Ligand source activities (1 row/activity)



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Ligands (move mouse cursor over ligand name to see structure) Receptor Activity Chemical information
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name		 GPCRdb
ID		 Reference
ligand		 Vendors

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 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
367 3824 None 10 Human Functional pAC50 = 9.5 9.5 -1 8
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1038/s41467-023-40064-9
5487427 3824 None 10 Human Functional pAC50 = 9.5 9.5 -1 8
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1038/s41467-023-40064-9
5487427.0 3824 None 10 Human Functional pAC50 = 9.5 9.5 -1 8
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1038/s41467-023-40064-9
8592 3824 None 10 Human Functional pAC50 = 9.5 9.5 -1 8
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1038/s41467-023-40064-9
CHEMBL1900528 3824 None 10 Human Functional pAC50 = 9.5 9.5 -1 8
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1038/s41467-023-40064-9
CHEMBL3305968 3824 None 10 Human Functional pAC50 = 9.5 9.5 -1 8
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1038/s41467-023-40064-9
CHEMBL4650755 3824 None 10 Human Functional pAC50 = 9.5 9.5 -1 8
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1038/s41467-023-40064-9
DB01409 3824 None 10 Human Functional pAC50 = 9.5 9.5 -1 8
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1038/s41467-023-40064-9
656603 194645 None 3 Human Functional pAC50 = 9.3 9.3 1 5
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 398 6 1 3 3.6 C[N@+]1(CCF)[C@@H]2CC[C@H]1C[C@@H](OC(=O)C(O)(c1ccccc1)c1ccccc1)C2 10.1038/s41467-023-40064-9
CHEMBL5292015 194645 None 3 Human Functional pAC50 = 9.3 9.3 1 5
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 398 6 1 3 3.6 C[N@+]1(CCF)[C@@H]2CC[C@H]1C[C@@H](OC(=O)C(O)(c1ccccc1)c1ccccc1)C2 10.1038/s41467-023-40064-9
367 3824 None 10 Human Functional pAC50 = 9.1 9.1 -1 8
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1038/s41467-023-40064-9
5487427 3824 None 10 Human Functional pAC50 = 9.1 9.1 -1 8
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1038/s41467-023-40064-9
5487427.0 3824 None 10 Human Functional pAC50 = 9.1 9.1 -1 8
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1038/s41467-023-40064-9
8592 3824 None 10 Human Functional pAC50 = 9.1 9.1 -1 8
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1038/s41467-023-40064-9
CHEMBL1900528 3824 None 10 Human Functional pAC50 = 9.1 9.1 -1 8
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1038/s41467-023-40064-9
CHEMBL3305968 3824 None 10 Human Functional pAC50 = 9.1 9.1 -1 8
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1038/s41467-023-40064-9
CHEMBL4650755 3824 None 10 Human Functional pAC50 = 9.1 9.1 -1 8
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1038/s41467-023-40064-9
DB01409 3824 None 10 Human Functional pAC50 = 9.1 9.1 -1 8
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 392 4 1 6 2.3 O=C(C(c1cccs1)(c1cccs1)O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1038/s41467-023-40064-9
1201549 597 None 17 Human Functional pAC50 = 9.0 9.0 -1 26
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
1201549.0 597 None 17 Human Functional pAC50 = 9.0 9.0 -1 26
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
333 597 None 17 Human Functional pAC50 = 9.0 9.0 -1 26
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
7601 597 None 17 Human Functional pAC50 = 9.0 9.0 -1 26
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL1201203 597 None 17 Human Functional pAC50 = 9.0 9.0 -1 26
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL438151 597 None 17 Human Functional pAC50 = 9.0 9.0 -1 26
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
DB00245 597 None 17 Human Functional pAC50 = 9.0 9.0 -1 26
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
3000322 3562 None 29 Human Functional pAC50 = 8.8 8.8 -1 4
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 303 4 1 5 0.9 OC[C@H](c1ccccc1)C(=O)O[C@@H]1C[C@H]2N([C@@H](C1)[C@H]1[C@@H]2O1)C 10.1038/s41467-023-40064-9
3000322.0 3562 None 29 Human Functional pAC50 = 8.8 8.8 -1 4
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 303 4 1 5 0.9 OC[C@H](c1ccccc1)C(=O)O[C@@H]1C[C@H]2N([C@@H](C1)[C@H]1[C@@H]2O1)C 10.1038/s41467-023-40064-9
330 3562 None 29 Human Functional pAC50 = 8.8 8.8 -1 4
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 303 4 1 5 0.9 OC[C@H](c1ccccc1)C(=O)O[C@@H]1C[C@H]2N([C@@H](C1)[C@H]1[C@@H]2O1)C 10.1038/s41467-023-40064-9
CHEMBL569713 3562 None 29 Human Functional pAC50 = 8.8 8.8 -1 4
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 303 4 1 5 0.9 OC[C@H](c1ccccc1)C(=O)O[C@@H]1C[C@H]2N([C@@H](C1)[C@H]1[C@@H]2O1)C 10.1038/s41467-023-40064-9
DB00747 3562 None 29 Human Functional pAC50 = 8.8 8.8 -1 4
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 303 4 1 5 0.9 OC[C@H](c1ccccc1)C(=O)O[C@@H]1C[C@H]2N([C@@H](C1)[C@H]1[C@@H]2O1)C 10.1038/s41467-023-40064-9
3000322 3562 None 29 Human Functional pAC50 = 8.8 8.8 -1 4
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 303 4 1 5 0.9 OC[C@H](c1ccccc1)C(=O)O[C@@H]1C[C@H]2N([C@@H](C1)[C@H]1[C@@H]2O1)C 10.1038/s41467-023-40064-9
3000322.0 3562 None 29 Human Functional pAC50 = 8.8 8.8 -1 4
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 303 4 1 5 0.9 OC[C@H](c1ccccc1)C(=O)O[C@@H]1C[C@H]2N([C@@H](C1)[C@H]1[C@@H]2O1)C 10.1038/s41467-023-40064-9
330 3562 None 29 Human Functional pAC50 = 8.8 8.8 -1 4
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 303 4 1 5 0.9 OC[C@H](c1ccccc1)C(=O)O[C@@H]1C[C@H]2N([C@@H](C1)[C@H]1[C@@H]2O1)C 10.1038/s41467-023-40064-9
CHEMBL569713 3562 None 29 Human Functional pAC50 = 8.8 8.8 -1 4
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 303 4 1 5 0.9 OC[C@H](c1ccccc1)C(=O)O[C@@H]1C[C@H]2N([C@@H](C1)[C@H]1[C@@H]2O1)C 10.1038/s41467-023-40064-9
DB00747 3562 None 29 Human Functional pAC50 = 8.8 8.8 -1 4
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 303 4 1 5 0.9 OC[C@H](c1ccccc1)C(=O)O[C@@H]1C[C@H]2N([C@@H](C1)[C@H]1[C@@H]2O1)C 10.1038/s41467-023-40064-9
4167 14506 None 28 Human Functional pAC50 = 8.0 8.0 -2 10
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 309 2 0 2 5.0 CN1CCCC(CC2c3ccccc3Sc3ccccc32)C1 10.1038/s41467-023-40064-9
4167.0 14506 None 28 Human Functional pAC50 = 8.0 8.0 -2 10
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 309 2 0 2 5.0 CN1CCCC(CC2c3ccccc3Sc3ccccc32)C1 10.1038/s41467-023-40064-9
CHEMBL1201342 14506 None 28 Human Functional pAC50 = 8.0 8.0 -2 10
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 309 2 0 2 5.0 CN1CCCC(CC2c3ccccc3Sc3ccccc32)C1 10.1038/s41467-023-40064-9
DB00340 14506 None 28 Human Functional pAC50 = 8.0 8.0 -2 10
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 309 2 0 2 5.0 CN1CCCC(CC2c3ccccc3Sc3ccccc32)C1 10.1038/s41467-023-40064-9
5022 1651 None 58 Human Functional pAC50 = 5 5.0 -229 9
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 390 4 1 4 3.2 O=c1[nH]c2c(n1CCN1CCN(CC1)c1cccc(c1)C(F)(F)F)cccc2 10.1038/s41467-023-40064-9
6918248 1651 None 58 Human Functional pAC50 = 5 5.0 -229 9
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 390 4 1 4 3.2 O=c1[nH]c2c(n1CCN1CCN(CC1)c1cccc(c1)C(F)(F)F)cccc2 10.1038/s41467-023-40064-9
6918248.0 1651 None 58 Human Functional pAC50 = 5 5.0 -229 9
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 390 4 1 4 3.2 O=c1[nH]c2c(n1CCN1CCN(CC1)c1cccc(c1)C(F)(F)F)cccc2 10.1038/s41467-023-40064-9
8182 1651 None 58 Human Functional pAC50 = 5 5.0 -229 9
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 390 4 1 4 3.2 O=c1[nH]c2c(n1CCN1CCN(CC1)c1cccc(c1)C(F)(F)F)cccc2 10.1038/s41467-023-40064-9
CHEMBL231068 1651 None 58 Human Functional pAC50 = 5 5.0 -229 9
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 390 4 1 4 3.2 O=c1[nH]c2c(n1CCN1CCN(CC1)c1cccc(c1)C(F)(F)F)cccc2 10.1038/s41467-023-40064-9
DB04908 1651 None 58 Human Functional pAC50 = 5 5.0 -229 9
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 390 4 1 4 3.2 O=c1[nH]c2c(n1CCN1CCN(CC1)c1cccc(c1)C(F)(F)F)cccc2 10.1038/s41467-023-40064-9
5330286 67592 None 57 Human Functional pAC50 = 5.0 5.0 -1 8
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 447 5 2 9 3.0 CC(=O)c1c(C)c2cnc(Nc3ccc(N4CCNCC4)cn3)nc2n(C2CCCC2)c1=O 10.1038/s41467-023-40064-9
CHEMBL189963 67592 None 57 Human Functional pAC50 = 5.0 5.0 -1 8
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 447 5 2 9 3.0 CC(=O)c1c(C)c2cnc(Nc3ccc(N4CCNCC4)cn3)nc2n(C2CCCC2)c1=O 10.1038/s41467-023-40064-9
37907 35407 None 55 Human Functional pAC50 = 5.0 5.0 1 3
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 292 4 0 4 3.7 CC(C)(C)C(=O)C(Oc1ccc(Cl)cc1)n1ccnc1 10.1038/s41467-023-40064-9
CHEMBL1437764 35407 None 55 Human Functional pAC50 = 5.0 5.0 1 3
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 292 4 0 4 3.7 CC(C)(C)C(=O)C(Oc1ccc(Cl)cc1)n1ccnc1 10.1038/s41467-023-40064-9
115368 3056 None 34 Human Functional pAC50 = 5.0 5.0 -3388 9
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 426 6 0 6 3.4 O=C1N(CCCCN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1CCCC2 10.1038/s41467-023-40064-9
2112 3056 None 34 Human Functional pAC50 = 5.0 5.0 -3388 9
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 426 6 0 6 3.4 O=C1N(CCCCN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1CCCC2 10.1038/s41467-023-40064-9
7556 3056 None 34 Human Functional pAC50 = 5.0 5.0 -3388 9
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 426 6 0 6 3.4 O=C1N(CCCCN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1CCCC2 10.1038/s41467-023-40064-9
CHEMBL1472975 3056 None 34 Human Functional pAC50 = 5.0 5.0 -3388 9
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 426 6 0 6 3.4 O=C1N(CCCCN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1CCCC2 10.1038/s41467-023-40064-9
DB08922 3056 None 34 Human Functional pAC50 = 5.0 5.0 -3388 9
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 426 6 0 6 3.4 O=C1N(CCCCN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1CCCC2 10.1038/s41467-023-40064-9
98941 46964 None 13 Human Functional pAC50 = 5.0 5.0 -51 11
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 457 7 0 4 6.3 COc1ccc2c(c1)OC(C)(C)C(c1ccccc1)C2c1ccc(OCCN2CCCC2)cc1 10.1038/s41467-023-40064-9
CHEMBL154126 46964 None 13 Human Functional pAC50 = 5.0 5.0 -51 11
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 457 7 0 4 6.3 COc1ccc2c(c1)OC(C)(C)C(c1ccccc1)C2c1ccc(OCCN2CCCC2)cc1 10.1038/s41467-023-40064-9
28061 36766 None 65 Human Functional pAC50 = 5.0 5.0 - 1
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 219 4 1 5 0.7 Cc1ncc([N+](=O)[O-])n1CC(O)CCl 10.1038/s41467-023-40064-9
CHEMBL1449676 36766 None 65 Human Functional pAC50 = 5.0 5.0 - 1
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 219 4 1 5 0.7 Cc1ncc([N+](=O)[O-])n1CC(O)CCl 10.1038/s41467-023-40064-9
456199 85594 None 52 Human Functional pAC50 = 5.0 5.0 - 1
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 359 5 0 7 2.7 O=[N+]([O-])c1cn2c(n1)OC[C@@H](OCc1ccc(OC(F)(F)F)cc1)C2 10.1038/s41467-023-40064-9
CHEMBL227875 85594 None 52 Human Functional pAC50 = 5.0 5.0 - 1
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 359 5 0 7 2.7 O=[N+]([O-])c1cn2c(n1)OC[C@@H](OCc1ccc(OC(F)(F)F)cc1)C2 10.1038/s41467-023-40064-9
54260 186945 None 28 Human Functional pAC50 = 5.0 5.0 1 3
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 317 6 0 2 4.7 CCC(C)(C)c1ccc(CC(C)CN2C[C@@H](C)O[C@@H](C)C2)cc1 10.1038/s41467-023-40064-9
CHEMBL489411 186945 None 28 Human Functional pAC50 = 5.0 5.0 1 3
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 317 6 0 2 4.7 CCC(C)(C)c1ccc(CC(C)CN2C[C@@H](C)O[C@@H](C)C2)cc1 10.1038/s41467-023-40064-9
12488 1657 None 39 Human Functional pAC50 = 5.0 5.0 -144 28
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F 10.1038/s41467-023-40064-9
941361 1657 None 39 Human Functional pAC50 = 5.0 5.0 -144 28
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F 10.1038/s41467-023-40064-9
CHEMBL30008 1657 None 39 Human Functional pAC50 = 5.0 5.0 -144 28
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F 10.1038/s41467-023-40064-9
DB04841 1657 None 39 Human Functional pAC50 = 5.0 5.0 -144 28
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F 10.1038/s41467-023-40064-9
54454 5260 None 48 Human Functional pAC50 = 5.0 5.0 -4 14
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 418 6 1 5 4.6 CCC(C)(C)C(=O)O[C@H]1C[C@@H](C)C=C2C=C[C@H](C)[C@H](CC[C@@H]3C[C@@H](O)CC(=O)O3)[C@H]21 10.1038/s41467-023-40064-9
CHEMBL1064 5260 None 48 Human Functional pAC50 = 5.0 5.0 -4 14
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 418 6 1 5 4.6 CCC(C)(C)C(=O)O[C@H]1C[C@@H](C)C=C2C=C[C@H](C)[C@H](CC[C@@H]3C[C@@H](O)CC(=O)O3)[C@H]21 10.1038/s41467-023-40064-9
5523 3851 None 17 Human Functional pAC50 = 5.0 5.0 -7 3
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 263 4 1 3 2.6 COc1cccc(c1)C1(O)CCCCC1CN(C)C 10.1038/s41467-023-40064-9
5523.0 3851 None 17 Human Functional pAC50 = 5.0 5.0 -7 3
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 263 4 1 3 2.6 COc1cccc(c1)C1(O)CCCCC1CN(C)C 10.1038/s41467-023-40064-9
8286 3851 None 17 Human Functional pAC50 = 5.0 5.0 -7 3
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 263 4 1 3 2.6 COc1cccc(c1)C1(O)CCCCC1CN(C)C 10.1038/s41467-023-40064-9
CHEMBL1237044 3851 None 17 Human Functional pAC50 = 5.0 5.0 -7 3
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 263 4 1 3 2.6 COc1cccc(c1)C1(O)CCCCC1CN(C)C 10.1038/s41467-023-40064-9
DB00193 3851 None 17 Human Functional pAC50 = 5.0 5.0 -7 3
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 263 4 1 3 2.6 COc1cccc(c1)C1(O)CCCCC1CN(C)C 10.1038/s41467-023-40064-9
11511120 78425 None 58 Human Functional pAC50 = 5.0 5.0 -1 5
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 469 7 2 6 5.2 COc1cc2ncnc(Nc3ccc(F)c(Cl)c3)c2cc1NC(=O)/C=C/CN1CCCCC1 10.1038/s41467-023-40064-9
CHEMBL2110732 78425 None 58 Human Functional pAC50 = 5.0 5.0 -1 5
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 469 7 2 6 5.2 COc1cc2ncnc(Nc3ccc(F)c(Cl)c3)c2cc1NC(=O)/C=C/CN1CCCCC1 10.1038/s41467-023-40064-9
3081361 93987 None 66 Human Functional pAC50 = 5.0 5.0 -17 14
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 474 5 1 5 4.4 COc1cc2/c(=N/c3ccc(Br)cc3F)nc[nH]c2cc1OCC1CCN(C)CC1 10.1038/s41467-023-40064-9
CHEMBL24828 93987 None 66 Human Functional pAC50 = 5.0 5.0 -17 14
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 474 5 1 5 4.4 COc1cc2/c(=N/c3ccc(Br)cc3F)nc[nH]c2cc1OCC1CCN(C)CC1 10.1038/s41467-023-40064-9
20628 96601 None 25 Human Functional pAC50 = 5.0 5.0 -28 13
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 324 6 1 5 3.7 CN(C)CCCNc1c2ccccc2nc2cccc([N+](=O)[O-])c12 10.1038/s41467-023-40064-9
CHEMBL26291 96601 None 25 Human Functional pAC50 = 5.0 5.0 -28 13
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 324 6 1 5 3.7 CN(C)CCCNc1c2ccccc2nc2cccc([N+](=O)[O-])c12 10.1038/s41467-023-40064-9
216416 111644 None 40 Human Functional pAC50 = 5.0 5.0 -128 23
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 413 6 1 3 5.7 Oc1ccc2c(c1)CC[C@H](c1ccccc1)[C@@H]2c1ccc(OCCN2CCCC2)cc1 10.1038/s41467-023-40064-9
CHEMBL328190 111644 None 40 Human Functional pAC50 = 5.0 5.0 -128 23
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 413 6 1 3 5.7 Oc1ccc2c(c1)CC[C@H](c1ccccc1)[C@@H]2c1ccc(OCCN2CCCC2)cc1 10.1038/s41467-023-40064-9
2165 206241 None 47 Human Functional pAC50 = 5.0 5.0 -7 8
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 355 6 2 4 5.2 CCN(CC)Cc1cc(Nc2ccnc3cc(Cl)ccc23)ccc1O 10.1038/s41467-023-40064-9
3647519 206241 None 47 Human Functional pAC50 = 5.0 5.0 -7 8
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 355 6 2 4 5.2 CCN(CC)Cc1cc(Nc2ccnc3cc(Cl)ccc23)ccc1O 10.1038/s41467-023-40064-9
CHEMBL682 206241 None 47 Human Functional pAC50 = 5.0 5.0 -7 8
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 355 6 2 4 5.2 CCN(CC)Cc1cc(Nc2ccnc3cc(Cl)ccc23)ccc1O 10.1038/s41467-023-40064-9
10102 2546 None 55 Human Functional pAC50 = 8.0 8.0 4 4
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 432 5 1 6 3.4 Fc1ccc(cc1)Cn1c(nc2c1cccc2)N1CCC(CC1)N(c1nccc(=O)[nH]1)C 10.1038/s41467-023-40064-9
1824 2546 None 55 Human Functional pAC50 = 8.0 8.0 4 4
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 432 5 1 6 3.4 Fc1ccc(cc1)Cn1c(nc2c1cccc2)N1CCC(CC1)N(c1nccc(=O)[nH]1)C 10.1038/s41467-023-40064-9
65906 2546 None 55 Human Functional pAC50 = 8.0 8.0 4 4
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 432 5 1 6 3.4 Fc1ccc(cc1)Cn1c(nc2c1cccc2)N1CCC(CC1)N(c1nccc(=O)[nH]1)C 10.1038/s41467-023-40064-9
65906.0 2546 None 55 Human Functional pAC50 = 8.0 8.0 4 4
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 432 5 1 6 3.4 Fc1ccc(cc1)Cn1c(nc2c1cccc2)N1CCC(CC1)N(c1nccc(=O)[nH]1)C 10.1038/s41467-023-40064-9
CHEMBL94454 2546 None 55 Human Functional pAC50 = 8.0 8.0 4 4
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 432 5 1 6 3.4 Fc1ccc(cc1)Cn1c(nc2c1cccc2)N1CCC(CC1)N(c1nccc(=O)[nH]1)C 10.1038/s41467-023-40064-9
DB12523 2546 None 55 Human Functional pAC50 = 8.0 8.0 4 4
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 432 5 1 6 3.4 Fc1ccc(cc1)Cn1c(nc2c1cccc2)N1CCC(CC1)N(c1nccc(=O)[nH]1)C 10.1038/s41467-023-40064-9
19861 209982 None 33 Human Functional pAC50 = 7.0 7.0 -5 10
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 290 0 0 2 3.7 CN1CCC(=C2c3ccccc3CCc3cccnc32)CC1 10.1038/s41467-023-40064-9
19861.0 209982 None 33 Human Functional pAC50 = 7.0 7.0 -5 10
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 290 0 0 2 3.7 CN1CCC(=C2c3ccccc3CCc3cccnc32)CC1 10.1038/s41467-023-40064-9
CHEMBL946 209982 None 33 Human Functional pAC50 = 7.0 7.0 -5 10
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 290 0 0 2 3.7 CN1CCC(=C2c3ccccc3CCc3cccnc32)CC1 10.1038/s41467-023-40064-9
DB00719 209982 None 33 Human Functional pAC50 = 7.0 7.0 -5 10
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 290 0 0 2 3.7 CN1CCC(=C2c3ccccc3CCc3cccnc32)CC1 10.1038/s41467-023-40064-9
4031 99367 None 27 Human Functional pAC50 = 6.0 6.0 -1 13
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 429 13 0 6 4.6 CCN(CCCCOC(=O)c1ccc(OC)c(OC)c1)C(C)Cc1ccc(OC)cc1 10.1038/s41467-023-40064-9
CHEMBL282121 99367 None 27 Human Functional pAC50 = 6.0 6.0 -1 13
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 429 13 0 6 4.6 CCN(CCCCOC(=O)c1ccc(OC)c(OC)c1)C(C)Cc1ccc(OC)cc1 10.1038/s41467-023-40064-9
9822750 78440 None 44 Human Functional pAC50 = 5.0 5.0 -2 8
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 408 8 2 7 2.3 CCOC(=O)C1=C(COCCN)NC(C)=C(C(=O)OC)[C@@H]1c1ccccc1Cl 10.1038/s41467-023-40064-9
CHEMBL2111097 78440 None 44 Human Functional pAC50 = 5.0 5.0 -2 8
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 408 8 2 7 2.3 CCOC(=O)C1=C(COCCN)NC(C)=C(C(=O)OC)[C@@H]1c1ccccc1Cl 10.1038/s41467-023-40064-9
216237 3843 None 51 Human Functional pAC50 = 5.0 5.0 -1584 11
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 10.1038/s41467-023-40064-9
216237.0 3843 None 51 Human Functional pAC50 = 5.0 5.0 -1584 11
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 10.1038/s41467-023-40064-9
2226 3843 None 51 Human Functional pAC50 = 5.0 5.0 -1584 11
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 10.1038/s41467-023-40064-9
4110 3843 None 51 Human Functional pAC50 = 5.0 5.0 -1584 11
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 10.1038/s41467-023-40064-9
443894 3843 None 51 Human Functional pAC50 = 5.0 5.0 -1584 11
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 10.1038/s41467-023-40064-9
443894.0 3843 None 51 Human Functional pAC50 = 5.0 5.0 -1584 11
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 10.1038/s41467-023-40064-9
CHEMBL344159 3843 None 51 Human Functional pAC50 = 5.0 5.0 -1584 11
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 10.1038/s41467-023-40064-9
DB06212 3843 None 51 Human Functional pAC50 = 5.0 5.0 -1584 11
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 10.1038/s41467-023-40064-9
6324616 168927 None 18 Human Functional pAC50 = 4.9 4.9 -1 3
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 697 2 6 12 4.8 CO[C@H]1/C=C/O[C@@]2(C)Oc3c(C)c(O)c4c(O)c(cc(O)c4c3C2=O)NC(=O)/C(C)=C\C=C\[C@H](C)[C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@H](OC(C)=O)[C@@H]1C 10.1038/s41467-023-40064-9
CHEMBL437765 168927 None 18 Human Functional pAC50 = 4.9 4.9 -1 3
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 697 2 6 12 4.8 CO[C@H]1/C=C/O[C@@]2(C)Oc3c(C)c(O)c4c(O)c(cc(O)c4c3C2=O)NC(=O)/C(C)=C\C=C\[C@H](C)[C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@H](OC(C)=O)[C@@H]1C 10.1038/s41467-023-40064-9
119607 208661 None 64 Human Functional pAC50 = 4.9 4.9 -1 6
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 314 3 1 4 3.0 Cc1onc(-c2ccccc2)c1-c1ccc(S(N)(=O)=O)cc1 10.1038/s41467-023-40064-9
CHEMBL865 208661 None 64 Human Functional pAC50 = 4.9 4.9 -1 6
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 314 3 1 4 3.0 Cc1onc(-c2ccccc2)c1-c1ccc(S(N)(=O)=O)cc1 10.1038/s41467-023-40064-9
1209 1658 None 52 Human Functional pAC50 = 4.9 4.9 -51 25
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 10.1038/s41467-023-40064-9
203 1658 None 52 Human Functional pAC50 = 4.9 4.9 -51 25
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 10.1038/s41467-023-40064-9
3386 1658 None 52 Human Functional pAC50 = 4.9 4.9 -51 25
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 10.1038/s41467-023-40064-9
CHEMBL41 1658 None 52 Human Functional pAC50 = 4.9 4.9 -51 25
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 10.1038/s41467-023-40064-9
DB00472 1658 None 52 Human Functional pAC50 = 4.9 4.9 -51 25
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 10.1038/s41467-023-40064-9
3627 44143 None 12 Human Functional pAC50 = 6.9 6.9 -1 9
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 314 3 0 2 4.1 CN1CCCN(C(c2ccccc2)c2ccc(Cl)cc2)CC1 10.1038/s41467-023-40064-9
CHEMBL1515447 44143 None 12 Human Functional pAC50 = 6.9 6.9 -1 9
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 314 3 0 2 4.1 CN1CCCN(C(c2ccccc2)c2ccc(Cl)cc2)CC1 10.1038/s41467-023-40064-9
3000322 3562 None 29 Human Functional pAC50 = 7.9 7.9 -1 4
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 303 4 1 5 0.9 OC[C@H](c1ccccc1)C(=O)O[C@@H]1C[C@H]2N([C@@H](C1)[C@H]1[C@@H]2O1)C 10.1038/s41467-023-40064-9
3000322.0 3562 None 29 Human Functional pAC50 = 7.9 7.9 -1 4
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 303 4 1 5 0.9 OC[C@H](c1ccccc1)C(=O)O[C@@H]1C[C@H]2N([C@@H](C1)[C@H]1[C@@H]2O1)C 10.1038/s41467-023-40064-9
330 3562 None 29 Human Functional pAC50 = 7.9 7.9 -1 4
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 303 4 1 5 0.9 OC[C@H](c1ccccc1)C(=O)O[C@@H]1C[C@H]2N([C@@H](C1)[C@H]1[C@@H]2O1)C 10.1038/s41467-023-40064-9
CHEMBL569713 3562 None 29 Human Functional pAC50 = 7.9 7.9 -1 4
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 303 4 1 5 0.9 OC[C@H](c1ccccc1)C(=O)O[C@@H]1C[C@H]2N([C@@H](C1)[C@H]1[C@@H]2O1)C 10.1038/s41467-023-40064-9
DB00747 3562 None 29 Human Functional pAC50 = 7.9 7.9 -1 4
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 303 4 1 5 0.9 OC[C@H](c1ccccc1)C(=O)O[C@@H]1C[C@H]2N([C@@H](C1)[C@H]1[C@@H]2O1)C 10.1038/s41467-023-40064-9
11976 920 None 44 Human Functional pAC50 = 6.9 6.9 -39 16
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl 10.1038/s41467-023-40064-9
667467 920 None 44 Human Functional pAC50 = 6.9 6.9 -39 16
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl 10.1038/s41467-023-40064-9
667467.0 920 None 44 Human Functional pAC50 = 6.9 6.9 -39 16
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl 10.1038/s41467-023-40064-9
CHEMBL908 920 None 44 Human Functional pAC50 = 6.9 6.9 -39 16
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl 10.1038/s41467-023-40064-9
DB01239 920 None 44 Human Functional pAC50 = 6.9 6.9 -39 16
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl 10.1038/s41467-023-40064-9
6127 14505 None 4 Human Functional pAC50 = 6.9 6.9 -1 6
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 278 2 0 0 4.4 C[N+]1(C)CCC(=C(c2ccccc2)c2ccccc2)CC1 10.1038/s41467-023-40064-9
6127.0 14505 None 4 Human Functional pAC50 = 6.9 6.9 -1 6
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 278 2 0 0 4.4 C[N+]1(C)CCC(=C(c2ccccc2)c2ccccc2)CC1 10.1038/s41467-023-40064-9
CHEMBL1201340 14505 None 4 Human Functional pAC50 = 6.9 6.9 -1 6
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 278 2 0 0 4.4 C[N+]1(C)CCC(=C(c2ccccc2)c2ccccc2)CC1 10.1038/s41467-023-40064-9
DB13720 14505 None 4 Human Functional pAC50 = 6.9 6.9 -1 6
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 278 2 0 0 4.4 C[N+]1(C)CCC(=C(c2ccccc2)c2ccccc2)CC1 10.1038/s41467-023-40064-9
4940 14476 None 26 Human Functional pAC50 = 6.9 6.9 -4 15
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 340 5 0 4 4.8 CCC(=O)c1ccc2c(c1)N(CC(C)N(C)C)c1ccccc1S2 10.1038/s41467-023-40064-9
CHEMBL1201210 14476 None 26 Human Functional pAC50 = 6.9 6.9 -4 15
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 340 5 0 4 4.8 CCC(=O)c1ccc2c(c1)N(CC(C)N(C)C)c1ccccc1S2 10.1038/s41467-023-40064-9
1224 1432 None 51 Human Functional pAC50 = 5.9 5.9 -416 22
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
3100 1432 None 51 Human Functional pAC50 = 5.9 5.9 -416 22
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
3100.0 1432 None 51 Human Functional pAC50 = 5.9 5.9 -416 22
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
8980 1432 None 51 Human Functional pAC50 = 5.9 5.9 -416 22
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
916 1432 None 51 Human Functional pAC50 = 5.9 5.9 -416 22
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
CHEMBL657 1432 None 51 Human Functional pAC50 = 5.9 5.9 -416 22
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
DB01075 1432 None 51 Human Functional pAC50 = 5.9 5.9 -416 22
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
2284 3182 None 26 Human Functional pAC50 = 5.9 5.9 -93 34
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1038/s41467-023-40064-9
4926 3182 None 26 Human Functional pAC50 = 5.9 5.9 -93 34
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1038/s41467-023-40064-9
7281 3182 None 26 Human Functional pAC50 = 5.9 5.9 -93 34
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1038/s41467-023-40064-9
CHEMBL564 3182 None 26 Human Functional pAC50 = 5.9 5.9 -93 34
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1038/s41467-023-40064-9
DB00420 3182 None 26 Human Functional pAC50 = 5.9 5.9 -93 34
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1038/s41467-023-40064-9
16722836 18992 None 63 Human Functional pAC50 = 5.9 5.9 2 13
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 524 10 3 8 4.8 Cc1cnc(Nc2ccc(OCCN3CCCC3)cc2)nc1Nc1cccc(S(=O)(=O)NC(C)(C)C)c1 10.1038/s41467-023-40064-9
CHEMBL1287853 18992 None 63 Human Functional pAC50 = 5.9 5.9 2 13
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 524 10 3 8 4.8 Cc1cnc(Nc2ccc(OCCN3CCCC3)cc2)nc1Nc1cccc(S(=O)(=O)NC(C)(C)C)c1 10.1038/s41467-023-40064-9
16351 102785 None 36 Human Functional pAC50 = 5.9 5.9 -114 17
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 343 0 0 4 4.1 CN1CCN(C2=Nc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1038/s41467-023-40064-9
16351.0 102785 None 36 Human Functional pAC50 = 5.9 5.9 -114 17
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 343 0 0 4 4.1 CN1CCN(C2=Nc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1038/s41467-023-40064-9
CHEMBL304902 102785 None 36 Human Functional pAC50 = 5.9 5.9 -114 17
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 343 0 0 4 4.1 CN1CCN(C2=Nc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1038/s41467-023-40064-9
DB13256 102785 None 36 Human Functional pAC50 = 5.9 5.9 -114 17
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 343 0 0 4 4.1 CN1CCN(C2=Nc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1038/s41467-023-40064-9
260 3869 None 33 Human Functional pAC50 = 4.9 4.9 -3 8
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 284 2 1 3 3.0 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(=O)c1c[nH]c2c1cccc2 10.1038/s41467-023-40064-9
2775 3869 None 33 Human Functional pAC50 = 4.9 4.9 -3 8
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 284 2 1 3 3.0 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(=O)c1c[nH]c2c1cccc2 10.1038/s41467-023-40064-9
656665 3869 None 33 Human Functional pAC50 = 4.9 4.9 -3 8
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 284 2 1 3 3.0 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(=O)c1c[nH]c2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL56564 3869 None 33 Human Functional pAC50 = 4.9 4.9 -3 8
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 284 2 1 3 3.0 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(=O)c1c[nH]c2c1cccc2 10.1038/s41467-023-40064-9
DB11699 3869 None 33 Human Functional pAC50 = 4.9 4.9 -3 8
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 284 2 1 3 3.0 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(=O)c1c[nH]c2c1cccc2 10.1038/s41467-023-40064-9
1549120 198942 None 55 Human Functional pAC50 = 4.9 4.9 -7 19
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 319 4 1 4 2.9 CC(/C=C1\SC(=S)N(CC(=O)O)C1=O)=C\c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL56337 198942 None 55 Human Functional pAC50 = 4.9 4.9 -7 19
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 319 4 1 4 2.9 CC(/C=C1\SC(=S)N(CC(=O)O)C1=O)=C\c1ccccc1 10.1038/s41467-023-40064-9
9429 204590 None 44 Human Functional pAC50 = 4.9 4.9 -645 18
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 446 6 0 6 3.2 CN1CCN(CCCN2c3ccccc3Sc3ccc(S(=O)(=O)N(C)C)cc32)CC1 10.1038/s41467-023-40064-9
9429.0 204590 None 44 Human Functional pAC50 = 4.9 4.9 -645 18
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 446 6 0 6 3.2 CN1CCN(CCCN2c3ccccc3Sc3ccc(S(=O)(=O)N(C)C)cc32)CC1 10.1038/s41467-023-40064-9
CHEMBL609109 204590 None 44 Human Functional pAC50 = 4.9 4.9 -645 18
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 446 6 0 6 3.2 CN1CCN(CCCN2c3ccccc3Sc3ccc(S(=O)(=O)N(C)C)cc32)CC1 10.1038/s41467-023-40064-9
DB01622 204590 None 44 Human Functional pAC50 = 4.9 4.9 -645 18
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 446 6 0 6 3.2 CN1CCN(CCCN2c3ccccc3Sc3ccc(S(=O)(=O)N(C)C)cc32)CC1 10.1038/s41467-023-40064-9
24821094 67115 None 58 Human Functional pAC50 = 4.9 4.9 -1 8
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 440 5 1 7 4.2 C=CC(=O)N1CCC[C@@H](n2nc(-c3ccc(Oc4ccccc4)cc3)c3c(N)ncnc32)C1 10.1038/s41467-023-40064-9
CHEMBL1873475 67115 None 58 Human Functional pAC50 = 4.9 4.9 -1 8
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 440 5 1 7 4.2 C=CC(=O)N1CCC[C@@H](n2nc(-c3ccc(Oc4ccccc4)cc3)c3c(N)ncnc32)C1 10.1038/s41467-023-40064-9
1712095 197848 None 22 Human Functional pAC50 = 4.9 4.9 -2 4
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 397 9 1 5 4.9 CCOc1ccc(/C=C2\NCCc3cc(OCC)c(OCC)cc32)cc1OCC 10.1038/s41467-023-40064-9
CHEMBL551978 197848 None 22 Human Functional pAC50 = 4.9 4.9 -2 4
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 397 9 1 5 4.9 CCOc1ccc(/C=C2\NCCc3cc(OCC)c(OCC)cc32)cc1OCC 10.1038/s41467-023-40064-9
5583 13049 None 39 Human Functional pAC50 = 4.9 4.9 -10 6
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 369 6 3 8 2.7 COc1cc(NCc2ccc3nc(N)nc(N)c3c2C)cc(OC)c1OC 10.1038/s41467-023-40064-9
CHEMBL119 13049 None 39 Human Functional pAC50 = 4.9 4.9 -10 6
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 369 6 3 8 2.7 COc1cc(NCc2ccc3nc(N)nc(N)c3c2C)cc(OC)c1OC 10.1038/s41467-023-40064-9
1909 2822 None 46 Human Functional pAC50 = 5.9 5.9 -2 13
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 479 9 1 8 3.7 COC(=O)C1=C(C)NC(=C(C1c1cccc(c1)[N+](=O)[O-])C(=O)OCCN(Cc1ccccc1)C)C 10.1038/s41467-023-40064-9
2559 2822 None 46 Human Functional pAC50 = 5.9 5.9 -2 13
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 479 9 1 8 3.7 COC(=O)C1=C(C)NC(=C(C1c1cccc(c1)[N+](=O)[O-])C(=O)OCCN(Cc1ccccc1)C)C 10.1038/s41467-023-40064-9
4474 2822 None 46 Human Functional pAC50 = 5.9 5.9 -2 13
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 479 9 1 8 3.7 COC(=O)C1=C(C)NC(=C(C1c1cccc(c1)[N+](=O)[O-])C(=O)OCCN(Cc1ccccc1)C)C 10.1038/s41467-023-40064-9
CHEMBL1484 2822 None 46 Human Functional pAC50 = 5.9 5.9 -2 13
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 479 9 1 8 3.7 COC(=O)C1=C(C)NC(=C(C1c1cccc(c1)[N+](=O)[O-])C(=O)OCCN(Cc1ccccc1)C)C 10.1038/s41467-023-40064-9
CHEMBL3302409 2822 None 46 Human Functional pAC50 = 5.9 5.9 -2 13
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 479 9 1 8 3.7 COC(=O)C1=C(C)NC(=C(C1c1cccc(c1)[N+](=O)[O-])C(=O)OCCN(Cc1ccccc1)C)C 10.1038/s41467-023-40064-9
DB00622 2822 None 46 Human Functional pAC50 = 5.9 5.9 -2 13
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 479 9 1 8 3.7 COC(=O)C1=C(C)NC(=C(C1c1cccc(c1)[N+](=O)[O-])C(=O)OCCN(Cc1ccccc1)C)C 10.1038/s41467-023-40064-9
25382 9159 None 27 Human Functional pAC50 = 6.9 6.9 -3 21
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 291 3 0 1 4.7 CN(C)CCC=C1c2ccccc2C(C)(C)c2ccccc21 10.1038/s41467-023-40064-9
CHEMBL110094 9159 None 27 Human Functional pAC50 = 6.9 6.9 -3 21
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 291 3 0 1 4.7 CN(C)CCC=C1c2ccccc2C(C)(C)c2ccccc21 10.1038/s41467-023-40064-9
92727 207010 None 50 Human Functional pAC50 = 4.9 4.9 -2 6
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 628 15 4 5 4.3 Cc1cccc(C)c1OCC(=O)N[C@@H](Cc1ccccc1)[C@@H](O)C[C@H](Cc1ccccc1)NC(=O)[C@H](C(C)C)N1CCCNC1=O 10.1038/s41467-023-40064-9
CHEMBL729 207010 None 50 Human Functional pAC50 = 4.9 4.9 -2 6
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 628 15 4 5 4.3 Cc1cccc(C)c1OCC(=O)N[C@@H](Cc1ccccc1)[C@@H](O)C[C@H](Cc1ccccc1)NC(=O)[C@H](C(C)C)N1CCCNC1=O 10.1038/s41467-023-40064-9
2865 4143 None 47 Human Functional pAC50 = 4.9 4.9 -6760 20
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
59 4143 None 47 Human Functional pAC50 = 4.9 4.9 -6760 20
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
60854 4143 None 47 Human Functional pAC50 = 4.9 4.9 -6760 20
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
60854.0 4143 None 47 Human Functional pAC50 = 4.9 4.9 -6760 20
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL708 4143 None 47 Human Functional pAC50 = 4.9 4.9 -6760 20
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
DB00246 4143 None 47 Human Functional pAC50 = 4.9 4.9 -6760 20
