 94942 | None | 0 | Human | Functional | pIC50 | = | 7.1 | 7.1 | - | 1 | ChEMBL | 597 | 9 | 0 | 5 | 6.5 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc2ccccc2cc1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2007.11.060 | |||
44447096 | 154508 | None | 0 | Human | Functional | pIC50 | = | 7.1 | 7.1 | - | 1 | ChEMBL | 586 | 9 | 0 | 6 | 5.6 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc2ccccn2c1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2007.11.060 | |||
CHEMBL398941 | 154508 | None | 0 | Human | Functional | pIC50 | = | 7.1 | 7.1 | - | 1 | ChEMBL | 586 | 9 | 0 | 6 | 5.6 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc2ccccn2c1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2007.11.060 | |||
57390209 | 69995 | None | 0 | Human | Functional | pIC50 | = | 7.1 | 7.1 | - | 1 | ChEMBL | 634 | 7 | 0 | 7 | 5.0 | C[C@H](c1nc2ncccc2c(=O)n1-c1ccc(F)cc1)N(CC1CCS(=O)(=O)CC1)C(=O)Cc1ccc(F)c(C(F)(F)F)c1 | 10.1016/j.bmcl.2011.10.120 | |||
CHEMBL1939562 | 69995 | None | 0 | Human | Functional | pIC50 | = | 7.1 | 7.1 | - | 1 | ChEMBL | 634 | 7 | 0 | 7 | 5.0 | C[C@H](c1nc2ncccc2c(=O)n1-c1ccc(F)cc1)N(CC1CCS(=O)(=O)CC1)C(=O)Cc1ccc(F)c(C(F)(F)F)c1 | 10.1016/j.bmcl.2011.10.120 | |||
56673941 | 64274 | None | 0 | Human | Functional | pIC50 | = | 7.1 | 7.1 | -1 | 2 | ChEMBL | 418 | 2 | 2 | 2 | 3.7 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)NC2CCCC2)C1)N1CCCC1 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1809027 | 64274 | None | 0 | Human | Functional | pIC50 | = | 7.1 | 7.1 | -1 | 2 | ChEMBL | 418 | 2 | 2 | 2 | 3.7 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)NC2CCCC2)C1)N1CCCC1 | 10.1016/j.bmcl.2011.06.070 | |||
53322507 | 58217 | None | 0 | Human | Functional | pIC50 | = | 5.1 | 5.1 | - | 1 | ChEMBL | 475 | 5 | 1 | 5 | 3.9 | CNC(=O)c1cnc(N2CCC(N3CCN(Cc4ccc(Cl)cc4)C[C@H]3C)CC2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
CHEMBL1681860 | 58217 | None | 0 | Human | Functional | pIC50 | = | 5.1 | 5.1 | - | 1 | ChEMBL | 475 | 5 | 1 | 5 | 3.9 | CNC(=O)c1cnc(N2CCC(N3CCN(Cc4ccc(Cl)cc4)C[C@H]3C)CC2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
45482789 | 201381 | None | 0 | Rat | Functional | pIC50 | = | 7.1 | 7.1 | -1 | 14 | ChEMBL | 428 | 4 | 2 | 2 | 4.5 | CCN(CC)C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL584554 | 201381 | None | 0 | Rat | Functional | pIC50 | = | 7.1 | 7.1 | -1 | 14 | ChEMBL | 428 | 4 | 2 | 2 | 4.5 | CCN(CC)C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1 | 10.1016/j.bmcl.2011.06.070 | |||
45482789 | 201381 | None | 0 | Human | Functional | pIC50 | = | 7.1 | 7.1 | 1 | 14 | ChEMBL | 428 | 4 | 2 | 2 | 4.5 | CCN(CC)C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1 | 10.1016/j.bmcl.2009.09.002 | |||
CHEMBL584554 | 201381 | None | 0 | Human | Functional | pIC50 | = | 7.1 | 7.1 | 1 | 14 | ChEMBL | 428 | 4 | 2 | 2 | 4.5 | CCN(CC)C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1 | 10.1016/j.bmcl.2009.09.002 | |||
56680571 | 64254 | None | 0 | Human | Functional | pIC50 | = | 7.1 | 7.1 | - | 1 | ChEMBL | 455 | 2 | 3 | 3 | 2.6 | O=C1CN(C(=O)[C@@H]2C=C3c4cccc5[nH]cc(c45)C[C@H]3N(C(=O)Nc3ccccc3)C2)CCN1 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1809005 | 64254 | None | 0 | Human | Functional | pIC50 | = | 7.1 | 7.1 | - | 1 | ChEMBL | 455 | 2 | 3 | 3 | 2.6 | O=C1CN(C(=O)[C@@H]2C=C3c4cccc5[nH]cc(c45)C[C@H]3N(C(=O)Nc3ccccc3)C2)CCN1 | 10.1016/j.bmcl.2011.06.070 | |||
134143368 | 145879 | None | 0 | Human | Functional | pIC50 | = | 7.1 | 7.1 | - | 1 | ChEMBL | 438 | 9 | 0 | 6 | 3.4 | COc1cc(CN(C)C(C)c2ccc3c(c2)CCO3)ccc1OCCN1C(=O)CCC1=O | 10.1016/j.bmcl.2016.10.035 | |||
CHEMBL3916901 | 145879 | None | 0 | Human | Functional | pIC50 | = | 7.1 | 7.1 | - | 1 | ChEMBL | 438 | 9 | 0 | 6 | 3.4 | COc1cc(CN(C)C(C)c2ccc3c(c2)CCO3)ccc1OCCN1C(=O)CCC1=O | 10.1016/j.bmcl.2016.10.035 | |||
56670451 | 64268 | None | 0 | Mouse | Functional | pIC50 | = | 7.1 | 7.1 | 1 | 2 | ChEMBL | 456 | 3 | 2 | 3 | 4.3 | COc1cccc(NC(=O)N2C[C@H](C(=O)N3CCCC3)C=C3c4cccc5[nH]cc(c45)C[C@H]32)c1 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1809019 | 64268 | None | 0 | Mouse | Functional | pIC50 | = | 7.1 | 7.1 | 1 | 2 | ChEMBL | 456 | 3 | 2 | 3 | 4.3 | COc1cccc(NC(=O)N2C[C@H](C(=O)N3CCCC3)C=C3c4cccc5[nH]cc(c45)C[C@H]32)c1 | 10.1016/j.bmcl.2011.06.070 | |||
71678461 | 146148 | None | 0 | Human | Functional | pIC50 | = | 6.1 | 6.1 | - | 1 | ChEMBL | 498 | 5 | 1 | 8 | 4.0 | C[C@@H]1CN(c2sc(C3CC3)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL3919018 | 146148 | None | 0 | Human | Functional | pIC50 | = | 6.1 | 6.1 | - | 1 | ChEMBL | 498 | 5 | 1 | 8 | 4.0 | C[C@@H]1CN(c2sc(C3CC3)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | 10.1021/acs.jmedchem.2c00675 | |||
89726090 | 144174 | None | 0 | Human | Functional | pIC50 | = | 6.1 | 6.1 | - | 1 | ChEMBL | 572 | 4 | 1 | 8 | 4.7 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4c(C(F)(F)F)cccc4[nH]3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00676 | |||
CHEMBL3903412 | 144174 | None | 0 | Human | Functional | pIC50 | = | 6.1 | 6.1 | - | 1 | ChEMBL | 572 | 4 | 1 | 8 | 4.7 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4c(C(F)(F)F)cccc4[nH]3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00676 | |||
46883299 | 5480 | None | 0 | Human | Functional | pIC50 | = | 7.1 | 7.1 | - | 1 | ChEMBL | 604 | 9 | 0 | 6 | 6.7 | CCOc1ccc(-n2c([C@@H](C)N(Cc3cccnc3)C(=O)Cc3ccc(C(F)(F)F)c(F)c3)nc3ccccc3c2=O)cc1 | 10.1016/j.bmcl.2009.07.032 | |||
CHEMBL1075640 | 5480 | None | 0 | Human | Functional | pIC50 | = | 7.1 | 7.1 | - | 1 | ChEMBL | 604 | 9 | 0 | 6 | 6.7 | CCOc1ccc(-n2c([C@@H](C)N(Cc3cccnc3)C(=O)Cc3ccc(C(F)(F)F)c(F)c3)nc3ccccc3c2=O)cc1 | 10.1016/j.bmcl.2009.07.032 | |||
45486534 | 200772 | None | 0 | Human | Functional | pIC50 | = | 7.1 | 7.1 | - | 1 | ChEMBL | 651 | 9 | 0 | 8 | 6.0 | C[C@H](c1nc2c(C3CC3)nccn2c1-c1ccc(C#N)cc1)N(CC1CCS(=O)(=O)CC1)C(=O)Cc1cccc(OC(F)(F)F)c1 | 10.1016/j.bmcl.2009.07.021 | |||
CHEMBL576099 | 200772 | None | 0 | Human | Functional | pIC50 | = | 7.1 | 7.1 | - | 1 | ChEMBL | 651 | 9 | 0 | 8 | 6.0 | C[C@H](c1nc2c(C3CC3)nccn2c1-c1ccc(C#N)cc1)N(CC1CCS(=O)(=O)CC1)C(=O)Cc1cccc(OC(F)(F)F)c1 | 10.1016/j.bmcl.2009.07.021 | |||
56660101 | 64257 | None | 0 | Rat | Functional | pIC50 | = | 7.1 | 7.1 | -6 | 3 | ChEMBL | 442 | 2 | 2 | 3 | 3.5 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CCOCC1 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1809008 | 64257 | None | 0 | Rat | Functional | pIC50 | = | 7.1 | 7.1 | -6 | 3 | ChEMBL | 442 | 2 | 2 | 3 | 3.5 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CCOCC1 | 10.1016/j.bmcl.2011.06.070 | |||
45482784 | 200455 | None | 0 | Human | Functional | pIC50 | = | 7.1 | 7.1 | - | 1 | ChEMBL | 434 | 4 | 2 | 2 | 4.3 | CCN(CC)C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)NC2CCCCC2)C1 | 10.1016/j.bmcl.2009.09.002 | |||
CHEMBL573728 | 200455 | None | 0 | Human | Functional | pIC50 | = | 7.1 | 7.1 | - | 1 | ChEMBL | 434 | 4 | 2 | 2 | 4.3 | CCN(CC)C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)NC2CCCCC2)C1 | 10.1016/j.bmcl.2009.09.002 | |||
90479960 | 192231 | None | 0 | Human | Functional | pIC50 | = | 7.1 | 7.1 | - | 1 | ChEMBL | 536 | 6 | 0 | 10 | 3.5 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3cnc(OC4CCC4)nc3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL5203452 | 192231 | None | 0 | Human | Functional | pIC50 | = | 7.1 | 7.1 | - | 1 | ChEMBL | 536 | 6 | 0 | 10 | 3.5 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3cnc(OC4CCC4)nc3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00675 | |||
14479864 | 4653 | None | 0 | Human | Functional | pIC50 | = | 6.1 | 6.1 | 13 | 2 | ChEMBL | 440 | 4 | 1 | 3 | 4.0 | O=C1CCC(c2ccccc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C(=O)N1 | 10.1016/j.bmcl.2008.07.115 | |||
CHEMBL10309 | 4653 | None | 0 | Human | Functional | pIC50 | = | 6.1 | 6.1 | 13 | 2 | ChEMBL | 440 | 4 | 1 | 3 | 4.0 | O=C1CCC(c2ccccc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C(=O)N1 | 10.1016/j.bmcl.2008.07.115 | |||
44570180 | 183654 | None | 0 | Human | Functional | pIC50 | = | 7.1 | 7.1 | 6 | 2 | ChEMBL | 477 | 4 | 0 | 5 | 3.5 | C[C@H]1CN(S(=O)(=O)C[C@]23CC[C@H](CC2=O)C3(C)C)CCN1c1ncc(C(F)(F)F)cc1F | 10.1016/j.bmcl.2008.11.008 | |||
CHEMBL480016 | 183654 | None | 0 | Human | Functional | pIC50 | = | 7.1 | 7.1 | 6 | 2 | ChEMBL | 477 | 4 | 0 | 5 | 3.5 | C[C@H]1CN(S(=O)(=O)C[C@]23CC[C@H](CC2=O)C3(C)C)CCN1c1ncc(C(F)(F)F)cc1F | 10.1016/j.bmcl.2008.11.008 | |||
44580796 | 187875 | None | 0 | Human | Functional | pIC50 | = | 6.1 | 6.1 | - | 1 | ChEMBL | 553 | 5 | 1 | 5 | 3.5 | O=C1CCC(c2cccc(C(=O)N3CCOCC3)c2)(C2CCN(Cc3ccc(Br)cc3)CC2)C(=O)N1 | 10.1016/j.bmcl.2008.07.115 | |||
CHEMBL495728 | 187875 | None | 0 | Human | Functional | pIC50 | = | 6.1 | 6.1 | - | 1 | ChEMBL | 553 | 5 | 1 | 5 | 3.5 | O=C1CCC(c2cccc(C(=O)N3CCOCC3)c2)(C2CCN(Cc3ccc(Br)cc3)CC2)C(=O)N1 | 10.1016/j.bmcl.2008.07.115 | |||
44570178 | 183509 | None | 0 | Human | Functional | pIC50 | = | 6.1 | 6.1 | - | 1 | ChEMBL | 517 | 6 | 2 | 5 | 3.1 | CCNC(=O)NC1C[C@H]2CC[C@]1(CS(=O)(=O)N1CCN(c3ccc(C(F)(F)F)cn3)CC1)C2(C)C | 10.1016/j.bmcl.2008.11.008 | |||
CHEMBL479824 | 183509 | None | 0 | Human | Functional | pIC50 | = | 6.1 | 6.1 | - | 1 | ChEMBL | 517 | 6 | 2 | 5 | 3.1 | CCNC(=O)NC1C[C@H]2CC[C@]1(CS(=O)(=O)N1CCN(c3ccc(C(F)(F)F)cn3)CC1)C2(C)C | 10.1016/j.bmcl.2008.11.008 | |||
24947459 | 184144 | None | 0 | Human | Functional | pIC50 | = | 6.1 | 6.1 | - | 1 | ChEMBL | 431 | 4 | 0 | 4 | 3.8 | CC1(C)[C@H]2CC[C@]1(CS(=O)(=O)N1CCN(c3ccc(C(F)(F)F)cn3)CC1)CC2 | 10.1016/j.bmcl.2008.11.008 | |||
CHEMBL482174 | 184144 | None | 0 | Human | Functional | pIC50 | = | 6.1 | 6.1 | - | 1 | ChEMBL | 431 | 4 | 0 | 4 | 3.8 | CC1(C)[C@H]2CC[C@]1(CS(=O)(=O)N1CCN(c3ccc(C(F)(F)F)cn3)CC1)CC2 | 10.1016/j.bmcl.2008.11.008 | |||
44570140 | 184179 | None | 0 | Human | Functional | pIC50 | = | 6.1 | 6.1 | - | 1 | ChEMBL | 446 | 4 | 1 | 5 | 2.7 | CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCN(c3ccc(C(F)(F)F)cn3)CC1)C(N)C2 | 10.1016/j.bmcl.2008.11.008 | |||
CHEMBL482369 | 184179 | None | 0 | Human | Functional | pIC50 | = | 6.1 | 6.1 | - | 1 | ChEMBL | 446 | 4 | 1 | 5 | 2.7 | CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCN(c3ccc(C(F)(F)F)cn3)CC1)C(N)C2 | 10.1016/j.bmcl.2008.11.008 | |||
44569943 | 190284 | None | 0 | Human | Functional | pIC50 | = | 6.1 | 6.1 | - | 1 | ChEMBL | 449 | 4 | 0 | 4 | 3.7 | CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCN(c3ccc(C(F)(F)F)cn3)CC1)C(F)C2 | 10.1016/j.bmcl.2008.11.008 | |||
CHEMBL517402 | 190284 | None | 0 | Human | Functional | pIC50 | = | 6.1 | 6.1 | - | 1 | ChEMBL | 449 | 4 | 0 | 4 | 3.7 | CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCN(c3ccc(C(F)(F)F)cn3)CC1)C(F)C2 | 10.1016/j.bmcl.2008.11.008 | |||
44570385 | 183171 | None | 0 | Mouse | Functional | pIC50 | = | 6.1 | 6.1 | -5 | 2 | ChEMBL | 463 | 4 | 0 | 5 | 3.1 | CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCN(c3ncc(C(F)(F)F)cc3F)CC1)C(=O)C2 | 10.1016/j.bmcl.2008.11.008 | |||
CHEMBL479426 | 183171 | None | 0 | Mouse | Functional | pIC50 | = | 6.1 | 6.1 | -5 | 2 | ChEMBL | 463 | 4 | 0 | 5 | 3.1 | CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCN(c3ncc(C(F)(F)F)cc3F)CC1)C(=O)C2 | 10.1016/j.bmcl.2008.11.008 | |||
44570179 | 190271 | None | 0 | Human | Functional | pIC50 | = | 5.1 | 5.1 | - | 1 | ChEMBL | 474 | 6 | 1 | 5 | 3.4 | CCNC1C[C@H]2CC[C@]1(CS(=O)(=O)N1CCN(c3ccc(C(F)(F)F)cn3)CC1)C2(C)C | 10.1016/j.bmcl.2008.11.008 | |||
CHEMBL517386 | 190271 | None | 0 | Human | Functional | pIC50 | = | 5.1 | 5.1 | - | 1 | ChEMBL | 474 | 6 | 1 | 5 | 3.4 | CCNC1C[C@H]2CC[C@]1(CS(=O)(=O)N1CCN(c3ccc(C(F)(F)F)cn3)CC1)C2(C)C | 10.1016/j.bmcl.2008.11.008 | |||
53322974 | 58197 | None | 0 | Human | Functional | pIC50 | = | 5.1 | 5.1 | - | 1 | ChEMBL | 442 | 5 | 1 | 6 | 2.7 | CNC(=O)c1cnc(N2CCN(C3CCN(Cc4ccccn4)CC3)[C@@H](C)C2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
CHEMBL1681838 | 58197 | None | 0 | Human | Functional | pIC50 | = | 5.1 | 5.1 | - | 1 | ChEMBL | 442 | 5 | 1 | 6 | 2.7 | CNC(=O)c1cnc(N2CCN(C3CCN(Cc4ccccn4)CC3)[C@@H](C)C2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
24957182 | 153602 | None | 39 | Human | Functional | pIC50 | = | 8.1 | 8.1 | 63 | 2 | ChEMBL | 603 | 10 | 0 | 8 | 5.8 | CCOc1ccc(-n2c([C@@H](C)N(Cc3cccnc3)C(=O)Cc3ccc(OC(F)(F)F)cc3)nc3ncccc3c2=O)cc1 | 10.1016/j.bmcl.2007.11.060 | |||
CHEMBL397983 | 153602 | None | 39 | Human | Functional | pIC50 | = | 8.1 | 8.1 | 63 | 2 | ChEMBL | 603 | 10 | 0 | 8 | 5.8 | CCOc1ccc(-n2c([C@@H](C)N(Cc3cccnc3)C(=O)Cc3ccc(OC(F)(F)F)cc3)nc3ncccc3c2=O)cc1 | 10.1016/j.bmcl.2007.11.060 | |||
53322508 | 58222 | None | 0 | Human | Functional | pIC50 | = | 8.1 | 8.1 | - | 1 | ChEMBL | 475 | 5 | 1 | 5 | 4.5 | CC(=O)Nc1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4)CC3)[C@@H](C)C2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
CHEMBL1681865 | 58222 | None | 0 | Human | Functional | pIC50 | = | 8.1 | 8.1 | - | 1 | ChEMBL | 475 | 5 | 1 | 5 | 4.5 | CC(=O)Nc1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4)CC3)[C@@H](C)C2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
11964007 | 64248 | None | 0 | Human | Functional | pIC50 | = | 8.1 | 8.1 | -1 | 2 | ChEMBL | 412 | 2 | 2 | 2 | 3.9 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CCC1 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1808999 | 64248 | None | 0 | Human | Functional | pIC50 | = | 8.1 | 8.1 | -1 | 2 | ChEMBL | 412 | 2 | 2 | 2 | 3.9 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CCC1 | 10.1016/j.bmcl.2011.06.070 | |||
56677273 | 64273 | None | 0 | Human | Functional | pIC50 | = | 8.1 | 8.1 | -1 | 2 | ChEMBL | 432 | 2 | 2 | 3 | 4.3 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2cccs2)C1)N1CCCC1 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1809025 | 64273 | None | 0 | Human | Functional | pIC50 | = | 8.1 | 8.1 | -1 | 2 | ChEMBL | 432 | 2 | 2 | 3 | 4.3 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2cccs2)C1)N1CCCC1 | 10.1016/j.bmcl.2011.06.070 | |||
56663563 | 64288 | None | 0 | Human | Functional | pIC50 | = | 8.1 | 8.1 | -2 | 3 | ChEMBL | 539 | 5 | 1 | 5 | 4.1 | O=C([C@@H]1C=C2c3cccc4c3c(cn4CCN3CCOCC3)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CCCC1 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1809043 | 64288 | None | 0 | Human | Functional | pIC50 | = | 8.1 | 8.1 | -2 | 3 | ChEMBL | 539 | 5 | 1 | 5 | 4.1 | O=C([C@@H]1C=C2c3cccc4c3c(cn4CCN3CCOCC3)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CCCC1 | 10.1016/j.bmcl.2011.06.070 | |||
56670448 | 64260 | None | 0 | Mouse | Functional | pIC50 | = | 8.1 | 8.1 | 3 | 3 | ChEMBL | 456 | 2 | 3 | 3 | 3.6 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CCC(O)CC1 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1809011 | 64260 | None | 0 | Mouse | Functional | pIC50 | = | 8.1 | 8.1 | 3 | 3 | ChEMBL | 456 | 2 | 3 | 3 | 3.6 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CCC(O)CC1 | 10.1016/j.bmcl.2011.06.070 | |||
24957182 | 153602 | None | 39 | Human | Functional | pIC50 | = | 8.1 | 8.1 | 63 | 2 | ChEMBL | 603 | 10 | 0 | 8 | 5.8 | CCOc1ccc(-n2c([C@@H](C)N(Cc3cccnc3)C(=O)Cc3ccc(OC(F)(F)F)cc3)nc3ncccc3c2=O)cc1 | 10.1016/j.bmcl.2007.03.106 | |||
CHEMBL397983 | 153602 | None | 39 | Human | Functional | pIC50 | = | 8.1 | 8.1 | 63 | 2 | ChEMBL | 603 | 10 | 0 | 8 | 5.8 | CCOc1ccc(-n2c([C@@H](C)N(Cc3cccnc3)C(=O)Cc3ccc(OC(F)(F)F)cc3)nc3ncccc3c2=O)cc1 | 10.1016/j.bmcl.2007.03.106 | |||
168283702 | 190875 | None | 0 | Human | Functional | pIC50 | = | 8.1 | 8.1 | - | 1 | ChEMBL | 522 | 4 | 0 | 9 | 3.9 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3cnc(C(C)(C)C)nc3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL5183171 | 190875 | None | 0 | Human | Functional | pIC50 | = | 8.1 | 8.1 | - | 1 | ChEMBL | 522 | 4 | 0 | 9 | 3.9 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3cnc(C(C)(C)C)nc3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00675 | |||
90480413 | 192543 | None | 0 | Human | Functional | pIC50 | = | 8.1 | 8.1 | - | 1 | ChEMBL | 509 | 6 | 0 | 9 | 3.6 | CCOc1ccc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3nc(C)nc3C)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL5208280 | 192543 | None | 0 | Human | Functional | pIC50 | = | 8.1 | 8.1 | - | 1 | ChEMBL | 509 | 6 | 0 | 9 | 3.6 | CCOc1ccc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3nc(C)nc3C)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
46883305 | 5666 | None | 0 | Human | Functional | pIC50 | = | 7.1 | 7.1 | - | 1 | ChEMBL | 639 | 10 | 0 | 7 | 6.3 | CCOc1ccc(-n2c([C@@H](C)N(C[C@@H]3CCCN3C(C)C)C(=O)Cc3ccc(F)c(C(F)(F)F)c3)nc3ncccc3c2=O)cc1 | 10.1016/j.bmcl.2009.07.032 | |||
CHEMBL1077825 | 5666 | None | 0 | Human | Functional | pIC50 | = | 7.1 | 7.1 | - | 1 | ChEMBL | 639 | 10 | 0 | 7 | 6.3 | CCOc1ccc(-n2c([C@@H](C)N(C[C@@H]3CCCN3C(C)C)C(=O)Cc3ccc(F)c(C(F)(F)F)c3)nc3ncccc3c2=O)cc1 | 10.1016/j.bmcl.2009.07.032 | |||
53325133 | 58220 | None | 0 | Human | Functional | pIC50 | = | 7.1 | 7.1 | - | 1 | ChEMBL | 460 | 5 | 2 | 5 | 3.8 | C[C@H]1CN(c2ncc(C(=N)N)cc2Cl)CCN1C1CCN(Cc2ccc(Cl)cc2)CC1 | 10.1016/j.bmcl.2010.12.114 | |||
CHEMBL1681863 | 58220 | None | 0 | Human | Functional | pIC50 | = | 7.1 | 7.1 | - | 1 | ChEMBL | 460 | 5 | 2 | 5 | 3.8 | C[C@H]1CN(c2ncc(C(=N)N)cc2Cl)CCN1C1CCN(Cc2ccc(Cl)cc2)CC1 | 10.1016/j.bmcl.2010.12.114 | |||
24739886 | 187975 | None | 0 | Human | Functional | pIC50 | = | 7.1 | 7.1 | 12 | 4 | ChEMBL | 469 | 6 | 1 | 3 | 4.2 | NC(=O)CN1CCCC(c2ccccc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C1 | 10.1016/j.bmcl.2008.07.115 | |||
CHEMBL496376 | 187975 | None | 0 | Human | Functional | pIC50 | = | 7.1 | 7.1 | 12 | 4 | ChEMBL | 469 | 6 | 1 | 3 | 4.2 | NC(=O)CN1CCCC(c2ccccc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C1 | 10.1016/j.bmcl.2008.07.115 | |||
25008271 | 95311 | None | 0 | Human | Functional | pIC50 | = | 7.1 | 7.1 | - | 1 | ChEMBL | 313 | 3 | 1 | 4 | 3.3 | Cc1cccc2c1n(C)c(=N)n2CC(=O)c1ccc(Cl)cc1 | 10.1016/j.bmcl.2008.01.074 | |||
CHEMBL256226 | 95311 | None | 0 | Human | Functional | pIC50 | = | 7.1 | 7.1 | - | 1 | ChEMBL | 313 | 3 | 1 | 4 | 3.3 | Cc1cccc2c1n(C)c(=N)n2CC(=O)c1ccc(Cl)cc1 | 10.1016/j.bmcl.2008.01.074 | |||
15604773 | 72630 | None | 0 | Human | Functional | pIC50 | = | 7.1 | 7.1 | - | 1 | ChEMBL | 606 | 8 | 3 | 5 | 5.3 | CCNC(=O)N1CCCN(c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2NC(=O)c2cccc(C#N)c2)CC1 | 10.1016/j.bmcl.2005.09.020 | |||
CHEMBL199370 | 72630 | None | 0 | Human | Functional | pIC50 | = | 7.1 | 7.1 | - | 1 | ChEMBL | 606 | 8 | 3 | 5 | 5.3 | CCNC(=O)N1CCCN(c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2NC(=O)c2cccc(C#N)c2)CC1 | 10.1016/j.bmcl.2005.09.020 | |||
44453296 | 155365 | None | 0 | Human | Functional | pIC50 | = | 6.1 | 6.1 | - | 1 | ChEMBL | 460 | 8 | 1 | 5 | 4.2 | CN(CCn1c(=N)n(CC(=O)c2ccc(Cl)cc2)c2ccccc21)C(=O)Cc1ccccc1 | 10.1016/j.bmcl.2008.02.049 | |||
CHEMBL402855 | 155365 | None | 0 | Human | Functional | pIC50 | = | 6.1 | 6.1 | - | 1 | ChEMBL | 460 | 8 | 1 | 5 | 4.2 | CN(CCn1c(=N)n(CC(=O)c2ccc(Cl)cc2)c2ccccc21)C(=O)Cc1ccccc1 | 10.1016/j.bmcl.2008.02.049 | |||
15604690 | 135298 | None | 0 | Human | Functional | pIC50 | = | 6.1 | 6.1 | - | 1 | ChEMBL | 601 | 7 | 3 | 4 | 5.7 | CNC(=O)N1CCCN(c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2NC(=O)c2cccc(Cl)c2)CC1 | 10.1016/j.bmcl.2005.09.020 | |||
CHEMBL372403 | 135298 | None | 0 | Human | Functional | pIC50 | = | 6.1 | 6.1 | - | 1 | ChEMBL | 601 | 7 | 3 | 4 | 5.7 | CNC(=O)N1CCCN(c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2NC(=O)c2cccc(Cl)c2)CC1 | 10.1016/j.bmcl.2005.09.020 | |||
71680142 | 143133 | None | 0 | Human | Functional | pIC50 | = | 5.1 | 5.1 | - | 1 | ChEMBL | 458 | 4 | 1 | 8 | 3.2 | C[C@H]1CN(c2scnc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL3894991 | 143133 | None | 0 | Human | Functional | pIC50 | = | 5.1 | 5.1 | - | 1 | ChEMBL | 458 | 4 | 1 | 8 | 3.2 | C[C@H]1CN(c2scnc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | 10.1021/acs.jmedchem.2c00675 | |||
117740323 | 152487 | None | 0 | Human | Functional | pIC50 | = | 6.1 | 6.1 | - | 1 | ChEMBL | 500 | 4 | 1 | 6 | 4.7 | Cc1ccc(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccccc4[nH]3)C[C@H]2C)cn1 | 10.1021/acs.jmedchem.2c00676 | |||
CHEMBL3970456 | 152487 | None | 0 | Human | Functional | pIC50 | = | 6.1 | 6.1 | - | 1 | ChEMBL | 500 | 4 | 1 | 6 | 4.7 | Cc1ccc(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccccc4[nH]3)C[C@H]2C)cn1 | 10.1021/acs.jmedchem.2c00676 | |||
53322461 | 58198 | None | 0 | Human | Functional | pIC50 | = | 5.1 | 5.1 | - | 1 | ChEMBL | 430 | 5 | 2 | 5 | 2.6 | CNC(=O)c1cnc(N2CCN(C3CCN(Cc4ccc[nH]4)CC3)[C@@H](C)C2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
CHEMBL1681839 | 58198 | None | 0 | Human | Functional | pIC50 | = | 5.1 | 5.1 | - | 1 | ChEMBL | 430 | 5 | 2 | 5 | 2.6 | CNC(=O)c1cnc(N2CCN(C3CCN(Cc4ccc[nH]4)CC3)[C@@H](C)C2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
45482796 | 200398 | None | 0 | Human | Functional | pIC50 | = | 6.1 | 6.1 | - | 1 | ChEMBL | 429 | 4 | 1 | 3 | 4.5 | CCN(CC)C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Oc2ccccc2)C1 | 10.1016/j.bmcl.2009.09.002 | |||
CHEMBL573242 | 200398 | None | 0 | Human | Functional | pIC50 | = | 6.1 | 6.1 | - | 1 | ChEMBL | 429 | 4 | 1 | 3 | 4.5 | CCN(CC)C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Oc2ccccc2)C1 | 10.1016/j.bmcl.2009.09.002 | |||
56673941 | 64274 | None | 0 | Mouse | Functional | pIC50 | = | 7.1 | 7.1 | 1 | 2 | ChEMBL | 418 | 2 | 2 | 2 | 3.7 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)NC2CCCC2)C1)N1CCCC1 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1809027 | 64274 | None | 0 | Mouse | Functional | pIC50 | = | 7.1 | 7.1 | 1 | 2 | ChEMBL | 418 | 2 | 2 | 2 | 3.7 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)NC2CCCC2)C1)N1CCCC1 | 10.1016/j.bmcl.2011.06.070 | |||
24739886 | 187975 | None | 0 | Human | Functional | pIC50 | = | 6.1 | 6.1 | 12 | 4 | ChEMBL | 469 | 6 | 1 | 3 | 4.2 | NC(=O)CN1CCCC(c2ccccc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C1 | 10.1016/j.bmcl.2008.07.115 | |||
CHEMBL496376 | 187975 | None | 0 | Human | Functional | pIC50 | = | 6.1 | 6.1 | 12 | 4 | ChEMBL | 469 | 6 | 1 | 3 | 4.2 | NC(=O)CN1CCCC(c2ccccc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C1 | 10.1016/j.bmcl.2008.07.115 | |||
53317216 | 58201 | None | 0 | Human | Functional | pIC50 | = | 5.1 | 5.1 | - | 1 | ChEMBL | 431 | 5 | 1 | 6 | 2.9 | CNC(=O)c1cnc(N2CCN(C3CCN(Cc4ccco4)CC3)[C@@H](C)C2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
CHEMBL1681842 | 58201 | None | 0 | Human | Functional | pIC50 | = | 5.1 | 5.1 | - | 1 | ChEMBL | 431 | 5 | 1 | 6 | 2.9 | CNC(=O)c1cnc(N2CCN(C3CCN(Cc4ccco4)CC3)[C@@H](C)C2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
168272582 | 190470 | None | 0 | Human | Functional | pIC50 | = | 6.1 | 6.1 | - | 1 | ChEMBL | 481 | 6 | 0 | 9 | 3.0 | CCOc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3cccn3)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL5177069 | 190470 | None | 0 | Human | Functional | pIC50 | = | 6.1 | 6.1 | - | 1 | ChEMBL | 481 | 6 | 0 | 9 | 3.0 | CCOc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3cccn3)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
53317663 | 58221 | None | 0 | Human | Functional | pIC50 | = | 7.1 | 7.1 | - | 1 | ChEMBL | 488 | 6 | 2 | 5 | 4.5 | CCNC(=N)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4)CC3)[C@@H](C)C2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
CHEMBL1681864 | 58221 | None | 0 | Human | Functional | pIC50 | = | 7.1 | 7.1 | - | 1 | ChEMBL | 488 | 6 | 2 | 5 | 4.5 | CCNC(=N)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4)CC3)[C@@H](C)C2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
56673938 | 64255 | None | 0 | Human | Functional | pIC50 | = | 7.1 | 7.1 | 1 | 2 | ChEMBL | 455 | 2 | 2 | 3 | 3.4 | CN1CCN(C(=O)[C@@H]2C=C3c4cccc5[nH]cc(c45)C[C@H]3N(C(=O)Nc3ccccc3)C2)CC1 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1809006 | 64255 | None | 0 | Human | Functional | pIC50 | = | 7.1 | 7.1 | 1 | 2 | ChEMBL | 455 | 2 | 2 | 3 | 3.4 | CN1CCN(C(=O)[C@@H]2C=C3c4cccc5[nH]cc(c45)C[C@H]3N(C(=O)Nc3ccccc3)C2)CC1 | 10.1016/j.bmcl.2011.06.070 | |||
53318914 | 58233 | None | 0 | Human | Functional | pIC50 | = | 6.1 | 6.1 | - | 1 | ChEMBL | 537 | 6 | 1 | 5 | 5.3 | CNC(=O)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4)CC3)[C@@H](c3ccccc3)C2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
CHEMBL1681876 | 58233 | None | 0 | Human | Functional | pIC50 | = | 6.1 | 6.1 | - | 1 | ChEMBL | 537 | 6 | 1 | 5 | 5.3 | CNC(=O)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4)CC3)[C@@H](c3ccccc3)C2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
14479861 | 4336 | None | 0 | Human | Functional | pIC50 | = | 6.1 | 6.1 | - | 1 | ChEMBL | 396 | 4 | 1 | 3 | 3.9 | O=C1CCC(c2ccccc2)(C2CCN(Cc3ccc(Cl)cc3)CC2)C(=O)N1 | 10.1016/j.bmcl.2008.07.115 | |||
CHEMBL10097 | 4336 | None | 0 | Human | Functional | pIC50 | = | 6.1 | 6.1 | - | 1 | ChEMBL | 396 | 4 | 1 | 3 | 3.9 | O=C1CCC(c2ccccc2)(C2CCN(Cc3ccc(Cl)cc3)CC2)C(=O)N1 | 10.1016/j.bmcl.2008.07.115 | |||
71679630 | 146051 | None | 0 | Human | Functional | pIC50 | = | 6.1 | 6.1 | - | 1 | ChEMBL | 458 | 4 | 1 | 8 | 3.2 | C[C@@H]1CN(c2scnc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL3918205 | 146051 | None | 0 | Human | Functional | pIC50 | = | 6.1 | 6.1 | - | 1 | ChEMBL | 458 | 4 | 1 | 8 | 3.2 | C[C@@H]1CN(c2scnc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | 10.1021/acs.jmedchem.2c00675 | |||
53322504 | 58205 | None | 0 | Mouse | Functional | pIC50 | = | 7.1 | 7.1 | -2 | 3 | ChEMBL | 573 | 7 | 1 | 5 | 5.4 | O=C(NCc1ccc(F)c(F)c1)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4)CC3)CC2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
CHEMBL1681848 | 58205 | None | 0 | Mouse | Functional | pIC50 | = | 7.1 | 7.1 | -2 | 3 | ChEMBL | 573 | 7 | 1 | 5 | 5.4 | O=C(NCc1ccc(F)c(F)c1)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4)CC3)CC2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
89725952 | 145568 | None | 0 | Human | Functional | pIC50 | = | 7.1 | 7.1 | - | 1 | ChEMBL | 601 | 5 | 1 | 9 | 4.5 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccc(C5CCN(C)CC5)cc4[nH]3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00676 | |||
CHEMBL3914555 | 145568 | None | 0 | Human | Functional | pIC50 | = | 7.1 | 7.1 | - | 1 | ChEMBL | 601 | 5 | 1 | 9 | 4.5 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccc(C5CCN(C)CC5)cc4[nH]3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00676 | |||
46891183 | 6950 | None | 0 | Human | Functional | pIC50 | = | 7.1 | 7.1 | - | 1 | ChEMBL | 539 | 9 | 1 | 4 | 5.7 | O=C(NCc1cccc(Cl)c1)c1ccc(CN(Cc2ccccn2)S(=O)(=O)c2ccc(Cl)cc2)cc1 | 10.1016/j.bmcl.2010.04.113 | |||
CHEMBL1084506 | 6950 | None | 0 | Human | Functional | pIC50 | = | 7.1 | 7.1 | - | 1 | ChEMBL | 539 | 9 | 1 | 4 | 5.7 | O=C(NCc1cccc(Cl)c1)c1ccc(CN(Cc2ccccn2)S(=O)(=O)c2ccc(Cl)cc2)cc1 | 10.1016/j.bmcl.2010.04.113 | |||
45484739 | 199754 | None | 0 | Human | Functional | pIC50 | = | 7.1 | 7.1 | - | 1 | ChEMBL | 558 | 9 | 1 | 7 | 4.2 | N#Cc1ccc(CN2CCC(N3CCN(c4ncc(C(=O)NCCOc5ccccc5)cc4Cl)CC3)CC2)cc1 | 10.1016/j.bmcl.2009.07.020 | |||
CHEMBL568676 | 199754 | None | 0 | Human | Functional | pIC50 | = | 7.1 | 7.1 | - | 1 | ChEMBL | 558 | 9 | 1 | 7 | 4.2 | N#Cc1ccc(CN2CCC(N3CCN(c4ncc(C(=O)NCCOc5ccccc5)cc4Cl)CC3)CC2)cc1 | 10.1016/j.bmcl.2009.07.020 | |||
89725785 | 143189 | None | 0 | Human | Functional | pIC50 | = | 6.1 | 6.1 | - | 1 | ChEMBL | 486 | 5 | 1 | 8 | 3.7 | CCc1nc(-c2nc3ccccc3[nH]2)c(N2CCN(C(=O)Cn3cnc4cccnc43)[C@H](C)C2)s1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL3895485 | 143189 | None | 0 | Human | Functional | pIC50 | = | 6.1 | 6.1 | - | 1 | ChEMBL | 486 | 5 | 1 | 8 | 3.7 | CCc1nc(-c2nc3ccccc3[nH]2)c(N2CCN(C(=O)Cn3cnc4cccnc43)[C@H](C)C2)s1 | 10.1021/acs.jmedchem.2c00675 | |||
53326389 | 58196 | None | 0 | Human | Functional | pIC50 | = | 7.1 | 7.1 | - | 1 | ChEMBL | 455 | 5 | 1 | 5 | 3.6 | CNC(=O)c1cnc(N2CCN(C3CCN(Cc4ccc(C)cc4)CC3)[C@@H](C)C2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
CHEMBL1681836 | 58196 | None | 0 | Human | Functional | pIC50 | = | 7.1 | 7.1 | - | 1 | ChEMBL | 455 | 5 | 1 | 5 | 3.6 | CNC(=O)c1cnc(N2CCN(C3CCN(Cc4ccc(C)cc4)CC3)[C@@H](C)C2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
168281055 | 191110 | None | 0 | Human | Functional | pIC50 | = | 7.1 | 7.1 | - | 1 | ChEMBL | 509 | 6 | 0 | 9 | 3.6 | CCOc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3nc(C)cc3C)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL5186627 | 191110 | None | 0 | Human | Functional | pIC50 | = | 7.1 | 7.1 | - | 1 | ChEMBL | 509 | 6 | 0 | 9 | 3.6 | CCOc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3nc(C)cc3C)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
44447094 | 94753 | None | 0 | Human | Functional | pIC50 | = | 7.1 | 7.1 | - | 1 | ChEMBL | 633 | 9 | 0 | 8 | 4.2 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc2c(c(=O)n1-c1ccc(C#N)cc1)CCCN2C | 10.1016/j.bmcl.2007.11.060 | |||
CHEMBL252820 | 94753 | None | 0 | Human | Functional | pIC50 | = | 7.1 | 7.1 | - | 1 | ChEMBL | 633 | 9 | 0 | 8 | 4.2 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc2c(c(=O)n1-c1ccc(C#N)cc1)CCCN2C | 10.1016/j.bmcl.2007.11.060 | |||
46891371 | 7430 | None | 0 | Human | Functional | pIC50 | = | 6.1 | 6.1 | - | 1 | ChEMBL | 473 | 7 | 1 | 5 | 4.6 | O=S(=O)(c1ccc(Cl)cc1)N(Cc1ccc(Cl)cc1)Cc1ccc(-c2nnn[nH]2)cc1 | 10.1016/j.bmcl.2010.04.113 | |||
CHEMBL1086590 | 7430 | None | 0 | Human | Functional | pIC50 | = | 6.1 | 6.1 | - | 1 | ChEMBL | 473 | 7 | 1 | 5 | 4.6 | O=S(=O)(c1ccc(Cl)cc1)N(Cc1ccc(Cl)cc1)Cc1ccc(-c2nnn[nH]2)cc1 | 10.1016/j.bmcl.2010.04.113 | |||
44253592 | 6880 | None | 0 | Human | Functional | pIC50 | = | 6.1 | 6.1 | - | 1 | ChEMBL | 469 | 8 | 1 | 6 | 3.9 | COc1ccc(CN(Cc2ccc(-c3nnn[nH]3)cc2)S(=O)(=O)c2ccc(Cl)cc2)cc1 | 10.1016/j.bmcl.2010.04.113 | |||
CHEMBL1084199 | 6880 | None | 0 | Human | Functional | pIC50 | = | 6.1 | 6.1 | - | 1 | ChEMBL | 469 | 8 | 1 | 6 | 3.9 | COc1ccc(CN(Cc2ccc(-c3nnn[nH]3)cc2)S(=O)(=O)c2ccc(Cl)cc2)cc1 | 10.1016/j.bmcl.2010.04.113 | |||
56677272 | 64269 | None | 0 | Human | Functional | pIC50 | = | 7.1 | 7.1 | - | 1 | ChEMBL | 456 | 3 | 2 | 3 | 4.3 | COc1ccc(NC(=O)N2C[C@H](C(=O)N3CCCC3)C=C3c4cccc5[nH]cc(c45)C[C@H]32)cc1 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1809020 | 64269 | None | 0 | Human | Functional | pIC50 | = | 7.1 | 7.1 | - | 1 | ChEMBL | 456 | 3 | 2 | 3 | 4.3 | COc1ccc(NC(=O)N2C[C@H](C(=O)N3CCCC3)C=C3c4cccc5[nH]cc(c45)C[C@H]32)cc1 | 10.1016/j.bmcl.2011.06.070 | |||
44406244 | 140968 | None | 0 | Human | Functional | pIC50 | = | 6.1 | 6.1 | - | 1 | ChEMBL | 615 | 7 | 2 | 4 | 6.1 | CN(C)C(=O)N1CCCN(c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2NC(=O)c2cccc(Cl)c2)CC1 | 10.1016/j.bmcl.2005.09.020 | |||
CHEMBL382000 | 140968 | None | 0 | Human | Functional | pIC50 | = | 6.1 | 6.1 | - | 1 | ChEMBL | 615 | 7 | 2 | 4 | 6.1 | CN(C)C(=O)N1CCCN(c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2NC(=O)c2cccc(Cl)c2)CC1 | 10.1016/j.bmcl.2005.09.020 | |||
53318563 | 58237 | None | 0 | Human | Functional | pIC50 | = | 5.1 | 5.1 | - | 1 | ChEMBL | 534 | 7 | 2 | 8 | 2.6 | CNOC(=O)C1CN(c2ncc(C(=O)NC)cc2Cl)CCN1C1CCN(Cc2ccc(Cl)cc2)CC1 | 10.1016/j.bmcl.2010.12.114 | |||
CHEMBL1681881 | 58237 | None | 0 | Human | Functional | pIC50 | = | 5.1 | 5.1 | - | 1 | ChEMBL | 534 | 7 | 2 | 8 | 2.6 | CNOC(=O)C1CN(c2ncc(C(=O)NC)cc2Cl)CCN1C1CCN(Cc2ccc(Cl)cc2)CC1 | 10.1016/j.bmcl.2010.12.114 | |||
56660099 | 64247 | None | 0 | Mouse | Functional | pIC50 | = | 8.1 | 8.1 | 3 | 2 | ChEMBL | 430 | 4 | 3 | 3 | 3.1 | CN(CCO)C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1808998 | 64247 | None | 0 | Mouse | Functional | pIC50 | = | 8.1 | 8.1 | 3 | 2 | ChEMBL | 430 | 4 | 3 | 3 | 3.1 | CN(CCO)C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1 | 10.1016/j.bmcl.2011.06.070 | |||