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL4743867 216518 None 10 Human Functional pAC50 = 5.9 5.9 -2137 15
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL None None None OCCN1CCN(CCC=C2c3ccccc3Sc3ccc(C(F)(F)F)cc32)CC1 10.1038/s41467-023-40064-9
2794 19387 None 54 Human Functional pAC50 = 4.9 4.9 -14 7
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 472 4 1 4 7.5 CC(C)/N=c1\cc2n(-c3ccc(Cl)cc3)c3ccccc3nc-2cc1Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
CHEMBL1292 19387 None 54 Human Functional pAC50 = 4.9 4.9 -14 7
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 472 4 1 4 7.5 CC(C)/N=c1\cc2n(-c3ccc(Cl)cc3)c3ccccc3nc-2cc1Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
4746 207349 None 24 Human Functional pAC50 = 4.9 4.9 -5 19
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 277 4 1 1 5.3 C1CCC(C(CC2CCCCN2)C2CCCCC2)CC1 10.1038/s41467-023-40064-9
CHEMBL1334033 207349 None 24 Human Functional pAC50 = 4.9 4.9 -5 19
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 277 4 1 1 5.3 C1CCC(C(CC2CCCCN2)C2CCCCC2)CC1 10.1038/s41467-023-40064-9
CHEMBL75880 207349 None 24 Human Functional pAC50 = 4.9 4.9 -5 19
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 277 4 1 1 5.3 C1CCC(C(CC2CCCCN2)C2CCCCC2)CC1 10.1038/s41467-023-40064-9
16363 596 None 33 Human Functional pAC50 = 4.9 4.9 -2454 21
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
16363.0 596 None 33 Human Functional pAC50 = 4.9 4.9 -2454 21
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
312 596 None 33 Human Functional pAC50 = 4.9 4.9 -2454 21
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
9215 596 None 33 Human Functional pAC50 = 4.9 4.9 -2454 21
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL297302 596 None 33 Human Functional pAC50 = 4.9 4.9 -2454 21
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
DB12867 596 None 33 Human Functional pAC50 = 4.9 4.9 -2454 21
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
2771 197264 None 50 Human Functional pAC50 = 4.9 4.9 -173 16
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 10.1038/s41467-023-40064-9
CHEMBL1200781 197264 None 50 Human Functional pAC50 = 4.9 4.9 -173 16
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 10.1038/s41467-023-40064-9
CHEMBL549 197264 None 50 Human Functional pAC50 = 4.9 4.9 -173 16
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 10.1038/s41467-023-40064-9
3775 14481 None 19 Human Functional pAC50 = 7.9 7.9 -2 3
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 353 8 1 1 4.1 CC(C)[N+](C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)C(C)C 10.1038/s41467-023-40064-9
3775.0 14481 None 19 Human Functional pAC50 = 7.9 7.9 -2 3
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 353 8 1 1 4.1 CC(C)[N+](C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)C(C)C 10.1038/s41467-023-40064-9
CHEMBL1201232 14481 None 19 Human Functional pAC50 = 7.9 7.9 -2 3
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 353 8 1 1 4.1 CC(C)[N+](C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)C(C)C 10.1038/s41467-023-40064-9
DB01625 14481 None 19 Human Functional pAC50 = 7.9 7.9 -2 3
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 353 8 1 1 4.1 CC(C)[N+](C)(CCC(C(N)=O)(c1ccccc1)c1ccccc1)C(C)C 10.1038/s41467-023-40064-9
72093 35070 None 5 Human Functional pAC50 = 5.9 5.9 -1 28
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 483 16 1 4 6.3 CCCCCCCCOc1ccccc1C(=O)Nc1ccc(C(=O)OCC[N+](C)(CC)CC)cc1 10.1038/s41467-023-40064-9
CHEMBL1433361 35070 None 5 Human Functional pAC50 = 5.9 5.9 -1 28
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 483 16 1 4 6.3 CCCCCCCCOc1ccccc1C(=O)Nc1ccc(C(=O)OCC[N+](C)(CC)CC)cc1 10.1038/s41467-023-40064-9
CHEMBL2103773 35070 None 5 Human Functional pAC50 = 5.9 5.9 -1 28
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 483 16 1 4 6.3 CCCCCCCCOc1ccccc1C(=O)Nc1ccc(C(=O)OCC[N+](C)(CC)CC)cc1 10.1038/s41467-023-40064-9
9846332 52074 None 27 Human Functional pAC50 = 4.9 4.9 1 3
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 444 2 3 5 2.4 C[C@@H]1C[C@H]2[C@@H]3C[C@H](F)C4=CC(=O)C(Cl)=C[C@]4(C)[C@@]3(F)[C@@H](O)C[C@]2(C)[C@@]1(O)C(=O)CO 10.1038/s41467-023-40064-9
CHEMBL1587228 52074 None 27 Human Functional pAC50 = 4.9 4.9 1 3
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 444 2 3 5 2.4 C[C@@H]1C[C@H]2[C@@H]3C[C@H](F)C4=CC(=O)C(Cl)=C[C@]4(C)[C@@]3(F)[C@@H](O)C[C@]2(C)[C@@]1(O)C(=O)CO 10.1038/s41467-023-40064-9
1054 2917 None 55 Human Functional pAC50 = 4.9 4.9 -43 5
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 282 15 1 1 6.1 CCCCCCCC/C=C\CCCCCCCC(=O)O 10.1038/s41467-023-40064-9
3400 2917 None 55 Human Functional pAC50 = 4.9 4.9 -43 5
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 282 15 1 1 6.1 CCCCCCCC/C=C\CCCCCCCC(=O)O 10.1038/s41467-023-40064-9
445639 2917 None 55 Human Functional pAC50 = 4.9 4.9 -43 5
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 282 15 1 1 6.1 CCCCCCCC/C=C\CCCCCCCC(=O)O 10.1038/s41467-023-40064-9
CHEMBL8659 2917 None 55 Human Functional pAC50 = 4.9 4.9 -43 5
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 282 15 1 1 6.1 CCCCCCCC/C=C\CCCCCCCC(=O)O 10.1038/s41467-023-40064-9
392622 56328 None 57 Human Functional pAC50 = 4.9 4.9 -11 20
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 720 17 4 9 5.9 CC(C)c1nc(CN(C)C(=O)N[C@H](C(=O)N[C@@H](Cc2ccccc2)C[C@H](O)[C@H](Cc2ccccc2)NC(=O)OCc2cncs2)C(C)C)cs1 10.1038/s41467-023-40064-9
CHEMBL163 56328 None 57 Human Functional pAC50 = 4.9 4.9 -11 20
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 720 17 4 9 5.9 CC(C)c1nc(CN(C)C(=O)N[C@H](C(=O)N[C@@H](Cc2ccccc2)C[C@H](O)[C@H](Cc2ccccc2)NC(=O)OCc2cncs2)C(C)C)cs1 10.1038/s41467-023-40064-9
37464 19228 None 19 Human Functional pAC50 = 4.9 4.9 -3715 8
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 291 6 2 3 3.5 CC(C)(C)NC[C@H](O)COc1ccccc1C1CCCC1 10.1038/s41467-023-40064-9
37464.0 19228 None 19 Human Functional pAC50 = 4.9 4.9 -3715 8
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 291 6 2 3 3.5 CC(C)(C)NC[C@H](O)COc1ccccc1C1CCCC1 10.1038/s41467-023-40064-9
CHEMBL1290 19228 None 19 Human Functional pAC50 = 4.9 4.9 -3715 8
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 291 6 2 3 3.5 CC(C)(C)NC[C@H](O)COc1ccccc1C1CCCC1 10.1038/s41467-023-40064-9
DB01359 19228 None 19 Human Functional pAC50 = 4.9 4.9 -3715 8
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 291 6 2 3 3.5 CC(C)(C)NC[C@H](O)COc1ccccc1C1CCCC1 10.1038/s41467-023-40064-9
3952 1888 None 32 Human Functional pAC50 = 4.9 4.9 -1548 21
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 10.1038/s41467-023-40064-9
5353646 1888 None 32 Human Functional pAC50 = 4.9 4.9 -1548 21
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 10.1038/s41467-023-40064-9
5353646.0 1888 None 32 Human Functional pAC50 = 4.9 4.9 -1548 21
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 10.1038/s41467-023-40064-9
5443 1888 None 32 Human Functional pAC50 = 4.9 4.9 -1548 21
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 10.1038/s41467-023-40064-9
5702063 1888 None 32 Human Functional pAC50 = 4.9 4.9 -1548 21
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 10.1038/s41467-023-40064-9
5702063.0 1888 None 32 Human Functional pAC50 = 4.9 4.9 -1548 21
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 10.1038/s41467-023-40064-9
CHEMBL1331786 1888 None 32 Human Functional pAC50 = 4.9 4.9 -1548 21
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 10.1038/s41467-023-40064-9
CHEMBL420 1888 None 32 Human Functional pAC50 = 4.9 4.9 -1548 21
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 10.1038/s41467-023-40064-9
DB00629 1888 None 32 Human Functional pAC50 = 4.9 4.9 -1548 21
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 10.1038/s41467-023-40064-9
44591583 184642 None 65 Human Functional pAC50 = 4.9 4.9 -3 2
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 251 2 1 4 1.6 N#Cc1ccc(Oc2ccc3c(c2)COB3O)cc1 10.1038/s41467-023-40064-9
CHEMBL484785 184642 None 65 Human Functional pAC50 = 4.9 4.9 -3 2
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 251 2 1 4 1.6 N#Cc1ccc(Oc2ccc3c(c2)COB3O)cc1 10.1038/s41467-023-40064-9
6989 101006 None 67 Human Functional pAC50 = 4.9 4.9 -1 3
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 150 1 1 1 2.8 Cc1ccc(C(C)C)c(O)c1 10.1038/s41467-023-40064-9
CHEMBL29411 101006 None 67 Human Functional pAC50 = 4.9 4.9 -1 3
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 150 1 1 1 2.8 Cc1ccc(C(C)C)c(O)c1 10.1038/s41467-023-40064-9
5354 155746 None 16 Human Functional pAC50 = 4.9 4.9 -74 20
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 337 12 2 3 5.6 CCCCCCCCNC(C)C(O)c1ccc(SC(C)C)cc1 10.1038/s41467-023-40064-9
CHEMBL404849 155746 None 16 Human Functional pAC50 = 4.9 4.9 -74 20
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 337 12 2 3 5.6 CCCCCCCCNC(C)C(O)c1ccc(SC(C)C)cc1 10.1038/s41467-023-40064-9
11693 1827 None 12 Human Functional pAC50 = 7.8 7.8 -4 7
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1038/s41467-023-40064-9
3494 1827 None 12 Human Functional pAC50 = 7.8 7.8 -4 7
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1038/s41467-023-40064-9
3494.0 1827 None 12 Human Functional pAC50 = 7.8 7.8 -4 7
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1038/s41467-023-40064-9
4302 1827 None 12 Human Functional pAC50 = 7.8 7.8 -4 7
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1038/s41467-023-40064-9
7459 1827 None 12 Human Functional pAC50 = 7.8 7.8 -4 7
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1038/s41467-023-40064-9
9933193 1827 None 12 Human Functional pAC50 = 7.8 7.8 -4 7
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1038/s41467-023-40064-9
9933193.0 1827 None 12 Human Functional pAC50 = 7.8 7.8 -4 7
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1038/s41467-023-40064-9
CHEMBL1201335 1827 None 12 Human Functional pAC50 = 7.8 7.8 -4 7
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1038/s41467-023-40064-9
DB00986 1827 None 12 Human Functional pAC50 = 7.8 7.8 -4 7
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1038/s41467-023-40064-9
2774 3868 None 59 Human Functional pAC50 = 5.9 5.9 -25 5
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 10.1038/s41467-023-40064-9
5593 3868 None 59 Human Functional pAC50 = 5.9 5.9 -25 5
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 10.1038/s41467-023-40064-9
5593.0 3868 None 59 Human Functional pAC50 = 5.9 5.9 -25 5
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 10.1038/s41467-023-40064-9
7319 3868 None 59 Human Functional pAC50 = 5.9 5.9 -25 5
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 10.1038/s41467-023-40064-9
CHEMBL1200604 3868 None 59 Human Functional pAC50 = 5.9 5.9 -25 5
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 10.1038/s41467-023-40064-9
DB00809 3868 None 59 Human Functional pAC50 = 5.9 5.9 -25 5
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 10.1038/s41467-023-40064-9
DB01199 3868 None 59 Human Functional pAC50 = 5.9 5.9 -25 5
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 284 6 1 3 2.2 CCN(C(=O)C(c1ccccc1)CO)Cc1ccncc1 10.1038/s41467-023-40064-9
4011 82440 None 34 Human Functional pAC50 = 5.9 5.9 -109 26
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 10.1038/s41467-023-40064-9
CHEMBL21731 82440 None 34 Human Functional pAC50 = 5.9 5.9 -109 26
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 10.1038/s41467-023-40064-9
23480 124157 None 21 Human Functional pAC50 = 5.9 5.9 -1 7
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 281 5 1 1 5.0 CC(CC(c1ccccc1)c1ccccc1)NC(C)(C)C 10.1038/s41467-023-40064-9
CHEMBL363295 124157 None 21 Human Functional pAC50 = 5.9 5.9 -1 7
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 281 5 1 1 5.0 CC(CC(c1ccccc1)c1ccccc1)NC(C)(C)C 10.1038/s41467-023-40064-9
2267 559 None 45 Human Functional pAC50 = 4.9 4.9 -32 14
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1038/s41467-023-40064-9
2267.0 559 None 45 Human Functional pAC50 = 4.9 4.9 -32 14
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1038/s41467-023-40064-9
271 559 None 45 Human Functional pAC50 = 4.9 4.9 -32 14
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1038/s41467-023-40064-9
7121 559 None 45 Human Functional pAC50 = 4.9 4.9 -32 14
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1038/s41467-023-40064-9
CHEMBL639 559 None 45 Human Functional pAC50 = 4.9 4.9 -32 14
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1038/s41467-023-40064-9
DB00972 559 None 45 Human Functional pAC50 = 4.9 4.9 -32 14
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1038/s41467-023-40064-9
68867 78202 None 29 Human Functional pAC50 = 4.9 4.9 -676 13
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 402 7 2 6 3.1 CCOc1cc(N)c([N+](=O)[O-])cc1C(=O)NC1CCN(CC2CC=CCC2)CC1 10.1038/s41467-023-40064-9
68867.0 78202 None 29 Human Functional pAC50 = 4.9 4.9 -676 13
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 402 7 2 6 3.1 CCOc1cc(N)c([N+](=O)[O-])cc1C(=O)NC1CCN(CC2CC=CCC2)CC1 10.1038/s41467-023-40064-9
CHEMBL2104523 78202 None 29 Human Functional pAC50 = 4.9 4.9 -676 13
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 402 7 2 6 3.1 CCOc1cc(N)c([N+](=O)[O-])cc1C(=O)NC1CCN(CC2CC=CCC2)CC1 10.1038/s41467-023-40064-9
DB08810 78202 None 29 Human Functional pAC50 = 4.9 4.9 -676 13
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 402 7 2 6 3.1 CCOc1cc(N)c([N+](=O)[O-])cc1C(=O)NC1CCN(CC2CC=CCC2)CC1 10.1038/s41467-023-40064-9
55483 207555 None 29 Human Functional pAC50 = 4.9 4.9 -89 11
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 356 13 4 4 3.6 Oc1ccc(CCNCCCCCCNCCc2ccccc2)cc1O 10.1038/s41467-023-40064-9
CHEMBL77622 207555 None 29 Human Functional pAC50 = 4.9 4.9 -89 11
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 356 13 4 4 3.6 Oc1ccc(CCNCCCCCCNCCc2ccccc2)cc1O 10.1038/s41467-023-40064-9
CHEMBL4743867 216518 None 10 Human Functional pAC50 = 4.9 4.9 -2137 15
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL None None None OCCN1CCN(CCC=C2c3ccccc3Sc3ccc(C(F)(F)F)cc32)CC1 10.1038/s41467-023-40064-9
64143 201320 None 42 Human Functional pAC50 = 4.9 4.9 -2 10
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 567 9 4 6 4.7 Cc1c(O)cccc1C(=O)N[C@@H](CSc1ccccc1)[C@H](O)CN1C[C@H]2CCCC[C@H]2C[C@H]1C(=O)NC(C)(C)C 10.1038/s41467-023-40064-9
CHEMBL584 201320 None 42 Human Functional pAC50 = 4.9 4.9 -2 10
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 567 9 4 6 4.7 Cc1c(O)cccc1C(=O)N[C@@H](CSc1ccccc1)[C@H](O)CN1C[C@H]2CCCC[C@H]2C[C@H]1C(=O)NC(C)(C)C 10.1038/s41467-023-40064-9
30323 62505 None 35 Human Functional pAC50 = 4.8 4.8 -7 21
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 527 4 5 11 1.0 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(C)=O)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 10.1038/s41467-023-40064-9
CHEMBL1563 62505 None 35 Human Functional pAC50 = 4.8 4.8 -7 21
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 527 4 5 11 1.0 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(C)=O)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 10.1038/s41467-023-40064-9
CHEMBL178 62505 None 35 Human Functional pAC50 = 4.8 4.8 -7 21
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 527 4 5 11 1.0 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(C)=O)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 10.1038/s41467-023-40064-9
3658 4107 None 38 Human Functional pAC50 = 4.8 4.8 -1513 18
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 10.1038/s41467-023-40064-9
517 4107 None 38 Human Functional pAC50 = 4.8 4.8 -1513 18
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 10.1038/s41467-023-40064-9
5709 4107 None 38 Human Functional pAC50 = 4.8 4.8 -1513 18
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 10.1038/s41467-023-40064-9
5709.0 4107 None 38 Human Functional pAC50 = 4.8 4.8 -1513 18
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 10.1038/s41467-023-40064-9
CHEMBL312448 4107 None 38 Human Functional pAC50 = 4.8 4.8 -1513 18
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 10.1038/s41467-023-40064-9
DB06694 4107 None 38 Human Functional pAC50 = 4.8 4.8 -1513 18
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 10.1038/s41467-023-40064-9
1613 2348 None 42 Human Functional pAC50 = 5.8 5.8 -35 33
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
205 2348 None 42 Human Functional pAC50 = 5.8 5.8 -35 33
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
3964 2348 None 42 Human Functional pAC50 = 5.8 5.8 -35 33
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
3964.0 2348 None 42 Human Functional pAC50 = 5.8 5.8 -35 33
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
CHEMBL831 2348 None 42 Human Functional pAC50 = 5.8 5.8 -35 33
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
DB00408 2348 None 42 Human Functional pAC50 = 5.8 5.8 -35 33
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
2218 15289 None 20 Human Functional pAC50 = 4.8 4.8 -18 12
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 322 8 0 2 4.4 CCN(CC)CCCN(c1ccccc1)C1Cc2ccccc2C1 10.1038/s41467-023-40064-9
CHEMBL1213033 15289 None 20 Human Functional pAC50 = 4.8 4.8 -18 12
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 322 8 0 2 4.4 CCN(CC)CCCN(c1ccccc1)C1Cc2ccccc2C1 10.1038/s41467-023-40064-9
3735 208689 None 52 Human Functional pAC50 = 4.8 4.8 1 3
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 571 4 2 2 3.7 CCC(Cc1c(I)cc(I)c(N)c1I)C(=O)O 10.1038/s41467-023-40064-9
CHEMBL867 208689 None 52 Human Functional pAC50 = 4.8 4.8 1 3
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 571 4 2 2 3.7 CCC(Cc1c(I)cc(I)c(N)c1I)C(=O)O 10.1038/s41467-023-40064-9
2398 954 None 43 Human Functional pAC50 = 6.8 6.8 -151 36
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
2801 954 None 43 Human Functional pAC50 = 6.8 6.8 -151 36
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
2801.0 954 None 43 Human Functional pAC50 = 6.8 6.8 -151 36
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
701 954 None 43 Human Functional pAC50 = 6.8 6.8 -151 36
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
CHEMBL415 954 None 43 Human Functional pAC50 = 6.8 6.8 -151 36
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
DB01242 954 None 43 Human Functional pAC50 = 6.8 6.8 -151 36
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
1570 57315 None 64 Human Functional pAC50 = 4.8 4.8 -2 3
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 127 0 1 3 1.5 On1ccccc1=S 10.1038/s41467-023-40064-9
CHEMBL1650619 57315 None 64 Human Functional pAC50 = 4.8 4.8 -2 3
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 127 0 1 3 1.5 On1ccccc1=S 10.1038/s41467-023-40064-9
444795 140086 None 62 Human Functional pAC50 = 4.8 4.8 -41 6
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 300 5 1 1 5.6 CC1=C(/C=C/C(C)=C/C=C/C(C)=C/C(=O)O)C(C)(C)CCC1 10.1038/s41467-023-40064-9
CHEMBL38 140086 None 62 Human Functional pAC50 = 4.8 4.8 -41 6
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 300 5 1 1 5.6 CC1=C(/C=C/C(C)=C/C=C/C(C)=C/C(=O)O)C(C)(C)CCC1 10.1038/s41467-023-40064-9
2444 14484 None 20 Human Functional pAC50 = 5.8 5.8 -1 8
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 333 6 0 2 4.1 CN(C)CCOC(c1ccccc1)c1ccc(Br)cc1 10.1038/s41467-023-40064-9
2444.0 14484 None 20 Human Functional pAC50 = 5.8 5.8 -1 8
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 333 6 0 2 4.1 CN(C)CCOC(c1ccccc1)c1ccc(Br)cc1 10.1038/s41467-023-40064-9
CHEMBL1201245 14484 None 20 Human Functional pAC50 = 5.8 5.8 -1 8
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 333 6 0 2 4.1 CN(C)CCOC(c1ccccc1)c1ccc(Br)cc1 10.1038/s41467-023-40064-9
DB01237 14484 None 20 Human Functional pAC50 = 5.8 5.8 -1 8
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 333 6 0 2 4.1 CN(C)CCOC(c1ccccc1)c1ccc(Br)cc1 10.1038/s41467-023-40064-9
6918178 14450 None 36 Human Functional pAC50 = 4.8 4.8 -1 3
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 484 4 1 5 4.1 CCC(=O)O[C@]1(C(=O)CCl)[C@@H](C)C[C@H]2[C@@H]3C[C@H](F)C4=CC(=O)C=C[C@]4(C)[C@@]3(F)[C@@H](O)C[C@@]21C 10.1038/s41467-023-40064-9
CHEMBL1200908 14450 None 36 Human Functional pAC50 = 4.8 4.8 -1 3
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 484 4 1 5 4.1 CCC(=O)O[C@]1(C(=O)CCl)[C@@H](C)C[C@H]2[C@@H]3C[C@H](F)C4=CC(=O)C=C[C@]4(C)[C@@]3(F)[C@@H](O)C[C@@]21C 10.1038/s41467-023-40064-9
4919 208692 None 16 Human Functional pAC50 = 6.8 6.8 1 5
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 287 5 1 2 3.9 OC(CCN1CCCC1)(c1ccccc1)C1CCCCC1 10.1038/s41467-023-40064-9
4919.0 208692 None 16 Human Functional pAC50 = 6.8 6.8 1 5
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 287 5 1 2 3.9 OC(CCN1CCCC1)(c1ccccc1)C1CCCCC1 10.1038/s41467-023-40064-9
CHEMBL86715 208692 None 16 Human Functional pAC50 = 6.8 6.8 1 5
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 287 5 1 2 3.9 OC(CCN1CCCC1)(c1ccccc1)C1CCCCC1 10.1038/s41467-023-40064-9
DB00387 208692 None 16 Human Functional pAC50 = 6.8 6.8 1 5
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 287 5 1 2 3.9 OC(CCN1CCCC1)(c1ccccc1)C1CCCCC1 10.1038/s41467-023-40064-9
2166 3123 None 33 Human Functional pAC50 = 5.8 5.8 -3 10
Agonist activity at human CHRM1 in an in vitro cell-based assay (NIBR assay) measured by Hamamatsu Functional Drug Screening SystemAgonist activity at human CHRM1 in an in vitro cell-based assay (NIBR assay) measured by Hamamatsu Functional Drug Screening System
ChEMBL 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 10.1038/s41467-023-40064-9
305 3123 None 33 Human Functional pAC50 = 5.8 5.8 -3 10
Agonist activity at human CHRM1 in an in vitro cell-based assay (NIBR assay) measured by Hamamatsu Functional Drug Screening SystemAgonist activity at human CHRM1 in an in vitro cell-based assay (NIBR assay) measured by Hamamatsu Functional Drug Screening System
ChEMBL 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 10.1038/s41467-023-40064-9
5910 3123 None 33 Human Functional pAC50 = 5.8 5.8 -3 10
Agonist activity at human CHRM1 in an in vitro cell-based assay (NIBR assay) measured by Hamamatsu Functional Drug Screening SystemAgonist activity at human CHRM1 in an in vitro cell-based assay (NIBR assay) measured by Hamamatsu Functional Drug Screening System
ChEMBL 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 10.1038/s41467-023-40064-9
5910.0 3123 None 33 Human Functional pAC50 = 5.8 5.8 -3 10
Agonist activity at human CHRM1 in an in vitro cell-based assay (NIBR assay) measured by Hamamatsu Functional Drug Screening SystemAgonist activity at human CHRM1 in an in vitro cell-based assay (NIBR assay) measured by Hamamatsu Functional Drug Screening System
ChEMBL 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 10.1038/s41467-023-40064-9
CHEMBL550 3123 None 33 Human Functional pAC50 = 5.8 5.8 -3 10
Agonist activity at human CHRM1 in an in vitro cell-based assay (NIBR assay) measured by Hamamatsu Functional Drug Screening SystemAgonist activity at human CHRM1 in an in vitro cell-based assay (NIBR assay) measured by Hamamatsu Functional Drug Screening System
ChEMBL 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 10.1038/s41467-023-40064-9
DB01085 3123 None 33 Human Functional pAC50 = 5.8 5.8 -3 10
Agonist activity at human CHRM1 in an in vitro cell-based assay (NIBR assay) measured by Hamamatsu Functional Drug Screening SystemAgonist activity at human CHRM1 in an in vitro cell-based assay (NIBR assay) measured by Hamamatsu Functional Drug Screening System
ChEMBL 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 10.1038/s41467-023-40064-9
43815 187026 None 38 Human Functional pAC50 = 5.8 5.8 -4 20
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 10.1038/s41467-023-40064-9
CHEMBL1708 187026 None 38 Human Functional pAC50 = 5.8 5.8 -4 20
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 10.1038/s41467-023-40064-9
CHEMBL490 187026 None 38 Human Functional pAC50 = 5.8 5.8 -4 20
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 10.1038/s41467-023-40064-9
115163 57319 None 32 Human Functional pAC50 = 4.8 4.8 -4 2
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 439 5 0 7 2.4 CC(C)(C)C(=O)OCOC(=O)[C@@H]1N2C(=O)[C@@H](/N=C/N3CCCCCC3)[C@H]2SC1(C)C 10.1038/s41467-023-40064-9
CHEMBL1650818 57319 None 32 Human Functional pAC50 = 4.8 4.8 -4 2
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 439 5 0 7 2.4 CC(C)(C)C(=O)OCOC(=O)[C@@H]1N2C(=O)[C@@H](/N=C/N3CCCCCC3)[C@H]2SC1(C)C 10.1038/s41467-023-40064-9
70695647 78242 None 0 Human Functional pAC50 = 4.8 4.8 -30 3
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 300 2 1 1 5.3 C=CC[C@]1(O)CC[C@H]2[C@@H]3CCC4=CCCCC4[C@H]3CC[C@@]21C 10.1038/s41467-023-40064-9
CHEMBL2105618 78242 None 0 Human Functional pAC50 = 4.8 4.8 -30 3
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 300 2 1 1 5.3 C=CC[C@]1(O)CC[C@H]2[C@@H]3CCC4=CCCCC4[C@H]3CC[C@@]21C 10.1038/s41467-023-40064-9
31101 729 None 28 Human Functional pAC50 = 4.8 4.8 -5370 29
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 10.1038/s41467-023-40064-9
31101.0 729 None 28 Human Functional pAC50 = 4.8 4.8 -5370 29
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 10.1038/s41467-023-40064-9
35 729 None 28 Human Functional pAC50 = 4.8 4.8 -5370 29
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 10.1038/s41467-023-40064-9
403 729 None 28 Human Functional pAC50 = 4.8 4.8 -5370 29
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 10.1038/s41467-023-40064-9
CHEMBL493 729 None 28 Human Functional pAC50 = 4.8 4.8 -5370 29
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 10.1038/s41467-023-40064-9
DB01200 729 None 28 Human Functional pAC50 = 4.8 4.8 -5370 29
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 10.1038/s41467-023-40064-9
6077 150786 None 16 Human Functional pAC50 = 6.8 6.8 -50 11
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 326 5 0 4 4.4 CC(=O)c1ccc2c(c1)N(CCCN(C)C)c1ccccc1S2 10.1038/s41467-023-40064-9
CHEMBL39560 150786 None 16 Human Functional pAC50 = 6.8 6.8 -50 11
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 326 5 0 4 4.4 CC(=O)c1ccc2c(c1)N(CCCN(C)C)c1ccccc1S2 10.1038/s41467-023-40064-9
CHEMBL4743867 216518 None 10 Human Functional pAC50 = 4.8 4.8 -2137 15
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL None None None OCCN1CCN(CCC=C2c3ccccc3Sc3ccc(C(F)(F)F)cc32)CC1 10.1038/s41467-023-40064-9
19090 156910 None 34 Human Functional pAC50 = 4.8 4.8 - 1
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 342 1 1 3 4.0 CC(=O)[C@@]1(O)CC[C@H]2[C@@H]3C=C(C)C4=CC(=O)CC[C@]4(C)[C@H]3CC[C@@]21C 10.1038/s41467-023-40064-9
CHEMBL4071215 156910 None 34 Human Functional pAC50 = 4.8 4.8 - 1
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 342 1 1 3 4.0 CC(=O)[C@@]1(O)CC[C@H]2[C@@H]3C=C(C)C4=CC(=O)CC[C@]4(C)[C@H]3CC[C@@]21C 10.1038/s41467-023-40064-9
71743 78296 None 47 Human Functional pAC50 = 4.8 4.8 1 4
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 353 3 0 4 3.6 O=C(Oc1ccc2c(c1)CCCN2C(=O)C(Cl)Cl)c1ccco1 10.1038/s41467-023-40064-9
CHEMBL2107014 78296 None 47 Human Functional pAC50 = 4.8 4.8 1 4
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 353 3 0 4 3.6 O=C(Oc1ccc2c(c1)CCCN2C(=O)C(Cl)Cl)c1ccco1 10.1038/s41467-023-40064-9
18609376 206817 None 38 Human Functional pAC50 = 4.8 4.8 -6 4
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 386 2 0 4 4.7 CC(=O)O[C@]1(C(C)=O)CC[C@H]2[C@@H]3C[C@H](C)C4=CC(=O)CC[C@]4(C)[C@H]3CC[C@@]21C 10.1038/s41467-023-40064-9
6279 206817 None 38 Human Functional pAC50 = 4.8 4.8 -6 4
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 386 2 0 4 4.7 CC(=O)O[C@]1(C(C)=O)CC[C@H]2[C@@H]3C[C@H](C)C4=CC(=O)CC[C@]4(C)[C@H]3CC[C@@]21C 10.1038/s41467-023-40064-9
CHEMBL717 206817 None 38 Human Functional pAC50 = 4.8 4.8 -6 4
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 386 2 0 4 4.7 CC(=O)O[C@]1(C(C)=O)CC[C@H]2[C@@H]3C[C@H](C)C4=CC(=O)CC[C@]4(C)[C@H]3CC[C@@]21C 10.1038/s41467-023-40064-9
151537 162759 None 30 Human Functional pAC50 = 4.8 4.8 -1 4
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 543 5 6 12 0.0 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(=O)CO)C[C@@H]3O[C@H]1C[C@H](N)[C@@H](O)[C@H](C)O1 10.1038/s41467-023-40064-9
41867 162759 None 30 Human Functional pAC50 = 4.8 4.8 -1 4
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 543 5 6 12 0.0 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(=O)CO)C[C@@H]3O[C@H]1C[C@H](N)[C@@H](O)[C@H](C)O1 10.1038/s41467-023-40064-9
CHEMBL417 162759 None 30 Human Functional pAC50 = 4.8 4.8 -1 4
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 543 5 6 12 0.0 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(=O)CO)C[C@@H]3O[C@H]1C[C@H](N)[C@@H](O)[C@H](C)O1 10.1038/s41467-023-40064-9
16119814 56359 None 20 Human Functional pAC50 = 4.8 4.8 -3 6
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 1093 23 16 18 -3.3 CC[C@H](C)C[C@H](C)CCCCCCCCC(=O)N[C@H]1C[C@@H](O)[C@@H](NCCN)NC(=O)[C@@H]2[C@@H](O)CCN2C(=O)[C@H]([C@H](O)CCN)NC(=O)[C@H]([C@H](O)[C@@H](O)c2ccc(O)cc2)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@H]([C@@H](C)O)NC1=O 10.1038/s41467-023-40064-9
CHEMBL1630575 56359 None 20 Human Functional pAC50 = 4.8 4.8 -3 6
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 1093 23 16 18 -3.3 CC[C@H](C)C[C@H](C)CCCCCCCCC(=O)N[C@H]1C[C@@H](O)[C@@H](NCCN)NC(=O)[C@@H]2[C@@H](O)CCN2C(=O)[C@H]([C@H](O)CCN)NC(=O)[C@H]([C@H](O)[C@@H](O)c2ccc(O)cc2)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@H]([C@@H](C)O)NC1=O 10.1038/s41467-023-40064-9
1440 2027 None 69 Human Functional pAC50 = 4.8 4.8 -40 7
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 357 4 1 4 3.9 COc1ccc2c(c1)c(CC(=O)O)c(n2C(=O)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
1909 2027 None 69 Human Functional pAC50 = 4.8 4.8 -40 7
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 357 4 1 4 3.9 COc1ccc2c(c1)c(CC(=O)O)c(n2C(=O)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
3715 2027 None 69 Human Functional pAC50 = 4.8 4.8 -40 7
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 357 4 1 4 3.9 COc1ccc2c(c1)c(CC(=O)O)c(n2C(=O)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
CHEMBL6 2027 None 69 Human Functional pAC50 = 4.8 4.8 -40 7
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 357 4 1 4 3.9 COc1ccc2c(c1)c(CC(=O)O)c(n2C(=O)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
DB00328 2027 None 69 Human Functional pAC50 = 4.8 4.8 -40 7
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 357 4 1 4 3.9 COc1ccc2c(c1)c(CC(=O)O)c(n2C(=O)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
135398737 958 None 57 Human Functional pAC50 = 7.8 7.8 -6 43
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
135398737.0 958 None 57 Human Functional pAC50 = 7.8 7.8 -6 43
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
38 958 None 57 Human Functional pAC50 = 7.8 7.8 -6 43
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
722 958 None 57 Human Functional pAC50 = 7.8 7.8 -6 43
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL42 958 None 57 Human Functional pAC50 = 7.8 7.8 -6 43
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
DB00363 958 None 57 Human Functional pAC50 = 7.8 7.8 -6 43
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
1371 1923 None 9 Human Functional pAC50 = 7.8 7.8 4 2
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 317 4 1 2 2.8 C[N+]1(C)CCN(CC1)CC(c1ccccc1)(C1CCCCC1)O 10.1038/s41467-023-40064-9
24199 1923 None 9 Human Functional pAC50 = 7.8 7.8 4 2
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 317 4 1 2 2.8 C[N+]1(C)CCN(CC1)CC(c1ccccc1)(C1CCCCC1)O 10.1038/s41467-023-40064-9
24199.0 1923 None 9 Human Functional pAC50 = 7.8 7.8 4 2
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 317 4 1 2 2.8 C[N+]1(C)CCN(CC1)CC(c1ccccc1)(C1CCCCC1)O 10.1038/s41467-023-40064-9
323 1923 None 9 Human Functional pAC50 = 7.8 7.8 4 2
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 317 4 1 2 2.8 C[N+]1(C)CCN(CC1)CC(c1ccccc1)(C1CCCCC1)O 10.1038/s41467-023-40064-9
CHEMBL1201325 1923 None 9 Human Functional pAC50 = 7.8 7.8 4 2
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 317 4 1 2 2.8 C[N+]1(C)CCN(CC1)CC(c1ccccc1)(C1CCCCC1)O 10.1038/s41467-023-40064-9
DB06787 1923 None 9 Human Functional pAC50 = 7.8 7.8 4 2
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 317 4 1 2 2.8 C[N+]1(C)CCN(CC1)CC(c1ccccc1)(C1CCCCC1)O 10.1038/s41467-023-40064-9
2131 57423 None 16 Human Functional pAC50 = 5.8 5.8 -2 7
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 536 14 2 2 4.6 CC[N+](CC)(CCNC(=O)C(=O)NCC[N+](CC)(CC)Cc1ccccc1Cl)Cc1ccccc1Cl 10.1038/s41467-023-40064-9
CHEMBL1652 57423 None 16 Human Functional pAC50 = 5.8 5.8 -2 7
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 536 14 2 2 4.6 CC[N+](CC)(CCNC(=O)C(=O)NCC[N+](CC)(CC)Cc1ccccc1Cl)Cc1ccccc1Cl 10.1038/s41467-023-40064-9
5440 28732 None 28 Human Functional pAC50 = 4.8 4.8 -6918 16
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 399 6 0 5 5.0 CCSc1ccc2c(c1)N(CCCN1CCN(C)CC1)c1ccccc1S2 10.1038/s41467-023-40064-9
5440.0 28732 None 28 Human Functional pAC50 = 4.8 4.8 -6918 16
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 399 6 0 5 5.0 CCSc1ccc2c(c1)N(CCCN1CCN(C)CC1)c1ccccc1S2 10.1038/s41467-023-40064-9
CHEMBL1378 28732 None 28 Human Functional pAC50 = 4.8 4.8 -6918 16
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 399 6 0 5 5.0 CCSc1ccc2c(c1)N(CCCN1CCN(C)CC1)c1ccccc1S2 10.1038/s41467-023-40064-9
DB00372 28732 None 28 Human Functional pAC50 = 4.8 4.8 -6918 16
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 399 6 0 5 5.0 CCSc1ccc2c(c1)N(CCCN1CCN(C)CC1)c1ccccc1S2 10.1038/s41467-023-40064-9
134018 10473 None 70 Human Functional pAC50 = 4.8 4.8 - 1
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 316 5 1 5 3.7 Cc1nc(-c2ccc(OCC(C)C)c(C#N)c2)sc1C(=O)O 10.1038/s41467-023-40064-9
CHEMBL1164729 10473 None 70 Human Functional pAC50 = 4.8 4.8 - 1
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 316 5 1 5 3.7 Cc1nc(-c2ccc(OCC(C)C)c(C#N)c2)sc1C(=O)O 10.1038/s41467-023-40064-9
49843517 78325 None 41 Human Functional pAC50 = 4.8 4.8 -48 8
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 590 13 2 6 8.5 CCCCCCO[C@@H](C)c1cccc(-c2csc(NC(=O)c3cc(Cl)c(/C=C(\C)C(=O)O)c(Cl)c3)n2)c1OC 10.1038/s41467-023-40064-9
CHEMBL2107831 78325 None 41 Human Functional pAC50 = 4.8 4.8 -48 8
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 590 13 2 6 8.5 CCCCCCO[C@@H](C)c1cccc(-c2csc(NC(=O)c3cc(Cl)c(/C=C(\C)C(=O)O)c(Cl)c3)n2)c1OC 10.1038/s41467-023-40064-9