89726154 | 152067 | None | 0 | Human | Functional | pIC50 | = | 8.1 | 8.1 | - | 1 | ChEMBL | 472 | 4 | 1 | 8 | 3.5 | Cc1nc(-c2nc3ccccc3[nH]2)c(N2CCN(C(=O)Cn3cnc4cccnc43)[C@H](C)C2)s1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL3966706 | 152067 | None | 0 | Human | Functional | pIC50 | = | 8.1 | 8.1 | - | 1 | ChEMBL | 472 | 4 | 1 | 8 | 3.5 | Cc1nc(-c2nc3ccccc3[nH]2)c(N2CCN(C(=O)Cn3cnc4cccnc43)[C@H](C)C2)s1 | 10.1021/acs.jmedchem.2c00675 | |||
168286385 | 191844 | None | 0 | Human | Functional | pIC50 | = | 8.0 | 8.0 | - | 1 | ChEMBL | 438 | 4 | 1 | 7 | 2.7 | O=C(Cn1cnc2cccnc21)N1CCN(c2cccnc2-c2nc3ccccc3[nH]2)CC1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL5197253 | 191844 | None | 0 | Human | Functional | pIC50 | = | 8.0 | 8.0 | - | 1 | ChEMBL | 438 | 4 | 1 | 7 | 2.7 | O=C(Cn1cnc2cccnc21)N1CCN(c2cccnc2-c2nc3ccccc3[nH]2)CC1 | 10.1021/acs.jmedchem.2c00675 | |||
168271575 | 190303 | None | 0 | Human | Functional | pIC50 | = | 8.0 | 8.0 | - | 1 | ChEMBL | 580 | 5 | 2 | 9 | 4.0 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccc(C(C)(C)O)c(F)c4[nH]3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00676 | |||
CHEMBL5174313 | 190303 | None | 0 | Human | Functional | pIC50 | = | 8.0 | 8.0 | - | 1 | ChEMBL | 580 | 5 | 2 | 9 | 4.0 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccc(C(C)(C)O)c(F)c4[nH]3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00676 | |||
71678461 | 146148 | None | 0 | Human | Functional | pIC50 | = | 8.0 | 8.0 | - | 1 | ChEMBL | 498 | 5 | 1 | 8 | 4.0 | C[C@@H]1CN(c2sc(C3CC3)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL3919018 | 146148 | None | 0 | Human | Functional | pIC50 | = | 8.0 | 8.0 | - | 1 | ChEMBL | 498 | 5 | 1 | 8 | 4.0 | C[C@@H]1CN(c2sc(C3CC3)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | 10.1021/acs.jmedchem.2c00675 | |||
53318560 | 58206 | None | 0 | Rat | Functional | pIC50 | = | 8 | 8.0 | -1 | 3 | ChEMBL | 587 | 7 | 1 | 5 | 5.8 | C[C@H]1CN(c2ncc(C(=O)NCc3ccc(F)c(F)c3)cc2Cl)CCN1C1CCN(Cc2ccc(Cl)cc2)CC1 | 10.1016/j.bmcl.2010.12.114 | |||
CHEMBL1681849 | 58206 | None | 0 | Rat | Functional | pIC50 | = | 8 | 8.0 | -1 | 3 | ChEMBL | 587 | 7 | 1 | 5 | 5.8 | C[C@H]1CN(c2ncc(C(=O)NCc3ccc(F)c(F)c3)cc2Cl)CCN1C1CCN(Cc2ccc(Cl)cc2)CC1 | 10.1016/j.bmcl.2010.12.114 | |||
44182602 | 70051 | None | 0 | Human | Functional | pIC50 | = | 7.1 | 7.1 | - | 1 | ChEMBL | 634 | 7 | 0 | 7 | 5.0 | C[C@H](c1nc2ncccc2c(=O)n1-c1ccc(F)cc1)N(CC1CCS(=O)(=O)CC1)C(=O)Cc1ccc(C(F)(F)F)c(F)c1 | 10.1016/j.bmcl.2011.10.120 | |||
CHEMBL1939692 | 70051 | None | 0 | Human | Functional | pIC50 | = | 7.1 | 7.1 | - | 1 | ChEMBL | 634 | 7 | 0 | 7 | 5.0 | C[C@H](c1nc2ncccc2c(=O)n1-c1ccc(F)cc1)N(CC1CCS(=O)(=O)CC1)C(=O)Cc1ccc(C(F)(F)F)c(F)c1 | 10.1016/j.bmcl.2011.10.120 | |||
56680588 | 64244 | None | 0 | Mouse | Functional | pIC50 | = | 7.1 | 7.1 | 1 | 2 | ChEMBL | 400 | 3 | 3 | 2 | 3.8 | CCNC(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1808995 | 64244 | None | 0 | Mouse | Functional | pIC50 | = | 7.1 | 7.1 | 1 | 2 | ChEMBL | 400 | 3 | 3 | 2 | 3.8 | CCNC(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1 | 10.1016/j.bmcl.2011.06.070 | |||
53322510 | 58229 | None | 0 | Human | Functional | pIC50 | = | 6.1 | 6.1 | - | 1 | ChEMBL | 529 | 5 | 0 | 5 | 5.2 | C[C@H]1CN(c2ncc(C(=O)N3CCCCC3)cc2Cl)CCN1C1CCN(Cc2ccc(Cl)cc2)CC1 | 10.1016/j.bmcl.2010.12.114 | |||
CHEMBL1681872 | 58229 | None | 0 | Human | Functional | pIC50 | = | 6.1 | 6.1 | - | 1 | ChEMBL | 529 | 5 | 0 | 5 | 5.2 | C[C@H]1CN(c2ncc(C(=O)N3CCCCC3)cc2Cl)CCN1C1CCN(Cc2ccc(Cl)cc2)CC1 | 10.1016/j.bmcl.2010.12.114 | |||
44453322 | 97585 | None | 0 | Human | Functional | pIC50 | = | 6.1 | 6.1 | - | 1 | ChEMBL | 452 | 7 | 1 | 5 | 4.5 | CN(CCn1c(=N)n(CC(=O)c2ccc(Cl)cc2)c2ccccc21)C(=O)C1CCCCC1 | 10.1016/j.bmcl.2008.02.049 | |||
CHEMBL270462 | 97585 | None | 0 | Human | Functional | pIC50 | = | 6.1 | 6.1 | - | 1 | ChEMBL | 452 | 7 | 1 | 5 | 4.5 | CN(CCn1c(=N)n(CC(=O)c2ccc(Cl)cc2)c2ccccc21)C(=O)C1CCCCC1 | 10.1016/j.bmcl.2008.02.049 | |||
703047 | 97922 | None | 6 | Human | Functional | pIC50 | = | 5.1 | 5.1 | - | 1 | ChEMBL | 299 | 3 | 1 | 4 | 3.0 | Cn1c(=N)n(CC(=O)c2ccc(Cl)cc2)c2ccccc21 | 10.1016/j.bmcl.2008.02.049 | |||
CHEMBL272282 | 97922 | None | 6 | Human | Functional | pIC50 | = | 5.1 | 5.1 | - | 1 | ChEMBL | 299 | 3 | 1 | 4 | 3.0 | Cn1c(=N)n(CC(=O)c2ccc(Cl)cc2)c2ccccc21 | 10.1016/j.bmcl.2008.02.049 | |||
703047 | 97922 | None | 6 | Human | Functional | pIC50 | = | 5.1 | 5.1 | - | 1 | ChEMBL | 299 | 3 | 1 | 4 | 3.0 | Cn1c(=N)n(CC(=O)c2ccc(Cl)cc2)c2ccccc21 | 10.1016/j.bmcl.2008.01.074 | |||
CHEMBL272282 | 97922 | None | 6 | Human | Functional | pIC50 | = | 5.1 | 5.1 | - | 1 | ChEMBL | 299 | 3 | 1 | 4 | 3.0 | Cn1c(=N)n(CC(=O)c2ccc(Cl)cc2)c2ccccc21 | 10.1016/j.bmcl.2008.01.074 | |||
53323854 | 58235 | None | 0 | Human | Functional | pIC50 | = | 6.0 | 6.0 | - | 1 | ChEMBL | 491 | 6 | 2 | 6 | 2.9 | CNC(=O)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4)CC3)C(CO)C2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
CHEMBL1681878 | 58235 | None | 0 | Human | Functional | pIC50 | = | 6.0 | 6.0 | - | 1 | ChEMBL | 491 | 6 | 2 | 6 | 2.9 | CNC(=O)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4)CC3)C(CO)C2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
46891476 | 6632 | None | 0 | Human | Functional | pIC50 | = | 6.0 | 6.0 | - | 1 | ChEMBL | 504 | 8 | 1 | 6 | 4.5 | O=S(=O)(c1ccc(Cl)cc1)N(CCc1cc2ccccc2cn1)Cc1ccc(-c2nnn[nH]2)cc1 | 10.1016/j.bmcl.2010.04.113 | |||
CHEMBL1083309 | 6632 | None | 0 | Human | Functional | pIC50 | = | 6.0 | 6.0 | - | 1 | ChEMBL | 504 | 8 | 1 | 6 | 4.5 | O=S(=O)(c1ccc(Cl)cc1)N(CCc1cc2ccccc2cn1)Cc1ccc(-c2nnn[nH]2)cc1 | 10.1016/j.bmcl.2010.04.113 | |||
89726228 | 150040 | None | 0 | Human | Functional | pIC50 | = | 7.0 | 7.0 | - | 1 | ChEMBL | 556 | 5 | 2 | 9 | 3.7 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccc(CO)cc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | 10.1021/acs.jmedchem.2c00676 | |||
CHEMBL3949824 | 150040 | None | 0 | Human | Functional | pIC50 | = | 7.0 | 7.0 | - | 1 | ChEMBL | 556 | 5 | 2 | 9 | 3.7 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccc(CO)cc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | 10.1021/acs.jmedchem.2c00676 | |||
71555361 | 133392 | None | 0 | Human | Functional | pIC50 | = | 6.0 | 6.0 | -478 | 5 | ChEMBL | 564 | 8 | 3 | 10 | 2.4 | Cc1ccc([C@H](Nc2c(Nc3ccc(Cl)c(S(=O)(=O)N4CCN(C)CC4)c3O)c(=O)c2=O)C2(C)COC2)o1 | nan | |||
CHEMBL3704573 | 133392 | None | 0 | Human | Functional | pIC50 | = | 6.0 | 6.0 | -478 | 5 | ChEMBL | 564 | 8 | 3 | 10 | 2.4 | Cc1ccc([C@H](Nc2c(Nc3ccc(Cl)c(S(=O)(=O)N4CCN(C)CC4)c3O)c(=O)c2=O)C2(C)COC2)o1 | nan | |||
168282319 | 191182 | None | 0 | Human | Functional | pIC50 | = | 7.0 | 7.0 | - | 1 | ChEMBL | 549 | 6 | 0 | 9 | 4.0 | CCOc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3ccc(C(F)(F)F)n3)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL5187464 | 191182 | None | 0 | Human | Functional | pIC50 | = | 7.0 | 7.0 | - | 1 | ChEMBL | 549 | 6 | 0 | 9 | 4.0 | CCOc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3ccc(C(F)(F)F)n3)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
44253725 | 6570 | None | 0 | Human | Functional | pIC50 | = | 6.0 | 6.0 | - | 1 | ChEMBL | 502 | 9 | 1 | 3 | 5.5 | O=C(NCC1CC1)c1ccc(CN(Cc2cccc(Cl)c2)S(=O)(=O)c2ccc(Cl)cc2)cc1 | 10.1016/j.bmcl.2010.04.113 | |||
CHEMBL1083024 | 6570 | None | 0 | Human | Functional | pIC50 | = | 6.0 | 6.0 | - | 1 | ChEMBL | 502 | 9 | 1 | 3 | 5.5 | O=C(NCC1CC1)c1ccc(CN(Cc2cccc(Cl)c2)S(=O)(=O)c2ccc(Cl)cc2)cc1 | 10.1016/j.bmcl.2010.04.113 | |||
56673943 | 64277 | None | 0 | Human | Functional | pIC50 | = | 5.0 | 5.0 | - | 1 | ChEMBL | 448 | 2 | 3 | 3 | 3.0 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)NC2CCC(O)CC2)C1)N1CCCC1 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1809030 | 64277 | None | 0 | Human | Functional | pIC50 | = | 5.0 | 5.0 | - | 1 | ChEMBL | 448 | 2 | 3 | 3 | 3.0 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)NC2CCC(O)CC2)C1)N1CCCC1 | 10.1016/j.bmcl.2011.06.070 | |||
168287429 | 191592 | None | 0 | Human | Functional | pIC50 | = | 6.0 | 6.0 | - | 1 | ChEMBL | 582 | 5 | 1 | 10 | 3.1 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccc(S(C)(=O)=O)cc4[nH]3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00676 | |||
CHEMBL5193530 | 191592 | None | 0 | Human | Functional | pIC50 | = | 6.0 | 6.0 | - | 1 | ChEMBL | 582 | 5 | 1 | 10 | 3.1 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccc(S(C)(=O)=O)cc4[nH]3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00676 | |||
53322504 | 58205 | None | 0 | Rat | Functional | pIC50 | = | 7.0 | 7.0 | -2 | 3 | ChEMBL | 573 | 7 | 1 | 5 | 5.4 | O=C(NCc1ccc(F)c(F)c1)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4)CC3)CC2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
CHEMBL1681848 | 58205 | None | 0 | Rat | Functional | pIC50 | = | 7.0 | 7.0 | -2 | 3 | ChEMBL | 573 | 7 | 1 | 5 | 5.4 | O=C(NCc1ccc(F)c(F)c1)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4)CC3)CC2)c(Cl)c1 | 10.1016/j.bmcl.2010.12.114 | |||
44406343 | 73038 | None | 0 | Human | Functional | pIC50 | = | 5.0 | 5.0 | - | 1 | ChEMBL | 602 | 7 | 2 | 5 | 6.2 | COC(=O)N1CCCN(c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2NC(=O)c2cccc(Cl)c2)CC1 | 10.1016/j.bmcl.2005.09.020 | |||
CHEMBL200891 | 73038 | None | 0 | Human | Functional | pIC50 | = | 5.0 | 5.0 | - | 1 | ChEMBL | 602 | 7 | 2 | 5 | 6.2 | COC(=O)N1CCCN(c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2NC(=O)c2cccc(Cl)c2)CC1 | 10.1016/j.bmcl.2005.09.020 | |||
168290539 | 192031 | None | 0 | Human | Functional | pIC50 | = | 7 | 7.0 | - | 1 | ChEMBL | 548 | 6 | 0 | 10 | 3.7 | CCOc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3c(=O)oc4ccccc43)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL5200240 | 192031 | None | 0 | Human | Functional | pIC50 | = | 7 | 7.0 | - | 1 | ChEMBL | 548 | 6 | 0 | 10 | 3.7 | CCOc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3c(=O)oc4ccccc43)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
117739802 | 152013 | None | 0 | Human | Functional | pIC50 | = | 7 | 7.0 | - | 1 | ChEMBL | 586 | 7 | 2 | 10 | 3.6 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3cc(OCCO)ccc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | 10.1021/acs.jmedchem.2c00676 | |||
CHEMBL3966250 | 152013 | None | 0 | Human | Functional | pIC50 | = | 7 | 7.0 | - | 1 | ChEMBL | 586 | 7 | 2 | 10 | 3.6 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3cc(OCCO)ccc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | 10.1021/acs.jmedchem.2c00676 | |||
27307547 | 177710 | None | 0 | Human | Functional | pKd | = | 6.9 | 6.9 | 5 | 2 | ChEMBL | 445 | 4 | 0 | 5 | 2.9 | CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCN(c3ccc(C(F)(F)F)cn3)CC1)C(=O)C2 | 10.1016/j.bmcl.2008.11.008 | |||
CHEMBL464081 | 177710 | None | 0 | Human | Functional | pKd | = | 6.9 | 6.9 | 5 | 2 | ChEMBL | 445 | 4 | 0 | 5 | 2.9 | CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCN(c3ccc(C(F)(F)F)cn3)CC1)C(=O)C2 | 10.1016/j.bmcl.2008.11.008 | |||
25265835 | 177833 | None | 0 | Human | Functional | pKd | = | 7.7 | 7.7 | 6 | 2 | ChEMBL | 479 | 4 | 1 | 5 | 3.3 | C[C@H]1CN(S(=O)(=O)C[C@]23CC[C@H](C[C@@H]2O)C3(C)C)CCN1c1ncc(C(F)(F)F)cc1F | 10.1016/j.bmcl.2008.11.008 | |||
CHEMBL464234 | 177833 | None | 0 | Human | Functional | pKd | = | 7.7 | 7.7 | 6 | 2 | ChEMBL | 479 | 4 | 1 | 5 | 3.3 | C[C@H]1CN(S(=O)(=O)C[C@]23CC[C@H](C[C@@H]2O)C3(C)C)CCN1c1ncc(C(F)(F)F)cc1F | 10.1016/j.bmcl.2008.11.008 | |||
44570180 | 183654 | None | 0 | Human | Functional | pKd | = | 7.6 | 7.6 | 6 | 2 | ChEMBL | 477 | 4 | 0 | 5 | 3.5 | C[C@H]1CN(S(=O)(=O)C[C@]23CC[C@H](CC2=O)C3(C)C)CCN1c1ncc(C(F)(F)F)cc1F | 10.1016/j.bmcl.2008.11.008 | |||
CHEMBL480016 | 183654 | None | 0 | Human | Functional | pKd | = | 7.6 | 7.6 | 6 | 2 | ChEMBL | 477 | 4 | 0 | 5 | 3.5 | C[C@H]1CN(S(=O)(=O)C[C@]23CC[C@H](CC2=O)C3(C)C)CCN1c1ncc(C(F)(F)F)cc1F | 10.1016/j.bmcl.2008.11.008 | |||
44446451 | 94899 | None | 0 | Human | Functional | pKi | = | 8 | 8.0 | - | 0 | ChEMBL | 524 | 4 | 2 | 3 | 5.6 | CC(C)(C)C(=O)N1C2C=C(CN3CCC(NC(=O)Nc4cc(F)cc(C(F)(F)F)c4)CC3)CC1CCC2 | 10.1016/j.bmcl.2007.10.109 | |||
CHEMBL253733 | 94899 | None | 0 | Human | Functional | pKi | = | 8 | 8.0 | - | 0 | ChEMBL | 524 | 4 | 2 | 3 | 5.6 | CC(C)(C)C(=O)N1C2C=C(CN3CCC(NC(=O)Nc4cc(F)cc(C(F)(F)F)c4)CC3)CC1CCC2 | 10.1016/j.bmcl.2007.10.109 | |||
44446445 | 95012 | None | 0 | Mouse | Functional | pKi | = | 7 | 7.0 | - | 0 | ChEMBL | 510 | 4 | 2 | 3 | 5.2 | CC(C)(C)C(=O)N1C2C=C(CN3CCC(NC(=O)Nc4cc(F)cc(C(F)(F)F)c4)CC3)CC1CC2 | 10.1016/j.bmcl.2007.10.109 | |||
CHEMBL254537 | 95012 | None | 0 | Mouse | Functional | pKi | = | 7 | 7.0 | - | 0 | ChEMBL | 510 | 4 | 2 | 3 | 5.2 | CC(C)(C)C(=O)N1C2C=C(CN3CCC(NC(=O)Nc4cc(F)cc(C(F)(F)F)c4)CC3)CC1CC2 | 10.1016/j.bmcl.2007.10.109 | |||
44426912 | 92546 | None | 0 | Human | Functional | pKi | = | 7.0 | 7.0 | - | 0 | ChEMBL | 425 | 5 | 2 | 3 | 5.5 | O=C(Nc1cccc(OC(F)(F)F)c1)NC1CCN(C/C2=C/CCCCCC2)CC1 | 10.1016/j.bmcl.2006.10.088 | |||
CHEMBL243131 | 92546 | None | 0 | Human | Functional | pKi | = | 7.0 | 7.0 | - | 0 | ChEMBL | 425 | 5 | 2 | 3 | 5.5 | O=C(Nc1cccc(OC(F)(F)F)c1)NC1CCN(C/C2=C/CCCCCC2)CC1 | 10.1016/j.bmcl.2006.10.088 | |||
44426931 | 144055 | None | 0 | Human | Functional | pKi | = | 6.0 | 6.0 | - | 0 | ChEMBL | 397 | 4 | 2 | 2 | 5.9 | CC(C)(C)c1ccc(NC(=O)NC2CCN(C/C3=C/CCCCCC3)CC2)cc1 | 10.1016/j.bmcl.2006.10.088 | |||
CHEMBL390264 | 144055 | None | 0 | Human | Functional | pKi | = | 6.0 | 6.0 | - | 0 | ChEMBL | 397 | 4 | 2 | 2 | 5.9 | CC(C)(C)c1ccc(NC(=O)NC2CCN(C/C3=C/CCCCCC3)CC2)cc1 | 10.1016/j.bmcl.2006.10.088 | |||
44427008 | 93260 | None | 0 | Human | Functional | pKi | = | 7.0 | 7.0 | - | 0 | ChEMBL | 436 | 5 | 2 | 4 | 5.4 | CC1(C)[C@H]2CC=C(CN3CCC(NC(=O)Nc4cncc(-c5ccsc5)c4)CC3)[C@@H]1C2 | 10.1016/j.bmcl.2006.10.088 | |||
CHEMBL244604 | 93260 | None | 0 | Human | Functional | pKi | = | 7.0 | 7.0 | - | 0 | ChEMBL | 436 | 5 | 2 | 4 | 5.4 | CC1(C)[C@H]2CC=C(CN3CCC(NC(=O)Nc4cncc(-c5ccsc5)c4)CC3)[C@@H]1C2 | 10.1016/j.bmcl.2006.10.088 | |||
44426935 | 92208 | None | 0 | Human | Functional | pKi | = | 7.0 | 7.0 | - | 0 | ChEMBL | 423 | 5 | 2 | 3 | 6.3 | O=C(Nc1ccc(-c2ccccc2)s1)NC1CCN(C/C2=C/CCCCCC2)CC1 | 10.1016/j.bmcl.2006.10.088 | |||
CHEMBL242268 | 92208 | None | 0 | Human | Functional | pKi | = | 7.0 | 7.0 | - | 0 | ChEMBL | 423 | 5 | 2 | 3 | 6.3 | O=C(Nc1ccc(-c2ccccc2)s1)NC1CCN(C/C2=C/CCCCCC2)CC1 | 10.1016/j.bmcl.2006.10.088 | |||
44446453 | 94824 | None | 0 | Human | Functional | pKi | = | 8.0 | 8.0 | - | 0 | ChEMBL | 454 | 6 | 2 | 4 | 4.2 | CC(=O)N1C2C=C(CN3CCC(NC(=O)Nc4cccc(OC(C)C)c4)CC3)CC1CCC2 | 10.1016/j.bmcl.2007.10.109 | |||
CHEMBL253247 | 94824 | None | 0 | Human | Functional | pKi | = | 8.0 | 8.0 | - | 0 | ChEMBL | 454 | 6 | 2 | 4 | 4.2 | CC(=O)N1C2C=C(CN3CCC(NC(=O)Nc4cccc(OC(C)C)c4)CC3)CC1CCC2 | 10.1016/j.bmcl.2007.10.109 | |||
9886775 | 93265 | None | 0 | Human | Functional | pKi | = | 7.0 | 7.0 | - | 0 | ChEMBL | 391 | 4 | 2 | 2 | 5.7 | O=C(Nc1ccc2ccccc2c1)NC1CCN(C/C2=C/CCCCCC2)CC1 | 10.1016/j.bmcl.2007.10.109 | |||
CHEMBL244610 | 93265 | None | 0 | Human | Functional | pKi | = | 7.0 | 7.0 | - | 0 | ChEMBL | 391 | 4 | 2 | 2 | 5.7 | O=C(Nc1ccc2ccccc2c1)NC1CCN(C/C2=C/CCCCCC2)CC1 | 10.1016/j.bmcl.2007.10.109 | |||
9886775 | 93265 | None | 0 | Human | Functional | pKi | = | 7.0 | 7.0 | - | 0 | ChEMBL | 391 | 4 | 2 | 2 | 5.7 | O=C(Nc1ccc2ccccc2c1)NC1CCN(C/C2=C/CCCCCC2)CC1 | 10.1016/j.bmcl.2006.10.088 | |||
CHEMBL244610 | 93265 | None | 0 | Human | Functional | pKi | = | 7.0 | 7.0 | - | 0 | ChEMBL | 391 | 4 | 2 | 2 | 5.7 | O=C(Nc1ccc2ccccc2c1)NC1CCN(C/C2=C/CCCCCC2)CC1 | 10.1016/j.bmcl.2006.10.088 | |||
44446421 | 94833 | None | 0 | Human | Functional | pKi | = | 6.0 | 6.0 | - | 0 | ChEMBL | 501 | 5 | 2 | 4 | 4.1 | O=C(Nc1cc(C(F)(F)F)cc(C(F)(F)F)c1)NC1CCN(CCC2CCS(=O)(=O)C2)CC1 | 10.1016/j.bmcl.2007.10.109 | |||
CHEMBL253293 | 94833 | None | 0 | Human | Functional | pKi | = | 6.0 | 6.0 | - | 0 | ChEMBL | 501 | 5 | 2 | 4 | 4.1 | O=C(Nc1cc(C(F)(F)F)cc(C(F)(F)F)c1)NC1CCN(CCC2CCS(=O)(=O)C2)CC1 | 10.1016/j.bmcl.2007.10.109 | |||
44446457 | 155518 | None | 0 | Human | Functional | pKi | = | 6.9 | 6.9 | - | 0 | ChEMBL | 470 | 4 | 2 | 3 | 4.2 | CC(=O)N1C2CCC1CC(CN1CCC(NC(=O)Nc3cc(F)cc(C(F)(F)F)c3)CC1)C2 | 10.1016/j.bmcl.2007.10.109 | |||
CHEMBL403740 | 155518 | None | 0 | Human | Functional | pKi | = | 6.9 | 6.9 | - | 0 | ChEMBL | 470 | 4 | 2 | 3 | 4.2 | CC(=O)N1C2CCC1CC(CN1CCC(NC(=O)Nc3cc(F)cc(C(F)(F)F)c3)CC1)C2 | 10.1016/j.bmcl.2007.10.109 | |||
44446439 | 155438 | None | 0 | Mouse | Functional | pKi | = | 6.9 | 6.9 | - | 0 | ChEMBL | 468 | 4 | 2 | 3 | 4.1 | CC(=O)N1C2C=C(CN3CCC(NC(=O)Nc4cc(F)cc(C(F)(F)F)c4)CC3)CC1CC2 | 10.1016/j.bmcl.2007.10.109 | |||
CHEMBL403267 | 155438 | None | 0 | Mouse | Functional | pKi | = | 6.9 | 6.9 | - | 0 | ChEMBL | 468 | 4 | 2 | 3 | 4.1 | CC(=O)N1C2C=C(CN3CCC(NC(=O)Nc4cc(F)cc(C(F)(F)F)c4)CC3)CC1CC2 | 10.1016/j.bmcl.2007.10.109 | |||
44426992 | 142107 | None | 0 | Human | Functional | pKi | = | 5.9 | 5.9 | - | 0 | ChEMBL | 373 | 5 | 2 | 2 | 4.7 | O=C(Nc1ccc2ccccc2c1)NC1CCN(CCc2ccccc2)CC1 | 10.1016/j.bmcl.2006.10.088 | |||
CHEMBL387596 | 142107 | None | 0 | Human | Functional | pKi | = | 5.9 | 5.9 | - | 0 | ChEMBL | 373 | 5 | 2 | 2 | 4.7 | O=C(Nc1ccc2ccccc2c1)NC1CCN(CCc2ccccc2)CC1 | 10.1016/j.bmcl.2006.10.088 | |||
44427009 | 93261 | None | 0 | Human | Functional | pKi | = | 6.9 | 6.9 | - | 0 | ChEMBL | 439 | 6 | 2 | 4 | 4.4 | CC1(C)[C@H]2CC=C(CN3CCC(NC(=O)Nc4cccc(OC5CCOC5)c4)CC3)[C@@H]1C2 | 10.1016/j.bmcl.2006.10.088 | |||
CHEMBL244605 | 93261 | None | 0 | Human | Functional | pKi | = | 6.9 | 6.9 | - | 0 | ChEMBL | 439 | 6 | 2 | 4 | 4.4 | CC1(C)[C@H]2CC=C(CN3CCC(NC(=O)Nc4cccc(OC5CCOC5)c4)CC3)[C@@H]1C2 | 10.1016/j.bmcl.2006.10.088 | |||
44427014 | 151931 | None | 0 | Human | Functional | pKi | = | 7.8 | 7.8 | - | 0 | ChEMBL | 439 | 4 | 2 | 2 | 5.4 | CC1(C)[C@H]2CC=C(CN3CCC(NC(=O)Nc4cc(F)cc(C(F)(F)F)c4)CC3)[C@@H]1C2 | 10.1016/j.bmcl.2006.10.088 | |||
CHEMBL396545 | 151931 | None | 0 | Human | Functional | pKi | = | 7.8 | 7.8 | - | 0 | ChEMBL | 439 | 4 | 2 | 2 | 5.4 | CC1(C)[C@H]2CC=C(CN3CCC(NC(=O)Nc4cc(F)cc(C(F)(F)F)c4)CC3)[C@@H]1C2 | 10.1016/j.bmcl.2006.10.088 | |||
44426998 | 149864 | None | 0 | Human | Functional | pKi | = | 6.8 | 6.8 | - | 0 | ChEMBL | 389 | 4 | 2 | 2 | 4.5 | CC1(C)[C@H]2CC=C(CN3CCC(NC(=O)Nc4cc(F)cc(F)c4)CC3)[C@@H]1C2 | 10.1016/j.bmcl.2006.10.088 | |||
CHEMBL394839 | 149864 | None | 0 | Human | Functional | pKi | = | 6.8 | 6.8 | - | 0 | ChEMBL | 389 | 4 | 2 | 2 | 4.5 | CC1(C)[C@H]2CC=C(CN3CCC(NC(=O)Nc4cc(F)cc(F)c4)CC3)[C@@H]1C2 | 10.1016/j.bmcl.2006.10.088 | |||
44427006 | 151609 | None | 0 | Human | Functional | pKi | = | 6.8 | 6.8 | - | 0 | ChEMBL | 432 | 4 | 2 | 3 | 4.4 | CC1(C)[C@H]2CC=C(CN3CCC(NC(=O)Nc4cncc(Br)c4)CC3)[C@@H]1C2 | 10.1016/j.bmcl.2006.10.088 | |||
CHEMBL396282 | 151609 | None | 0 | Human | Functional | pKi | = | 6.8 | 6.8 | - | 0 | ChEMBL | 432 | 4 | 2 | 3 | 4.4 | CC1(C)[C@H]2CC=C(CN3CCC(NC(=O)Nc4cncc(Br)c4)CC3)[C@@H]1C2 | 10.1016/j.bmcl.2006.10.088 | |||
44427001 | 93101 | None | 0 | Human | Functional | pKi | = | 6.8 | 6.8 | - | 0 | ChEMBL | 437 | 5 | 2 | 3 | 5.2 | CC1(C)[C@H]2CC=C(CN3CCC(NC(=O)Nc4ccc(OC(F)(F)F)cc4)CC3)[C@@H]1C2 | 10.1016/j.bmcl.2006.10.088 | |||
CHEMBL244187 | 93101 | None | 0 | Human | Functional | pKi | = | 6.8 | 6.8 | - | 0 | ChEMBL | 437 | 5 | 2 | 3 | 5.2 | CC1(C)[C@H]2CC=C(CN3CCC(NC(=O)Nc4ccc(OC(F)(F)F)cc4)CC3)[C@@H]1C2 | 10.1016/j.bmcl.2006.10.088 | |||
44446445 | 95012 | None | 0 | Human | Functional | pKi | = | 7.8 | 7.8 | - | 0 | ChEMBL | 510 | 4 | 2 | 3 | 5.2 | CC(C)(C)C(=O)N1C2C=C(CN3CCC(NC(=O)Nc4cc(F)cc(C(F)(F)F)c4)CC3)CC1CC2 | 10.1016/j.bmcl.2007.10.109 | |||
CHEMBL254537 | 95012 | None | 0 | Human | Functional | pKi | = | 7.8 | 7.8 | - | 0 | ChEMBL | 510 | 4 | 2 | 3 | 5.2 | CC(C)(C)C(=O)N1C2C=C(CN3CCC(NC(=O)Nc4cc(F)cc(C(F)(F)F)c4)CC3)CC1CC2 | 10.1016/j.bmcl.2007.10.109 | |||
44446422 | 94706 | None | 0 | Human | Functional | pKi | = | 6.8 | 6.8 | - | 0 | ChEMBL | 494 | 4 | 2 | 3 | 4.6 | CC(=O)N1CCC(CN2CCC(NC(=O)Nc3cc(C(F)(F)F)cc(C(F)(F)F)c3)CC2)CC1 | 10.1016/j.bmcl.2007.10.109 | |||
CHEMBL252502 | 94706 | None | 0 | Human | Functional | pKi | = | 6.8 | 6.8 | - | 0 | ChEMBL | 494 | 4 | 2 | 3 | 4.6 | CC(=O)N1CCC(CN2CCC(NC(=O)Nc3cc(C(F)(F)F)cc(C(F)(F)F)c3)CC2)CC1 | 10.1016/j.bmcl.2007.10.109 | |||
44446441 | 94798 | None | 0 | Mouse | Functional | pKi | = | 6.8 | 6.8 | - | 0 | ChEMBL | 496 | 5 | 2 | 3 | 4.8 | CC(C)C(=O)N1C2C=C(CN3CCC(NC(=O)Nc4cc(F)cc(C(F)(F)F)c4)CC3)CC1CC2 | 10.1016/j.bmcl.2007.10.109 | |||
CHEMBL253102 | 94798 | None | 0 | Mouse | Functional | pKi | = | 6.8 | 6.8 | - | 0 | ChEMBL | 496 | 5 | 2 | 3 | 4.8 | CC(C)C(=O)N1C2C=C(CN3CCC(NC(=O)Nc4cc(F)cc(C(F)(F)F)c4)CC3)CC1CC2 | 10.1016/j.bmcl.2007.10.109 | |||
44446438 | 94926 | None | 0 | Human | Functional | pKi | = | 6.7 | 6.7 | - | 0 | ChEMBL | 498 | 5 | 2 | 4 | 4.8 | CCOC(=O)N1C2C=C(CN3CCC(NC(=O)Nc4cc(F)cc(C(F)(F)F)c4)CC3)CC1CC2 | 10.1016/j.bmcl.2007.10.109 | |||
CHEMBL253928 | 94926 | None | 0 | Human | Functional | pKi | = | 6.7 | 6.7 | - | 0 | ChEMBL | 498 | 5 | 2 | 4 | 4.8 | CCOC(=O)N1C2C=C(CN3CCC(NC(=O)Nc4cc(F)cc(C(F)(F)F)c4)CC3)CC1CC2 | 10.1016/j.bmcl.2007.10.109 | |||
44427011 | 93294 | None | 0 | Human | Functional | pKi | = | 6.7 | 6.7 | - | 0 | ChEMBL | 453 | 6 | 2 | 4 | 4.8 | CC1(C)[C@H]2CC=C(CN3CCC(NC(=O)Nc4cccc(OC5CCOCC5)c4)CC3)[C@@H]1C2 | 10.1016/j.bmcl.2006.10.088 | |||
CHEMBL244814 | 93294 | None | 0 | Human | Functional | pKi | = | 6.7 | 6.7 | - | 0 | ChEMBL | 453 | 6 | 2 | 4 | 4.8 | CC1(C)[C@H]2CC=C(CN3CCC(NC(=O)Nc4cccc(OC5CCOCC5)c4)CC3)[C@@H]1C2 | 10.1016/j.bmcl.2006.10.088 | |||
44427002 | 149865 | None | 0 | Human | Functional | pKi | = | 6.7 | 6.7 | - | 0 | ChEMBL | 435 | 5 | 2 | 3 | 6.0 | CC1(C)[C@H]2CC=C(CN3CCC(NC(=O)Nc4ccc(-c5ccccc5)s4)CC3)[C@@H]1C2 | 10.1016/j.bmcl.2006.10.088 | |||
CHEMBL394840 | 149865 | None | 0 | Human | Functional | pKi | = | 6.7 | 6.7 | - | 0 | ChEMBL | 435 | 5 | 2 | 3 | 6.0 | CC1(C)[C@H]2CC=C(CN3CCC(NC(=O)Nc4ccc(-c5ccccc5)s4)CC3)[C@@H]1C2 | 10.1016/j.bmcl.2006.10.088 | |||
44446443 | 95011 | None | 0 | Human | Functional | pKi | = | 7.7 | 7.7 | - | 0 | ChEMBL | 494 | 5 | 2 | 3 | 4.5 | O=C(Nc1cc(F)cc(C(F)(F)F)c1)NC1CCN(CC2=CC3CCC(C2)N3C(=O)C2CC2)CC1 | 10.1016/j.bmcl.2007.10.109 | |||
CHEMBL254536 | 95011 | None | 0 | Human | Functional | pKi | = | 7.7 | 7.7 | - | 0 | ChEMBL | 494 | 5 | 2 | 3 | 4.5 | O=C(Nc1cc(F)cc(C(F)(F)F)c1)NC1CCN(CC2=CC3CCC(C2)N3C(=O)C2CC2)CC1 | 10.1016/j.bmcl.2007.10.109 | |||
44426994 | 92464 | None | 0 | Human | Functional | pKi | = | 5.7 | 5.7 | - | 0 | ChEMBL | 353 | 4 | 2 | 2 | 4.3 | CC1(C)[C@H]2CC=C(CN3CCC(NC(=O)Nc4ccccc4)CC3)[C@@H]1C2 | 10.1016/j.bmcl.2006.10.088 | |||
CHEMBL243115 | 92464 | None | 0 | Human | Functional | pKi | = | 5.7 | 5.7 | - | 0 | ChEMBL | 353 | 4 | 2 | 2 | 4.3 | CC1(C)[C@H]2CC=C(CN3CCC(NC(=O)Nc4ccccc4)CC3)[C@@H]1C2 | 10.1016/j.bmcl.2006.10.088 | |||
44426911 | 93302 | None | 0 | Human | Functional | pKi | = | 6.7 | 6.7 | - | 0 | ChEMBL | 375 | 4 | 2 | 2 | 5.2 | O=C(Nc1cccc(Cl)c1)NC1CCN(C/C2=C/CCCCCC2)CC1 | 10.1016/j.bmcl.2006.10.088 | |||
CHEMBL244822 | 93302 | None | 0 | Human | Functional | pKi | = | 6.7 | 6.7 | - | 0 | ChEMBL | 375 | 4 | 2 | 2 | 5.2 | O=C(Nc1cccc(Cl)c1)NC1CCN(C/C2=C/CCCCCC2)CC1 | 10.1016/j.bmcl.2006.10.088 | |||
44426993 | 92463 | None | 0 | Human | Functional | pKi | = | 5.7 | 5.7 | - | 0 | ChEMBL | 387 | 6 | 2 | 2 | 5.1 | O=C(Nc1ccc2ccccc2c1)NC1CCN(CCCc2ccccc2)CC1 | 10.1016/j.bmcl.2006.10.088 | |||
CHEMBL243114 | 92463 | None | 0 | Human | Functional | pKi | = | 5.7 | 5.7 | - | 0 | ChEMBL | 387 | 6 | 2 | 2 | 5.1 | O=C(Nc1ccc2ccccc2c1)NC1CCN(CCCc2ccccc2)CC1 | 10.1016/j.bmcl.2006.10.088 | |||
44427013 | 93296 | None | 0 | Human | Functional | pKi | = | 6.6 | 6.6 | - | 0 | ChEMBL | 439 | 4 | 2 | 2 | 5.4 | CC1(C)[C@H]2CC=C(CN3CCC(NC(=O)Nc4cc(C(F)(F)F)ccc4F)CC3)[C@@H]1C2 | 10.1016/j.bmcl.2006.10.088 | |||
CHEMBL244816 | 93296 | None | 0 | Human | Functional | pKi | = | 6.6 | 6.6 | - | 0 | ChEMBL | 439 | 4 | 2 | 2 | 5.4 | CC1(C)[C@H]2CC=C(CN3CCC(NC(=O)Nc4cc(C(F)(F)F)ccc4F)CC3)[C@@H]1C2 | 10.1016/j.bmcl.2006.10.088 | |||
44426996 | 167620 | None | 0 | Human | Functional | pKi | = | 6.6 | 6.6 | - | 0 | ChEMBL | 395 | 5 | 2 | 3 | 4.5 | CC(=O)c1cccc(NC(=O)NC2CCN(CC3=CC[C@H]4C[C@@H]3C4(C)C)CC2)c1 | 10.1016/j.bmcl.2006.10.088 | |||
CHEMBL430005 | 167620 | None | 0 | Human | Functional | pKi | = | 6.6 | 6.6 | - | 0 | ChEMBL | 395 | 5 | 2 | 3 | 4.5 | CC(=O)c1cccc(NC(=O)NC2CCN(CC3=CC[C@H]4C[C@@H]3C4(C)C)CC2)c1 | 10.1016/j.bmcl.2006.10.088 | |||
44426995 | 169132 | None | 0 | Human | Functional | pKi | = | 7.6 | 7.6 | - | 0 | ChEMBL | 489 | 4 | 2 | 2 | 6.3 | CC1(C)[C@H]2CC=C(CN3CCC(NC(=O)Nc4cc(C(F)(F)F)cc(C(F)(F)F)c4)CC3)[C@@H]1C2 | 10.1016/j.bmcl.2007.10.109 | |||
CHEMBL439399 | 169132 | None | 0 | Human | Functional | pKi | = | 7.6 | 7.6 | - | 0 | ChEMBL | 489 | 4 | 2 | 2 | 6.3 | CC1(C)[C@H]2CC=C(CN3CCC(NC(=O)Nc4cc(C(F)(F)F)cc(C(F)(F)F)c4)CC3)[C@@H]1C2 | 10.1016/j.bmcl.2007.10.109 | |||
44446439 | 155438 | None | 0 | Human | Functional | pKi | = | 7.6 | 7.6 | - | 0 | ChEMBL | 468 | 4 | 2 | 3 | 4.1 | CC(=O)N1C2C=C(CN3CCC(NC(=O)Nc4cc(F)cc(C(F)(F)F)c4)CC3)CC1CC2 | 10.1016/j.bmcl.2007.10.109 | |||
CHEMBL403267 | 155438 | None | 0 | Human | Functional | pKi | = | 7.6 | 7.6 | - | 0 | ChEMBL | 468 | 4 | 2 | 3 | 4.1 | CC(=O)N1C2C=C(CN3CCC(NC(=O)Nc4cc(F)cc(C(F)(F)F)c4)CC3)CC1CC2 | 10.1016/j.bmcl.2007.10.109 | |||
44446441 | 94798 | None | 0 | Human | Functional | pKi | = | 7.6 | 7.6 | - | 0 | ChEMBL | 496 | 5 | 2 | 3 | 4.8 | CC(C)C(=O)N1C2C=C(CN3CCC(NC(=O)Nc4cc(F)cc(C(F)(F)F)c4)CC3)CC1CC2 | 10.1016/j.bmcl.2007.10.109 | |||
CHEMBL253102 | 94798 | None | 0 | Human | Functional | pKi | = | 7.6 | 7.6 | - | 0 | ChEMBL | 496 | 5 | 2 | 3 | 4.8 | CC(C)C(=O)N1C2C=C(CN3CCC(NC(=O)Nc4cc(F)cc(C(F)(F)F)c4)CC3)CC1CC2 | 10.1016/j.bmcl.2007.10.109 | |||
44427020 | 11911 | None | 0 | Human | Functional | pKi | = | 7.6 | 7.6 | - | 0 | ChEMBL | 454 | 4 | 2 | 1 | 5.6 | CC1(C)[C@H]2CC=C(C[N+]3(C)CCC(NC(=O)Nc4cc(F)cc(C(F)(F)F)c4)CC3)[C@@H]1C2 | 10.1016/j.bmcl.2006.10.088 | |||
CHEMBL1182550 | 11911 | None | 0 | Human | Functional | pKi | = | 7.6 | 7.6 | - | 0 | ChEMBL | 454 | 4 | 2 | 1 | 5.6 | CC1(C)[C@H]2CC=C(C[N+]3(C)CCC(NC(=O)Nc4cc(F)cc(C(F)(F)F)c4)CC3)[C@@H]1C2 | 10.1016/j.bmcl.2006.10.088 | |||
CHEMBL245257 | 11911 | None | 0 | Human | Functional | pKi | = | 7.6 | 7.6 | - | 0 | ChEMBL | 454 | 4 | 2 | 1 | 5.6 | CC1(C)[C@H]2CC=C(C[N+]3(C)CCC(NC(=O)Nc4cc(F)cc(C(F)(F)F)c4)CC3)[C@@H]1C2 | 10.1016/j.bmcl.2006.10.088 | |||
44446452 | 155189 | None | 0 | Human | Functional | pKi | = | 6.6 | 6.6 | - | 0 | ChEMBL | 438 | 5 | 2 | 4 | 3.6 | CC(=O)c1cccc(NC(=O)NC2CCN(CC3=CC4CCCC(C3)N4C(C)=O)CC2)c1 | 10.1016/j.bmcl.2007.10.109 | |||
CHEMBL401915 | 155189 | None | 0 | Human | Functional | pKi | = | 6.6 | 6.6 | - | 0 | ChEMBL | 438 | 5 | 2 | 4 | 3.6 | CC(=O)c1cccc(NC(=O)NC2CCN(CC3=CC4CCCC(C3)N4C(C)=O)CC2)c1 | 10.1016/j.bmcl.2007.10.109 | |||
44427004 | 93232 | None | 0 | Human | Functional | pKi | = | 7.5 | 7.5 | - | 0 | ChEMBL | 465 | 6 | 2 | 4 | 6.0 | COc1cccc(-c2ccc(NC(=O)NC3CCN(CC4=CC[C@H]5C[C@@H]4C5(C)C)CC3)s2)c1 | 10.1016/j.bmcl.2006.10.088 | |||
CHEMBL244399 | 93232 | None | 0 | Human | Functional | pKi | = | 7.5 | 7.5 | - | 0 | ChEMBL | 465 | 6 | 2 | 4 | 6.0 | COc1cccc(-c2ccc(NC(=O)NC3CCN(CC4=CC[C@H]5C[C@@H]4C5(C)C)CC3)s2)c1 | 10.1016/j.bmcl.2006.10.088 | |||
44426990 | 92364 | None | 0 | Human | Functional | pKi | = | 6.5 | 6.5 | - | 0 | ChEMBL | 417 | 5 | 2 | 2 | 5.8 | CC1(C)C2CC=C(CCN3CCC(NC(=O)Nc4ccc5ccccc5c4)CC3)C1C2 | 10.1016/j.bmcl.2006.10.088 | |||
CHEMBL242889 | 92364 | None | 0 | Human | Functional | pKi | = | 6.5 | 6.5 | - | 0 | ChEMBL | 417 | 5 | 2 | 2 | 5.8 | CC1(C)C2CC=C(CCN3CCC(NC(=O)Nc4ccc5ccccc5c4)CC3)C1C2 | 10.1016/j.bmcl.2006.10.088 | |||
44446454 | 94825 | None | 0 | Human | Functional | pKi | = | 8.5 | 8.5 | - | 0 | ChEMBL | 472 | 6 | 2 | 4 | 4.3 | CC(=O)N1C2C=C(CN3CCC(NC(=O)Nc4cc(F)cc(OC(C)C)c4)CC3)CC1CCC2 | 10.1016/j.bmcl.2007.10.109 | |||
CHEMBL253248 | 94825 | None | 0 | Human | Functional | pKi | = | 8.5 | 8.5 | - | 0 | ChEMBL | 472 | 6 | 2 | 4 | 4.3 | CC(=O)N1C2C=C(CN3CCC(NC(=O)Nc4cc(F)cc(OC(C)C)c4)CC3)CC1CCC2 | 10.1016/j.bmcl.2007.10.109 | |||
44426920 | 93375 | None | 0 | Human | Functional | pKi | = | 6.5 | 6.5 | - | 0 | ChEMBL | 433 | 6 | 2 | 3 | 6.3 | O=C(Nc1ccc(Oc2ccccc2)cc1)NC1CCN(C/C2=C/CCCCCC2)CC1 | 10.1016/j.bmcl.2006.10.088 | |||
CHEMBL245271 | 93375 | None | 0 | Human | Functional | pKi | = | 6.5 | 6.5 | - | 0 | ChEMBL | 433 | 6 | 2 | 3 | 6.3 | O=C(Nc1ccc(Oc2ccccc2)cc1)NC1CCN(C/C2=C/CCCCCC2)CC1 | 10.1016/j.bmcl.2006.10.088 | |||
44427000 | 93100 | None | 0 | Human | Functional | pKi | = | 7.5 | 7.5 | - | 0 | ChEMBL | 437 | 5 | 2 | 3 | 5.2 | CC1(C)[C@H]2CC=C(CN3CCC(NC(=O)Nc4cccc(OC(F)(F)F)c4)CC3)[C@@H]1C2 | 10.1016/j.bmcl.2006.10.088 | |||
CHEMBL244186 | 93100 | None | 0 | Human | Functional | pKi | = | 7.5 | 7.5 | - | 0 | ChEMBL | 437 | 5 | 2 | 3 | 5.2 | CC1(C)[C@H]2CC=C(CN3CCC(NC(=O)Nc4cccc(OC(F)(F)F)c4)CC3)[C@@H]1C2 | 10.1016/j.bmcl.2006.10.088 | |||
44446453 | 94824 | None | 0 | Mouse | Functional | pKi | = | 7.5 | 7.5 | - | 0 | ChEMBL | 454 | 6 | 2 | 4 | 4.2 | CC(=O)N1C2C=C(CN3CCC(NC(=O)Nc4cccc(OC(C)C)c4)CC3)CC1CCC2 | 10.1016/j.bmcl.2007.10.109 | |||
CHEMBL253247 | 94824 | None | 0 | Mouse | Functional | pKi | = | 7.5 | 7.5 | - | 0 | ChEMBL | 454 | 6 | 2 | 4 | 4.2 | CC(=O)N1C2C=C(CN3CCC(NC(=O)Nc4cccc(OC(C)C)c4)CC3)CC1CCC2 | 10.1016/j.bmcl.2007.10.109 | |||
44426932 | 92169 | None | 0 | Human | Functional | pKi | = | 5.5 | 5.5 | - | 0 | ChEMBL | 410 | 4 | 2 | 3 | 5.3 | O=C(Nc1c(Cl)cncc1Cl)NC1CCN(C/C2=C/CCCCCC2)CC1 | 10.1016/j.bmcl.2006.10.088 | |||
CHEMBL242045 | 92169 | None | 0 | Human | Functional | pKi | = | 5.5 | 5.5 | - | 0 | ChEMBL | 410 | 4 | 2 | 3 | 5.3 | O=C(Nc1c(Cl)cncc1Cl)NC1CCN(C/C2=C/CCCCCC2)CC1 | 10.1016/j.bmcl.2006.10.088 | |||
44426914 | 152222 | None | 0 | Human | Functional | pKi | = | 7.4 | 7.4 | - | 0 | ChEMBL | 477 | 4 | 2 | 2 | 6.6 | O=C(Nc1cc(C(F)(F)F)cc(C(F)(F)F)c1)NC1CCN(C/C2=C/CCCCCC2)CC1 | 10.1016/j.bmcl.2006.10.088 | |||
CHEMBL396793 | 152222 | None | 0 | Human | Functional | pKi | = | 7.4 | 7.4 | - | 0 | ChEMBL | 477 | 4 | 2 | 2 | 6.6 | O=C(Nc1cc(C(F)(F)F)cc(C(F)(F)F)c1)NC1CCN(C/C2=C/CCCCCC2)CC1 | 10.1016/j.bmcl.2006.10.088 | |||
44427016 | 93336 | None | 0 | Human | Functional | pKi | = | 6.4 | 6.4 | - | 0 | ChEMBL | 411 | 5 | 2 | 4 | 4.1 | COC(=O)c1cccc(NC(=O)NC2CCN(CC3=CC[C@H]4C[C@@H]3C4(C)C)CC2)c1 | 10.1016/j.bmcl.2006.10.088 | |||
CHEMBL245034 | 93336 | None | 0 | Human | Functional | pKi | = | 6.4 | 6.4 | - | 0 | ChEMBL | 411 | 5 | 2 | 4 | 4.1 | COC(=O)c1cccc(NC(=O)NC2CCN(CC3=CC[C@H]4C[C@@H]3C4(C)C)CC2)c1 | 10.1016/j.bmcl.2006.10.088 | |||
44446450 | 155733 | None | 0 | Mouse | Functional | pKi | = | 7.4 | 7.4 | - | 0 | ChEMBL | 482 | 4 | 2 | 3 | 4.5 | CC(=O)N1C2C=C(CN3CCC(NC(=O)Nc4cc(F)cc(C(F)(F)F)c4)CC3)CC1CCC2 | 10.1016/j.bmcl.2007.10.109 | |||
CHEMBL404736 | 155733 | None | 0 | Mouse | Functional | pKi | = | 7.4 | 7.4 | - | 0 | ChEMBL | 482 | 4 | 2 | 3 | 4.5 | CC(=O)N1C2C=C(CN3CCC(NC(=O)Nc4cc(F)cc(C(F)(F)F)c4)CC3)CC1CCC2 | 10.1016/j.bmcl.2007.10.109 | |||
44427003 | 93231 | None | 0 | Human | Functional | pKi | = | 7.4 | 7.4 | - | 0 | ChEMBL | 503 | 5 | 2 | 3 | 7.0 | CC1(C)[C@H]2CC=C(CN3CCC(NC(=O)Nc4ccc(-c5ccc(C(F)(F)F)cc5)s4)CC3)[C@@H]1C2 | 10.1016/j.bmcl.2006.10.088 | |||
CHEMBL244398 | 93231 | None | 0 | Human | Functional | pKi | = | 7.4 | 7.4 | - | 0 | ChEMBL | 503 | 5 | 2 | 3 | 7.0 | CC1(C)[C@H]2CC=C(CN3CCC(NC(=O)Nc4ccc(-c5ccc(C(F)(F)F)cc5)s4)CC3)[C@@H]1C2 | 10.1016/j.bmcl.2006.10.088 | |||
9886775 | 93265 | None | 0 | Mouse | Functional | pKi | = | 6.4 | 6.4 | - | 0 | ChEMBL | 391 | 4 | 2 | 2 | 5.7 | O=C(Nc1ccc2ccccc2c1)NC1CCN(C/C2=C/CCCCCC2)CC1 | 10.1016/j.bmcl.2007.10.109 | |||
CHEMBL244610 | 93265 | None | 0 | Mouse | Functional | pKi | = | 6.4 | 6.4 | - | 0 | ChEMBL | 391 | 4 | 2 | 2 | 5.7 | O=C(Nc1ccc2ccccc2c1)NC1CCN(C/C2=C/CCCCCC2)CC1 | 10.1016/j.bmcl.2007.10.109 | |||
44426995 | 169132 | None | 0 | Mouse | Functional | pKi | = | 6.4 | 6.4 | - | 0 | ChEMBL | 489 | 4 | 2 | 2 | 6.3 | CC1(C)[C@H]2CC=C(CN3CCC(NC(=O)Nc4cc(C(F)(F)F)cc(C(F)(F)F)c4)CC3)[C@@H]1C2 | 10.1016/j.bmcl.2007.10.109 | |||
CHEMBL439399 | 169132 | None | 0 | Mouse | Functional | pKi | = | 6.4 | 6.4 | - | 0 | ChEMBL | 489 | 4 | 2 | 2 | 6.3 | CC1(C)[C@H]2CC=C(CN3CCC(NC(=O)Nc4cc(C(F)(F)F)cc(C(F)(F)F)c4)CC3)[C@@H]1C2 | 10.1016/j.bmcl.2007.10.109 | |||
9886775 | 93265 | None | 0 | Mouse | Functional | pKi | = | 6.4 | 6.4 | - | 0 | ChEMBL | 391 | 4 | 2 | 2 | 5.7 | O=C(Nc1ccc2ccccc2c1)NC1CCN(C/C2=C/CCCCCC2)CC1 | 10.1016/j.bmcl.2006.10.088 | |||
CHEMBL244610 | 93265 | None | 0 | Mouse | Functional | pKi | = | 6.4 | 6.4 | - | 0 | ChEMBL | 391 | 4 | 2 | 2 | 5.7 | O=C(Nc1ccc2ccccc2c1)NC1CCN(C/C2=C/CCCCCC2)CC1 | 10.1016/j.bmcl.2006.10.088 | |||
44426917 | 92621 | None | 0 | Human | Functional | pKi | = | 7.4 | 7.4 | - | 0 | ChEMBL | 409 | 4 | 2 | 2 | 5.9 | O=C(Nc1cc(Cl)cc(Cl)c1)NC1CCN(C/C2=C/CCCCCC2)CC1 | 10.1016/j.bmcl.2006.10.088 | |||
CHEMBL243341 | 92621 | None | 0 | Human | Functional | pKi | = | 7.4 | 7.4 | - | 0 | ChEMBL | 409 | 4 | 2 | 2 | 5.9 | O=C(Nc1cc(Cl)cc(Cl)c1)NC1CCN(C/C2=C/CCCCCC2)CC1 | 10.1016/j.bmcl.2006.10.088 | |||
44426999 | 93099 | None | 0 | Human | Functional | pKi | = | 6.4 | 6.4 | - | 0 | ChEMBL | 383 | 5 | 2 | 3 | 4.3 | COc1cccc(NC(=O)NC2CCN(CC3=CC[C@H]4C[C@@H]3C4(C)C)CC2)c1 | 10.1016/j.bmcl.2006.10.088 | |||
CHEMBL244185 | 93099 | None | 0 | Human | Functional | pKi | = | 6.4 | 6.4 | - | 0 | ChEMBL | 383 | 5 | 2 | 3 | 4.3 | COc1cccc(NC(=O)NC2CCN(CC3=CC[C@H]4C[C@@H]3C4(C)C)CC2)c1 | 10.1016/j.bmcl.2006.10.088 | |||
44427005 | 93233 | None | 0 | Human | Functional | pKi | = | 7.3 | 7.3 | - | 0 | ChEMBL | 469 | 5 | 2 | 3 | 6.6 | CC1(C)[C@H]2CC=C(CN3CCC(NC(=O)Nc4ccc(-c5ccccc5Cl)s4)CC3)[C@@H]1C2 | 10.1016/j.bmcl.2006.10.088 | |||
CHEMBL244400 | 93233 | None | 0 | Human | Functional | pKi | = | 7.3 | 7.3 | - | 0 | ChEMBL | 469 | 5 | 2 | 3 | 6.6 | CC1(C)[C@H]2CC=C(CN3CCC(NC(=O)Nc4ccc(-c5ccccc5Cl)s4)CC3)[C@@H]1C2 | 10.1016/j.bmcl.2006.10.088 | |||
44426915 | 92620 | None | 0 | Human | Functional | pKi | = | 7.3 | 7.3 | - | 0 | ChEMBL | 427 | 4 | 2 | 2 | 5.7 | O=C(Nc1cc(F)cc(C(F)(F)F)c1)NC1CCN(C/C2=C/CCCCCC2)CC1 | 10.1016/j.bmcl.2006.10.088 | |||
CHEMBL243340 | 92620 | None | 0 | Human | Functional | pKi | = | 7.3 | 7.3 | - | 0 | ChEMBL | 427 | 4 | 2 | 2 | 5.7 | O=C(Nc1cc(F)cc(C(F)(F)F)c1)NC1CCN(C/C2=C/CCCCCC2)CC1 | 10.1016/j.bmcl.2006.10.088 | |||
44591872 | 189390 | None | 0 | Human | Functional | pKi | = | 6.3 | 6.3 | - | 0 | ChEMBL | 416 | 4 | 1 | 2 | 5.2 | CC1(C)[C@@H]2CC[C@@]1(C)[C@H](NC1CCN(Cc3c(F)c(F)c(F)c(F)c3F)CC1)C2 | 10.1016/j.bmcl.2009.02.093 | |||
CHEMBL511976 | 189390 | None | 0 | Human | Functional | pKi | = | 6.3 | 6.3 | - | 0 | ChEMBL | 416 | 4 | 1 | 2 | 5.2 | CC1(C)[C@@H]2CC[C@@]1(C)[C@H](NC1CCN(Cc3c(F)c(F)c(F)c(F)c3F)CC1)C2 | 10.1016/j.bmcl.2009.02.093 | |||
44446451 | 94899 | None | 0 | Mouse | Functional | pKi | = | 7.2 | 7.2 | - | 0 | ChEMBL | 524 | 4 | 2 | 3 | 5.6 | CC(C)(C)C(=O)N1C2C=C(CN3CCC(NC(=O)Nc4cc(F)cc(C(F)(F)F)c4)CC3)CC1CCC2 | 10.1016/j.bmcl.2007.10.109 | |||
CHEMBL253733 | 94899 | None | 0 | Mouse | Functional | pKi | = | 7.2 | 7.2 | - | 0 | ChEMBL | 524 | 4 | 2 | 3 | 5.6 | CC(C)(C)C(=O)N1C2C=C(CN3CCC(NC(=O)Nc4cc(F)cc(C(F)(F)F)c4)CC3)CC1CCC2 | 10.1016/j.bmcl.2007.10.109 | |||
24936155 | 94675 | None | 0 | Mouse | Functional | pKi | = | 8.2 | 8.2 | - | 0 | ChEMBL | 508 | 4 | 2 | 3 | 5.1 | CC(=O)N1C2C=C(CN3C4CCC3CC(NC(=O)Nc3cc(F)cc(C(F)(F)F)c3)C4)CC1CCC2 | 10.1016/j.bmcl.2007.10.109 | |||
CHEMBL252258 | 94675 | None | 0 | Mouse | Functional | pKi | = | 8.2 | 8.2 | - | 0 | ChEMBL | 508 | 4 | 2 | 3 | 5.1 | CC(=O)N1C2C=C(CN3C4CCC3CC(NC(=O)Nc3cc(F)cc(C(F)(F)F)c3)C4)CC1CCC2 | 10.1016/j.bmcl.2007.10.109 | |||
44446454 | 94825 | None | 0 | Mouse | Functional | pKi | = | 8.2 | 8.2 | - | 0 | ChEMBL | 472 | 6 | 2 | 4 | 4.3 | CC(=O)N1C2C=C(CN3CCC(NC(=O)Nc4cc(F)cc(OC(C)C)c4)CC3)CC1CCC2 | 10.1016/j.bmcl.2007.10.109 | |||
CHEMBL253248 | 94825 | None | 0 | Mouse | Functional | pKi | = | 8.2 | 8.2 | - | 0 | ChEMBL | 472 | 6 | 2 | 4 | 4.3 | CC(=O)N1C2C=C(CN3CCC(NC(=O)Nc4cc(F)cc(OC(C)C)c4)CC3)CC1CCC2 | 10.1016/j.bmcl.2007.10.109 | |||
44446423 | 94707 | None | 0 | Human | Functional | pKi | = | 7.2 | 7.2 | - | 0 | ChEMBL | 536 | 4 | 2 | 3 | 5.6 | CC(C)(C)C(=O)N1CCC(CN2CCC(NC(=O)Nc3cc(C(F)(F)F)cc(C(F)(F)F)c3)CC2)CC1 | 10.1016/j.bmcl.2007.10.109 | |||
CHEMBL252503 | 94707 | None | 0 | Human | Functional | pKi | = | 7.2 | 7.2 | - | 0 | ChEMBL | 536 | 4 | 2 | 3 | 5.6 | CC(C)(C)C(=O)N1CCC(CN2CCC(NC(=O)Nc3cc(C(F)(F)F)cc(C(F)(F)F)c3)CC2)CC1 | 10.1016/j.bmcl.2007.10.109 | |||
44426913 | 150437 | None | 0 | Human | Functional | pKi | = | 6.2 | 6.2 | - | 0 | ChEMBL | 383 | 5 | 2 | 3 | 4.8 | CC(=O)c1cccc(NC(=O)NC2CCN(C/C3=C/CCCCCC3)CC2)c1 | 10.1016/j.bmcl.2006.10.088 | |||
CHEMBL395314 | 150437 | None | 0 | Human | Functional | pKi | = | 6.2 | 6.2 | - | 0 | ChEMBL | 383 | 5 | 2 | 3 | 4.8 | CC(=O)c1cccc(NC(=O)NC2CCN(C/C3=C/CCCCCC3)CC2)c1 | 10.1016/j.bmcl.2006.10.088 | |||
44446457 | 155518 | None | 0 | Mouse | Functional | pKi | = | 6.2 | 6.2 | - | 0 | ChEMBL | 470 | 4 | 2 | 3 | 4.2 | CC(=O)N1C2CCC1CC(CN1CCC(NC(=O)Nc3cc(F)cc(C(F)(F)F)c3)CC1)C2 | 10.1016/j.bmcl.2007.10.109 | |||
CHEMBL403740 | 155518 | None | 0 | Mouse | Functional | pKi | = | 6.2 | 6.2 | - | 0 | ChEMBL | 470 | 4 | 2 | 3 | 4.2 | CC(=O)N1C2CCC1CC(CN1CCC(NC(=O)Nc3cc(F)cc(C(F)(F)F)c3)CC1)C2 | 10.1016/j.bmcl.2007.10.109 | |||
44426934 | 92207 | None | 0 | Human | Functional | pKi | = | 6.2 | 6.2 | - | 0 | ChEMBL | 399 | 5 | 2 | 4 | 4.3 | COC(=O)c1cccc(NC(=O)NC2CCN(C/C3=C/CCCCCC3)CC2)c1 | 10.1016/j.bmcl.2006.10.088 | |||
CHEMBL242267 | 92207 | None | 0 | Human | Functional | pKi | = | 6.2 | 6.2 | - | 0 | ChEMBL | 399 | 5 | 2 | 4 | 4.3 | COC(=O)c1cccc(NC(=O)NC2CCN(C/C3=C/CCCCCC3)CC2)c1 | 10.1016/j.bmcl.2006.10.088 | |||
24936155 | 94675 | None | 0 | Human | Functional | pKi | = | 8.2 | 8.2 | - | 0 | ChEMBL | 508 | 4 | 2 | 3 | 5.1 | CC(=O)N1C2C=C(CN3C4CCC3CC(NC(=O)Nc3cc(F)cc(C(F)(F)F)c3)C4)CC1CCC2 | 10.1016/j.bmcl.2007.10.109 | |||
CHEMBL252258 | 94675 | None | 0 | Human | Functional | pKi | = | 8.2 | 8.2 | - | 0 | ChEMBL | 508 | 4 | 2 | 3 | 5.1 | CC(=O)N1C2C=C(CN3C4CCC3CC(NC(=O)Nc3cc(F)cc(C(F)(F)F)c3)C4)CC1CCC2 | 10.1016/j.bmcl.2007.10.109 | |||
44427007 | 93259 | None | 0 | Human | Functional | pKi | = | 7.2 | 7.2 | - | 0 | ChEMBL | 436 | 5 | 2 | 4 | 5.4 | CC1(C)[C@H]2CC=C(CN3CCC(NC(=O)Nc4cncc(-c5cccs5)c4)CC3)[C@@H]1C2 | 10.1016/j.bmcl.2006.10.088 | |||
CHEMBL244603 | 93259 | None | 0 | Human | Functional | pKi | = | 7.2 | 7.2 | - | 0 | ChEMBL | 436 | 5 | 2 | 4 | 5.4 | CC1(C)[C@H]2CC=C(CN3CCC(NC(=O)Nc4cncc(-c5cccs5)c4)CC3)[C@@H]1C2 | 10.1016/j.bmcl.2006.10.088 | |||
44426995 | 169132 | None | 0 | Human | Functional | pKi | = | 7.1 | 7.1 | - | 0 | ChEMBL | 489 | 4 | 2 | 2 | 6.3 | CC1(C)[C@H]2CC=C(CN3CCC(NC(=O)Nc4cc(C(F)(F)F)cc(C(F)(F)F)c4)CC3)[C@@H]1C2 | 10.1016/j.bmcl.2006.10.088 | |||
CHEMBL439399 | 169132 | None | 0 | Human | Functional | pKi | = | 7.1 | 7.1 | - | 0 | ChEMBL | 489 | 4 | 2 | 2 | 6.3 | CC1(C)[C@H]2CC=C(CN3CCC(NC(=O)Nc4cc(C(F)(F)F)cc(C(F)(F)F)c4)CC3)[C@@H]1C2 | 10.1016/j.bmcl.2006.10.088 | |||
44446443 | 95011 | None | 0 | Mouse | Functional | pKi | = | 7.1 | 7.1 | - | 0 | ChEMBL | 494 | 5 | 2 | 3 | 4.5 | O=C(Nc1cc(F)cc(C(F)(F)F)c1)NC1CCN(CC2=CC3CCC(C2)N3C(=O)C2CC2)CC1 | 10.1016/j.bmcl.2007.10.109 | |||
CHEMBL254536 | 95011 | None | 0 | Mouse | Functional | pKi | = | 7.1 | 7.1 | - | 0 | ChEMBL | 494 | 5 | 2 | 3 | 4.5 | O=C(Nc1cc(F)cc(C(F)(F)F)c1)NC1CCN(CC2=CC3CCC(C2)N3C(=O)C2CC2)CC1 | 10.1016/j.bmcl.2007.10.109 | |||
44427015 | 93335 | None | 0 | Human | Functional | pKi | = | 7.1 | 7.1 | - | 0 | ChEMBL | 439 | 4 | 2 | 2 | 5.4 | CC1(C)[C@H]2CC=C(CN3CCC(NC(=O)Nc4ccc(F)c(C(F)(F)F)c4)CC3)[C@@H]1C2 | 10.1016/j.bmcl.2006.10.088 | |||
CHEMBL245033 | 93335 | None | 0 | Human | Functional | pKi | = | 7.1 | 7.1 | - | 0 | ChEMBL | 439 | 4 | 2 | 2 | 5.4 | CC1(C)[C@H]2CC=C(CN3CCC(NC(=O)Nc4ccc(F)c(C(F)(F)F)c4)CC3)[C@@H]1C2 | 10.1016/j.bmcl.2006.10.088 | |||
44427010 | 151929 | None | 0 | Human | Functional | pKi | = | 7.1 | 7.1 | - | 0 | ChEMBL | 457 | 6 | 2 | 4 | 4.6 | CC1(C)[C@H]2CC=C(CN3CCC(NC(=O)Nc4cc(F)cc(OC5CCOC5)c4)CC3)[C@@H]1C2 | 10.1016/j.bmcl.2006.10.088 | |||
CHEMBL396544 | 151929 | None | 0 | Human | Functional | pKi | = | 7.1 | 7.1 | - | 0 | ChEMBL | 457 | 6 | 2 | 4 | 4.6 | CC1(C)[C@H]2CC=C(CN3CCC(NC(=O)Nc4cc(F)cc(OC5CCOC5)c4)CC3)[C@@H]1C2 | 10.1016/j.bmcl.2006.10.088 | |||
44426909 | 93301 | None | 0 | Human | Functional | pKi | = | 7.1 | 7.1 | - | 0 | ChEMBL | 409 | 4 | 2 | 2 | 5.6 | O=C(Nc1cccc(C(F)(F)F)c1)NC1CCN(C/C2=C/CCCCCC2)CC1 | 10.1016/j.bmcl.2006.10.088 | |||
CHEMBL244821 | 93301 | None | 0 | Human | Functional | pKi | = | 7.1 | 7.1 | - | 0 | ChEMBL | 409 | 4 | 2 | 2 | 5.6 | O=C(Nc1cccc(C(F)(F)F)c1)NC1CCN(C/C2=C/CCCCCC2)CC1 | 10.1016/j.bmcl.2006.10.088 | |||
44446450 | 155733 | None | 0 | Human | Functional | pKi | = | 8.1 | 8.1 | - | 0 | ChEMBL | 482 | 4 | 2 | 3 | 4.5 | CC(=O)N1C2C=C(CN3CCC(NC(=O)Nc4cc(F)cc(C(F)(F)F)c4)CC3)CC1CCC2 | 10.1016/j.bmcl.2007.10.109 | |||
CHEMBL404736 | 155733 | None | 0 | Human | Functional | pKi | = | 8.1 | 8.1 | - | 0 | ChEMBL | 482 | 4 | 2 | 3 | 4.5 | CC(=O)N1C2C=C(CN3CCC(NC(=O)Nc4cc(F)cc(C(F)(F)F)c4)CC3)CC1CCC2 | 10.1016/j.bmcl.2007.10.109 | |||
44446438 | 94926 | None | 0 | Mouse | Functional | pKi | = | 6.0 | 6.0 | - | 0 | ChEMBL | 498 | 5 | 2 | 4 | 4.8 | CCOC(=O)N1C2C=C(CN3CCC(NC(=O)Nc4cc(F)cc(C(F)(F)F)c4)CC3)CC1CC2 | 10.1016/j.bmcl.2007.10.109 | |||
CHEMBL253928 | 94926 | None | 0 | Mouse | Functional | pKi | = | 6.0 | 6.0 | - | 0 | ChEMBL | 498 | 5 | 2 | 4 | 4.8 | CCOC(=O)N1C2C=C(CN3CCC(NC(=O)Nc4cc(F)cc(C(F)(F)F)c4)CC3)CC1CC2 | 10.1016/j.bmcl.2007.10.109 | |||
121485701 | 276 | None | 10 | Human | Functional | pIC50 | = | 8.5 | 8.5 | -2 | 4 | Guide to Pharmacology | 550 | 6 | 1 | 10 | 2.6 | CC1=NN(C=N1)CC(=O)N2CCN(C[C@H]2CCO)C3=C(N=C(S3)C(F)(F)F)C4=CN=C(N=C4)C(F)(F)F | 36883854 | |||
12584 | 276 | None | 10 | Human | Functional | pIC50 | = | 8.5 | 8.5 | -2 | 4 | Guide to Pharmacology | 550 | 6 | 1 | 10 | 2.6 | CC1=NN(C=N1)CC(=O)N2CCN(C[C@H]2CCO)C3=C(N=C(S3)C(F)(F)F)C4=CN=C(N=C4)C(F)(F)F | 36883854 | |||
CHEMBL5279308 | 276 | None | 10 | Human | Functional | pIC50 | = | 8.5 | 8.5 | -2 | 4 | Guide to Pharmacology | 550 | 6 | 1 | 10 | 2.6 | CC1=NN(C=N1)CC(=O)N2CCN(C[C@H]2CCO)C3=C(N=C(S3)C(F)(F)F)C4=CN=C(N=C4)C(F)(F)F | 36883854 | |||
12207 | 275 | None | 12 | Human | Functional | pIC50 | = | 8.6 | 8.6 | -7 | 2 | Guide to Pharmacology | 534 | 4 | 0 | 9 | 3.6 | C[C@@H]1CN(CCN1C(=O)Cn1nc(C)nc1C)c1c(c2cnc(C(F)(F)F)nc2)nc(C(F)(F)F)s1 | 35947786 | |||
87056189 | 275 | None | 12 | Human | Functional | pIC50 | = | 8.6 | 8.6 | -7 | 2 | Guide to Pharmacology | 534 | 4 | 0 | 9 | 3.6 | C[C@@H]1CN(CCN1C(=O)Cn1nc(C)nc1C)c1c(c2cnc(C(F)(F)F)nc2)nc(C(F)(F)F)s1 | 35947786 | |||
CHEMBL5202301 | 275 | None | 12 | Human | Functional | pIC50 | = | 8.6 | 8.6 | -7 | 2 | Guide to Pharmacology | 534 | 4 | 0 | 9 | 3.6 | C[C@@H]1CN(CCN1C(=O)Cn1nc(C)nc1C)c1c(c2cnc(C(F)(F)F)nc2)nc(C(F)(F)F)s1 | 35947786 | |||
73754998 | 2176 | None | 0 | Human | Functional | pIC50 | None | 5.5 | 5.5 | - | 1 | Guide to Pharmacology | 1015 | 9 | 10 | 20 | 0.4 | CC1CCC2(OC1)OC1C(C2C)C2(C(C1)C1CC=C3C(C1CC2)(C)CCC(C3)OC1OC(COC2OC(C)C(C(C2OC2(CC(O)C(C(O2)C)O)OC2OC(C)C(C(C2O)O)O)O)O)C(C(C1O)O)O)C | 15789559 | |||
843 | 2176 | None | 0 | Human | Functional | pIC50 | None | 5.5 | 5.5 | - | 1 | Guide to Pharmacology | 1015 | 9 | 10 | 20 | 0.4 | CC1CCC2(OC1)OC1C(C2C)C2(C(C1)C1CC=C3C(C1CC2)(C)CCC(C3)OC1OC(COC2OC(C)C(C(C2OC2(CC(O)C(C(O2)C)O)OC2OC(C)C(C(C2O)O)O)O)O)C(C(C1O)O)O)C | 15789559 | |||
71446540 | 1958 | None | 0 | Human | Functional | pIC50 | None | 5.7 | 5.7 | - | 1 | Guide to Pharmacology | 867 | 7 | 8 | 15 | 1.9 | OC[C@H]1O[C@@H](O[C@H]2CC[C@]3(C(=CC[C@@H]4[C@@H]3CC[C@]3([C@H]4C[C@H]4[C@@H]3[C@H](C)[C@]3(O4)CC[C@@H](CO3)C)C)C2)C)[C@@H]([C@H]([C@@H]1O)O[C@@H]1O[C@@H](C)[C@@H]([C@H]([C@H]1O)O)O)O[C@H]1C[C@H](C)[C@H]([C@H]([C@H]1O)O)O | 15789559 | |||
842 | 1958 | None | 0 | Human | Functional | pIC50 | None | 5.7 | 5.7 | - | 1 | Guide to Pharmacology | 867 | 7 | 8 | 15 | 1.9 | OC[C@H]1O[C@@H](O[C@H]2CC[C@]3(C(=CC[C@@H]4[C@@H]3CC[C@]3([C@H]4C[C@H]4[C@@H]3[C@H](C)[C@]3(O4)CC[C@@H](CO3)C)C)C2)C)[C@@H]([C@H]([C@@H]1O)O[C@@H]1O[C@@H](C)[C@@H]([C@H]([C@H]1O)O)O)O[C@H]1C[C@H](C)[C@H]([C@H]([C@H]1O)O)O | 15789559 | |||
119245 | 1431 | None | 0 | Human | Functional | pIC50 | None | 6.3 | 6.3 | - | 1 | Guide to Pharmacology | 868 | 7 | 8 | 16 | 1.2 | OC[C@H]1O[C@@H](O[C@H]2CC[C@]3(C(=CC[C@@H]4[C@@H]3CC[C@]3([C@H]4C[C@H]4[C@@H]3[C@H](C)[C@]3(O4)CC[C@H](CO3)C)C)C2)C)[C@@H]([C@H]([C@@H]1O[C@@H]1O[C@@H](C)[C@@H]([C@H]([C@H]1O)O)O)O)O[C@@H]1O[C@@H](C)[C@@H]([C@H]([C@H]1O)O)O | 15789559 | |||
840 | 1431 | None | 0 | Human | Functional | pIC50 | None | 6.3 | 6.3 | - | 1 | Guide to Pharmacology | 868 | 7 | 8 | 16 | 1.2 | OC[C@H]1O[C@@H](O[C@H]2CC[C@]3(C(=CC[C@@H]4[C@@H]3CC[C@]3([C@H]4C[C@H]4[C@@H]3[C@H](C)[C@]3(O4)CC[C@H](CO3)C)C)C2)C)[C@@H]([C@H]([C@@H]1O[C@@H]1O[C@@H](C)[C@@H]([C@H]([C@H]1O)O)O)O)O[C@@H]1O[C@@H](C)[C@@H]([C@H]([C@H]1O)O)O | 15789559 | |||
CHEMBL507001 | 1431 | None | 0 | Human | Functional | pIC50 | None | 6.3 | 6.3 | - | 1 | Guide to Pharmacology | 868 | 7 | 8 | 16 | 1.2 | OC[C@H]1O[C@@H](O[C@H]2CC[C@]3(C(=CC[C@@H]4[C@@H]3CC[C@]3([C@H]4C[C@H]4[C@@H]3[C@H](C)[C@]3(O4)CC[C@H](CO3)C)C)C2)C)[C@@H]([C@H]([C@@H]1O[C@@H]1O[C@@H](C)[C@@H]([C@H]([C@H]1O)O)O)O)O[C@@H]1O[C@@H](C)[C@@H]([C@H]([C@H]1O)O)O | 15789559 | |||
841 | 1510 | None | 0 | Human | Functional | pIC50 | None | 7 | 7.0 | - | 1 | Guide to Pharmacology | None | None | None | None | 15789559 |
Ligands (move mouse cursor over ligand name to see structure) | Receptor | Activity | Chemical information | |||||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Sel. page | Common name |
GPCRdb ID |
Reference ligand |
Vendors |
Species |
Assay Type |
Activity Type |
Activity Relation |
Activity Value |
p-value (-log) |
Fold selectivity |
Tested GPCRs |
Assay Description |
Source |
Mol weight |
Rot Bonds |
H don |
H acc |
LogP |
Smiles |
DOI |
|
127030694 | 139302 | None | 0 | Human | Binding | pEC50 | = | 6.0 | 6.0 | - | 0 | ChEMBL | 644 | 15 | 3 | 5 | 5.2 | NCCCC[C@@H](NC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCC(=O)c1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.5b01965 | |||
CHEMBL3786670 | 139302 | None | 0 | Human | Binding | pEC50 | = | 6.0 | 6.0 | - | 0 | ChEMBL | 644 | 15 | 3 | 5 | 5.2 | NCCCC[C@@H](NC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCC(=O)c1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.5b01965 | |||
CHEMBL3787750 | 139302 | None | 0 | Human | Binding | pEC50 | = | 6.0 | 6.0 | - | 0 | ChEMBL | 644 | 15 | 3 | 5 | 5.2 | NCCCC[C@@H](NC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCC(=O)c1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.5b01965 | |||
127031899 | 139168 | None | 0 | Human | Binding | pEC50 | = | 7.0 | 7.0 | - | 0 | ChEMBL | 744 | 16 | 3 | 6 | 6.7 | CC(C)(C)OC(=O)N[C@H](CCCCNC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCC(=O)c1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.5b01965 | |||
CHEMBL3786480 | 139168 | None | 0 | Human | Binding | pEC50 | = | 7.0 | 7.0 | - | 0 | ChEMBL | 744 | 16 | 3 | 6 | 6.7 | CC(C)(C)OC(=O)N[C@H](CCCCNC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCC(=O)c1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.5b01965 | |||
127032166 | 139298 | None | 0 | Human | Binding | pEC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 658 | 16 | 3 | 5 | 5.6 | N[C@@H](CCCCNC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCCC(=O)c1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.5b01965 | |||
CHEMBL3785622 | 139298 | None | 0 | Human | Binding | pEC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 658 | 16 | 3 | 5 | 5.6 | N[C@@H](CCCCNC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCCC(=O)c1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.5b01965 | |||
CHEMBL3787717 | 139298 | None | 0 | Human | Binding | pEC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 658 | 16 | 3 | 5 | 5.6 | N[C@@H](CCCCNC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCCC(=O)c1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.5b01965 | |||
71457439 | 83058 | None | 8 | Human | Binding | pEC50 | = | 5.9 | 5.9 | - | 1 | ChEMBL | 644 | 15 | 3 | 5 | 5.2 | NCCCC[C@H](NC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCC(=O)c1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.5b01965 | |||
CHEMBL2181467 | 83058 | None | 8 | Human | Binding | pEC50 | = | 5.9 | 5.9 | - | 1 | ChEMBL | 644 | 15 | 3 | 5 | 5.2 | NCCCC[C@H](NC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCC(=O)c1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.5b01965 | |||
CHEMBL3787171 | 83058 | None | 8 | Human | Binding | pEC50 | = | 5.9 | 5.9 | - | 1 | ChEMBL | 644 | 15 | 3 | 5 | 5.2 | NCCCC[C@H](NC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCC(=O)c1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.5b01965 | |||
127031899 | 139168 | None | 0 | Human | Binding | pEC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 744 | 16 | 3 | 6 | 6.7 | CC(C)(C)OC(=O)N[C@H](CCCCNC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCC(=O)c1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.5b01965 | |||
CHEMBL3786480 | 139168 | None | 0 | Human | Binding | pEC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 744 | 16 | 3 | 6 | 6.7 | CC(C)(C)OC(=O)N[C@H](CCCCNC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCC(=O)c1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.5b01965 | |||
127032750 | 139138 | None | 0 | Human | Binding | pEC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 758 | 17 | 3 | 6 | 7.1 | CC(C)(C)OC(=O)N[C@@H](CCCCNC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCCC(=O)c1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.5b01965 | |||
CHEMBL3786152 | 139138 | None | 0 | Human | Binding | pEC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 758 | 17 | 3 | 6 | 7.1 | CC(C)(C)OC(=O)N[C@@H](CCCCNC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCCC(=O)c1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.5b01965 | |||
127032164 | 139297 | None | 0 | Human | Binding | pEC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 644 | 15 | 3 | 5 | 5.2 | N[C@@H](CCCCNC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCC(=O)c1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.5b01965 | |||
CHEMBL3786535 | 139297 | None | 0 | Human | Binding | pEC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 644 | 15 | 3 | 5 | 5.2 | N[C@@H](CCCCNC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCC(=O)c1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.5b01965 | |||
CHEMBL3787716 | 139297 | None | 0 | Human | Binding | pEC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 644 | 15 | 3 | 5 | 5.2 | N[C@@H](CCCCNC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCC(=O)c1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.5b01965 | |||
127032169 | 139299 | None | 0 | Human | Binding | pEC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 484 | 11 | 4 | 4 | 3.3 | N[C@@H](CCCCNC(=O)[C@@H]1Cc2ccccc2CN1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.5b01965 | |||
CHEMBL3787326 | 139299 | None | 0 | Human | Binding | pEC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 484 | 11 | 4 | 4 | 3.3 | N[C@@H](CCCCNC(=O)[C@@H]1Cc2ccccc2CN1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.5b01965 | |||
CHEMBL3787718 | 139299 | None | 0 | Human | Binding | pEC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 484 | 11 | 4 | 4 | 3.3 | N[C@@H](CCCCNC(=O)[C@@H]1Cc2ccccc2CN1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.5b01965 | |||
127030990 | 139209 | None | 0 | Human | Binding | pEC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 682 | 15 | 3 | 6 | 5.4 | CC(=O)CCC(=O)N1Cc2ccccc2C[C@H]1C(=O)NCCCC[C@H](NC(=O)OC(C)(C)C)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.5b01965 | |||
CHEMBL3786864 | 139209 | None | 0 | Human | Binding | pEC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 682 | 15 | 3 | 6 | 5.4 | CC(=O)CCC(=O)N1Cc2ccccc2C[C@H]1C(=O)NCCCC[C@H](NC(=O)OC(C)(C)C)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.5b01965 | |||
127032750 | 139138 | None | 0 | Human | Binding | pEC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 758 | 17 | 3 | 6 | 7.1 | CC(C)(C)OC(=O)N[C@@H](CCCCNC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCCC(=O)c1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.5b01965 | |||
CHEMBL3786152 | 139138 | None | 0 | Human | Binding | pEC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 758 | 17 | 3 | 6 | 7.1 | CC(C)(C)OC(=O)N[C@@H](CCCCNC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCCC(=O)c1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.5b01965 | |||
127032166 | 139298 | None | 0 | Human | Binding | pEC50 | = | 6.7 | 6.7 | - | 0 | ChEMBL | 658 | 16 | 3 | 5 | 5.6 | N[C@@H](CCCCNC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCCC(=O)c1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.5b01965 | |||
CHEMBL3785622 | 139298 | None | 0 | Human | Binding | pEC50 | = | 6.7 | 6.7 | - | 0 | ChEMBL | 658 | 16 | 3 | 5 | 5.6 | N[C@@H](CCCCNC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCCC(=O)c1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.5b01965 | |||
CHEMBL3787717 | 139298 | None | 0 | Human | Binding | pEC50 | = | 6.7 | 6.7 | - | 0 | ChEMBL | 658 | 16 | 3 | 5 | 5.6 | N[C@@H](CCCCNC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCCC(=O)c1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.5b01965 | |||
127030984 | 139258 | None | 0 | Human | Binding | pEC50 | = | 6.7 | 6.7 | - | 0 | ChEMBL | 584 | 12 | 4 | 5 | 4.8 | CC(C)(C)OC(=O)N[C@@H](CCCCNC(=O)[C@@H]1Cc2ccccc2CN1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.5b01965 | |||
CHEMBL3787404 | 139258 | None | 0 | Human | Binding | pEC50 | = | 6.7 | 6.7 | - | 0 | ChEMBL | 584 | 12 | 4 | 5 | 4.8 | CC(C)(C)OC(=O)N[C@@H](CCCCNC(=O)[C@@H]1Cc2ccccc2CN1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.5b01965 | |||
127032455 | 139274 | None | 0 | Human | Binding | pEC50 | = | 6.7 | 6.7 | - | 0 | ChEMBL | 716 | 15 | 3 | 5 | 6.7 | CC(C)(C)OC(=O)N[C@@H](CCCCNC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCc1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.5b01965 | |||
CHEMBL3787609 | 139274 | None | 0 | Human | Binding | pEC50 | = | 6.7 | 6.7 | - | 0 | ChEMBL | 716 | 15 | 3 | 5 | 6.7 | CC(C)(C)OC(=O)N[C@@H](CCCCNC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCc1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.5b01965 | |||
127030985 | 139137 | None | 2 | Human | Binding | pEC50 | = | 6.6 | 6.6 | - | 0 | ChEMBL | 744 | 16 | 3 | 6 | 6.7 | CC(C)(C)OC(=O)N[C@@H](CCCCNC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCC(=O)c1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.5b01965 | |||
CHEMBL3786144 | 139137 | None | 2 | Human | Binding | pEC50 | = | 6.6 | 6.6 | - | 0 | ChEMBL | 744 | 16 | 3 | 6 | 6.7 | CC(C)(C)OC(=O)N[C@@H](CCCCNC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCC(=O)c1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.5b01965 | |||
127030990 | 139209 | None | 0 | Human | Binding | pEC50 | = | 6.6 | 6.6 | - | 0 | ChEMBL | 682 | 15 | 3 | 6 | 5.4 | CC(=O)CCC(=O)N1Cc2ccccc2C[C@H]1C(=O)NCCCC[C@H](NC(=O)OC(C)(C)C)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.5b01965 | |||
CHEMBL3786864 | 139209 | None | 0 | Human | Binding | pEC50 | = | 6.6 | 6.6 | - | 0 | ChEMBL | 682 | 15 | 3 | 6 | 5.4 | CC(=O)CCC(=O)N1Cc2ccccc2C[C@H]1C(=O)NCCCC[C@H](NC(=O)OC(C)(C)C)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.5b01965 | |||
127032486 | 139188 | None | 0 | Human | Binding | pEC50 | = | 6.6 | 6.6 | - | 0 | ChEMBL | 744 | 16 | 3 | 6 | 6.7 | CC(C)(C)OC(=O)NCCCC[C@@H](NC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCC(=O)c1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.5b01965 | |||
CHEMBL3786631 | 139188 | None | 0 | Human | Binding | pEC50 | = | 6.6 | 6.6 | - | 0 | ChEMBL | 744 | 16 | 3 | 6 | 6.7 | CC(C)(C)OC(=O)NCCCC[C@@H](NC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCC(=O)c1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.5b01965 | |||
127030985 | 139137 | None | 2 | Human | Binding | pEC50 | = | 6.6 | 6.6 | - | 0 | ChEMBL | 744 | 16 | 3 | 6 | 6.7 | CC(C)(C)OC(=O)N[C@@H](CCCCNC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCC(=O)c1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.5b01965 | |||
CHEMBL3786144 | 139137 | None | 2 | Human | Binding | pEC50 | = | 6.6 | 6.6 | - | 0 | ChEMBL | 744 | 16 | 3 | 6 | 6.7 | CC(C)(C)OC(=O)N[C@@H](CCCCNC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCC(=O)c1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.5b01965 | |||
127032169 | 139299 | None | 0 | Human | Binding | pEC50 | = | 6.6 | 6.6 | - | 0 | ChEMBL | 484 | 11 | 4 | 4 | 3.3 | N[C@@H](CCCCNC(=O)[C@@H]1Cc2ccccc2CN1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.5b01965 | |||
CHEMBL3787326 | 139299 | None | 0 | Human | Binding | pEC50 | = | 6.6 | 6.6 | - | 0 | ChEMBL | 484 | 11 | 4 | 4 | 3.3 | N[C@@H](CCCCNC(=O)[C@@H]1Cc2ccccc2CN1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.5b01965 | |||
CHEMBL3787718 | 139299 | None | 0 | Human | Binding | pEC50 | = | 6.6 | 6.6 | - | 0 | ChEMBL | 484 | 11 | 4 | 4 | 3.3 | N[C@@H](CCCCNC(=O)[C@@H]1Cc2ccccc2CN1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.5b01965 | |||
127031901 | 139300 | None | 0 | Human | Binding | pEC50 | = | 6.5 | 6.5 | - | 0 | ChEMBL | 644 | 15 | 3 | 5 | 5.2 | N[C@H](CCCCNC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCC(=O)c1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.5b01965 | |||
CHEMBL3787077 | 139300 | None | 0 | Human | Binding | pEC50 | = | 6.5 | 6.5 | - | 0 | ChEMBL | 644 | 15 | 3 | 5 | 5.2 | N[C@H](CCCCNC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCC(=O)c1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.5b01965 | |||
CHEMBL3787719 | 139300 | None | 0 | Human | Binding | pEC50 | = | 6.5 | 6.5 | - | 0 | ChEMBL | 644 | 15 | 3 | 5 | 5.2 | N[C@H](CCCCNC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCC(=O)c1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.5b01965 | |||
127032164 | 139297 | None | 0 | Human | Binding | pEC50 | = | 6.5 | 6.5 | - | 0 | ChEMBL | 644 | 15 | 3 | 5 | 5.2 | N[C@@H](CCCCNC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCC(=O)c1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.5b01965 | |||
CHEMBL3786535 | 139297 | None | 0 | Human | Binding | pEC50 | = | 6.5 | 6.5 | - | 0 | ChEMBL | 644 | 15 | 3 | 5 | 5.2 | N[C@@H](CCCCNC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCC(=O)c1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.5b01965 | |||
CHEMBL3787716 | 139297 | None | 0 | Human | Binding | pEC50 | = | 6.5 | 6.5 | - | 0 | ChEMBL | 644 | 15 | 3 | 5 | 5.2 | N[C@@H](CCCCNC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCC(=O)c1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.5b01965 | |||
127030984 | 139258 | None | 0 | Human | Binding | pEC50 | = | 6.5 | 6.5 | - | 0 | ChEMBL | 584 | 12 | 4 | 5 | 4.8 | CC(C)(C)OC(=O)N[C@@H](CCCCNC(=O)[C@@H]1Cc2ccccc2CN1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.5b01965 | |||
CHEMBL3787404 | 139258 | None | 0 | Human | Binding | pEC50 | = | 6.5 | 6.5 | - | 0 | ChEMBL | 584 | 12 | 4 | 5 | 4.8 | CC(C)(C)OC(=O)N[C@@H](CCCCNC(=O)[C@@H]1Cc2ccccc2CN1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.5b01965 | |||
127032486 | 139188 | None | 0 | Human | Binding | pEC50 | = | 7.2 | 7.2 | - | 0 | ChEMBL | 744 | 16 | 3 | 6 | 6.7 | CC(C)(C)OC(=O)NCCCC[C@@H](NC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCC(=O)c1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.5b01965 | |||
CHEMBL3786631 | 139188 | None | 0 | Human | Binding | pEC50 | = | 7.2 | 7.2 | - | 0 | ChEMBL | 744 | 16 | 3 | 6 | 6.7 | CC(C)(C)OC(=O)NCCCC[C@@H](NC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCC(=O)c1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.5b01965 | |||
127032455 | 139274 | None | 0 | Human | Binding | pEC50 | = | 7.2 | 7.2 | - | 0 | ChEMBL | 716 | 15 | 3 | 5 | 6.7 | CC(C)(C)OC(=O)N[C@@H](CCCCNC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCc1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.5b01965 | |||
CHEMBL3787609 | 139274 | None | 0 | Human | Binding | pEC50 | = | 7.2 | 7.2 | - | 0 | ChEMBL | 716 | 15 | 3 | 5 | 6.7 | CC(C)(C)OC(=O)N[C@@H](CCCCNC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCc1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.5b01965 | |||
127031901 | 139300 | None | 0 | Human | Binding | pEC50 | = | 7.2 | 7.2 | - | 0 | ChEMBL | 644 | 15 | 3 | 5 | 5.2 | N[C@H](CCCCNC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCC(=O)c1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.5b01965 | |||
CHEMBL3787077 | 139300 | None | 0 | Human | Binding | pEC50 | = | 7.2 | 7.2 | - | 0 | ChEMBL | 644 | 15 | 3 | 5 | 5.2 | N[C@H](CCCCNC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCC(=O)c1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.5b01965 | |||
CHEMBL3787719 | 139300 | None | 0 | Human | Binding | pEC50 | = | 7.2 | 7.2 | - | 0 | ChEMBL | 644 | 15 | 3 | 5 | 5.2 | N[C@H](CCCCNC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCC(=O)c1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.5b01965 | |||
127030694 | 139302 | None | 0 | Human | Binding | pEC50 | = | 6.1 | 6.1 | - | 0 | ChEMBL | 644 | 15 | 3 | 5 | 5.2 | NCCCC[C@@H](NC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCC(=O)c1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.5b01965 | |||
CHEMBL3786670 | 139302 | None | 0 | Human | Binding | pEC50 | = | 6.1 | 6.1 | - | 0 | ChEMBL | 644 | 15 | 3 | 5 | 5.2 | NCCCC[C@@H](NC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCC(=O)c1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.5b01965 | |||
CHEMBL3787750 | 139302 | None | 0 | Human | Binding | pEC50 | = | 6.1 | 6.1 | - | 0 | ChEMBL | 644 | 15 | 3 | 5 | 5.2 | NCCCC[C@@H](NC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCC(=O)c1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.5b01965 | |||
71657827 | 144431 | None | 0 | Human | Binding | pIC50 | = | 10 | 10.0 | - | 0 | ChEMBL | 547 | 6 | 2 | 9 | 3.2 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4cc(CCN)ccc4[nH]3)C[C@H]2C)n1 | nan | |||
CHEMBL3905581 | 144431 | None | 0 | Human | Binding | pIC50 | = | 10 | 10.0 | - | 0 | ChEMBL | 547 | 6 | 2 | 9 | 3.2 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4cc(CCN)ccc4[nH]3)C[C@H]2C)n1 | nan | |||
117739261 | 146893 | None | 0 | Human | Binding | pIC50 | = | 10 | 10.0 | - | 0 | ChEMBL | 509 | 4 | 1 | 7 | 4.3 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cc(Cl)cn1 | nan | |||
CHEMBL3924716 | 146893 | None | 0 | Human | Binding | pIC50 | = | 10 | 10.0 | - | 0 | ChEMBL | 509 | 4 | 1 | 7 | 4.3 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cc(Cl)cn1 | nan | |||
117739838 | 149295 | None | 0 | Human | Binding | pIC50 | = | 10 | 10.0 | - | 0 | ChEMBL | 489 | 4 | 1 | 7 | 3.9 | Cc1ccnn1CC(=O)N1CCN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)C[C@H]1C | nan | |||
CHEMBL3944008 | 149295 | None | 0 | Human | Binding | pIC50 | = | 10 | 10.0 | - | 0 | ChEMBL | 489 | 4 | 1 | 7 | 3.9 | Cc1ccnn1CC(=O)N1CCN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)C[C@H]1C | nan | |||
71680304 | 148497 | None | 0 | Human | Binding | pIC50 | = | 9.7 | 9.7 | - | 0 | ChEMBL | 457 | 4 | 1 | 7 | 3.8 | C[C@H]1CN(c2scnc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1ccc2cccnc21 | 10.1021/acs.jmedchem.5b01337 | |||
CHEMBL3937630 | 148497 | None | 0 | Human | Binding | pIC50 | = | 9.7 | 9.7 | - | 0 | ChEMBL | 457 | 4 | 1 | 7 | 3.8 | C[C@H]1CN(c2scnc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1ccc2cccnc21 | 10.1021/acs.jmedchem.5b01337 | |||
11569938 | 58238 | None | 0 | Human | Binding | pIC50 | = | 9.7 | 9.7 | - | 1 | ChEMBL | 521 | 7 | 1 | 5 | 4.8 | CCNC(=O)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4F)CC3)[C@@H](CC)C2)c(Cl)c1 | 10.1016/j.bmcl.2014.01.009 | |||