176870 197941 None 62 Human Functional pAC50 = 5.8 5.8 5 6
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 393 10 1 7 3.4 C#Cc1cccc(Nc2ncnc3cc(OCCOC)c(OCCOC)cc23)c1 10.1038/s41467-023-40064-9
CHEMBL553 197941 None 62 Human Functional pAC50 = 5.8 5.8 5 6
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 393 10 1 7 3.4 C#Cc1cccc(Nc2ncnc3cc(OCCOC)c(OCCOC)cc23)c1 10.1038/s41467-023-40064-9
5625 202124 None 46 Human Functional pAC50 = 4.8 4.8 -1 5
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 456 6 3 6 2.7 CC(C)Nc1cccnc1N1CCN(C(=O)c2cc3cc(NS(C)(=O)=O)ccc3[nH]2)CC1 10.1038/s41467-023-40064-9
CHEMBL593 202124 None 46 Human Functional pAC50 = 4.8 4.8 -1 5
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 456 6 3 6 2.7 CC(C)Nc1cccnc1N1CCN(C(=O)c2cc3cc(NS(C)(=O)=O)ccc3[nH]2)CC1 10.1038/s41467-023-40064-9
3280 48463 None 17 Human Functional pAC50 = 5.8 5.8 1 8
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 395 10 0 5 5.4 CCOc1ccc(Cc2nccc3cc(OCC)c(OCC)cc23)cc1OCC 10.1038/s41467-023-40064-9
CHEMBL1555736 48463 None 17 Human Functional pAC50 = 5.8 5.8 1 8
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 395 10 0 5 5.4 CCOc1ccc(Cc2nccc3cc(OCC)c(OCC)cc23)cc1OCC 10.1038/s41467-023-40064-9
6314185 191515 None 17 Human Functional pAC50 = 4.8 4.8 -7 3
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 353 7 1 2 5.2 CCNC(=O)/C=C(C)/C=C/C=C(C)/C=C/c1c(C)cc(OC)c(C)c1C 10.1038/s41467-023-40064-9
CHEMBL519260 191515 None 17 Human Functional pAC50 = 4.8 4.8 -7 3
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 353 7 1 2 5.2 CCNC(=O)/C=C(C)/C=C/C=C(C)/C=C/c1c(C)cc(OC)c(C)c1C 10.1038/s41467-023-40064-9
3463 175250 None 68 Human Functional pAC50 = 4.8 4.8 -3 4
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 250 6 1 2 3.6 Cc1ccc(C)c(OCCCC(C)(C)C(=O)O)c1 10.1038/s41467-023-40064-9
CHEMBL457 175250 None 68 Human Functional pAC50 = 4.8 4.8 -3 4
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 250 6 1 2 3.6 Cc1ccc(C)c(OCCCC(C)(C)C(=O)O)c1 10.1038/s41467-023-40064-9
1353 1911 None 63 Human Functional pAC50 = 4.8 4.8 -2238 39
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
3559 1911 None 63 Human Functional pAC50 = 4.8 4.8 -2238 39
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
3559.0 1911 None 63 Human Functional pAC50 = 4.8 4.8 -2238 39
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
86 1911 None 63 Human Functional pAC50 = 4.8 4.8 -2238 39
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
CHEMBL54 1911 None 63 Human Functional pAC50 = 4.8 4.8 -2238 39
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
DB00502 1911 None 63 Human Functional pAC50 = 4.8 4.8 -2238 39
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
2726 919 None 48 Human Functional pAC50 = 5.8 5.8 -177 42
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
2726.0 919 None 48 Human Functional pAC50 = 5.8 5.8 -177 42
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
621 919 None 48 Human Functional pAC50 = 5.8 5.8 -177 42
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
83 919 None 48 Human Functional pAC50 = 5.8 5.8 -177 42
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
CHEMBL71 919 None 48 Human Functional pAC50 = 5.8 5.8 -177 42
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
DB00477 919 None 48 Human Functional pAC50 = 5.8 5.8 -177 42
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
4037 189124 None 43 Human Functional pAC50 = 4.8 4.8 -1 4
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 295 3 2 2 4.7 Cc1ccc(Cl)c(Nc2ccccc2C(=O)O)c1Cl 10.1038/s41467-023-40064-9
CHEMBL509 189124 None 43 Human Functional pAC50 = 4.8 4.8 -1 4
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 295 3 2 2 4.7 Cc1ccc(Cl)c(Nc2ccccc2C(=O)O)c1Cl 10.1038/s41467-023-40064-9
CHEMBL876 189124 None 43 Human Functional pAC50 = 4.8 4.8 -1 4
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 295 3 2 2 4.7 Cc1ccc(Cl)c(Nc2ccccc2C(=O)O)c1Cl 10.1038/s41467-023-40064-9
3042 1414 None 26 Human Functional pAC50 = 7.8 7.8 -5 17
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC 10.1038/s41467-023-40064-9
3042.0 1414 None 26 Human Functional pAC50 = 7.8 7.8 -5 17
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC 10.1038/s41467-023-40064-9
355 1414 None 26 Human Functional pAC50 = 7.8 7.8 -5 17
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC 10.1038/s41467-023-40064-9
868 1414 None 26 Human Functional pAC50 = 7.8 7.8 -5 17
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC 10.1038/s41467-023-40064-9
CHEMBL1123 1414 None 26 Human Functional pAC50 = 7.8 7.8 -5 17
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC 10.1038/s41467-023-40064-9
DB00804 1414 None 26 Human Functional pAC50 = 7.8 7.8 -5 17
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC 10.1038/s41467-023-40064-9
277 1301 None 39 Human Functional pAC50 = 7.8 7.8 -16 29
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 10.1038/s41467-023-40064-9
2913 1301 None 39 Human Functional pAC50 = 7.8 7.8 -16 29
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 10.1038/s41467-023-40064-9
2913.0 1301 None 39 Human Functional pAC50 = 7.8 7.8 -16 29
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 10.1038/s41467-023-40064-9
765 1301 None 39 Human Functional pAC50 = 7.8 7.8 -16 29
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 10.1038/s41467-023-40064-9
CHEMBL516 1301 None 39 Human Functional pAC50 = 7.8 7.8 -16 29
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 10.1038/s41467-023-40064-9
DB00434 1301 None 39 Human Functional pAC50 = 7.8 7.8 -16 29
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 10.1038/s41467-023-40064-9
657202 12534 None 3 Human Functional pAC50 = 6.8 6.8 -4 4
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 282 6 0 2 3.5 CCCC(CCC)C(=O)O[C@H]1C[C@H]2CC[C@@H](C1)[N+]2(C)C 10.1038/s41467-023-40064-9
CHEMBL1186610 12534 None 3 Human Functional pAC50 = 6.8 6.8 -4 4
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 282 6 0 2 3.5 CCCC(CCC)C(=O)O[C@H]1C[C@H]2CC[C@@H](C1)[N+]2(C)C 10.1038/s41467-023-40064-9
191 403 None 60 Human Functional pAC50 = 5.8 5.8 -239 36
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
201 403 None 60 Human Functional pAC50 = 5.8 5.8 -239 36
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
2170 403 None 60 Human Functional pAC50 = 5.8 5.8 -239 36
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
2170.0 403 None 60 Human Functional pAC50 = 5.8 5.8 -239 36
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
CHEMBL1113 403 None 60 Human Functional pAC50 = 5.8 5.8 -239 36
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
DB00543 403 None 60 Human Functional pAC50 = 5.8 5.8 -239 36
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
1530 2182 None 36 Human Functional pAC50 = 5.8 5.8 -100 25
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 10.1038/s41467-023-40064-9
3827 2182 None 36 Human Functional pAC50 = 5.8 5.8 -100 25
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 10.1038/s41467-023-40064-9
3827.0 2182 None 36 Human Functional pAC50 = 5.8 5.8 -100 25
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 10.1038/s41467-023-40064-9
7206 2182 None 36 Human Functional pAC50 = 5.8 5.8 -100 25
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 10.1038/s41467-023-40064-9
CHEMBL534 2182 None 36 Human Functional pAC50 = 5.8 5.8 -100 25
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 10.1038/s41467-023-40064-9
DB00920 2182 None 36 Human Functional pAC50 = 5.8 5.8 -100 25
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 10.1038/s41467-023-40064-9
4942 5720 None 27 Human Functional pAC50 = 5.8 5.8 -1 11
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 367 7 0 4 4.0 CCCOC(C(=O)OC1CCN(C)CC1)(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
4942.0 5720 None 27 Human Functional pAC50 = 5.8 5.8 -1 11
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 367 7 0 4 4.0 CCCOC(C(=O)OC1CCN(C)CC1)(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL1078261 5720 None 27 Human Functional pAC50 = 5.8 5.8 -1 11
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 367 7 0 4 4.0 CCCOC(C(=O)OC1CCN(C)CC1)(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
DB12278 5720 None 27 Human Functional pAC50 = 5.8 5.8 -1 11
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 367 7 0 4 4.0 CCCOC(C(=O)OC1CCN(C)CC1)(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
156419 938 None 48 Human Functional pAC50 = 4.8 4.8 -398 20
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 10.1038/s41467-023-40064-9
156419.0 938 None 48 Human Functional pAC50 = 4.8 4.8 -398 20
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 10.1038/s41467-023-40064-9
3308 938 None 48 Human Functional pAC50 = 4.8 4.8 -398 20
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 10.1038/s41467-023-40064-9
647 938 None 48 Human Functional pAC50 = 4.8 4.8 -398 20
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 10.1038/s41467-023-40064-9
CHEMBL1201284 938 None 48 Human Functional pAC50 = 4.8 4.8 -398 20
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 10.1038/s41467-023-40064-9
DB01012 938 None 48 Human Functional pAC50 = 4.8 4.8 -398 20
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 10.1038/s41467-023-40064-9
3157 1470 None 44 Human Functional pAC50 = 4.8 4.8 -16982 21
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1038/s41467-023-40064-9
3157.0 1470 None 44 Human Functional pAC50 = 4.8 4.8 -16982 21
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1038/s41467-023-40064-9
7170 1470 None 44 Human Functional pAC50 = 4.8 4.8 -16982 21
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1038/s41467-023-40064-9
954 1470 None 44 Human Functional pAC50 = 4.8 4.8 -16982 21
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1038/s41467-023-40064-9
CHEMBL707 1470 None 44 Human Functional pAC50 = 4.8 4.8 -16982 21
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1038/s41467-023-40064-9
DB00590 1470 None 44 Human Functional pAC50 = 4.8 4.8 -16982 21
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1038/s41467-023-40064-9
8609 14449 None 44 Human Functional pAC50 = 4.8 4.8 1 4
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 229 2 2 4 2.2 Nc1ccc(C(=O)Oc2ccccc2)c(O)c1 10.1038/s41467-023-40064-9
CHEMBL1200868 14449 None 44 Human Functional pAC50 = 4.8 4.8 1 4
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 229 2 2 4 2.2 Nc1ccc(C(=O)Oc2ccccc2)c(O)c1 10.1038/s41467-023-40064-9
4886 14115 None 19 Human Functional pAC50 = 4.8 4.8 -7 5
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 293 9 0 4 3.0 CCCCOc1ccc(OCCCN2CCOCC2)cc1 10.1038/s41467-023-40064-9
CHEMBL1198 14115 None 19 Human Functional pAC50 = 4.8 4.8 -7 5
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 293 9 0 4 3.0 CCCCOc1ccc(OCCCN2CCOCC2)cc1 10.1038/s41467-023-40064-9
16222096 80514 None 50 Human Functional pAC50 = 4.8 4.8 -64 7
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 531 4 3 4 3.8 O=C(c1ccc(F)c(F)c1Nc1ccc(I)cc1F)N1CC(O)([C@@H]2CCCCN2)C1 10.1038/s41467-023-40064-9
CHEMBL2146883 80514 None 50 Human Functional pAC50 = 4.8 4.8 -64 7
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 531 4 3 4 3.8 O=C(c1ccc(F)c(F)c1Nc1ccc(I)cc1F)N1CC(O)([C@@H]2CCCCN2)C1 10.1038/s41467-023-40064-9
3634 84142 None 43 Human Functional pAC50 = 4.8 4.8 -12 9
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 356 7 2 5 3.7 CCN(CC)CCNc1ccc(CO)c2sc3ccccc3c(=O)c12 10.1038/s41467-023-40064-9
CHEMBL22077 84142 None 43 Human Functional pAC50 = 4.8 4.8 -12 9
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 356 7 2 5 3.7 CCN(CC)CCNc1ccc(CO)c2sc3ccccc3c(=O)c12 10.1038/s41467-023-40064-9
2910 205143 None 46 Human Functional pAC50 = 4.8 4.8 - 1
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 389 2 3 5 1.2 NS(=O)(=O)c1cc2c(cc1Cl)NC(C1CC3C=CC1C3)NS2(=O)=O 10.1038/s41467-023-40064-9
CHEMBL61593 205143 None 46 Human Functional pAC50 = 4.8 4.8 - 1
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 389 2 3 5 1.2 NS(=O)(=O)c1cc2c(cc1Cl)NC(C1CC3C=CC1C3)NS2(=O)=O 10.1038/s41467-023-40064-9
2898 32659 None 43 Human Functional pAC50 = 4.8 4.8 -7 3
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 364 4 0 4 5.3 CC(=O)Oc1ccc(C(=C2CCCCC2)c2ccc(OC(C)=O)cc2)cc1 10.1038/s41467-023-40064-9
CHEMBL141305 32659 None 43 Human Functional pAC50 = 4.8 4.8 -7 3
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 364 4 0 4 5.3 CC(=O)Oc1ccc(C(=C2CCCCC2)c2ccc(OC(C)=O)cc2)cc1 10.1038/s41467-023-40064-9
2583 3776 None 69 Human Functional pAC50 = 4.8 4.8 -10000 16
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 514 7 1 5 7.3 CCCc1nc2c(n1Cc1ccc(cc1)c1ccccc1C(=O)O)cc(cc2C)c1nc2c(n1C)cccc2 10.1038/s41467-023-40064-9
592 3776 None 69 Human Functional pAC50 = 4.8 4.8 -10000 16
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 514 7 1 5 7.3 CCCc1nc2c(n1Cc1ccc(cc1)c1ccccc1C(=O)O)cc(cc2C)c1nc2c(n1C)cccc2 10.1038/s41467-023-40064-9
65999 3776 None 69 Human Functional pAC50 = 4.8 4.8 -10000 16
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 514 7 1 5 7.3 CCCc1nc2c(n1Cc1ccc(cc1)c1ccccc1C(=O)O)cc(cc2C)c1nc2c(n1C)cccc2 10.1038/s41467-023-40064-9
65999.0 3776 None 69 Human Functional pAC50 = 4.8 4.8 -10000 16
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 514 7 1 5 7.3 CCCc1nc2c(n1Cc1ccc(cc1)c1ccccc1C(=O)O)cc(cc2C)c1nc2c(n1C)cccc2 10.1038/s41467-023-40064-9
CHEMBL1017 3776 None 69 Human Functional pAC50 = 4.8 4.8 -10000 16
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 514 7 1 5 7.3 CCCc1nc2c(n1Cc1ccc(cc1)c1ccccc1C(=O)O)cc(cc2C)c1nc2c(n1C)cccc2 10.1038/s41467-023-40064-9
DB00966 3776 None 69 Human Functional pAC50 = 4.8 4.8 -10000 16
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 514 7 1 5 7.3 CCCc1nc2c(n1Cc1ccc(cc1)c1ccccc1C(=O)O)cc(cc2C)c1nc2c(n1C)cccc2 10.1038/s41467-023-40064-9
5744 8052 None 45 Human Functional pAC50 = 4.8 4.8 - 1
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 404 3 2 6 2.4 CC(=O)OCC(=O)[C@@]1(O)CC[C@H]2[C@@H]3CCC4=CC(=O)CC[C@]4(C)[C@H]3[C@@H](O)C[C@@]21C 10.1038/s41467-023-40064-9
CHEMBL1091 8052 None 45 Human Functional pAC50 = 4.8 4.8 - 1
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 404 3 2 6 2.4 CC(=O)OCC(=O)[C@@]1(O)CC[C@H]2[C@@H]3CCC4=CC(=O)CC[C@]4(C)[C@H]3[C@@H](O)C[C@@]21C 10.1038/s41467-023-40064-9
60663 175773 None 30 Human Functional pAC50 = 4.8 4.8 -23 12
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 495 11 1 5 5.3 COCC(=O)O[C@]1(CCN(C)CCCc2nc3ccccc3[nH]2)CCc2cc(F)ccc2[C@@H]1C(C)C 10.1038/s41467-023-40064-9
CHEMBL1421212 175773 None 30 Human Functional pAC50 = 4.8 4.8 -23 12
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 495 11 1 5 5.3 COCC(=O)O[C@]1(CCN(C)CCCc2nc3ccccc3[nH]2)CCc2cc(F)ccc2[C@@H]1C(C)C 10.1038/s41467-023-40064-9
CHEMBL1534525 175773 None 30 Human Functional pAC50 = 4.8 4.8 -23 12
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 495 11 1 5 5.3 COCC(=O)O[C@]1(CCN(C)CCCc2nc3ccccc3[nH]2)CCc2cc(F)ccc2[C@@H]1C(C)C 10.1038/s41467-023-40064-9
CHEMBL45816 175773 None 30 Human Functional pAC50 = 4.8 4.8 -23 12
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 495 11 1 5 5.3 COCC(=O)O[C@]1(CCN(C)CCCc2nc3ccccc3[nH]2)CCc2cc(F)ccc2[C@@H]1C(C)C 10.1038/s41467-023-40064-9
2683 102943 None 17 Human Functional pAC50 = 4.8 4.8 -75 24
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 304 15 0 0 6.5 CCCCCCCCCCCCCCCC[n+]1ccccc1 10.1038/s41467-023-40064-9
CHEMBL305906 102943 None 17 Human Functional pAC50 = 4.8 4.8 -75 24
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 304 15 0 0 6.5 CCCCCCCCCCCCCCCC[n+]1ccccc1 10.1038/s41467-023-40064-9
CHEMBL334255 102943 None 17 Human Functional pAC50 = 4.8 4.8 -75 24
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 304 15 0 0 6.5 CCCCCCCCCCCCCCCC[n+]1ccccc1 10.1038/s41467-023-40064-9
131411 15398 None 50 Human Functional pAC50 = 4.8 4.8 -6 10
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 476 7 1 6 5.2 CCOC(=O)c1c(CSc2ccccc2)n(C)c2cc(Br)c(O)c(CN(C)C)c12 10.1038/s41467-023-40064-9
28446253 15398 None 50 Human Functional pAC50 = 4.8 4.8 -6 10
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 476 7 1 6 5.2 CCOC(=O)c1c(CSc2ccccc2)n(C)c2cc(Br)c(O)c(CN(C)C)c12 10.1038/s41467-023-40064-9
CHEMBL1214598 15398 None 50 Human Functional pAC50 = 4.8 4.8 -6 10
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 476 7 1 6 5.2 CCOC(=O)c1c(CSc2ccccc2)n(C)c2cc(Br)c(O)c(CN(C)C)c12 10.1038/s41467-023-40064-9
5318 15583 None 40 Human Functional pAC50 = 4.8 4.8 -4 18
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 396 6 0 3 6.5 Clc1ccc(CSC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 10.1038/s41467-023-40064-9
CHEMBL1200348 15583 None 40 Human Functional pAC50 = 4.8 4.8 -4 18
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 396 6 0 3 6.5 Clc1ccc(CSC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 10.1038/s41467-023-40064-9
CHEMBL1221 15583 None 40 Human Functional pAC50 = 4.8 4.8 -4 18
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 396 6 0 3 6.5 Clc1ccc(CSC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 10.1038/s41467-023-40064-9
2324 77126 None 16 Human Functional pAC50 = 4.8 4.8 -11 11
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 505 7 1 8 4.2 COC(=O)C1=C(C)NC(C)=C(C(=O)OC2CCCN(Cc3ccccc3)C2)C1c1cccc([N+](=O)[O-])c1 10.1038/s41467-023-40064-9
CHEMBL2074972 77126 None 16 Human Functional pAC50 = 4.8 4.8 -11 11
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 505 7 1 8 4.2 COC(=O)C1=C(C)NC(C)=C(C(=O)OC2CCCN(Cc3ccccc3)C2)C1c1cccc([N+](=O)[O-])c1 10.1038/s41467-023-40064-9
11434515 261 None 6 Human Functional pAC50 = 7.8 7.8 -1 11
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1038/s41467-023-40064-9
11434515.0 261 None 6 Human Functional pAC50 = 7.8 7.8 -1 11
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1038/s41467-023-40064-9
11519741 261 None 6 Human Functional pAC50 = 7.8 7.8 -1 11
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1038/s41467-023-40064-9
4484 261 None 6 Human Functional pAC50 = 7.8 7.8 -1 11
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1038/s41467-023-40064-9
7449 261 None 6 Human Functional pAC50 = 7.8 7.8 -1 11
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1038/s41467-023-40064-9
CHEMBL1194325 261 None 6 Human Functional pAC50 = 7.8 7.8 -1 11
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1038/s41467-023-40064-9
DB08897 261 None 6 Human Functional pAC50 = 7.8 7.8 -1 11
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 484 9 1 6 4.7 O=C(C(c1cccs1)(c1cccs1)O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2 10.1038/s41467-023-40064-9
2895 206050 None 27 Human Functional pAC50 = 6.8 6.8 -1 15
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 275 3 0 1 4.6 CN(C)CCC=C1c2ccccc2C=Cc2ccccc21 10.1038/s41467-023-40064-9
2895.0 206050 None 27 Human Functional pAC50 = 6.8 6.8 -1 15
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 275 3 0 1 4.6 CN(C)CCC=C1c2ccccc2C=Cc2ccccc21 10.1038/s41467-023-40064-9
CHEMBL669 206050 None 27 Human Functional pAC50 = 6.8 6.8 -1 15
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 275 3 0 1 4.6 CN(C)CCC=C1c2ccccc2C=Cc2ccccc21 10.1038/s41467-023-40064-9
DB00924 206050 None 27 Human Functional pAC50 = 6.8 6.8 -1 15
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 275 3 0 1 4.6 CN(C)CCC=C1c2ccccc2C=Cc2ccccc21 10.1038/s41467-023-40064-9
242 470 None 70 Human Functional pAC50 = 5.8 5.8 -741 33
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
34 470 None 70 Human Functional pAC50 = 5.8 5.8 -741 33
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
60795 470 None 70 Human Functional pAC50 = 5.8 5.8 -741 33
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
60795.0 470 None 70 Human Functional pAC50 = 5.8 5.8 -741 33
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
CHEMBL1112 470 None 70 Human Functional pAC50 = 5.8 5.8 -741 33
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
DB01238 470 None 70 Human Functional pAC50 = 5.8 5.8 -741 33
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
1228 3866 None 24 Human Functional pAC50 = 5.8 5.8 -100 6
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 10.1038/s41467-023-40064-9
2763 3866 None 24 Human Functional pAC50 = 5.8 5.8 -100 6
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 10.1038/s41467-023-40064-9
5282443 3866 None 24 Human Functional pAC50 = 5.8 5.8 -100 6
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 10.1038/s41467-023-40064-9
5282443.0 3866 None 24 Human Functional pAC50 = 5.8 5.8 -100 6
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 10.1038/s41467-023-40064-9
CHEMBL855 3866 None 24 Human Functional pAC50 = 5.8 5.8 -100 6
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 10.1038/s41467-023-40064-9
DB00427 3866 None 24 Human Functional pAC50 = 5.8 5.8 -100 6
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 278 4 0 2 3.9 Cc1ccc(cc1)/C(=C\CN1CCCC1)/c1ccccn1 10.1038/s41467-023-40064-9
2335 11852 None 18 Human Functional pAC50 = 5.7 5.7 -14 34
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1038/s41467-023-40064-9
8478 11852 None 18 Human Functional pAC50 = 5.7 5.7 -14 34
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1038/s41467-023-40064-9
CHEMBL1182210 11852 None 18 Human Functional pAC50 = 5.7 5.7 -14 34
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1038/s41467-023-40064-9
CHEMBL221753 11852 None 18 Human Functional pAC50 = 5.7 5.7 -14 34
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1038/s41467-023-40064-9
3035016 12598 None 44 Human Functional pAC50 = 4.7 4.7 -1 3
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 483 3 5 10 0.6 CC(=O)[C@]1(N)Cc2c(O)c3c(c(O)c2[C@@H](O[C@H]2C[C@H](O)[C@H](O)CO2)C1)C(=O)c1ccccc1C3=O 10.1038/s41467-023-40064-9
CHEMBL1186894 12598 None 44 Human Functional pAC50 = 4.7 4.7 -1 3
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 483 3 5 10 0.6 CC(=O)[C@]1(N)Cc2c(O)c3c(c(O)c2[C@@H](O[C@H]2C[C@H](O)[C@H](O)CO2)C1)C(=O)c1ccccc1C3=O 10.1038/s41467-023-40064-9
34040 28093 None 52 Human Functional pAC50 = 5.7 5.7 -616 11
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 483 4 0 6 3.9 CO[C@]12C[C@@H](COC(=O)c3cncc(Br)c3)CN(C)[C@@H]1Cc1cn(C)c3cccc2c13 10.1038/s41467-023-40064-9
34040.0 28093 None 52 Human Functional pAC50 = 5.7 5.7 -616 11
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 483 4 0 6 3.9 CO[C@]12C[C@@H](COC(=O)c3cncc(Br)c3)CN(C)[C@@H]1Cc1cn(C)c3cccc2c13 10.1038/s41467-023-40064-9
CHEMBL1372950 28093 None 52 Human Functional pAC50 = 5.7 5.7 -616 11
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 483 4 0 6 3.9 CO[C@]12C[C@@H](COC(=O)c3cncc(Br)c3)CN(C)[C@@H]1Cc1cn(C)c3cccc2c13 10.1038/s41467-023-40064-9
DB00699 28093 None 52 Human Functional pAC50 = 5.7 5.7 -616 11
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 483 4 0 6 3.9 CO[C@]12C[C@@H](COC(=O)c3cncc(Br)c3)CN(C)[C@@H]1Cc1cn(C)c3cccc2c13 10.1038/s41467-023-40064-9
60151560 167540 None 37 Human Functional pAC50 = 4.7 4.7 -1 5
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 439 11 1 5 5.3 CCO[C@@H](Cc1ccc(OCCn2c(C)ccc2-c2ccc(SC)cc2)cc1)C(=O)O 10.1038/s41467-023-40064-9
CHEMBL4297530 167540 None 37 Human Functional pAC50 = 4.7 4.7 -1 5
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 439 11 1 5 5.3 CCO[C@@H](Cc1ccc(OCCn2c(C)ccc2-c2ccc(SC)cc2)cc1)C(=O)O 10.1038/s41467-023-40064-9
2247 505 None 55 Human Functional pAC50 = 4.7 4.7 -338 42
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
249 505 None 55 Human Functional pAC50 = 4.7 4.7 -338 42
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
2603 505 None 55 Human Functional pAC50 = 4.7 4.7 -338 42
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
CHEMBL296419 505 None 55 Human Functional pAC50 = 4.7 4.7 -338 42
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
DB00637 505 None 55 Human Functional pAC50 = 4.7 4.7 -338 42
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
123603 883 None 21 Human Functional pAC50 = 4.7 4.7 -64 5
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 199 0 0 3 1.6 CC1SCC2(O1)CN1CCC2CC1 10.1038/s41467-023-40064-9
2684 883 None 21 Human Functional pAC50 = 4.7 4.7 -64 5
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 199 0 0 3 1.6 CC1SCC2(O1)CN1CCC2CC1 10.1038/s41467-023-40064-9
2684.0 883 None 21 Human Functional pAC50 = 4.7 4.7 -64 5
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 199 0 0 3 1.6 CC1SCC2(O1)CN1CCC2CC1 10.1038/s41467-023-40064-9
584 883 None 21 Human Functional pAC50 = 4.7 4.7 -64 5
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 199 0 0 3 1.6 CC1SCC2(O1)CN1CCC2CC1 10.1038/s41467-023-40064-9
9658 883 None 21 Human Functional pAC50 = 4.7 4.7 -64 5
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 199 0 0 3 1.6 CC1SCC2(O1)CN1CCC2CC1 10.1038/s41467-023-40064-9
CHEMBL168815 883 None 21 Human Functional pAC50 = 4.7 4.7 -64 5
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 199 0 0 3 1.6 CC1SCC2(O1)CN1CCC2CC1 10.1038/s41467-023-40064-9
DB00185 883 None 21 Human Functional pAC50 = 4.7 4.7 -64 5
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 199 0 0 3 1.6 CC1SCC2(O1)CN1CCC2CC1 10.1038/s41467-023-40064-9
118422671 2757 None 41 Human Functional pAC50 = 4.7 4.7 -6309 23
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
1887 2757 None 41 Human Functional pAC50 = 4.7 4.7 -6309 23
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
189562 2757 None 41 Human Functional pAC50 = 4.7 4.7 -6309 23
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
189562.0 2757 None 41 Human Functional pAC50 = 4.7 4.7 -6309 23
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
71301 2757 None 41 Human Functional pAC50 = 4.7 4.7 -6309 23
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
71301.0 2757 None 41 Human Functional pAC50 = 4.7 4.7 -6309 23
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
7246 2757 None 41 Human Functional pAC50 = 4.7 4.7 -6309 23
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
9844194 2757 None 41 Human Functional pAC50 = 4.7 4.7 -6309 23
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
9844194.0 2757 None 41 Human Functional pAC50 = 4.7 4.7 -6309 23
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
CHEMBL2365658 2757 None 41 Human Functional pAC50 = 4.7 4.7 -6309 23
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
CHEMBL3526436 2757 None 41 Human Functional pAC50 = 4.7 4.7 -6309 23
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
CHEMBL434394 2757 None 41 Human Functional pAC50 = 4.7 4.7 -6309 23
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
DB04861 2757 None 41 Human Functional pAC50 = 4.7 4.7 -6309 23
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
26248 161633 None 72 Human Functional pAC50 = 4.7 4.7 -1 11
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 368 3 1 7 2.0 CC(=O)Oc1cccc2c1C(=O)c1c(OC(C)=O)cc(C(=O)O)cc1C2=O 10.1038/s41467-023-40064-9
CHEMBL41286 161633 None 72 Human Functional pAC50 = 4.7 4.7 -1 11
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 368 3 1 7 2.0 CC(=O)Oc1cccc2c1C(=O)c1c(OC(C)=O)cc(C(=O)O)cc1C2=O 10.1038/s41467-023-40064-9
4642 42000 None 22 Human Functional pAC50 = 7.7 7.7 2 3
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 344 5 1 5 2.7 CN1CCCN=C1COC(=O)C(O)(c1ccccc1)C1CCCCC1 10.1038/s41467-023-40064-9
4642.0 42000 None 22 Human Functional pAC50 = 7.7 7.7 2 3
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 344 5 1 5 2.7 CN1CCCN=C1COC(=O)C(O)(c1ccccc1)C1CCCCC1 10.1038/s41467-023-40064-9
CHEMBL1495 42000 None 22 Human Functional pAC50 = 7.7 7.7 2 3
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 344 5 1 5 2.7 CN1CCCN=C1COC(=O)C(O)(c1ccccc1)C1CCCCC1 10.1038/s41467-023-40064-9
DB00383 42000 None 22 Human Functional pAC50 = 7.7 7.7 2 3
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 344 5 1 5 2.7 CN1CCCN=C1COC(=O)C(O)(c1ccccc1)C1CCCCC1 10.1038/s41467-023-40064-9
2337 3256 None 51 Human Functional pAC50 = 5.7 5.7 -162 29
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
50 3256 None 51 Human Functional pAC50 = 5.7 5.7 -162 29
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
5002 3256 None 51 Human Functional pAC50 = 5.7 5.7 -162 29
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
5002.0 3256 None 51 Human Functional pAC50 = 5.7 5.7 -162 29
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL716 3256 None 51 Human Functional pAC50 = 5.7 5.7 -162 29
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
DB01224 3256 None 51 Human Functional pAC50 = 5.7 5.7 -162 29
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
3117 210300 None 60 Human Functional pAC50 = 4.7 4.7 -26 24
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC 10.1038/s41467-023-40064-9
CHEMBL964 210300 None 60 Human Functional pAC50 = 4.7 4.7 -26 24
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC 10.1038/s41467-023-40064-9
5568 199956 None 21 Human Functional pAC50 = 6.7 6.7 -63 13
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 352 4 0 3 5.3 CN(C)CCCN1c2ccccc2Sc2ccc(C(F)(F)F)cc21 10.1038/s41467-023-40064-9
5568.0 199956 None 21 Human Functional pAC50 = 6.7 6.7 -63 13
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 352 4 0 3 5.3 CN(C)CCCN1c2ccccc2Sc2ccc(C(F)(F)F)cc21 10.1038/s41467-023-40064-9
66069 199956 None 21 Human Functional pAC50 = 6.7 6.7 -63 13
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 352 4 0 3 5.3 CN(C)CCCN1c2ccccc2Sc2ccc(C(F)(F)F)cc21 10.1038/s41467-023-40064-9
CHEMBL1201102 199956 None 21 Human Functional pAC50 = 6.7 6.7 -63 13
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 352 4 0 3 5.3 CN(C)CCCN1c2ccccc2Sc2ccc(C(F)(F)F)cc21 10.1038/s41467-023-40064-9
CHEMBL570 199956 None 21 Human Functional pAC50 = 6.7 6.7 -63 13
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 352 4 0 3 5.3 CN(C)CCCN1c2ccccc2Sc2ccc(C(F)(F)F)cc21 10.1038/s41467-023-40064-9
DB00508 199956 None 21 Human Functional pAC50 = 6.7 6.7 -63 13
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 352 4 0 3 5.3 CN(C)CCCN1c2ccccc2Sc2ccc(C(F)(F)F)cc21 10.1038/s41467-023-40064-9
16362 3125 None 49 Human Functional pAC50 = 5.7 5.7 -208 35
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
16362.0 3125 None 49 Human Functional pAC50 = 5.7 5.7 -208 35
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
2172 3125 None 49 Human Functional pAC50 = 5.7 5.7 -208 35
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
90 3125 None 49 Human Functional pAC50 = 5.7 5.7 -208 35
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL1423 3125 None 49 Human Functional pAC50 = 5.7 5.7 -208 35
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
DB01100 3125 None 49 Human Functional pAC50 = 5.7 5.7 -208 35
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
4034 55838 None 37 Human Functional pAC50 = 4.7 4.7 -45 18
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 390 5 0 2 5.6 Cc1cccc(CN2CCN(C(c3ccccc3)c3ccc(Cl)cc3)CC2)c1 10.1038/s41467-023-40064-9
4034.0 55838 None 37 Human Functional pAC50 = 4.7 4.7 -45 18
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 390 5 0 2 5.6 Cc1cccc(CN2CCN(C(c3ccccc3)c3ccc(Cl)cc3)CC2)c1 10.1038/s41467-023-40064-9
CHEMBL1623 55838 None 37 Human Functional pAC50 = 4.7 4.7 -45 18
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 390 5 0 2 5.6 Cc1cccc(CN2CCN(C(c3ccccc3)c3ccc(Cl)cc3)CC2)c1 10.1038/s41467-023-40064-9
DB00737 55838 None 37 Human Functional pAC50 = 4.7 4.7 -45 18
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 390 5 0 2 5.6 Cc1cccc(CN2CCN(C(c3ccccc3)c3ccc(Cl)cc3)CC2)c1 10.1038/s41467-023-40064-9
68921 78271 None 31 Human Functional pAC50 = 4.7 4.7 - 1
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 460 5 1 7 3.3 CCC(=O)O[C@]1(C(=O)COC(C)=O)CC[C@H]2[C@@H]3CCC4=CC(=O)CC[C@]4(C)[C@H]3[C@@H](O)C[C@@]21C 10.1038/s41467-023-40064-9
CHEMBL2106309 78271 None 31 Human Functional pAC50 = 4.7 4.7 - 1
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 460 5 1 7 3.3 CCC(=O)O[C@]1(C(=O)COC(C)=O)CC[C@H]2[C@@H]3CCC4=CC(=O)CC[C@]4(C)[C@H]3[C@@H](O)C[C@@]21C 10.1038/s41467-023-40064-9
22530 56146 None 40 Human Functional pAC50 = 5.7 5.7 -7 9
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 276 2 0 2 3.7 CN1CCc2c(c3ccccc3n2Cc2ccccc2)C1 10.1038/s41467-023-40064-9
CHEMBL1600878 56146 None 40 Human Functional pAC50 = 5.7 5.7 -7 9
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 276 2 0 2 3.7 CN1CCc2c(c3ccccc3n2Cc2ccccc2)C1 10.1038/s41467-023-40064-9
CHEMBL1625607 56146 None 40 Human Functional pAC50 = 5.7 5.7 -7 9
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 276 2 0 2 3.7 CN1CCc2c(c3ccccc3n2Cc2ccccc2)C1 10.1038/s41467-023-40064-9
3678 94845 None 37 Human Functional pAC50 = 6.7 6.7 -6 8
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 281 9 0 1 4.6 CCN(CCCc1ccccc1)CCCc1ccccc1 10.1038/s41467-023-40064-9
3678.0 94845 None 37 Human Functional pAC50 = 6.7 6.7 -6 8
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 281 9 0 1 4.6 CCN(CCCc1ccccc1)CCCc1ccccc1 10.1038/s41467-023-40064-9
CHEMBL253371 94845 None 37 Human Functional pAC50 = 6.7 6.7 -6 8
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 281 9 0 1 4.6 CCN(CCCc1ccccc1)CCCc1ccccc1 10.1038/s41467-023-40064-9
DB01616 94845 None 37 Human Functional pAC50 = 6.7 6.7 -6 8
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 281 9 0 1 4.6 CCN(CCCc1ccccc1)CCCc1ccccc1 10.1038/s41467-023-40064-9
21700 593 None 36 Human Functional pAC50 = 4.7 4.7 -3801 5
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 520 6 1 7 4.1 CCC(=O)O[C@@]1([C@@H](C)C[C@@H]2[C@]1(C)C[C@H](O)[C@]1([C@H]2CCC2=CC(=O)C=C[C@]12C)Cl)C(=O)COC(=O)CC 10.1038/s41467-023-40064-9
294 593 None 36 Human Functional pAC50 = 4.7 4.7 -3801 5
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 520 6 1 7 4.1 CCC(=O)O[C@@]1([C@@H](C)C[C@@H]2[C@]1(C)C[C@H](O)[C@]1([C@H]2CCC2=CC(=O)C=C[C@]12C)Cl)C(=O)COC(=O)CC 10.1038/s41467-023-40064-9
5894 593 None 36 Human Functional pAC50 = 4.7 4.7 -3801 5
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 520 6 1 7 4.1 CCC(=O)O[C@@]1([C@@H](C)C[C@@H]2[C@]1(C)C[C@H](O)[C@]1([C@H]2CCC2=CC(=O)C=C[C@]12C)Cl)C(=O)COC(=O)CC 10.1038/s41467-023-40064-9
CHEMBL1200500 593 None 36 Human Functional pAC50 = 4.7 4.7 -3801 5
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 520 6 1 7 4.1 CCC(=O)O[C@@]1([C@@H](C)C[C@@H]2[C@]1(C)C[C@H](O)[C@]1([C@H]2CCC2=CC(=O)C=C[C@]12C)Cl)C(=O)COC(=O)CC 10.1038/s41467-023-40064-9
DB00394 593 None 36 Human Functional pAC50 = 4.7 4.7 -3801 5
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 520 6 1 7 4.1 CCC(=O)O[C@@]1([C@@H](C)C[C@@H]2[C@]1(C)C[C@H](O)[C@]1([C@H]2CCC2=CC(=O)C=C[C@]12C)Cl)C(=O)COC(=O)CC 10.1038/s41467-023-40064-9
6834 208010 None 36 Human Functional pAC50 = 4.7 4.7 -380 6
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 318 5 0 2 3.9 CN(C)CCC(c1ccc(Br)cc1)c1ccccn1 10.1038/s41467-023-40064-9
6834.0 208010 None 36 Human Functional pAC50 = 4.7 4.7 -380 6
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 318 5 0 2 3.9 CN(C)CCC(c1ccc(Br)cc1)c1ccccn1 10.1038/s41467-023-40064-9
CHEMBL811 208010 None 36 Human Functional pAC50 = 4.7 4.7 -380 6
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 318 5 0 2 3.9 CN(C)CCC(c1ccc(Br)cc1)c1ccccn1 10.1038/s41467-023-40064-9
DB00835 208010 None 36 Human Functional pAC50 = 4.7 4.7 -380 6
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 318 5 0 2 3.9 CN(C)CCC(c1ccc(Br)cc1)c1ccccn1 10.1038/s41467-023-40064-9
10453870 73688 None 45 Human Functional pAC50 = 4.7 4.7 1 2
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 404 4 4 6 2.1 OC[C@H]1O[C@@H](c2ccc(F)c(Cc3cc4ccccc4s3)c2)[C@H](O)[C@@H](O)[C@@H]1O 10.1038/s41467-023-40064-9
CHEMBL2018096 73688 None 45 Human Functional pAC50 = 4.7 4.7 1 2
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 404 4 4 6 2.1 OC[C@H]1O[C@@H](c2ccc(F)c(Cc3cc4ccccc4s3)c2)[C@H](O)[C@@H](O)[C@@H]1O 10.1038/s41467-023-40064-9
15942715 78222 None 18 Human Functional pAC50 = 4.7 4.7 -2 3
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 446 5 1 5 4.0 CCCCOC(=O)C(=O)[C@H]1[C@H](C)C[C@H]2[C@@H]3C[C@H](F)C4=CC(=O)C=C[C@]4(C)[C@H]3[C@@H](O)C[C@@]21C 10.1038/s41467-023-40064-9
CHEMBL2105087 78222 None 18 Human Functional pAC50 = 4.7 4.7 -2 3
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 446 5 1 5 4.0 CCCCOC(=O)C(=O)[C@H]1[C@H](C)C[C@H]2[C@@H]3C[C@H](F)C4=CC(=O)C=C[C@]4(C)[C@H]3[C@@H](O)C[C@@]21C 10.1038/s41467-023-40064-9
11693 1827 None 12 Human Functional pAC50 = 8.6 8.6 -4 7
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1038/s41467-023-40064-9
3494 1827 None 12 Human Functional pAC50 = 8.6 8.6 -4 7
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1038/s41467-023-40064-9
3494.0 1827 None 12 Human Functional pAC50 = 8.6 8.6 -4 7
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1038/s41467-023-40064-9
4302 1827 None 12 Human Functional pAC50 = 8.6 8.6 -4 7
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1038/s41467-023-40064-9
7459 1827 None 12 Human Functional pAC50 = 8.6 8.6 -4 7
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1038/s41467-023-40064-9
9933193 1827 None 12 Human Functional pAC50 = 8.6 8.6 -4 7
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1038/s41467-023-40064-9
9933193.0 1827 None 12 Human Functional pAC50 = 8.6 8.6 -4 7
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1038/s41467-023-40064-9
CHEMBL1201335 1827 None 12 Human Functional pAC50 = 8.6 8.6 -4 7
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1038/s41467-023-40064-9
DB00986 1827 None 12 Human Functional pAC50 = 8.6 8.6 -4 7
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1038/s41467-023-40064-9
5284632 67423 None 10 Human Functional pAC50 = 8.6 8.6 1 4
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 392 4 1 3 3.8 O=C(O[C@@H]1C[C@@H]2CC[C@H](C1)[N+]21CCCC1)C(O)(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
5284632.0 67423 None 10 Human Functional pAC50 = 8.6 8.6 1 4
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 392 4 1 3 3.8 O=C(O[C@@H]1C[C@@H]2CC[C@H](C1)[N+]21CCCC1)C(O)(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL1888176 67423 None 10 Human Functional pAC50 = 8.6 8.6 1 4
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 392 4 1 3 3.8 O=C(O[C@@H]1C[C@@H]2CC[C@H](C1)[N+]21CCCC1)C(O)(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL3084748 67423 None 10 Human Functional pAC50 = 8.6 8.6 1 4
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 392 4 1 3 3.8 O=C(O[C@@H]1C[C@@H]2CC[C@H](C1)[N+]21CCCC1)C(O)(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
DB00209 67423 None 10 Human Functional pAC50 = 8.6 8.6 1 4
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 392 4 1 3 3.8 O=C(O[C@@H]1C[C@@H]2CC[C@H](C1)[N+]21CCCC1)C(O)(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
3000322 3562 None 29 Human Functional pAC50 = 8.6 8.6 -1 4
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 303 4 1 5 0.9 OC[C@H](c1ccccc1)C(=O)O[C@@H]1C[C@H]2N([C@@H](C1)[C@H]1[C@@H]2O1)C 10.1038/s41467-023-40064-9
3000322.0 3562 None 29 Human Functional pAC50 = 8.6 8.6 -1 4
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 303 4 1 5 0.9 OC[C@H](c1ccccc1)C(=O)O[C@@H]1C[C@H]2N([C@@H](C1)[C@H]1[C@@H]2O1)C 10.1038/s41467-023-40064-9
330 3562 None 29 Human Functional pAC50 = 8.6 8.6 -1 4
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 303 4 1 5 0.9 OC[C@H](c1ccccc1)C(=O)O[C@@H]1C[C@H]2N([C@@H](C1)[C@H]1[C@@H]2O1)C 10.1038/s41467-023-40064-9
CHEMBL569713 3562 None 29 Human Functional pAC50 = 8.6 8.6 -1 4
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 303 4 1 5 0.9 OC[C@H](c1ccccc1)C(=O)O[C@@H]1C[C@H]2N([C@@H](C1)[C@H]1[C@@H]2O1)C 10.1038/s41467-023-40064-9
DB00747 3562 None 29 Human Functional pAC50 = 8.6 8.6 -1 4
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 303 4 1 5 0.9 OC[C@H](c1ccccc1)C(=O)O[C@@H]1C[C@H]2N([C@@H](C1)[C@H]1[C@@H]2O1)C 10.1038/s41467-023-40064-9
25897919 55668 None 12 Human Functional pAC50 = 8.6 8.6 -2 5
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1038/s41467-023-40064-9
657308 55668 None 12 Human Functional pAC50 = 8.6 8.6 -2 5
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1038/s41467-023-40064-9
657309 55668 None 12 Human Functional pAC50 = 8.6 8.6 -2 5
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1038/s41467-023-40064-9
CHEMBL1621597 55668 None 12 Human Functional pAC50 = 8.6 8.6 -2 5
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1038/s41467-023-40064-9
DB00332 55668 None 12 Human Functional pAC50 = 8.6 8.6 -2 5
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1038/s41467-023-40064-9
2705 3842 None 44 Human Functional pAC50 = 7.7 7.7 -1 12
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1038/s41467-023-40064-9
360 3842 None 44 Human Functional pAC50 = 7.7 7.7 -1 12
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1038/s41467-023-40064-9
443879 3842 None 44 Human Functional pAC50 = 7.7 7.7 -1 12
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1038/s41467-023-40064-9
443879.0 3842 None 44 Human Functional pAC50 = 7.7 7.7 -1 12
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1038/s41467-023-40064-9
CHEMBL1382 3842 None 44 Human Functional pAC50 = 7.7 7.7 -1 12
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1038/s41467-023-40064-9
DB01036 3842 None 44 Human Functional pAC50 = 7.7 7.7 -1 12
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1038/s41467-023-40064-9
2865 4143 None 47 Human Functional pAC50 = 4.7 4.7 -6760 20
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
59 4143 None 47 Human Functional pAC50 = 4.7 4.7 -6760 20
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
60854 4143 None 47 Human Functional pAC50 = 4.7 4.7 -6760 20
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
60854.0 4143 None 47 Human Functional pAC50 = 4.7 4.7 -6760 20
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL708 4143 None 47 Human Functional pAC50 = 4.7 4.7 -6760 20
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
DB00246 4143 None 47 Human Functional pAC50 = 4.7 4.7 -6760 20
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
2448 99377 None 50 Human Functional pAC50 = 4.7 4.7 -912 15
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 419 6 1 3 4.5 O=C(CCCN1CCC(O)(c2ccc(Br)cc2)CC1)c1ccc(F)cc1 10.1038/s41467-023-40064-9
2448.0 99377 None 50 Human Functional pAC50 = 4.7 4.7 -912 15
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 419 6 1 3 4.5 O=C(CCCN1CCC(O)(c2ccc(Br)cc2)CC1)c1ccc(F)cc1 10.1038/s41467-023-40064-9
CHEMBL28218 99377 None 50 Human Functional pAC50 = 4.7 4.7 -912 15
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 419 6 1 3 4.5 O=C(CCCN1CCC(O)(c2ccc(Br)cc2)CC1)c1ccc(F)cc1 10.1038/s41467-023-40064-9
DB12401 99377 None 50 Human Functional pAC50 = 4.7 4.7 -912 15
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 419 6 1 3 4.5 O=C(CCCN1CCC(O)(c2ccc(Br)cc2)CC1)c1ccc(F)cc1 10.1038/s41467-023-40064-9
68704 100787 None 27 Human Functional pAC50 = 4.7 4.7 - 1
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 221 4 2 2 2.5 CC(C)Cc1ccc(C(C)C(=O)NO)cc1 10.1038/s41467-023-40064-9
CHEMBL292707 100787 None 27 Human Functional pAC50 = 4.7 4.7 - 1
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 221 4 2 2 2.5 CC(C)Cc1ccc(C(C)C(=O)NO)cc1 10.1038/s41467-023-40064-9
7019 168079 None 72 Human Functional pAC50 = 4.7 4.7 -4 8
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 194 0 1 2 3.0 Nc1c2ccccc2nc2ccccc12 10.1038/s41467-023-40064-9
CHEMBL1308088 168079 None 72 Human Functional pAC50 = 4.7 4.7 -4 8
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 194 0 1 2 3.0 Nc1c2ccccc2nc2ccccc12 10.1038/s41467-023-40064-9
CHEMBL43184 168079 None 72 Human Functional pAC50 = 4.7 4.7 -4 8
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 194 0 1 2 3.0 Nc1c2ccccc2nc2ccccc12 10.1038/s41467-023-40064-9
5329102 194838 None 50 Human Functional pAC50 = 5.7 5.7 -18 37
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 398 7 3 3 3.3 CCN(CC)CCNC(=O)c1c(C)[nH]c(/C=C2\C(=O)Nc3ccc(F)cc32)c1C 10.1038/s41467-023-40064-9
CHEMBL535 194838 None 50 Human Functional pAC50 = 5.7 5.7 -18 37
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 398 7 3 3 3.3 CCN(CC)CCNC(=O)c1c(C)[nH]c(/C=C2\C(=O)Nc3ccc(F)cc32)c1C 10.1038/s41467-023-40064-9
4044 206306 None 69 Human Functional pAC50 = 4.7 4.7 - 1
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 241 3 2 2 3.7 Cc1cccc(Nc2ccccc2C(=O)O)c1C 10.1038/s41467-023-40064-9
CHEMBL686 206306 None 69 Human Functional pAC50 = 4.7 4.7 - 1
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 241 3 2 2 3.7 Cc1cccc(Nc2ccccc2C(=O)O)c1C 10.1038/s41467-023-40064-9
4822 45046 None 35 Human Functional pAC50 = 7.7 7.7 -3 10
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 293 0 0 2 4.7 CN1CCC(=C2c3ccccc3Sc3ccccc32)CC1 10.1038/s41467-023-40064-9
CHEMBL152408 45046 None 35 Human Functional pAC50 = 7.7 7.7 -3 10
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 293 0 0 2 4.7 CN1CCC(=C2c3ccccc3Sc3ccccc32)CC1 10.1038/s41467-023-40064-9
5732 209393 None 28 Human Functional pAC50 = 6.7 6.7 32 4
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 307 3 0 3 3.2 Cc1ccc(-c2nc3ccc(C)cn3c2CC(=O)N(C)C)cc1 10.1038/s41467-023-40064-9
CHEMBL911 209393 None 28 Human Functional pAC50 = 6.7 6.7 32 4
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 307 3 0 3 3.2 Cc1ccc(-c2nc3ccc(C)cn3c2CC(=O)N(C)C)cc1 10.1038/s41467-023-40064-9
6075 150196 None 34 Human Functional pAC50 = 6.7 6.7 -28 20
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 310 2 0 3 4.6 CN1CCCC(CN2c3ccccc3Sc3ccccc32)C1 10.1038/s41467-023-40064-9
CHEMBL395110 150196 None 34 Human Functional pAC50 = 6.7 6.7 -28 20
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 310 2 0 3 4.6 CN1CCCC(CN2c3ccccc3Sc3ccccc32)C1 10.1038/s41467-023-40064-9
4121 50850 None 43 Human Functional pAC50 = 4.7 4.7 1 2
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 359 2 2 5 0.6 CN1C(CCl)Nc2cc(Cl)c(S(N)(=O)=O)cc2S1(=O)=O 10.1038/s41467-023-40064-9
CHEMBL1577 50850 None 43 Human Functional pAC50 = 4.7 4.7 1 2
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 359 2 2 5 0.6 CN1C(CCl)Nc2cc(Cl)c(S(N)(=O)=O)cc2S1(=O)=O 10.1038/s41467-023-40064-9
5284616 161721 None 39 Human Functional pAC50 = 4.7 4.7 -138 8
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 914 6 3 13 6.2 CO[C@H]1C[C@@H]2CC[C@@H](C)[C@@](O)(O2)C(=O)C(=O)N2CCCC[C@H]2C(=O)O[C@H]([C@H](C)C[C@@H]2CC[C@@H](O)[C@H](OC)C2)CC(=O)[C@H](C)/C=C(\C)[C@@H](O)[C@@H](OC)C(=O)[C@H](C)C[C@H](C)/C=C/C=C/C=C/1C 10.1038/s41467-023-40064-9
CHEMBL413 161721 None 39 Human Functional pAC50 = 4.7 4.7 -138 8
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 914 6 3 13 6.2 CO[C@H]1C[C@@H]2CC[C@@H](C)[C@@](O)(O2)C(=O)C(=O)N2CCCC[C@H]2C(=O)O[C@H]([C@H](C)C[C@@H]2CC[C@@H](O)[C@H](OC)C2)CC(=O)[C@H](C)/C=C(\C)[C@@H](O)[C@@H](OC)C(=O)[C@H](C)C[C@H](C)/C=C/C=C/C=C/1C 10.1038/s41467-023-40064-9
460612 208502 None 43 Human Functional pAC50 = 4.7 4.7 -1 5
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 304 8 2 3 1.9 N[C@@H](Cc1ccc(N(CCCl)CCCl)cc1)C(=O)O 10.1038/s41467-023-40064-9
6918992 208502 None 43 Human Functional pAC50 = 4.7 4.7 -1 5
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 304 8 2 3 1.9 N[C@@H](Cc1ccc(N(CCCl)CCCl)cc1)C(=O)O 10.1038/s41467-023-40064-9
CHEMBL852 208502 None 43 Human Functional pAC50 = 4.7 4.7 -1 5
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 304 8 2 3 1.9 N[C@@H](Cc1ccc(N(CCCl)CCCl)cc1)C(=O)O 10.1038/s41467-023-40064-9
34633 5466 None 43 Human Functional pAC50 = 4.7 4.7 -1 2
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 427 5 1 6 4.1 CCOC(=O)Nc1ccc2c(c1)N(C(=O)CCN1CCOCC1)c1ccccc1S2 10.1038/s41467-023-40064-9
CHEMBL1075 5466 None 43 Human Functional pAC50 = 4.7 4.7 -1 2
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 427 5 1 6 4.1 CCOC(=O)Nc1ccc2c(c1)N(C(=O)CCN1CCOCC1)c1ccccc1S2 10.1038/s41467-023-40064-9
154257 178724 None 43 Human Functional pAC50 = 4.7 4.7 -97 19
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 470 7 2 5 6.3 Cc1c(-c2ccc(O)cc2)n(Cc2ccc(OCCN3CCCCCC3)cc2)c2ccc(O)cc12 10.1038/s41467-023-40064-9
CHEMBL46740 178724 None 43 Human Functional pAC50 = 4.7 4.7 -97 19
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 470 7 2 5 6.3 Cc1c(-c2ccc(O)cc2)n(Cc2ccc(OCCN3CCCCCC3)cc2)c2ccc(O)cc12 10.1038/s41467-023-40064-9
5282592 14482 None 2 Human Functional pAC50 = 6.7 6.7 -1 2
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 290 3 1 3 2.0 C[N+]1(C)[C@@H]2CC[C@H]1C[C@@H](OC(=O)C(O)c1ccccc1)C2 10.1038/s41467-023-40064-9
5282592.0 14482 None 2 Human Functional pAC50 = 6.7 6.7 -1 2
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 290 3 1 3 2.0 C[N+]1(C)[C@@H]2CC[C@H]1C[C@@H](OC(=O)C(O)c1ccccc1)C2 10.1038/s41467-023-40064-9
6646 14482 None 2 Human Functional pAC50 = 6.7 6.7 -1 2
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 290 3 1 3 2.0 C[N+]1(C)[C@@H]2CC[C@H]1C[C@@H](OC(=O)C(O)c1ccccc1)C2 10.1038/s41467-023-40064-9
6646.0 14482 None 2 Human Functional pAC50 = 6.7 6.7 -1 2
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 290 3 1 3 2.0 C[N+]1(C)[C@@H]2CC[C@H]1C[C@@H](OC(=O)C(O)c1ccccc1)C2 10.1038/s41467-023-40064-9
CHEMBL1200851 14482 None 2 Human Functional pAC50 = 6.7 6.7 -1 2
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 290 3 1 3 2.0 C[N+]1(C)[C@@H]2CC[C@H]1C[C@@H](OC(=O)C(O)c1ccccc1)C2 10.1038/s41467-023-40064-9
CHEMBL1201235 14482 None 2 Human Functional pAC50 = 6.7 6.7 -1 2
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 290 3 1 3 2.0 C[N+]1(C)[C@@H]2CC[C@H]1C[C@@H](OC(=O)C(O)c1ccccc1)C2 10.1038/s41467-023-40064-9
CHEMBL1615437 14482 None 2 Human Functional pAC50 = 6.7 6.7 -1 2
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 290 3 1 3 2.0 C[N+]1(C)[C@@H]2CC[C@H]1C[C@@H](OC(=O)C(O)c1ccccc1)C2 10.1038/s41467-023-40064-9
DB00725 14482 None 2 Human Functional pAC50 = 6.7 6.7 -1 2
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 290 3 1 3 2.0 C[N+]1(C)[C@@H]2CC[C@H]1C[C@@H](OC(=O)C(O)c1ccccc1)C2 10.1038/s41467-023-40064-9
124087 1389 None 72 Human Functional pAC50 = 5.7 5.7 -12 27
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1038/s41467-023-40064-9
124087.0 1389 None 72 Human Functional pAC50 = 5.7 5.7 -12 27
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1038/s41467-023-40064-9
7157 1389 None 72 Human Functional pAC50 = 5.7 5.7 -12 27
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1038/s41467-023-40064-9
814 1389 None 72 Human Functional pAC50 = 5.7 5.7 -12 27
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1038/s41467-023-40064-9
CHEMBL1172 1389 None 72 Human Functional pAC50 = 5.7 5.7 -12 27
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1038/s41467-023-40064-9
DB00967 1389 None 72 Human Functional pAC50 = 5.7 5.7 -12 27
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1038/s41467-023-40064-9
2580 78426 None 10 Human Functional pAC50 = 4.7 4.7 -1047 10
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 446 6 1 4 4.1 NC(=O)C1(N2CCCCC2)CCN(CCCN2c3ccccc3CCc3ccccc32)CC1 10.1038/s41467-023-40064-9
CHEMBL2110775 78426 None 10 Human Functional pAC50 = 4.7 4.7 -1047 10
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 446 6 1 4 4.1 NC(=O)C1(N2CCCCC2)CCN(CCCN2c3ccccc3CCc3ccccc32)CC1 10.1038/s41467-023-40064-9
23497 22900 None 21 Human Functional pAC50 = 4.7 4.7 -4 3
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 211 3 3 5 0.1 COC(=O)[C@@H](N)Cc1ccc(O)c(O)c1 10.1038/s41467-023-40064-9
CHEMBL1328898 22900 None 21 Human Functional pAC50 = 4.7 4.7 -4 3
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 211 3 3 5 0.1 COC(=O)[C@@H](N)Cc1ccc(O)c(O)c1 10.1038/s41467-023-40064-9
1599 2341 None 28 Human Functional pAC50 = 4.7 4.7 -12022 32
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
3955 2341 None 28 Human Functional pAC50 = 4.7 4.7 -12022 32
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
3955.0 2341 None 28 Human Functional pAC50 = 4.7 4.7 -12022 32
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
7215 2341 None 28 Human Functional pAC50 = 4.7 4.7 -12022 32
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL841 2341 None 28 Human Functional pAC50 = 4.7 4.7 -12022 32
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
DB00836 2341 None 28 Human Functional pAC50 = 4.7 4.7 -12022 32
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
10311 57517 None 24 Human Functional pAC50 = 4.7 4.7 -11 2
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 398 4 4 9 0.3 Nc1nc(N)nc(Nc2ccc([As]3SCC(CO)S3)cc2)n1 10.1038/s41467-023-40064-9
CHEMBL166 57517 None 24 Human Functional pAC50 = 4.7 4.7 -11 2
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 398 4 4 9 0.3 Nc1nc(N)nc(Nc2ccc([As]3SCC(CO)S3)cc2)n1 10.1038/s41467-023-40064-9
25295 13625 None 28 Human Functional pAC50 = 5.6 5.6 -1 8
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 289 6 0 3 3.3 CN(C)CCN(Cc1ccc(Cl)cc1)c1ccccn1 10.1038/s41467-023-40064-9
CHEMBL1194287 13625 None 28 Human Functional pAC50 = 5.6 5.6 -1 8
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 289 6 0 3 3.3 CN(C)CCN(Cc1ccc(Cl)cc1)c1ccccn1 10.1038/s41467-023-40064-9
2771 197264 None 50 Human Functional pAC50 = 4.6 4.6 -173 16
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 10.1038/s41467-023-40064-9
CHEMBL1200781 197264 None 50 Human Functional pAC50 = 4.6 4.6 -173 16
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 10.1038/s41467-023-40064-9
CHEMBL549 197264 None 50 Human Functional pAC50 = 4.6 4.6 -173 16
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 10.1038/s41467-023-40064-9
5311067 61225 None 46 Human Functional pAC50 = 4.6 4.6 - 1
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 376 2 2 4 2.8 C[C@@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)[C@@]3(F)[C@@H](O)C[C@]2(C)[C@H]1C(=O)CO 10.1038/s41467-023-40064-9
CHEMBL1766 61225 None 46 Human Functional pAC50 = 4.6 4.6 - 1
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 376 2 2 4 2.8 C[C@@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)[C@@]3(F)[C@@H](O)C[C@]2(C)[C@H]1C(=O)CO 10.1038/s41467-023-40064-9
2389 3331 None 72 Human Functional pAC50 = 4.6 4.6 -23442 29
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
5073 3331 None 72 Human Functional pAC50 = 4.6 4.6 -23442 29
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
5073.0 3331 None 72 Human Functional pAC50 = 4.6 4.6 -23442 29
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
96 3331 None 72 Human Functional pAC50 = 4.6 4.6 -23442 29
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
CHEMBL85 3331 None 72 Human Functional pAC50 = 4.6 4.6 -23442 29
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
DB00734 3331 None 72 Human Functional pAC50 = 4.6 4.6 -23442 29
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
446156 39838 None 23 Human Functional pAC50 = 4.6 4.6 -1 3
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 459 11 3 5 4.9 COCc1c(C(C)C)nc(C(C)C)c(/C=C/[C@@H](O)C[C@@H](O)CC(=O)O)c1-c1ccc(F)cc1 10.1038/s41467-023-40064-9
CHEMBL1477 39838 None 23 Human Functional pAC50 = 4.6 4.6 -1 3
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 459 11 3 5 4.9 COCc1c(C(C)C)nc(C(C)C)c(/C=C/[C@@H](O)C[C@@H](O)CC(=O)O)c1-c1ccc(F)cc1 10.1038/s41467-023-40064-9
3606 205946 None 40 Human Functional pAC50 = 4.6 4.6 -2 8
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 270 5 2 2 4.8 CCC(c1ccc(O)cc1)C(CC)c1ccc(O)cc1 10.1038/s41467-023-40064-9
CHEMBL6615 205946 None 40 Human Functional pAC50 = 4.6 4.6 -2 8
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 270 5 2 2 4.8 CCC(c1ccc(O)cc1)C(CC)c1ccc(O)cc1 10.1038/s41467-023-40064-9
54758501 139154 None 52 Human Functional pAC50 = 5.6 5.6 -758 11
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 486 7 2 8 5.1 C=CC(=O)Nc1cccc(Oc2nc(Nc3ccc(N4CCN(C)CC4)cc3)nc3ccsc23)c1 10.1038/s41467-023-40064-9
CHEMBL3786343 139154 None 52 Human Functional pAC50 = 5.6 5.6 -758 11
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 486 7 2 8 5.1 C=CC(=O)Nc1cccc(Oc2nc(Nc3ccc(N4CCN(C)CC4)cc3)nc3ccsc23)c1 10.1038/s41467-023-40064-9
12555 17968 None 39 Human Functional pAC50 = 5.6 5.6 -4 9
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 309 7 0 4 3.4 CN(C)CCCOc1nn(Cc2ccccc2)c2ccccc12 10.1038/s41467-023-40064-9
CHEMBL12610 17968 None 39 Human Functional pAC50 = 5.6 5.6 -4 9
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 309 7 0 4 3.4 CN(C)CCCOc1nn(Cc2ccccc2)c2ccccc12 10.1038/s41467-023-40064-9
4832 55436 None 14 Human Functional pAC50 = 7.6 7.6 -1 4
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 354 5 1 3 3.1 CC[N+]1(C)CCCC(OC(=O)C(O)(c2ccccc2)c2ccccc2)C1 10.1038/s41467-023-40064-9
CHEMBL1619528 55436 None 14 Human Functional pAC50 = 7.6 7.6 -1 4
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 354 5 1 3 3.1 CC[N+]1(C)CCCC(OC(=O)C(O)(c2ccccc2)c2ccccc2)C1 10.1038/s41467-023-40064-9
21772 78430 None 26 Human Functional pAC50 = 6.6 6.6 -15 10
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 293 4 0 1 4.5 CC(CC1c2ccccc2CCc2ccccc21)CN(C)C 10.1038/s41467-023-40064-9
CHEMBL2110816 78430 None 26 Human Functional pAC50 = 6.6 6.6 -15 10
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 293 4 0 1 4.5 CC(CC1c2ccccc2CCc2ccccc21)CN(C)C 10.1038/s41467-023-40064-9
2351 4301 None 35 Human Functional pAC50 = 4.6 4.6 -10 22
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 366 10 0 3 4.8 CC(C)COCC(CN(Cc1ccccc1)c1ccccc1)N1CCCC1 10.1038/s41467-023-40064-9
CHEMBL1008 4301 None 35 Human Functional pAC50 = 4.6 4.6 -10 22
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 366 10 0 3 4.8 CC(C)COCC(CN(Cc1ccccc1)c1ccccc1)N1CCCC1 10.1038/s41467-023-40064-9
CHEMBL1257078 4301 None 35 Human Functional pAC50 = 4.6 4.6 -10 22
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 366 10 0 3 4.8 CC(C)COCC(CN(Cc1ccccc1)c1ccccc1)N1CCCC1 10.1038/s41467-023-40064-9
42890 9427 None 34 Human Functional pAC50 = 4.6 4.6 -2 13
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 497 3 5 10 1.0 CC(=O)[C@]1(O)Cc2c(O)c3c(c(O)c2[C@@H](O[C@H]2C[C@H](N)[C@H](O)[C@H](C)O2)C1)C(=O)c1ccccc1C3=O 10.1038/s41467-023-40064-9
CHEMBL1117 9427 None 34 Human Functional pAC50 = 4.6 4.6 -2 13
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 497 3 5 10 1.0 CC(=O)[C@]1(O)Cc2c(O)c3c(c(O)c2[C@@H](O[C@H]2C[C@H](N)[C@H](O)[C@H](C)O2)C1)C(=O)c1ccccc1C3=O 10.1038/s41467-023-40064-9
3191 102913 None 65 Human Functional pAC50 = 4.6 4.6 -27 33
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 10.1038/s41467-023-40064-9
3191.0 102913 None 65 Human Functional pAC50 = 4.6 4.6 -27 33
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 10.1038/s41467-023-40064-9
CHEMBL305660 102913 None 65 Human Functional pAC50 = 4.6 4.6 -27 33
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 10.1038/s41467-023-40064-9
DB11742 102913 None 65 Human Functional pAC50 = 4.6 4.6 -27 33
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 10.1038/s41467-023-40064-9
33478 107496 None 16 Human Functional pAC50 = 4.6 4.6 - 1
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 463 6 2 8 1.3 CC(C)(C)C(=O)OCOC(=O)[C@@H]1N2C(=O)[C@@H](NC(=O)[C@H](N)c3ccccc3)[C@H]2SC1(C)C 10.1038/s41467-023-40064-9
CHEMBL3182343 107496 None 16 Human Functional pAC50 = 4.6 4.6 - 1
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 463 6 2 8 1.3 CC(C)(C)C(=O)OCOC(=O)[C@@H]1N2C(=O)[C@@H](NC(=O)[C@H](N)c3ccccc3)[C@H]2SC1(C)C 10.1038/s41467-023-40064-9
13791 43805 None 46 Human Functional pAC50 = 4.6 4.6 -3 3
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 356 4 1 3 5.4 CCCCC(=O)O[C@H]1CC[C@H]2[C@@H]3CCc4cc(O)ccc4[C@H]3CC[C@]12C 10.1038/s41467-023-40064-9
CHEMBL1511 43805 None 46 Human Functional pAC50 = 4.6 4.6 -3 3
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 356 4 1 3 5.4 CCCCC(=O)O[C@H]1CC[C@H]2[C@@H]3CCc4cc(O)ccc4[C@H]3CC[C@]12C 10.1038/s41467-023-40064-9
7175 70148 None 59 Human Functional pAC50 = 4.6 4.6 -1 2
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 180 3 1 3 2.0 CCCOC(=O)c1ccc(O)cc1 10.1038/s41467-023-40064-9
CHEMBL194014 70148 None 59 Human Functional pAC50 = 4.6 4.6 -1 2
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 180 3 1 3 2.0 CCCOC(=O)c1ccc(O)cc1 10.1038/s41467-023-40064-9
24765256 173401 None 21 Human Functional pAC50 = 4.6 4.6 -1 4
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 757 6 3 9 3.9 CC[C@@H]1C[C@]1(NC(=O)[C@@H]1C[C@@H]2CN1C(=O)[C@H](C(C)(C)C)NC(=O)OCC(C)(C)CCCCc1cccc3c1CN(C3)C(=O)O2)C(=O)NS(=O)(=O)C1CC1 10.1038/s41467-023-40064-9
CHEMBL4525964 173401 None 21 Human Functional pAC50 = 4.6 4.6 -1 4
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 757 6 3 9 3.9 CC[C@@H]1C[C@]1(NC(=O)[C@@H]1C[C@@H]2CN1C(=O)[C@H](C(C)(C)C)NC(=O)OCC(C)(C)CCCCc1cccc3c1CN(C3)C(=O)O2)C(=O)NS(=O)(=O)C1CC1 10.1038/s41467-023-40064-9
65394 49842 None 28 Human Functional pAC50 = 4.6 4.6 - 1
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 296 4 1 2 4.4 O=C(O)Cc1ccccc1Oc1ccc(Cl)cc1Cl 10.1038/s41467-023-40064-9
CHEMBL15677 49842 None 28 Human Functional pAC50 = 4.6 4.6 - 1
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 296 4 1 2 4.4 O=C(O)Cc1ccccc1Oc1ccc(Cl)cc1Cl 10.1038/s41467-023-40064-9
119369 2606 None 50 Human Functional pAC50 = 4.6 4.6 -776 7
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 10.1038/s41467-023-40064-9
2197 2606 None 50 Human Functional pAC50 = 4.6 4.6 -776 7
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 10.1038/s41467-023-40064-9
4004 2606 None 50 Human Functional pAC50 = 4.6 4.6 -776 7
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 10.1038/s41467-023-40064-9
CHEMBL420762 2606 None 50 Human Functional pAC50 = 4.6 4.6 -776 7
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 10.1038/s41467-023-40064-9
40 1547 None 36 Human Functional pAC50 = 4.6 4.6 -2041 8
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 382 6 1 3 3.8 CN1CCC[C@@H]1Cc1c[nH]c2c1cc(cc2)CCS(=O)(=O)c1ccccc1 10.1038/s41467-023-40064-9
77993 1547 None 36 Human Functional pAC50 = 4.6 4.6 -2041 8
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 382 6 1 3 3.8 CN1CCC[C@@H]1Cc1c[nH]c2c1cc(cc2)CCS(=O)(=O)c1ccccc1 10.1038/s41467-023-40064-9
77993.0 1547 None 36 Human Functional pAC50 = 4.6 4.6 -2041 8
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 382 6 1 3 3.8 CN1CCC[C@@H]1Cc1c[nH]c2c1cc(cc2)CCS(=O)(=O)c1ccccc1 10.1038/s41467-023-40064-9
995 1547 None 36 Human Functional pAC50 = 4.6 4.6 -2041 8
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 382 6 1 3 3.8 CN1CCC[C@@H]1Cc1c[nH]c2c1cc(cc2)CCS(=O)(=O)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL1510 1547 None 36 Human Functional pAC50 = 4.6 4.6 -2041 8
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 382 6 1 3 3.8 CN1CCC[C@@H]1Cc1c[nH]c2c1cc(cc2)CCS(=O)(=O)c1ccccc1 10.1038/s41467-023-40064-9
DB00216 1547 None 36 Human Functional pAC50 = 4.6 4.6 -2041 8
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 382 6 1 3 3.8 CN1CCC[C@@H]1Cc1c[nH]c2c1cc(cc2)CCS(=O)(=O)c1ccccc1 10.1038/s41467-023-40064-9
124087 1389 None 72 Human Functional pAC50 = 6.6 6.6 -12 27
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1038/s41467-023-40064-9
124087.0 1389 None 72 Human Functional pAC50 = 6.6 6.6 -12 27
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1038/s41467-023-40064-9
7157 1389 None 72 Human Functional pAC50 = 6.6 6.6 -12 27
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1038/s41467-023-40064-9
814 1389 None 72 Human Functional pAC50 = 6.6 6.6 -12 27
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1038/s41467-023-40064-9
CHEMBL1172 1389 None 72 Human Functional pAC50 = 6.6 6.6 -12 27
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1038/s41467-023-40064-9
DB00967 1389 None 72 Human Functional pAC50 = 6.6 6.6 -12 27
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1038/s41467-023-40064-9
89683805 154523 None 55 Human Functional pAC50 = 4.6 4.6 -7943 6
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 473 6 3 8 4.3 CC(C)(O)CNc1nc(Nc2ccnc(C(F)(F)F)c2)nc(-c2cccc(C(F)(F)F)n2)n1 10.1038/s41467-023-40064-9
CHEMBL3989908 154523 None 55 Human Functional pAC50 = 4.6 4.6 -7943 6
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 473 6 3 8 4.3 CC(C)(O)CNc1nc(Nc2ccnc(C(F)(F)F)c2)nc(-c2cccc(C(F)(F)F)n2)n1 10.1038/s41467-023-40064-9
124 2981 None 32 Human Functional pAC50 = 4.6 4.6 -12022 24
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1038/s41467-023-40064-9
2032 2981 None 32 Human Functional pAC50 = 4.6 4.6 -12022 24
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1038/s41467-023-40064-9
4636 2981 None 32 Human Functional pAC50 = 4.6 4.6 -12022 24
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1038/s41467-023-40064-9
4636.0 2981 None 32 Human Functional pAC50 = 4.6 4.6 -12022 24
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1038/s41467-023-40064-9
CHEMBL762 2981 None 32 Human Functional pAC50 = 4.6 4.6 -12022 24
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1038/s41467-023-40064-9
DB00935 2981 None 32 Human Functional pAC50 = 4.6 4.6 -12022 24
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1038/s41467-023-40064-9
67462786 120581 None 50 Human Functional pAC50 = 4.6 4.6 -5 6
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 446 9 1 8 4.2 COc1cc(OC)cc(N(CCNC(C)C)c2ccc3ncc(-c4cnn(C)c4)nc3c2)c1 10.1038/s41467-023-40064-9
CHEMBL3545376 120581 None 50 Human Functional pAC50 = 4.6 4.6 -5 6
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 446 9 1 8 4.2 COc1cc(OC)cc(N(CCNC(C)C)c2ccc3ncc(-c4cnn(C)c4)nc3c2)c1 10.1038/s41467-023-40064-9
174174 523 None 33 Human Functional pAC50 = 7.6 7.6 -8 7
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1038/s41467-023-40064-9
174174.0 523 None 33 Human Functional pAC50 = 7.6 7.6 -8 7
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1038/s41467-023-40064-9
260 523 None 33 Human Functional pAC50 = 7.6 7.6 -8 7
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1038/s41467-023-40064-9
320 523 None 33 Human Functional pAC50 = 7.6 7.6 -8 7
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1038/s41467-023-40064-9
CHEMBL517712 523 None 33 Human Functional pAC50 = 7.6 7.6 -8 7
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1038/s41467-023-40064-9
DB00572 523 None 33 Human Functional pAC50 = 7.6 7.6 -8 7
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1038/s41467-023-40064-9
6726 1280 None 38 Human Functional pAC50 = 5.6 5.6 -33 16
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
6726.0 1280 None 38 Human Functional pAC50 = 5.6 5.6 -33 16
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
7151 1280 None 38 Human Functional pAC50 = 5.6 5.6 -33 16
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
749 1280 None 38 Human Functional pAC50 = 5.6 5.6 -33 16
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL648 1280 None 38 Human Functional pAC50 = 5.6 5.6 -33 16
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
DB01176 1280 None 38 Human Functional pAC50 = 5.6 5.6 -33 16
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 266 3 0 2 3.0 CN1CCN(CC1)C(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
4417 55578 None 40 Human Functional pAC50 = 4.6 4.6 -120 5
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 383 10 0 4 4.5 CCN(CC)CCOC(=O)C(Cc1cccc2ccccc12)CC1CCCO1 10.1038/s41467-023-40064-9
CHEMBL1439099 55578 None 40 Human Functional pAC50 = 4.6 4.6 -120 5
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 383 10 0 4 4.5 CCN(CC)CCOC(=O)C(Cc1cccc2ccccc12)CC1CCCO1 10.1038/s41467-023-40064-9
CHEMBL1620794 55578 None 40 Human Functional pAC50 = 4.6 4.6 -120 5
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 383 10 0 4 4.5 CCN(CC)CCOC(=O)C(Cc1cccc2ccccc12)CC1CCCO1 10.1038/s41467-023-40064-9
3158 56283 None 21 Human Functional pAC50 = 6.6 6.6 -281 28
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 10.1038/s41467-023-40064-9
3158.0 56283 None 21 Human Functional pAC50 = 6.6 6.6 -281 28
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 10.1038/s41467-023-40064-9
CHEMBL1628227 56283 None 21 Human Functional pAC50 = 6.6 6.6 -281 28
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 10.1038/s41467-023-40064-9
DB01142 56283 None 21 Human Functional pAC50 = 6.6 6.6 -281 28
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 10.1038/s41467-023-40064-9
2407 3372 None 50 Human Functional pAC50 = 4.6 4.6 -7585 17
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1038/s41467-023-40064-9
59227 3372 None 50 Human Functional pAC50 = 4.6 4.6 -7585 17
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1038/s41467-023-40064-9
59227.0 3372 None 50 Human Functional pAC50 = 4.6 4.6 -7585 17
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1038/s41467-023-40064-9
941 3372 None 50 Human Functional pAC50 = 4.6 4.6 -7585 17
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1038/s41467-023-40064-9
CHEMBL1303 3372 None 50 Human Functional pAC50 = 4.6 4.6 -7585 17
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1038/s41467-023-40064-9
DB05271 3372 None 50 Human Functional pAC50 = 4.6 4.6 -7585 17
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1038/s41467-023-40064-9
5502 155612 None 47 Human Functional pAC50 = 4.6 4.6 - 1