CHEMBL1681882 | 58238 | None | 0 | Human | Binding | pIC50 | = | 9.7 | 9.7 | - | 1 | ChEMBL | 521 | 7 | 1 | 5 | 4.8 | CCNC(=O)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4F)CC3)[C@@H](CC)C2)c(Cl)c1 | 10.1016/j.bmcl.2014.01.009 | |||
71679472 | 143622 | None | 0 | Human | Binding | pIC50 | = | 9.7 | 9.7 | - | 0 | ChEMBL | 491 | 4 | 1 | 7 | 4.4 | C[C@@H]1CN(c2scnc2-c2nc3ccc(Cl)cc3[nH]2)CCN1C(=O)Cn1ccc2cccnc21 | nan | |||
CHEMBL3898933 | 143622 | None | 0 | Human | Binding | pIC50 | = | 9.7 | 9.7 | - | 0 | ChEMBL | 491 | 4 | 1 | 7 | 4.4 | C[C@@H]1CN(c2scnc2-c2nc3ccc(Cl)cc3[nH]2)CCN1C(=O)Cn1ccc2cccnc21 | nan | |||
117739723 | 145360 | None | 0 | Human | Binding | pIC50 | = | 9.7 | 9.7 | - | 0 | ChEMBL | 489 | 4 | 1 | 7 | 3.9 | Cc1ccn(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccccc4[nH]3)C[C@H]2C)n1 | nan | |||
CHEMBL3912920 | 145360 | None | 0 | Human | Binding | pIC50 | = | 9.7 | 9.7 | - | 0 | ChEMBL | 489 | 4 | 1 | 7 | 3.9 | Cc1ccn(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccccc4[nH]3)C[C@H]2C)n1 | nan | |||
124037277 | 149983 | None | 0 | Human | Binding | pIC50 | = | 9.7 | 9.7 | - | 0 | ChEMBL | 457 | 4 | 1 | 7 | 3.8 | C[C@@H]1CN(c2scnc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1ccc2ccncc21 | nan | |||
CHEMBL3949279 | 149983 | None | 0 | Human | Binding | pIC50 | = | 9.7 | 9.7 | - | 0 | ChEMBL | 457 | 4 | 1 | 7 | 3.8 | C[C@@H]1CN(c2scnc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1ccc2ccncc21 | nan | |||
59772541 | 105412 | None | 0 | Human | Binding | pIC50 | = | 9.5 | 9.5 | - | 0 | ChEMBL | 516 | 6 | 1 | 5 | 5.5 | CC[C@H]1CN(c2ncc(-c3ncc[nH]3)cc2Cl)CCN1C1CCN(Cc2ccc(Cl)cc2F)CC1 | 10.1016/j.bmcl.2014.01.009 | |||
CHEMBL3116468 | 105412 | None | 0 | Human | Binding | pIC50 | = | 9.5 | 9.5 | - | 0 | ChEMBL | 516 | 6 | 1 | 5 | 5.5 | CC[C@H]1CN(c2ncc(-c3ncc[nH]3)cc2Cl)CCN1C1CCN(Cc2ccc(Cl)cc2F)CC1 | 10.1016/j.bmcl.2014.01.009 | |||
11997695 | 68731 | None | 0 | Human | Binding | pIC50 | = | 9.5 | 9.5 | - | 0 | ChEMBL | 505 | 6 | 2 | 7 | 3.3 | CC[C@H]1CN(c2nc(N)c(C(=O)NC)nc2Cl)CCN1C1CCN(Cc2ccc(Cl)cc2)CC1 | 10.1016/j.bmcl.2011.09.120 | |||
CHEMBL1921863 | 68731 | None | 0 | Human | Binding | pIC50 | = | 9.5 | 9.5 | - | 0 | ChEMBL | 505 | 6 | 2 | 7 | 3.3 | CC[C@H]1CN(c2nc(N)c(C(=O)NC)nc2Cl)CCN1C1CCN(Cc2ccc(Cl)cc2)CC1 | 10.1016/j.bmcl.2011.09.120 | |||
11997995 | 68734 | None | 0 | Human | Binding | pIC50 | = | 9.5 | 9.5 | - | 0 | ChEMBL | 549 | 8 | 3 | 8 | 3.0 | CC[C@H]1CN(c2nc(N)c(C(=O)NCC(C)O)nc2Cl)CCN1C1CCN(Cc2ccc(Cl)cc2)CC1 | 10.1016/j.bmcl.2011.09.120 | |||
CHEMBL1921866 | 68734 | None | 0 | Human | Binding | pIC50 | = | 9.5 | 9.5 | - | 0 | ChEMBL | 549 | 8 | 3 | 8 | 3.0 | CC[C@H]1CN(c2nc(N)c(C(=O)NCC(C)O)nc2Cl)CCN1C1CCN(Cc2ccc(Cl)cc2)CC1 | 10.1016/j.bmcl.2011.09.120 | |||
44592137 | 179284 | None | 5 | Human | Binding | pIC50 | = | 9.5 | 9.5 | - | 1 | ChEMBL | 503 | 7 | 1 | 5 | 4.7 | CCNC(=O)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4)CC3)[C@@H](CC)C2)c(Cl)c1 | 10.1016/j.bmcl.2011.09.120 | |||
CHEMBL472288 | 179284 | None | 5 | Human | Binding | pIC50 | = | 9.5 | 9.5 | - | 1 | ChEMBL | 503 | 7 | 1 | 5 | 4.7 | CCNC(=O)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4)CC3)[C@@H](CC)C2)c(Cl)c1 | 10.1016/j.bmcl.2011.09.120 | |||
89726471 | 143666 | None | 0 | Human | Binding | pIC50 | = | 9.5 | 9.5 | - | 0 | ChEMBL | 527 | 4 | 1 | 9 | 3.6 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3cccnc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | nan | |||
CHEMBL3899279 | 143666 | None | 0 | Human | Binding | pIC50 | = | 9.5 | 9.5 | - | 0 | ChEMBL | 527 | 4 | 1 | 9 | 3.6 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3cccnc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | nan | |||
89726634 | 144900 | None | 0 | Human | Binding | pIC50 | = | 9.5 | 9.5 | - | 0 | ChEMBL | 508 | 4 | 1 | 6 | 3.9 | C[C@@H]1CN(c2scnc2-c2nc3ccccc3[nH]2)CCN1C(=O)CN1C(=O)C(F)(F)c2ccccc21 | nan | |||
CHEMBL3909429 | 144900 | None | 0 | Human | Binding | pIC50 | = | 9.5 | 9.5 | - | 0 | ChEMBL | 508 | 4 | 1 | 6 | 3.9 | C[C@@H]1CN(c2scnc2-c2nc3ccccc3[nH]2)CCN1C(=O)CN1C(=O)C(F)(F)c2ccccc21 | nan | |||
11997761 | 105420 | None | 0 | Human | Binding | pIC50 | = | 9.4 | 9.4 | - | 0 | ChEMBL | 530 | 6 | 1 | 9 | 4.3 | CC[C@H]1CN(c2nc(N)c(-c3nnc(C)o3)nc2Cl)CCN1C1CCN(Cc2ccc(Cl)cc2)CC1 | 10.1016/j.bmcl.2014.01.009 | |||
CHEMBL3116476 | 105420 | None | 0 | Human | Binding | pIC50 | = | 9.4 | 9.4 | - | 0 | ChEMBL | 530 | 6 | 1 | 9 | 4.3 | CC[C@H]1CN(c2nc(N)c(-c3nnc(C)o3)nc2Cl)CCN1C1CCN(Cc2ccc(Cl)cc2)CC1 | 10.1016/j.bmcl.2014.01.009 | |||
11997845 | 68733 | None | 0 | Human | Binding | pIC50 | = | 9.4 | 9.4 | - | 0 | ChEMBL | 535 | 8 | 3 | 8 | 2.7 | CC[C@H]1CN(c2nc(N)c(C(=O)NCCO)nc2Cl)CCN1C1CCN(Cc2ccc(Cl)cc2)CC1 | 10.1016/j.bmcl.2011.09.120 | |||
CHEMBL1921865 | 68733 | None | 0 | Human | Binding | pIC50 | = | 9.4 | 9.4 | - | 0 | ChEMBL | 535 | 8 | 3 | 8 | 2.7 | CC[C@H]1CN(c2nc(N)c(C(=O)NCCO)nc2Cl)CCN1C1CCN(Cc2ccc(Cl)cc2)CC1 | 10.1016/j.bmcl.2011.09.120 | |||
44455751 | 95388 | None | 0 | Human | Binding | pIC50 | = | 9.4 | 9.4 | - | 0 | ChEMBL | 631 | 12 | 0 | 6 | 6.7 | CCOc1ccc(-n2cc(-c3ccccc3)nc2[C@@H](C)N(CCS(=O)(=O)CC)C(=O)Cc2ccc(F)c(C(F)(F)F)c2)cc1 | 10.1016/j.bmcl.2007.11.072 | |||
CHEMBL256589 | 95388 | None | 0 | Human | Binding | pIC50 | = | 9.4 | 9.4 | - | 0 | ChEMBL | 631 | 12 | 0 | 6 | 6.7 | CCOc1ccc(-n2cc(-c3ccccc3)nc2[C@@H](C)N(CCS(=O)(=O)CC)C(=O)Cc2ccc(F)c(C(F)(F)F)c2)cc1 | 10.1016/j.bmcl.2007.11.072 | |||
71679476 | 143077 | None | 0 | Human | Binding | pIC50 | = | 9.4 | 9.4 | - | 0 | ChEMBL | 494 | 4 | 1 | 8 | 3.4 | C[C@@H]1CN(c2scnc2-c2nc3cc(F)c(F)cc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | nan | |||
CHEMBL3894522 | 143077 | None | 0 | Human | Binding | pIC50 | = | 9.4 | 9.4 | - | 0 | ChEMBL | 494 | 4 | 1 | 8 | 3.4 | C[C@@H]1CN(c2scnc2-c2nc3cc(F)c(F)cc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | nan | |||
117740323 | 152487 | None | 0 | Human | Binding | pIC50 | = | 9.4 | 9.4 | - | 0 | ChEMBL | 500 | 4 | 1 | 6 | 4.7 | Cc1ccc(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccccc4[nH]3)C[C@H]2C)cn1 | nan | |||
CHEMBL3970456 | 152487 | None | 0 | Human | Binding | pIC50 | = | 9.4 | 9.4 | - | 0 | ChEMBL | 500 | 4 | 1 | 6 | 4.7 | Cc1ccc(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccccc4[nH]3)C[C@H]2C)cn1 | nan | |||
71679314 | 152569 | None | 0 | Human | Binding | pIC50 | = | 9.3 | 9.3 | - | 0 | ChEMBL | 506 | 4 | 1 | 8 | 4.1 | Cc1c(Cl)ccc2[nH]c(-c3ncsc3N3CCN(C(=O)Cn4cnc5cccnc54)[C@H](C)C3)nc12 | nan | |||
CHEMBL3971111 | 152569 | None | 0 | Human | Binding | pIC50 | = | 9.3 | 9.3 | - | 0 | ChEMBL | 506 | 4 | 1 | 8 | 4.1 | Cc1c(Cl)ccc2[nH]c(-c3ncsc3N3CCN(C(=O)Cn4cnc5cccnc54)[C@H](C)C3)nc12 | nan | |||
117740035 | 153942 | None | 0 | Human | Binding | pIC50 | = | 9.3 | 9.3 | - | 0 | ChEMBL | 475 | 4 | 1 | 7 | 3.6 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cccn1 | nan | |||
CHEMBL3982804 | 153942 | None | 0 | Human | Binding | pIC50 | = | 9.3 | 9.3 | - | 0 | ChEMBL | 475 | 4 | 1 | 7 | 3.6 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cccn1 | nan | |||
71679312 | 154367 | None | 0 | Human | Binding | pIC50 | = | 9.3 | 9.3 | - | 0 | ChEMBL | 476 | 4 | 1 | 8 | 3.3 | C[C@@H]1CN(c2scnc2-c2nc3cc(F)ccc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | nan | |||
CHEMBL3986477 | 154367 | None | 0 | Human | Binding | pIC50 | = | 9.3 | 9.3 | - | 0 | ChEMBL | 476 | 4 | 1 | 8 | 3.3 | C[C@@H]1CN(c2scnc2-c2nc3cc(F)ccc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | nan | |||
44455604 | 155404 | None | 0 | Human | Binding | pIC50 | = | 9.2 | 9.2 | - | 0 | ChEMBL | 612 | 10 | 0 | 6 | 6.1 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc(-c2ccccc2)cn1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2009.07.021 | |||
CHEMBL403036 | 155404 | None | 0 | Human | Binding | pIC50 | = | 9.2 | 9.2 | - | 0 | ChEMBL | 612 | 10 | 0 | 6 | 6.1 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc(-c2ccccc2)cn1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2009.07.021 | |||
44455604 | 155404 | None | 0 | Human | Binding | pIC50 | = | 9.2 | 9.2 | - | 0 | ChEMBL | 612 | 10 | 0 | 6 | 6.1 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc(-c2ccccc2)cn1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2007.11.072 | |||
CHEMBL403036 | 155404 | None | 0 | Human | Binding | pIC50 | = | 9.2 | 9.2 | - | 0 | ChEMBL | 612 | 10 | 0 | 6 | 6.1 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc(-c2ccccc2)cn1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2007.11.072 | |||
11995774 | 68726 | None | 36 | Human | Binding | pIC50 | = | 9.1 | 9.1 | - | 1 | ChEMBL | 491 | 6 | 2 | 7 | 3.0 | CC[C@H]1CN(c2nc(N)c(C(N)=O)nc2Cl)CCN1C1CCN(Cc2ccc(Cl)cc2)CC1 | 10.1016/j.bmcl.2014.01.009 | |||
CHEMBL1921858 | 68726 | None | 36 | Human | Binding | pIC50 | = | 9.1 | 9.1 | - | 1 | ChEMBL | 491 | 6 | 2 | 7 | 3.0 | CC[C@H]1CN(c2nc(N)c(C(N)=O)nc2Cl)CCN1C1CCN(Cc2ccc(Cl)cc2)CC1 | 10.1016/j.bmcl.2014.01.009 | |||
11997912 | 105431 | None | 0 | Human | Binding | pIC50 | = | 9.1 | 9.1 | - | 0 | ChEMBL | 574 | 7 | 2 | 11 | 3.4 | CCNc1nnc(-c2cnc(N3CCN(C4CCN(C(=O)c5ccc(Cl)nc5N)CC4)[C@@H](CC)C3)c(Cl)n2)o1 | 10.1016/j.bmcl.2014.01.009 | |||
CHEMBL3116487 | 105431 | None | 0 | Human | Binding | pIC50 | = | 9.1 | 9.1 | - | 0 | ChEMBL | 574 | 7 | 2 | 11 | 3.4 | CCNc1nnc(-c2cnc(N3CCN(C4CCN(C(=O)c5ccc(Cl)nc5N)CC4)[C@@H](CC)C3)c(Cl)n2)o1 | 10.1016/j.bmcl.2014.01.009 | |||
11995774 | 68726 | None | 36 | Human | Binding | pIC50 | = | 9.1 | 9.1 | - | 1 | ChEMBL | 491 | 6 | 2 | 7 | 3.0 | CC[C@H]1CN(c2nc(N)c(C(N)=O)nc2Cl)CCN1C1CCN(Cc2ccc(Cl)cc2)CC1 | 10.1016/j.bmcl.2011.09.120 | |||
CHEMBL1921858 | 68726 | None | 36 | Human | Binding | pIC50 | = | 9.1 | 9.1 | - | 1 | ChEMBL | 491 | 6 | 2 | 7 | 3.0 | CC[C@H]1CN(c2nc(N)c(C(N)=O)nc2Cl)CCN1C1CCN(Cc2ccc(Cl)cc2)CC1 | 10.1016/j.bmcl.2011.09.120 | |||
11997994 | 68732 | None | 0 | Human | Binding | pIC50 | = | 9.1 | 9.1 | - | 0 | ChEMBL | 573 | 7 | 2 | 7 | 4.2 | CC[C@H]1CN(c2nc(N)c(C(=O)NCC(F)(F)F)nc2Cl)CCN1C1CCN(Cc2ccc(Cl)cc2)CC1 | 10.1016/j.bmcl.2011.09.120 | |||
CHEMBL1921864 | 68732 | None | 0 | Human | Binding | pIC50 | = | 9.1 | 9.1 | - | 0 | ChEMBL | 573 | 7 | 2 | 7 | 4.2 | CC[C@H]1CN(c2nc(N)c(C(=O)NCC(F)(F)F)nc2Cl)CCN1C1CCN(Cc2ccc(Cl)cc2)CC1 | 10.1016/j.bmcl.2011.09.120 | |||
44447090 | 94942 | None | 0 | Human | Binding | pIC50 | = | 9.1 | 9.1 | - | 0 | ChEMBL | 597 | 9 | 0 | 5 | 6.5 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc2ccccc2cc1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2007.11.060 | |||
CHEMBL254083 | 94942 | None | 0 | Human | Binding | pIC50 | = | 9.1 | 9.1 | - | 0 | ChEMBL | 597 | 9 | 0 | 5 | 6.5 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc2ccccc2cc1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2007.11.060 | |||
57392574 | 68736 | None | 0 | Human | Binding | pIC50 | = | 9.1 | 9.1 | - | 0 | ChEMBL | 666 | 10 | 3 | 9 | 3.1 | CC[C@H]1CN(c2nc(N)c(C(=O)NCCNS(=O)(=O)C(F)(F)F)nc2Cl)CCN1C1CCN(Cc2ccc(Cl)cc2)CC1 | 10.1016/j.bmcl.2011.09.120 | |||
CHEMBL1921868 | 68736 | None | 0 | Human | Binding | pIC50 | = | 9.1 | 9.1 | - | 0 | ChEMBL | 666 | 10 | 3 | 9 | 3.1 | CC[C@H]1CN(c2nc(N)c(C(=O)NCCNS(=O)(=O)C(F)(F)F)nc2Cl)CCN1C1CCN(Cc2ccc(Cl)cc2)CC1 | 10.1016/j.bmcl.2011.09.120 | |||
57390765 | 68747 | None | 0 | Human | Binding | pIC50 | = | 9.1 | 9.1 | - | 0 | ChEMBL | 548 | 6 | 2 | 8 | 3.1 | CC[C@H]1CN(c2ncc(C(=O)NC(C)C)nc2Cl)CCN1C1CCN(C(=O)c2ccc(Cl)nc2N)CC1 | 10.1016/j.bmcl.2011.09.120 | |||
CHEMBL1921879 | 68747 | None | 0 | Human | Binding | pIC50 | = | 9.1 | 9.1 | - | 0 | ChEMBL | 548 | 6 | 2 | 8 | 3.1 | CC[C@H]1CN(c2ncc(C(=O)NC(C)C)nc2Cl)CCN1C1CCN(C(=O)c2ccc(Cl)nc2N)CC1 | 10.1016/j.bmcl.2011.09.120 | |||
45486526 | 200066 | None | 0 | Human | Binding | pIC50 | = | 9.1 | 9.1 | - | 0 | ChEMBL | 627 | 10 | 0 | 7 | 5.9 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(C(F)(F)F)c(F)c1)[C@H](C)c1nc2c(C3CC3)nccn2c1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2009.07.021 | |||
CHEMBL570665 | 200066 | None | 0 | Human | Binding | pIC50 | = | 9.1 | 9.1 | - | 0 | ChEMBL | 627 | 10 | 0 | 7 | 5.9 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(C(F)(F)F)c(F)c1)[C@H](C)c1nc2c(C3CC3)nccn2c1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2009.07.021 | |||
45486531 | 200770 | None | 0 | Human | Binding | pIC50 | = | 9.1 | 9.1 | - | 0 | ChEMBL | 653 | 8 | 0 | 7 | 6.3 | C[C@H](c1nc2c(C3CC3)nccn2c1-c1ccc(C#N)cc1)N(CC1CCS(=O)(=O)CC1)C(=O)Cc1ccc(F)c(C(F)(F)F)c1 | 10.1016/j.bmcl.2009.07.021 | |||
CHEMBL576097 | 200770 | None | 0 | Human | Binding | pIC50 | = | 9.1 | 9.1 | - | 0 | ChEMBL | 653 | 8 | 0 | 7 | 6.3 | C[C@H](c1nc2c(C3CC3)nccn2c1-c1ccc(C#N)cc1)N(CC1CCS(=O)(=O)CC1)C(=O)Cc1ccc(F)c(C(F)(F)F)c1 | 10.1016/j.bmcl.2009.07.021 | |||
45486523 | 201007 | None | 0 | Human | Binding | pIC50 | = | 9.1 | 9.1 | - | 0 | ChEMBL | 617 | 10 | 0 | 8 | 5.0 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(C(F)(F)F)c(F)c1)[C@H](C)c1nc2c(OC)nccn2c1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2009.07.021 | |||
CHEMBL578187 | 201007 | None | 0 | Human | Binding | pIC50 | = | 9.1 | 9.1 | - | 0 | ChEMBL | 617 | 10 | 0 | 8 | 5.0 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(C(F)(F)F)c(F)c1)[C@H](C)c1nc2c(OC)nccn2c1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2009.07.021 | |||
45379650 | 201011 | None | 0 | Human | Binding | pIC50 | = | 9.1 | 9.1 | - | 0 | ChEMBL | 653 | 8 | 0 | 7 | 6.3 | C[C@H](c1nc2c(C3CC3)nccn2c1-c1ccc(C#N)cc1)N(CC1CCS(=O)(=O)CC1)C(=O)Cc1ccc(C(F)(F)F)c(F)c1 | 10.1016/j.bmcl.2009.07.021 | |||
CHEMBL578192 | 201011 | None | 0 | Human | Binding | pIC50 | = | 9.1 | 9.1 | - | 0 | ChEMBL | 653 | 8 | 0 | 7 | 6.3 | C[C@H](c1nc2c(C3CC3)nccn2c1-c1ccc(C#N)cc1)N(CC1CCS(=O)(=O)CC1)C(=O)Cc1ccc(C(F)(F)F)c(F)c1 | 10.1016/j.bmcl.2009.07.021 | |||
11995700 | 105430 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 589 | 7 | 3 | 12 | 3.0 | CCNc1nnc(-c2nc(Cl)c(N3CCN(C4CCN(C(=O)c5ccc(Cl)nc5N)CC4)[C@@H](CC)C3)nc2N)o1 | 10.1016/j.bmcl.2014.01.009 | |||
CHEMBL3116486 | 105430 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 589 | 7 | 3 | 12 | 3.0 | CCNc1nnc(-c2nc(Cl)c(N3CCN(C4CCN(C(=O)c5ccc(Cl)nc5N)CC4)[C@@H](CC)C3)nc2N)o1 | 10.1016/j.bmcl.2014.01.009 | |||
46883308 | 5669 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 639 | 9 | 0 | 7 | 6.3 | CCOc1ccc(-n2c([C@@H](C)N(C(=O)Cc3ccc(F)c(C(F)(F)F)c3)C3CCN(C(C)C)CC3)nc3ncccc3c2=O)cc1 | 10.1016/j.bmcl.2009.07.032 | |||
CHEMBL1077828 | 5669 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 639 | 9 | 0 | 7 | 6.3 | CCOc1ccc(-n2c([C@@H](C)N(C(=O)Cc3ccc(F)c(C(F)(F)F)c3)C3CCN(C(C)C)CC3)nc3ncccc3c2=O)cc1 | 10.1016/j.bmcl.2009.07.032 | |||
46883311 | 5671 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 634 | 11 | 0 | 8 | 4.9 | CCOc1ccc(-n2c([C@@H](C)N(CCS(=O)(=O)CC)C(=O)Cc3ccc(F)c(C(F)(F)F)c3)nc3ncccc3c2=O)cc1 | 10.1016/j.bmcl.2009.07.032 | |||
CHEMBL1077830 | 5671 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 634 | 11 | 0 | 8 | 4.9 | CCOc1ccc(-n2c([C@@H](C)N(CCS(=O)(=O)CC)C(=O)Cc3ccc(F)c(C(F)(F)F)c3)nc3ncccc3c2=O)cc1 | 10.1016/j.bmcl.2009.07.032 | |||
45101529 | 5672 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 688 | 11 | 0 | 8 | 5.4 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc2ncccc2c(=O)n1-c1ccc(OCC(F)(F)F)cc1 | 10.1016/j.bmcl.2009.07.032 | |||
CHEMBL1077831 | 5672 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 688 | 11 | 0 | 8 | 5.4 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc2ncccc2c(=O)n1-c1ccc(OCC(F)(F)F)cc1 | 10.1016/j.bmcl.2009.07.032 | |||
45101529 | 5672 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 688 | 11 | 0 | 8 | 5.4 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc2ncccc2c(=O)n1-c1ccc(OCC(F)(F)F)cc1 | 10.1016/j.bmcl.2009.07.032 | |||
CHEMBL1077831 | 5672 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 688 | 11 | 0 | 8 | 5.4 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc2ncccc2c(=O)n1-c1ccc(OCC(F)(F)F)cc1 | 10.1016/j.bmcl.2009.07.032 | |||
44455870 | 155604 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 604 | 9 | 0 | 6 | 6.7 | CCOc1ccc(-n2c([C@@H](C)N(Cc3cccnc3)C(=O)Cc3ccc(F)c(C(F)(F)F)c3)nc3ccccc3c2=O)cc1 | 10.1016/j.bmcl.2007.11.072 | |||
CHEMBL404201 | 155604 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 604 | 9 | 0 | 6 | 6.7 | CCOc1ccc(-n2c([C@@H](C)N(Cc3cccnc3)C(=O)Cc3ccc(F)c(C(F)(F)F)c3)nc3ccccc3c2=O)cc1 | 10.1016/j.bmcl.2007.11.072 | |||
71679478 | 142496 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 510 | 4 | 1 | 8 | 4.0 | C[C@@H]1CN(c2scnc2-c2nc3cc(Cl)c(F)cc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | nan | |||
CHEMBL3889786 | 142496 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 510 | 4 | 1 | 8 | 4.0 | C[C@@H]1CN(c2scnc2-c2nc3cc(Cl)c(F)cc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | nan | |||
89726146 | 142560 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 528 | 4 | 1 | 10 | 3.0 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3cncnc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | nan | |||
CHEMBL3890323 | 142560 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 528 | 4 | 1 | 10 | 3.0 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3cncnc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | nan | |||
89726440 | 142782 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 522 | 4 | 1 | 8 | 3.8 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4c(F)cccc4[nH]3)C[C@H]2C)n1 | nan | |||
CHEMBL3892103 | 142782 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 522 | 4 | 1 | 8 | 3.8 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4c(F)cccc4[nH]3)C[C@H]2C)n1 | nan | |||
89726592 | 143170 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 498 | 5 | 1 | 8 | 4.0 | C[C@@H]1CN(c2scnc2-c2nc3ccc(C4CC4)cc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | nan | |||
CHEMBL3895316 | 143170 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 498 | 5 | 1 | 8 | 4.0 | C[C@@H]1CN(c2scnc2-c2nc3ccc(C4CC4)cc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | nan | |||
89725785 | 143189 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 486 | 5 | 1 | 8 | 3.7 | CCc1nc(-c2nc3ccccc3[nH]2)c(N2CCN(C(=O)Cn3cnc4cccnc43)[C@H](C)C2)s1 | nan | |||
CHEMBL3895485 | 143189 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 486 | 5 | 1 | 8 | 3.7 | CCc1nc(-c2nc3ccccc3[nH]2)c(N2CCN(C(=O)Cn3cnc4cccnc43)[C@H](C)C2)s1 | nan | |||
71678462 | 143306 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 506 | 4 | 1 | 8 | 4.2 | C[C@H]1CN(c2scnc2-c2nc3cc(Cl)ccc3[nH]2)C[C@@H](C)N1C(=O)Cn1cnc2cccnc21 | nan | |||
CHEMBL3896434 | 143306 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 506 | 4 | 1 | 8 | 4.2 | C[C@H]1CN(c2scnc2-c2nc3cc(Cl)ccc3[nH]2)C[C@@H](C)N1C(=O)Cn1cnc2cccnc21 | nan | |||
117739850 | 143894 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 490 | 4 | 1 | 8 | 3.3 | Cc1ncn(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccccc4[nH]3)C[C@H]2C)n1 | nan | |||
CHEMBL3901259 | 143894 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 490 | 4 | 1 | 8 | 3.3 | Cc1ncn(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccccc4[nH]3)C[C@H]2C)n1 | nan | |||
71679798 | 143943 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 534 | 5 | 1 | 8 | 4.8 | C[C@@H]1CN(c2scnc2-c2nc3ccc(-c4ccccc4)cc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | nan | |||
CHEMBL3901665 | 143943 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 534 | 5 | 1 | 8 | 4.8 | C[C@@H]1CN(c2scnc2-c2nc3ccc(-c4ccccc4)cc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | nan | |||
71679315 | 144179 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 560 | 4 | 1 | 8 | 4.8 | C[C@@H]1CN(c2scnc2-c2nc3cc(Cl)c(C(F)(F)F)cc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | nan | |||
CHEMBL3903462 | 144179 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 560 | 4 | 1 | 8 | 4.8 | C[C@@H]1CN(c2scnc2-c2nc3cc(Cl)c(C(F)(F)F)cc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | nan | |||
71679633 | 144240 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 514 | 4 | 1 | 8 | 4.5 | C[C@@H]1CN(c2scnc2-c2nc3cc(C(C)(C)C)ccc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | nan | |||
CHEMBL3903948 | 144240 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 514 | 4 | 1 | 8 | 4.5 | C[C@@H]1CN(c2scnc2-c2nc3cc(C(C)(C)C)ccc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | nan | |||
71679310 | 144435 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 509 | 4 | 1 | 7 | 4.6 | C[C@@H]1CN(c2scnc2-c2nc3cc(Cl)c(F)cc3[nH]2)CCN1C(=O)Cn1ccc2cccnc21 | nan | |||
CHEMBL3905608 | 144435 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 509 | 4 | 1 | 7 | 4.6 | C[C@@H]1CN(c2scnc2-c2nc3cc(Cl)c(F)cc3[nH]2)CCN1C(=O)Cn1ccc2cccnc21 | nan | |||
71679480 | 144841 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 506 | 4 | 1 | 8 | 4.1 | Cc1cc2[nH]c(-c3ncsc3N3CCN(C(=O)Cn4cnc5cccnc54)[C@H](C)C3)nc2cc1Cl | nan | |||
CHEMBL3908992 | 144841 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 506 | 4 | 1 | 8 | 4.1 | Cc1cc2[nH]c(-c3ncsc3N3CCN(C(=O)Cn4cnc5cccnc54)[C@H](C)C3)nc2cc1Cl | nan | |||
71679636 | 145062 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 492 | 4 | 1 | 8 | 3.8 | C[C@@H]1CN(c2scnc2-c2nc3ccc(Cl)cc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | nan | |||
CHEMBL3910696 | 145062 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 492 | 4 | 1 | 8 | 3.8 | C[C@@H]1CN(c2scnc2-c2nc3ccc(Cl)cc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | nan | |||
117739228 | 145460 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 546 | 6 | 1 | 8 | 4.0 | Cc1nn(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccccc4[nH]3)C[C@H]2C)cc1CN(C)C | nan | |||
CHEMBL3913741 | 145460 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 546 | 6 | 1 | 8 | 4.0 | Cc1nn(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccccc4[nH]3)C[C@H]2C)cc1CN(C)C | nan | |||
71678126 | 145541 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 493 | 4 | 1 | 7 | 4.1 | C[C@@H]1CN(c2scnc2-c2nc3c(F)c(F)ccc3[nH]2)CCN1C(=O)Cn1ccc2cccnc21 | nan | |||
CHEMBL3914293 | 145541 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 493 | 4 | 1 | 7 | 4.1 | C[C@@H]1CN(c2scnc2-c2nc3c(F)c(F)ccc3[nH]2)CCN1C(=O)Cn1ccc2cccnc21 | nan | |||
89726264 | 145914 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 526 | 4 | 1 | 8 | 4.2 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cc2cccnc2n1 | nan | |||
CHEMBL3917131 | 145914 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 526 | 4 | 1 | 8 | 4.2 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cc2cccnc2n1 | nan | |||
89726197 | 146096 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 488 | 5 | 2 | 9 | 2.7 | C[C@@H]1CN(c2scnc2-c2nc3ccc(CO)cc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | nan | |||
CHEMBL3918533 | 146096 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 488 | 5 | 2 | 9 | 2.7 | C[C@@H]1CN(c2scnc2-c2nc3ccc(CO)cc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | nan | |||
117739704 | 146515 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 525 | 4 | 1 | 7 | 4.8 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cnc2ccccc21 | nan | |||
CHEMBL3921901 | 146515 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 525 | 4 | 1 | 7 | 4.8 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cnc2ccccc21 | nan | |||
117740351 | 146765 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 583 | 5 | 1 | 7 | 4.7 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cc1ccccc1N1CCN(C)CC1 | nan | |||
CHEMBL3923803 | 146765 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 583 | 5 | 1 | 7 | 4.7 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cc1ccccc1N1CCN(C)CC1 | nan | |||
117740387 | 146768 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 489 | 4 | 1 | 7 | 3.9 | Cc1cnn(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccccc4[nH]3)C[C@H]2C)c1 | nan | |||
CHEMBL3923811 | 146768 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 489 | 4 | 1 | 7 | 3.9 | Cc1cnn(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccccc4[nH]3)C[C@H]2C)c1 | nan | |||
89726576 | 147458 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 458 | 4 | 1 | 8 | 3.2 | C[C@@H]1CN(c2scnc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1ncc2cccnc21 | nan | |||
CHEMBL3929525 | 147458 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 458 | 4 | 1 | 8 | 3.2 | C[C@@H]1CN(c2scnc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1ncc2cccnc21 | nan | |||
89726451 | 147490 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 512 | 4 | 1 | 8 | 3.8 | O=C(Cn1cnc2cccnc21)N1CCN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CC1 | nan | |||
CHEMBL3929775 | 147490 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 512 | 4 | 1 | 8 | 3.8 | O=C(Cn1cnc2cccnc21)N1CCN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CC1 | nan | |||
89725938 | 147582 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 501 | 6 | 1 | 9 | 2.7 | CN(C)C[C@@H]1CN(c2scnc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | nan | |||
CHEMBL3930468 | 147582 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 501 | 6 | 1 | 9 | 2.7 | CN(C)C[C@@H]1CN(c2scnc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | nan | |||
71679479 | 148274 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 500 | 5 | 1 | 8 | 4.3 | CC(C)c1ccc2nc(-c3ncsc3N3CCN(C(=O)Cn4cnc5cccnc54)[C@H](C)C3)[nH]c2c1 | nan | |||
CHEMBL3935793 | 148274 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 500 | 5 | 1 | 8 | 4.3 | CC(C)c1ccc2nc(-c3ncsc3N3CCN(C(=O)Cn4cnc5cccnc54)[C@H](C)C3)[nH]c2c1 | nan | |||
117739638 | 148329 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 543 | 4 | 1 | 7 | 4.7 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1ccc(C(F)(F)F)n1 | nan | |||
CHEMBL3936265 | 148329 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 543 | 4 | 1 | 7 | 4.7 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1ccc(C(F)(F)F)n1 | nan | |||
89726525 | 148408 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 491 | 4 | 1 | 7 | 4.4 | C[C@@H]1CN(c2scnc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cc(Cl)c2cccnc21 | nan | |||
CHEMBL3936959 | 148408 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 491 | 4 | 1 | 7 | 4.4 | C[C@@H]1CN(c2scnc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cc(Cl)c2cccnc21 | nan | |||
117739351 | 148559 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 536 | 4 | 1 | 6 | 5.5 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cc1cccc2cccnc12 | nan | |||
CHEMBL3938074 | 148559 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 536 | 4 | 1 | 6 | 5.5 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cc1cccc2cccnc12 | nan | |||
71679635 | 148845 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 508 | 4 | 1 | 8 | 4.0 | C[C@@H]1CN(c2scnc2-c2nc3cc(Cl)ccc3[nH]2)CCN1C(=O)Cn1c(=O)oc2ccccc21 | nan | |||
CHEMBL3940474 | 148845 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 508 | 4 | 1 | 8 | 4.0 | C[C@@H]1CN(c2scnc2-c2nc3cc(Cl)ccc3[nH]2)CCN1C(=O)Cn1c(=O)oc2ccccc21 | nan | |||
71679316 | 149637 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 526 | 4 | 1 | 8 | 4.2 | C[C@@H]1CN(c2scnc2-c2nc3cc(C(F)(F)F)ccc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | nan | |||
CHEMBL3946677 | 149637 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 526 | 4 | 1 | 8 | 4.2 | C[C@@H]1CN(c2scnc2-c2nc3cc(C(F)(F)F)ccc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | nan | |||
89725963 | 149910 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 568 | 5 | 1 | 9 | 4.4 | CC(=O)c1ccc2[nH]c(-c3nc(C(F)(F)F)sc3N3CCN(C(=O)Cn4cnc5cccnc54)[C@H](C)C3)nc2c1 | nan | |||
CHEMBL3948779 | 149910 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 568 | 5 | 1 | 9 | 4.4 | CC(=O)c1ccc2[nH]c(-c3nc(C(F)(F)F)sc3N3CCN(C(=O)Cn4cnc5cccnc54)[C@H](C)C3)nc2c1 | nan | |||
89726410 | 150239 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 503 | 4 | 1 | 7 | 4.3 | Cc1cc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccccc4[nH]3)C[C@H]2C)n1 | nan | |||
CHEMBL3951530 | 150239 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 503 | 4 | 1 | 7 | 4.3 | Cc1cc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccccc4[nH]3)C[C@H]2C)n1 | nan | |||
89726560 | 150829 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 540 | 4 | 1 | 6 | 4.3 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)CN1C(=O)Cc2ccccc21 | nan | |||
CHEMBL3956337 | 150829 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 540 | 4 | 1 | 6 | 4.3 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)CN1C(=O)Cc2ccccc21 | nan | |||
89726516 | 151438 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 554 | 4 | 1 | 8 | 3.8 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cnc(Br)n1 | nan | |||
CHEMBL3961149 | 151438 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 554 | 4 | 1 | 8 | 3.8 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cnc(Br)n1 | nan | |||
89726222 | 151794 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 584 | 5 | 1 | 10 | 4.0 | COC(=O)c1ccc2[nH]c(-c3nc(C(F)(F)F)sc3N3CCN(C(=O)Cn4cnc5cccnc54)[C@H](C)C3)nc2c1 | nan | |||
CHEMBL3964312 | 151794 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 584 | 5 | 1 | 10 | 4.0 | COC(=O)c1ccc2[nH]c(-c3nc(C(F)(F)F)sc3N3CCN(C(=O)Cn4cnc5cccnc54)[C@H](C)C3)nc2c1 | nan | |||
117739802 | 152013 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 586 | 7 | 2 | 10 | 3.6 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3cc(OCCO)ccc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | nan | |||
CHEMBL3966250 | 152013 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 586 | 7 | 2 | 10 | 3.6 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3cc(OCCO)ccc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | nan | |||
71679629 | 152226 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 471 | 5 | 1 | 7 | 4.2 | CC[C@@H]1CN(c2scnc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1ccc2cccnc21 | nan | |||
CHEMBL3967981 | 152226 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 471 | 5 | 1 | 7 | 4.2 | CC[C@@H]1CN(c2scnc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1ccc2cccnc21 | nan | |||
89726625 | 152560 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 536 | 4 | 1 | 8 | 3.9 | C[C@@H]1CN(c2sc(Br)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | nan | |||
CHEMBL3971056 | 152560 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 536 | 4 | 1 | 8 | 3.9 | C[C@@H]1CN(c2sc(Br)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | nan | |||
71679799 | 152773 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 486 | 5 | 1 | 8 | 3.7 | CCc1ccc2nc(-c3ncsc3N3CCN(C(=O)Cn4cnc5cccnc54)[C@H](C)C3)[nH]c2c1 | nan | |||
CHEMBL3972743 | 152773 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 486 | 5 | 1 | 8 | 3.7 | CCc1ccc2nc(-c3ncsc3N3CCN(C(=O)Cn4cnc5cccnc54)[C@H](C)C3)[nH]c2c1 | nan | |||
89726538 | 152825 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 560 | 4 | 1 | 8 | 4.8 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3cc(Cl)ccc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | nan | |||
CHEMBL3973196 | 152825 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 560 | 4 | 1 | 8 | 4.8 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3cc(Cl)ccc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | nan | |||
89726679 | 152960 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 540 | 4 | 1 | 8 | 3.9 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4c(F)c(F)ccc4[nH]3)C[C@H]2C)n1 | nan | |||
CHEMBL3974351 | 152960 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 540 | 4 | 1 | 8 | 3.9 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4c(F)c(F)ccc4[nH]3)C[C@H]2C)n1 | nan | |||
71679634 | 153010 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 472 | 4 | 1 | 8 | 3.5 | Cc1ccc2[nH]c(-c3ncsc3N3CCN(C(=O)Cn4cnc5cccnc54)[C@H](C)C3)nc2c1 | nan | |||
CHEMBL3974833 | 153010 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 472 | 4 | 1 | 8 | 3.5 | Cc1ccc2[nH]c(-c3ncsc3N3CCN(C(=O)Cn4cnc5cccnc54)[C@H](C)C3)nc2c1 | nan | |||
71679471 | 153024 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 513 | 4 | 1 | 7 | 5.1 | C[C@@H]1CN(c2scnc2-c2nc3ccc(C(C)(C)C)cc3[nH]2)CCN1C(=O)Cn1ccc2cccnc21 | nan | |||
CHEMBL3974991 | 153024 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 513 | 4 | 1 | 7 | 5.1 | C[C@@H]1CN(c2scnc2-c2nc3ccc(C(C)(C)C)cc3[nH]2)CCN1C(=O)Cn1ccc2cccnc21 | nan | |||
71679473 | 153075 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 471 | 4 | 1 | 7 | 4.1 | Cc1cccc2[nH]c(-c3ncsc3N3CCN(C(=O)Cn4ccc5cccnc54)[C@H](C)C3)nc12 | nan | |||
CHEMBL3975264 | 153075 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 471 | 4 | 1 | 7 | 4.1 | Cc1cccc2[nH]c(-c3ncsc3N3CCN(C(=O)Cn4ccc5cccnc54)[C@H](C)C3)nc12 | nan | |||
117739020 | 153388 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 570 | 5 | 2 | 9 | 4.2 | CC(O)c1ccc2[nH]c(-c3nc(C(F)(F)F)sc3N3CCN(C(=O)Cn4cnc5cccnc54)[C@H](C)C3)nc2c1 | nan | |||
CHEMBL3977943 | 153388 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 570 | 5 | 2 | 9 | 4.2 | CC(O)c1ccc2[nH]c(-c3nc(C(F)(F)F)sc3N3CCN(C(=O)Cn4cnc5cccnc54)[C@H](C)C3)nc2c1 | nan | |||
71679146 | 153498 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 526 | 4 | 1 | 8 | 4.2 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | nan | |||
CHEMBL3978935 | 153498 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 526 | 4 | 1 | 8 | 4.2 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | nan | |||
117740233 | 153750 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 588 | 5 | 1 | 9 | 4.5 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccc(C5CCOCC5)cc4[nH]3)C[C@H]2C)n1 | nan | |||
CHEMBL3981151 | 153750 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 588 | 5 | 1 | 9 | 4.5 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3nc4ccc(C5CCOCC5)cc4[nH]3)C[C@H]2C)n1 | nan | |||
117739250 | 154144 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 544 | 4 | 1 | 8 | 3.6 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cnc2c1CN(C)CC2 | nan | |||
CHEMBL3984468 | 154144 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 544 | 4 | 1 | 8 | 3.6 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cnc2c1CN(C)CC2 | nan | |||
89726463 | 154193 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 542 | 4 | 2 | 8 | 3.5 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1c(=O)[nH]c2cccnc21 | nan | |||
CHEMBL3985006 | 154193 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | ChEMBL | 542 | 4 | 2 | 8 | 3.5 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1c(=O)[nH]c2cccnc21 | nan | |||
57394301 | 68759 | None | 0 | Human | Binding | pIC50 | = | 9.0 | 9.0 | - | 0 | ChEMBL | 510 | 6 | 1 | 6 | 3.5 | CC[C@H]1CN(c2ncc(C(=O)NC3CC3)nc2C)CCN1C1CCN(C(=O)c2ccc(Cl)cc2)CC1 | 10.1016/j.bmcl.2011.09.120 | |||
CHEMBL1921891 | 68759 | None | 0 | Human | Binding | pIC50 | = | 9.0 | 9.0 | - | 0 | ChEMBL | 510 | 6 | 1 | 6 | 3.5 | CC[C@H]1CN(c2ncc(C(=O)NC3CC3)nc2C)CCN1C1CCN(C(=O)c2ccc(Cl)cc2)CC1 | 10.1016/j.bmcl.2011.09.120 | |||
45486530 | 200769 | None | 0 | Human | Binding | pIC50 | = | 9.0 | 9.0 | - | 0 | ChEMBL | 651 | 9 | 0 | 8 | 6.0 | C[C@H](c1nc2c(C3CC3)nccn2c1-c1ccc(C#N)cc1)N(CC1CCS(=O)(=O)CC1)C(=O)Cc1ccc(OC(F)(F)F)cc1 | 10.1016/j.bmcl.2009.07.021 | |||
CHEMBL576096 | 200769 | None | 0 | Human | Binding | pIC50 | = | 9.0 | 9.0 | - | 0 | ChEMBL | 651 | 9 | 0 | 8 | 6.0 | C[C@H](c1nc2c(C3CC3)nccn2c1-c1ccc(C#N)cc1)N(CC1CCS(=O)(=O)CC1)C(=O)Cc1ccc(OC(F)(F)F)cc1 | 10.1016/j.bmcl.2009.07.021 | |||
45486534 | 200772 | None | 0 | Human | Binding | pIC50 | = | 9.0 | 9.0 | - | 0 | ChEMBL | 651 | 9 | 0 | 8 | 6.0 | C[C@H](c1nc2c(C3CC3)nccn2c1-c1ccc(C#N)cc1)N(CC1CCS(=O)(=O)CC1)C(=O)Cc1cccc(OC(F)(F)F)c1 | 10.1016/j.bmcl.2009.07.021 | |||
CHEMBL576099 | 200772 | None | 0 | Human | Binding | pIC50 | = | 9.0 | 9.0 | - | 0 | ChEMBL | 651 | 9 | 0 | 8 | 6.0 | C[C@H](c1nc2c(C3CC3)nccn2c1-c1ccc(C#N)cc1)N(CC1CCS(=O)(=O)CC1)C(=O)Cc1cccc(OC(F)(F)F)c1 | 10.1016/j.bmcl.2009.07.021 | |||
45486525 | 201009 | None | 0 | Human | Binding | pIC50 | = | 9.0 | 9.0 | - | 0 | ChEMBL | 615 | 10 | 0 | 7 | 5.6 | CCc1nccn2c(-c3ccc(C#N)cc3)c([C@@H](C)N(CCS(=O)(=O)CC)C(=O)Cc3ccc(C(F)(F)F)c(F)c3)nc12 | 10.1016/j.bmcl.2009.07.021 | |||
CHEMBL578189 | 201009 | None | 0 | Human | Binding | pIC50 | = | 9.0 | 9.0 | - | 0 | ChEMBL | 615 | 10 | 0 | 7 | 5.6 | CCc1nccn2c(-c3ccc(C#N)cc3)c([C@@H](C)N(CCS(=O)(=O)CC)C(=O)Cc3ccc(C(F)(F)F)c(F)c3)nc12 | 10.1016/j.bmcl.2009.07.021 | |||
11995702 | 105432 | None | 0 | Human | Binding | pIC50 | = | 8.9 | 8.9 | - | 0 | ChEMBL | 554 | 7 | 2 | 11 | 3.1 | CCNc1nnc(-c2cnc(N3CCN(C4CCN(C(=O)c5ccc(Cl)nc5N)CC4)[C@@H](CC)C3)c(C)n2)o1 | 10.1016/j.bmcl.2014.01.009 | |||
CHEMBL3116488 | 105432 | None | 0 | Human | Binding | pIC50 | = | 8.9 | 8.9 | - | 0 | ChEMBL | 554 | 7 | 2 | 11 | 3.1 | CCNc1nnc(-c2cnc(N3CCN(C4CCN(C(=O)c5ccc(Cl)nc5N)CC4)[C@@H](CC)C3)c(C)n2)o1 | 10.1016/j.bmcl.2014.01.009 | |||
58768048 | 105440 | None | 0 | Human | Binding | pIC50 | = | 8.9 | 8.9 | - | 0 | ChEMBL | 538 | 7 | 1 | 9 | 4.1 | CCNc1nnc(-c2cnc(N3CCN(C4CCN(C(=O)c5ccc(Cl)cc5)CC4)[C@@H](CC)C3)c(C)n2)o1 | 10.1016/j.bmcl.2014.01.009 | |||
CHEMBL3116496 | 105440 | None | 0 | Human | Binding | pIC50 | = | 8.9 | 8.9 | - | 0 | ChEMBL | 538 | 7 | 1 | 9 | 4.1 | CCNc1nnc(-c2cnc(N3CCN(C4CCN(C(=O)c5ccc(Cl)cc5)CC4)[C@@H](CC)C3)c(C)n2)o1 | 10.1016/j.bmcl.2014.01.009 | |||
57401269 | 68746 | None | 0 | Human | Binding | pIC50 | = | 8.9 | 8.9 | - | 0 | ChEMBL | 546 | 6 | 2 | 8 | 2.9 | CC[C@H]1CN(c2ncc(C(=O)NC3CC3)nc2Cl)CCN1C1CCN(C(=O)c2ccc(Cl)nc2N)CC1 | 10.1016/j.bmcl.2011.09.120 | |||
CHEMBL1921878 | 68746 | None | 0 | Human | Binding | pIC50 | = | 8.9 | 8.9 | - | 0 | ChEMBL | 546 | 6 | 2 | 8 | 2.9 | CC[C@H]1CN(c2ncc(C(=O)NC3CC3)nc2Cl)CCN1C1CCN(C(=O)c2ccc(Cl)nc2N)CC1 | 10.1016/j.bmcl.2011.09.120 | |||
71525976 | 153578 | None | 0 | Human | Binding | pIC50 | = | 8.9 | 8.9 | - | 0 | ChEMBL | 453 | 7 | 3 | 8 | 3.1 | Cc1ccc(C(Nc2c(Nc3cccc(C(=O)N(C)C)c3O)c(=O)c2=O)C2(C)CCCO2)o1 | 10.1021/acs.jmedchem.5b01337 | |||
CHEMBL3979652 | 153578 | None | 0 | Human | Binding | pIC50 | = | 8.9 | 8.9 | - | 0 | ChEMBL | 453 | 7 | 3 | 8 | 3.1 | Cc1ccc(C(Nc2c(Nc3cccc(C(=O)N(C)C)c3O)c(=O)c2=O)C2(C)CCCO2)o1 | 10.1021/acs.jmedchem.5b01337 | |||
11856829 | 105413 | None | 0 | Human | Binding | pIC50 | = | 8.9 | 8.9 | - | 0 | ChEMBL | 518 | 6 | 1 | 6 | 4.4 | CC[C@H]1CN(c2ncc(C3=NCCN3)cc2Cl)CCN1C1CCN(Cc2ccc(Cl)cc2F)CC1 | 10.1016/j.bmcl.2014.01.009 | |||
CHEMBL3116469 | 105413 | None | 0 | Human | Binding | pIC50 | = | 8.9 | 8.9 | - | 0 | ChEMBL | 518 | 6 | 1 | 6 | 4.4 | CC[C@H]1CN(c2ncc(C3=NCCN3)cc2Cl)CCN1C1CCN(Cc2ccc(Cl)cc2F)CC1 | 10.1016/j.bmcl.2014.01.009 | |||
11995703 | 105425 | None | 0 | Human | Binding | pIC50 | = | 8.9 | 8.9 | - | 0 | ChEMBL | 561 | 5 | 3 | 12 | 2.2 | CC[C@H]1CN(c2nc(N)c(-c3nnc(N)o3)nc2Cl)CCN1C1CCN(C(=O)c2ccc(Cl)nc2N)CC1 | 10.1016/j.bmcl.2014.01.009 | |||
CHEMBL3116481 | 105425 | None | 0 | Human | Binding | pIC50 | = | 8.9 | 8.9 | - | 0 | ChEMBL | 561 | 5 | 3 | 12 | 2.2 | CC[C@H]1CN(c2nc(N)c(-c3nnc(N)o3)nc2Cl)CCN1C1CCN(C(=O)c2ccc(Cl)nc2N)CC1 | 10.1016/j.bmcl.2014.01.009 | |||
54764847 | 68763 | None | 0 | Human | Binding | pIC50 | = | 8.9 | 8.9 | - | 0 | ChEMBL | 524 | 6 | 1 | 6 | 3.9 | CC[C@H]1CN(c2ncc(C(=O)NC3CC3)nc2C)[C@H](C)CN1C1CCN(C(=O)c2ccc(Cl)cc2)CC1 | 10.1016/j.bmcl.2011.09.120 | |||
CHEMBL1921896 | 68763 | None | 0 | Human | Binding | pIC50 | = | 8.9 | 8.9 | - | 0 | ChEMBL | 524 | 6 | 1 | 6 | 3.9 | CC[C@H]1CN(c2ncc(C(=O)NC3CC3)nc2C)[C@H](C)CN1C1CCN(C(=O)c2ccc(Cl)cc2)CC1 | 10.1016/j.bmcl.2011.09.120 | |||
45486533 | 200094 | None | 0 | Human | Binding | pIC50 | = | 8.9 | 8.9 | - | 0 | ChEMBL | 635 | 8 | 0 | 7 | 6.1 | C[C@H](c1nc2c(C3CC3)nccn2c1-c1ccc(C#N)cc1)N(CC1CCS(=O)(=O)CC1)C(=O)Cc1ccc(C(F)(F)F)cc1 | 10.1016/j.bmcl.2009.07.021 | |||
CHEMBL570858 | 200094 | None | 0 | Human | Binding | pIC50 | = | 8.9 | 8.9 | - | 0 | ChEMBL | 635 | 8 | 0 | 7 | 6.1 | C[C@H](c1nc2c(C3CC3)nccn2c1-c1ccc(C#N)cc1)N(CC1CCS(=O)(=O)CC1)C(=O)Cc1ccc(C(F)(F)F)cc1 | 10.1016/j.bmcl.2009.07.021 | |||
11856830 | 105418 | None | 0 | Human | Binding | pIC50 | = | 8.9 | 8.9 | - | 0 | ChEMBL | 518 | 6 | 0 | 7 | 5.1 | CC[C@H]1CN(c2ncc(-c3nnco3)cc2Cl)CCN1C1CCN(Cc2ccc(Cl)cc2F)CC1 | 10.1016/j.bmcl.2014.01.009 | |||
CHEMBL3116474 | 105418 | None | 0 | Human | Binding | pIC50 | = | 8.9 | 8.9 | - | 0 | ChEMBL | 518 | 6 | 0 | 7 | 5.1 | CC[C@H]1CN(c2ncc(-c3nnco3)cc2Cl)CCN1C1CCN(Cc2ccc(Cl)cc2F)CC1 | 10.1016/j.bmcl.2014.01.009 | |||
45486528 | 200093 | None | 0 | Human | Binding | pIC50 | = | 8.9 | 8.9 | - | 0 | ChEMBL | 630 | 10 | 0 | 8 | 5.1 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(C(F)(F)F)c(F)c1)C(C)c1nc2c(N(C)C)nccn2c1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2009.07.021 | |||
CHEMBL570857 | 200093 | None | 0 | Human | Binding | pIC50 | = | 8.9 | 8.9 | - | 0 | ChEMBL | 630 | 10 | 0 | 8 | 5.1 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(C(F)(F)F)c(F)c1)C(C)c1nc2c(N(C)C)nccn2c1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2009.07.021 | |||
121485701 | 276 | None | 10 | Mouse | Binding | pIC50 | = | 8.8 | 8.8 | - | 1 | ChEMBL | 550 | 6 | 1 | 10 | 2.6 | CC1=NN(C=N1)CC(=O)N2CCN(C[C@H]2CCO)C3=C(N=C(S3)C(F)(F)F)C4=CN=C(N=C4)C(F)(F)F | 10.1021/acs.jmedchem.3c00074 | |||
12584 | 276 | None | 10 | Mouse | Binding | pIC50 | = | 8.8 | 8.8 | - | 1 | ChEMBL | 550 | 6 | 1 | 10 | 2.6 | CC1=NN(C=N1)CC(=O)N2CCN(C[C@H]2CCO)C3=C(N=C(S3)C(F)(F)F)C4=CN=C(N=C4)C(F)(F)F | 10.1021/acs.jmedchem.3c00074 | |||
CHEMBL5279308 | 276 | None | 10 | Mouse | Binding | pIC50 | = | 8.8 | 8.8 | - | 1 | ChEMBL | 550 | 6 | 1 | 10 | 2.6 | CC1=NN(C=N1)CC(=O)N2CCN(C[C@H]2CCO)C3=C(N=C(S3)C(F)(F)F)C4=CN=C(N=C4)C(F)(F)F | 10.1021/acs.jmedchem.3c00074 | |||
11997620 | 105433 | None | 0 | Human | Binding | pIC50 | = | 8.8 | 8.8 | - | 0 | ChEMBL | 608 | 7 | 2 | 11 | 3.8 | CCNc1nnc(-c2cnc(N3CCN(C4CCN(C(=O)c5ccc(Cl)nc5N)CC4)[C@@H](CC)C3)c(C(F)(F)F)n2)o1 | 10.1016/j.bmcl.2014.01.009 | |||
CHEMBL3116489 | 105433 | None | 0 | Human | Binding | pIC50 | = | 8.8 | 8.8 | - | 0 | ChEMBL | 608 | 7 | 2 | 11 | 3.8 | CCNc1nnc(-c2cnc(N3CCN(C4CCN(C(=O)c5ccc(Cl)nc5N)CC4)[C@@H](CC)C3)c(C(F)(F)F)n2)o1 | 10.1016/j.bmcl.2014.01.009 | |||
11996050 | 68739 | None | 0 | Human | Binding | pIC50 | = | 8.8 | 8.8 | - | 0 | ChEMBL | 575 | 7 | 2 | 9 | 3.0 | CC[C@H]1CN(c2nc(N)c(C(=O)N[C@@H]3CCOC3=O)nc2Cl)CCN1C1CCN(Cc2ccc(Cl)cc2)CC1 | 10.1016/j.bmcl.2011.09.120 | |||
CHEMBL1921871 | 68739 | None | 0 | Human | Binding | pIC50 | = | 8.8 | 8.8 | - | 0 | ChEMBL | 575 | 7 | 2 | 9 | 3.0 | CC[C@H]1CN(c2nc(N)c(C(=O)N[C@@H]3CCOC3=O)nc2Cl)CCN1C1CCN(Cc2ccc(Cl)cc2)CC1 | 10.1016/j.bmcl.2011.09.120 | |||
57397855 | 68745 | None | 0 | Human | Binding | pIC50 | = | 8.8 | 8.8 | - | 0 | ChEMBL | 562 | 5 | 2 | 8 | 3.5 | CC[C@H]1CN(c2ncc(C(=O)NC(C)(C)C)nc2Cl)CCN1C1CCN(C(=O)c2ccc(Cl)nc2N)CC1 | 10.1016/j.bmcl.2011.09.120 | |||
CHEMBL1921877 | 68745 | None | 0 | Human | Binding | pIC50 | = | 8.8 | 8.8 | - | 0 | ChEMBL | 562 | 5 | 2 | 8 | 3.5 | CC[C@H]1CN(c2ncc(C(=O)NC(C)(C)C)nc2Cl)CCN1C1CCN(C(=O)c2ccc(Cl)nc2N)CC1 | 10.1016/j.bmcl.2011.09.120 | |||
57394299 | 68751 | None | 0 | Human | Binding | pIC50 | = | 8.8 | 8.8 | - | 0 | ChEMBL | 554 | 5 | 2 | 8 | 2.7 | CC[C@H]1CN(c2ncc(C(=O)NC)nc2C(F)(F)F)CCN1C1CCN(C(=O)c2ccc(Cl)nc2N)CC1 | 10.1016/j.bmcl.2011.09.120 | |||
CHEMBL1921883 | 68751 | None | 0 | Human | Binding | pIC50 | = | 8.8 | 8.8 | - | 0 | ChEMBL | 554 | 5 | 2 | 8 | 2.7 | CC[C@H]1CN(c2ncc(C(=O)NC)nc2C(F)(F)F)CCN1C1CCN(C(=O)c2ccc(Cl)nc2N)CC1 | 10.1016/j.bmcl.2011.09.120 | |||
76332481 | 105429 | None | 0 | Human | Binding | pIC50 | = | 8.8 | 8.8 | - | 0 | ChEMBL | 575 | 6 | 3 | 12 | 2.6 | CC[C@H]1CN(c2nc(N)c(-c3nnc(NC)o3)nc2Cl)CCN1C1CCN(C(=O)c2ccc(Cl)nc2N)CC1 | 10.1016/j.bmcl.2014.01.009 | |||
CHEMBL3116485 | 105429 | None | 0 | Human | Binding | pIC50 | = | 8.8 | 8.8 | - | 0 | ChEMBL | 575 | 6 | 3 | 12 | 2.6 | CC[C@H]1CN(c2nc(N)c(-c3nnc(NC)o3)nc2Cl)CCN1C1CCN(C(=O)c2ccc(Cl)nc2N)CC1 | 10.1016/j.bmcl.2014.01.009 | |||
58768061 | 105445 | None | 0 | Human | Binding | pIC50 | = | 8.8 | 8.8 | - | 0 | ChEMBL | 507 | 5 | 1 | 6 | 4.4 | CC[C@H]1CN(c2ncc(-c3ncc[nH]3)nc2C)[C@H](C)CN1C1CCN(C(=O)c2ccc(Cl)cc2)CC1 | 10.1016/j.bmcl.2014.01.009 | |||
CHEMBL3116501 | 105445 | None | 0 | Human | Binding | pIC50 | = | 8.8 | 8.8 | - | 0 | ChEMBL | 507 | 5 | 1 | 6 | 4.4 | CC[C@H]1CN(c2ncc(-c3ncc[nH]3)nc2C)[C@H](C)CN1C1CCN(C(=O)c2ccc(Cl)cc2)CC1 | 10.1016/j.bmcl.2014.01.009 | |||
45486524 | 201008 | None | 0 | Human | Binding | pIC50 | = | 8.8 | 8.8 | - | 0 | ChEMBL | 601 | 9 | 0 | 7 | 5.3 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(C(F)(F)F)c(F)c1)[C@H](C)c1nc2c(C)nccn2c1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2009.07.021 | |||
CHEMBL578188 | 201008 | None | 0 | Human | Binding | pIC50 | = | 8.8 | 8.8 | - | 0 | ChEMBL | 601 | 9 | 0 | 7 | 5.3 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(C(F)(F)F)c(F)c1)[C@H](C)c1nc2c(C)nccn2c1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2009.07.021 | |||
45486532 | 200771 | None | 0 | Human | Binding | pIC50 | = | 8.8 | 8.8 | - | 0 | ChEMBL | 635 | 8 | 0 | 7 | 6.1 | C[C@H](c1nc2c(C3CC3)nccn2c1-c1ccc(C#N)cc1)N(CC1CCS(=O)(=O)CC1)C(=O)Cc1cccc(C(F)(F)F)c1 | 10.1016/j.bmcl.2009.07.021 | |||
CHEMBL576098 | 200771 | None | 0 | Human | Binding | pIC50 | = | 8.8 | 8.8 | - | 0 | ChEMBL | 635 | 8 | 0 | 7 | 6.1 | C[C@H](c1nc2c(C3CC3)nccn2c1-c1ccc(C#N)cc1)N(CC1CCS(=O)(=O)CC1)C(=O)Cc1cccc(C(F)(F)F)c1 | 10.1016/j.bmcl.2009.07.021 | |||
11997334 | 105439 | None | 0 | Human | Binding | pIC50 | = | 8.7 | 8.7 | - | 0 | ChEMBL | 523 | 5 | 2 | 8 | 3.4 | CC[C@H]1CN(c2ncc(-c3ncc[nH]3)nc2C)[C@H](C)CN1C1CCN(C(=O)c2ccc(Cl)nc2N)CC1 | 10.1016/j.bmcl.2014.01.009 | |||
CHEMBL3116495 | 105439 | None | 0 | Human | Binding | pIC50 | = | 8.7 | 8.7 | - | 0 | ChEMBL | 523 | 5 | 2 | 8 | 3.4 | CC[C@H]1CN(c2ncc(-c3ncc[nH]3)nc2C)[C@H](C)CN1C1CCN(C(=O)c2ccc(Cl)nc2N)CC1 | 10.1016/j.bmcl.2014.01.009 | |||
58768027 | 105442 | None | 0 | Human | Binding | pIC50 | = | 8.7 | 8.7 | - | 0 | ChEMBL | 606 | 7 | 1 | 9 | 5.2 | CCNc1nnc(-c2cnc(N3C[C@H](CC)N(C4CCN(C(=O)c5ccc(Cl)cc5)CC4)C[C@H]3C)c(C(F)(F)F)n2)o1 | 10.1016/j.bmcl.2014.01.009 | |||
CHEMBL3116498 | 105442 | None | 0 | Human | Binding | pIC50 | = | 8.7 | 8.7 | - | 0 | ChEMBL | 606 | 7 | 1 | 9 | 5.2 | CCNc1nnc(-c2cnc(N3C[C@H](CC)N(C4CCN(C(=O)c5ccc(Cl)cc5)CC4)C[C@H]3C)c(C(F)(F)F)n2)o1 | 10.1016/j.bmcl.2014.01.009 | |||
57394300 | 68752 | None | 0 | Human | Binding | pIC50 | = | 8.7 | 8.7 | - | 0 | ChEMBL | 580 | 6 | 2 | 8 | 3.2 | CC[C@H]1CN(c2ncc(C(=O)NC3CC3)nc2C(F)(F)F)CCN1C1CCN(C(=O)c2ccc(Cl)nc2N)CC1 | 10.1016/j.bmcl.2011.09.120 | |||
CHEMBL1921884 | 68752 | None | 0 | Human | Binding | pIC50 | = | 8.7 | 8.7 | - | 0 | ChEMBL | 580 | 6 | 2 | 8 | 3.2 | CC[C@H]1CN(c2ncc(C(=O)NC3CC3)nc2C(F)(F)F)CCN1C1CCN(C(=O)c2ccc(Cl)nc2N)CC1 | 10.1016/j.bmcl.2011.09.120 | |||
44455843 | 97468 | None | 0 | Human | Binding | pIC50 | = | 8.7 | 8.7 | - | 0 | ChEMBL | 526 | 9 | 0 | 5 | 6.2 | CCOc1ccc(-n2ccnc2[C@@H](C)N(Cc2cccnc2)C(=O)Cc2ccc(F)c(C(F)(F)F)c2)cc1 | 10.1016/j.bmcl.2007.11.072 | |||
CHEMBL269932 | 97468 | None | 0 | Human | Binding | pIC50 | = | 8.7 | 8.7 | - | 0 | ChEMBL | 526 | 9 | 0 | 5 | 6.2 | CCOc1ccc(-n2ccnc2[C@@H](C)N(Cc2cccnc2)C(=O)Cc2ccc(F)c(C(F)(F)F)c2)cc1 | 10.1016/j.bmcl.2007.11.072 | |||
11996051 | 68729 | None | 1 | Human | Binding | pIC50 | = | 8.7 | 8.7 | - | 0 | ChEMBL | 521 | 7 | 3 | 8 | 2.6 | CC[C@H]1CN(c2nc(N)c(C(N)=O)nc2Cl)CCN1C1CCN(C(CO)c2ccc(Cl)cc2)CC1 | 10.1016/j.bmcl.2011.09.120 | |||
CHEMBL1921861 | 68729 | None | 1 | Human | Binding | pIC50 | = | 8.7 | 8.7 | - | 0 | ChEMBL | 521 | 7 | 3 | 8 | 2.6 | CC[C@H]1CN(c2nc(N)c(C(N)=O)nc2Cl)CCN1C1CCN(C(CO)c2ccc(Cl)cc2)CC1 | 10.1016/j.bmcl.2011.09.120 | |||
11996344 | 68737 | None | 0 | Human | Binding | pIC50 | = | 8.7 | 8.7 | - | 0 | ChEMBL | 613 | 10 | 4 | 9 | 1.5 | CC[C@H]1CN(c2nc(N)c(C(=O)NCCNS(N)(=O)=O)nc2Cl)CCN1C1CCN(Cc2ccc(Cl)cc2)CC1 | 10.1016/j.bmcl.2011.09.120 | |||
CHEMBL1921869 | 68737 | None | 0 | Human | Binding | pIC50 | = | 8.7 | 8.7 | - | 0 | ChEMBL | 613 | 10 | 4 | 9 | 1.5 | CC[C@H]1CN(c2nc(N)c(C(=O)NCCNS(N)(=O)=O)nc2Cl)CCN1C1CCN(Cc2ccc(Cl)cc2)CC1 | 10.1016/j.bmcl.2011.09.120 | |||
57396055 | 68750 | None | 0 | Human | Binding | pIC50 | = | 8.7 | 8.7 | - | 0 | ChEMBL | 540 | 5 | 2 | 8 | 2.4 | CC[C@H]1CN(c2ncc(C(N)=O)nc2C(F)(F)F)CCN1C1CCN(C(=O)c2ccc(Cl)nc2N)CC1 | 10.1016/j.bmcl.2011.09.120 | |||
CHEMBL1921882 | 68750 | None | 0 | Human | Binding | pIC50 | = | 8.7 | 8.7 | - | 0 | ChEMBL | 540 | 5 | 2 | 8 | 2.4 | CC[C@H]1CN(c2ncc(C(N)=O)nc2C(F)(F)F)CCN1C1CCN(C(=O)c2ccc(Cl)nc2N)CC1 | 10.1016/j.bmcl.2011.09.120 | |||
57397856 | 68755 | None | 0 | Human | Binding | pIC50 | = | 8.7 | 8.7 | - | 0 | ChEMBL | 526 | 6 | 2 | 8 | 2.5 | CC[C@H]1CN(c2ncc(C(=O)NC3CC3)nc2C)CCN1C1CCN(C(=O)c2ccc(Cl)nc2N)CC1 | 10.1016/j.bmcl.2011.09.120 | |||
CHEMBL1921887 | 68755 | None | 0 | Human | Binding | pIC50 | = | 8.7 | 8.7 | - | 0 | ChEMBL | 526 | 6 | 2 | 8 | 2.5 | CC[C@H]1CN(c2ncc(C(=O)NC3CC3)nc2C)CCN1C1CCN(C(=O)c2ccc(Cl)nc2N)CC1 | 10.1016/j.bmcl.2011.09.120 | |||
53255348 | 194203 | None | 0 | Human | Binding | pIC50 | = | 8.7 | 8.7 | - | 0 | ChEMBL | 469 | 7 | 2 | 5 | 5.8 | O=C(Nc1cc(Cl)cnc1N1CCC(CCNc2cccnc2)CC1)c1cccc(Cl)c1 | 10.1021/acs.jmedchem.5b01337 | |||
CHEMBL5281002 | 194203 | None | 0 | Human | Binding | pIC50 | = | 8.7 | 8.7 | - | 0 | ChEMBL | 469 | 7 | 2 | 5 | 5.8 | O=C(Nc1cc(Cl)cnc1N1CCC(CCNc2cccnc2)CC1)c1cccc(Cl)c1 | 10.1021/acs.jmedchem.5b01337 | |||
171344809 | 194493 | None | 0 | Human | Binding | pIC50 | = | 8.7 | 8.7 | - | 0 | ChEMBL | 499 | 5 | 1 | 4 | 3.9 | CN(C)CCn1cc2c3c1CC=CC3C1=C[C@@H](C(=O)N3CCCC3)CN(C(=O)Nc3ccccc3)[C@@H]1C2 | 10.1021/acs.jmedchem.5b01337 | |||
CHEMBL5287540 | 194493 | None | 0 | Human | Binding | pIC50 | = | 8.7 | 8.7 | - | 0 | ChEMBL | 499 | 5 | 1 | 4 | 3.9 | CN(C)CCn1cc2c3c1CC=CC3C1=C[C@@H](C(=O)N3CCCC3)CN(C(=O)Nc3ccccc3)[C@@H]1C2 | 10.1021/acs.jmedchem.5b01337 | |||
171344809 | 194493 | None | 0 | Human | Binding | pIC50 | = | 8.7 | 8.7 | - | 0 | ChEMBL | 499 | 5 | 1 | 4 | 3.9 | CN(C)CCn1cc2c3c1CC=CC3C1=C[C@@H](C(=O)N3CCCC3)CN(C(=O)Nc3ccccc3)[C@@H]1C2 | 10.1021/acs.jmedchem.5b01337 | |||
CHEMBL5287540 | 194493 | None | 0 | Human | Binding | pIC50 | = | 8.7 | 8.7 | - | 0 | ChEMBL | 499 | 5 | 1 | 4 | 3.9 | CN(C)CCn1cc2c3c1CC=CC3C1=C[C@@H](C(=O)N3CCCC3)CN(C(=O)Nc3ccccc3)[C@@H]1C2 | 10.1021/acs.jmedchem.5b01337 | |||
171347346 | 194311 | None | 0 | Human | Binding | pIC50 | = | 8 | 8.0 | - | 0 | ChEMBL | 548 | 5 | 2 | 9 | 2.1 | O=C(Cn1c(=O)[nH]c2ccccc21)N1CCN(c2ncc(Cl)cc2-c2cnc(N3CCC(O)CC3)nc2)CC1 | 10.1021/acs.jmedchem.5b01337 | |||
CHEMBL5283371 | 194311 | None | 0 | Human | Binding | pIC50 | = | 8 | 8.0 | - | 0 | ChEMBL | 548 | 5 | 2 | 9 | 2.1 | O=C(Cn1c(=O)[nH]c2ccccc21)N1CCN(c2ncc(Cl)cc2-c2cnc(N3CCC(O)CC3)nc2)CC1 | 10.1021/acs.jmedchem.5b01337 | |||
72188563 | 143059 | None | 0 | Human | Binding | pIC50 | = | 8 | 8.0 | - | 0 | ChEMBL | 486 | 12 | 1 | 5 | 4.6 | CCCN(Cc1ccc(OCCN2C(=O)CCC2=O)c(C)c1)[C@@H](CC(=O)O)c1ccc(Cl)cc1 | 10.1021/acs.jmedchem.5b01337 | |||
CHEMBL3894359 | 143059 | None | 0 | Human | Binding | pIC50 | = | 8 | 8.0 | - | 0 | ChEMBL | 486 | 12 | 1 | 5 | 4.6 | CCCN(Cc1ccc(OCCN2C(=O)CCC2=O)c(C)c1)[C@@H](CC(=O)O)c1ccc(Cl)cc1 | 10.1021/acs.jmedchem.5b01337 | |||
45486560 | 201013 | None | 0 | Human | Binding | pIC50 | = | 8 | 8.0 | - | 0 | ChEMBL | 615 | 9 | 0 | 8 | 4.4 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(C(F)(F)F)c(F)c1)[C@H](C)c1nc2ncccc2c(=O)n1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2011.10.120 | |||
CHEMBL578197 | 201013 | None | 0 | Human | Binding | pIC50 | = | 8 | 8.0 | - | 0 | ChEMBL | 615 | 9 | 0 | 8 | 4.4 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(C(F)(F)F)c(F)c1)[C@H](C)c1nc2ncccc2c(=O)n1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2011.10.120 | |||
44447097 | 154971 | None | 0 | Human | Binding | pIC50 | = | 8 | 8.0 | - | 0 | ChEMBL | 587 | 9 | 0 | 7 | 5.0 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc2ncccn2c1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2007.11.060 | |||
CHEMBL400736 | 154971 | None | 0 | Human | Binding | pIC50 | = | 8 | 8.0 | - | 0 | ChEMBL | 587 | 9 | 0 | 7 | 5.0 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc2ncccn2c1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2007.11.060 | |||
44447097 | 154971 | None | 0 | Human | Binding | pIC50 | = | 8 | 8.0 | - | 0 | ChEMBL | 587 | 9 | 0 | 7 | 5.0 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc2ncccn2c1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2009.07.021 | |||
CHEMBL400736 | 154971 | None | 0 | Human | Binding | pIC50 | = | 8 | 8.0 | - | 0 | ChEMBL | 587 | 9 | 0 | 7 | 5.0 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc2ncccn2c1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2009.07.021 | |||
45486560 | 201013 | None | 0 | Human | Binding | pIC50 | = | 8 | 8.0 | - | 0 | ChEMBL | 615 | 9 | 0 | 8 | 4.4 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(C(F)(F)F)c(F)c1)[C@H](C)c1nc2ncccc2c(=O)n1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2009.07.021 | |||
CHEMBL578197 | 201013 | None | 0 | Human | Binding | pIC50 | = | 8 | 8.0 | - | 0 | ChEMBL | 615 | 9 | 0 | 8 | 4.4 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(C(F)(F)F)c(F)c1)[C@H](C)c1nc2ncccc2c(=O)n1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2009.07.021 | |||
45486556 | 200130 | None | 0 | Human | Binding | pIC50 | = | 8 | 8.0 | - | 0 | ChEMBL | 645 | 10 | 0 | 9 | 4.4 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc2nc(OC)ccc2c(=O)n1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2009.07.021 | |||
CHEMBL571081 | 200130 | None | 0 | Human | Binding | pIC50 | = | 8 | 8.0 | - | 0 | ChEMBL | 645 | 10 | 0 | 9 | 4.4 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc2nc(OC)ccc2c(=O)n1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2009.07.021 | |||
45486524 | 201008 | None | 0 | Human | Binding | pIC50 | = | 8 | 8.0 | - | 0 | ChEMBL | 601 | 9 | 0 | 7 | 5.3 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(C(F)(F)F)c(F)c1)[C@H](C)c1nc2c(C)nccn2c1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2009.07.021 | |||
CHEMBL578188 | 201008 | None | 0 | Human | Binding | pIC50 | = | 8 | 8.0 | - | 0 | ChEMBL | 601 | 9 | 0 | 7 | 5.3 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(C(F)(F)F)c(F)c1)[C@H](C)c1nc2c(C)nccn2c1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2009.07.021 | |||
44455463 | 95684 | None | 0 | Human | Binding | pIC50 | = | 8 | 8.0 | - | 0 | ChEMBL | 606 | 11 | 1 | 7 | 4.8 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc(C2CC2)c(CO)n1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2007.11.072 | |||
CHEMBL257908 | 95684 | None | 0 | Human | Binding | pIC50 | = | 8 | 8.0 | - | 0 | ChEMBL | 606 | 11 | 1 | 7 | 4.8 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc(C2CC2)c(CO)n1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2007.11.072 | |||
71677963 | 143125 | None | 0 | Human | Binding | pIC50 | = | 8 | 8.0 | - | 0 | ChEMBL | 491 | 4 | 1 | 8 | 2.8 | Cn1c(=O)n(CC(=O)N2CCN(c3scnc3-c3nc4ccc(F)cc4[nH]3)CC2)c2ccccc21 | nan | |||
CHEMBL3894900 | 143125 | None | 0 | Human | Binding | pIC50 | = | 8 | 8.0 | - | 0 | ChEMBL | 491 | 4 | 1 | 8 | 2.8 | Cn1c(=O)n(CC(=O)N2CCN(c3scnc3-c3nc4ccc(F)cc4[nH]3)CC2)c2ccccc21 | nan | |||
124037260 | 153310 | None | 0 | Human | Binding | pIC50 | = | 8 | 8.0 | - | 0 | ChEMBL | 456 | 4 | 2 | 5 | 4.4 | C[C@@H]1CN(c2scnc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cc1c[nH]c2ccccc12 | nan | |||
CHEMBL3977300 | 153310 | None | 0 | Human | Binding | pIC50 | = | 8 | 8.0 | - | 0 | ChEMBL | 456 | 4 | 2 | 5 | 4.4 | C[C@@H]1CN(c2scnc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cc1c[nH]c2ccccc12 | nan | |||
71678295 | 153648 | None | 0 | Human | Binding | pIC50 | = | 8 | 8.0 | - | 0 | ChEMBL | 503 | 5 | 2 | 9 | 2.2 | Cn1c(=O)n(CC(=O)N2CCN(c3scnc3-c3nc4ccc(CO)cc4[nH]3)CC2)c2ccccc21 | nan | |||
CHEMBL3980213 | 153648 | None | 0 | Human | Binding | pIC50 | = | 8 | 8.0 | - | 0 | ChEMBL | 503 | 5 | 2 | 9 | 2.2 | Cn1c(=O)n(CC(=O)N2CCN(c3scnc3-c3nc4ccc(CO)cc4[nH]3)CC2)c2ccccc21 | nan | |||
89726299 | 153813 | None | 0 | Human | Binding | pIC50 | = | 8 | 8.0 | - | 0 | ChEMBL | 489 | 4 | 2 | 9 | 2.4 | Cn1c(=O)n(CC(=O)N2CCN(c3scnc3-c3nc4c(O)cccc4[nH]3)CC2)c2ccccc21 | nan | |||
CHEMBL3981664 | 153813 | None | 0 | Human | Binding | pIC50 | = | 8 | 8.0 | - | 0 | ChEMBL | 489 | 4 | 2 | 9 | 2.4 | Cn1c(=O)n(CC(=O)N2CCN(c3scnc3-c3nc4c(O)cccc4[nH]3)CC2)c2ccccc21 | nan | |||
121485701 | 276 | None | 10 | Mouse | Binding | pIC50 | = | 8.0 | 8.0 | - | 1 | ChEMBL | 550 | 6 | 1 | 10 | 2.6 | CC1=NN(C=N1)CC(=O)N2CCN(C[C@H]2CCO)C3=C(N=C(S3)C(F)(F)F)C4=CN=C(N=C4)C(F)(F)F | 10.1021/acs.jmedchem.3c00074 | |||
12584 | 276 | None | 10 | Mouse | Binding | pIC50 | = | 8.0 | 8.0 | - | 1 | ChEMBL | 550 | 6 | 1 | 10 | 2.6 | CC1=NN(C=N1)CC(=O)N2CCN(C[C@H]2CCO)C3=C(N=C(S3)C(F)(F)F)C4=CN=C(N=C4)C(F)(F)F | 10.1021/acs.jmedchem.3c00074 | |||
CHEMBL5279308 | 276 | None | 10 | Mouse | Binding | pIC50 | = | 8.0 | 8.0 | - | 1 | ChEMBL | 550 | 6 | 1 | 10 | 2.6 | CC1=NN(C=N1)CC(=O)N2CCN(C[C@H]2CCO)C3=C(N=C(S3)C(F)(F)F)C4=CN=C(N=C4)C(F)(F)F | 10.1021/acs.jmedchem.3c00074 | |||
121485701 | 276 | None | 10 | Human | Binding | pIC50 | = | 8.0 | 8.0 | - | 1 | ChEMBL | 550 | 6 | 1 | 10 | 2.6 | CC1=NN(C=N1)CC(=O)N2CCN(C[C@H]2CCO)C3=C(N=C(S3)C(F)(F)F)C4=CN=C(N=C4)C(F)(F)F | 10.1021/acs.jmedchem.3c00074 | |||
12584 | 276 | None | 10 | Human | Binding | pIC50 | = | 8.0 | 8.0 | - | 1 | ChEMBL | 550 | 6 | 1 | 10 | 2.6 | CC1=NN(C=N1)CC(=O)N2CCN(C[C@H]2CCO)C3=C(N=C(S3)C(F)(F)F)C4=CN=C(N=C4)C(F)(F)F | 10.1021/acs.jmedchem.3c00074 | |||
CHEMBL5279308 | 276 | None | 10 | Human | Binding | pIC50 | = | 8.0 | 8.0 | - | 1 | ChEMBL | 550 | 6 | 1 | 10 | 2.6 | CC1=NN(C=N1)CC(=O)N2CCN(C[C@H]2CCO)C3=C(N=C(S3)C(F)(F)F)C4=CN=C(N=C4)C(F)(F)F | 10.1021/acs.jmedchem.3c00074 | |||
6143230 | 7191 | None | 0 | Human | Binding | pIC50 | = | 7 | 7.0 | - | 1 | ChEMBL | 588 | 10 | 2 | 5 | 5.8 | CC(=O)Nc1cccc(/C(C)=N\NC(=O)c2ccc(CN(Cc3ccccc3)S(=O)(=O)c3ccc(Cl)cc3)cc2)c1 | 10.1021/acs.jmedchem.5b01337 | |||
CHEMBL1085565 | 7191 | None | 0 | Human | Binding | pIC50 | = | 7 | 7.0 | - | 1 | ChEMBL | 588 | 10 | 2 | 5 | 5.8 | CC(=O)Nc1cccc(/C(C)=N\NC(=O)c2ccc(CN(Cc3ccccc3)S(=O)(=O)c3ccc(Cl)cc3)cc2)c1 | 10.1021/acs.jmedchem.5b01337 | |||
11296495 | 72755 | None | 22 | Human | Binding | pIC50 | = | 7 | 7.0 | - | 0 | ChEMBL | 615 | 8 | 3 | 4 | 6.1 | CCNC(=O)N1CCCN(c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2NC(=O)c2cccc(Cl)c2)CC1 | 10.1021/acs.jmedchem.5b01337 | |||
CHEMBL199839 | 72755 | None | 22 | Human | Binding | pIC50 | = | 7 | 7.0 | - | 0 | ChEMBL | 615 | 8 | 3 | 4 | 6.1 | CCNC(=O)N1CCCN(c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2NC(=O)c2cccc(Cl)c2)CC1 | 10.1021/acs.jmedchem.5b01337 | |||
11296495 | 72755 | None | 22 | Human | Binding | pIC50 | = | 7 | 7.0 | - | 0 | ChEMBL | 615 | 8 | 3 | 4 | 6.1 | CCNC(=O)N1CCCN(c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2NC(=O)c2cccc(Cl)c2)CC1 | 10.1021/acs.jmedchem.5b01337 | |||
CHEMBL199839 | 72755 | None | 22 | Human | Binding | pIC50 | = | 7 | 7.0 | - | 0 | ChEMBL | 615 | 8 | 3 | 4 | 6.1 | CCNC(=O)N1CCCN(c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2NC(=O)c2cccc(Cl)c2)CC1 | 10.1021/acs.jmedchem.5b01337 | |||
44426697 | 152461 | None | 0 | Human | Binding | pIC50 | = | 7 | 7.0 | - | 0 | ChEMBL | 566 | 7 | 0 | 6 | 6.3 | C[C@H](c1nc2ccccc2c(=O)n1-c1ccc(F)cc1)N(Cc1nccs1)C(=O)Cc1ccc(C(F)(F)F)cc1 | 10.1016/j.bmcl.2007.03.106 | |||
CHEMBL397020 | 152461 | None | 0 | Human | Binding | pIC50 | = | 7 | 7.0 | - | 0 | ChEMBL | 566 | 7 | 0 | 6 | 6.3 | C[C@H](c1nc2ccccc2c(=O)n1-c1ccc(F)cc1)N(Cc1nccs1)C(=O)Cc1ccc(C(F)(F)F)cc1 | 10.1016/j.bmcl.2007.03.106 | |||
25008271 | 95311 | None | 0 | Human | Binding | pIC50 | = | 7 | 7.0 | - | 0 | ChEMBL | 313 | 3 | 1 | 4 | 3.3 | Cc1cccc2c1n(C)c(=N)n2CC(=O)c1ccc(Cl)cc1 | 10.1021/acs.jmedchem.5b01337 | |||
CHEMBL256226 | 95311 | None | 0 | Human | Binding | pIC50 | = | 7 | 7.0 | - | 0 | ChEMBL | 313 | 3 | 1 | 4 | 3.3 | Cc1cccc2c1n(C)c(=N)n2CC(=O)c1ccc(Cl)cc1 | 10.1021/acs.jmedchem.5b01337 | |||
25008271 | 95311 | None | 0 | Human | Binding | pIC50 | = | 7 | 7.0 | - | 0 | ChEMBL | 313 | 3 | 1 | 4 | 3.3 | Cc1cccc2c1n(C)c(=N)n2CC(=O)c1ccc(Cl)cc1 | 10.1016/j.bmcl.2008.01.074 | |||
CHEMBL256226 | 95311 | None | 0 | Human | Binding | pIC50 | = | 7 | 7.0 | - | 0 | ChEMBL | 313 | 3 | 1 | 4 | 3.3 | Cc1cccc2c1n(C)c(=N)n2CC(=O)c1ccc(Cl)cc1 | 10.1016/j.bmcl.2008.01.074 | |||
89726207 | 146692 | None | 0 | Human | Binding | pIC50 | = | 7 | 7.0 | - | 0 | ChEMBL | 529 | 7 | 2 | 8 | 3.8 | C[C@@H]1CN(c2sc(CCC(=O)O)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1ccc2cccnc21 | nan | |||
CHEMBL3923194 | 146692 | None | 0 | Human | Binding | pIC50 | = | 7 | 7.0 | - | 0 | ChEMBL | 529 | 7 | 2 | 8 | 3.8 | C[C@@H]1CN(c2sc(CCC(=O)O)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1ccc2cccnc21 | nan | |||
72548179 | 146786 | None | 0 | Human | Binding | pIC50 | = | 7 | 7.0 | - | 0 | ChEMBL | 534 | 13 | 1 | 5 | 5.6 | CCCCN(Cc1ccc(OCCN2C(=O)CCC2=O)c(C)c1)C(CC(=O)O)c1ccc(Cl)c(Cl)c1 | nan | |||
CHEMBL3923943 | 146786 | None | 0 | Human | Binding | pIC50 | = | 7 | 7.0 | - | 0 | ChEMBL | 534 | 13 | 1 | 5 | 5.6 | CCCCN(Cc1ccc(OCCN2C(=O)CCC2=O)c(C)c1)C(CC(=O)O)c1ccc(Cl)c(Cl)c1 | nan | |||
71585401 | 132388 | None | 0 | Human | Binding | pIC50 | = | 6 | 6.0 | - | 0 | ChEMBL | 566 | 11 | 1 | 5 | 5.8 | COc1cc(CN(C[C@H]2CC[C@H](C(=O)O)CC2)[C@@H]2CCc3cc(Cl)ccc32)ccc1CCCN1C(=O)CCC1=O | nan | |||
CHEMBL3697083 | 132388 | None | 0 | Human | Binding | pIC50 | = | 6 | 6.0 | - | 0 | ChEMBL | 566 | 11 | 1 | 5 | 5.8 | COc1cc(CN(C[C@H]2CC[C@H](C(=O)O)CC2)[C@@H]2CCc3cc(Cl)ccc32)ccc1CCCN1C(=O)CCC1=O | nan | |||
71585504 | 132387 | None | 0 | Human | Binding | pIC50 | = | 6 | 6.0 | - | 0 | ChEMBL | 566 | 11 | 1 | 5 | 5.8 | COc1cc(CN(C[C@H]2CC[C@H](C(=O)O)CC2)[C@H]2CCc3cc(Cl)ccc32)ccc1CCCN1C(=O)CCC1=O | 10.1016/j.bmcl.2016.10.035 | |||
CHEMBL3697082 | 132387 | None | 0 | Human | Binding | pIC50 | = | 6 | 6.0 | - | 0 | ChEMBL | 566 | 11 | 1 | 5 | 5.8 | COc1cc(CN(C[C@H]2CC[C@H](C(=O)O)CC2)[C@H]2CCc3cc(Cl)ccc32)ccc1CCCN1C(=O)CCC1=O | 10.1016/j.bmcl.2016.10.035 | |||
44454895 | 95396 | None | 1 | Human | Binding | pIC50 | = | 6 | 6.0 | - | 0 | ChEMBL | 313 | 3 | 1 | 4 | 3.3 | Cc1ccc2c(c1)n(C)c(=N)n2CC(=O)c1ccc(Cl)cc1 | 10.1016/j.bmcl.2008.01.074 | |||
CHEMBL256647 | 95396 | None | 1 | Human | Binding | pIC50 | = | 6 | 6.0 | - | 0 | ChEMBL | 313 | 3 | 1 | 4 | 3.3 | Cc1ccc2c(c1)n(C)c(=N)n2CC(=O)c1ccc(Cl)cc1 | 10.1016/j.bmcl.2008.01.074 | |||
17754836 | 98086 | None | 0 | Human | Binding | pIC50 | = | 6 | 6.0 | - | 0 | ChEMBL | 401 | 6 | 0 | 5 | 3.2 | COCC/N=c1/n(C)c2ccccc2n1CC(=O)c1ccc(Br)cc1 | 10.1016/j.bmcl.2008.01.074 | |||
CHEMBL273013 | 98086 | None | 0 | Human | Binding | pIC50 | = | 6 | 6.0 | - | 0 | ChEMBL | 401 | 6 | 0 | 5 | 3.2 | COCC/N=c1/n(C)c2ccccc2n1CC(=O)c1ccc(Br)cc1 | 10.1016/j.bmcl.2008.01.074 | |||
71457439 | 83058 | None | 8 | Human | Binding | pIC50 | = | 6 | 6.0 | - | 1 | ChEMBL | 644 | 15 | 3 | 5 | 5.2 | NCCCC[C@H](NC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCC(=O)c1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.6b01309 | |||
CHEMBL2181467 | 83058 | None | 8 | Human | Binding | pIC50 | = | 6 | 6.0 | - | 1 | ChEMBL | 644 | 15 | 3 | 5 | 5.2 | NCCCC[C@H](NC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCC(=O)c1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.6b01309 | |||
CHEMBL3787171 | 83058 | None | 8 | Human | Binding | pIC50 | = | 6 | 6.0 | - | 1 | ChEMBL | 644 | 15 | 3 | 5 | 5.2 | NCCCC[C@H](NC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCC(=O)c1ccccc1)C(=O)NCC(c1ccccc1)c1ccccc1 | 10.1021/acs.jmedchem.6b01309 | |||
44426715 | 150979 | None | 0 | Human | Binding | pIC50 | = | 5 | 5.0 | - | 0 | ChEMBL | 620 | 8 | 0 | 7 | 5.5 | C[C@H](c1nc2ccccc2c(=O)n1-c1ccc(S(C)(=O)=O)cc1)N(Cc1cccnc1)C(=O)Cc1ccc(C(F)(F)F)cc1 | 10.1016/j.bmcl.2007.03.106 | |||
CHEMBL395747 | 150979 | None | 0 | Human | Binding | pIC50 | = | 5 | 5.0 | - | 0 | ChEMBL | 620 | 8 | 0 | 7 | 5.5 | C[C@H](c1nc2ccccc2c(=O)n1-c1ccc(S(C)(=O)=O)cc1)N(Cc1cccnc1)C(=O)Cc1ccc(C(F)(F)F)cc1 | 10.1016/j.bmcl.2007.03.106 | |||