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 382 6 0 6 4.4 CCC1C(C)=NN=C(c2ccc(OC)c(OC)c2)c2cc(OC)c(OC)cc21 10.1038/s41467-023-40064-9
CHEMBL404216 155612 None 47 Human Functional pAC50 = 4.6 4.6 - 1
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 382 6 0 6 4.4 CCC1C(C)=NN=C(c2ccc(OC)c(OC)c2)c2cc(OC)c(OC)cc21 10.1038/s41467-023-40064-9
5281004 27679 None 38 Human Functional pAC50 = 4.6 4.6 - 1
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 430 4 2 6 2.7 CCCC1O[C@@H]2C[C@H]3[C@@H]4CCC5=CC(=O)C=C[C@]5(C)[C@H]4[C@@H](O)C[C@]3(C)[C@]2(C(=O)CO)O1 10.1038/s41467-023-40064-9
CHEMBL1370 27679 None 38 Human Functional pAC50 = 4.6 4.6 - 1
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 430 4 2 6 2.7 CCCC1O[C@@H]2C[C@H]3[C@@H]4CCC5=CC(=O)C=C[C@]5(C)[C@H]4[C@@H](O)C[C@]3(C)[C@]2(C(=O)CO)O1 10.1038/s41467-023-40064-9
9417 133581 None 40 Human Functional pAC50 = 4.6 4.6 -316 15
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 363 6 1 4 3.3 OCCN1CCN(CCCN2c3ccccc3C=Cc3ccccc32)CC1 10.1038/s41467-023-40064-9
CHEMBL1524185 133581 None 40 Human Functional pAC50 = 4.6 4.6 -316 15
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 363 6 1 4 3.3 OCCN1CCN(CCCN2c3ccccc3C=Cc3ccccc32)CC1 10.1038/s41467-023-40064-9
CHEMBL370753 133581 None 40 Human Functional pAC50 = 4.6 4.6 -316 15
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 363 6 1 4 3.3 OCCN1CCN(CCCN2c3ccccc3C=Cc3ccccc32)CC1 10.1038/s41467-023-40064-9
448537 160344 None 54 Human Functional pAC50 = 5.6 5.6 -20 31
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 10.1038/s41467-023-40064-9
CHEMBL411 160344 None 54 Human Functional pAC50 = 5.6 5.6 -20 31
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 10.1038/s41467-023-40064-9
2370 623 None 23 Human Functional pAC50 = 4.6 4.6 -128 3
Agonist activity at human CHRM1 in an in vitro cell-based assay (NIBR assay) measured by Hamamatsu Functional Drug Screening SystemAgonist activity at human CHRM1 in an in vitro cell-based assay (NIBR assay) measured by Hamamatsu Functional Drug Screening System
ChEMBL 161 3 1 2 0.2 CC(C[N+](C)(C)C)OC(=O)N 10.1038/s41467-023-40064-9
2370.0 623 None 23 Human Functional pAC50 = 4.6 4.6 -128 3
Agonist activity at human CHRM1 in an in vitro cell-based assay (NIBR assay) measured by Hamamatsu Functional Drug Screening SystemAgonist activity at human CHRM1 in an in vitro cell-based assay (NIBR assay) measured by Hamamatsu Functional Drug Screening System
ChEMBL 161 3 1 2 0.2 CC(C[N+](C)(C)C)OC(=O)N 10.1038/s41467-023-40064-9
297 623 None 23 Human Functional pAC50 = 4.6 4.6 -128 3
Agonist activity at human CHRM1 in an in vitro cell-based assay (NIBR assay) measured by Hamamatsu Functional Drug Screening SystemAgonist activity at human CHRM1 in an in vitro cell-based assay (NIBR assay) measured by Hamamatsu Functional Drug Screening System
ChEMBL 161 3 1 2 0.2 CC(C[N+](C)(C)C)OC(=O)N 10.1038/s41467-023-40064-9
358 623 None 23 Human Functional pAC50 = 4.6 4.6 -128 3
Agonist activity at human CHRM1 in an in vitro cell-based assay (NIBR assay) measured by Hamamatsu Functional Drug Screening SystemAgonist activity at human CHRM1 in an in vitro cell-based assay (NIBR assay) measured by Hamamatsu Functional Drug Screening System
ChEMBL 161 3 1 2 0.2 CC(C[N+](C)(C)C)OC(=O)N 10.1038/s41467-023-40064-9
CHEMBL1482 623 None 23 Human Functional pAC50 = 4.6 4.6 -128 3
Agonist activity at human CHRM1 in an in vitro cell-based assay (NIBR assay) measured by Hamamatsu Functional Drug Screening SystemAgonist activity at human CHRM1 in an in vitro cell-based assay (NIBR assay) measured by Hamamatsu Functional Drug Screening System
ChEMBL 161 3 1 2 0.2 CC(C[N+](C)(C)C)OC(=O)N 10.1038/s41467-023-40064-9
DB01019 623 None 23 Human Functional pAC50 = 4.6 4.6 -128 3
Agonist activity at human CHRM1 in an in vitro cell-based assay (NIBR assay) measured by Hamamatsu Functional Drug Screening SystemAgonist activity at human CHRM1 in an in vitro cell-based assay (NIBR assay) measured by Hamamatsu Functional Drug Screening System
ChEMBL 161 3 1 2 0.2 CC(C[N+](C)(C)C)OC(=O)N 10.1038/s41467-023-40064-9
4066 207084 None 54 Human Functional pAC50 = 7.6 7.6 -1 16
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 322 2 0 3 4.6 c1ccc2c(c1)Sc1ccccc1N2CC1CN2CCC1CC2 10.1038/s41467-023-40064-9
4066.0 207084 None 54 Human Functional pAC50 = 7.6 7.6 -1 16
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 322 2 0 3 4.6 c1ccc2c(c1)Sc1ccccc1N2CC1CN2CCC1CC2 10.1038/s41467-023-40064-9
CHEMBL73451 207084 None 54 Human Functional pAC50 = 7.6 7.6 -1 16
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 322 2 0 3 4.6 c1ccc2c(c1)Sc1ccccc1N2CC1CN2CCC1CC2 10.1038/s41467-023-40064-9
DB01071 207084 None 54 Human Functional pAC50 = 7.6 7.6 -1 16
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 322 2 0 3 4.6 c1ccc2c(c1)Sc1ccccc1N2CC1CN2CCC1CC2 10.1038/s41467-023-40064-9
10077130 4007 None 47 Human Functional pAC50 = 4.6 4.6 -954 6
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1038/s41467-023-40064-9
10077130.0 4007 None 47 Human Functional pAC50 = 4.6 4.6 -954 6
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1038/s41467-023-40064-9
4047 4007 None 47 Human Functional pAC50 = 4.6 4.6 -954 6
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1038/s41467-023-40064-9
4870 4007 None 47 Human Functional pAC50 = 4.6 4.6 -954 6
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1038/s41467-023-40064-9
CHEMBL493982 4007 None 47 Human Functional pAC50 = 4.6 4.6 -954 6
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1038/s41467-023-40064-9
DB09030 4007 None 47 Human Functional pAC50 = 4.6 4.6 -954 6
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1038/s41467-023-40064-9
71897 78277 None 10 Human Functional pAC50 = 4.6 4.6 -8709 7
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 304 4 1 3 2.7 Cc1cc(CCN2CCN(c3cccc(Cl)c3)CC2)n[nH]1 10.1038/s41467-023-40064-9
CHEMBL2106537 78277 None 10 Human Functional pAC50 = 4.6 4.6 -8709 7
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 304 4 1 3 2.7 Cc1cc(CCN2CCN(c3cccc(Cl)c3)CC2)n[nH]1 10.1038/s41467-023-40064-9
667492 43919 None 36 Human Functional pAC50 = 4.6 4.6 -1 4
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 234 1 2 3 0.2 CN1C(=O)/C(=N\NC(N)=S)c2ccccc21 10.1038/s41467-023-40064-9
CHEMBL1512080 43919 None 36 Human Functional pAC50 = 4.6 4.6 -1 4
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 234 1 2 3 0.2 CN1C(=O)/C(=N\NC(N)=S)c2ccccc21 10.1038/s41467-023-40064-9
9400 14497 None 27 Human Functional pAC50 = 4.6 4.6 1 2
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 472 4 4 6 2.0 C[C@@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)[C@@]3(F)[C@@H](O)C[C@]2(C)[C@@]1(O)C(=O)COP(=O)(O)O 10.1038/s41467-023-40064-9
CHEMBL1201302 14497 None 27 Human Functional pAC50 = 4.6 4.6 1 2
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 472 4 4 6 2.0 C[C@@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)[C@@]3(F)[C@@H](O)C[C@]2(C)[C@@]1(O)C(=O)COP(=O)(O)O 10.1038/s41467-023-40064-9
4594 42886 None 68 Human Functional pAC50 = 4.6 4.6 -9 6
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 345 5 1 5 2.9 COc1ccc2[nH]c([S+]([O-])Cc3ncc(C)c(OC)c3C)nc2c1 10.1038/s41467-023-40064-9
CHEMBL1503 42886 None 68 Human Functional pAC50 = 4.6 4.6 -9 6
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 345 5 1 5 2.9 COc1ccc2[nH]c([S+]([O-])Cc3ncc(C)c(OC)c3C)nc2c1 10.1038/s41467-023-40064-9
3336 95054 None 22 Human Functional pAC50 = 4.6 4.6 -5495 14
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 315 7 1 1 5.6 CC(NCCC(c1ccccc1)c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL1405922 95054 None 22 Human Functional pAC50 = 4.6 4.6 -5495 14
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 315 7 1 1 5.6 CC(NCCC(c1ccccc1)c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL254832 95054 None 22 Human Functional pAC50 = 4.6 4.6 -5495 14
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 315 7 1 1 5.6 CC(NCCC(c1ccccc1)c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
6075 150196 None 34 Human Functional pAC50 = 4.6 4.6 -28 20
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 310 2 0 3 4.6 CN1CCCC(CN2c3ccccc3Sc3ccccc32)C1 10.1038/s41467-023-40064-9
CHEMBL395110 150196 None 34 Human Functional pAC50 = 4.6 4.6 -28 20
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 310 2 0 3 4.6 CN1CCCC(CN2c3ccccc3Sc3ccccc32)C1 10.1038/s41467-023-40064-9
54585 14508 None 49 Human Functional pAC50 = 4.6 4.6 1 7
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 357 7 4 6 2.7 O=C(O)CCNC(=O)c1ccc(/N=N/c2ccc(O)c(C(=O)O)c2)cc1 10.1038/s41467-023-40064-9
CHEMBL1201346 14508 None 49 Human Functional pAC50 = 4.6 4.6 1 7
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 357 7 4 6 2.7 O=C(O)CCNC(=O)c1ccc(/N=N/c2ccc(O)c(C(=O)O)c2)cc1 10.1038/s41467-023-40064-9
54686904 137957 None 54 Human Functional pAC50 = 4.6 4.6 1 2
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 585 6 7 11 0.5 CN(C)c1cc(NC(=O)CNC(C)(C)C)c(O)c2c1C[C@H]1C[C@H]3[C@H](N(C)C)C(O)=C(C(N)=O)C(=O)[C@@]3(O)C(O)=C1C2=O 10.1038/s41467-023-40064-9
CHEMBL376140 137957 None 54 Human Functional pAC50 = 4.6 4.6 1 2
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 585 6 7 11 0.5 CN(C)c1cc(NC(=O)CNC(C)(C)C)c(O)c2c1C[C@H]1C[C@H]3[C@H](N(C)C)C(O)=C(C(N)=O)C(=O)[C@@]3(O)C(O)=C1C2=O 10.1038/s41467-023-40064-9
193962 103848 None 63 Human Functional pAC50 = 5.6 5.6 1 6
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 434 4 2 7 4.7 Cc1cc(C#N)cc(C)c1Oc1nc(Nc2ccc(C#N)cc2)nc(N)c1Br 10.1038/s41467-023-40064-9
CHEMBL308954 103848 None 63 Human Functional pAC50 = 5.6 5.6 1 6
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 434 4 2 7 4.7 Cc1cc(C#N)cc(C)c1Oc1nc(Nc2ccc(C#N)cc2)nc(N)c1Br 10.1038/s41467-023-40064-9
4004 14426 None 33 Human Functional pAC50 = 4.6 4.6 -2 2
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 330 9 0 8 2.1 CCOC(=O)CC(SP(=S)(OC)OC)C(=O)OCC 10.1038/s41467-023-40064-9
CHEMBL1200468 14426 None 33 Human Functional pAC50 = 4.6 4.6 -2 2
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 330 9 0 8 2.1 CCOC(=O)CC(SP(=S)(OC)OC)C(=O)OCC 10.1038/s41467-023-40064-9
25102847 78250 None 62 Human Functional pAC50 = 5.6 5.6 -2 10
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 501 8 2 6 5.5 COc1cc2nccc(Oc3ccc(NC(=O)C4(C(=O)Nc5ccc(F)cc5)CC4)cc3)c2cc1OC 10.1038/s41467-023-40064-9
CHEMBL2105717 78250 None 62 Human Functional pAC50 = 5.6 5.6 -2 10
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 501 8 2 6 5.5 COc1cc2nccc(Oc3ccc(NC(=O)C4(C(=O)Nc5ccc(F)cc5)CC4)cc3)c2cc1OC 10.1038/s41467-023-40064-9
6231 29778 None 23 Human Functional pAC50 = 5.6 5.6 3 4
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 298 0 1 2 3.6 C#C[C@]1(O)CC[C@H]2[C@@H]3CCC4=C(CCC(=O)C4)[C@H]3CC[C@@]21C 10.1038/s41467-023-40064-9
CHEMBL1387 29778 None 23 Human Functional pAC50 = 5.6 5.6 3 4
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 298 0 1 2 3.6 C#C[C@]1(O)CC[C@H]2[C@@H]3CCC4=C(CCC(=O)C4)[C@H]3CC[C@@]21C 10.1038/s41467-023-40064-9
31703 194829 None 40 Human Functional pAC50 = 4.6 4.6 -33 8
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 543 5 6 12 0.0 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(=O)CO)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 10.1038/s41467-023-40064-9
CHEMBL359744 194829 None 40 Human Functional pAC50 = 4.6 4.6 -33 8
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 543 5 6 12 0.0 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(=O)CO)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 10.1038/s41467-023-40064-9
CHEMBL53463 194829 None 40 Human Functional pAC50 = 4.6 4.6 -33 8
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 543 5 6 12 0.0 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(=O)CO)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 10.1038/s41467-023-40064-9
1727 99708 None 65 Human Functional pAC50 = 4.6 4.6 -223 2
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 94 0 1 2 0.7 Nc1ccncc1 10.1038/s41467-023-40064-9
CHEMBL284348 99708 None 65 Human Functional pAC50 = 4.6 4.6 -223 2
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 94 0 1 2 0.7 Nc1ccncc1 10.1038/s41467-023-40064-9
5284632 67423 None 10 Human Functional pAC50 = 7.6 7.6 1 4
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 392 4 1 3 3.8 O=C(O[C@@H]1C[C@@H]2CC[C@H](C1)[N+]21CCCC1)C(O)(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
5284632.0 67423 None 10 Human Functional pAC50 = 7.6 7.6 1 4
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 392 4 1 3 3.8 O=C(O[C@@H]1C[C@@H]2CC[C@H](C1)[N+]21CCCC1)C(O)(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL1888176 67423 None 10 Human Functional pAC50 = 7.6 7.6 1 4
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 392 4 1 3 3.8 O=C(O[C@@H]1C[C@@H]2CC[C@H](C1)[N+]21CCCC1)C(O)(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL3084748 67423 None 10 Human Functional pAC50 = 7.6 7.6 1 4
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 392 4 1 3 3.8 O=C(O[C@@H]1C[C@@H]2CC[C@H](C1)[N+]21CCCC1)C(O)(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
DB00209 67423 None 10 Human Functional pAC50 = 7.6 7.6 1 4
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 392 4 1 3 3.8 O=C(O[C@@H]1C[C@@H]2CC[C@H](C1)[N+]21CCCC1)C(O)(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
4097 14488 None 8 Human Functional pAC50 = 7.5 7.5 -2 2
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 340 6 0 3 4.0 CC[N+](C)(CC)CCOC(=O)C1c2ccccc2Oc2ccccc21 10.1038/s41467-023-40064-9
4097.0 14488 None 8 Human Functional pAC50 = 7.5 7.5 -2 2
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 340 6 0 3 4.0 CC[N+](C)(CC)CCOC(=O)C1c2ccccc2Oc2ccccc21 10.1038/s41467-023-40064-9
CHEMBL1201264 14488 None 8 Human Functional pAC50 = 7.5 7.5 -2 2
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 340 6 0 3 4.0 CC[N+](C)(CC)CCOC(=O)C1c2ccccc2Oc2ccccc21 10.1038/s41467-023-40064-9
DB00940 14488 None 8 Human Functional pAC50 = 7.5 7.5 -2 2
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 340 6 0 3 4.0 CC[N+](C)(CC)CCOC(=O)C1c2ccccc2Oc2ccccc21 10.1038/s41467-023-40064-9
54841 205585 None 33 Human Functional pAC50 = 4.6 4.6 -15 11
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 255 6 1 2 3.7 CNCC[C@@H](Oc1ccccc1C)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL641 205585 None 33 Human Functional pAC50 = 4.6 4.6 -15 11
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 255 6 1 2 3.7 CNCC[C@@H](Oc1ccccc1C)c1ccccc1 10.1038/s41467-023-40064-9
68802 110091 None 27 Human Functional pAC50 = 4.6 4.6 -15 4
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 226 0 1 2 2.9 Cc1ccc2c(c1)c1c3n2CCNC3CCC1 10.1038/s41467-023-40064-9
CHEMBL32350 110091 None 27 Human Functional pAC50 = 4.6 4.6 -15 4
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 226 0 1 2 2.9 Cc1ccc2c(c1)c1c3n2CCNC3CCC1 10.1038/s41467-023-40064-9
2749 32651 None 61 Human Functional pAC50 = 4.6 4.6 -1 3
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 207 1 1 3 2.4 Cc1cc(C2CCCCC2)n(O)c(=O)c1 10.1038/s41467-023-40064-9
CHEMBL1413 32651 None 61 Human Functional pAC50 = 4.6 4.6 -1 3
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 207 1 1 3 2.4 Cc1cc(C2CCCCC2)n(O)c(=O)c1 10.1038/s41467-023-40064-9
2337 3256 None 51 Human Functional pAC50 = 5.6 5.6 -162 29
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
50 3256 None 51 Human Functional pAC50 = 5.6 5.6 -162 29
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
5002 3256 None 51 Human Functional pAC50 = 5.6 5.6 -162 29
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
5002.0 3256 None 51 Human Functional pAC50 = 5.6 5.6 -162 29
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL716 3256 None 51 Human Functional pAC50 = 5.6 5.6 -162 29
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
DB01224 3256 None 51 Human Functional pAC50 = 5.6 5.6 -162 29
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
35935 67451 None 16 Human Functional pAC50 = 4.5 4.5 - 1
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 251 3 1 2 2.9 CC(C(=O)O)c1ccc(N2CC=CC2)c(Cl)c1 10.1038/s41467-023-40064-9
CHEMBL188952 67451 None 16 Human Functional pAC50 = 4.5 4.5 - 1
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 251 3 1 2 2.9 CC(C(=O)O)c1ccc(N2CC=CC2)c(Cl)c1 10.1038/s41467-023-40064-9
54697325 58996 None 30 Human Functional pAC50 = 4.5 4.5 -2 7
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 556 6 6 10 1.3 CN(C)c1cc(CNCC(C)(C)C)c(O)c2c1C[C@H]1C[C@H]3[C@H](N(C)C)C(O)=C(C(N)=O)C(=O)[C@@]3(O)C(O)=C1C2=O 10.1038/s41467-023-40064-9
CHEMBL1689772 58996 None 30 Human Functional pAC50 = 4.5 4.5 -2 7
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 556 6 6 10 1.3 CN(C)c1cc(CNCC(C)(C)C)c(O)c2c1C[C@H]1C[C@H]3[C@H](N(C)C)C(O)=C(C(N)=O)C(=O)[C@@]3(O)C(O)=C1C2=O 10.1038/s41467-023-40064-9
71398 106495 None 32 Human Functional pAC50 = 4.5 4.5 -4073 14
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 302 5 4 4 3.6 C[C@@H](Cc1ccc(O)c(O)c1)[C@H](C)Cc1ccc(O)c(O)c1 10.1038/s41467-023-40064-9
CHEMBL313972 106495 None 32 Human Functional pAC50 = 4.5 4.5 -4073 14
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 302 5 4 4 3.6 C[C@@H](Cc1ccc(O)c(O)c1)[C@H](C)Cc1ccc(O)c(O)c1 10.1038/s41467-023-40064-9
135415564 170388 None 10 Human Functional pAC50 = 4.5 4.5 - 1
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 846 4 5 14 4.6 CO[C@H]1/C=C/O[C@@]2(C)Oc3c(C)c(O)c4c(c3C2=O)C2=NC3(CCN(CC(C)C)CC3)NC2=C(NC(=O)/C(C)=C\C=C\[C@H](C)[C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@H](OC(C)=O)[C@@H]1C)C4=O 10.1038/s41467-023-40064-9
CHEMBL444633 170388 None 10 Human Functional pAC50 = 4.5 4.5 - 1
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 846 4 5 14 4.6 CO[C@H]1/C=C/O[C@@]2(C)Oc3c(C)c(O)c4c(c3C2=O)C2=NC3(CCN(CC(C)C)CC3)NC2=C(NC(=O)/C(C)=C\C=C\[C@H](C)[C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@H](OC(C)=O)[C@@H]1C)C4=O 10.1038/s41467-023-40064-9
5440 28732 None 28 Human Functional pAC50 = 4.5 4.5 -6918 16
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 399 6 0 5 5.0 CCSc1ccc2c(c1)N(CCCN1CCN(C)CC1)c1ccccc1S2 10.1038/s41467-023-40064-9
5440.0 28732 None 28 Human Functional pAC50 = 4.5 4.5 -6918 16
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 399 6 0 5 5.0 CCSc1ccc2c(c1)N(CCCN1CCN(C)CC1)c1ccccc1S2 10.1038/s41467-023-40064-9
CHEMBL1378 28732 None 28 Human Functional pAC50 = 4.5 4.5 -6918 16
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 399 6 0 5 5.0 CCSc1ccc2c(c1)N(CCCN1CCN(C)CC1)c1ccccc1S2 10.1038/s41467-023-40064-9
DB00372 28732 None 28 Human Functional pAC50 = 4.5 4.5 -6918 16
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 399 6 0 5 5.0 CCSc1ccc2c(c1)N(CCCN1CCN(C)CC1)c1ccccc1S2 10.1038/s41467-023-40064-9
1353 1911 None 63 Human Functional pAC50 = 5.5 5.5 -2238 39
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
3559 1911 None 63 Human Functional pAC50 = 5.5 5.5 -2238 39
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
3559.0 1911 None 63 Human Functional pAC50 = 5.5 5.5 -2238 39
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
86 1911 None 63 Human Functional pAC50 = 5.5 5.5 -2238 39
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
CHEMBL54 1911 None 63 Human Functional pAC50 = 5.5 5.5 -2238 39
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
DB00502 1911 None 63 Human Functional pAC50 = 5.5 5.5 -2238 39
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
3598 187927 None 45 Human Functional pAC50 = 4.5 4.5 -41 17
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 404 2 2 2 6.6 Oc1c(Cl)cc(Cl)c(Cl)c1Cc1c(O)c(Cl)cc(Cl)c1Cl 10.1038/s41467-023-40064-9
CHEMBL496 187927 None 45 Human Functional pAC50 = 4.5 4.5 -41 17
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 404 2 2 2 6.6 Oc1c(Cl)cc(Cl)c(Cl)c1Cc1c(O)c(Cl)cc(Cl)c1Cl 10.1038/s41467-023-40064-9
CHEMBL508338 189074 None 0 Human Functional pAC50 = 4.5 4.5 -323 15
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL None None None None 10.1038/s41467-023-40064-9
57363 206695 None 54 Human Functional pAC50 = 4.5 4.5 -2 2
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 372 1 2 2 3.8 CC(C)(C)NC(=O)[C@H]1CC[C@H]2[C@@H]3CC[C@H]4NC(=O)C=C[C@]4(C)[C@H]3CC[C@]12C 10.1038/s41467-023-40064-9
CHEMBL710 206695 None 54 Human Functional pAC50 = 4.5 4.5 -2 2
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 372 1 2 2 3.8 CC(C)(C)NC(=O)[C@H]1CC[C@H]2[C@@H]3CC[C@H]4NC(=O)C=C[C@]4(C)[C@H]3CC[C@]12C 10.1038/s41467-023-40064-9
10071196 3124 None 53 Human Functional pAC50 = 4.5 4.5 -2041 15
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 427 8 1 3 4.7 CC(COc1ccc(cc1)CNC(=O)N(C1CCN(CC1)C)Cc1ccc(cc1)F)C 10.1038/s41467-023-40064-9
10071196.0 3124 None 53 Human Functional pAC50 = 4.5 4.5 -2041 15
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 427 8 1 3 4.7 CC(COc1ccc(cc1)CNC(=O)N(C1CCN(CC1)C)Cc1ccc(cc1)F)C 10.1038/s41467-023-40064-9
5142 3124 None 53 Human Functional pAC50 = 4.5 4.5 -2041 15
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 427 8 1 3 4.7 CC(COc1ccc(cc1)CNC(=O)N(C1CCN(CC1)C)Cc1ccc(cc1)F)C 10.1038/s41467-023-40064-9
8423 3124 None 53 Human Functional pAC50 = 4.5 4.5 -2041 15
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 427 8 1 3 4.7 CC(COc1ccc(cc1)CNC(=O)N(C1CCN(CC1)C)Cc1ccc(cc1)F)C 10.1038/s41467-023-40064-9
CHEMBL2111101 3124 None 53 Human Functional pAC50 = 4.5 4.5 -2041 15
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 427 8 1 3 4.7 CC(COc1ccc(cc1)CNC(=O)N(C1CCN(CC1)C)Cc1ccc(cc1)F)C 10.1038/s41467-023-40064-9
DB05316 3124 None 53 Human Functional pAC50 = 4.5 4.5 -2041 15
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 427 8 1 3 4.7 CC(COc1ccc(cc1)CNC(=O)N(C1CCN(CC1)C)Cc1ccc(cc1)F)C 10.1038/s41467-023-40064-9
4739544 202554 None 61 Human Functional pAC50 = 4.5 4.5 - 1
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 190 3 2 2 1.6 O=C(O)CCc1nc2ccccc2[nH]1 10.1038/s41467-023-40064-9
52957676 202554 None 61 Human Functional pAC50 = 4.5 4.5 - 1
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 190 3 2 2 1.6 O=C(O)CCc1nc2ccccc2[nH]1 10.1038/s41467-023-40064-9
65708 202554 None 61 Human Functional pAC50 = 4.5 4.5 - 1
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 190 3 2 2 1.6 O=C(O)CCc1nc2ccccc2[nH]1 10.1038/s41467-023-40064-9
CHEMBL596009 202554 None 61 Human Functional pAC50 = 4.5 4.5 - 1
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 190 3 2 2 1.6 O=C(O)CCc1nc2ccccc2[nH]1 10.1038/s41467-023-40064-9
23724781 2835 None 13 Human Functional pAC50 = 8.5 8.5 -4 8
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1038/s41467-023-40064-9
23724781.0 2835 None 13 Human Functional pAC50 = 8.5 8.5 -4 8
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1038/s41467-023-40064-9
316 2835 None 13 Human Functional pAC50 = 8.5 8.5 -4 8
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1038/s41467-023-40064-9
317 2835 None 13 Human Functional pAC50 = 8.5 8.5 -4 8
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1038/s41467-023-40064-9
71183 2835 None 13 Human Functional pAC50 = 8.5 8.5 -4 8
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1038/s41467-023-40064-9
CHEMBL1354199 2835 None 13 Human Functional pAC50 = 8.5 8.5 -4 8
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1038/s41467-023-40064-9
CHEMBL3140030 2835 None 13 Human Functional pAC50 = 8.5 8.5 -4 8
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1038/s41467-023-40064-9
CHEMBL376897 2835 None 13 Human Functional pAC50 = 8.5 8.5 -4 8
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1038/s41467-023-40064-9
DB00462 2835 None 13 Human Functional pAC50 = 8.5 8.5 -4 8
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 318 4 1 4 1.1 OC[C@H](c1ccccc1)C(=O)OC1C[C@@H]2[C@@H]3[C@H]([C@H](C1)[N+]2(C)C)O3 10.1038/s41467-023-40064-9
2039 2982 None 13 Human Functional pAC50 = 8.5 8.5 1 2
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 348 8 1 3 3.5 CC[N+](CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)(CC)C 10.1038/s41467-023-40064-9
5749 2982 None 13 Human Functional pAC50 = 8.5 8.5 1 2
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 348 8 1 3 3.5 CC[N+](CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)(CC)C 10.1038/s41467-023-40064-9
5749.0 2982 None 13 Human Functional pAC50 = 8.5 8.5 1 2
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 348 8 1 3 3.5 CC[N+](CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)(CC)C 10.1038/s41467-023-40064-9
7257 2982 None 13 Human Functional pAC50 = 8.5 8.5 1 2
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 348 8 1 3 3.5 CC[N+](CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)(CC)C 10.1038/s41467-023-40064-9
CHEMBL1201286 2982 None 13 Human Functional pAC50 = 8.5 8.5 1 2
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 348 8 1 3 3.5 CC[N+](CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)(CC)C 10.1038/s41467-023-40064-9
DB00219 2982 None 13 Human Functional pAC50 = 8.5 8.5 1 2
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 348 8 1 3 3.5 CC[N+](CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)(CC)C 10.1038/s41467-023-40064-9
2293 3186 None 19 Human Functional pAC50 = 8.5 8.5 1 4
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 368 6 0 3 4.7 O=C(C1c2ccccc2Oc2c1cccc2)OCC[N+](C(C)C)(C(C)C)C 10.1038/s41467-023-40064-9
329 3186 None 19 Human Functional pAC50 = 8.5 8.5 1 4
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 368 6 0 3 4.7 O=C(C1c2ccccc2Oc2c1cccc2)OCC[N+](C(C)C)(C(C)C)C 10.1038/s41467-023-40064-9
4934 3186 None 19 Human Functional pAC50 = 8.5 8.5 1 4
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 368 6 0 3 4.7 O=C(C1c2ccccc2Oc2c1cccc2)OCC[N+](C(C)C)(C(C)C)C 10.1038/s41467-023-40064-9
4934.0 3186 None 19 Human Functional pAC50 = 8.5 8.5 1 4
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 368 6 0 3 4.7 O=C(C1c2ccccc2Oc2c1cccc2)OCC[N+](C(C)C)(C(C)C)C 10.1038/s41467-023-40064-9
CHEMBL1180725 3186 None 19 Human Functional pAC50 = 8.5 8.5 1 4
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 368 6 0 3 4.7 O=C(C1c2ccccc2Oc2c1cccc2)OCC[N+](C(C)C)(C(C)C)C 10.1038/s41467-023-40064-9
DB00782 3186 None 19 Human Functional pAC50 = 8.5 8.5 1 4
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 368 6 0 3 4.7 O=C(C1c2ccccc2Oc2c1cccc2)OCC[N+](C(C)C)(C(C)C)C 10.1038/s41467-023-40064-9
3000322 3562 None 29 Human Functional pAC50 = 8.5 8.5 -1 4
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 303 4 1 5 0.9 OC[C@H](c1ccccc1)C(=O)O[C@@H]1C[C@H]2N([C@@H](C1)[C@H]1[C@@H]2O1)C 10.1038/s41467-023-40064-9
3000322.0 3562 None 29 Human Functional pAC50 = 8.5 8.5 -1 4
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 303 4 1 5 0.9 OC[C@H](c1ccccc1)C(=O)O[C@@H]1C[C@H]2N([C@@H](C1)[C@H]1[C@@H]2O1)C 10.1038/s41467-023-40064-9
330 3562 None 29 Human Functional pAC50 = 8.5 8.5 -1 4
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 303 4 1 5 0.9 OC[C@H](c1ccccc1)C(=O)O[C@@H]1C[C@H]2N([C@@H](C1)[C@H]1[C@@H]2O1)C 10.1038/s41467-023-40064-9
CHEMBL569713 3562 None 29 Human Functional pAC50 = 8.5 8.5 -1 4
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 303 4 1 5 0.9 OC[C@H](c1ccccc1)C(=O)O[C@@H]1C[C@H]2N([C@@H](C1)[C@H]1[C@@H]2O1)C 10.1038/s41467-023-40064-9
DB00747 3562 None 29 Human Functional pAC50 = 8.5 8.5 -1 4
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 303 4 1 5 0.9 OC[C@H](c1ccccc1)C(=O)O[C@@H]1C[C@H]2N([C@@H](C1)[C@H]1[C@@H]2O1)C 10.1038/s41467-023-40064-9
2745 3861 None 30 Human Functional pAC50 = 8.5 8.5 1 7
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 10.1038/s41467-023-40064-9
5572 3861 None 30 Human Functional pAC50 = 8.5 8.5 1 7
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 10.1038/s41467-023-40064-9
5572.0 3861 None 30 Human Functional pAC50 = 8.5 8.5 1 7
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 10.1038/s41467-023-40064-9
66007 3861 None 30 Human Functional pAC50 = 8.5 8.5 1 7
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 10.1038/s41467-023-40064-9
7315 3861 None 30 Human Functional pAC50 = 8.5 8.5 1 7
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 10.1038/s41467-023-40064-9
CHEMBL1490 3861 None 30 Human Functional pAC50 = 8.5 8.5 1 7
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 10.1038/s41467-023-40064-9
DB00376 3861 None 30 Human Functional pAC50 = 8.5 8.5 1 7
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 301 5 1 2 4.3 OC(c1ccccc1)(C1CCCCC1)CCN1CCCCC1 10.1038/s41467-023-40064-9
6917866 167534 None 5 Human Functional pAC50 = 8.5 8.5 1 2
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 332 5 1 4 1.5 CC[N+]1(C)[C@@H]2CC(OC(=O)[C@H](CO)c3ccccc3)C[C@H]1[C@@H]1O[C@@H]12 10.1038/s41467-023-40064-9
CHEMBL4297364 167534 None 5 Human Functional pAC50 = 8.5 8.5 1 2
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 332 5 1 4 1.5 CC[N+]1(C)[C@@H]2CC(OC(=O)[C@H](CO)c3ccccc3)C[C@H]1[C@@H]1O[C@@H]12 10.1038/s41467-023-40064-9
187 255 None 24 Human Functional pAC50 = 8.5 8.5 -5 8
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1038/s41467-023-40064-9
187.0 255 None 24 Human Functional pAC50 = 8.5 8.5 -5 8
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1038/s41467-023-40064-9
294 255 None 24 Human Functional pAC50 = 8.5 8.5 -5 8
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1038/s41467-023-40064-9
65 255 None 24 Human Functional pAC50 = 8.5 8.5 -5 8
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1038/s41467-023-40064-9
8593 255 None 24 Human Functional pAC50 = 8.5 8.5 -5 8
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1038/s41467-023-40064-9
CHEMBL667 255 None 24 Human Functional pAC50 = 8.5 8.5 -5 8
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1038/s41467-023-40064-9
DB03128 255 None 24 Human Functional pAC50 = 8.5 8.5 -5 8
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1038/s41467-023-40064-9
2784 952 None 9 Human Functional pAC50 = 8.5 8.5 -1 5
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 352 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1C[N+]2(C)CCC1CC2 10.1038/s41467-023-40064-9
2784.0 952 None 9 Human Functional pAC50 = 8.5 8.5 -1 5
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 352 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1C[N+]2(C)CCC1CC2 10.1038/s41467-023-40064-9
351 952 None 9 Human Functional pAC50 = 8.5 8.5 -1 5
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 352 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1C[N+]2(C)CCC1CC2 10.1038/s41467-023-40064-9
366 952 None 9 Human Functional pAC50 = 8.5 8.5 -1 5
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 352 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1C[N+]2(C)CCC1CC2 10.1038/s41467-023-40064-9
676 952 None 9 Human Functional pAC50 = 8.5 8.5 -1 5
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 352 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1C[N+]2(C)CCC1CC2 10.1038/s41467-023-40064-9
CHEMBL620 952 None 9 Human Functional pAC50 = 8.5 8.5 -1 5
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 352 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1C[N+]2(C)CCC1CC2 10.1038/s41467-023-40064-9
DB00771 952 None 9 Human Functional pAC50 = 8.5 8.5 -1 5
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 352 4 1 3 2.7 O=C(C(c1ccccc1)(c1ccccc1)O)OC1C[N+]2(C)CCC1CC2 10.1038/s41467-023-40064-9
2381 663 None 30 Human Functional pAC50 = 8.4 8.4 25 5
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 10.1038/s41467-023-40064-9
2381.0 663 None 30 Human Functional pAC50 = 8.4 8.4 25 5
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 10.1038/s41467-023-40064-9
374 663 None 30 Human Functional pAC50 = 8.4 8.4 25 5
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 10.1038/s41467-023-40064-9
7128 663 None 30 Human Functional pAC50 = 8.4 8.4 25 5
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 10.1038/s41467-023-40064-9
CHEMBL1101 663 None 30 Human Functional pAC50 = 8.4 8.4 25 5
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 10.1038/s41467-023-40064-9
DB00810 663 None 30 Human Functional pAC50 = 8.4 8.4 25 5
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 10.1038/s41467-023-40064-9
11980903 14498 None 13 Human Functional pAC50 = 5.5 5.5 -83 25
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 382 4 0 2 5.3 Cc1cc(/C=C/c2ccc3cc(N(C)C)ccc3[n+]2C)c(C)n1-c1ccccc1 10.1038/s41467-023-40064-9
22526 14498 None 13 Human Functional pAC50 = 5.5 5.5 -83 25
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 382 4 0 2 5.3 Cc1cc(/C=C/c2ccc3cc(N(C)C)ccc3[n+]2C)c(C)n1-c1ccccc1 10.1038/s41467-023-40064-9
5281035 14498 None 13 Human Functional pAC50 = 5.5 5.5 -83 25
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 382 4 0 2 5.3 Cc1cc(/C=C/c2ccc3cc(N(C)C)ccc3[n+]2C)c(C)n1-c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL1201303 14498 None 13 Human Functional pAC50 = 5.5 5.5 -83 25
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 382 4 0 2 5.3 Cc1cc(/C=C/c2ccc3cc(N(C)C)ccc3[n+]2C)c(C)n1-c1ccccc1 10.1038/s41467-023-40064-9
2749 344 None 32 Human Functional pAC50 = 6.5 6.5 -10 10
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 298 4 0 3 4.5 CN(CC(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
5574 344 None 32 Human Functional pAC50 = 6.5 6.5 -10 10
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 298 4 0 3 4.5 CN(CC(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
5574.0 344 None 32 Human Functional pAC50 = 6.5 6.5 -10 10
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 298 4 0 3 4.5 CN(CC(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
7237 344 None 32 Human Functional pAC50 = 6.5 6.5 -10 10
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 298 4 0 3 4.5 CN(CC(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
CHEMBL829 344 None 32 Human Functional pAC50 = 6.5 6.5 -10 10
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 298 4 0 3 4.5 CN(CC(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
DB01246 344 None 32 Human Functional pAC50 = 6.5 6.5 -10 10
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 298 4 0 3 4.5 CN(CC(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
2406 100458 None 56 Human Functional pAC50 = 5.5 5.5 -18 17
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 354 2 2 3 5.9 Oc1c(Cl)cc(Cl)cc1Sc1cc(Cl)cc(Cl)c1O 10.1038/s41467-023-40064-9
CHEMBL290106 100458 None 56 Human Functional pAC50 = 5.5 5.5 -18 17
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 354 2 2 3 5.9 Oc1c(Cl)cc(Cl)cc1Sc1cc(Cl)cc(Cl)c1O 10.1038/s41467-023-40064-9
4919 208692 None 16 Human Functional pAC50 = 7.5 7.5 1 5