44455825 | 155180 | None | 0 | Human | Binding | pIC50 | = | 5 | 5.0 | - | 0 | ChEMBL | 652 | 11 | 0 | 6 | 7.0 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc(C2CC2)c(-c2ccccc2)n1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2007.11.072 | |||
CHEMBL401888 | 155180 | None | 0 | Human | Binding | pIC50 | = | 5 | 5.0 | - | 0 | ChEMBL | 652 | 11 | 0 | 6 | 7.0 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc(C2CC2)c(-c2ccccc2)n1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2007.11.072 | |||
44402370 | 133430 | None | 0 | Human | Binding | pIC50 | = | 5 | 5.0 | - | 0 | ChEMBL | 515 | 14 | 0 | 6 | 5.8 | CCCCCCCCCC(=O)N(CCN(C)C)C(C)c1nc2ccccc2c(=O)n1-c1ccccc1C#N | 10.1016/j.bmcl.2005.03.070 | |||
CHEMBL370482 | 133430 | None | 0 | Human | Binding | pIC50 | = | 5 | 5.0 | - | 0 | ChEMBL | 515 | 14 | 0 | 6 | 5.8 | CCCCCCCCCC(=O)N(CCN(C)C)C(C)c1nc2ccccc2c(=O)n1-c1ccccc1C#N | 10.1016/j.bmcl.2005.03.070 | |||
56667005 | 64253 | None | 0 | Human | Binding | pIC50 | = | 6 | 6.0 | - | 0 | ChEMBL | 441 | 2 | 3 | 3 | 3.1 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CCNCC1 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1809004 | 64253 | None | 0 | Human | Binding | pIC50 | = | 6 | 6.0 | - | 0 | ChEMBL | 441 | 2 | 3 | 3 | 3.1 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CCNCC1 | 10.1016/j.bmcl.2011.06.070 | |||
89610566 | 132403 | None | 0 | Human | Binding | pIC50 | = | 7.0 | 7.0 | - | 0 | ChEMBL | 531 | 11 | 1 | 6 | 4.8 | Cc1cc(CN(C[C@H]2CC[C@H](C(=O)O)CC2)C(C)c2ccc(C#N)cc2)ccc1OCCN1C(=O)CCC1=O | nan | |||
CHEMBL3697098 | 132403 | None | 0 | Human | Binding | pIC50 | = | 7.0 | 7.0 | - | 0 | ChEMBL | 531 | 11 | 1 | 6 | 4.8 | Cc1cc(CN(C[C@H]2CC[C@H](C(=O)O)CC2)C(C)c2ccc(C#N)cc2)ccc1OCCN1C(=O)CCC1=O | nan | |||
168279606 | 191087 | None | 0 | Human | Binding | pIC50 | = | 7.0 | 7.0 | - | 0 | ChEMBL | 495 | 6 | 0 | 9 | 3.3 | CCOc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3ccc(C)n3)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL5186167 | 191087 | None | 0 | Human | Binding | pIC50 | = | 7.0 | 7.0 | - | 0 | ChEMBL | 495 | 6 | 0 | 9 | 3.3 | CCOc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3ccc(C)n3)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
89610480 | 132840 | None | 0 | Human | Binding | pIC50 | = | 7.0 | 7.0 | - | 0 | ChEMBL | 548 | 11 | 1 | 6 | 5.0 | COc1cc(CN(C(C)c2ccc(Cl)c(Cl)c2)[C@H]2C[C@@H](C(=O)O)C2)ccc1OCCN1C(=O)CCC1=O | nan | |||
CHEMBL3700571 | 132840 | None | 0 | Human | Binding | pIC50 | = | 7.0 | 7.0 | - | 0 | ChEMBL | 548 | 11 | 1 | 6 | 5.0 | COc1cc(CN(C(C)c2ccc(Cl)c(Cl)c2)[C@H]2C[C@@H](C(=O)O)C2)ccc1OCCN1C(=O)CCC1=O | nan | |||
168288472 | 191828 | None | 0 | Human | Binding | pIC50 | = | 7.0 | 7.0 | - | 0 | ChEMBL | 502 | 4 | 0 | 9 | 3.4 | Cc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3cnc4cccnc43)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL5197065 | 191828 | None | 0 | Human | Binding | pIC50 | = | 7.0 | 7.0 | - | 0 | ChEMBL | 502 | 4 | 0 | 9 | 3.4 | Cc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3cnc4cccnc43)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
90479922 | 190733 | None | 0 | Human | Binding | pIC50 | = | 6.0 | 6.0 | - | 0 | ChEMBL | 496 | 5 | 0 | 10 | 2.6 | COc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3nc(C)nc3C)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL5181086 | 190733 | None | 0 | Human | Binding | pIC50 | = | 6.0 | 6.0 | - | 0 | ChEMBL | 496 | 5 | 0 | 10 | 2.6 | COc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3nc(C)nc3C)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
89610570 | 132468 | None | 0 | Human | Binding | pIC50 | = | 7.0 | 7.0 | - | 0 | ChEMBL | 512 | 10 | 1 | 5 | 4.9 | Cc1cc([C@@H](C)N(Cc2ccc(OCCN3C(=O)CCC3=O)c(C)c2)[C@H]2C[C@@H](C(=O)O)C2)ccc1Cl | nan | |||
CHEMBL3697163 | 132468 | None | 0 | Human | Binding | pIC50 | = | 7.0 | 7.0 | - | 0 | ChEMBL | 512 | 10 | 1 | 5 | 4.9 | Cc1cc([C@@H](C)N(Cc2ccc(OCCN3C(=O)CCC3=O)c(C)c2)[C@H]2C[C@@H](C(=O)O)C2)ccc1Cl | nan | |||
90014252 | 145147 | None | 0 | Human | Binding | pIC50 | = | 7.0 | 7.0 | - | 0 | ChEMBL | 492 | 12 | 1 | 6 | 4.7 | CCCN(Cc1ccc(OCCN2C(=O)CCC2=O)c(C)c1)C(CC(=O)O)c1ccc(Cl)s1 | 10.1016/j.bmcl.2016.10.038 | |||
CHEMBL3911387 | 145147 | None | 0 | Human | Binding | pIC50 | = | 7.0 | 7.0 | - | 0 | ChEMBL | 492 | 12 | 1 | 6 | 4.7 | CCCN(Cc1ccc(OCCN2C(=O)CCC2=O)c(C)c1)C(CC(=O)O)c1ccc(Cl)s1 | 10.1016/j.bmcl.2016.10.038 | |||
CHEMBL3958513 | 145147 | None | 0 | Human | Binding | pIC50 | = | 7.0 | 7.0 | - | 0 | ChEMBL | 492 | 12 | 1 | 6 | 4.7 | CCCN(Cc1ccc(OCCN2C(=O)CCC2=O)c(C)c1)C(CC(=O)O)c1ccc(Cl)s1 | 10.1016/j.bmcl.2016.10.038 | |||
90014252 | 145147 | None | 0 | Human | Binding | pIC50 | = | 7.0 | 7.0 | - | 0 | ChEMBL | 492 | 12 | 1 | 6 | 4.7 | CCCN(Cc1ccc(OCCN2C(=O)CCC2=O)c(C)c1)C(CC(=O)O)c1ccc(Cl)s1 | nan | |||
CHEMBL3911387 | 145147 | None | 0 | Human | Binding | pIC50 | = | 7.0 | 7.0 | - | 0 | ChEMBL | 492 | 12 | 1 | 6 | 4.7 | CCCN(Cc1ccc(OCCN2C(=O)CCC2=O)c(C)c1)C(CC(=O)O)c1ccc(Cl)s1 | nan | |||
CHEMBL3958513 | 145147 | None | 0 | Human | Binding | pIC50 | = | 7.0 | 7.0 | - | 0 | ChEMBL | 492 | 12 | 1 | 6 | 4.7 | CCCN(Cc1ccc(OCCN2C(=O)CCC2=O)c(C)c1)C(CC(=O)O)c1ccc(Cl)s1 | nan | |||
89610739 | 132861 | None | 0 | Human | Binding | pIC50 | = | 6.0 | 6.0 | - | 0 | ChEMBL | 540 | 11 | 1 | 6 | 4.5 | COc1cc(CN(CC2CC(C(=O)O)C2)[C@H]2CCc3cc(Cl)ccc32)ccc1OCCN1C(=O)CCC1=O | nan | |||
CHEMBL3700592 | 132861 | None | 0 | Human | Binding | pIC50 | = | 6.0 | 6.0 | - | 0 | ChEMBL | 540 | 11 | 1 | 6 | 4.5 | COc1cc(CN(CC2CC(C(=O)O)C2)[C@H]2CCc3cc(Cl)ccc32)ccc1OCCN1C(=O)CCC1=O | nan | |||
89610442 | 148303 | None | 0 | Human | Binding | pIC50 | = | 6.0 | 6.0 | - | 0 | ChEMBL | 438 | 10 | 1 | 6 | 3.4 | CCC(NCc1ccc(OCCN2C(=O)CCC2=O)c(OC)c1)c1ccc2c(c1)CCO2 | 10.1016/j.bmcl.2016.10.035 | |||
CHEMBL3936007 | 148303 | None | 0 | Human | Binding | pIC50 | = | 6.0 | 6.0 | - | 0 | ChEMBL | 438 | 10 | 1 | 6 | 3.4 | CCC(NCc1ccc(OCCN2C(=O)CCC2=O)c(OC)c1)c1ccc2c(c1)CCO2 | 10.1016/j.bmcl.2016.10.035 | |||
89726154 | 152067 | None | 0 | Human | Binding | pIC50 | = | 6.0 | 6.0 | - | 0 | ChEMBL | 472 | 4 | 1 | 8 | 3.5 | Cc1nc(-c2nc3ccccc3[nH]2)c(N2CCN(C(=O)Cn3cnc4cccnc43)[C@H](C)C2)s1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL3966706 | 152067 | None | 0 | Human | Binding | pIC50 | = | 6.0 | 6.0 | - | 0 | ChEMBL | 472 | 4 | 1 | 8 | 3.5 | Cc1nc(-c2nc3ccccc3[nH]2)c(N2CCN(C(=O)Cn3cnc4cccnc43)[C@H](C)C2)s1 | 10.1021/acs.jmedchem.2c00675 | |||
71586103 | 132425 | None | 0 | Human | Binding | pIC50 | = | 7.0 | 7.0 | - | 0 | ChEMBL | 536 | 12 | 1 | 6 | 5.0 | COc1cc(CN(C[C@H]2CC[C@H](C(=O)O)CC2)C(C)c2ccc(C)cc2)ccc1OCCN1C(=O)CCC1=O | nan | |||
CHEMBL3697121 | 132425 | None | 0 | Human | Binding | pIC50 | = | 7.0 | 7.0 | - | 0 | ChEMBL | 536 | 12 | 1 | 6 | 5.0 | COc1cc(CN(C[C@H]2CC[C@H](C(=O)O)CC2)C(C)c2ccc(C)cc2)ccc1OCCN1C(=O)CCC1=O | nan | |||
72550476 | 146227 | None | 0 | Human | Binding | pIC50 | = | 7.0 | 7.0 | - | 0 | ChEMBL | 520 | 13 | 1 | 6 | 4.4 | CCCN(Cc1ccc(OCCN2C(=O)CCC2=O)c(OC)c1)C(CC(=O)O)c1ccc(Cl)c(F)c1 | nan | |||
CHEMBL3919682 | 146227 | None | 0 | Human | Binding | pIC50 | = | 7.0 | 7.0 | - | 0 | ChEMBL | 520 | 13 | 1 | 6 | 4.4 | CCCN(Cc1ccc(OCCN2C(=O)CCC2=O)c(OC)c1)C(CC(=O)O)c1ccc(Cl)c(F)c1 | nan | |||
71679797 | 148643 | None | 0 | Human | Binding | pIC50 | = | 6.0 | 6.0 | - | 0 | ChEMBL | 422 | 4 | 1 | 8 | 2.2 | Cc1nc(C)n(CC(=O)N2CCN(c3scnc3-c3nc4ccccc4[nH]3)CC2)n1 | nan | |||
CHEMBL3938795 | 148643 | None | 0 | Human | Binding | pIC50 | = | 6.0 | 6.0 | - | 0 | ChEMBL | 422 | 4 | 1 | 8 | 2.2 | Cc1nc(C)n(CC(=O)N2CCN(c3scnc3-c3nc4ccccc4[nH]3)CC2)n1 | nan | |||
71586305 | 132440 | None | 0 | Human | Binding | pIC50 | = | 7.0 | 7.0 | - | 0 | ChEMBL | 542 | 12 | 1 | 6 | 4.9 | COc1cc(CN(C[C@H]2CC[C@H](C(=O)O)C2)[C@@H](C)c2ccc(Cl)cc2)ccc1OCCN1C(=O)CCC1=O | nan | |||
CHEMBL3697136 | 132440 | None | 0 | Human | Binding | pIC50 | = | 7.0 | 7.0 | - | 0 | ChEMBL | 542 | 12 | 1 | 6 | 4.9 | COc1cc(CN(C[C@H]2CC[C@H](C(=O)O)C2)[C@@H](C)c2ccc(Cl)cc2)ccc1OCCN1C(=O)CCC1=O | nan | |||
72549588 | 146849 | None | 0 | Human | Binding | pIC50 | = | 7.0 | 7.0 | - | 0 | ChEMBL | 543 | 13 | 1 | 8 | 4.0 | COc1cc(CN(CC(C)C)[C@H](CC(=O)O)c2ccc(Cl)cc2)ccc1OCCn1c(=O)ccn(C)c1=O | 10.1016/j.bmcl.2016.10.038 | |||
CHEMBL3924414 | 146849 | None | 0 | Human | Binding | pIC50 | = | 7.0 | 7.0 | - | 0 | ChEMBL | 543 | 13 | 1 | 8 | 4.0 | COc1cc(CN(CC(C)C)[C@H](CC(=O)O)c2ccc(Cl)cc2)ccc1OCCn1c(=O)ccn(C)c1=O | 10.1016/j.bmcl.2016.10.038 | |||
72549588 | 146849 | None | 0 | Human | Binding | pIC50 | = | 7.0 | 7.0 | - | 0 | ChEMBL | 543 | 13 | 1 | 8 | 4.0 | COc1cc(CN(CC(C)C)[C@H](CC(=O)O)c2ccc(Cl)cc2)ccc1OCCn1c(=O)ccn(C)c1=O | nan | |||
CHEMBL3924414 | 146849 | None | 0 | Human | Binding | pIC50 | = | 7.0 | 7.0 | - | 0 | ChEMBL | 543 | 13 | 1 | 8 | 4.0 | COc1cc(CN(CC(C)C)[C@H](CC(=O)O)c2ccc(Cl)cc2)ccc1OCCn1c(=O)ccn(C)c1=O | nan | |||
124037265 | 152265 | None | 0 | Human | Binding | pIC50 | = | 7.0 | 7.0 | - | 0 | ChEMBL | 491 | 4 | 2 | 6 | 4.5 | C[C@@H]1CN(c2scnc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cc1nc2cc(Cl)ccc2[nH]1 | nan | |||
CHEMBL3968313 | 152265 | None | 0 | Human | Binding | pIC50 | = | 7.0 | 7.0 | - | 0 | ChEMBL | 491 | 4 | 2 | 6 | 4.5 | C[C@@H]1CN(c2scnc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cc1nc2cc(Cl)ccc2[nH]1 | nan | |||
72551141 | 152034 | None | 0 | Human | Binding | pIC50 | = | 7.0 | 7.0 | - | 0 | ChEMBL | 522 | 13 | 1 | 5 | 5.0 | CCCCN(Cc1ccc(OCCN2C(=O)CCC2=O)c(F)c1)C(CC(=O)O)c1ccc(Cl)c(F)c1 | nan | |||
CHEMBL3966388 | 152034 | None | 0 | Human | Binding | pIC50 | = | 7.0 | 7.0 | - | 0 | ChEMBL | 522 | 13 | 1 | 5 | 5.0 | CCCCN(Cc1ccc(OCCN2C(=O)CCC2=O)c(F)c1)C(CC(=O)O)c1ccc(Cl)c(F)c1 | nan | |||
71586397 | 132467 | None | 0 | Human | Binding | pIC50 | = | 6.0 | 6.0 | - | 0 | ChEMBL | 526 | 10 | 1 | 6 | 4.2 | COc1cc(CN(C2CC(C(=O)O)C2)C2CCc3cc(Cl)ccc32)ccc1OCCN1C(=O)CCC1=O | nan | |||
CHEMBL3697162 | 132467 | None | 0 | Human | Binding | pIC50 | = | 6.0 | 6.0 | - | 0 | ChEMBL | 526 | 10 | 1 | 6 | 4.2 | COc1cc(CN(C2CC(C(=O)O)C2)C2CCc3cc(Cl)ccc32)ccc1OCCN1C(=O)CCC1=O | nan | |||
44426714 | 86536 | None | 0 | Human | Binding | pIC50 | = | 8.0 | 8.0 | - | 0 | ChEMBL | 567 | 7 | 0 | 6 | 6.0 | C[C@H](c1nc2ccccc2c(=O)n1-c1ccc(C#N)cc1)N(Cc1cccnc1)C(=O)Cc1ccc(C(F)(F)F)cc1 | 10.1016/j.bmcl.2007.03.106 | |||
CHEMBL231486 | 86536 | None | 0 | Human | Binding | pIC50 | = | 8.0 | 8.0 | - | 0 | ChEMBL | 567 | 7 | 0 | 6 | 6.0 | C[C@H](c1nc2ccccc2c(=O)n1-c1ccc(C#N)cc1)N(Cc1cccnc1)C(=O)Cc1ccc(C(F)(F)F)cc1 | 10.1016/j.bmcl.2007.03.106 | |||
46883292 | 5653 | None | 0 | Human | Binding | pIC50 | = | 8.0 | 8.0 | - | 0 | ChEMBL | 586 | 9 | 0 | 6 | 6.5 | CCOc1ccc(-n2c([C@@H](C)N(Cc3cccnc3)C(=O)Cc3cccc(C(F)(F)F)c3)nc3ccccc3c2=O)cc1 | 10.1016/j.bmcl.2009.07.032 | |||
CHEMBL1077812 | 5653 | None | 0 | Human | Binding | pIC50 | = | 8.0 | 8.0 | - | 0 | ChEMBL | 586 | 9 | 0 | 6 | 6.5 | CCOc1ccc(-n2c([C@@H](C)N(Cc3cccnc3)C(=O)Cc3cccc(C(F)(F)F)c3)nc3ccccc3c2=O)cc1 | 10.1016/j.bmcl.2009.07.032 | |||
16040696 | 94850 | None | 1 | Human | Binding | pIC50 | = | 8.0 | 8.0 | - | 0 | ChEMBL | 615 | 9 | 0 | 8 | 4.4 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc2ncccc2c(=O)n1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2009.07.032 | |||
CHEMBL253431 | 94850 | None | 1 | Human | Binding | pIC50 | = | 8.0 | 8.0 | - | 0 | ChEMBL | 615 | 9 | 0 | 8 | 4.4 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc2ncccc2c(=O)n1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2009.07.032 | |||
72188563 | 143059 | None | 0 | Human | Binding | pIC50 | = | 8.0 | 8.0 | - | 0 | ChEMBL | 486 | 12 | 1 | 5 | 4.6 | CCCN(Cc1ccc(OCCN2C(=O)CCC2=O)c(C)c1)[C@@H](CC(=O)O)c1ccc(Cl)cc1 | 10.1016/j.bmcl.2016.10.038 | |||
CHEMBL3894359 | 143059 | None | 0 | Human | Binding | pIC50 | = | 8.0 | 8.0 | - | 0 | ChEMBL | 486 | 12 | 1 | 5 | 4.6 | CCCN(Cc1ccc(OCCN2C(=O)CCC2=O)c(C)c1)[C@@H](CC(=O)O)c1ccc(Cl)cc1 | 10.1016/j.bmcl.2016.10.038 | |||
16040696 | 94850 | None | 1 | Human | Binding | pIC50 | = | 8.0 | 8.0 | - | 0 | ChEMBL | 615 | 9 | 0 | 8 | 4.4 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc2ncccc2c(=O)n1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2011.10.120 | |||
CHEMBL253431 | 94850 | None | 1 | Human | Binding | pIC50 | = | 8.0 | 8.0 | - | 0 | ChEMBL | 615 | 9 | 0 | 8 | 4.4 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc2ncccc2c(=O)n1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2011.10.120 | |||
16040696 | 94850 | None | 1 | Human | Binding | pIC50 | = | 8.0 | 8.0 | - | 0 | ChEMBL | 615 | 9 | 0 | 8 | 4.4 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc2ncccc2c(=O)n1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2007.11.060 | |||
CHEMBL253431 | 94850 | None | 1 | Human | Binding | pIC50 | = | 8.0 | 8.0 | - | 0 | ChEMBL | 615 | 9 | 0 | 8 | 4.4 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc2ncccc2c(=O)n1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2007.11.060 | |||
16040696 | 94850 | None | 1 | Human | Binding | pIC50 | = | 8.0 | 8.0 | - | 0 | ChEMBL | 615 | 9 | 0 | 8 | 4.4 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc2ncccc2c(=O)n1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2009.07.021 | |||
CHEMBL253431 | 94850 | None | 1 | Human | Binding | pIC50 | = | 8.0 | 8.0 | - | 0 | ChEMBL | 615 | 9 | 0 | 8 | 4.4 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc2ncccc2c(=O)n1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2009.07.021 | |||
45486525 | 201009 | None | 0 | Human | Binding | pIC50 | = | 8.0 | 8.0 | - | 0 | ChEMBL | 615 | 10 | 0 | 7 | 5.6 | CCc1nccn2c(-c3ccc(C#N)cc3)c([C@@H](C)N(CCS(=O)(=O)CC)C(=O)Cc3ccc(C(F)(F)F)c(F)c3)nc12 | 10.1016/j.bmcl.2009.07.021 | |||
CHEMBL578189 | 201009 | None | 0 | Human | Binding | pIC50 | = | 8.0 | 8.0 | - | 0 | ChEMBL | 615 | 10 | 0 | 7 | 5.6 | CCc1nccn2c(-c3ccc(C#N)cc3)c([C@@H](C)N(CCS(=O)(=O)CC)C(=O)Cc3ccc(C(F)(F)F)c(F)c3)nc12 | 10.1016/j.bmcl.2009.07.021 | |||
11498089 | 97927 | None | 0 | Human | Binding | pIC50 | = | 8.0 | 8.0 | - | 0 | ChEMBL | 602 | 10 | 0 | 5 | 7.8 | CCOc1ccc(-n2cc(-c3ccccc3)nc2[C@@H](C)N(Cc2cccnc2)C(=O)Cc2ccc(F)c(C(F)(F)F)c2)cc1 | 10.1016/j.bmcl.2007.11.072 | |||
CHEMBL272290 | 97927 | None | 0 | Human | Binding | pIC50 | = | 8.0 | 8.0 | - | 0 | ChEMBL | 602 | 10 | 0 | 5 | 7.8 | CCOc1ccc(-n2cc(-c3ccccc3)nc2[C@@H](C)N(Cc2cccnc2)C(=O)Cc2ccc(F)c(C(F)(F)F)c2)cc1 | 10.1016/j.bmcl.2007.11.072 | |||
44455800 | 155140 | None | 0 | Human | Binding | pIC50 | = | 8.0 | 8.0 | - | 0 | ChEMBL | 594 | 10 | 1 | 5 | 7.0 | CCOc1ccc(-n2cc(-c3ccccc3)nc2[C@@H](C)N(C[C@@H]2CCCN2)C(=O)Cc2ccc(F)c(C(F)(F)F)c2)cc1 | 10.1016/j.bmcl.2007.11.072 | |||
CHEMBL401662 | 155140 | None | 0 | Human | Binding | pIC50 | = | 8.0 | 8.0 | - | 0 | ChEMBL | 594 | 10 | 1 | 5 | 7.0 | CCOc1ccc(-n2cc(-c3ccccc3)nc2[C@@H](C)N(C[C@@H]2CCCN2)C(=O)Cc2ccc(F)c(C(F)(F)F)c2)cc1 | 10.1016/j.bmcl.2007.11.072 | |||
44455774 | 155456 | None | 0 | Human | Binding | pIC50 | = | 8.0 | 8.0 | - | 0 | ChEMBL | 583 | 12 | 0 | 5 | 7.3 | CCOCCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc(-c2ccccc2)cn1-c1ccc(OCC)cc1 | 10.1016/j.bmcl.2007.11.072 | |||
CHEMBL403379 | 155456 | None | 0 | Human | Binding | pIC50 | = | 8.0 | 8.0 | - | 0 | ChEMBL | 583 | 12 | 0 | 5 | 7.3 | CCOCCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc(-c2ccccc2)cn1-c1ccc(OCC)cc1 | 10.1016/j.bmcl.2007.11.072 | |||
71678293 | 145192 | None | 0 | Human | Binding | pIC50 | = | 8.0 | 8.0 | - | 0 | ChEMBL | 474 | 4 | 1 | 7 | 2.8 | O=C(CN1C(=O)COc2ccccc21)N1CCN(c2scnc2-c2nc3ccccc3[nH]2)CC1 | nan | |||
CHEMBL3911782 | 145192 | None | 0 | Human | Binding | pIC50 | = | 8.0 | 8.0 | - | 0 | ChEMBL | 474 | 4 | 1 | 7 | 2.8 | O=C(CN1C(=O)COc2ccccc21)N1CCN(c2scnc2-c2nc3ccccc3[nH]2)CC1 | nan | |||
71679792 | 146935 | None | 0 | Human | Binding | pIC50 | = | 8.0 | 8.0 | - | 0 | ChEMBL | 444 | 4 | 1 | 8 | 2.8 | O=C(Cn1cnc2cccnc21)N1CCN(c2scnc2-c2nc3ccccc3[nH]2)CC1 | nan | |||
CHEMBL3925131 | 146935 | None | 0 | Human | Binding | pIC50 | = | 8.0 | 8.0 | - | 0 | ChEMBL | 444 | 4 | 1 | 8 | 2.8 | O=C(Cn1cnc2cccnc21)N1CCN(c2scnc2-c2nc3ccccc3[nH]2)CC1 | nan | |||
89726144 | 147732 | None | 0 | Human | Binding | pIC50 | = | 8.0 | 8.0 | - | 0 | ChEMBL | 492 | 4 | 1 | 6 | 4.4 | C[C@@H]1CN(c2scnc2-c2nc3cc(Cl)ccc3[nH]2)CCN1C(=O)CN1CCc2ccccc21 | nan | |||
CHEMBL3931545 | 147732 | None | 0 | Human | Binding | pIC50 | = | 8.0 | 8.0 | - | 0 | ChEMBL | 492 | 4 | 1 | 6 | 4.4 | C[C@@H]1CN(c2scnc2-c2nc3cc(Cl)ccc3[nH]2)CCN1C(=O)CN1CCc2ccccc21 | nan | |||
72188563 | 143059 | None | 0 | Human | Binding | pIC50 | = | 8.0 | 8.0 | - | 0 | ChEMBL | 486 | 12 | 1 | 5 | 4.6 | CCCN(Cc1ccc(OCCN2C(=O)CCC2=O)c(C)c1)[C@@H](CC(=O)O)c1ccc(Cl)cc1 | nan | |||
CHEMBL3894359 | 143059 | None | 0 | Human | Binding | pIC50 | = | 8.0 | 8.0 | - | 0 | ChEMBL | 486 | 12 | 1 | 5 | 4.6 | CCCN(Cc1ccc(OCCN2C(=O)CCC2=O)c(C)c1)[C@@H](CC(=O)O)c1ccc(Cl)cc1 | nan | |||
46883301 | 5662 | None | 0 | Human | Binding | pIC50 | = | 7.0 | 7.0 | - | 0 | ChEMBL | 605 | 9 | 0 | 7 | 6.1 | CCOc1ccc(-n2c([C@@H](C)N(Cc3cccnc3)C(=O)Cc3ccc(F)c(C(F)(F)F)c3)nc3cccnc3c2=O)cc1 | 10.1016/j.bmcl.2009.07.032 | |||
CHEMBL1077821 | 5662 | None | 0 | Human | Binding | pIC50 | = | 7.0 | 7.0 | - | 0 | ChEMBL | 605 | 9 | 0 | 7 | 6.1 | CCOc1ccc(-n2c([C@@H](C)N(Cc3cccnc3)C(=O)Cc3ccc(F)c(C(F)(F)F)c3)nc3cccnc3c2=O)cc1 | 10.1016/j.bmcl.2009.07.032 | |||
134140497 | 146314 | None | 0 | Human | Binding | pIC50 | = | 7.0 | 7.0 | - | 0 | ChEMBL | 466 | 11 | 0 | 6 | 4.1 | CCCC(c1ccc2c(c1)CCO2)N(C)Cc1ccc(OCCN2C(=O)CCC2=O)c(OC)c1 | 10.1016/j.bmcl.2016.10.035 | |||
CHEMBL3920319 | 146314 | None | 0 | Human | Binding | pIC50 | = | 7.0 | 7.0 | - | 0 | ChEMBL | 466 | 11 | 0 | 6 | 4.1 | CCCC(c1ccc2c(c1)CCO2)N(C)Cc1ccc(OCCN2C(=O)CCC2=O)c(OC)c1 | 10.1016/j.bmcl.2016.10.035 | |||
134149982 | 151940 | None | 0 | Human | Binding | pIC50 | = | 7.0 | 7.0 | - | 0 | ChEMBL | 466 | 11 | 0 | 6 | 4.1 | CCC(c1ccc2c(c1)CCO2)N(CC)Cc1ccc(OCCN2C(=O)CCC2=O)c(OC)c1 | 10.1016/j.bmcl.2016.10.035 | |||
CHEMBL3965490 | 151940 | None | 0 | Human | Binding | pIC50 | = | 7.0 | 7.0 | - | 0 | ChEMBL | 466 | 11 | 0 | 6 | 4.1 | CCC(c1ccc2c(c1)CCO2)N(CC)Cc1ccc(OCCN2C(=O)CCC2=O)c(OC)c1 | 10.1016/j.bmcl.2016.10.035 | |||
90014472 | 152966 | None | 0 | Human | Binding | pIC50 | = | 7.0 | 7.0 | - | 0 | ChEMBL | 550 | 13 | 1 | 6 | 5.2 | COc1cc(CN(CC(C)C)C(CC(=O)O)c2ccc(Cl)cc2Cl)ccc1OCCN1C(=O)CCC1=O | 10.1016/j.bmcl.2016.10.038 | |||
CHEMBL3974433 | 152966 | None | 0 | Human | Binding | pIC50 | = | 7.0 | 7.0 | - | 0 | ChEMBL | 550 | 13 | 1 | 6 | 5.2 | COc1cc(CN(CC(C)C)C(CC(=O)O)c2ccc(Cl)cc2Cl)ccc1OCCN1C(=O)CCC1=O | 10.1016/j.bmcl.2016.10.038 | |||
90014472 | 152966 | None | 0 | Human | Binding | pIC50 | = | 7.0 | 7.0 | - | 0 | ChEMBL | 550 | 13 | 1 | 6 | 5.2 | COc1cc(CN(CC(C)C)C(CC(=O)O)c2ccc(Cl)cc2Cl)ccc1OCCN1C(=O)CCC1=O | nan | |||
CHEMBL3974433 | 152966 | None | 0 | Human | Binding | pIC50 | = | 7.0 | 7.0 | - | 0 | ChEMBL | 550 | 13 | 1 | 6 | 5.2 | COc1cc(CN(CC(C)C)C(CC(=O)O)c2ccc(Cl)cc2Cl)ccc1OCCN1C(=O)CCC1=O | nan | |||
871434 | 97878 | None | 2 | Human | Binding | pIC50 | = | 6.0 | 6.0 | - | 0 | ChEMBL | 327 | 5 | 1 | 4 | 3.9 | CCCn1c(=N)n(CC(=O)c2ccc(Cl)cc2)c2ccccc21 | 10.1016/j.bmcl.2008.02.049 | |||
CHEMBL272060 | 97878 | None | 2 | Human | Binding | pIC50 | = | 6.0 | 6.0 | - | 0 | ChEMBL | 327 | 5 | 1 | 4 | 3.9 | CCCn1c(=N)n(CC(=O)c2ccc(Cl)cc2)c2ccccc21 | 10.1016/j.bmcl.2008.02.049 | |||
44453468 | 155176 | None | 0 | Mouse | Binding | pIC50 | = | 6.0 | 6.0 | - | 0 | ChEMBL | 571 | 9 | 1 | 6 | 6.4 | N=c1n(CC(=O)c2ccc(Cl)cc2)c2cccc(Cl)c2n1CCCN(C(=O)c1cccc2cccnc12)C1CC1 | 10.1016/j.bmcl.2008.02.049 | |||
CHEMBL401868 | 155176 | None | 0 | Mouse | Binding | pIC50 | = | 6.0 | 6.0 | - | 0 | ChEMBL | 571 | 9 | 1 | 6 | 6.4 | N=c1n(CC(=O)c2ccc(Cl)cc2)c2cccc(Cl)c2n1CCCN(C(=O)c1cccc2cccnc12)C1CC1 | 10.1016/j.bmcl.2008.02.049 | |||
44454591 | 95734 | None | 0 | Human | Binding | pIC50 | = | 5.0 | 5.0 | - | 0 | ChEMBL | 343 | 5 | 0 | 6 | 2.6 | C[S+]([O-])c1nc2ccccc2n1CC(=O)c1ccc([N+](=O)[O-])cc1 | 10.1016/j.bmcl.2008.01.074 | |||
CHEMBL258126 | 95734 | None | 0 | Human | Binding | pIC50 | = | 5.0 | 5.0 | - | 0 | ChEMBL | 343 | 5 | 0 | 6 | 2.6 | C[S+]([O-])c1nc2ccccc2n1CC(=O)c1ccc([N+](=O)[O-])cc1 | 10.1016/j.bmcl.2008.01.074 | |||
44454490 | 98036 | None | 0 | Human | Binding | pIC50 | = | 5.0 | 5.0 | - | 0 | ChEMBL | 329 | 3 | 1 | 3 | 3.5 | Cn1c(=N)n(CCc2ccc(Br)cc2)c2ccccc21 | 10.1016/j.bmcl.2008.01.074 | |||
CHEMBL272742 | 98036 | None | 0 | Human | Binding | pIC50 | = | 5.0 | 5.0 | - | 0 | ChEMBL | 329 | 3 | 1 | 3 | 3.5 | Cn1c(=N)n(CCc2ccc(Br)cc2)c2ccccc21 | 10.1016/j.bmcl.2008.01.074 | |||
71678806 | 142473 | None | 0 | Human | Binding | pIC50 | = | 7.0 | 7.0 | - | 0 | ChEMBL | 511 | 4 | 1 | 7 | 4.4 | O=C(Cn1c(C(F)(F)F)nc2ccccc21)N1CCN(c2scnc2-c2nc3ccccc3[nH]2)CC1 | nan | |||
CHEMBL3889614 | 142473 | None | 0 | Human | Binding | pIC50 | = | 7.0 | 7.0 | - | 0 | ChEMBL | 511 | 4 | 1 | 7 | 4.4 | O=C(Cn1c(C(F)(F)F)nc2ccccc21)N1CCN(c2scnc2-c2nc3ccccc3[nH]2)CC1 | nan | |||
71586486 | 132363 | None | 0 | Human | Binding | pIC50 | = | 7.0 | 7.0 | - | 0 | ChEMBL | 583 | 11 | 1 | 6 | 5.0 | CC(c1ccc2c(c1)CCO2)N(Cc1ccc(OCCN2C(=O)CN(C)C2=O)c(Cl)c1)C[C@H]1CC[C@H](C(=O)O)CC1 | nan | |||
CHEMBL3697059 | 132363 | None | 0 | Human | Binding | pIC50 | = | 7.0 | 7.0 | - | 0 | ChEMBL | 583 | 11 | 1 | 6 | 5.0 | CC(c1ccc2c(c1)CCO2)N(Cc1ccc(OCCN2C(=O)CN(C)C2=O)c(Cl)c1)C[C@H]1CC[C@H](C(=O)O)CC1 | nan | |||
71679143 | 148564 | None | 0 | Human | Binding | pIC50 | = | 7.0 | 7.0 | - | 0 | ChEMBL | 510 | 4 | 1 | 6 | 5.0 | O=C(Cn1ccc2ccc(C(F)(F)F)cc21)N1CCN(c2scnc2-c2nc3ccccc3[nH]2)CC1 | nan | |||
CHEMBL3938108 | 148564 | None | 0 | Human | Binding | pIC50 | = | 7.0 | 7.0 | - | 0 | ChEMBL | 510 | 4 | 1 | 6 | 5.0 | O=C(Cn1ccc2ccc(C(F)(F)F)cc21)N1CCN(c2scnc2-c2nc3ccccc3[nH]2)CC1 | nan | |||
44455603 | 155745 | None | 0 | Human | Binding | pIC50 | = | 6.0 | 6.0 | - | 0 | ChEMBL | 603 | 12 | 0 | 8 | 5.2 | CCOc1ccc(-n2cc(-c3ccccc3)nc2[C@@H](C)N(CCS(=O)(=O)CC)C(=O)Cn2ccc(C(F)(F)F)n2)cc1 | 10.1016/j.bmcl.2007.11.072 | |||
CHEMBL404841 | 155745 | None | 0 | Human | Binding | pIC50 | = | 6.0 | 6.0 | - | 0 | ChEMBL | 603 | 12 | 0 | 8 | 5.2 | CCOc1ccc(-n2cc(-c3ccccc3)nc2[C@@H](C)N(CCS(=O)(=O)CC)C(=O)Cn2ccc(C(F)(F)F)n2)cc1 | 10.1016/j.bmcl.2007.11.072 | |||
44447093 | 154617 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 597 | 9 | 0 | 5 | 6.5 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1cc2ccccc2nc1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2007.11.060 | |||
CHEMBL399084 | 154617 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 597 | 9 | 0 | 5 | 6.5 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1cc2ccccc2nc1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2007.11.060 | |||
124037270 | 150818 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 507 | 4 | 1 | 6 | 5.8 | C[C@@H]1CN(c2scnc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cc1csc2ccc(Cl)cc12 | nan | |||
CHEMBL3956258 | 150818 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 507 | 4 | 1 | 6 | 5.8 | C[C@@H]1CN(c2scnc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cc1csc2ccc(Cl)cc12 | nan | |||
89726367 | 147175 | None | 0 | Human | Binding | pIC50 | = | 5.9 | 5.9 | - | 0 | ChEMBL | 514 | 5 | 1 | 9 | 3.3 | C[C@@H]1CN(c2sc(C3COC3)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL3927250 | 147175 | None | 0 | Human | Binding | pIC50 | = | 5.9 | 5.9 | - | 0 | ChEMBL | 514 | 5 | 1 | 9 | 3.3 | C[C@@H]1CN(c2sc(C3COC3)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | 10.1021/acs.jmedchem.2c00675 | |||
89726522 | 149533 | None | 0 | Human | Binding | pIC50 | = | 5.9 | 5.9 | - | 0 | ChEMBL | 515 | 6 | 1 | 9 | 3.2 | C[C@@H]1CN(c2sc(CN(C)C)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL3945976 | 149533 | None | 0 | Human | Binding | pIC50 | = | 5.9 | 5.9 | - | 0 | ChEMBL | 515 | 6 | 1 | 9 | 3.2 | C[C@@H]1CN(c2sc(CN(C)C)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cnc2cccnc21 | 10.1021/acs.jmedchem.2c00675 | |||
168283702 | 190875 | None | 0 | Human | Binding | pIC50 | = | 5.9 | 5.9 | - | 0 | ChEMBL | 522 | 4 | 0 | 9 | 3.9 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3cnc(C(C)(C)C)nc3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL5183171 | 190875 | None | 0 | Human | Binding | pIC50 | = | 5.9 | 5.9 | - | 0 | ChEMBL | 522 | 4 | 0 | 9 | 3.9 | Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3cnc(C(C)(C)C)nc3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.2c00675 | |||
71586577 | 132365 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 575 | 11 | 1 | 5 | 5.7 | C[C@@H](c1ccc(Cl)cc1)N(Cc1ccc(OCCN2C(=O)CN(C)C2=O)c(Cl)c1)C[C@H]1CC[C@H](C(=O)O)CC1 | nan | |||
CHEMBL3697060 | 132365 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 575 | 11 | 1 | 5 | 5.7 | C[C@@H](c1ccc(Cl)cc1)N(Cc1ccc(OCCN2C(=O)CN(C)C2=O)c(Cl)c1)C[C@H]1CC[C@H](C(=O)O)CC1 | nan | |||
90066442 | 142711 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 514 | 14 | 1 | 5 | 5.2 | CCCCN(Cc1ccc(CCCN2C(=O)CCC2=O)c(OC)c1)C(CC(=O)O)c1ccc(Cl)cc1 | nan | |||
CHEMBL3891543 | 142711 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 514 | 14 | 1 | 5 | 5.2 | CCCCN(Cc1ccc(CCCN2C(=O)CCC2=O)c(OC)c1)C(CC(=O)O)c1ccc(Cl)cc1 | nan | |||
72548177 | 144298 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 520 | 12 | 1 | 5 | 5.3 | CCCN(Cc1ccc(OCCN2C(=O)CCC2=O)c(C)c1)C(CC(=O)O)c1ccc(Cl)c(Cl)c1 | nan | |||
CHEMBL3904396 | 144298 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 520 | 12 | 1 | 5 | 5.3 | CCCN(Cc1ccc(OCCN2C(=O)CCC2=O)c(C)c1)C(CC(=O)O)c1ccc(Cl)c(Cl)c1 | nan | |||
56673939 | 64258 | None | 0 | Human | Binding | pIC50 | = | 5.9 | 5.9 | - | 0 | ChEMBL | 470 | 2 | 2 | 3 | 4.3 | CC1CN(C(=O)[C@@H]2C=C3c4cccc5[nH]cc(c45)C[C@H]3N(C(=O)Nc3ccccc3)C2)CC(C)O1 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1809009 | 64258 | None | 0 | Human | Binding | pIC50 | = | 5.9 | 5.9 | - | 0 | ChEMBL | 470 | 2 | 2 | 3 | 4.3 | CC1CN(C(=O)[C@@H]2C=C3c4cccc5[nH]cc(c45)C[C@H]3N(C(=O)Nc3ccccc3)C2)CC(C)O1 | 10.1016/j.bmcl.2011.06.070 | |||
121485465 | 194004 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 534 | 5 | 0 | 9 | 3.5 | CCc1ncn(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3cnc(C(F)(F)F)nc3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.3c00074 | |||
CHEMBL5276329 | 194004 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 534 | 5 | 0 | 9 | 3.5 | CCc1ncn(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3cnc(C(F)(F)F)nc3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.3c00074 | |||
44455824 | 155757 | None | 0 | Human | Binding | pIC50 | = | 5.9 | 5.9 | - | 0 | ChEMBL | 602 | 10 | 0 | 5 | 7.8 | CCOc1ccc(-n2cc(-c3ccccc3)nc2[C@@H](C)N(Cc2ccccn2)C(=O)Cc2ccc(F)c(C(F)(F)F)c2)cc1 | 10.1016/j.bmcl.2007.11.072 | |||
CHEMBL404898 | 155757 | None | 0 | Human | Binding | pIC50 | = | 5.9 | 5.9 | - | 0 | ChEMBL | 602 | 10 | 0 | 5 | 7.8 | CCOc1ccc(-n2cc(-c3ccccc3)nc2[C@@H](C)N(Cc2ccccn2)C(=O)Cc2ccc(F)c(C(F)(F)F)c2)cc1 | 10.1016/j.bmcl.2007.11.072 | |||
90015039 | 143545 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 498 | 11 | 1 | 5 | 4.7 | Cc1cc(CN(C2CCC2)C(CC(=O)O)c2ccc(Cl)cc2)ccc1OCCN1C(=O)CCC1=O | 10.1016/j.bmcl.2016.10.038 | |||
CHEMBL3898394 | 143545 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 498 | 11 | 1 | 5 | 4.7 | Cc1cc(CN(C2CCC2)C(CC(=O)O)c2ccc(Cl)cc2)ccc1OCCN1C(=O)CCC1=O | 10.1016/j.bmcl.2016.10.038 | |||
90015039 | 143545 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 498 | 11 | 1 | 5 | 4.7 | Cc1cc(CN(C2CCC2)C(CC(=O)O)c2ccc(Cl)cc2)ccc1OCCN1C(=O)CCC1=O | nan | |||
CHEMBL3898394 | 143545 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 498 | 11 | 1 | 5 | 4.7 | Cc1cc(CN(C2CCC2)C(CC(=O)O)c2ccc(Cl)cc2)ccc1OCCN1C(=O)CCC1=O | nan | |||
72550479 | 146679 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 536 | 13 | 1 | 6 | 5.0 | CCCN(Cc1ccc(OCCN2C(=O)CCC2=O)c(OC)c1)C(CC(=O)O)c1ccc(Cl)c(Cl)c1 | nan | |||
CHEMBL3923088 | 146679 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 536 | 13 | 1 | 6 | 5.0 | CCCN(Cc1ccc(OCCN2C(=O)CCC2=O)c(OC)c1)C(CC(=O)O)c1ccc(Cl)c(Cl)c1 | nan | |||
90015284 | 159933 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 591 | 13 | 1 | 9 | 4.2 | COc1cc(CN(CC2CCCCC2)C(CC(=O)O)c2ccc3c(c2)CCO3)ccc1OCCn1c(=O)ccn(C)c1=O | nan | |||
CHEMBL4106525 | 159933 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 591 | 13 | 1 | 9 | 4.2 | COc1cc(CN(CC2CCCCC2)C(CC(=O)O)c2ccc3c(c2)CCO3)ccc1OCCn1c(=O)ccn(C)c1=O | nan | |||
72548180 | 145461 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 560 | 12 | 1 | 5 | 6.0 | Cc1cc(CN(CC2CCCC2)C(CC(=O)O)c2ccc(Cl)c(Cl)c2)ccc1OCCN1C(=O)CCC1=O | nan | |||
CHEMBL3913744 | 145461 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 560 | 12 | 1 | 5 | 6.0 | Cc1cc(CN(CC2CCCC2)C(CC(=O)O)c2ccc(Cl)c(Cl)c2)ccc1OCCN1C(=O)CCC1=O | nan | |||
171343120 | 193685 | None | 0 | Human | Binding | pIC50 | = | 5.9 | 5.9 | - | 0 | ChEMBL | 534 | 5 | 0 | 9 | 3.5 | CCc1ncnn1CC(=O)N1CCN(c2sc(C(F)(F)F)nc2-c2cnc(C(F)(F)F)nc2)C[C@H]1C | 10.1021/acs.jmedchem.3c00074 | |||
CHEMBL5268766 | 193685 | None | 0 | Human | Binding | pIC50 | = | 5.9 | 5.9 | - | 0 | ChEMBL | 534 | 5 | 0 | 9 | 3.5 | CCc1ncnn1CC(=O)N1CCN(c2sc(C(F)(F)F)nc2-c2cnc(C(F)(F)F)nc2)C[C@H]1C | 10.1021/acs.jmedchem.3c00074 | |||
171357455 | 194175 | None | 0 | Human | Binding | pIC50 | = | 5.9 | 5.9 | - | 0 | ChEMBL | 534 | 5 | 0 | 9 | 3.5 | CCc1nncn1CC(=O)N1CCN(c2sc(C(F)(F)F)nc2-c2cnc(C(F)(F)F)nc2)C[C@H]1C | 10.1021/acs.jmedchem.3c00074 | |||
CHEMBL5280406 | 194175 | None | 0 | Human | Binding | pIC50 | = | 5.9 | 5.9 | - | 0 | ChEMBL | 534 | 5 | 0 | 9 | 3.5 | CCc1nncn1CC(=O)N1CCN(c2sc(C(F)(F)F)nc2-c2cnc(C(F)(F)F)nc2)C[C@H]1C | 10.1021/acs.jmedchem.3c00074 | |||
168284279 | 191651 | None | 0 | Human | Binding | pIC50 | = | 5.9 | 5.9 | - | 0 | ChEMBL | 516 | 5 | 0 | 8 | 4.3 | COc1ccc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3cnc4cccnc43)[C@H](C)C2)cc1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL5194504 | 191651 | None | 0 | Human | Binding | pIC50 | = | 5.9 | 5.9 | - | 0 | ChEMBL | 516 | 5 | 0 | 8 | 4.3 | COc1ccc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3cnc4cccnc43)[C@H](C)C2)cc1 | 10.1021/acs.jmedchem.2c00675 | |||
44426705 | 86052 | None | 0 | Human | Binding | pIC50 | = | 7.9 | 7.9 | - | 0 | ChEMBL | 560 | 7 | 0 | 5 | 6.3 | C[C@H](c1nc2ccccc2c(=O)n1-c1ccc(F)cc1)N(Cc1cccnc1)C(=O)Cc1ccc(C(F)(F)F)cc1 | 10.1016/j.bmcl.2007.03.106 | |||
CHEMBL230560 | 86052 | None | 0 | Human | Binding | pIC50 | = | 7.9 | 7.9 | - | 0 | ChEMBL | 560 | 7 | 0 | 5 | 6.3 | C[C@H](c1nc2ccccc2c(=O)n1-c1ccc(F)cc1)N(Cc1cccnc1)C(=O)Cc1ccc(C(F)(F)F)cc1 | 10.1016/j.bmcl.2007.03.106 | |||
CHEMBL553862 | 86052 | None | 0 | Human | Binding | pIC50 | = | 7.9 | 7.9 | - | 0 | ChEMBL | 560 | 7 | 0 | 5 | 6.3 | C[C@H](c1nc2ccccc2c(=O)n1-c1ccc(F)cc1)N(Cc1cccnc1)C(=O)Cc1ccc(C(F)(F)F)cc1 | 10.1016/j.bmcl.2007.03.106 | |||
57394143 | 69872 | None | 0 | Human | Binding | pIC50 | = | 7.9 | 7.9 | - | 0 | ChEMBL | 641 | 7 | 0 | 8 | 4.8 | C[C@H](c1nc2ncccc2c(=O)n1-c1ccc(C#N)cc1)N(CC1CCS(=O)(=O)CC1)C(=O)Cc1ccc(F)c(C(F)(F)F)c1 | 10.1016/j.bmcl.2011.10.120 | |||
CHEMBL1938408 | 69872 | None | 0 | Human | Binding | pIC50 | = | 7.9 | 7.9 | - | 0 | ChEMBL | 641 | 7 | 0 | 8 | 4.8 | C[C@H](c1nc2ncccc2c(=O)n1-c1ccc(C#N)cc1)N(CC1CCS(=O)(=O)CC1)C(=O)Cc1ccc(F)c(C(F)(F)F)c1 | 10.1016/j.bmcl.2011.10.120 | |||
56834986 | 69992 | None | 0 | Human | Binding | pIC50 | = | 7.9 | 7.9 | - | 0 | ChEMBL | 650 | 7 | 0 | 7 | 5.5 | C[C@H](c1nc2ncccc2c(=O)n1-c1ccc(Cl)cc1)N(CC1CCS(=O)(=O)CC1)C(=O)Cc1ccc(F)c(C(F)(F)F)c1 | 10.1016/j.bmcl.2011.10.120 | |||
CHEMBL1939559 | 69992 | None | 0 | Human | Binding | pIC50 | = | 7.9 | 7.9 | - | 0 | ChEMBL | 650 | 7 | 0 | 7 | 5.5 | C[C@H](c1nc2ncccc2c(=O)n1-c1ccc(Cl)cc1)N(CC1CCS(=O)(=O)CC1)C(=O)Cc1ccc(F)c(C(F)(F)F)c1 | 10.1016/j.bmcl.2011.10.120 | |||
45486555 | 200129 | None | 0 | Human | Binding | pIC50 | = | 7.9 | 7.9 | - | 0 | ChEMBL | 629 | 9 | 0 | 8 | 4.7 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc2nc(C)ccc2c(=O)n1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2009.07.021 | |||