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 287 5 1 2 3.9 OC(CCN1CCCC1)(c1ccccc1)C1CCCCC1 10.1038/s41467-023-40064-9
4919.0 208692 None 16 Human Functional pAC50 = 7.5 7.5 1 5
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 287 5 1 2 3.9 OC(CCN1CCCC1)(c1ccccc1)C1CCCCC1 10.1038/s41467-023-40064-9
CHEMBL86715 208692 None 16 Human Functional pAC50 = 7.5 7.5 1 5
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 287 5 1 2 3.9 OC(CCN1CCCC1)(c1ccccc1)C1CCCCC1 10.1038/s41467-023-40064-9
DB00387 208692 None 16 Human Functional pAC50 = 7.5 7.5 1 5
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 287 5 1 2 3.9 OC(CCN1CCCC1)(c1ccccc1)C1CCCCC1 10.1038/s41467-023-40064-9
5584 205669 None 29 Human Functional pAC50 = 6.5 6.5 -17 9
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 294 4 0 2 4.1 CC(CN(C)C)CN1c2ccccc2CCc2ccccc21 10.1038/s41467-023-40064-9
5584.0 205669 None 29 Human Functional pAC50 = 6.5 6.5 -17 9
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 294 4 0 2 4.1 CC(CN(C)C)CN1c2ccccc2CCc2ccccc21 10.1038/s41467-023-40064-9
CHEMBL644 205669 None 29 Human Functional pAC50 = 6.5 6.5 -17 9
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 294 4 0 2 4.1 CC(CN(C)C)CN1c2ccccc2CCc2ccccc21 10.1038/s41467-023-40064-9
DB00726 205669 None 29 Human Functional pAC50 = 6.5 6.5 -17 9
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 294 4 0 2 4.1 CC(CN(C)C)CN1c2ccccc2CCc2ccccc21 10.1038/s41467-023-40064-9
5832 14466 None 37 Human Functional pAC50 = 5.5 5.5 -3 5
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 340 1 0 3 4.1 C#C[C@]1(OC(C)=O)CC[C@H]2[C@@H]3CCC4=CC(=O)CC[C@@H]4[C@H]3CC[C@@]21C 10.1038/s41467-023-40064-9
CHEMBL1201146 14466 None 37 Human Functional pAC50 = 5.5 5.5 -3 5
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 340 1 0 3 4.1 C#C[C@]1(OC(C)=O)CC[C@H]2[C@@H]3CCC4=CC(=O)CC[C@@H]4[C@H]3CC[C@@]21C 10.1038/s41467-023-40064-9
135 2532 None 33 Human Functional pAC50 = 5.5 5.5 -1230 33
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
1796 2532 None 33 Human Functional pAC50 = 5.5 5.5 -1230 33
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
4184 2532 None 33 Human Functional pAC50 = 5.5 5.5 -1230 33
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
4184.0 2532 None 33 Human Functional pAC50 = 5.5 5.5 -1230 33
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
CHEMBL6437 2532 None 33 Human Functional pAC50 = 5.5 5.5 -1230 33
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
DB06148 2532 None 33 Human Functional pAC50 = 5.5 5.5 -1230 33
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
4614 5393 None 62 Human Functional pAC50 = 5.5 5.5 -39 10
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 293 5 1 3 4.0 O=C(O)CCc1nc(-c2ccccc2)c(-c2ccccc2)o1 10.1038/s41467-023-40064-9
CHEMBL1071 5393 None 62 Human Functional pAC50 = 5.5 5.5 -39 10
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 293 5 1 3 4.0 O=C(O)CCc1nc(-c2ccccc2)c(-c2ccccc2)o1 10.1038/s41467-023-40064-9
72287 61081 None 27 Human Functional pAC50 = 6.5 6.5 -23 9
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 328 5 0 4 4.5 COc1ccc2c(c1)N(C[C@H](C)CN(C)C)c1ccccc1S2 10.1038/s41467-023-40064-9
72287.0 61081 None 27 Human Functional pAC50 = 6.5 6.5 -23 9
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 328 5 0 4 4.5 COc1ccc2c(c1)N(C[C@H](C)CN(C)C)c1ccccc1S2 10.1038/s41467-023-40064-9
CHEMBL1764 61081 None 27 Human Functional pAC50 = 6.5 6.5 -23 9
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 328 5 0 4 4.5 COc1ccc2c(c1)N(C[C@H](C)CN(C)C)c1ccccc1S2 10.1038/s41467-023-40064-9
DB01403 61081 None 27 Human Functional pAC50 = 6.5 6.5 -23 9
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 328 5 0 4 4.5 COc1ccc2c(c1)N(C[C@H](C)CN(C)C)c1ccccc1S2 10.1038/s41467-023-40064-9
6918558 14520 None 31 Human Functional pAC50 = 6.5 6.5 1 2
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 411 10 1 4 5.4 CC(C)C(=O)Oc1ccc(CO)cc1[C@H](CCN(C(C)C)C(C)C)c1ccccc1 10.1038/s41467-023-40064-9
6918558.0 14520 None 31 Human Functional pAC50 = 6.5 6.5 1 2
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 411 10 1 4 5.4 CC(C)C(=O)Oc1ccc(CO)cc1[C@H](CCN(C(C)C)C(C)C)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL1201764 14520 None 31 Human Functional pAC50 = 6.5 6.5 1 2
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 411 10 1 4 5.4 CC(C)C(=O)Oc1ccc(CO)cc1[C@H](CCN(C(C)C)C(C)C)c1ccccc1 10.1038/s41467-023-40064-9
DB06702 14520 None 31 Human Functional pAC50 = 6.5 6.5 1 2
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 411 10 1 4 5.4 CC(C)C(=O)Oc1ccc(CO)cc1[C@H](CCN(C(C)C)C(C)C)c1ccccc1 10.1038/s41467-023-40064-9
242 470 None 70 Human Functional pAC50 = 5.5 5.5 -741 33
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
34 470 None 70 Human Functional pAC50 = 5.5 5.5 -741 33
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
60795 470 None 70 Human Functional pAC50 = 5.5 5.5 -741 33
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
60795.0 470 None 70 Human Functional pAC50 = 5.5 5.5 -741 33
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
CHEMBL1112 470 None 70 Human Functional pAC50 = 5.5 5.5 -741 33
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
DB01238 470 None 70 Human Functional pAC50 = 5.5 5.5 -741 33
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
1201549 597 None 17 Human Functional pAC50 = 7.4 7.4 -1 26
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
1201549.0 597 None 17 Human Functional pAC50 = 7.4 7.4 -1 26
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
333 597 None 17 Human Functional pAC50 = 7.4 7.4 -1 26
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
7601 597 None 17 Human Functional pAC50 = 7.4 7.4 -1 26
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL1201203 597 None 17 Human Functional pAC50 = 7.4 7.4 -1 26
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL438151 597 None 17 Human Functional pAC50 = 7.4 7.4 -1 26
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
DB00245 597 None 17 Human Functional pAC50 = 7.4 7.4 -1 26
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
1086 1590 None 21 Human Functional pAC50 = 7.4 7.4 1 9
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 312 5 0 3 5.0 CCN(C(CN1c2ccccc2Sc2c1cccc2)C)CC 10.1038/s41467-023-40064-9
3290 1590 None 21 Human Functional pAC50 = 7.4 7.4 1 9
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 312 5 0 3 5.0 CCN(C(CN1c2ccccc2Sc2c1cccc2)C)CC 10.1038/s41467-023-40064-9
3290.0 1590 None 21 Human Functional pAC50 = 7.4 7.4 1 9
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 312 5 0 3 5.0 CCN(C(CN1c2ccccc2Sc2c1cccc2)C)CC 10.1038/s41467-023-40064-9
7181 1590 None 21 Human Functional pAC50 = 7.4 7.4 1 9
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 312 5 0 3 5.0 CCN(C(CN1c2ccccc2Sc2c1cccc2)C)CC 10.1038/s41467-023-40064-9
CHEMBL1206 1590 None 21 Human Functional pAC50 = 7.4 7.4 1 9
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 312 5 0 3 5.0 CCN(C(CN1c2ccccc2Sc2c1cccc2)C)CC 10.1038/s41467-023-40064-9
DB00392 1590 None 21 Human Functional pAC50 = 7.4 7.4 1 9
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 312 5 0 3 5.0 CCN(C(CN1c2ccccc2Sc2c1cccc2)C)CC 10.1038/s41467-023-40064-9
2995 206863 None 31 Human Functional pAC50 = 5.4 5.4 -1348 18
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 10.1038/s41467-023-40064-9
2995.0 206863 None 31 Human Functional pAC50 = 5.4 5.4 -1348 18
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 10.1038/s41467-023-40064-9
CHEMBL1696 206863 None 31 Human Functional pAC50 = 5.4 5.4 -1348 18
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 10.1038/s41467-023-40064-9
CHEMBL72 206863 None 31 Human Functional pAC50 = 5.4 5.4 -1348 18
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 10.1038/s41467-023-40064-9
DB01151 206863 None 31 Human Functional pAC50 = 5.4 5.4 -1348 18
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 10.1038/s41467-023-40064-9
103 4153 None 44 Human Functional pAC50 = 5.4 5.4 -131 22
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
2875 4153 None 44 Human Functional pAC50 = 5.4 5.4 -131 22
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
5736 4153 None 44 Human Functional pAC50 = 5.4 5.4 -131 22
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
CHEMBL285802 4153 None 44 Human Functional pAC50 = 5.4 5.4 -131 22
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
DB09225 4153 None 44 Human Functional pAC50 = 5.4 5.4 -131 22
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
24821094 67115 None 58 Human Functional pAC50 = 5.4 5.4 -1 8
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 440 5 1 7 4.2 C=CC(=O)N1CCC[C@@H](n2nc(-c3ccc(Oc4ccccc4)cc3)c3c(N)ncnc32)C1 10.1038/s41467-023-40064-9
CHEMBL1873475 67115 None 58 Human Functional pAC50 = 5.4 5.4 -1 8
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 440 5 1 7 4.2 C=CC(=O)N1CCC[C@@H](n2nc(-c3ccc(Oc4ccccc4)cc3)c3c(N)ncnc32)C1 10.1038/s41467-023-40064-9
135 2532 None 33 Human Functional pAC50 = 5.4 5.4 -1230 33
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
1796 2532 None 33 Human Functional pAC50 = 5.4 5.4 -1230 33
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
4184 2532 None 33 Human Functional pAC50 = 5.4 5.4 -1230 33
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
4184.0 2532 None 33 Human Functional pAC50 = 5.4 5.4 -1230 33
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
CHEMBL6437 2532 None 33 Human Functional pAC50 = 5.4 5.4 -1230 33
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
DB06148 2532 None 33 Human Functional pAC50 = 5.4 5.4 -1230 33
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
2166 3123 None 33 Human Functional pAC50 = 7.4 7.4 -3 10
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 10.1038/s41467-023-40064-9
305 3123 None 33 Human Functional pAC50 = 7.4 7.4 -3 10
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 10.1038/s41467-023-40064-9
5910 3123 None 33 Human Functional pAC50 = 7.4 7.4 -3 10
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 10.1038/s41467-023-40064-9
5910.0 3123 None 33 Human Functional pAC50 = 7.4 7.4 -3 10
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 10.1038/s41467-023-40064-9
CHEMBL550 3123 None 33 Human Functional pAC50 = 7.4 7.4 -3 10
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 10.1038/s41467-023-40064-9
DB01085 3123 None 33 Human Functional pAC50 = 7.4 7.4 -3 10
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 10.1038/s41467-023-40064-9
122262 102447 None 38 Human Functional pAC50 = 5.4 5.4 1 4
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 534 6 0 6 5.4 Clc1ccc2c(N3CCN(CCCN4CCN(c5ccnc6cc(Cl)ccc56)CC4)CC3)ccnc2c1 10.1038/s41467-023-40064-9
CHEMBL303933 102447 None 38 Human Functional pAC50 = 5.4 5.4 1 4
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 534 6 0 6 5.4 Clc1ccc2c(N3CCN(CCCN4CCN(c5ccnc6cc(Cl)ccc56)CC4)CC3)ccnc2c1 10.1038/s41467-023-40064-9
9853053 120583 None 54 Human Functional pAC50 = 5.4 5.4 -2 9
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 693 10 2 3 8.4 O=C(NC1CCN(CCCCC2(C(=O)NCC(F)(F)F)c3ccccc3-c3ccccc32)CC1)c1ccccc1-c1ccc(C(F)(F)F)cc1 10.1038/s41467-023-40064-9
CHEMBL354541 120583 None 54 Human Functional pAC50 = 5.4 5.4 -2 9
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 693 10 2 3 8.4 O=C(NC1CCN(CCCCC2(C(=O)NCC(F)(F)F)c3ccccc3-c3ccccc32)CC1)c1ccccc1-c1ccc(C(F)(F)F)cc1 10.1038/s41467-023-40064-9
25151352 140693 None 56 Human Functional pAC50 = 6.4 6.4 1 11
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 417 5 2 4 5.2 FC(F)(F)c1ccc(CNc2ccc(Cc3c[nH]c4ncc(Cl)cc34)cn2)cn1 10.1038/s41467-023-40064-9
CHEMBL3813873 140693 None 56 Human Functional pAC50 = 6.4 6.4 1 11
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 417 5 2 4 5.2 FC(F)(F)c1ccc(CNc2ccc(Cc3c[nH]c4ncc(Cl)cc34)cn2)cn1 10.1038/s41467-023-40064-9
5453 206077 None 58 Human Functional pAC50 = 6.4 6.4 -8 14
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 189 3 0 1 0.2 S=P(N1CC1)(N1CC1)N1CC1 10.1038/s41467-023-40064-9
CHEMBL671 206077 None 58 Human Functional pAC50 = 6.4 6.4 -8 14
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 189 3 0 1 0.2 S=P(N1CC1)(N1CC1)N1CC1 10.1038/s41467-023-40064-9
25897919 55668 None 12 Human Functional pAC50 = 8.4 8.4 -2 5
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1038/s41467-023-40064-9
657308 55668 None 12 Human Functional pAC50 = 8.4 8.4 -2 5
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1038/s41467-023-40064-9
657309 55668 None 12 Human Functional pAC50 = 8.4 8.4 -2 5
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1038/s41467-023-40064-9
CHEMBL1621597 55668 None 12 Human Functional pAC50 = 8.4 8.4 -2 5
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1038/s41467-023-40064-9
DB00332 55668 None 12 Human Functional pAC50 = 8.4 8.4 -2 5
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 332 5 1 3 2.9 CC(C)[N+]1(C)[C@H]2CC[C@@H]1C[C@H](OC(=O)C(CO)c1ccccc1)C2 10.1038/s41467-023-40064-9
2381 663 None 30 Human Functional pAC50 = 8.4 8.4 25 5
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 10.1038/s41467-023-40064-9
2381.0 663 None 30 Human Functional pAC50 = 8.4 8.4 25 5
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 10.1038/s41467-023-40064-9
374 663 None 30 Human Functional pAC50 = 8.4 8.4 25 5
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 10.1038/s41467-023-40064-9
7128 663 None 30 Human Functional pAC50 = 8.4 8.4 25 5
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 10.1038/s41467-023-40064-9
CHEMBL1101 663 None 30 Human Functional pAC50 = 8.4 8.4 25 5
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 10.1038/s41467-023-40064-9
DB00810 663 None 30 Human Functional pAC50 = 8.4 8.4 25 5
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 10.1038/s41467-023-40064-9
135398737 958 None 57 Human Functional pAC50 = 7.4 7.4 -6 43
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
135398737.0 958 None 57 Human Functional pAC50 = 7.4 7.4 -6 43
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
38 958 None 57 Human Functional pAC50 = 7.4 7.4 -6 43
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
722 958 None 57 Human Functional pAC50 = 7.4 7.4 -6 43
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL42 958 None 57 Human Functional pAC50 = 7.4 7.4 -6 43
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
DB00363 958 None 57 Human Functional pAC50 = 7.4 7.4 -6 43
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
4921596 98836 None 55 Human Functional pAC50 = 4.4 4.4 -8 4
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 365 3 2 5 2.4 NC1CCN(c2c(F)cc3c(=O)c(C(=O)O)cn(C4CC4)c3c2Cl)C1 10.1038/s41467-023-40064-9
60063 98836 None 55 Human Functional pAC50 = 4.4 4.4 -8 4
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 365 3 2 5 2.4 NC1CCN(c2c(F)cc3c(=O)c(C(=O)O)cn(C4CC4)c3c2Cl)C1 10.1038/s41467-023-40064-9
CHEMBL278255 98836 None 55 Human Functional pAC50 = 4.4 4.4 -8 4
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 365 3 2 5 2.4 NC1CCN(c2c(F)cc3c(=O)c(C(=O)O)cn(C4CC4)c3c2Cl)C1 10.1038/s41467-023-40064-9
443869 78170 None 28 Human Functional pAC50 = 5.4 5.4 -3 10
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 491 7 1 8 3.8 COC(=O)C1=C(C)NC(C)=C(C(=O)O[C@H]2CCN(Cc3ccccc3)C2)[C@H]1c1cccc([N+](=O)[O-])c1 10.1038/s41467-023-40064-9
CHEMBL2103761 78170 None 28 Human Functional pAC50 = 5.4 5.4 -3 10
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 491 7 1 8 3.8 COC(=O)C1=C(C)NC(C)=C(C(=O)O[C@H]2CCN(Cc3ccccc3)C2)[C@H]1c1cccc([N+](=O)[O-])c1 10.1038/s41467-023-40064-9
2551 794 None 13 Human Functional pAC50 = 7.4 7.4 -27 13
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1038/s41467-023-40064-9
2551.0 794 None 13 Human Functional pAC50 = 7.4 7.4 -27 13
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1038/s41467-023-40064-9
298 794 None 13 Human Functional pAC50 = 7.4 7.4 -27 13
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1038/s41467-023-40064-9
488 794 None 13 Human Functional pAC50 = 7.4 7.4 -27 13
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1038/s41467-023-40064-9
CHEMBL965 794 None 13 Human Functional pAC50 = 7.4 7.4 -27 13
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1038/s41467-023-40064-9
DB00411 794 None 13 Human Functional pAC50 = 7.4 7.4 -27 13
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1038/s41467-023-40064-9
6127 14505 None 4 Human Functional pAC50 = 6.4 6.4 -1 6
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 278 2 0 0 4.4 C[N+]1(C)CCC(=C(c2ccccc2)c2ccccc2)CC1 10.1038/s41467-023-40064-9
6127.0 14505 None 4 Human Functional pAC50 = 6.4 6.4 -1 6
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 278 2 0 0 4.4 C[N+]1(C)CCC(=C(c2ccccc2)c2ccccc2)CC1 10.1038/s41467-023-40064-9
CHEMBL1201340 14505 None 4 Human Functional pAC50 = 6.4 6.4 -1 6
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 278 2 0 0 4.4 C[N+]1(C)CCC(=C(c2ccccc2)c2ccccc2)CC1 10.1038/s41467-023-40064-9
DB13720 14505 None 4 Human Functional pAC50 = 6.4 6.4 -1 6
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 278 2 0 0 4.4 C[N+]1(C)CCC(=C(c2ccccc2)c2ccccc2)CC1 10.1038/s41467-023-40064-9
2337 3256 None 51 Human Functional pAC50 = 5.4 5.4 -162 29
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
50 3256 None 51 Human Functional pAC50 = 5.4 5.4 -162 29
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
5002 3256 None 51 Human Functional pAC50 = 5.4 5.4 -162 29
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
5002.0 3256 None 51 Human Functional pAC50 = 5.4 5.4 -162 29
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL716 3256 None 51 Human Functional pAC50 = 5.4 5.4 -162 29
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
DB01224 3256 None 51 Human Functional pAC50 = 5.4 5.4 -162 29
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
4756 16656 None 34 Human Functional pAC50 = 5.4 5.4 -2 16
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 213 2 2 5 2.7 Nc1ccc(/N=N/c2ccccc2)c(N)n1 10.1038/s41467-023-40064-9
CHEMBL1201022 16656 None 34 Human Functional pAC50 = 5.4 5.4 -2 16
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 213 2 2 5 2.7 Nc1ccc(/N=N/c2ccccc2)c(N)n1 10.1038/s41467-023-40064-9
CHEMBL1242 16656 None 34 Human Functional pAC50 = 5.4 5.4 -2 16
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 213 2 2 5 2.7 Nc1ccc(/N=N/c2ccccc2)c(N)n1 10.1038/s41467-023-40064-9
4450 178333 None 41 Human Functional pAC50 = 5.4 5.4 -6 11
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 253 1 0 2 3.2 CN1CCOC(c2ccccc2)c2ccccc2C1 10.1038/s41467-023-40064-9
CHEMBL465026 178333 None 41 Human Functional pAC50 = 5.4 5.4 -6 11
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 253 1 0 2 3.2 CN1CCOC(c2ccccc2)c2ccccc2C1 10.1038/s41467-023-40064-9
5994 4643 None 51 Human Functional pAC50 = 5.4 5.4 -1 10
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 314 1 0 2 4.7 CC(=O)[C@H]1CC[C@H]2[C@@H]3CCC4=CC(=O)CC[C@]4(C)[C@H]3CC[C@]12C 10.1038/s41467-023-40064-9
CHEMBL103 4643 None 51 Human Functional pAC50 = 5.4 5.4 -1 10
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 314 1 0 2 4.7 CC(=O)[C@H]1CC[C@H]2[C@@H]3CCC4=CC(=O)CC[C@]4(C)[C@H]3CC[C@]12C 10.1038/s41467-023-40064-9
16351 102785 None 36 Human Functional pAC50 = 6.4 6.4 -114 17
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 343 0 0 4 4.1 CN1CCN(C2=Nc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1038/s41467-023-40064-9
16351.0 102785 None 36 Human Functional pAC50 = 6.4 6.4 -114 17
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 343 0 0 4 4.1 CN1CCN(C2=Nc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1038/s41467-023-40064-9
CHEMBL304902 102785 None 36 Human Functional pAC50 = 6.4 6.4 -114 17
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 343 0 0 4 4.1 CN1CCN(C2=Nc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1038/s41467-023-40064-9
DB13256 102785 None 36 Human Functional pAC50 = 6.4 6.4 -114 17
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 343 0 0 4 4.1 CN1CCN(C2=Nc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1038/s41467-023-40064-9
10180 98923 None 36 Human Functional pAC50 = 5.4 5.4 -7 11
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 340 6 1 4 4.5 CCN(CC)CCNc1ccc(C)c2sc3ccccc3c(=O)c12 10.1038/s41467-023-40064-9
CHEMBL279014 98923 None 36 Human Functional pAC50 = 5.4 5.4 -7 11
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 340 6 1 4 4.5 CCN(CC)CCNc1ccc(C)c2sc3ccccc3c(=O)c12 10.1038/s41467-023-40064-9
3947 208853 None 39 Human Functional pAC50 = 5.4 5.4 -6 16
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 418 7 0 3 5.8 CN(CCCN1c2ccccc2CCc2ccccc21)CC(=O)c1ccc(Cl)cc1 10.1038/s41467-023-40064-9
CHEMBL87708 208853 None 39 Human Functional pAC50 = 5.4 5.4 -6 16
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 418 7 0 3 5.8 CN(CCCN1c2ccccc2CCc2ccccc21)CC(=O)c1ccc(Cl)cc1 10.1038/s41467-023-40064-9
41684 31229 None 62 Human Functional pAC50 = 5.4 5.4 -9 32
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 307 4 1 7 2.2 CC(=O)Oc1ccccc1C(=O)Nc1ncc([N+](=O)[O-])s1 10.1038/s41467-023-40064-9
CHEMBL1401 31229 None 62 Human Functional pAC50 = 5.4 5.4 -9 32
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 307 4 1 7 2.2 CC(=O)Oc1ccccc1C(=O)Nc1ncc([N+](=O)[O-])s1 10.1038/s41467-023-40064-9
82146 4532 None 68 Human Functional pAC50 = 5.4 5.4 -1 8
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 348 3 1 1 6.1 C=C(c1ccc(C(=O)O)cc1)c1cc2c(cc1C)C(C)(C)CCC2(C)C 10.1038/s41467-023-40064-9
CHEMBL1023 4532 None 68 Human Functional pAC50 = 5.4 5.4 -1 8
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 348 3 1 1 6.1 C=C(c1ccc(C(=O)O)cc1)c1cc2c(cc1C)C(C)(C)CCC2(C)C 10.1038/s41467-023-40064-9
1224 1432 None 51 Human Functional pAC50 = 5.4 5.4 -416 22
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
3100 1432 None 51 Human Functional pAC50 = 5.4 5.4 -416 22
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
3100.0 1432 None 51 Human Functional pAC50 = 5.4 5.4 -416 22
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
8980 1432 None 51 Human Functional pAC50 = 5.4 5.4 -416 22
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
916 1432 None 51 Human Functional pAC50 = 5.4 5.4 -416 22
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
CHEMBL657 1432 None 51 Human Functional pAC50 = 5.4 5.4 -416 22
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
DB01075 1432 None 51 Human Functional pAC50 = 5.4 5.4 -416 22
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
150311 9814 None 69 Human Functional pAC50 = 5.3 5.3 1 7
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 409 6 2 3 4.9 O=C1[C@H](CC[C@H](O)c2ccc(F)cc2)[C@@H](c2ccc(O)cc2)N1c1ccc(F)cc1 10.1038/s41467-023-40064-9
CHEMBL1138 9814 None 69 Human Functional pAC50 = 5.3 5.3 1 7
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 409 6 2 3 4.9 O=C1[C@H](CC[C@H](O)c2ccc(F)cc2)[C@@H](c2ccc(O)cc2)N1c1ccc(F)cc1 10.1038/s41467-023-40064-9
135398745 2914 None 65 Human Functional pAC50 = 7.3 7.3 -5 33
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
135398745.0 2914 None 65 Human Functional pAC50 = 7.3 7.3 -5 33
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
47 2914 None 65 Human Functional pAC50 = 7.3 7.3 -5 33
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
CHEMBL715 2914 None 65 Human Functional pAC50 = 7.3 7.3 -5 33
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
DB00334 2914 None 65 Human Functional pAC50 = 7.3 7.3 -5 33
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
100 3805 None 44 Human Functional pAC50 = 6.3 6.3 -12 38
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1038/s41467-023-40064-9
2637 3805 None 44 Human Functional pAC50 = 6.3 6.3 -12 38
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1038/s41467-023-40064-9
5452 3805 None 44 Human Functional pAC50 = 6.3 6.3 -12 38
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1038/s41467-023-40064-9
CHEMBL479 3805 None 44 Human Functional pAC50 = 6.3 6.3 -12 38
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1038/s41467-023-40064-9
DB00679 3805 None 44 Human Functional pAC50 = 6.3 6.3 -12 38
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1038/s41467-023-40064-9
1971 2866 None 32 Human Functional pAC50 = 6.3 6.3 -269 32
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1038/s41467-023-40064-9
2404 2866 None 32 Human Functional pAC50 = 6.3 6.3 -269 32
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1038/s41467-023-40064-9
4543 2866 None 32 Human Functional pAC50 = 6.3 6.3 -269 32
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1038/s41467-023-40064-9
4543.0 2866 None 32 Human Functional pAC50 = 6.3 6.3 -269 32
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL445 2866 None 32 Human Functional pAC50 = 6.3 6.3 -269 32
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1038/s41467-023-40064-9
DB00540 2866 None 32 Human Functional pAC50 = 6.3 6.3 -269 32
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1038/s41467-023-40064-9
160883 55280 None 4 Human Functional pAC50 = 5.3 5.3 -12 2
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 360 7 1 4 2.2 CCCC[N+]1(C)[C@@H]2C[C@@H](OC(=O)[C@H](CO)c3ccccc3)C[C@H]1[C@@H]1O[C@@H]12 10.1038/s41467-023-40064-9
160883.0 55280 None 4 Human Functional pAC50 = 5.3 5.3 -12 2
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 360 7 1 4 2.2 CCCC[N+]1(C)[C@@H]2C[C@@H](OC(=O)[C@H](CO)c3ccccc3)C[C@H]1[C@@H]1O[C@@H]12 10.1038/s41467-023-40064-9
6852391 55280 None 4 Human Functional pAC50 = 5.3 5.3 -12 2
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 360 7 1 4 2.2 CCCC[N+]1(C)[C@@H]2C[C@@H](OC(=O)[C@H](CO)c3ccccc3)C[C@H]1[C@@H]1O[C@@H]12 10.1038/s41467-023-40064-9
6852391.0 55280 None 4 Human Functional pAC50 = 5.3 5.3 -12 2
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 360 7 1 4 2.2 CCCC[N+]1(C)[C@@H]2C[C@@H](OC(=O)[C@H](CO)c3ccccc3)C[C@H]1[C@@H]1O[C@@H]12 10.1038/s41467-023-40064-9
CHEMBL1618102 55280 None 4 Human Functional pAC50 = 5.3 5.3 -12 2
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 360 7 1 4 2.2 CCCC[N+]1(C)[C@@H]2C[C@@H](OC(=O)[C@H](CO)c3ccccc3)C[C@H]1[C@@H]1O[C@@H]12 10.1038/s41467-023-40064-9
DB09300 55280 None 4 Human Functional pAC50 = 5.3 5.3 -12 2
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 360 7 1 4 2.2 CCCC[N+]1(C)[C@@H]2C[C@@H](OC(=O)[C@H](CO)c3ccccc3)C[C@H]1[C@@H]1O[C@@H]12 10.1038/s41467-023-40064-9
180 401 None 38 Human Functional pAC50 = 7.3 7.3 -147 38
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
200 401 None 38 Human Functional pAC50 = 7.3 7.3 -147 38
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
2160 401 None 38 Human Functional pAC50 = 7.3 7.3 -147 38
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
2160.0 401 None 38 Human Functional pAC50 = 7.3 7.3 -147 38
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
CHEMBL629 401 None 38 Human Functional pAC50 = 7.3 7.3 -147 38
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
DB00321 401 None 38 Human Functional pAC50 = 7.3 7.3 -147 38
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
1427 2013 None 42 Human Functional pAC50 = 6.3 6.3 -630 30
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
357 2013 None 42 Human Functional pAC50 = 6.3 6.3 -630 30
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
3696 2013 None 42 Human Functional pAC50 = 6.3 6.3 -630 30
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
CHEMBL11 2013 None 42 Human Functional pAC50 = 6.3 6.3 -630 30
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
DB00458 2013 None 42 Human Functional pAC50 = 6.3 6.3 -630 30
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
3158 56283 None 21 Human Functional pAC50 = 6.3 6.3 -281 28
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 10.1038/s41467-023-40064-9
3158.0 56283 None 21 Human Functional pAC50 = 6.3 6.3 -281 28
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 10.1038/s41467-023-40064-9
CHEMBL1628227 56283 None 21 Human Functional pAC50 = 6.3 6.3 -281 28
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 10.1038/s41467-023-40064-9
DB01142 56283 None 21 Human Functional pAC50 = 6.3 6.3 -281 28
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 10.1038/s41467-023-40064-9
43082 60303 None 26 Human Functional pAC50 = 6.3 6.3 -1 10
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 357 6 0 2 5.5 CC(OCCN1CCCCCC1)(c1ccccc1)c1ccc(Cl)cc1 10.1038/s41467-023-40064-9
CHEMBL1742452 60303 None 26 Human Functional pAC50 = 6.3 6.3 -1 10
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 357 6 0 2 5.5 CC(OCCN1CCCCCC1)(c1ccccc1)c1ccc(Cl)cc1 10.1038/s41467-023-40064-9
174174 523 None 33 Human Functional pAC50 = 8.3 8.3 -8 7
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1038/s41467-023-40064-9
174174.0 523 None 33 Human Functional pAC50 = 8.3 8.3 -8 7
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1038/s41467-023-40064-9
260 523 None 33 Human Functional pAC50 = 8.3 8.3 -8 7
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1038/s41467-023-40064-9
320 523 None 33 Human Functional pAC50 = 8.3 8.3 -8 7
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1038/s41467-023-40064-9
CHEMBL517712 523 None 33 Human Functional pAC50 = 8.3 8.3 -8 7
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1038/s41467-023-40064-9
DB00572 523 None 33 Human Functional pAC50 = 8.3 8.3 -8 7
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1038/s41467-023-40064-9
2705 3842 None 44 Human Functional pAC50 = 8.3 8.3 -1 12
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1038/s41467-023-40064-9
360 3842 None 44 Human Functional pAC50 = 8.3 8.3 -1 12
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1038/s41467-023-40064-9
443879 3842 None 44 Human Functional pAC50 = 8.3 8.3 -1 12
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1038/s41467-023-40064-9
443879.0 3842 None 44 Human Functional pAC50 = 8.3 8.3 -1 12
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1038/s41467-023-40064-9
CHEMBL1382 3842 None 44 Human Functional pAC50 = 8.3 8.3 -1 12
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1038/s41467-023-40064-9
DB01036 3842 None 44 Human Functional pAC50 = 8.3 8.3 -1 12
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1038/s41467-023-40064-9
2028 2979 None 52 Human Functional pAC50 = 8.3 8.3 -2 14
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 10.1038/s41467-023-40064-9
359 2979 None 52 Human Functional pAC50 = 8.3 8.3 -2 14
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 10.1038/s41467-023-40064-9
4634 2979 None 52 Human Functional pAC50 = 8.3 8.3 -2 14
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 10.1038/s41467-023-40064-9
4634.0 2979 None 52 Human Functional pAC50 = 8.3 8.3 -2 14
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 10.1038/s41467-023-40064-9
CHEMBL1231 2979 None 52 Human Functional pAC50 = 8.3 8.3 -2 14
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 10.1038/s41467-023-40064-9
DB01062 2979 None 52 Human Functional pAC50 = 8.3 8.3 -2 14
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 10.1038/s41467-023-40064-9
11519069 3939 None 2 Human Functional pAC50 = 8.3 8.3 -1 3
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
11519070 3939 None 2 Human Functional pAC50 = 8.3 8.3 -1 3
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
11519070.0 3939 None 2 Human Functional pAC50 = 8.3 8.3 -1 3
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
4816 3939 None 2 Human Functional pAC50 = 8.3 8.3 -1 3
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
7354 3939 None 2 Human Functional pAC50 = 8.3 8.3 -1 3
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL1187833 3939 None 2 Human Functional pAC50 = 8.3 8.3 -1 3
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
DB09076 3939 None 2 Human Functional pAC50 = 8.3 8.3 -1 3
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 428 8 1 2 5.1 OC(C12CC[N+](CC1)(CC2)CCOCc1ccccc1)(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
11693 1827 None 12 Human Functional pAC50 = 8.3 8.3 -4 7
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1038/s41467-023-40064-9
3494 1827 None 12 Human Functional pAC50 = 8.3 8.3 -4 7
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1038/s41467-023-40064-9
3494.0 1827 None 12 Human Functional pAC50 = 8.3 8.3 -4 7
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1038/s41467-023-40064-9
4302 1827 None 12 Human Functional pAC50 = 8.3 8.3 -4 7
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1038/s41467-023-40064-9
7459 1827 None 12 Human Functional pAC50 = 8.3 8.3 -4 7
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1038/s41467-023-40064-9
9933193 1827 None 12 Human Functional pAC50 = 8.3 8.3 -4 7
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1038/s41467-023-40064-9
9933193.0 1827 None 12 Human Functional pAC50 = 8.3 8.3 -4 7
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1038/s41467-023-40064-9
CHEMBL1201335 1827 None 12 Human Functional pAC50 = 8.3 8.3 -4 7
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1038/s41467-023-40064-9
DB00986 1827 None 12 Human Functional pAC50 = 8.3 8.3 -4 7
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 318 4 1 3 2.5 O=C(C(c1ccccc1)(C1CCCC1)O)OC1CC[N+](C1)(C)C 10.1038/s41467-023-40064-9
2435 3590 None 59 Human Functional pAC50 = 5.3 5.3 -1230 21
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1038/s41467-023-40064-9
60149 3590 None 59 Human Functional pAC50 = 5.3 5.3 -1230 21
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1038/s41467-023-40064-9
98 3590 None 59 Human Functional pAC50 = 5.3 5.3 -1230 21
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1038/s41467-023-40064-9
CHEMBL12713 3590 None 59 Human Functional pAC50 = 5.3 5.3 -1230 21
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1038/s41467-023-40064-9
DB06144 3590 None 59 Human Functional pAC50 = 5.3 5.3 -1230 21
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1038/s41467-023-40064-9
9051 14447 None 46 Human Functional pAC50 = 5.3 5.3 5 3
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 312 1 0 2 4.5 CC(=O)[C@H]1CC[C@H]2[C@@H]3C=CC4=CC(=O)CC[C@@]4(C)[C@@H]3CC[C@]12C 10.1038/s41467-023-40064-9
CHEMBL1200853 14447 None 46 Human Functional pAC50 = 5.3 5.3 5 3
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 312 1 0 2 4.5 CC(=O)[C@H]1CC[C@H]2[C@@H]3C=CC4=CC(=O)CC[C@@]4(C)[C@@H]3CC[C@]12C 10.1038/s41467-023-40064-9
5591 157623 None 57 Human Functional pAC50 = 5.3 5.3 -3 17