CHEMBL571080 | 200129 | None | 0 | Human | Binding | pIC50 | = | 7.9 | 7.9 | - | 0 | ChEMBL | 629 | 9 | 0 | 8 | 4.7 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc2nc(C)ccc2c(=O)n1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2009.07.021 | |||
25032696 | 155394 | None | 0 | Human | Binding | pIC50 | = | 7.9 | 7.9 | - | 0 | ChEMBL | 626 | 11 | 0 | 6 | 6.3 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc(C2CC2)c(C(F)F)n1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2007.11.072 | |||
CHEMBL402989 | 155394 | None | 0 | Human | Binding | pIC50 | = | 7.9 | 7.9 | - | 0 | ChEMBL | 626 | 11 | 0 | 6 | 6.3 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc(C2CC2)c(C(F)F)n1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2007.11.072 | |||
56680570 | 64252 | None | 0 | Human | Binding | pIC50 | = | 7.9 | 7.9 | - | 0 | ChEMBL | 438 | 2 | 2 | 2 | 4.8 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1C=CCCC1 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1809003 | 64252 | None | 0 | Human | Binding | pIC50 | = | 7.9 | 7.9 | - | 0 | ChEMBL | 438 | 2 | 2 | 2 | 4.8 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1C=CCCC1 | 10.1016/j.bmcl.2011.06.070 | |||
72548414 | 148338 | None | 0 | Human | Binding | pIC50 | = | 7.9 | 7.9 | - | 0 | ChEMBL | 514 | 13 | 1 | 5 | 5.1 | CCc1cc(CN(CC(C)C)C(CC(=O)O)c2ccc(Cl)cc2)ccc1OCCN1C(=O)CCC1=O | nan | |||
CHEMBL3936341 | 148338 | None | 0 | Human | Binding | pIC50 | = | 7.9 | 7.9 | - | 0 | ChEMBL | 514 | 13 | 1 | 5 | 5.1 | CCc1cc(CN(CC(C)C)C(CC(=O)O)c2ccc(Cl)cc2)ccc1OCCN1C(=O)CCC1=O | nan | |||
71572192 | 132352 | None | 0 | Human | Binding | pIC50 | = | 7.9 | 7.9 | - | 0 | ChEMBL | 568 | 11 | 1 | 6 | 5.3 | COc1cc(CN(C[C@H]2CC[C@H](C(=O)O)CC2)[C@H]2CCc3cc(Cl)ccc32)ccc1OCCN1C(=O)CCC1=O | 10.1021/acs.jmedchem.5b01337 | |||
CHEMBL3697049 | 132352 | None | 0 | Human | Binding | pIC50 | = | 7.9 | 7.9 | - | 0 | ChEMBL | 568 | 11 | 1 | 6 | 5.3 | COc1cc(CN(C[C@H]2CC[C@H](C(=O)O)CC2)[C@H]2CCc3cc(Cl)ccc32)ccc1OCCN1C(=O)CCC1=O | 10.1021/acs.jmedchem.5b01337 | |||
89610575 | 132845 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 532 | 11 | 1 | 6 | 4.4 | COc1cc(CN(C(C)c2ccc(Cl)c(F)c2)[C@H]2C[C@@H](C(=O)O)C2)ccc1OCCN1C(=O)CCC1=O | nan | |||
CHEMBL3700576 | 132845 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 532 | 11 | 1 | 6 | 4.4 | COc1cc(CN(C(C)c2ccc(Cl)c(F)c2)[C@H]2C[C@@H](C(=O)O)C2)ccc1OCCN1C(=O)CCC1=O | nan | |||
134146842 | 150133 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 456 | 9 | 0 | 7 | 3.9 | COc1cc(CN(C)C(C)c2ccc3c(c2)CCO3)ccc1OCCN1C(=O)CSC1=O | 10.1016/j.bmcl.2016.10.035 | |||
CHEMBL3950573 | 150133 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 456 | 9 | 0 | 7 | 3.9 | COc1cc(CN(C)C(C)c2ccc3c(c2)CCO3)ccc1OCCN1C(=O)CSC1=O | 10.1016/j.bmcl.2016.10.035 | |||
134153150 | 152835 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 558 | 12 | 1 | 7 | 4.6 | COc1cc(CN(Cc2ccc(C(=O)O)cc2)C(C)c2ccc3c(c2)CCO3)ccc1OCCN1C(=O)CCC1=O | 10.1016/j.bmcl.2016.10.035 | |||
CHEMBL3973261 | 152835 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 558 | 12 | 1 | 7 | 4.6 | COc1cc(CN(Cc2ccc(C(=O)O)cc2)C(C)c2ccc3c(c2)CCO3)ccc1OCCN1C(=O)CCC1=O | 10.1016/j.bmcl.2016.10.035 | |||
90014835 | 142849 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 575 | 13 | 1 | 8 | 4.4 | COc1cc(CN(CC2CC2)C(CC(=O)O)c2ccc(Cl)cc2Cl)ccc1OCCn1c(=O)ccn(C)c1=O | nan | |||
CHEMBL3892586 | 142849 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 575 | 13 | 1 | 8 | 4.4 | COc1cc(CN(CC2CC2)C(CC(=O)O)c2ccc(Cl)cc2Cl)ccc1OCCn1c(=O)ccn(C)c1=O | nan | |||
72549348 | 147789 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 576 | 13 | 1 | 6 | 5.7 | COc1cc(CN(CC2CCCC2)C(CC(=O)O)c2ccc(Cl)cc2Cl)ccc1OCCN1C(=O)CCC1=O | nan | |||
CHEMBL3931958 | 147789 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 576 | 13 | 1 | 6 | 5.7 | COc1cc(CN(CC2CCCC2)C(CC(=O)O)c2ccc(Cl)cc2Cl)ccc1OCCN1C(=O)CCC1=O | nan | |||
72549127 | 153709 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 548 | 14 | 1 | 5 | 5.9 | CCCCN(Cc1ccc(OCCN2C(=O)CCC2=O)c(CC)c1)C(CC(=O)O)c1ccc(Cl)c(Cl)c1 | nan | |||
CHEMBL3980801 | 153709 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 548 | 14 | 1 | 5 | 5.9 | CCCCN(Cc1ccc(OCCN2C(=O)CCC2=O)c(CC)c1)C(CC(=O)O)c1ccc(Cl)c(Cl)c1 | nan | |||
71586488 | 132361 | None | 0 | Human | Binding | pIC50 | = | 5.9 | 5.9 | - | 0 | ChEMBL | 587 | 10 | 1 | 5 | 5.6 | CN1CC(=O)N(CCOc2ccc(CN(C[C@H]3CC[C@H](C(=O)O)CC3)C3CCc4cc(Cl)ccc43)cc2Cl)C1=O | nan | |||
CHEMBL3697057 | 132361 | None | 0 | Human | Binding | pIC50 | = | 5.9 | 5.9 | - | 0 | ChEMBL | 587 | 10 | 1 | 5 | 5.6 | CN1CC(=O)N(CCOc2ccc(CN(C[C@H]3CC[C@H](C(=O)O)CC3)C3CCc4cc(Cl)ccc43)cc2Cl)C1=O | nan | |||
89610627 | 132842 | None | 0 | Human | Binding | pIC50 | = | 5.9 | 5.9 | - | 0 | ChEMBL | 546 | 11 | 1 | 5 | 5.5 | CCc1cc(CN(C(C)c2ccc(Cl)c(Cl)c2)[C@H]2C[C@@H](C(=O)O)C2)ccc1OCCN1C(=O)CCC1=O | nan | |||
CHEMBL3700573 | 132842 | None | 0 | Human | Binding | pIC50 | = | 5.9 | 5.9 | - | 0 | ChEMBL | 546 | 11 | 1 | 5 | 5.5 | CCc1cc(CN(C(C)c2ccc(Cl)c(Cl)c2)[C@H]2C[C@@H](C(=O)O)C2)ccc1OCCN1C(=O)CCC1=O | nan | |||
44453439 | 97701 | None | 1 | Human | Binding | pIC50 | = | 5.9 | 5.9 | - | 0 | ChEMBL | 385 | 7 | 1 | 6 | 3.4 | CCOC(=O)CCn1c(=N)n(CC(=O)c2ccc(Cl)cc2)c2ccccc21 | 10.1016/j.bmcl.2008.02.049 | |||
CHEMBL271081 | 97701 | None | 1 | Human | Binding | pIC50 | = | 5.9 | 5.9 | - | 0 | ChEMBL | 385 | 7 | 1 | 6 | 3.4 | CCOC(=O)CCn1c(=N)n(CC(=O)c2ccc(Cl)cc2)c2ccccc21 | 10.1016/j.bmcl.2008.02.049 | |||
134148525 | 148620 | None | 0 | Human | Binding | pIC50 | = | 5.9 | 5.9 | - | 0 | ChEMBL | 452 | 11 | 1 | 6 | 3.8 | CCCC(NCc1ccc(OCCN2C(=O)CCC2=O)c(OC)c1)c1ccc2c(c1)CCO2 | 10.1016/j.bmcl.2016.10.035 | |||
CHEMBL3938584 | 148620 | None | 0 | Human | Binding | pIC50 | = | 5.9 | 5.9 | - | 0 | ChEMBL | 452 | 11 | 1 | 6 | 3.8 | CCCC(NCc1ccc(OCCN2C(=O)CCC2=O)c(OC)c1)c1ccc2c(c1)CCO2 | 10.1016/j.bmcl.2016.10.035 | |||
71585713 | 132407 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 554 | 12 | 1 | 5 | 6.0 | CCC(c1ccc(Cl)cc1)N(Cc1ccc(OCCN2C(=O)CCC2=O)c(C)c1)C[C@H]1CC[C@H](C(=O)O)CC1 | nan | |||
CHEMBL3697102 | 132407 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 554 | 12 | 1 | 5 | 6.0 | CCC(c1ccc(Cl)cc1)N(Cc1ccc(OCCN2C(=O)CCC2=O)c(C)c1)C[C@H]1CC[C@H](C(=O)O)CC1 | nan | |||
89610672 | 132432 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 572 | 12 | 1 | 5 | 6.0 | CCc1cc(CN(C[C@H]2CC[C@H](C(=O)O)CC2)[C@@H](C)c2ccc(Cl)c(F)c2)ccc1OCCN1C(=O)CCC1=O | nan | |||
CHEMBL3697128 | 132432 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 572 | 12 | 1 | 5 | 6.0 | CCc1cc(CN(C[C@H]2CC[C@H](C(=O)O)CC2)[C@@H](C)c2ccc(Cl)c(F)c2)ccc1OCCN1C(=O)CCC1=O | nan | |||
134146441 | 149392 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 605 | 10 | 1 | 7 | 5.8 | CCOc1ccc(N2C(=O)c3cccnc3NC2[C@@H](C)N(Cc2cccnc2)C(=O)Cc2ccc(OC(F)(F)F)cc2)cc1 | 10.1016/j.bmcl.2016.10.035 | |||
CHEMBL3944817 | 149392 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 605 | 10 | 1 | 7 | 5.8 | CCOc1ccc(N2C(=O)c3cccnc3NC2[C@@H](C)N(Cc2cccnc2)C(=O)Cc2ccc(OC(F)(F)F)cc2)cc1 | 10.1016/j.bmcl.2016.10.035 | |||
44447092 | 94941 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 598 | 9 | 0 | 6 | 5.9 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc2ccccc2nc1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2007.11.060 | |||
CHEMBL254082 | 94941 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 598 | 9 | 0 | 6 | 5.9 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc2ccccc2nc1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2007.11.060 | |||
90014694 | 149867 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 551 | 14 | 1 | 9 | 3.4 | CCCCN(Cc1ccc(OCCn2c(=O)ccn(C)c2=O)c(OC)c1)C(CC(=O)O)c1ccc2c(c1)CCO2 | 10.1016/j.bmcl.2016.10.038 | |||
CHEMBL3948432 | 149867 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 551 | 14 | 1 | 9 | 3.4 | CCCCN(Cc1ccc(OCCn2c(=O)ccn(C)c2=O)c(OC)c1)C(CC(=O)O)c1ccc2c(c1)CCO2 | 10.1016/j.bmcl.2016.10.038 | |||
90014694 | 149867 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 551 | 14 | 1 | 9 | 3.4 | CCCCN(Cc1ccc(OCCn2c(=O)ccn(C)c2=O)c(OC)c1)C(CC(=O)O)c1ccc2c(c1)CCO2 | nan | |||
CHEMBL3948432 | 149867 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 551 | 14 | 1 | 9 | 3.4 | CCCCN(Cc1ccc(OCCn2c(=O)ccn(C)c2=O)c(OC)c1)C(CC(=O)O)c1ccc2c(c1)CCO2 | nan | |||
71586681 | 132374 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 560 | 11 | 1 | 5 | 6.0 | C[C@@H](c1ccc(Cl)cc1)N(Cc1ccc(OCCN2C(=O)CCC2=O)c(Cl)c1)C[C@H]1CC[C@H](C(=O)O)CC1 | nan | |||
CHEMBL3697069 | 132374 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 560 | 11 | 1 | 5 | 6.0 | C[C@@H](c1ccc(Cl)cc1)N(Cc1ccc(OCCN2C(=O)CCC2=O)c(Cl)c1)C[C@H]1CC[C@H](C(=O)O)CC1 | nan | |||
72549595 | 145596 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 513 | 12 | 1 | 7 | 4.0 | CCCN(Cc1ccc(OCCn2c(=O)ccn(C)c2=O)c(C)c1)C(CC(=O)O)c1ccc(Cl)cc1 | 10.1016/j.bmcl.2016.10.038 | |||
CHEMBL3914758 | 145596 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 513 | 12 | 1 | 7 | 4.0 | CCCN(Cc1ccc(OCCn2c(=O)ccn(C)c2=O)c(C)c1)C(CC(=O)O)c1ccc(Cl)cc1 | 10.1016/j.bmcl.2016.10.038 | |||
72549595 | 145596 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 513 | 12 | 1 | 7 | 4.0 | CCCN(Cc1ccc(OCCn2c(=O)ccn(C)c2=O)c(C)c1)C(CC(=O)O)c1ccc(Cl)cc1 | nan | |||
CHEMBL3914758 | 145596 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 513 | 12 | 1 | 7 | 4.0 | CCCN(Cc1ccc(OCCn2c(=O)ccn(C)c2=O)c(C)c1)C(CC(=O)O)c1ccc(Cl)cc1 | nan | |||
71585500 | 132392 | None | 0 | Human | Binding | pIC50 | = | 5.9 | 5.9 | - | 0 | ChEMBL | 581 | 11 | 1 | 5 | 5.6 | COc1cc(CN(C[C@H]2CC[C@H](C(=O)O)CC2)C2CCc3cc(Cl)ccc32)ccc1CCCN1C(=O)CN(C)C1=O | nan | |||
CHEMBL3697087 | 132392 | None | 0 | Human | Binding | pIC50 | = | 5.9 | 5.9 | - | 0 | ChEMBL | 581 | 11 | 1 | 5 | 5.6 | COc1cc(CN(C[C@H]2CC[C@H](C(=O)O)CC2)C2CCc3cc(Cl)ccc32)ccc1CCCN1C(=O)CN(C)C1=O | nan | |||
72550919 | 150674 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 504 | 12 | 1 | 5 | 4.7 | CC(C)CN(Cc1ccc(OCCN2C(=O)CCC2=O)c(F)c1)C(CC(=O)O)c1ccc(Cl)cc1 | nan | |||
CHEMBL3955101 | 150674 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 504 | 12 | 1 | 5 | 4.7 | CC(C)CN(Cc1ccc(OCCN2C(=O)CCC2=O)c(F)c1)C(CC(=O)O)c1ccc(Cl)cc1 | nan | |||
11963990 | 193991 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 439 | 6 | 1 | 3 | 3.7 | CCCN1C(=O)[C@@H](Cc2ccccc2)NC(=O)C12CCN(Cc1ccc(Cl)cc1)CC2 | 10.1021/acs.jmedchem.5b01337 | |||
CHEMBL5276105 | 193991 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 439 | 6 | 1 | 3 | 3.7 | CCCN1C(=O)[C@@H](Cc2ccccc2)NC(=O)C12CCN(Cc1ccc(Cl)cc1)CC2 | 10.1021/acs.jmedchem.5b01337 | |||
90014753 | 143938 | None | 0 | Human | Binding | pIC50 | = | 5.9 | 5.9 | - | 0 | ChEMBL | 583 | 13 | 1 | 8 | 4.3 | COc1cc(CN(CCC(F)(F)F)C(CC(=O)O)c2ccc(Cl)cc2)ccc1OCCn1c(=O)ccn(C)c1=O | nan | |||
CHEMBL3901619 | 143938 | None | 0 | Human | Binding | pIC50 | = | 5.9 | 5.9 | - | 0 | ChEMBL | 583 | 13 | 1 | 8 | 4.3 | COc1cc(CN(CCC(F)(F)F)C(CC(=O)O)c2ccc(Cl)cc2)ccc1OCCn1c(=O)ccn(C)c1=O | nan | |||
134156632 | 153766 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 582 | 12 | 1 | 9 | 4.1 | COc1cc(CN(Cc2ccc(-c3nnn[nH]3)cc2)C(C)c2ccc3c(c2)CCO3)ccc1OCCN1C(=O)CCC1=O | 10.1016/j.bmcl.2016.10.035 | |||
CHEMBL3981260 | 153766 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 582 | 12 | 1 | 9 | 4.1 | COc1cc(CN(Cc2ccc(-c3nnn[nH]3)cc2)C(C)c2ccc3c(c2)CCO3)ccc1OCCN1C(=O)CCC1=O | 10.1016/j.bmcl.2016.10.035 | |||
121485362 | 193924 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 548 | 5 | 0 | 9 | 4.1 | CC(C)c1ncn(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3cnc(C(F)(F)F)nc3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.3c00074 | |||
CHEMBL5274429 | 193924 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 548 | 5 | 0 | 9 | 4.1 | CC(C)c1ncn(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3cnc(C(F)(F)F)nc3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.3c00074 | |||
44455823 | 98069 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 602 | 10 | 0 | 5 | 7.8 | CCOc1ccc(-n2cc(-c3ccccc3)nc2[C@@H](C)N(Cc2ccncc2)C(=O)Cc2ccc(F)c(C(F)(F)F)c2)cc1 | 10.1016/j.bmcl.2007.11.072 | |||
CHEMBL272919 | 98069 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 602 | 10 | 0 | 5 | 7.8 | CCOc1ccc(-n2cc(-c3ccccc3)nc2[C@@H](C)N(Cc2ccncc2)C(=O)Cc2ccc(F)c(C(F)(F)F)c2)cc1 | 10.1016/j.bmcl.2007.11.072 | |||
71572192 | 132352 | None | 0 | Human | Binding | pIC50 | = | 7.9 | 7.9 | - | 0 | ChEMBL | 568 | 11 | 1 | 6 | 5.3 | COc1cc(CN(C[C@H]2CC[C@H](C(=O)O)CC2)[C@H]2CCc3cc(Cl)ccc32)ccc1OCCN1C(=O)CCC1=O | nan | |||
CHEMBL3697049 | 132352 | None | 0 | Human | Binding | pIC50 | = | 7.9 | 7.9 | - | 0 | ChEMBL | 568 | 11 | 1 | 6 | 5.3 | COc1cc(CN(C[C@H]2CC[C@H](C(=O)O)CC2)[C@H]2CCc3cc(Cl)ccc32)ccc1OCCN1C(=O)CCC1=O | nan | |||
45379650 | 201011 | None | 0 | Mouse | Binding | pIC50 | = | 7.9 | 7.9 | - | 0 | ChEMBL | 653 | 8 | 0 | 7 | 6.3 | C[C@H](c1nc2c(C3CC3)nccn2c1-c1ccc(C#N)cc1)N(CC1CCS(=O)(=O)CC1)C(=O)Cc1ccc(C(F)(F)F)c(F)c1 | 10.1016/j.bmcl.2009.07.021 | |||
CHEMBL578192 | 201011 | None | 0 | Mouse | Binding | pIC50 | = | 7.9 | 7.9 | - | 0 | ChEMBL | 653 | 8 | 0 | 7 | 6.3 | C[C@H](c1nc2c(C3CC3)nccn2c1-c1ccc(C#N)cc1)N(CC1CCS(=O)(=O)CC1)C(=O)Cc1ccc(C(F)(F)F)c(F)c1 | 10.1016/j.bmcl.2009.07.021 | |||
44426705 | 86052 | None | 0 | Human | Binding | pIC50 | = | 7.9 | 7.9 | - | 0 | ChEMBL | 560 | 7 | 0 | 5 | 6.3 | C[C@H](c1nc2ccccc2c(=O)n1-c1ccc(F)cc1)N(Cc1cccnc1)C(=O)Cc1ccc(C(F)(F)F)cc1 | 10.1016/j.bmcl.2007.03.106 | |||
CHEMBL230560 | 86052 | None | 0 | Human | Binding | pIC50 | = | 7.9 | 7.9 | - | 0 | ChEMBL | 560 | 7 | 0 | 5 | 6.3 | C[C@H](c1nc2ccccc2c(=O)n1-c1ccc(F)cc1)N(Cc1cccnc1)C(=O)Cc1ccc(C(F)(F)F)cc1 | 10.1016/j.bmcl.2007.03.106 | |||
CHEMBL553862 | 86052 | None | 0 | Human | Binding | pIC50 | = | 7.9 | 7.9 | - | 0 | ChEMBL | 560 | 7 | 0 | 5 | 6.3 | C[C@H](c1nc2ccccc2c(=O)n1-c1ccc(F)cc1)N(Cc1cccnc1)C(=O)Cc1ccc(C(F)(F)F)cc1 | 10.1016/j.bmcl.2007.03.106 | |||
46883290 | 5651 | None | 0 | Human | Binding | pIC50 | = | 7.9 | 7.9 | - | 0 | ChEMBL | 587 | 9 | 0 | 7 | 5.9 | CCOc1ccc(-n2c([C@@H](C)N(Cc3cccnc3)C(=O)Cc3ccc(C(F)(F)F)cn3)nc3ccccc3c2=O)cc1 | 10.1016/j.bmcl.2009.07.032 | |||
CHEMBL1077810 | 5651 | None | 0 | Human | Binding | pIC50 | = | 7.9 | 7.9 | - | 0 | ChEMBL | 587 | 9 | 0 | 7 | 5.9 | CCOc1ccc(-n2c([C@@H](C)N(Cc3cccnc3)C(=O)Cc3ccc(C(F)(F)F)cn3)nc3ccccc3c2=O)cc1 | 10.1016/j.bmcl.2009.07.032 | |||
71572192 | 132352 | None | 0 | Human | Binding | pIC50 | = | 7.9 | 7.9 | - | 0 | ChEMBL | 568 | 11 | 1 | 6 | 5.3 | COc1cc(CN(C[C@H]2CC[C@H](C(=O)O)CC2)[C@H]2CCc3cc(Cl)ccc32)ccc1OCCN1C(=O)CCC1=O | 10.1016/j.bmcl.2016.10.035 | |||
CHEMBL3697049 | 132352 | None | 0 | Human | Binding | pIC50 | = | 7.9 | 7.9 | - | 0 | ChEMBL | 568 | 11 | 1 | 6 | 5.3 | COc1cc(CN(C[C@H]2CC[C@H](C(=O)O)CC2)[C@H]2CCc3cc(Cl)ccc32)ccc1OCCN1C(=O)CCC1=O | 10.1016/j.bmcl.2016.10.035 | |||
57390182 | 69986 | None | 0 | Human | Binding | pIC50 | = | 7.9 | 7.9 | - | 0 | ChEMBL | 601 | 8 | 0 | 8 | 4.0 | C[C@H](c1nc2ncccc2c(=O)n1-c1ccc(C#N)cc1)N(CCS(C)(=O)=O)C(=O)Cc1ccc(F)c(C(F)(F)F)c1 | 10.1016/j.bmcl.2011.10.120 | |||
CHEMBL1939553 | 69986 | None | 0 | Human | Binding | pIC50 | = | 7.9 | 7.9 | - | 0 | ChEMBL | 601 | 8 | 0 | 8 | 4.0 | C[C@H](c1nc2ncccc2c(=O)n1-c1ccc(C#N)cc1)N(CCS(C)(=O)=O)C(=O)Cc1ccc(F)c(C(F)(F)F)c1 | 10.1016/j.bmcl.2011.10.120 | |||
44137674 | 69993 | None | 0 | Human | Binding | pIC50 | = | 7.9 | 7.9 | - | 0 | ChEMBL | 650 | 7 | 0 | 7 | 5.5 | C[C@H](c1nc2ncccc2c(=O)n1-c1ccc(Cl)cc1)N(CC1CCS(=O)(=O)CC1)C(=O)Cc1ccc(C(F)(F)F)c(F)c1 | 10.1016/j.bmcl.2011.10.120 | |||
CHEMBL1939560 | 69993 | None | 0 | Human | Binding | pIC50 | = | 7.9 | 7.9 | - | 0 | ChEMBL | 650 | 7 | 0 | 7 | 5.5 | C[C@H](c1nc2ncccc2c(=O)n1-c1ccc(Cl)cc1)N(CC1CCS(=O)(=O)CC1)C(=O)Cc1ccc(C(F)(F)F)c(F)c1 | 10.1016/j.bmcl.2011.10.120 | |||
45486530 | 200769 | None | 0 | Human | Binding | pIC50 | = | 7.9 | 7.9 | - | 0 | ChEMBL | 651 | 9 | 0 | 8 | 6.0 | C[C@H](c1nc2c(C3CC3)nccn2c1-c1ccc(C#N)cc1)N(CC1CCS(=O)(=O)CC1)C(=O)Cc1ccc(OC(F)(F)F)cc1 | 10.1016/j.bmcl.2009.07.021 | |||
CHEMBL576096 | 200769 | None | 0 | Human | Binding | pIC50 | = | 7.9 | 7.9 | - | 0 | ChEMBL | 651 | 9 | 0 | 8 | 6.0 | C[C@H](c1nc2c(C3CC3)nccn2c1-c1ccc(C#N)cc1)N(CC1CCS(=O)(=O)CC1)C(=O)Cc1ccc(OC(F)(F)F)cc1 | 10.1016/j.bmcl.2009.07.021 | |||
71678464 | 144403 | None | 0 | Human | Binding | pIC50 | = | 7.9 | 7.9 | - | 0 | ChEMBL | 457 | 4 | 1 | 7 | 3.7 | Cc1ccc2ccn(CC(=O)N3CCN(c4scnc4-c4nc5ccccc5[nH]4)CC3)c2n1 | nan | |||
CHEMBL3905362 | 144403 | None | 0 | Human | Binding | pIC50 | = | 7.9 | 7.9 | - | 0 | ChEMBL | 457 | 4 | 1 | 7 | 3.7 | Cc1ccc2ccn(CC(=O)N3CCN(c4scnc4-c4nc5ccccc5[nH]4)CC3)c2n1 | nan | |||
71678807 | 145971 | None | 0 | Human | Binding | pIC50 | = | 7.9 | 7.9 | - | 0 | ChEMBL | 474 | 4 | 1 | 6 | 4.4 | Cc1cn(CC(=O)N2CCN(c3scnc3-c3nc4ccccc4[nH]3)CC2)c2ccc(F)cc12 | nan | |||
CHEMBL3917619 | 145971 | None | 0 | Human | Binding | pIC50 | = | 7.9 | 7.9 | - | 0 | ChEMBL | 474 | 4 | 1 | 6 | 4.4 | Cc1cn(CC(=O)N2CCN(c3scnc3-c3nc4ccccc4[nH]3)CC2)c2ccc(F)cc12 | nan | |||
134136033 | 144434 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 515 | 11 | 0 | 7 | 4.3 | COc1cc(CN(Cc2ccncc2)C(C)c2ccc3c(c2)CCO3)ccc1OCCN1C(=O)CCC1=O | 10.1016/j.bmcl.2016.10.035 | |||
CHEMBL3905602 | 144434 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 515 | 11 | 0 | 7 | 4.3 | COc1cc(CN(Cc2ccncc2)C(C)c2ccc3c(c2)CCO3)ccc1OCCN1C(=O)CCC1=O | 10.1016/j.bmcl.2016.10.035 | |||
72549591 | 152360 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 486 | 12 | 1 | 5 | 4.6 | CCCN(Cc1ccc(OCCN2C(=O)CCC2=O)c(C)c1)[C@H](CC(=O)O)c1ccc(Cl)cc1 | 10.1016/j.bmcl.2016.10.038 | |||
CHEMBL3969199 | 152360 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 486 | 12 | 1 | 5 | 4.6 | CCCN(Cc1ccc(OCCN2C(=O)CCC2=O)c(C)c1)[C@H](CC(=O)O)c1ccc(Cl)cc1 | 10.1016/j.bmcl.2016.10.038 | |||
71679963 | 151333 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 407 | 4 | 1 | 7 | 2.5 | Cc1ccn(CC(=O)N2CCN(c3scnc3-c3nc4ccccc4[nH]3)CC2)n1 | nan | |||
CHEMBL3960168 | 151333 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 407 | 4 | 1 | 7 | 2.5 | Cc1ccn(CC(=O)N2CCN(c3scnc3-c3nc4ccccc4[nH]3)CC2)n1 | nan | |||
72548897 | 147746 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 548 | 13 | 1 | 5 | 5.8 | CCc1cc(CN(CC(C)C)C(CC(=O)O)c2ccc(Cl)c(Cl)c2)ccc1OCCN1C(=O)CCC1=O | nan | |||
CHEMBL3931658 | 147746 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 548 | 13 | 1 | 5 | 5.8 | CCc1cc(CN(CC(C)C)C(CC(=O)O)c2ccc(Cl)c(Cl)c2)ccc1OCCN1C(=O)CCC1=O | nan | |||
72549591 | 152360 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 486 | 12 | 1 | 5 | 4.6 | CCCN(Cc1ccc(OCCN2C(=O)CCC2=O)c(C)c1)[C@H](CC(=O)O)c1ccc(Cl)cc1 | nan | |||
CHEMBL3969199 | 152360 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 486 | 12 | 1 | 5 | 4.6 | CCCN(Cc1ccc(OCCN2C(=O)CCC2=O)c(C)c1)[C@H](CC(=O)O)c1ccc(Cl)cc1 | nan | |||
117945202 | 160865 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 535 | 12 | 2 | 5 | 5.5 | N=C1CCC(=O)N1CCOc1ccc(CN(CC2CC2)[C@H](CC(=O)O)c2ccc(Cl)c(F)c2)cc1Cl | nan | |||
CHEMBL4114158 | 160865 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 535 | 12 | 2 | 5 | 5.5 | N=C1CCC(=O)N1CCOc1ccc(CN(CC2CC2)[C@H](CC(=O)O)c2ccc(Cl)c(F)c2)cc1Cl | nan | |||
44453362 | 97533 | None | 0 | Human | Binding | pIC50 | = | 5.9 | 5.9 | - | 0 | ChEMBL | 384 | 6 | 1 | 5 | 2.9 | CC(=O)N(C)CCn1c(=N)n(CC(=O)c2ccc(Cl)cc2)c2ccccc21 | 10.1016/j.bmcl.2008.02.049 | |||
CHEMBL270222 | 97533 | None | 0 | Human | Binding | pIC50 | = | 5.9 | 5.9 | - | 0 | ChEMBL | 384 | 6 | 1 | 5 | 2.9 | CC(=O)N(C)CCn1c(=N)n(CC(=O)c2ccc(Cl)cc2)c2ccccc21 | 10.1016/j.bmcl.2008.02.049 | |||
134132003 | 145254 | None | 0 | Human | Binding | pIC50 | = | 5.9 | 5.9 | - | 0 | ChEMBL | 485 | 10 | 1 | 7 | 3.2 | Cc1cc(CN(C)C(CC(=O)O)c2ccc(Cl)cc2)ccc1OCCn1c(=O)ccn(C)c1=O | 10.1016/j.bmcl.2016.10.038 | |||
CHEMBL3912263 | 145254 | None | 0 | Human | Binding | pIC50 | = | 5.9 | 5.9 | - | 0 | ChEMBL | 485 | 10 | 1 | 7 | 3.2 | Cc1cc(CN(C)C(CC(=O)O)c2ccc(Cl)cc2)ccc1OCCn1c(=O)ccn(C)c1=O | 10.1016/j.bmcl.2016.10.038 | |||
71585300 | 132383 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 564 | 12 | 1 | 7 | 4.6 | COc1cc(CN(CC2CCCC(C(=O)O)C2)C(C)c2ccc3c(c2)CCO3)ccc1OCCN1C(=O)CCC1=O | nan | |||
CHEMBL3697078 | 132383 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 564 | 12 | 1 | 7 | 4.6 | COc1cc(CN(CC2CCCC(C(=O)O)C2)C(C)c2ccc3c(c2)CCO3)ccc1OCCN1C(=O)CCC1=O | nan | |||
56673938 | 64255 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 455 | 2 | 2 | 3 | 3.4 | CN1CCN(C(=O)[C@@H]2C=C3c4cccc5[nH]cc(c45)C[C@H]3N(C(=O)Nc3ccccc3)C2)CC1 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1809006 | 64255 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 455 | 2 | 2 | 3 | 3.4 | CN1CCN(C(=O)[C@@H]2C=C3c4cccc5[nH]cc(c45)C[C@H]3N(C(=O)Nc3ccccc3)C2)CC1 | 10.1016/j.bmcl.2011.06.070 | |||
90014726 | 148041 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 529 | 13 | 1 | 8 | 3.7 | CCCN(Cc1ccc(OCCn2c(=O)ccn(C)c2=O)c(OC)c1)C(CC(=O)O)c1ccc(Cl)cc1 | 10.1016/j.bmcl.2016.10.038 | |||
CHEMBL3933856 | 148041 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 529 | 13 | 1 | 8 | 3.7 | CCCN(Cc1ccc(OCCn2c(=O)ccn(C)c2=O)c(OC)c1)C(CC(=O)O)c1ccc(Cl)cc1 | 10.1016/j.bmcl.2016.10.038 | |||
90014726 | 148041 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 529 | 13 | 1 | 8 | 3.7 | CCCN(Cc1ccc(OCCn2c(=O)ccn(C)c2=O)c(OC)c1)C(CC(=O)O)c1ccc(Cl)cc1 | nan | |||
CHEMBL3933856 | 148041 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 529 | 13 | 1 | 8 | 3.7 | CCCN(Cc1ccc(OCCn2c(=O)ccn(C)c2=O)c(OC)c1)C(CC(=O)O)c1ccc(Cl)cc1 | nan | |||
141491517 | 193716 | None | 0 | Human | Binding | pIC50 | = | 5.9 | 5.9 | - | 0 | ChEMBL | 531 | 4 | 0 | 10 | 2.8 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2cnc(C(F)(F)F)nc2)CCN1C(=O)Cn1cnc(C#N)n1 | 10.1021/acs.jmedchem.3c00074 | |||
CHEMBL5269745 | 193716 | None | 0 | Human | Binding | pIC50 | = | 5.9 | 5.9 | - | 0 | ChEMBL | 531 | 4 | 0 | 10 | 2.8 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2cnc(C(F)(F)F)nc2)CCN1C(=O)Cn1cnc(C#N)n1 | 10.1021/acs.jmedchem.3c00074 | |||
72550703 | 151367 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 502 | 12 | 1 | 5 | 4.4 | O=C(O)CC(c1ccc(Cl)cc1)N(Cc1ccc(OCCN2C(=O)CCC2=O)c(F)c1)CC1CC1 | nan | |||
CHEMBL3960394 | 151367 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 502 | 12 | 1 | 5 | 4.4 | O=C(O)CC(c1ccc(Cl)cc1)N(Cc1ccc(OCCN2C(=O)CCC2=O)c(F)c1)CC1CC1 | nan | |||
90014502 | 151726 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 534 | 13 | 1 | 5 | 5.6 | CCCCN(Cc1ccc(OCCN2C(=O)CCC2=O)c(C)c1)C(CC(=O)O)c1ccc(Cl)cc1Cl | nan | |||
CHEMBL3963806 | 151726 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 534 | 13 | 1 | 5 | 5.6 | CCCCN(Cc1ccc(OCCN2C(=O)CCC2=O)c(C)c1)C(CC(=O)O)c1ccc(Cl)cc1Cl | nan | |||
90015254 | 143588 | None | 0 | Human | Binding | pIC50 | = | 5.9 | 5.9 | - | 0 | ChEMBL | 498 | 10 | 1 | 5 | 4.4 | CCCN(Cc1ccc(OCCN2C(=O)CCC2=O)c(C)c1)C1c2ccc(Cl)cc2CC1C(=O)O | 10.1016/j.bmcl.2016.10.038 | |||
CHEMBL3898743 | 143588 | None | 0 | Human | Binding | pIC50 | = | 5.9 | 5.9 | - | 0 | ChEMBL | 498 | 10 | 1 | 5 | 4.4 | CCCN(Cc1ccc(OCCN2C(=O)CCC2=O)c(C)c1)C1c2ccc(Cl)cc2CC1C(=O)O | 10.1016/j.bmcl.2016.10.038 | |||
90015254 | 143588 | None | 0 | Human | Binding | pIC50 | = | 5.9 | 5.9 | - | 0 | ChEMBL | 498 | 10 | 1 | 5 | 4.4 | CCCN(Cc1ccc(OCCN2C(=O)CCC2=O)c(C)c1)C1c2ccc(Cl)cc2CC1C(=O)O | nan | |||
CHEMBL3898743 | 143588 | None | 0 | Human | Binding | pIC50 | = | 5.9 | 5.9 | - | 0 | ChEMBL | 498 | 10 | 1 | 5 | 4.4 | CCCN(Cc1ccc(OCCN2C(=O)CCC2=O)c(C)c1)C1c2ccc(Cl)cc2CC1C(=O)O | nan | |||
71679145 | 144508 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 472 | 5 | 1 | 7 | 4.0 | COc1cccc2c1ccn2CC(=O)N1CCN(c2scnc2-c2nc3ccccc3[nH]2)CC1 | nan | |||
CHEMBL3906246 | 144508 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 472 | 5 | 1 | 7 | 4.0 | COc1cccc2c1ccn2CC(=O)N1CCN(c2scnc2-c2nc3ccccc3[nH]2)CC1 | nan | |||
44426716 | 150980 | None | 0 | Human | Binding | pIC50 | = | 5.9 | 5.9 | - | 0 | ChEMBL | 586 | 8 | 1 | 6 | 5.8 | C[C@H](c1nc2ccccc2c(=O)n1-c1ccc(C(=O)O)cc1)N(Cc1cccnc1)C(=O)Cc1ccc(C(F)(F)F)cc1 | 10.1016/j.bmcl.2007.03.106 | |||
CHEMBL395748 | 150980 | None | 0 | Human | Binding | pIC50 | = | 5.9 | 5.9 | - | 0 | ChEMBL | 586 | 8 | 1 | 6 | 5.8 | C[C@H](c1nc2ccccc2c(=O)n1-c1ccc(C(=O)O)cc1)N(Cc1cccnc1)C(=O)Cc1ccc(C(F)(F)F)cc1 | 10.1016/j.bmcl.2007.03.106 | |||
59772590 | 105415 | None | 0 | Human | Binding | pIC50 | = | 5.9 | 5.9 | - | 0 | ChEMBL | 518 | 6 | 1 | 7 | 4.3 | CC[C@H]1CN(c2ncc(-c3nnn[nH]3)cc2Cl)CCN1C1CCN(Cc2ccc(Cl)cc2F)CC1 | 10.1016/j.bmcl.2014.01.009 | |||
CHEMBL3116471 | 105415 | None | 0 | Human | Binding | pIC50 | = | 5.9 | 5.9 | - | 0 | ChEMBL | 518 | 6 | 1 | 7 | 4.3 | CC[C@H]1CN(c2ncc(-c3nnn[nH]3)cc2Cl)CCN1C1CCN(Cc2ccc(Cl)cc2F)CC1 | 10.1016/j.bmcl.2014.01.009 | |||
134140635 | 147273 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 584 | 13 | 1 | 7 | 5.0 | COc1cc(CN(Cc2ccc(/C=C/C(=O)O)cc2)C(C)c2ccc3c(c2)CCO3)ccc1OCCN1C(=O)CCC1=O | 10.1016/j.bmcl.2016.10.035 | |||
CHEMBL3928025 | 147273 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 584 | 13 | 1 | 7 | 5.0 | COc1cc(CN(Cc2ccc(/C=C/C(=O)O)cc2)C(C)c2ccc3c(c2)CCO3)ccc1OCCN1C(=O)CCC1=O | 10.1016/j.bmcl.2016.10.035 | |||
44426711 | 153251 | None | 0 | Human | Binding | pIC50 | = | 7.9 | 7.9 | - | 0 | ChEMBL | 572 | 8 | 0 | 6 | 6.1 | COc1ccc(-n2c([C@@H](C)N(Cc3cccnc3)C(=O)Cc3ccc(C(F)(F)F)cc3)nc3ccccc3c2=O)cc1 | 10.1016/j.bmcl.2007.03.106 | |||
CHEMBL397678 | 153251 | None | 0 | Human | Binding | pIC50 | = | 7.9 | 7.9 | - | 0 | ChEMBL | 572 | 8 | 0 | 6 | 6.1 | COc1ccc(-n2c([C@@H](C)N(Cc3cccnc3)C(=O)Cc3ccc(C(F)(F)F)cc3)nc3ccccc3c2=O)cc1 | 10.1016/j.bmcl.2007.03.106 | |||
9938965 | 5673 | None | 2 | Human | Binding | pIC50 | = | 7.9 | 7.9 | - | 0 | ChEMBL | 619 | 10 | 0 | 8 | 5.0 | CCOc1ccc(-n2c([C@@H](C)N(Cc3ccc[n+]([O-])c3)C(=O)Cc3ccc(OC(F)(F)F)cc3)nc3ncccc3c2=O)cc1 | 10.1016/j.bmcl.2011.10.120 | |||
CHEMBL1077832 | 5673 | None | 2 | Human | Binding | pIC50 | = | 7.9 | 7.9 | - | 0 | ChEMBL | 619 | 10 | 0 | 8 | 5.0 | CCOc1ccc(-n2c([C@@H](C)N(Cc3ccc[n+]([O-])c3)C(=O)Cc3ccc(OC(F)(F)F)cc3)nc3ncccc3c2=O)cc1 | 10.1016/j.bmcl.2011.10.120 | |||
44455801 | 168878 | None | 0 | Human | Binding | pIC50 | = | 7.9 | 7.9 | - | 0 | ChEMBL | 608 | 10 | 0 | 5 | 7.3 | CCOc1ccc(-n2cc(-c3ccccc3)nc2[C@@H](C)N(C[C@H]2CCCN2C)C(=O)Cc2ccc(F)c(C(F)(F)F)c2)cc1 | 10.1016/j.bmcl.2007.11.072 | |||
CHEMBL437401 | 168878 | None | 0 | Human | Binding | pIC50 | = | 7.9 | 7.9 | - | 0 | ChEMBL | 608 | 10 | 0 | 5 | 7.3 | CCOc1ccc(-n2cc(-c3ccccc3)nc2[C@@H](C)N(C[C@H]2CCCN2C)C(=O)Cc2ccc(F)c(C(F)(F)F)c2)cc1 | 10.1016/j.bmcl.2007.11.072 | |||
44455604 | 155404 | None | 0 | Human | Binding | pIC50 | = | 7.9 | 7.9 | - | 0 | ChEMBL | 612 | 10 | 0 | 6 | 6.1 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc(-c2ccccc2)cn1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2007.11.072 | |||
CHEMBL403036 | 155404 | None | 0 | Human | Binding | pIC50 | = | 7.9 | 7.9 | - | 0 | ChEMBL | 612 | 10 | 0 | 6 | 6.1 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)[C@H](C)c1nc(-c2ccccc2)cn1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2007.11.072 | |||
56670448 | 64260 | None | 0 | Human | Binding | pIC50 | = | 7.9 | 7.9 | - | 0 | ChEMBL | 456 | 2 | 3 | 3 | 3.6 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CCC(O)CC1 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1809011 | 64260 | None | 0 | Human | Binding | pIC50 | = | 7.9 | 7.9 | - | 0 | ChEMBL | 456 | 2 | 3 | 3 | 3.6 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CCC(O)CC1 | 10.1016/j.bmcl.2011.06.070 | |||
56673945 | 64285 | None | 0 | Rat | Binding | pIC50 | = | 7.9 | 7.9 | - | 0 | ChEMBL | 523 | 5 | 1 | 4 | 4.8 | O=C([C@@H]1C=C2c3cccc4c3c(cn4CCN3CCCC3)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CCCC1 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1809040 | 64285 | None | 0 | Rat | Binding | pIC50 | = | 7.9 | 7.9 | - | 0 | ChEMBL | 523 | 5 | 1 | 4 | 4.8 | O=C([C@@H]1C=C2c3cccc4c3c(cn4CCN3CCCC3)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CCCC1 | 10.1016/j.bmcl.2011.06.070 | |||
89726247 | 143277 | None | 0 | Human | Binding | pIC50 | = | 7.9 | 7.9 | - | 0 | ChEMBL | 547 | 8 | 1 | 10 | 2.7 | COCCOc1ccc2[nH]c(-c3ncsc3N3CCN(C(=O)Cn4c(=O)n(C)c5ccccc54)CC3)nc2c1 | nan | |||
CHEMBL3896194 | 143277 | None | 0 | Human | Binding | pIC50 | = | 7.9 | 7.9 | - | 0 | ChEMBL | 547 | 8 | 1 | 10 | 2.7 | COCCOc1ccc2[nH]c(-c3ncsc3N3CCN(C(=O)Cn4c(=O)n(C)c5ccccc54)CC3)nc2c1 | nan | |||
71679632 | 144929 | None | 0 | Human | Binding | pIC50 | = | 7.9 | 7.9 | - | 0 | ChEMBL | 443 | 4 | 1 | 7 | 3.4 | O=C(Cn1ccc2cccnc21)N1CCN(c2scnc2-c2nc3ccccc3[nH]2)CC1 | nan | |||
CHEMBL3909669 | 144929 | None | 0 | Human | Binding | pIC50 | = | 7.9 | 7.9 | - | 0 | ChEMBL | 443 | 4 | 1 | 7 | 3.4 | O=C(Cn1ccc2cccnc21)N1CCN(c2scnc2-c2nc3ccccc3[nH]2)CC1 | nan | |||
89726431 | 146317 | None | 0 | Human | Binding | pIC50 | = | 7.9 | 7.9 | - | 0 | ChEMBL | 487 | 5 | 2 | 8 | 3.3 | C[C@@H]1CN(c2scnc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1c(CO)cc2cccnc21 | nan | |||
CHEMBL3920326 | 146317 | None | 0 | Human | Binding | pIC50 | = | 7.9 | 7.9 | - | 0 | ChEMBL | 487 | 5 | 2 | 8 | 3.3 | C[C@@H]1CN(c2scnc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1c(CO)cc2cccnc21 | nan | |||
71679637 | 151502 | None | 0 | Human | Binding | pIC50 | = | 7.9 | 7.9 | - | 0 | ChEMBL | 533 | 7 | 2 | 10 | 2.1 | Cn1c(=O)n(CC(=O)N2CCN(c3scnc3-c3nc4cc(OCCO)ccc4[nH]3)CC2)c2ccccc21 | nan | |||
CHEMBL3961715 | 151502 | None | 0 | Human | Binding | pIC50 | = | 7.9 | 7.9 | - | 0 | ChEMBL | 533 | 7 | 2 | 10 | 2.1 | Cn1c(=O)n(CC(=O)N2CCN(c3scnc3-c3nc4cc(OCCO)ccc4[nH]3)CC2)c2ccccc21 | nan | |||
121485715 | 194231 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 562 | 6 | 1 | 10 | 2.8 | O=C(Cn1cnc(C2CC2)n1)N1CCN(c2sc(C(F)(F)F)nc2-c2cnc(C(F)(F)F)nc2)C[C@H]1CO | 10.1021/acs.jmedchem.3c00074 | |||
CHEMBL5281745 | 194231 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 562 | 6 | 1 | 10 | 2.8 | O=C(Cn1cnc(C2CC2)n1)N1CCN(c2sc(C(F)(F)F)nc2-c2cnc(C(F)(F)F)nc2)C[C@H]1CO | 10.1021/acs.jmedchem.3c00074 | |||
90014982 | 145917 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 550 | 14 | 1 | 6 | 5.3 | CCCCN(Cc1ccc(OCCN2C(=O)CCC2=O)c(OC)c1)C(CC(=O)O)c1ccc(Cl)cc1Cl | nan | |||
CHEMBL3917146 | 145917 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 550 | 14 | 1 | 6 | 5.3 | CCCCN(Cc1ccc(OCCN2C(=O)CCC2=O)c(OC)c1)C(CC(=O)O)c1ccc(Cl)cc1Cl | nan | |||
44426682 | 85972 | None | 0 | Human | Binding | pIC50 | = | 5.9 | 5.9 | - | 0 | ChEMBL | 530 | 14 | 0 | 6 | 5.1 | CCCCCCCCS(=O)(=O)N(CCN(C)C)[C@H](C)c1nc2ccccc2c(=O)n1-c1ccc(F)cc1 | 10.1016/j.bmcl.2007.03.106 | |||
CHEMBL230020 | 85972 | None | 0 | Human | Binding | pIC50 | = | 5.9 | 5.9 | - | 0 | ChEMBL | 530 | 14 | 0 | 6 | 5.1 | CCCCCCCCS(=O)(=O)N(CCN(C)C)[C@H](C)c1nc2ccccc2c(=O)n1-c1ccc(F)cc1 | 10.1016/j.bmcl.2007.03.106 | |||
44426725 | 137266 | None | 0 | Human | Binding | pIC50 | = | 5.9 | 5.9 | - | 0 | ChEMBL | 603 | 10 | 0 | 8 | 5.8 | CCOc1ccc(-n2c([C@@H](C)N(Cc3cccnc3)C(=O)Cc3ccc(OC(F)(F)F)cc3)nc3cccnc3c2=O)cc1 | 10.1016/j.bmcl.2007.03.106 | |||
CHEMBL374820 | 137266 | None | 0 | Human | Binding | pIC50 | = | 5.9 | 5.9 | - | 0 | ChEMBL | 603 | 10 | 0 | 8 | 5.8 | CCOc1ccc(-n2c([C@@H](C)N(Cc3cccnc3)C(=O)Cc3ccc(OC(F)(F)F)cc3)nc3cccnc3c2=O)cc1 | 10.1016/j.bmcl.2007.03.106 | |||
44453267 | 95181 | None | 0 | Mouse | Binding | pIC50 | = | 5.9 | 5.9 | - | 0 | ChEMBL | 508 | 9 | 1 | 5 | 5.2 | CN(CCCn1c(=N)n(CC(=O)c2ccc(Cl)cc2)c2cccc(Cl)c21)C(=O)Cc1ccccc1 | 10.1016/j.bmcl.2008.02.049 | |||
CHEMBL255583 | 95181 | None | 0 | Mouse | Binding | pIC50 | = | 5.9 | 5.9 | - | 0 | ChEMBL | 508 | 9 | 1 | 5 | 5.2 | CN(CCCn1c(=N)n(CC(=O)c2ccc(Cl)cc2)c2cccc(Cl)c21)C(=O)Cc1ccccc1 | 10.1016/j.bmcl.2008.02.049 | |||
45486557 | 200131 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 659 | 11 | 0 | 9 | 4.8 | CCOc1ccc2c(=O)n(-c3ccc(C#N)cc3)c(C(C)N(CCS(=O)(=O)CC)C(=O)Cc3ccc(F)c(C(F)(F)F)c3)nc2n1 | 10.1016/j.bmcl.2009.07.021 | |||
CHEMBL571082 | 200131 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 659 | 11 | 0 | 9 | 4.8 | CCOc1ccc2c(=O)n(-c3ccc(C#N)cc3)c(C(C)N(CCS(=O)(=O)CC)C(=O)Cc3ccc(F)c(C(F)(F)F)c3)nc2n1 | 10.1016/j.bmcl.2009.07.021 | |||