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 441 5 2 6 4.4 Cc1c(C)c2c(c(C)c1O)CCC(C)(COc1ccc(CC3SC(=O)NC3=O)cc1)O2 10.1038/s41467-023-40064-9
CHEMBL408 157623 None 57 Human Functional pAC50 = 5.3 5.3 -3 17
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 441 5 2 6 4.4 Cc1c(C)c2c(c(C)c1O)CCC(C)(COc1ccc(CC3SC(=O)NC3=O)cc1)O2 10.1038/s41467-023-40064-9
3055 1433 None 30 Human Functional pAC50 = 6.3 6.3 -1 12
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 309 6 1 2 4.2 OC(c1ccccc1)(c1ccccc1)CCCN1CCCCC1 10.1038/s41467-023-40064-9
313 1433 None 30 Human Functional pAC50 = 6.3 6.3 -1 12
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 309 6 1 2 4.2 OC(c1ccccc1)(c1ccccc1)CCCN1CCCCC1 10.1038/s41467-023-40064-9
7163 1433 None 30 Human Functional pAC50 = 6.3 6.3 -1 12
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 309 6 1 2 4.2 OC(c1ccccc1)(c1ccccc1)CCCN1CCCCC1 10.1038/s41467-023-40064-9
CHEMBL936 1433 None 30 Human Functional pAC50 = 6.3 6.3 -1 12
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 309 6 1 2 4.2 OC(c1ccccc1)(c1ccccc1)CCCN1CCCCC1 10.1038/s41467-023-40064-9
DB01231 1433 None 30 Human Functional pAC50 = 6.3 6.3 -1 12
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 309 6 1 2 4.2 OC(c1ccccc1)(c1ccccc1)CCCN1CCCCC1 10.1038/s41467-023-40064-9
1923 104780 None 79 Human Functional pAC50 = 5.3 5.3 3 3
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 145 0 1 2 1.9 Oc1cccc2cccnc12 10.1038/s41467-023-40064-9
CHEMBL310555 104780 None 79 Human Functional pAC50 = 5.3 5.3 3 3
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 145 0 1 2 1.9 Oc1cccc2cccnc12 10.1038/s41467-023-40064-9
3152 188518 None 61 Human Functional pAC50 = 5.3 5.3 -15 10
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 379 6 0 4 4.4 COc1cc2c(cc1OC)C(=O)C(CC1CCN(Cc3ccccc3)CC1)C2 10.1038/s41467-023-40064-9
CHEMBL502 188518 None 61 Human Functional pAC50 = 5.3 5.3 -15 10
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 379 6 0 4 4.4 COc1cc2c(cc1OC)C(=O)C(CC1CCN(Cc3ccccc3)CC1)C2 10.1038/s41467-023-40064-9
1547484 940 None 51 Human Functional pAC50 = 5.3 5.3 -45 26
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
1547484.0 940 None 51 Human Functional pAC50 = 5.3 5.3 -45 26
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
654 940 None 51 Human Functional pAC50 = 5.3 5.3 -45 26
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
9072 940 None 51 Human Functional pAC50 = 5.3 5.3 -45 26
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL43064 940 None 51 Human Functional pAC50 = 5.3 5.3 -45 26
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
DB00568 940 None 51 Human Functional pAC50 = 5.3 5.3 -45 26
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
1193 1656 None 64 Human Functional pAC50 = 6.3 6.3 -6 11
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 281 3 2 2 4.1 OC(=O)c1ccccc1Nc1cccc(c1)C(F)(F)F 10.1038/s41467-023-40064-9
2447 1656 None 64 Human Functional pAC50 = 6.3 6.3 -6 11
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 281 3 2 2 4.1 OC(=O)c1ccccc1Nc1cccc(c1)C(F)(F)F 10.1038/s41467-023-40064-9
3371 1656 None 64 Human Functional pAC50 = 6.3 6.3 -6 11
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 281 3 2 2 4.1 OC(=O)c1ccccc1Nc1cccc(c1)C(F)(F)F 10.1038/s41467-023-40064-9
CHEMBL23588 1656 None 64 Human Functional pAC50 = 6.3 6.3 -6 11
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 281 3 2 2 4.1 OC(=O)c1ccccc1Nc1cccc(c1)C(F)(F)F 10.1038/s41467-023-40064-9
DB02266 1656 None 64 Human Functional pAC50 = 6.3 6.3 -6 11
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 281 3 2 2 4.1 OC(=O)c1ccccc1Nc1cccc(c1)C(F)(F)F 10.1038/s41467-023-40064-9
2805 161984 None 27 Human Functional pAC50 = 6.3 6.3 -1 9
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 329 6 0 2 4.9 Clc1ccc(C(OCCN2CCCCC2)c2ccccc2)cc1 10.1038/s41467-023-40064-9
CHEMBL415087 161984 None 27 Human Functional pAC50 = 6.3 6.3 -1 9
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 329 6 0 2 4.9 Clc1ccc(C(OCCN2CCCCC2)c2ccccc2)cc1 10.1038/s41467-023-40064-9
2107 3055 None 44 Human Functional pAC50 = 5.3 5.3 -1737 9
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 365 4 1 5 4.0 N#Cc1ccc2c(c1)N(CCCN1CCC(CC1)O)c1c(S2)cccc1 10.1038/s41467-023-40064-9
4747 3055 None 44 Human Functional pAC50 = 5.3 5.3 -1737 9
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 365 4 1 5 4.0 N#Cc1ccc2c(c1)N(CCCN1CCC(CC1)O)c1c(S2)cccc1 10.1038/s41467-023-40064-9
4747.0 3055 None 44 Human Functional pAC50 = 5.3 5.3 -1737 9
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 365 4 1 5 4.0 N#Cc1ccc2c(c1)N(CCCN1CCC(CC1)O)c1c(S2)cccc1 10.1038/s41467-023-40064-9
9216 3055 None 44 Human Functional pAC50 = 5.3 5.3 -1737 9
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 365 4 1 5 4.0 N#Cc1ccc2c(c1)N(CCCN1CCC(CC1)O)c1c(S2)cccc1 10.1038/s41467-023-40064-9
CHEMBL251940 3055 None 44 Human Functional pAC50 = 5.3 5.3 -1737 9
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 365 4 1 5 4.0 N#Cc1ccc2c(c1)N(CCCN1CCC(CC1)O)c1c(S2)cccc1 10.1038/s41467-023-40064-9
DB01608 3055 None 44 Human Functional pAC50 = 5.3 5.3 -1737 9
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 365 4 1 5 4.0 N#Cc1ccc2c(c1)N(CCCN1CCC(CC1)O)c1c(S2)cccc1 10.1038/s41467-023-40064-9
176 398 None 47 Human Functional pAC50 = 5.3 5.3 -22 40
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 10.1038/s41467-023-40064-9
2157 398 None 47 Human Functional pAC50 = 5.3 5.3 -22 40
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 10.1038/s41467-023-40064-9
2157.0 398 None 47 Human Functional pAC50 = 5.3 5.3 -22 40
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 10.1038/s41467-023-40064-9
2566 398 None 47 Human Functional pAC50 = 5.3 5.3 -22 40
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 10.1038/s41467-023-40064-9
CHEMBL633 398 None 47 Human Functional pAC50 = 5.3 5.3 -22 40
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 10.1038/s41467-023-40064-9
DB01118 398 None 47 Human Functional pAC50 = 5.3 5.3 -22 40
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 10.1038/s41467-023-40064-9
1548955 88615 None 14 Human Functional pAC50 = 5.3 5.3 -15 11
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 405 9 0 2 6.6 CCN(CC)CCOc1ccc(C(=C(Cl)c2ccccc2)c2ccccc2)cc1 10.1038/s41467-023-40064-9
2800 88615 None 14 Human Functional pAC50 = 5.3 5.3 -15 11
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 405 9 0 2 6.6 CCN(CC)CCOc1ccc(C(=C(Cl)c2ccccc2)c2ccccc2)cc1 10.1038/s41467-023-40064-9
CHEMBL2355051 88615 None 14 Human Functional pAC50 = 5.3 5.3 -15 11
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 405 9 0 2 6.6 CCN(CC)CCOc1ccc(C(=C(Cl)c2ccccc2)c2ccccc2)cc1 10.1038/s41467-023-40064-9
68778 115269 None 46 Human Functional pAC50 = 6.2 6.2 -1 3
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 293 2 0 1 4.9 CC(C)(C)N1CCC(c2ccccc2)(c2ccccc2)CC1 10.1038/s41467-023-40064-9
CHEMBL334491 115269 None 46 Human Functional pAC50 = 6.2 6.2 -1 3
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 293 2 0 1 4.9 CC(C)(C)N1CCC(c2ccccc2)(c2ccccc2)CC1 10.1038/s41467-023-40064-9
4976 206037 None 20 Human Functional pAC50 = 6.2 6.2 -64 15
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 263 4 1 1 4.3 CNCCCC1c2ccccc2C=Cc2ccccc21 10.1038/s41467-023-40064-9
CHEMBL668 206037 None 20 Human Functional pAC50 = 6.2 6.2 -64 15
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 263 4 1 1 4.3 CNCCCC1c2ccccc2C=Cc2ccccc21 10.1038/s41467-023-40064-9
3397 207946 None 70 Human Functional pAC50 = 5.2 5.2 1 7
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 276 3 1 3 3.2 CC(C)C(=O)Nc1ccc([N+](=O)[O-])c(C(F)(F)F)c1 10.1038/s41467-023-40064-9
CHEMBL806 207946 None 70 Human Functional pAC50 = 5.2 5.2 1 7
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 276 3 1 3 3.2 CC(C)C(=O)Nc1ccc([N+](=O)[O-])c(C(F)(F)F)c1 10.1038/s41467-023-40064-9
1385580 29284 None 49 Human Functional pAC50 = 5.2 5.2 -676 19
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 426 7 1 4 4.1 O=c1[nH]c2ccccc2n1CCCN1CCN(C(c2ccccc2)c2ccccc2)CC1 10.1038/s41467-023-40064-9
4615 29284 None 49 Human Functional pAC50 = 5.2 5.2 -676 19
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 426 7 1 4 4.1 O=c1[nH]c2ccccc2n1CCCN1CCN(C(c2ccccc2)c2ccccc2)CC1 10.1038/s41467-023-40064-9
4615.0 29284 None 49 Human Functional pAC50 = 5.2 5.2 -676 19
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 426 7 1 4 4.1 O=c1[nH]c2ccccc2n1CCCN1CCN(C(c2ccccc2)c2ccccc2)CC1 10.1038/s41467-023-40064-9
CHEMBL13828 29284 None 49 Human Functional pAC50 = 5.2 5.2 -676 19
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 426 7 1 4 4.1 O=c1[nH]c2ccccc2n1CCCN1CCN(C(c2ccccc2)c2ccccc2)CC1 10.1038/s41467-023-40064-9
DB12877 29284 None 49 Human Functional pAC50 = 5.2 5.2 -676 19
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 426 7 1 4 4.1 O=c1[nH]c2ccccc2n1CCCN1CCN(C(c2ccccc2)c2ccccc2)CC1 10.1038/s41467-023-40064-9
3042 1414 None 26 Human Functional pAC50 = 7.2 7.2 -5 17
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC 10.1038/s41467-023-40064-9
3042.0 1414 None 26 Human Functional pAC50 = 7.2 7.2 -5 17
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC 10.1038/s41467-023-40064-9
355 1414 None 26 Human Functional pAC50 = 7.2 7.2 -5 17
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC 10.1038/s41467-023-40064-9
868 1414 None 26 Human Functional pAC50 = 7.2 7.2 -5 17
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC 10.1038/s41467-023-40064-9
CHEMBL1123 1414 None 26 Human Functional pAC50 = 7.2 7.2 -5 17
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC 10.1038/s41467-023-40064-9
DB00804 1414 None 26 Human Functional pAC50 = 7.2 7.2 -5 17
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC 10.1038/s41467-023-40064-9
4942 5720 None 27 Human Functional pAC50 = 6.2 6.2 -1 11
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 367 7 0 4 4.0 CCCOC(C(=O)OC1CCN(C)CC1)(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
4942.0 5720 None 27 Human Functional pAC50 = 6.2 6.2 -1 11
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 367 7 0 4 4.0 CCCOC(C(=O)OC1CCN(C)CC1)(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL1078261 5720 None 27 Human Functional pAC50 = 6.2 6.2 -1 11
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 367 7 0 4 4.0 CCCOC(C(=O)OC1CCN(C)CC1)(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
DB12278 5720 None 27 Human Functional pAC50 = 6.2 6.2 -1 11
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 367 7 0 4 4.0 CCCOC(C(=O)OC1CCN(C)CC1)(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
154417 23189 None 39 Human Functional pAC50 = 8.2 8.2 -1 7
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 289 4 1 4 1.9 CN1[C@@H]2CC[C@H]1C[C@@H](OC(=O)[C@H](CO)c1ccccc1)C2 10.1038/s41467-023-40064-9
CHEMBL1331216 23189 None 39 Human Functional pAC50 = 8.2 8.2 -1 7
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 289 4 1 4 1.9 CN1[C@@H]2CC[C@H]1C[C@@H](OC(=O)[C@H](CO)c1ccccc1)C2 10.1038/s41467-023-40064-9
656603 194645 None 3 Human Functional pAC50 = 8.2 8.2 1 5
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 398 6 1 3 3.6 C[N@+]1(CCF)[C@@H]2CC[C@H]1C[C@@H](OC(=O)C(O)(c1ccccc1)c1ccccc1)C2 10.1038/s41467-023-40064-9
CHEMBL5292015 194645 None 3 Human Functional pAC50 = 8.2 8.2 1 5
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 398 6 1 3 3.6 C[N@+]1(CCF)[C@@H]2CC[C@H]1C[C@@H](OC(=O)C(O)(c1ccccc1)c1ccccc1)C2 10.1038/s41467-023-40064-9
3652 4097 None 50 Human Functional pAC50 = 8.2 8.2 -18 15
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1038/s41467-023-40064-9
57 4097 None 50 Human Functional pAC50 = 8.2 8.2 -18 15
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1038/s41467-023-40064-9
60809 4097 None 50 Human Functional pAC50 = 8.2 8.2 -18 15
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1038/s41467-023-40064-9
60809.0 4097 None 50 Human Functional pAC50 = 8.2 8.2 -18 15
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1038/s41467-023-40064-9
CHEMBL21536 4097 None 50 Human Functional pAC50 = 8.2 8.2 -18 15
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1038/s41467-023-40064-9
DB15357 4097 None 50 Human Functional pAC50 = 8.2 8.2 -18 15
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1038/s41467-023-40064-9
2600 3779 None 53 Human Functional pAC50 = 5.2 5.2 -13 32
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
2608 3779 None 53 Human Functional pAC50 = 5.2 5.2 -13 32
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
5405 3779 None 53 Human Functional pAC50 = 5.2 5.2 -13 32
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
CHEMBL17157 3779 None 53 Human Functional pAC50 = 5.2 5.2 -13 32
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
DB00342 3779 None 53 Human Functional pAC50 = 5.2 5.2 -13 32
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
180 401 None 38 Human Functional pAC50 = 6.2 6.2 -147 38
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
200 401 None 38 Human Functional pAC50 = 6.2 6.2 -147 38
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
2160 401 None 38 Human Functional pAC50 = 6.2 6.2 -147 38
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
2160.0 401 None 38 Human Functional pAC50 = 6.2 6.2 -147 38
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
CHEMBL629 401 None 38 Human Functional pAC50 = 6.2 6.2 -147 38
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
DB00321 401 None 38 Human Functional pAC50 = 6.2 6.2 -147 38
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
2993 114756 None 14 Human Functional pAC50 = 6.2 6.2 -12 13
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 456 11 2 2 6.2 Cc1cc(N)c2ccccc2[n+]1CCCCCCCCCC[n+]1c(C)cc(N)c2ccccc21 10.1038/s41467-023-40064-9
CHEMBL121663 114756 None 14 Human Functional pAC50 = 6.2 6.2 -12 13
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 456 11 2 2 6.2 Cc1cc(N)c2ccccc2[n+]1CCCCCCCCCC[n+]1c(C)cc(N)c2ccccc21 10.1038/s41467-023-40064-9
CHEMBL333826 114756 None 14 Human Functional pAC50 = 6.2 6.2 -12 13
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 456 11 2 2 6.2 Cc1cc(N)c2ccccc2[n+]1CCCCCCCCCC[n+]1c(C)cc(N)c2ccccc21 10.1038/s41467-023-40064-9
9270 14435 None 44 Human Functional pAC50 = 5.2 5.2 -2 3
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 384 2 0 4 4.4 C#C[C@]1(OC(C)=O)CC[C@H]2[C@@H]3CCC4=C[C@@H](OC(C)=O)CC[C@@H]4[C@H]3CC[C@@]21C 10.1038/s41467-023-40064-9
CHEMBL1200624 14435 None 44 Human Functional pAC50 = 5.2 5.2 -2 3
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 384 2 0 4 4.4 C#C[C@]1(OC(C)=O)CC[C@H]2[C@@H]3CCC4=C[C@@H](OC(C)=O)CC[C@@H]4[C@H]3CC[C@@]21C 10.1038/s41467-023-40064-9
3351 95055 None 40 Human Functional pAC50 = 5.2 5.2 1 6
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 388 5 0 5 2.8 O=C(COc1ccc(Cl)cc1)N1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1038/s41467-023-40064-9
CHEMBL254857 95055 None 40 Human Functional pAC50 = 5.2 5.2 1 6
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 388 5 0 5 2.8 O=C(COc1ccc(Cl)cc1)N1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1038/s41467-023-40064-9
5351322 94844 None 30 Human Functional pAC50 = 5.2 5.2 -4 9
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 398 4 4 8 1.8 C(=N/NC1=NCCN1)\c1c2ccccc2c(/C=N/NC2=NCCN2)c2ccccc12 10.1038/s41467-023-40064-9
CHEMBL25336 94844 None 30 Human Functional pAC50 = 5.2 5.2 -4 9
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 398 4 4 8 1.8 C(=N/NC1=NCCN1)\c1c2ccccc2c(/C=N/NC2=NCCN2)c2ccccc12 10.1038/s41467-023-40064-9
3294 2006 None 61 Human Functional pAC50 = 5.2 5.2 -6606 23
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 10.1038/s41467-023-40064-9
71360 2006 None 61 Human Functional pAC50 = 5.2 5.2 -6606 23
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 10.1038/s41467-023-40064-9
71360.0 2006 None 61 Human Functional pAC50 = 5.2 5.2 -6606 23
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 10.1038/s41467-023-40064-9
87 2006 None 61 Human Functional pAC50 = 5.2 5.2 -6606 23
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 10.1038/s41467-023-40064-9
CHEMBL14376 2006 None 61 Human Functional pAC50 = 5.2 5.2 -6606 23
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 10.1038/s41467-023-40064-9
DB04946 2006 None 61 Human Functional pAC50 = 5.2 5.2 -6606 23
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 10.1038/s41467-023-40064-9
2200 3131 None 31 Human Functional pAC50 = 7.2 7.2 -3 10
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1038/s41467-023-40064-9
328 3131 None 31 Human Functional pAC50 = 7.2 7.2 -3 10
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1038/s41467-023-40064-9
4848 3131 None 31 Human Functional pAC50 = 7.2 7.2 -3 10
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1038/s41467-023-40064-9
4848.0 3131 None 31 Human Functional pAC50 = 7.2 7.2 -3 10
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1038/s41467-023-40064-9
CHEMBL9967 3131 None 31 Human Functional pAC50 = 7.2 7.2 -3 10
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1038/s41467-023-40064-9
DB00670 3131 None 31 Human Functional pAC50 = 7.2 7.2 -3 10
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1038/s41467-023-40064-9
1210 918 None 42 Human Functional pAC50 = 5.2 5.2 -457 22
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
1213 918 None 42 Human Functional pAC50 = 5.2 5.2 -457 22
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
2725 918 None 42 Human Functional pAC50 = 5.2 5.2 -457 22
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
33036 918 None 42 Human Functional pAC50 = 5.2 5.2 -457 22
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
33036.0 918 None 42 Human Functional pAC50 = 5.2 5.2 -457 22
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
4411 918 None 42 Human Functional pAC50 = 5.2 5.2 -457 22
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
616 918 None 42 Human Functional pAC50 = 5.2 5.2 -457 22
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
6976 918 None 42 Human Functional pAC50 = 5.2 5.2 -457 22
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
716121 918 None 42 Human Functional pAC50 = 5.2 5.2 -457 22
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
CHEMBL1201353 918 None 42 Human Functional pAC50 = 5.2 5.2 -457 22
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
CHEMBL1554789 918 None 42 Human Functional pAC50 = 5.2 5.2 -457 22
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
CHEMBL505 918 None 42 Human Functional pAC50 = 5.2 5.2 -457 22
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
DB01114 918 None 42 Human Functional pAC50 = 5.2 5.2 -457 22
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
DB13679 918 None 42 Human Functional pAC50 = 5.2 5.2 -457 22
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
1816 2540 None 64 Human Functional pAC50 = 5.2 5.2 -999 12
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 10.1038/s41467-023-40064-9
4205 2540 None 64 Human Functional pAC50 = 5.2 5.2 -999 12
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 10.1038/s41467-023-40064-9
4205.0 2540 None 64 Human Functional pAC50 = 5.2 5.2 -999 12
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 10.1038/s41467-023-40064-9
7241 2540 None 64 Human Functional pAC50 = 5.2 5.2 -999 12
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 10.1038/s41467-023-40064-9
CHEMBL654 2540 None 64 Human Functional pAC50 = 5.2 5.2 -999 12
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 10.1038/s41467-023-40064-9
DB00370 2540 None 64 Human Functional pAC50 = 5.2 5.2 -999 12
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 10.1038/s41467-023-40064-9
441383 20340 None 41 Human Functional pAC50 = 5.2 5.2 -64 19
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 531 8 0 8 4.5 CC(C)N1CCN(c2ccc(OC[C@H]3CO[C@](Cn4cncn4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 10.1038/s41467-023-40064-9
CHEMBL1306 20340 None 41 Human Functional pAC50 = 5.2 5.2 -64 19
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 531 8 0 8 4.5 CC(C)N1CCN(c2ccc(OC[C@H]3CO[C@](Cn4cncn4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 10.1038/s41467-023-40064-9
4846 27995 None 38 Human Functional pAC50 = 5.2 5.2 -4 10
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 308 1 2 6 2.2 O=C(O)c1cc(O)c2c3nc4ccccc4oc-3cc(=O)c2n1 10.1038/s41467-023-40064-9
CHEMBL1372341 27995 None 38 Human Functional pAC50 = 5.2 5.2 -4 10
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 308 1 2 6 2.2 O=C(O)c1cc(O)c2c3nc4ccccc4oc-3cc(=O)c2n1 10.1038/s41467-023-40064-9
5284550 41735 None 12 Human Functional pAC50 = 6.2 6.2 -35 16
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 295 3 0 2 4.7 CN(C)CC/C=C1\c2ccccc2CSc2ccccc21 10.1038/s41467-023-40064-9
5284550.0 41735 None 12 Human Functional pAC50 = 6.2 6.2 -35 16
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 295 3 0 2 4.7 CN(C)CC/C=C1\c2ccccc2CSc2ccccc21 10.1038/s41467-023-40064-9
CHEMBL108947 41735 None 12 Human Functional pAC50 = 6.2 6.2 -35 16
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 295 3 0 2 4.7 CN(C)CC/C=C1\c2ccccc2CSc2ccccc21 10.1038/s41467-023-40064-9
CHEMBL1492500 41735 None 12 Human Functional pAC50 = 6.2 6.2 -35 16
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 295 3 0 2 4.7 CN(C)CC/C=C1\c2ccccc2CSc2ccccc21 10.1038/s41467-023-40064-9
DB09167 41735 None 12 Human Functional pAC50 = 6.2 6.2 -35 16
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 295 3 0 2 4.7 CN(C)CC/C=C1\c2ccccc2CSc2ccccc21 10.1038/s41467-023-40064-9
6917906 67795 None 17 Human Functional pAC50 = 5.2 5.2 -3 5
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 887 35 10 12 1.7 CCCCCCCCCCCCCCCCCC(=O)NCCCC[C@H](NC(=O)CC[C@@H](NC(=O)[C@H](C)NC(=O)[C@@H](C)O[C@H]1[C@H](O)[C@@H](CO)OC(O)[C@@H]1NC(C)=O)C(N)=O)C(=O)O 10.1038/s41467-023-40064-9
CHEMBL1908331 67795 None 17 Human Functional pAC50 = 5.2 5.2 -3 5
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 887 35 10 12 1.7 CCCCCCCCCCCCCCCCCC(=O)NCCCC[C@H](NC(=O)CC[C@@H](NC(=O)[C@H](C)NC(=O)[C@@H](C)O[C@H]1[C@H](O)[C@@H](CO)OC(O)[C@@H]1NC(C)=O)C(N)=O)C(=O)O 10.1038/s41467-023-40064-9
2286 3183 None 36 Human Functional pAC50 = 6.2 6.2 -10 28
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
4927 3183 None 36 Human Functional pAC50 = 6.2 6.2 -10 28
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
4927.0 3183 None 36 Human Functional pAC50 = 6.2 6.2 -10 28
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
7282 3183 None 36 Human Functional pAC50 = 6.2 6.2 -10 28
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
CHEMBL643 3183 None 36 Human Functional pAC50 = 6.2 6.2 -10 28
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
DB01069 3183 None 36 Human Functional pAC50 = 6.2 6.2 -10 28
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
72015 117164 None 27 Human Functional pAC50 = 4.2 4.2 - 1
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 339 4 3 5 0.7 CC(=N)N1CC[C@H](SC2=C(C(=O)O)N3C(=O)[C@H]([C@@H](C)O)[C@H]3C2)C1 10.1038/s41467-023-40064-9
CHEMBL339323 117164 None 27 Human Functional pAC50 = 4.2 4.2 - 1
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 339 4 3 5 0.7 CC(=N)N1CC[C@H](SC2=C(C(=O)O)N3C(=O)[C@H]([C@@H](C)O)[C@H]3C2)C1 10.1038/s41467-023-40064-9
2905 14504 None 36 Human Functional pAC50 = 7.2 7.2 -1 3
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 291 6 1 4 2.2 CN(C)CCOC(=O)C(c1ccccc1)C1(O)CCCC1 10.1038/s41467-023-40064-9
2905.0 14504 None 36 Human Functional pAC50 = 7.2 7.2 -1 3
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 291 6 1 4 2.2 CN(C)CCOC(=O)C(c1ccccc1)C1(O)CCCC1 10.1038/s41467-023-40064-9
CHEMBL1201338 14504 None 36 Human Functional pAC50 = 7.2 7.2 -1 3
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 291 6 1 4 2.2 CN(C)CCOC(=O)C(c1ccccc1)C1(O)CCCC1 10.1038/s41467-023-40064-9
DB00979 14504 None 36 Human Functional pAC50 = 7.2 7.2 -1 3
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 291 6 1 4 2.2 CN(C)CCOC(=O)C(c1ccccc1)C1(O)CCCC1 10.1038/s41467-023-40064-9
2710 84342 None 29 Human Functional pAC50 = 6.2 6.2 -1 10
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 300 3 0 2 3.7 CN1CCN(C(c2ccccc2)c2ccc(Cl)cc2)CC1 10.1038/s41467-023-40064-9
2710.0 84342 None 29 Human Functional pAC50 = 6.2 6.2 -1 10
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 300 3 0 2 3.7 CN1CCN(C(c2ccccc2)c2ccc(Cl)cc2)CC1 10.1038/s41467-023-40064-9
CHEMBL1889091 84342 None 29 Human Functional pAC50 = 6.2 6.2 -1 10
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 300 3 0 2 3.7 CN1CCN(C(c2ccccc2)c2ccc(Cl)cc2)CC1 10.1038/s41467-023-40064-9
CHEMBL22150 84342 None 29 Human Functional pAC50 = 6.2 6.2 -1 10
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 300 3 0 2 3.7 CN1CCN(C(c2ccccc2)c2ccc(Cl)cc2)CC1 10.1038/s41467-023-40064-9
DB08936 84342 None 29 Human Functional pAC50 = 6.2 6.2 -1 10
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 300 3 0 2 3.7 CN1CCN(C(c2ccccc2)c2ccc(Cl)cc2)CC1 10.1038/s41467-023-40064-9
154417 23189 None 39 Human Functional pAC50 = 8.1 8.1 -1 7
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 289 4 1 4 1.9 CN1[C@@H]2CC[C@H]1C[C@@H](OC(=O)[C@H](CO)c1ccccc1)C2 10.1038/s41467-023-40064-9
CHEMBL1331216 23189 None 39 Human Functional pAC50 = 8.1 8.1 -1 7
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 289 4 1 4 1.9 CN1[C@@H]2CC[C@H]1C[C@@H](OC(=O)[C@H](CO)c1ccccc1)C2 10.1038/s41467-023-40064-9
93154 5438 None 24 Human Functional pAC50 = 8.1 8.1 4 8
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 304 1 0 2 4.0 c1ccc2c(c1)CCc1ccccc1N2C1CN2CCC1CC2 10.1038/s41467-023-40064-9
CHEMBL107360 5438 None 24 Human Functional pAC50 = 8.1 8.1 4 8
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 304 1 0 2 4.0 c1ccc2c(c1)CCc1ccccc1N2C1CN2CCC1CC2 10.1038/s41467-023-40064-9
3166 169523 None 18 Human Functional pAC50 = 8.1 8.1 4 8
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 317 8 0 3 4.2 CCN(CC)CCOC(=O)C(c1ccccc1)C1CCCCC1 10.1038/s41467-023-40064-9
CHEMBL442444 169523 None 18 Human Functional pAC50 = 8.1 8.1 4 8
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 317 8 0 3 4.2 CCN(CC)CCOC(=O)C(c1ccccc1)C1CCCCC1 10.1038/s41467-023-40064-9
1726 2497 None 8 Human Functional pAC50 = 8.1 8.1 5 8
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 10.1038/s41467-023-40064-9
1993 2497 None 8 Human Functional pAC50 = 8.1 8.1 5 8
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 10.1038/s41467-023-40064-9
1993.0 2497 None 8 Human Functional pAC50 = 8.1 8.1 5 8
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 10.1038/s41467-023-40064-9
7438 2497 None 8 Human Functional pAC50 = 8.1 8.1 5 8
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 10.1038/s41467-023-40064-9
CHEMBL978 2497 None 8 Human Functional pAC50 = 8.1 8.1 5 8
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 10.1038/s41467-023-40064-9
DB06709 2497 None 8 Human Functional pAC50 = 8.1 8.1 5 8
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 10.1038/s41467-023-40064-9
2398 954 None 43 Human Functional pAC50 = 6.2 6.2 -151 36
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
2801 954 None 43 Human Functional pAC50 = 6.2 6.2 -151 36
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
2801.0 954 None 43 Human Functional pAC50 = 6.2 6.2 -151 36
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
701 954 None 43 Human Functional pAC50 = 6.2 6.2 -151 36
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
CHEMBL415 954 None 43 Human Functional pAC50 = 6.2 6.2 -151 36
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
DB01242 954 None 43 Human Functional pAC50 = 6.2 6.2 -151 36
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
319 1324 None 32 Human Functional pAC50 = 6.2 6.2 -691 18
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1038/s41467-023-40064-9
321 1324 None 32 Human Functional pAC50 = 6.2 6.2 -691 18
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1038/s41467-023-40064-9
444031 1324 None 32 Human Functional pAC50 = 6.2 6.2 -691 18
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1038/s41467-023-40064-9
444031.0 1324 None 32 Human Functional pAC50 = 6.2 6.2 -691 18
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1038/s41467-023-40064-9
784 1324 None 32 Human Functional pAC50 = 6.2 6.2 -691 18
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1038/s41467-023-40064-9
CHEMBL1346 1324 None 32 Human Functional pAC50 = 6.2 6.2 -691 18
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1038/s41467-023-40064-9
DB00496 1324 None 32 Human Functional pAC50 = 6.2 6.2 -691 18
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1038/s41467-023-40064-9
2136 3095 None 24 Human Functional pAC50 = 5.2 5.2 -138 21
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 303 8 0 2 4.2 ClCCN(C(COc1ccccc1)C)Cc1ccccc1 10.1038/s41467-023-40064-9
4768 3095 None 24 Human Functional pAC50 = 5.2 5.2 -138 21
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 303 8 0 2 4.2 ClCCN(C(COc1ccccc1)C)Cc1ccccc1 10.1038/s41467-023-40064-9
4768.0 3095 None 24 Human Functional pAC50 = 5.2 5.2 -138 21
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 303 8 0 2 4.2 ClCCN(C(COc1ccccc1)C)Cc1ccccc1 10.1038/s41467-023-40064-9
7268 3095 None 24 Human Functional pAC50 = 5.2 5.2 -138 21
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 303 8 0 2 4.2 ClCCN(C(COc1ccccc1)C)Cc1ccccc1 10.1038/s41467-023-40064-9
CHEMBL753 3095 None 24 Human Functional pAC50 = 5.2 5.2 -138 21
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 303 8 0 2 4.2 ClCCN(C(COc1ccccc1)C)Cc1ccccc1 10.1038/s41467-023-40064-9
DB00925 3095 None 24 Human Functional pAC50 = 5.2 5.2 -138 21
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 303 8 0 2 4.2 ClCCN(C(COc1ccccc1)C)Cc1ccccc1 10.1038/s41467-023-40064-9
7547 5506 None 61 Human Functional pAC50 = 6.2 6.2 2 4
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 314 2 2 1 5.3 O=C(Nc1ccc(Cl)cc1)Nc1ccc(Cl)c(Cl)c1 10.1038/s41467-023-40064-9
CHEMBL1076347 5506 None 61 Human Functional pAC50 = 6.2 6.2 2 4
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 314 2 2 1 5.3 O=C(Nc1ccc(Cl)cc1)Nc1ccc(Cl)c(Cl)c1 10.1038/s41467-023-40064-9
135398735 137055 None 20 Human Functional pAC50 = 5.2 5.2 -3 28
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 822 4 6 15 4.3 CO[C@H]1/C=C/O[C@@]2(C)Oc3c(C)c(O)c4c(O)c(c(/C=N/N5CCN(C)CC5)c(O)c4c3C2=O)NC(=O)/C(C)=C\C=C\[C@H](C)[C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@H](OC(C)=O)[C@@H]1C 10.1038/s41467-023-40064-9
136262914 137055 None 20 Human Functional pAC50 = 5.2 5.2 -3 28
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 822 4 6 15 4.3 CO[C@H]1/C=C/O[C@@]2(C)Oc3c(C)c(O)c4c(O)c(c(/C=N/N5CCN(C)CC5)c(O)c4c3C2=O)NC(=O)/C(C)=C\C=C\[C@H](C)[C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@H](OC(C)=O)[C@@H]1C 10.1038/s41467-023-40064-9
CHEMBL374478 137055 None 20 Human Functional pAC50 = 5.2 5.2 -3 28
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 822 4 6 15 4.3 CO[C@H]1/C=C/O[C@@]2(C)Oc3c(C)c(O)c4c(O)c(c(/C=N/N5CCN(C)CC5)c(O)c4c3C2=O)NC(=O)/C(C)=C\C=C\[C@H](C)[C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@H](OC(C)=O)[C@@H]1C 10.1038/s41467-023-40064-9
9818306 14424 None 13 Human Functional pAC50 = 5.1 5.1 1 5
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 314 1 1 3 3.8 CC(=O)Oc1ccc2c(c1)CC[C@@H]1[C@@H]2CC[C@]2(C)[C@@H](O)CC[C@@H]12 10.1038/s41467-023-40064-9
CHEMBL1200430 14424 None 13 Human Functional pAC50 = 5.1 5.1 1 5
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 314 1 1 3 3.8 CC(=O)Oc1ccc2c(c1)CC[C@@H]1[C@@H]2CC[C@]2(C)[C@@H](O)CC[C@@H]12 10.1038/s41467-023-40064-9
6719 32676 None 23 Human Functional pAC50 = 5.1 5.1 -10 4
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 340 4 0 3 4.1 O=C1c2ccccc2C(=O)C1C(=O)C(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL1413199 32676 None 23 Human Functional pAC50 = 5.1 5.1 -10 4
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 340 4 0 3 4.1 O=C1c2ccccc2C(=O)C1C(=O)C(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
5330286 67592 None 57 Human Functional pAC50 = 5.1 5.1 -1 8
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 447 5 2 9 3.0 CC(=O)c1c(C)c2cnc(Nc3ccc(N4CCNCC4)cn3)nc2n(C2CCCC2)c1=O 10.1038/s41467-023-40064-9
CHEMBL189963 67592 None 57 Human Functional pAC50 = 5.1 5.1 -1 8
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 447 5 2 9 3.0 CC(=O)c1c(C)c2cnc(Nc3ccc(N4CCNCC4)cn3)nc2n(C2CCCC2)c1=O 10.1038/s41467-023-40064-9
135398745 2914 None 65 Human Functional pAC50 = 7.1 7.1 -5 33
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
135398745.0 2914 None 65 Human Functional pAC50 = 7.1 7.1 -5 33
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
47 2914 None 65 Human Functional pAC50 = 7.1 7.1 -5 33
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
CHEMBL715 2914 None 65 Human Functional pAC50 = 7.1 7.1 -5 33
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
DB00334 2914 None 65 Human Functional pAC50 = 7.1 7.1 -5 33
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
3601 14509 None 4 Human Functional pAC50 = 5.1 5.1 -109 9
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 502 9 0 0 8.2 C[N+](C)(CCCCCC[N+](C)(C)C1c2ccccc2-c2ccccc21)C1c2ccccc2-c2ccccc21 10.1038/s41467-023-40064-9
CHEMBL1201349 14509 None 4 Human Functional pAC50 = 5.1 5.1 -109 9
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 502 9 0 0 8.2 C[N+](C)(CCCCCC[N+](C)(C)C1c2ccccc2-c2ccccc21)C1c2ccccc2-c2ccccc21 10.1038/s41467-023-40064-9
3474 38112 None 43 Human Functional pAC50 = 5.1 5.1 -2 8
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 372 6 3 6 3.1 O=C(OCC(O)CO)c1ccccc1Nc1ccnc2cc(Cl)ccc12 10.1038/s41467-023-40064-9
CHEMBL146095 38112 None 43 Human Functional pAC50 = 5.1 5.1 -2 8
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 372 6 3 6 3.1 O=C(OCC(O)CO)c1ccccc1Nc1ccnc2cc(Cl)ccc12 10.1038/s41467-023-40064-9
5353853 17993 None 30 Human Functional pAC50 = 5.1 5.1 -34 20
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 10.1038/s41467-023-40064-9
9556529 17993 None 30 Human Functional pAC50 = 5.1 5.1 -34 20
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 10.1038/s41467-023-40064-9
CHEMBL1262 17993 None 30 Human Functional pAC50 = 5.1 5.1 -34 20
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 10.1038/s41467-023-40064-9
11154555 800 None 50 Human Functional pAC50 = 5.1 5.1 -3019 10
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
11154555.0 800 None 50 Human Functional pAC50 = 5.1 5.1 -3019 10
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
5037 800 None 50 Human Functional pAC50 = 5.1 5.1 -3019 10