145440630 | 193780 | None | 0 | Human | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 549 | 6 | 1 | 9 | 3.2 | Cc1ccn(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3cnc(C(F)(F)F)nc3)C[C@@H]2CCO)n1 | 10.1021/acs.jmedchem.3c00074 | |||
CHEMBL5271152 | 193780 | None | 0 | Human | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 549 | 6 | 1 | 9 | 3.2 | Cc1ccn(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3cnc(C(F)(F)F)nc3)C[C@@H]2CCO)n1 | 10.1021/acs.jmedchem.3c00074 | |||
71585811 | 150695 | None | 0 | Human | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 597 | 13 | 1 | 8 | 5.1 | CCC(c1ccc(Cl)cc1)N(Cc1ccc(OCCn2c(=O)ccn(C)c2=O)c(OC)c1)CC1CCC(C(=O)O)CC1 | nan | |||
CHEMBL3955242 | 150695 | None | 0 | Human | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 597 | 13 | 1 | 8 | 5.1 | CCC(c1ccc(Cl)cc1)N(Cc1ccc(OCCn2c(=O)ccn(C)c2=O)c(OC)c1)CC1CCC(C(=O)O)CC1 | nan | |||
72550699 | 143567 | None | 0 | Human | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 550 | 13 | 1 | 6 | 5.2 | COc1cc(CN(CC(C)C)C(CC(=O)O)c2ccc(Cl)c(Cl)c2)ccc1OCCN1C(=O)CCC1=O | 10.1016/j.bmcl.2016.10.038 | |||
CHEMBL3898564 | 143567 | None | 0 | Human | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 550 | 13 | 1 | 6 | 5.2 | COc1cc(CN(CC(C)C)C(CC(=O)O)c2ccc(Cl)c(Cl)c2)ccc1OCCN1C(=O)CCC1=O | 10.1016/j.bmcl.2016.10.038 | |||
72550699 | 143567 | None | 0 | Human | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 550 | 13 | 1 | 6 | 5.2 | COc1cc(CN(CC(C)C)C(CC(=O)O)c2ccc(Cl)c(Cl)c2)ccc1OCCN1C(=O)CCC1=O | nan | |||
CHEMBL3898564 | 143567 | None | 0 | Human | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 550 | 13 | 1 | 6 | 5.2 | COc1cc(CN(CC(C)C)C(CC(=O)O)c2ccc(Cl)c(Cl)c2)ccc1OCCN1C(=O)CCC1=O | nan | |||
71585197 | 132377 | None | 0 | Human | Binding | pIC50 | = | 5.8 | 5.8 | - | 0 | ChEMBL | 560 | 11 | 1 | 6 | 5.2 | COc1cc(CN(C[C@H]2CC[C@H](C(=O)O)CC2)C(C)c2ccc3c(c2)CCO3)ccc1/C=C/CN1C(=O)CCC1=O | nan | |||
CHEMBL3697072 | 132377 | None | 0 | Human | Binding | pIC50 | = | 5.8 | 5.8 | - | 0 | ChEMBL | 560 | 11 | 1 | 6 | 5.2 | COc1cc(CN(C[C@H]2CC[C@H](C(=O)O)CC2)C(C)c2ccc3c(c2)CCO3)ccc1/C=C/CN1C(=O)CCC1=O | nan | |||
71679792 | 146935 | None | 0 | Human | Binding | pIC50 | = | 5.8 | 5.8 | - | 0 | ChEMBL | 444 | 4 | 1 | 8 | 2.8 | O=C(Cn1cnc2cccnc21)N1CCN(c2scnc2-c2nc3ccccc3[nH]2)CC1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL3925131 | 146935 | None | 0 | Human | Binding | pIC50 | = | 5.8 | 5.8 | - | 0 | ChEMBL | 444 | 4 | 1 | 8 | 2.8 | O=C(Cn1cnc2cccnc21)N1CCN(c2scnc2-c2nc3ccccc3[nH]2)CC1 | 10.1021/acs.jmedchem.2c00675 | |||
121485407 | 193936 | None | 0 | Human | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 520 | 4 | 0 | 9 | 3.3 | Cc1ncn(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3cnc(C(F)(F)F)nc3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.3c00074 | |||
CHEMBL5274784 | 193936 | None | 0 | Human | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 520 | 4 | 0 | 9 | 3.3 | Cc1ncn(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3cnc(C(F)(F)F)nc3)C[C@H]2C)n1 | 10.1021/acs.jmedchem.3c00074 | |||
71586308 | 132447 | None | 0 | Human | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 550 | 12 | 1 | 7 | 4.2 | COc1cc(CN(C[C@@H]2CC[C@H](C(=O)O)C2)[C@@H](C)c2ccc3c(c2)CCO3)ccc1OCCN1C(=O)CCC1=O | nan | |||
CHEMBL3697142 | 132447 | None | 0 | Human | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 550 | 12 | 1 | 7 | 4.2 | COc1cc(CN(C[C@@H]2CC[C@H](C(=O)O)C2)[C@@H](C)c2ccc3c(c2)CCO3)ccc1OCCN1C(=O)CCC1=O | nan | |||
44426724 | 153606 | None | 0 | Human | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 603 | 10 | 0 | 8 | 5.8 | CCOc1ccc(-n2c([C@@H](C)N(Cc3cccnc3)C(=O)Cc3ccc(OC(F)(F)F)cc3)nc3cnccc3c2=O)cc1 | 10.1016/j.bmcl.2007.03.106 | |||
CHEMBL397984 | 153606 | None | 0 | Human | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 603 | 10 | 0 | 8 | 5.8 | CCOc1ccc(-n2c([C@@H](C)N(Cc3cccnc3)C(=O)Cc3ccc(OC(F)(F)F)cc3)nc3cnccc3c2=O)cc1 | 10.1016/j.bmcl.2007.03.106 | |||
90014586 | 143491 | None | 0 | Human | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 572 | 13 | 1 | 5 | 6.2 | CCc1cc(CN(CC2CCCCC2)C(CC(=O)O)c2ccc(Cl)c(F)c2)ccc1OCCN1C(=O)CCC1=O | nan | |||
CHEMBL3897980 | 143491 | None | 0 | Human | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 572 | 13 | 1 | 5 | 6.2 | CCc1cc(CN(CC2CCCCC2)C(CC(=O)O)c2ccc(Cl)c(F)c2)ccc1OCCN1C(=O)CCC1=O | nan | |||
89610809 | 132453 | None | 0 | Human | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 522 | 12 | 1 | 7 | 3.4 | COc1cc(CN(C[C@@H]2C[C@H]2C(=O)O)C(C)c2ccc3c(c2)CCO3)ccc1OCCN1C(=O)CCC1=O | nan | |||
CHEMBL3697148 | 132453 | None | 0 | Human | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 522 | 12 | 1 | 7 | 3.4 | COc1cc(CN(C[C@@H]2C[C@H]2C(=O)O)C(C)c2ccc3c(c2)CCO3)ccc1OCCN1C(=O)CCC1=O | nan | |||
56663561 | 64282 | None | 0 | Human | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 526 | 5 | 1 | 5 | 4.7 | CC(C)OC(=O)Cn1cc2c3c(cccc31)C1=C[C@@H](C(=O)N3CCCC3)CN(C(=O)Nc3ccccc3)[C@@H]1C2 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1809037 | 64282 | None | 0 | Human | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 526 | 5 | 1 | 5 | 4.7 | CC(C)OC(=O)Cn1cc2c3c(cccc31)C1=C[C@@H](C(=O)N3CCCC3)CN(C(=O)Nc3ccccc3)[C@@H]1C2 | 10.1016/j.bmcl.2011.06.070 | |||
72549131 | 151943 | None | 0 | Human | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 532 | 12 | 1 | 5 | 5.3 | O=C(O)C[C@@H](c1ccc(Cl)cc1)N(Cc1ccc(OCCN2C(=O)CCC2=O)c(Cl)c1)CC1CCC1 | nan | |||
CHEMBL3965504 | 151943 | None | 0 | Human | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 532 | 12 | 1 | 5 | 5.3 | O=C(O)C[C@@H](c1ccc(Cl)cc1)N(Cc1ccc(OCCN2C(=O)CCC2=O)c(Cl)c1)CC1CCC1 | nan | |||
71586008 | 132424 | None | 0 | Human | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 520 | 11 | 1 | 5 | 5.3 | Cc1ccc(C(C)N(Cc2ccc(OCCN3C(=O)CCC3=O)c(C)c2)C[C@H]2CC[C@H](C(=O)O)CC2)cc1 | nan | |||
CHEMBL3697120 | 132424 | None | 0 | Human | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 520 | 11 | 1 | 5 | 5.3 | Cc1ccc(C(C)N(Cc2ccc(OCCN3C(=O)CCC3=O)c(C)c2)C[C@H]2CC[C@H](C(=O)O)CC2)cc1 | nan | |||
89610584 | 132848 | None | 0 | Human | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 577 | 12 | 1 | 6 | 4.9 | COc1cc(CN(C[C@H]2CC[C@H](C(=O)O)CC2)C(C)c2ccc3c(c2)CCC3)ccc1OCCN1C(=O)CN(C)C1=O | nan | |||
CHEMBL3700579 | 132848 | None | 0 | Human | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 577 | 12 | 1 | 6 | 4.9 | COc1cc(CN(C[C@H]2CC[C@H](C(=O)O)CC2)C(C)c2ccc3c(c2)CCC3)ccc1OCCN1C(=O)CN(C)C1=O | nan | |||
44426595 | 137644 | None | 0 | Human | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 508 | 14 | 0 | 5 | 6.1 | CCCCCCCCCC(=O)N(CCN(C)C)[C@H](C)c1nc2ccccc2c(=O)n1-c1ccc(F)cc1 | 10.1016/j.bmcl.2007.03.106 | |||
CHEMBL375457 | 137644 | None | 0 | Human | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 508 | 14 | 0 | 5 | 6.1 | CCCCCCCCCC(=O)N(CCN(C)C)[C@H](C)c1nc2ccccc2c(=O)n1-c1ccc(F)cc1 | 10.1016/j.bmcl.2007.03.106 | |||
90014869 | 145492 | None | 0 | Human | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 551 | 13 | 1 | 9 | 3.2 | COc1cc(CN(CC(C)C)C(CC(=O)O)c2ccc3c(c2)CCO3)ccc1OCCn1c(=O)ccn(C)c1=O | 10.1016/j.bmcl.2016.10.038 | |||
CHEMBL3913989 | 145492 | None | 0 | Human | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 551 | 13 | 1 | 9 | 3.2 | COc1cc(CN(CC(C)C)C(CC(=O)O)c2ccc3c(c2)CCO3)ccc1OCCn1c(=O)ccn(C)c1=O | 10.1016/j.bmcl.2016.10.038 | |||
45482849 | 201303 | None | 2 | Human | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 442 | 4 | 2 | 2 | 4.8 | CCN(CC)C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2C)C1 | 10.1016/j.bmcl.2009.09.002 | |||
CHEMBL583761 | 201303 | None | 2 | Human | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 442 | 4 | 2 | 2 | 4.8 | CCN(CC)C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2C)C1 | 10.1016/j.bmcl.2009.09.002 | |||
90014869 | 145492 | None | 0 | Human | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 551 | 13 | 1 | 9 | 3.2 | COc1cc(CN(CC(C)C)C(CC(=O)O)c2ccc3c(c2)CCO3)ccc1OCCn1c(=O)ccn(C)c1=O | nan | |||
CHEMBL3913989 | 145492 | None | 0 | Human | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 551 | 13 | 1 | 9 | 3.2 | COc1cc(CN(CC(C)C)C(CC(=O)O)c2ccc3c(c2)CCO3)ccc1OCCn1c(=O)ccn(C)c1=O | nan | |||
89610621 | 132855 | None | 0 | Human | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 548 | 11 | 1 | 6 | 5.0 | COc1cc(CN([C@H]2C[C@@H](C(=O)O)C2)[C@H](C)c2ccc(Cl)c(Cl)c2)ccc1OCCN1C(=O)CCC1=O | nan | |||
CHEMBL3700586 | 132855 | None | 0 | Human | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 548 | 11 | 1 | 6 | 5.0 | COc1cc(CN([C@H]2C[C@@H](C(=O)O)C2)[C@H](C)c2ccc(Cl)c(Cl)c2)ccc1OCCN1C(=O)CCC1=O | nan | |||
45486559 | 201012 | None | 0 | Human | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 683 | 9 | 0 | 8 | 5.4 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)C(C)c1nc2nc(C(F)(F)F)ccc2c(=O)n1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2009.07.021 | |||
CHEMBL578196 | 201012 | None | 0 | Human | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 683 | 9 | 0 | 8 | 5.4 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(F)c(C(F)(F)F)c1)C(C)c1nc2nc(C(F)(F)F)ccc2c(=O)n1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2009.07.021 | |||
89610511 | 132445 | None | 0 | Human | Binding | pIC50 | = | 7.8 | 7.8 | - | 0 | ChEMBL | 550 | 12 | 1 | 7 | 4.2 | COc1cc(CN(C[C@@H]2CC[C@@H](C(=O)O)C2)[C@H](C)c2ccc3c(c2)CCO3)ccc1OCCN1C(=O)CCC1=O | nan | |||
CHEMBL3697140 | 132445 | None | 0 | Human | Binding | pIC50 | = | 7.8 | 7.8 | - | 0 | ChEMBL | 550 | 12 | 1 | 7 | 4.2 | COc1cc(CN(C[C@@H]2CC[C@@H](C(=O)O)C2)[C@H](C)c2ccc3c(c2)CCO3)ccc1OCCN1C(=O)CCC1=O | nan | |||
44453168 | 95357 | None | 0 | Human | Binding | pIC50 | = | 7.8 | 7.8 | - | 0 | ChEMBL | 544 | 8 | 1 | 5 | 6.4 | CN(CCCn1c(=N)n(CC(=O)c2ccc(Cl)cc2)c2cccc(Cl)c21)C(=O)c1ccc2ccccc2c1 | 10.1016/j.bmcl.2008.02.049 | |||
CHEMBL256457 | 95357 | None | 0 | Human | Binding | pIC50 | = | 7.8 | 7.8 | - | 0 | ChEMBL | 544 | 8 | 1 | 5 | 6.4 | CN(CCCn1c(=N)n(CC(=O)c2ccc(Cl)cc2)c2cccc(Cl)c21)C(=O)c1ccc2ccccc2c1 | 10.1016/j.bmcl.2008.02.049 | |||
44453558 | 95486 | None | 0 | Human | Binding | pIC50 | = | 7.8 | 7.8 | - | 0 | ChEMBL | 571 | 6 | 1 | 6 | 6.2 | N=c1n(CC(=O)c2ccc(Cl)cc2)c2cccc(Cl)c2n1C[C@@H]1CCCN(C(=O)c2cccc3cccnc23)C1 | 10.1016/j.bmcl.2008.02.049 | |||
CHEMBL257038 | 95486 | None | 0 | Human | Binding | pIC50 | = | 7.8 | 7.8 | - | 0 | ChEMBL | 571 | 6 | 1 | 6 | 6.2 | N=c1n(CC(=O)c2ccc(Cl)cc2)c2cccc(Cl)c2n1C[C@@H]1CCCN(C(=O)c2cccc3cccnc23)C1 | 10.1016/j.bmcl.2008.02.049 | |||
44453583 | 97975 | None | 0 | Human | Binding | pIC50 | = | 7.8 | 7.8 | - | 0 | ChEMBL | 571 | 6 | 1 | 6 | 6.2 | N=c1n(CC(=O)c2ccc(Cl)cc2)c2cccc(Cl)c2n1CC1CCCN(C(=O)c2cccc3cccnc23)C1 | 10.1016/j.bmcl.2008.02.049 | |||
CHEMBL272522 | 97975 | None | 0 | Human | Binding | pIC50 | = | 7.8 | 7.8 | - | 0 | ChEMBL | 571 | 6 | 1 | 6 | 6.2 | N=c1n(CC(=O)c2ccc(Cl)cc2)c2cccc(Cl)c2n1CC1CCCN(C(=O)c2cccc3cccnc23)C1 | 10.1016/j.bmcl.2008.02.049 | |||
57402420 | 69987 | None | 0 | Human | Binding | pIC50 | = | 7.8 | 7.8 | - | 0 | ChEMBL | 641 | 7 | 0 | 8 | 4.8 | C[C@H](c1nc2ncccc2c(=O)n1-c1ccc(C#N)cc1)N(CC1CCS(=O)(=O)CC1)C(=O)Cc1ccc(C(F)(F)F)c(F)c1 | 10.1016/j.bmcl.2011.10.120 | |||
CHEMBL1939554 | 69987 | None | 0 | Human | Binding | pIC50 | = | 7.8 | 7.8 | - | 0 | ChEMBL | 641 | 7 | 0 | 8 | 4.8 | C[C@H](c1nc2ncccc2c(=O)n1-c1ccc(C#N)cc1)N(CC1CCS(=O)(=O)CC1)C(=O)Cc1ccc(C(F)(F)F)c(F)c1 | 10.1016/j.bmcl.2011.10.120 | |||
45486520 | 201366 | None | 0 | Human | Binding | pIC50 | = | 7.8 | 7.8 | - | 0 | ChEMBL | 587 | 9 | 0 | 7 | 5.0 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(C(F)(F)F)c(F)c1)[C@H](C)c1nc2cnccn2c1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2009.07.021 | |||
CHEMBL584518 | 201366 | None | 0 | Human | Binding | pIC50 | = | 7.8 | 7.8 | - | 0 | ChEMBL | 587 | 9 | 0 | 7 | 5.0 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(C(F)(F)F)c(F)c1)[C@H](C)c1nc2cnccn2c1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2009.07.021 | |||
71678296 | 144532 | None | 0 | Human | Binding | pIC50 | = | 7.8 | 7.8 | - | 0 | ChEMBL | 498 | 4 | 1 | 9 | 2.6 | Cn1c(=O)n(CC(=O)N2CCN(c3scnc3-c3nc4cc(C#N)ccc4[nH]3)CC2)c2ccccc21 | nan | |||
CHEMBL3906483 | 144532 | None | 0 | Human | Binding | pIC50 | = | 7.8 | 7.8 | - | 0 | ChEMBL | 498 | 4 | 1 | 9 | 2.6 | Cn1c(=O)n(CC(=O)N2CCN(c3scnc3-c3nc4cc(C#N)ccc4[nH]3)CC2)c2ccccc21 | nan | |||
89726402 | 147708 | None | 0 | Human | Binding | pIC50 | = | 7.8 | 7.8 | - | 0 | ChEMBL | 588 | 7 | 1 | 9 | 3.9 | COC1CCN(Cc2ccc3nc(-c4nc(C(F)(F)F)sc4N4CCN(C(=O)Cn5cccn5)[C@H](C)C4)[nH]c3c2)C1 | nan | |||
CHEMBL3931292 | 147708 | None | 0 | Human | Binding | pIC50 | = | 7.8 | 7.8 | - | 0 | ChEMBL | 588 | 7 | 1 | 9 | 3.9 | COC1CCN(Cc2ccc3nc(-c4nc(C(F)(F)F)sc4N4CCN(C(=O)Cn5cccn5)[C@H](C)C4)[nH]c3c2)C1 | nan | |||
71680470 | 148917 | None | 0 | Human | Binding | pIC50 | = | 7.8 | 7.8 | - | 0 | ChEMBL | 471 | 5 | 1 | 7 | 3.9 | CCc1nc(-c2nc3ccccc3[nH]2)c(N2CCN(C(=O)Cn3ccc4cccnc43)CC2)s1 | nan | |||
CHEMBL3941049 | 148917 | None | 0 | Human | Binding | pIC50 | = | 7.8 | 7.8 | - | 0 | ChEMBL | 471 | 5 | 1 | 7 | 3.9 | CCc1nc(-c2nc3ccccc3[nH]2)c(N2CCN(C(=O)Cn3ccc4cccnc43)CC2)s1 | nan | |||
71679965 | 150234 | None | 0 | Human | Binding | pIC50 | = | 7.8 | 7.8 | - | 0 | ChEMBL | 442 | 4 | 1 | 6 | 4.0 | O=C(Cn1ccc2ccccc21)N1CCN(c2scnc2-c2nc3ccccc3[nH]2)CC1 | nan | |||
CHEMBL3951435 | 150234 | None | 0 | Human | Binding | pIC50 | = | 7.8 | 7.8 | - | 0 | ChEMBL | 442 | 4 | 1 | 6 | 4.0 | O=C(Cn1ccc2ccccc21)N1CCN(c2scnc2-c2nc3ccccc3[nH]2)CC1 | nan | |||
71679966 | 153304 | None | 0 | Human | Binding | pIC50 | = | 7.8 | 7.8 | - | 0 | ChEMBL | 473 | 4 | 1 | 8 | 2.7 | Cn1c(=O)n(CC(=O)N2CCN(c3scnc3-c3nc4ccccc4[nH]3)CC2)c2ccccc21 | nan | |||
CHEMBL3977272 | 153304 | None | 0 | Human | Binding | pIC50 | = | 7.8 | 7.8 | - | 0 | ChEMBL | 473 | 4 | 1 | 8 | 2.7 | Cn1c(=O)n(CC(=O)N2CCN(c3scnc3-c3nc4ccccc4[nH]3)CC2)c2ccccc21 | nan | |||
71679144 | 154064 | None | 0 | Human | Binding | pIC50 | = | 7.8 | 7.8 | - | 0 | ChEMBL | 510 | 4 | 1 | 6 | 5.3 | O=C(Cn1ccc2cc(Cl)c(Cl)cc21)N1CCN(c2scnc2-c2nc3ccccc3[nH]2)CC1 | nan | |||
CHEMBL3983801 | 154064 | None | 0 | Human | Binding | pIC50 | = | 7.8 | 7.8 | - | 0 | ChEMBL | 510 | 4 | 1 | 6 | 5.3 | O=C(Cn1ccc2cc(Cl)c(Cl)cc21)N1CCN(c2scnc2-c2nc3ccccc3[nH]2)CC1 | nan | |||
44592137 | 179284 | None | 5 | Human | Binding | pIC50 | = | 7.8 | 7.8 | - | 1 | ChEMBL | 503 | 7 | 1 | 5 | 4.7 | CCNC(=O)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4)CC3)[C@@H](CC)C2)c(Cl)c1 | 10.1021/acs.jmedchem.6b01309 | |||
CHEMBL472288 | 179284 | None | 5 | Human | Binding | pIC50 | = | 7.8 | 7.8 | - | 1 | ChEMBL | 503 | 7 | 1 | 5 | 4.7 | CCNC(=O)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4)CC3)[C@@H](CC)C2)c(Cl)c1 | 10.1021/acs.jmedchem.6b01309 | |||
44592137 | 179284 | None | 5 | Human | Binding | pIC50 | = | 7.8 | 7.8 | - | 1 | ChEMBL | 503 | 7 | 1 | 5 | 4.7 | CCNC(=O)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4)CC3)[C@@H](CC)C2)c(Cl)c1 | 10.1021/acs.jmedchem.6b01309 | |||
CHEMBL472288 | 179284 | None | 5 | Human | Binding | pIC50 | = | 7.8 | 7.8 | - | 1 | ChEMBL | 503 | 7 | 1 | 5 | 4.7 | CCNC(=O)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4)CC3)[C@@H](CC)C2)c(Cl)c1 | 10.1021/acs.jmedchem.6b01309 | |||
71586678 | 132371 | None | 0 | Human | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 552 | 10 | 1 | 5 | 5.6 | Cc1cc(CN(C[C@H]2CC[C@H](C(=O)O)CC2)C2CCc3cc(Cl)ccc32)ccc1OCCN1C(=O)CCC1=O | nan | |||
CHEMBL3697066 | 132371 | None | 0 | Human | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 552 | 10 | 1 | 5 | 5.6 | Cc1cc(CN(C[C@H]2CC[C@H](C(=O)O)CC2)C2CCc3cc(Cl)ccc32)ccc1OCCN1C(=O)CCC1=O | nan | |||
44453640 | 97988 | None | 0 | Mouse | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 524 | 9 | 1 | 6 | 5.3 | COc1ccccc1C(=O)N(C)CCCn1c(=N)n(CC(=O)c2ccc(Cl)cc2)c2cccc(Cl)c21 | 10.1016/j.bmcl.2008.02.049 | |||
CHEMBL272558 | 97988 | None | 0 | Mouse | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 524 | 9 | 1 | 6 | 5.3 | COc1ccccc1C(=O)N(C)CCCn1c(=N)n(CC(=O)c2ccc(Cl)cc2)c2cccc(Cl)c21 | 10.1016/j.bmcl.2008.02.049 | |||
17754758 | 97516 | None | 0 | Mouse | Binding | pIC50 | = | 5.8 | 5.8 | - | 0 | ChEMBL | 494 | 8 | 1 | 5 | 4.8 | CN(CCn1c(=N)n(CC(=O)c2ccc(Cl)cc2)c2cccc(Cl)c21)C(=O)Cc1ccccc1 | 10.1016/j.bmcl.2008.02.049 | |||
CHEMBL270166 | 97516 | None | 0 | Mouse | Binding | pIC50 | = | 5.8 | 5.8 | - | 0 | ChEMBL | 494 | 8 | 1 | 5 | 4.8 | CN(CCn1c(=N)n(CC(=O)c2ccc(Cl)cc2)c2cccc(Cl)c21)C(=O)Cc1ccccc1 | 10.1016/j.bmcl.2008.02.049 | |||
9913494 | 71506 | None | 0 | Human | Binding | pIC50 | = | 4.8 | 4.8 | - | 0 | ChEMBL | 490 | 14 | 0 | 5 | 6.0 | CCCCCCCCCC(=O)N(CCN(C)C)C(C)c1nc2ccccc2c(=O)n1-c1ccccc1 | 10.1016/j.bmcl.2005.03.070 | |||
CHEMBL196248 | 71506 | None | 0 | Human | Binding | pIC50 | = | 4.8 | 4.8 | - | 0 | ChEMBL | 490 | 14 | 0 | 5 | 6.0 | CCCCCCCCCC(=O)N(CCN(C)C)C(C)c1nc2ccccc2c(=O)n1-c1ccccc1 | 10.1016/j.bmcl.2005.03.070 | |||
89610337 | 132462 | None | 0 | Human | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 549 | 11 | 1 | 9 | 3.0 | COc1cc(CN(C(C)c2ccc3c(c2)CCO3)[C@H]2C[C@@H](C(=O)O)C2)ccc1OCCn1c(=O)ccn(C)c1=O | nan | |||
CHEMBL3697157 | 132462 | None | 0 | Human | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 549 | 11 | 1 | 9 | 3.0 | COc1cc(CN(C(C)c2ccc3c(c2)CCO3)[C@H]2C[C@@H](C(=O)O)C2)ccc1OCCn1c(=O)ccn(C)c1=O | nan | |||
90014377 | 148619 | None | 0 | Human | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 541 | 12 | 1 | 8 | 3.9 | COc1cc(CN(C2CCC2)C(CC(=O)O)c2ccc(Cl)cc2)ccc1OCCn1c(=O)ccn(C)c1=O | 10.1016/j.bmcl.2016.10.038 | |||
CHEMBL3938574 | 148619 | None | 0 | Human | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 541 | 12 | 1 | 8 | 3.9 | COc1cc(CN(C2CCC2)C(CC(=O)O)c2ccc(Cl)cc2)ccc1OCCn1c(=O)ccn(C)c1=O | 10.1016/j.bmcl.2016.10.038 | |||
124037258 | 148683 | None | 0 | Human | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 488 | 4 | 2 | 7 | 3.3 | C[C@@H]1CN(c2scnc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cc1ccc2c(c1)NC(=O)CO2 | nan | |||
CHEMBL3939129 | 148683 | None | 0 | Human | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 488 | 4 | 2 | 7 | 3.3 | C[C@@H]1CN(c2scnc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cc1ccc2c(c1)NC(=O)CO2 | nan | |||
90014377 | 148619 | None | 0 | Human | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 541 | 12 | 1 | 8 | 3.9 | COc1cc(CN(C2CCC2)C(CC(=O)O)c2ccc(Cl)cc2)ccc1OCCn1c(=O)ccn(C)c1=O | nan | |||
CHEMBL3938574 | 148619 | None | 0 | Human | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 541 | 12 | 1 | 8 | 3.9 | COc1cc(CN(C2CCC2)C(CC(=O)O)c2ccc(Cl)cc2)ccc1OCCn1c(=O)ccn(C)c1=O | nan | |||
89610528 | 132413 | None | 0 | Human | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 544 | 11 | 1 | 5 | 5.5 | C[C@@H](c1ccc(Cl)cc1)N(Cc1ccc(OCCN2C(=O)CCC2=O)c(F)c1)C[C@H]1CC[C@H](C(=O)O)CC1 | nan | |||
CHEMBL3697110 | 132413 | None | 0 | Human | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 544 | 11 | 1 | 5 | 5.5 | C[C@@H](c1ccc(Cl)cc1)N(Cc1ccc(OCCN2C(=O)CCC2=O)c(F)c1)C[C@H]1CC[C@H](C(=O)O)CC1 | nan | |||
71586006 | 132419 | None | 0 | Human | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 526 | 11 | 1 | 5 | 5.3 | C[C@@H](c1ccc(Cl)cc1)N(Cc1ccc(OCCN2C(=O)CCC2=O)cc1)C[C@H]1CC[C@H](C(=O)O)CC1 | nan | |||
CHEMBL3697116 | 132419 | None | 0 | Human | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 526 | 11 | 1 | 5 | 5.3 | C[C@@H](c1ccc(Cl)cc1)N(Cc1ccc(OCCN2C(=O)CCC2=O)cc1)C[C@H]1CC[C@H](C(=O)O)CC1 | nan | |||
89610553 | 132442 | None | 0 | Human | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 542 | 12 | 1 | 6 | 4.9 | COc1cc(CN(C[C@@H]2CC[C@H](C(=O)O)C2)[C@@H](C)c2ccc(Cl)cc2)ccc1OCCN1C(=O)CCC1=O | nan | |||
CHEMBL3697138 | 132442 | None | 0 | Human | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 542 | 12 | 1 | 6 | 4.9 | COc1cc(CN(C[C@@H]2CC[C@H](C(=O)O)C2)[C@@H](C)c2ccc(Cl)cc2)ccc1OCCN1C(=O)CCC1=O | nan | |||
44426676 | 86612 | None | 0 | Human | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 536 | 16 | 0 | 5 | 6.9 | CCCCCCCCCCCC(=O)N(CCN(C)C)[C@H](C)c1nc2ccccc2c(=O)n1-c1ccc(F)cc1 | 10.1016/j.bmcl.2007.03.106 | |||
CHEMBL231587 | 86612 | None | 0 | Human | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 536 | 16 | 0 | 5 | 6.9 | CCCCCCCCCCCC(=O)N(CCN(C)C)[C@H](C)c1nc2ccccc2c(=O)n1-c1ccc(F)cc1 | 10.1016/j.bmcl.2007.03.106 | |||
90014675 | 142461 | None | 0 | Human | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 537 | 13 | 1 | 9 | 3.0 | CCCN(Cc1ccc(OCCn2c(=O)ccn(C)c2=O)c(OC)c1)C(CC(=O)O)c1ccc2c(c1)CCO2 | 10.1016/j.bmcl.2016.10.038 | |||
CHEMBL3889529 | 142461 | None | 0 | Human | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 537 | 13 | 1 | 9 | 3.0 | CCCN(Cc1ccc(OCCn2c(=O)ccn(C)c2=O)c(OC)c1)C(CC(=O)O)c1ccc2c(c1)CCO2 | 10.1016/j.bmcl.2016.10.038 | |||
134137191 | 142829 | None | 0 | Human | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 438 | 9 | 0 | 6 | 3.4 | COc1cc(CN(C)[C@@H](C)c2ccc3c(c2)CCO3)ccc1OCCN1C(=O)CCC1=O | 10.1016/j.bmcl.2016.10.035 | |||
CHEMBL3892445 | 142829 | None | 0 | Human | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 438 | 9 | 0 | 6 | 3.4 | COc1cc(CN(C)[C@@H](C)c2ccc3c(c2)CCO3)ccc1OCCN1C(=O)CCC1=O | 10.1016/j.bmcl.2016.10.035 | |||
90014675 | 142461 | None | 0 | Human | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 537 | 13 | 1 | 9 | 3.0 | CCCN(Cc1ccc(OCCn2c(=O)ccn(C)c2=O)c(OC)c1)C(CC(=O)O)c1ccc2c(c1)CCO2 | nan | |||
CHEMBL3889529 | 142461 | None | 0 | Human | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 537 | 13 | 1 | 9 | 3.0 | CCCN(Cc1ccc(OCCn2c(=O)ccn(C)c2=O)c(OC)c1)C(CC(=O)O)c1ccc2c(c1)CCO2 | nan | |||
89610706 | 132438 | None | 0 | Human | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 586 | 11 | 1 | 6 | 5.4 | COc1cc(CN(C[C@H]2CC[C@H](C(=O)O)CC2)C2CCc3cc(Cl)c(F)cc32)ccc1OCCN1C(=O)CCC1=O | nan | |||
CHEMBL3697134 | 132438 | None | 0 | Human | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 586 | 11 | 1 | 6 | 5.4 | COc1cc(CN(C[C@H]2CC[C@H](C(=O)O)CC2)C2CCc3cc(Cl)c(F)cc32)ccc1OCCN1C(=O)CCC1=O | nan | |||
44426691 | 86014 | None | 0 | Human | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 556 | 9 | 0 | 6 | 5.1 | C[C@H](c1nc2ccccc2c(=O)n1-c1ccc(F)cc1)N(CCN(C)C)C(=O)Cc1ccc(OC(F)(F)F)cc1 | 10.1016/j.bmcl.2007.03.106 | |||
CHEMBL230344 | 86014 | None | 0 | Human | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 556 | 9 | 0 | 6 | 5.1 | C[C@H](c1nc2ccccc2c(=O)n1-c1ccc(F)cc1)N(CCN(C)C)C(=O)Cc1ccc(OC(F)(F)F)cc1 | 10.1016/j.bmcl.2007.03.106 | |||
71585501 | 132393 | None | 0 | Human | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 569 | 12 | 1 | 5 | 5.6 | COc1cc(CN(C[C@H]2CC[C@H](C(=O)O)CC2)[C@@H](C)c2ccc(Cl)cc2)ccc1CCCN1C(=O)CN(C)C1=O | nan | |||
CHEMBL3697088 | 132393 | None | 0 | Human | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 569 | 12 | 1 | 5 | 5.6 | COc1cc(CN(C[C@H]2CC[C@H](C(=O)O)CC2)[C@@H](C)c2ccc(Cl)cc2)ccc1CCCN1C(=O)CN(C)C1=O | nan | |||
90480414 | 190778 | None | 0 | Human | Binding | pIC50 | = | 5.8 | 5.8 | - | 0 | ChEMBL | 495 | 5 | 0 | 9 | 3.2 | COc1ccc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3nc(C)nc3C)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL5181702 | 190778 | None | 0 | Human | Binding | pIC50 | = | 5.8 | 5.8 | - | 0 | ChEMBL | 495 | 5 | 0 | 9 | 3.2 | COc1ccc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3nc(C)nc3C)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
168273430 | 190794 | None | 0 | Human | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 518 | 5 | 0 | 10 | 3.1 | COc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3cnc4cccnc43)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
CHEMBL5181928 | 190794 | None | 0 | Human | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 518 | 5 | 0 | 10 | 3.1 | COc1ncc(-c2nc(C(F)(F)F)sc2N2CCN(C(=O)Cn3cnc4cccnc43)[C@H](C)C2)cn1 | 10.1021/acs.jmedchem.2c00675 | |||
66599753 | 194315 | None | 0 | Human | Binding | pIC50 | = | 5.8 | 5.8 | - | 0 | ChEMBL | 374 | 4 | 0 | 4 | 3.5 | Cc1cc(C)n(CC(=O)N2CCN(c3ccccc3-c3ccccc3)CC2)n1 | 10.1021/acs.jmedchem.5b01337 | |||
CHEMBL5283420 | 194315 | None | 0 | Human | Binding | pIC50 | = | 5.8 | 5.8 | - | 0 | ChEMBL | 374 | 4 | 0 | 4 | 3.5 | Cc1cc(C)n(CC(=O)N2CCN(c3ccccc3-c3ccccc3)CC2)n1 | 10.1021/acs.jmedchem.5b01337 | |||
171343098 | 193670 | None | 0 | Human | Binding | pIC50 | = | 4.8 | 4.8 | - | 0 | ChEMBL | 819 | 24 | 9 | 15 | 1.9 | CC[C@H](C)C[C@H](C)C[C@H](C)[C@@H](O[C@@H]1O[C@H](COC(C)=O)[C@@H](O)[C@@H](O)[C@@H]1O)[C@@H](C)/C=C(\C)[C@@H](O)[C@@H](C)/C=C(\C)[C@@H](O)[C@@H](C)/C=C(\C)C(=O)OC[C@@H](O)[C@H](O)[C@H](O)CO | 10.1021/acs.jmedchem.5b01337 | |||
CHEMBL5268341 | 193670 | None | 0 | Human | Binding | pIC50 | = | 4.8 | 4.8 | - | 0 | ChEMBL | 819 | 24 | 9 | 15 | 1.9 | CC[C@H](C)C[C@H](C)C[C@H](C)[C@@H](O[C@@H]1O[C@H](COC(C)=O)[C@@H](O)[C@@H](O)[C@@H]1O)[C@@H](C)/C=C(\C)[C@@H](O)[C@@H](C)/C=C(\C)[C@@H](O)[C@@H](C)/C=C(\C)C(=O)OC[C@@H](O)[C@H](O)[C@H](O)CO | 10.1021/acs.jmedchem.5b01337 | |||
44453530 | 155443 | None | 0 | Human | Binding | pIC50 | = | 7.8 | 7.8 | - | 0 | ChEMBL | 571 | 6 | 1 | 6 | 6.2 | N=c1n(CC(=O)c2ccc(Cl)cc2)c2cccc(Cl)c2n1C[C@H]1CCCN(C(=O)c2cccc3cccnc23)C1 | 10.1016/j.bmcl.2008.02.049 | |||
CHEMBL403290 | 155443 | None | 0 | Human | Binding | pIC50 | = | 7.8 | 7.8 | - | 0 | ChEMBL | 571 | 6 | 1 | 6 | 6.2 | N=c1n(CC(=O)c2ccc(Cl)cc2)c2cccc(Cl)c2n1C[C@H]1CCCN(C(=O)c2cccc3cccnc23)C1 | 10.1016/j.bmcl.2008.02.049 | |||
45486526 | 200066 | None | 0 | Human | Binding | pIC50 | = | 7.8 | 7.8 | - | 0 | ChEMBL | 627 | 10 | 0 | 7 | 5.9 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(C(F)(F)F)c(F)c1)[C@H](C)c1nc2c(C3CC3)nccn2c1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2009.07.021 | |||
CHEMBL570665 | 200066 | None | 0 | Human | Binding | pIC50 | = | 7.8 | 7.8 | - | 0 | ChEMBL | 627 | 10 | 0 | 7 | 5.9 | CCS(=O)(=O)CCN(C(=O)Cc1ccc(C(F)(F)F)c(F)c1)[C@H](C)c1nc2c(C3CC3)nccn2c1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2009.07.021 | |||
45486533 | 200094 | None | 0 | Human | Binding | pIC50 | = | 7.8 | 7.8 | - | 0 | ChEMBL | 635 | 8 | 0 | 7 | 6.1 | C[C@H](c1nc2c(C3CC3)nccn2c1-c1ccc(C#N)cc1)N(CC1CCS(=O)(=O)CC1)C(=O)Cc1ccc(C(F)(F)F)cc1 | 10.1016/j.bmcl.2009.07.021 | |||
CHEMBL570858 | 200094 | None | 0 | Human | Binding | pIC50 | = | 7.8 | 7.8 | - | 0 | ChEMBL | 635 | 8 | 0 | 7 | 6.1 | C[C@H](c1nc2c(C3CC3)nccn2c1-c1ccc(C#N)cc1)N(CC1CCS(=O)(=O)CC1)C(=O)Cc1ccc(C(F)(F)F)cc1 | 10.1016/j.bmcl.2009.07.021 | |||
44455489 | 168905 | None | 0 | Human | Binding | pIC50 | = | 7.8 | 7.8 | - | 0 | ChEMBL | 604 | 11 | 0 | 6 | 5.9 | CCc1c(C2CC2)nc([C@@H](C)N(CCS(=O)(=O)CC)C(=O)Cc2ccc(F)c(C(F)(F)F)c2)n1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2007.11.072 | |||
CHEMBL437598 | 168905 | None | 0 | Human | Binding | pIC50 | = | 7.8 | 7.8 | - | 0 | ChEMBL | 604 | 11 | 0 | 6 | 5.9 | CCc1c(C2CC2)nc([C@@H](C)N(CCS(=O)(=O)CC)C(=O)Cc2ccc(F)c(C(F)(F)F)c2)n1-c1ccc(C#N)cc1 | 10.1016/j.bmcl.2007.11.072 | |||
56660102 | 64286 | None | 0 | Rat | Binding | pIC50 | = | 7.8 | 7.8 | - | 0 | ChEMBL | 537 | 5 | 1 | 4 | 5.2 | O=C([C@@H]1C=C2c3cccc4c3c(cn4CCN3CCCCC3)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CCCC1 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1809041 | 64286 | None | 0 | Rat | Binding | pIC50 | = | 7.8 | 7.8 | - | 0 | ChEMBL | 537 | 5 | 1 | 4 | 5.2 | O=C([C@@H]1C=C2c3cccc4c3c(cn4CCN3CCCCC3)C[C@H]2N(C(=O)Nc2ccccc2)C1)N1CCCC1 | 10.1016/j.bmcl.2011.06.070 | |||
124037256 | 142922 | None | 0 | Human | Binding | pIC50 | = | 7.8 | 7.8 | - | 0 | ChEMBL | 468 | 4 | 1 | 6 | 4.5 | C[C@@H]1CN(c2scnc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cc1ccc2cccnc2c1 | nan | |||
CHEMBL3893096 | 142922 | None | 0 | Human | Binding | pIC50 | = | 7.8 | 7.8 | - | 0 | ChEMBL | 468 | 4 | 1 | 6 | 4.5 | C[C@@H]1CN(c2scnc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cc1ccc2cccnc2c1 | nan | |||
89726114 | 145349 | None | 0 | Human | Binding | pIC50 | = | 7.8 | 7.8 | - | 0 | ChEMBL | 443 | 4 | 1 | 7 | 3.4 | O=C(Cn1ncc2ccccc21)N1CCN(c2scnc2-c2nc3ccccc3[nH]2)CC1 | nan | |||
CHEMBL3912870 | 145349 | None | 0 | Human | Binding | pIC50 | = | 7.8 | 7.8 | - | 0 | ChEMBL | 443 | 4 | 1 | 7 | 3.4 | O=C(Cn1ncc2ccccc21)N1CCN(c2scnc2-c2nc3ccccc3[nH]2)CC1 | nan | |||
89726091 | 147124 | None | 0 | Human | Binding | pIC50 | = | 7.8 | 7.8 | - | 0 | ChEMBL | 572 | 5 | 1 | 8 | 4.4 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cc(C2CCN(C)CC2)cn1 | nan | |||
CHEMBL3926820 | 147124 | None | 0 | Human | Binding | pIC50 | = | 7.8 | 7.8 | - | 0 | ChEMBL | 572 | 5 | 1 | 8 | 4.4 | C[C@@H]1CN(c2sc(C(F)(F)F)nc2-c2nc3ccccc3[nH]2)CCN1C(=O)Cn1cc(C2CCN(C)CC2)cn1 | nan | |||
89725837 | 148655 | None | 0 | Human | Binding | pIC50 | = | 7.8 | 7.8 | - | 0 | ChEMBL | 548 | 5 | 1 | 8 | 5.1 | Cc1cccc(-c2nc(-c3nc4ccccc4[nH]3)c(N3CCN(C(=O)Cn4cnc5cccnc54)[C@H](C)C3)s2)c1 | nan | |||
CHEMBL3938895 | 148655 | None | 0 | Human | Binding | pIC50 | = | 7.8 | 7.8 | - | 0 | ChEMBL | 548 | 5 | 1 | 8 | 5.1 | Cc1cccc(-c2nc(-c3nc4ccccc4[nH]3)c(N3CCN(C(=O)Cn4cnc5cccnc54)[C@H](C)C3)s2)c1 | nan | |||
71585504 | 132387 | None | 0 | Human | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 566 | 11 | 1 | 5 | 5.8 | COc1cc(CN(C[C@H]2CC[C@H](C(=O)O)CC2)[C@H]2CCc3cc(Cl)ccc32)ccc1CCCN1C(=O)CCC1=O | nan | |||
CHEMBL3697082 | 132387 | None | 0 | Human | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 566 | 11 | 1 | 5 | 5.8 | COc1cc(CN(C[C@H]2CC[C@H](C(=O)O)CC2)[C@H]2CCc3cc(Cl)ccc32)ccc1CCCN1C(=O)CCC1=O | nan | |||
71586396 | 132457 | None | 0 | Human | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 571 | 13 | 1 | 6 | 4.9 | CCC(c1ccc(Cl)cc1)N(Cc1ccc(OCCN2C(=O)CN(C)C2=O)c(OC)c1)C[C@H]1[C@H](C(=O)O)C1(C)C | nan | |||
CHEMBL3697152 | 132457 | None | 0 | Human | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 571 | 13 | 1 | 6 | 4.9 | CCC(c1ccc(Cl)cc1)N(Cc1ccc(OCCN2C(=O)CN(C)C2=O)c(OC)c1)C[C@H]1[C@H](C(=O)O)C1(C)C | nan | |||
134145500 | 149272 | None | 0 | Human | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 572 | 13 | 1 | 7 | 5.0 | CCC(c1ccc2c(c1)CCO2)N(Cc1ccc(C(=O)O)cc1)Cc1ccc(OCCN2C(=O)CCC2=O)c(OC)c1 | 10.1016/j.bmcl.2016.10.035 | |||
CHEMBL3943746 | 149272 | None | 0 | Human | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 572 | 13 | 1 | 7 | 5.0 | CCC(c1ccc2c(c1)CCO2)N(Cc1ccc(C(=O)O)cc1)Cc1ccc(OCCN2C(=O)CCC2=O)c(OC)c1 | 10.1016/j.bmcl.2016.10.035 | |||
56673941 | 64274 | None | 0 | Human | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 418 | 2 | 2 | 2 | 3.7 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)NC2CCCC2)C1)N1CCCC1 | 10.1016/j.bmcl.2011.06.070 | |||
CHEMBL1809027 | 64274 | None | 0 | Human | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 418 | 2 | 2 | 2 | 3.7 | O=C([C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)NC2CCCC2)C1)N1CCCC1 | 10.1016/j.bmcl.2011.06.070 | |||
44454527 | 95403 | None | 0 | Human | Binding | pIC50 | = | 4.8 | 4.8 | - | 0 | ChEMBL | 299 | 3 | 1 | 4 | 3.0 | Cn1c(=N)n(CC(=O)c2cccc(Cl)c2)c2ccccc21 | 10.1016/j.bmcl.2008.01.074 | |||
CHEMBL256660 | 95403 | None | 0 | Human | Binding | pIC50 | = | 4.8 | 4.8 | - | 0 | ChEMBL | 299 | 3 | 1 | 4 | 3.0 | Cn1c(=N)n(CC(=O)c2cccc(Cl)c2)c2ccccc21 | 10.1016/j.bmcl.2008.01.074 | |||
121485695 | 194561 | None | 0 | Human | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 564 | 6 | 1 | 10 | 3.1 | CC(C)c1ncn(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3cnc(C(F)(F)F)nc3)C[C@@H]2CO)n1 | 10.1021/acs.jmedchem.3c00074 | |||
CHEMBL5289006 | 194561 | None | 0 | Human | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 564 | 6 | 1 | 10 | 3.1 | CC(C)c1ncn(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3cnc(C(F)(F)F)nc3)C[C@@H]2CO)n1 | 10.1021/acs.jmedchem.3c00074 | |||
121485701 | 276 | None | 10 | Mouse | Binding | pIC50 | = | 6.8 | 6.8 | - | 1 | ChEMBL | 550 | 6 | 1 | 10 | 2.6 | CC1=NN(C=N1)CC(=O)N2CCN(C[C@H]2CCO)C3=C(N=C(S3)C(F)(F)F)C4=CN=C(N=C4)C(F)(F)F | 10.1021/acs.jmedchem.3c00074 | |||
12584 | 276 | None | 10 | Mouse | Binding | pIC50 | = | 6.8 | 6.8 | - | 1 |