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
7671 800 None 50 Human Functional pAC50 = 5.1 5.1 -3019 10
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
CHEMBL2028019 800 None 50 Human Functional pAC50 = 5.1 5.1 -3019 10
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
CHEMBL3085826 800 None 50 Human Functional pAC50 = 5.1 5.1 -3019 10
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
DB06016 800 None 50 Human Functional pAC50 = 5.1 5.1 -3019 10
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
21855 84280 None 37 Human Functional pAC50 = 5.1 5.1 -97 9
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 292 5 0 2 4.1 CC(C1=C(CCN(C)C)Cc2ccccc21)c1ccccn1 10.1038/s41467-023-40064-9
21855.0 84280 None 37 Human Functional pAC50 = 5.1 5.1 -97 9
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 292 5 0 2 4.1 CC(C1=C(CCN(C)C)Cc2ccccc21)c1ccccn1 10.1038/s41467-023-40064-9
CHEMBL22108 84280 None 37 Human Functional pAC50 = 5.1 5.1 -97 9
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 292 5 0 2 4.1 CC(C1=C(CCN(C)C)Cc2ccccc21)c1ccccn1 10.1038/s41467-023-40064-9
DB08801 84280 None 37 Human Functional pAC50 = 5.1 5.1 -97 9
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 292 5 0 2 4.1 CC(C1=C(CCN(C)C)Cc2ccccc21)c1ccccn1 10.1038/s41467-023-40064-9
27901 78236 None 18 Human Functional pAC50 = 6.1 6.1 -1 8
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 286 4 0 3 3.8 CN1CCC(N(Cc2cccs2)c2ccccc2)CC1 10.1038/s41467-023-40064-9
CHEMBL2105458 78236 None 18 Human Functional pAC50 = 6.1 6.1 -1 8
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 286 4 0 3 3.8 CN1CCC(N(Cc2cccs2)c2ccccc2)CC1 10.1038/s41467-023-40064-9
208898 66220 None 50 Human Functional pAC50 = 5.1 5.1 -12 11
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 556 18 1 6 7.0 CCCCc1oc2ccc(NS(C)(=O)=O)cc2c1C(=O)c1ccc(OCCCN(CCCC)CCCC)cc1 10.1038/s41467-023-40064-9
208898.0 66220 None 50 Human Functional pAC50 = 5.1 5.1 -12 11
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 556 18 1 6 7.0 CCCCc1oc2ccc(NS(C)(=O)=O)cc2c1C(=O)c1ccc(OCCCN(CCCC)CCCC)cc1 10.1038/s41467-023-40064-9
CHEMBL184412 66220 None 50 Human Functional pAC50 = 5.1 5.1 -12 11
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 556 18 1 6 7.0 CCCCc1oc2ccc(NS(C)(=O)=O)cc2c1C(=O)c1ccc(OCCCN(CCCC)CCCC)cc1 10.1038/s41467-023-40064-9
DB04855 66220 None 50 Human Functional pAC50 = 5.1 5.1 -12 11
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 556 18 1 6 7.0 CCCCc1oc2ccc(NS(C)(=O)=O)cc2c1C(=O)c1ccc(OCCCN(CCCC)CCCC)cc1 10.1038/s41467-023-40064-9
1164 1630 None 10 Human Functional pAC50 = 5.1 5.1 -1096 13
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 336 6 0 2 4.1 CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1 10.1038/s41467-023-40064-9
1626 1630 None 10 Human Functional pAC50 = 5.1 5.1 -1096 13
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 336 6 0 2 4.1 CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1 10.1038/s41467-023-40064-9
3345 1630 None 10 Human Functional pAC50 = 5.1 5.1 -1096 13
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 336 6 0 2 4.1 CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1 10.1038/s41467-023-40064-9
3345.0 1630 None 10 Human Functional pAC50 = 5.1 5.1 -1096 13
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 336 6 0 2 4.1 CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1 10.1038/s41467-023-40064-9
CHEMBL596 1630 None 10 Human Functional pAC50 = 5.1 5.1 -1096 13
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 336 6 0 2 4.1 CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1 10.1038/s41467-023-40064-9
DB00813 1630 None 10 Human Functional pAC50 = 5.1 5.1 -1096 13
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 336 6 0 2 4.1 CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1 10.1038/s41467-023-40064-9
62867 3129 None 27 Human Functional pAC50 = 5.1 5.1 -2570 9
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 475 8 1 6 4.0 OCCC1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
7557 3129 None 27 Human Functional pAC50 = 5.1 5.1 -2570 9
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 475 8 1 6 4.0 OCCC1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
CHEMBL398880 3129 None 27 Human Functional pAC50 = 5.1 5.1 -2570 9
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 475 8 1 6 4.0 OCCC1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
DB01621 3129 None 27 Human Functional pAC50 = 5.1 5.1 -2570 9
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 475 8 1 6 4.0 OCCC1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
19675 51685 None 37 Human Functional pAC50 = 5.1 5.1 -616 15
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 410 7 1 5 5.0 CC(=O)c1ccc2c(c1)N(CCCN1CCC(CCO)CC1)c1ccccc1S2 10.1038/s41467-023-40064-9
CHEMBL1584 51685 None 37 Human Functional pAC50 = 5.1 5.1 -616 15
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 410 7 1 5 5.0 CC(=O)c1ccc2c(c1)N(CCCN1CCC(CCO)CC1)c1ccccc1S2 10.1038/s41467-023-40064-9
2179 167616 None 49 Human Functional pAC50 = 5.1 5.1 -6 15
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 393 5 2 5 4.5 COc1cc(NS(C)(=O)=O)ccc1Nc1c2ccccc2nc2ccccc12 10.1038/s41467-023-40064-9
CHEMBL1256655 167616 None 49 Human Functional pAC50 = 5.1 5.1 -6 15
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 393 5 2 5 4.5 COc1cc(NS(C)(=O)=O)ccc1Nc1c2ccccc2nc2ccccc12 10.1038/s41467-023-40064-9
CHEMBL43 167616 None 49 Human Functional pAC50 = 5.1 5.1 -6 15
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 393 5 2 5 4.5 COc1cc(NS(C)(=O)=O)ccc1Nc1c2ccccc2nc2ccccc12 10.1038/s41467-023-40064-9
1613 2348 None 42 Human Functional pAC50 = 6.1 6.1 -35 33
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
205 2348 None 42 Human Functional pAC50 = 6.1 6.1 -35 33
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
3964 2348 None 42 Human Functional pAC50 = 6.1 6.1 -35 33
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
3964.0 2348 None 42 Human Functional pAC50 = 6.1 6.1 -35 33
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
CHEMBL831 2348 None 42 Human Functional pAC50 = 6.1 6.1 -35 33
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
DB00408 2348 None 42 Human Functional pAC50 = 6.1 6.1 -35 33
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
20299 14511 None 12 Human Functional pAC50 = 8.1 8.1 1 2
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 318 8 1 1 4.7 CC[N+](CC)(CC)CCC(O)(c1ccccc1)C1CCCCC1 10.1038/s41467-023-40064-9
20299.0 14511 None 12 Human Functional pAC50 = 8.1 8.1 1 2
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 318 8 1 1 4.7 CC[N+](CC)(CC)CCC(O)(c1ccccc1)C1CCCCC1 10.1038/s41467-023-40064-9
CHEMBL1201354 14511 None 12 Human Functional pAC50 = 8.1 8.1 1 2
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 318 8 1 1 4.7 CC[N+](CC)(CC)CCC(O)(c1ccccc1)C1CCCCC1 10.1038/s41467-023-40064-9
DB00505 14511 None 12 Human Functional pAC50 = 8.1 8.1 1 2
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 318 8 1 1 4.7 CC[N+](CC)(CC)CCC(O)(c1ccccc1)C1CCCCC1 10.1038/s41467-023-40064-9
152946 108581 None 53 Human Functional pAC50 = 5.1 5.1 -25 2
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 401 4 2 6 2.4 COc1c(N2C[C@@H]3CCCN[C@@H]3C2)c(F)cc2c(=O)c(C(=O)O)cn(C3CC3)c12 10.1038/s41467-023-40064-9
40467042 108581 None 53 Human Functional pAC50 = 5.1 5.1 -25 2
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 401 4 2 6 2.4 COc1c(N2C[C@@H]3CCCN[C@@H]3C2)c(F)cc2c(=O)c(C(=O)O)cn(C3CC3)c12 10.1038/s41467-023-40064-9
CHEMBL32 108581 None 53 Human Functional pAC50 = 5.1 5.1 -25 2
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 401 4 2 6 2.4 COc1c(N2C[C@@H]3CCCN[C@@H]3C2)c(F)cc2c(=O)c(C(=O)O)cn(C3CC3)c12 10.1038/s41467-023-40064-9
3152 188518 None 61 Human Functional pAC50 = 5.1 5.1 -15 10
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 379 6 0 4 4.4 COc1cc2c(cc1OC)C(=O)C(CC1CCN(Cc3ccccc3)CC1)C2 10.1038/s41467-023-40064-9
CHEMBL502 188518 None 61 Human Functional pAC50 = 5.1 5.1 -15 10
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 379 6 0 4 4.4 COc1cc2c(cc1OC)C(=O)C(CC1CCN(Cc3ccccc3)CC1)C2 10.1038/s41467-023-40064-9
2200 3131 None 31 Human Functional pAC50 = 7.1 7.1 -3 10
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1038/s41467-023-40064-9
328 3131 None 31 Human Functional pAC50 = 7.1 7.1 -3 10
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1038/s41467-023-40064-9
4848 3131 None 31 Human Functional pAC50 = 7.1 7.1 -3 10
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1038/s41467-023-40064-9
4848.0 3131 None 31 Human Functional pAC50 = 7.1 7.1 -3 10
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1038/s41467-023-40064-9
CHEMBL9967 3131 None 31 Human Functional pAC50 = 7.1 7.1 -3 10
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1038/s41467-023-40064-9
DB00670 3131 None 31 Human Functional pAC50 = 7.1 7.1 -3 10
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 351 2 1 5 1.6 CN1CCN(CC1)CC(=O)n1c2ccccc2c(=O)[nH]c2c1nccc2 10.1038/s41467-023-40064-9
4904 155611 None 29 Human Functional pAC50 = 7.1 7.1 1 4
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 295 5 1 2 3.8 OC(CCN1CCCCC1)(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL404215 155611 None 29 Human Functional pAC50 = 7.1 7.1 1 4
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 295 5 1 2 3.8 OC(CCN1CCCCC1)(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
196122 112651 None 39 Human Functional pAC50 = 5.1 5.1 1 4
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 478 13 1 6 4.5 CCOC1O[C@H]([C@@H](COCc2ccccc2)OCc2ccccc2)[C@H](OCc2ccccc2)[C@H]1O 10.1038/s41467-023-40064-9
CHEMBL3301681 112651 None 39 Human Functional pAC50 = 5.1 5.1 1 4
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 478 13 1 6 4.5 CCOC1O[C@H]([C@@H](COCc2ccccc2)OCc2ccccc2)[C@H](OCc2ccccc2)[C@H]1O 10.1038/s41467-023-40064-9
5205 78216 None 42 Human Functional pAC50 = 5.1 5.1 -93 8
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 261 0 0 1 3.8 CN1CCC2=C(C1)c1ccccc1Cc1ccccc12 10.1038/s41467-023-40064-9
CHEMBL2104895 78216 None 42 Human Functional pAC50 = 5.1 5.1 -93 8
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 261 0 0 1 3.8 CN1CCC2=C(C1)c1ccccc1Cc1ccccc12 10.1038/s41467-023-40064-9
1765 3817 None 60 Human Functional pAC50 = 5.1 5.1 -89 10
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 522 10 4 11 2.0 CCCSc1nc(N[C@@H]2C[C@H]2c2ccc(c(c2)F)F)c2c(n1)n(nn2)[C@@H]1C[C@@H]([C@H]([C@H]1O)O)OCCO 10.1038/s41467-023-40064-9
4184 3817 None 60 Human Functional pAC50 = 5.1 5.1 -89 10
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 522 10 4 11 2.0 CCCSc1nc(N[C@@H]2C[C@H]2c2ccc(c(c2)F)F)c2c(n1)n(nn2)[C@@H]1C[C@@H]([C@H]([C@H]1O)O)OCCO 10.1038/s41467-023-40064-9
9871419 3817 None 60 Human Functional pAC50 = 5.1 5.1 -89 10
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 522 10 4 11 2.0 CCCSc1nc(N[C@@H]2C[C@H]2c2ccc(c(c2)F)F)c2c(n1)n(nn2)[C@@H]1C[C@@H]([C@H]([C@H]1O)O)OCCO 10.1038/s41467-023-40064-9
9871419.0 3817 None 60 Human Functional pAC50 = 5.1 5.1 -89 10
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 522 10 4 11 2.0 CCCSc1nc(N[C@@H]2C[C@H]2c2ccc(c(c2)F)F)c2c(n1)n(nn2)[C@@H]1C[C@@H]([C@H]([C@H]1O)O)OCCO 10.1038/s41467-023-40064-9
CHEMBL398435 3817 None 60 Human Functional pAC50 = 5.1 5.1 -89 10
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 522 10 4 11 2.0 CCCSc1nc(N[C@@H]2C[C@H]2c2ccc(c(c2)F)F)c2c(n1)n(nn2)[C@@H]1C[C@@H]([C@H]([C@H]1O)O)OCCO 10.1038/s41467-023-40064-9
DB08816 3817 None 60 Human Functional pAC50 = 5.1 5.1 -89 10
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 522 10 4 11 2.0 CCCSc1nc(N[C@@H]2C[C@H]2c2ccc(c(c2)F)F)c2c(n1)n(nn2)[C@@H]1C[C@@H]([C@H]([C@H]1O)O)OCCO 10.1038/s41467-023-40064-9
1570 57315 None 64 Human Functional pAC50 = 6.1 6.1 -2 3
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 127 0 1 3 1.5 On1ccccc1=S 10.1038/s41467-023-40064-9
CHEMBL1650619 57315 None 64 Human Functional pAC50 = 6.1 6.1 -2 3
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 127 0 1 3 1.5 On1ccccc1=S 10.1038/s41467-023-40064-9
3121 7887 None 64 Human Functional pAC50 = 6.1 6.1 -42 10
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 144 5 1 1 2.3 CCCC(CCC)C(=O)O 10.1038/s41467-023-40064-9
CHEMBL109 7887 None 64 Human Functional pAC50 = 6.1 6.1 -42 10
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 144 5 1 1 2.3 CCCC(CCC)C(=O)O 10.1038/s41467-023-40064-9
CHEMBL433 7887 None 64 Human Functional pAC50 = 6.1 6.1 -42 10
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 144 5 1 1 2.3 CCCC(CCC)C(=O)O 10.1038/s41467-023-40064-9
19910 37419 None 62 Human Functional pAC50 = 5.1 5.1 -1 10
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 190 1 1 4 1.8 O=[N+]([O-])c1ccc(O)c2ncccc12 10.1038/s41467-023-40064-9
CHEMBL1454910 37419 None 62 Human Functional pAC50 = 5.1 5.1 -1 10
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 190 1 1 4 1.8 O=[N+]([O-])c1ccc(O)c2ncccc12 10.1038/s41467-023-40064-9
2162 41527 None 58 Human Functional pAC50 = 5.1 5.1 -7 22
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 408 8 2 7 2.3 CCOC(=O)C1=C(COCCN)NC(C)=C(C(=O)OC)C1c1ccccc1Cl 10.1038/s41467-023-40064-9
CHEMBL1491 41527 None 58 Human Functional pAC50 = 5.1 5.1 -7 22
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 408 8 2 7 2.3 CCOC(=O)C1=C(COCCN)NC(C)=C(C(=O)OC)C1c1ccccc1Cl 10.1038/s41467-023-40064-9
127151 35339 None 12 Human Functional pAC50 = 5.1 5.1 1 7
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 313 6 1 4 3.2 CCOc1ccccc1OC(c1ccccc1)C1CNCCO1 10.1038/s41467-023-40064-9
3022645 35339 None 12 Human Functional pAC50 = 5.1 5.1 1 7
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 313 6 1 4 3.2 CCOc1ccccc1OC(c1ccccc1)C1CNCCO1 10.1038/s41467-023-40064-9
CHEMBL14370 35339 None 12 Human Functional pAC50 = 5.1 5.1 1 7
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 313 6 1 4 3.2 CCOc1ccccc1OC(c1ccccc1)C1CNCCO1 10.1038/s41467-023-40064-9
5039 63203 None 12 Human Functional pAC50 = 5.1 5.1 -28 9
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 314 10 2 7 1.5 CNC(=C[N+](=O)[O-])NCCSCc1ccc(CN(C)C)o1 10.1038/s41467-023-40064-9
5039.0 63203 None 12 Human Functional pAC50 = 5.1 5.1 -28 9
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 314 10 2 7 1.5 CNC(=C[N+](=O)[O-])NCCSCc1ccc(CN(C)C)o1 10.1038/s41467-023-40064-9
CHEMBL1790041 63203 None 12 Human Functional pAC50 = 5.1 5.1 -28 9
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 314 10 2 7 1.5 CNC(=C[N+](=O)[O-])NCCSCc1ccc(CN(C)C)o1 10.1038/s41467-023-40064-9
DB00863 63203 None 12 Human Functional pAC50 = 5.1 5.1 -28 9
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 314 10 2 7 1.5 CNC(=C[N+](=O)[O-])NCCSCc1ccc(CN(C)C)o1 10.1038/s41467-023-40064-9
5311064 1366 None 35 Human Functional pAC50 = 6.1 6.1 -3 7
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 317 8 3 5 2.3 COc1cc(CCNC[C@@H](c2ccc(cc2)O)O)ccc1OC 10.1038/s41467-023-40064-9
534 1366 None 35 Human Functional pAC50 = 6.1 6.1 -3 7
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 317 8 3 5 2.3 COc1cc(CCNC[C@@H](c2ccc(cc2)O)O)ccc1OC 10.1038/s41467-023-40064-9
806 1366 None 35 Human Functional pAC50 = 6.1 6.1 -3 7
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 317 8 3 5 2.3 COc1cc(CCNC[C@@H](c2ccc(cc2)O)O)ccc1OC 10.1038/s41467-023-40064-9
CHEMBL493682 1366 None 35 Human Functional pAC50 = 6.1 6.1 -3 7
Agonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human CHRM1 in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 317 8 3 5 2.3 COc1cc(CCNC[C@@H](c2ccc(cc2)O)O)ccc1OC 10.1038/s41467-023-40064-9
4413 98126 None 43 Human Functional pAC50 = 5.1 5.1 -2 15
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 347 4 5 4 2.6 N=C(N)Nc1ccc(C(=O)Oc2ccc3cc(C(=N)N)ccc3c2)cc1 10.1038/s41467-023-40064-9
CHEMBL273264 98126 None 43 Human Functional pAC50 = 5.1 5.1 -2 15
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 347 4 5 4 2.6 N=C(N)Nc1ccc(C(=O)Oc2ccc3cc(C(=N)N)ccc3c2)cc1 10.1038/s41467-023-40064-9
16960 14493 None 19 Human Functional pAC50 = 5.1 5.1 -1412 7
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 318 5 0 2 3.9 CN(C)CC[C@@H](c1ccc(Br)cc1)c1ccccn1 10.1038/s41467-023-40064-9
16960.0 14493 None 19 Human Functional pAC50 = 5.1 5.1 -1412 7
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 318 5 0 2 3.9 CN(C)CC[C@@H](c1ccc(Br)cc1)c1ccccn1 10.1038/s41467-023-40064-9
CHEMBL1201287 14493 None 19 Human Functional pAC50 = 5.1 5.1 -1412 7
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 318 5 0 2 3.9 CN(C)CC[C@@H](c1ccc(Br)cc1)c1ccccn1 10.1038/s41467-023-40064-9
DB00405 14493 None 19 Human Functional pAC50 = 5.1 5.1 -1412 7
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 318 5 0 2 3.9 CN(C)CC[C@@H](c1ccc(Br)cc1)c1ccccn1 10.1038/s41467-023-40064-9
214 3860 None 43 Human Functional pAC50 = 5.1 5.1 -602 28
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
2740 3860 None 43 Human Functional pAC50 = 5.1 5.1 -602 28
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
5566 3860 None 43 Human Functional pAC50 = 5.1 5.1 -602 28
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
5566.0 3860 None 43 Human Functional pAC50 = 5.1 5.1 -602 28
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
66064 3860 None 43 Human Functional pAC50 = 5.1 5.1 -602 28
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
CHEMBL422 3860 None 43 Human Functional pAC50 = 5.1 5.1 -602 28
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
DB00831 3860 None 43 Human Functional pAC50 = 5.1 5.1 -602 28
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
2335 11852 None 18 Human Functional pAC50 = 5.1 5.1 -14 34
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1038/s41467-023-40064-9
8478 11852 None 18 Human Functional pAC50 = 5.1 5.1 -14 34
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1038/s41467-023-40064-9
CHEMBL1182210 11852 None 18 Human Functional pAC50 = 5.1 5.1 -14 34
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1038/s41467-023-40064-9
CHEMBL221753 11852 None 18 Human Functional pAC50 = 5.1 5.1 -14 34
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1038/s41467-023-40064-9
3149 12618 None 11 Human Functional pAC50 = 5.1 5.1 -24 26
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 334 15 0 1 6.1 CCCCCCCCCCCC[N+](C)(C)CCOc1ccccc1 10.1038/s41467-023-40064-9
CHEMBL1187011 12618 None 11 Human Functional pAC50 = 5.1 5.1 -24 26
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 334 15 0 1 6.1 CCCCCCCCCCCC[N+](C)(C)CCOc1ccccc1 10.1038/s41467-023-40064-9
174174 523 None 33 Human Functional pAC50 = 8.1 8.1 -8 7
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1038/s41467-023-40064-9
174174.0 523 None 33 Human Functional pAC50 = 8.1 8.1 -8 7
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1038/s41467-023-40064-9
260 523 None 33 Human Functional pAC50 = 8.1 8.1 -8 7
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1038/s41467-023-40064-9
320 523 None 33 Human Functional pAC50 = 8.1 8.1 -8 7
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1038/s41467-023-40064-9
CHEMBL517712 523 None 33 Human Functional pAC50 = 8.1 8.1 -8 7
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1038/s41467-023-40064-9
DB00572 523 None 33 Human Functional pAC50 = 8.1 8.1 -8 7
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 289 4 1 4 1.9 OCC(c1ccccc1)C(=O)O[C@@H]1C[C@@H]2CC[C@H](C1)N2C 10.1038/s41467-023-40064-9
3042 1414 None 26 Human Functional pAC50 = 8.0 8.0 -5 17
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC 10.1038/s41467-023-40064-9
3042.0 1414 None 26 Human Functional pAC50 = 8.0 8.0 -5 17
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC 10.1038/s41467-023-40064-9
355 1414 None 26 Human Functional pAC50 = 8.0 8.0 -5 17
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC 10.1038/s41467-023-40064-9
868 1414 None 26 Human Functional pAC50 = 8.0 8.0 -5 17
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC 10.1038/s41467-023-40064-9
CHEMBL1123 1414 None 26 Human Functional pAC50 = 8.0 8.0 -5 17
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC 10.1038/s41467-023-40064-9
DB00804 1414 None 26 Human Functional pAC50 = 8.0 8.0 -5 17
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC 10.1038/s41467-023-40064-9
477468 175502 None 22 Human Functional pAC50 = 5.0 5.0 -1 4
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 1269 18 16 23 -3.9 CCCCCOc1ccc(-c2cc(-c3ccc(C(=O)N[C@H]4C[C@@H](O)[C@@H](O)NC(=O)[C@@H]5[C@@H](O)[C@@H](C)CN5C(=O)[C@H]([C@H](O)CC(N)=O)NC(=O)[C@H]([C@H](O)[C@@H](O)c5ccc(O)c(OS(=O)(=O)O)c5)NC(=O)[C@@H]5C[C@@H](O)CN5C(=O)[C@H]([C@@H](C)O)NC4=O)cc3)no2)cc1 10.1038/s41467-023-40064-9
CHEMBL457547 175502 None 22 Human Functional pAC50 = 5.0 5.0 -1 4
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 1269 18 16 23 -3.9 CCCCCOc1ccc(-c2cc(-c3ccc(C(=O)N[C@H]4C[C@@H](O)[C@@H](O)NC(=O)[C@@H]5[C@@H](O)[C@@H](C)CN5C(=O)[C@H]([C@H](O)CC(N)=O)NC(=O)[C@H]([C@H](O)[C@@H](O)c5ccc(O)c(OS(=O)(=O)O)c5)NC(=O)[C@@H]5C[C@@H](O)CN5C(=O)[C@H]([C@@H](C)O)NC4=O)cc3)no2)cc1 10.1038/s41467-023-40064-9
135564886 14499 None 5 Human Functional pAC50 = 5.0 5.0 -3 25
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 752 14 1 6 8.7 CC1(C)C(/C=C/C=C/C=C/C=C2\N(CCCCS(=O)(=O)O)c3ccc4ccccc4c3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccc3ccccc3c21 10.1038/s41467-023-40064-9
135673376 14499 None 5 Human Functional pAC50 = 5.0 5.0 -3 25
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 752 14 1 6 8.7 CC1(C)C(/C=C/C=C/C=C/C=C2\N(CCCCS(=O)(=O)O)c3ccc4ccccc4c3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccc3ccccc3c21 10.1038/s41467-023-40064-9
137157436 14499 None 5 Human Functional pAC50 = 5.0 5.0 -3 25
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 752 14 1 6 8.7 CC1(C)C(/C=C/C=C/C=C/C=C2\N(CCCCS(=O)(=O)O)c3ccc4ccccc4c3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccc3ccccc3c21 10.1038/s41467-023-40064-9
145948239 14499 None 5 Human Functional pAC50 = 5.0 5.0 -3 25
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 752 14 1 6 8.7 CC1(C)C(/C=C/C=C/C=C/C=C2\N(CCCCS(=O)(=O)O)c3ccc4ccccc4c3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccc3ccccc3c21 10.1038/s41467-023-40064-9
71587099 14499 None 5 Human Functional pAC50 = 5.0 5.0 -3 25
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 752 14 1 6 8.7 CC1(C)C(/C=C/C=C/C=C/C=C2\N(CCCCS(=O)(=O)O)c3ccc4ccccc4c3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccc3ccccc3c21 10.1038/s41467-023-40064-9
CHEMBL1201304 14499 None 5 Human Functional pAC50 = 5.0 5.0 -3 25
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 752 14 1 6 8.7 CC1(C)C(/C=C/C=C/C=C/C=C2\N(CCCCS(=O)(=O)O)c3ccc4ccccc4c3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccc3ccccc3c21 10.1038/s41467-023-40064-9
65646 121365 None 16 Human Functional pAC50 = 5.0 5.0 2 3
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 461 6 2 9 0.8 Cc1oc(=O)oc1COC(=O)[C@@H]1N2C(=O)[C@@H](NC(=O)[C@H](N)c3ccccc3)[C@H]2SC1(C)C 10.1038/s41467-023-40064-9
CHEMBL3580454 121365 None 16 Human Functional pAC50 = 5.0 5.0 2 3
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 461 6 2 9 0.8 Cc1oc(=O)oc1COC(=O)[C@@H]1N2C(=O)[C@@H](NC(=O)[C@H](N)c3ccccc3)[C@H]2SC1(C)C 10.1038/s41467-023-40064-9
1210 918 None 42 Human Functional pAC50 = 5.0 5.0 -457 22
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
1213 918 None 42 Human Functional pAC50 = 5.0 5.0 -457 22
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
2725 918 None 42 Human Functional pAC50 = 5.0 5.0 -457 22
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
33036 918 None 42 Human Functional pAC50 = 5.0 5.0 -457 22
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
33036.0 918 None 42 Human Functional pAC50 = 5.0 5.0 -457 22
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
4411 918 None 42 Human Functional pAC50 = 5.0 5.0 -457 22
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
616 918 None 42 Human Functional pAC50 = 5.0 5.0 -457 22
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
6976 918 None 42 Human Functional pAC50 = 5.0 5.0 -457 22
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
716121 918 None 42 Human Functional pAC50 = 5.0 5.0 -457 22
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
CHEMBL1201353 918 None 42 Human Functional pAC50 = 5.0 5.0 -457 22
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
CHEMBL1554789 918 None 42 Human Functional pAC50 = 5.0 5.0 -457 22
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
CHEMBL505 918 None 42 Human Functional pAC50 = 5.0 5.0 -457 22
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
DB01114 918 None 42 Human Functional pAC50 = 5.0 5.0 -457 22
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
DB13679 918 None 42 Human Functional pAC50 = 5.0 5.0 -457 22
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 274 5 0 2 3.8 CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C 10.1038/s41467-023-40064-9
2220 3134 None 58 Human Functional pAC50 = 7.0 7.0 -33 17
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 10.1038/s41467-023-40064-9
27400 3134 None 58 Human Functional pAC50 = 7.0 7.0 -33 17
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 10.1038/s41467-023-40064-9
27400.0 3134 None 58 Human Functional pAC50 = 7.0 7.0 -33 17
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 10.1038/s41467-023-40064-9
93 3134 None 58 Human Functional pAC50 = 7.0 7.0 -33 17
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 10.1038/s41467-023-40064-9
CHEMBL294951 3134 None 58 Human Functional pAC50 = 7.0 7.0 -33 17
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 10.1038/s41467-023-40064-9
DB06153 3134 None 58 Human Functional pAC50 = 7.0 7.0 -33 17
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 10.1038/s41467-023-40064-9
26987 949 None 27 Human Functional pAC50 = 7.0 7.0 -22 34
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C 10.1038/s41467-023-40064-9
26987.0 949 None 27 Human Functional pAC50 = 7.0 7.0 -22 34
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C 10.1038/s41467-023-40064-9
6063 949 None 27 Human Functional pAC50 = 7.0 7.0 -22 34
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C 10.1038/s41467-023-40064-9
671 949 None 27 Human Functional pAC50 = 7.0 7.0 -22 34
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C 10.1038/s41467-023-40064-9
CHEMBL1626 949 None 27 Human Functional pAC50 = 7.0 7.0 -22 34
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C 10.1038/s41467-023-40064-9
DB00283 949 None 27 Human Functional pAC50 = 7.0 7.0 -22 34
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C 10.1038/s41467-023-40064-9
3949 100668 None 35 Human Functional pAC50 = 6.0 6.0 2 16
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 468 8 0 5 4.9 COc1ccc(CN2CCN(C(c3ccc(F)cc3)c3ccc(F)cc3)CC2)c(OC)c1OC 10.1038/s41467-023-40064-9
CHEMBL29188 100668 None 35 Human Functional pAC50 = 6.0 6.0 2 16
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 468 8 0 5 4.9 COc1ccc(CN2CCN(C(c3ccc(F)cc3)c3ccc(F)cc3)CC2)c(OC)c1OC 10.1038/s41467-023-40064-9
11057 176253 None 16 Human Functional pAC50 = 6.0 6.0 -1 25
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 10.1038/s41467-023-40064-9
3468 176253 None 16 Human Functional pAC50 = 6.0 6.0 -1 25
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 10.1038/s41467-023-40064-9
CHEMBL459265 176253 None 16 Human Functional pAC50 = 6.0 6.0 -1 25
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 10.1038/s41467-023-40064-9
CHEMBL64894 176253 None 16 Human Functional pAC50 = 6.0 6.0 -1 25
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 10.1038/s41467-023-40064-9
65863 14471 None 40 Human Functional pAC50 = 5.0 5.0 -5 11
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 436 6 0 4 7.0 Clc1ccc(C(Cn2ccnc2)OCc2csc3c(Cl)cccc23)c(Cl)c1 10.1038/s41467-023-40064-9
CHEMBL1201196 14471 None 40 Human Functional pAC50 = 5.0 5.0 -5 11
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 436 6 0 4 7.0 Clc1ccc(C(Cn2ccnc2)OCc2csc3c(Cl)cccc23)c(Cl)c1 10.1038/s41467-023-40064-9
8569 22651 None 59 Human Functional pAC50 = 5.0 5.0 1 4
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 244 3 2 4 2.3 COc1ccc(C(=O)c2ccccc2O)c(O)c1 10.1038/s41467-023-40064-9
CHEMBL1326877 22651 None 59 Human Functional pAC50 = 5.0 5.0 1 4
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 244 3 2 4 2.3 COc1ccc(C(=O)c2ccccc2O)c(O)c1 10.1038/s41467-023-40064-9
3652 4097 None 50 Human Functional pAC50 = 7.0 7.0 -18 15
Agonist activity at human CHRM1 in an in vitro cell-based assay (NIBR assay) measured by Hamamatsu Functional Drug Screening SystemAgonist activity at human CHRM1 in an in vitro cell-based assay (NIBR assay) measured by Hamamatsu Functional Drug Screening System
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1038/s41467-023-40064-9
57 4097 None 50 Human Functional pAC50 = 7.0 7.0 -18 15
Agonist activity at human CHRM1 in an in vitro cell-based assay (NIBR assay) measured by Hamamatsu Functional Drug Screening SystemAgonist activity at human CHRM1 in an in vitro cell-based assay (NIBR assay) measured by Hamamatsu Functional Drug Screening System
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1038/s41467-023-40064-9
60809 4097 None 50 Human Functional pAC50 = 7.0 7.0 -18 15
Agonist activity at human CHRM1 in an in vitro cell-based assay (NIBR assay) measured by Hamamatsu Functional Drug Screening SystemAgonist activity at human CHRM1 in an in vitro cell-based assay (NIBR assay) measured by Hamamatsu Functional Drug Screening System
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1038/s41467-023-40064-9
60809.0 4097 None 50 Human Functional pAC50 = 7.0 7.0 -18 15
Agonist activity at human CHRM1 in an in vitro cell-based assay (NIBR assay) measured by Hamamatsu Functional Drug Screening SystemAgonist activity at human CHRM1 in an in vitro cell-based assay (NIBR assay) measured by Hamamatsu Functional Drug Screening System
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1038/s41467-023-40064-9
CHEMBL21536 4097 None 50 Human Functional pAC50 = 7.0 7.0 -18 15
Agonist activity at human CHRM1 in an in vitro cell-based assay (NIBR assay) measured by Hamamatsu Functional Drug Screening SystemAgonist activity at human CHRM1 in an in vitro cell-based assay (NIBR assay) measured by Hamamatsu Functional Drug Screening System
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1038/s41467-023-40064-9
DB15357 4097 None 50 Human Functional pAC50 = 7.0 7.0 -18 15
Agonist activity at human CHRM1 in an in vitro cell-based assay (NIBR assay) measured by Hamamatsu Functional Drug Screening SystemAgonist activity at human CHRM1 in an in vitro cell-based assay (NIBR assay) measured by Hamamatsu Functional Drug Screening System
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1038/s41467-023-40064-9
3354 41798 None 37 Human Functional pAC50 = 5.0 5.0 -10 9
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 391 5 0 5 4.4 Cc1c(-c2ccccc2)oc2c(C(=O)OCCN3CCCCC3)cccc2c1=O 10.1038/s41467-023-40064-9
3354.0 41798 None 37 Human Functional pAC50 = 5.0 5.0 -10 9
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 391 5 0 5 4.4 Cc1c(-c2ccccc2)oc2c(C(=O)OCCN3CCCCC3)cccc2c1=O 10.1038/s41467-023-40064-9
CHEMBL1493 41798 None 37 Human Functional pAC50 = 5.0 5.0 -10 9
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 391 5 0 5 4.4 Cc1c(-c2ccccc2)oc2c(C(=O)OCCN3CCCCC3)cccc2c1=O 10.1038/s41467-023-40064-9
DB01148 41798 None 37 Human Functional pAC50 = 5.0 5.0 -10 9
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 391 5 0 5 4.4 Cc1c(-c2ccccc2)oc2c(C(=O)OCCN3CCCCC3)cccc2c1=O 10.1038/s41467-023-40064-9
3103 41672 None 36 Human Functional pAC50 = 7.0 7.0 1 9
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 281 4 0 2 3.9 CN1CCC(OC(c2ccccc2)c2ccccc2)CC1 10.1038/s41467-023-40064-9
3103.0 41672 None 36 Human Functional pAC50 = 7.0 7.0 1 9
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 281 4 0 2 3.9 CN1CCC(OC(c2ccccc2)c2ccccc2)CC1 10.1038/s41467-023-40064-9
CHEMBL1492 41672 None 36 Human Functional pAC50 = 7.0 7.0 1 9
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 281 4 0 2 3.9 CN1CCC(OC(c2ccccc2)c2ccccc2)CC1 10.1038/s41467-023-40064-9
DB01146 41672 None 36 Human Functional pAC50 = 7.0 7.0 1 9
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 281 4 0 2 3.9 CN1CCC(OC(c2ccccc2)c2ccccc2)CC1 10.1038/s41467-023-40064-9
4601 209205 None 27 Human Functional pAC50 = 6.0 6.0 -19 19
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 10.1038/s41467-023-40064-9
4601.0 209205 None 27 Human Functional pAC50 = 6.0 6.0 -19 19
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL1201023 209205 None 27 Human Functional pAC50 = 6.0 6.0 -19 19
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL900 209205 None 27 Human Functional pAC50 = 6.0 6.0 -19 19
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 10.1038/s41467-023-40064-9
DB01173 209205 None 27 Human Functional pAC50 = 6.0 6.0 -19 19
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 10.1038/s41467-023-40064-9
2381 663 None 30 Human Functional pAC50 = 7.0 7.0 25 5
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 10.1038/s41467-023-40064-9
2381.0 663 None 30 Human Functional pAC50 = 7.0 7.0 25 5
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 10.1038/s41467-023-40064-9
374 663 None 30 Human Functional pAC50 = 7.0 7.0 25 5
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 10.1038/s41467-023-40064-9
7128 663 None 30 Human Functional pAC50 = 7.0 7.0 25 5
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 10.1038/s41467-023-40064-9
CHEMBL1101 663 None 30 Human Functional pAC50 = 7.0 7.0 25 5
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 10.1038/s41467-023-40064-9
DB00810 663 None 30 Human Functional pAC50 = 7.0 7.0 25 5
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 311 5 1 2 4.0 OC(C1CC2CC1C=C2)(c1ccccc1)CCN1CCCCC1 10.1038/s41467-023-40064-9
68617 207985 None 33 Human Functional pAC50 = 5.0 5.0 -10 30
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 10.1038/s41467-023-40064-9
CHEMBL1709 207985 None 33 Human Functional pAC50 = 5.0 5.0 -10 30
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 10.1038/s41467-023-40064-9
CHEMBL809 207985 None 33 Human Functional pAC50 = 5.0 5.0 -10 30
Compound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assayCompound was evaluated for inhibition of human CHRM1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 10.1038/s41467-023-40064-9
3157 1470 None 44 Human Functional pAC50 = 5.0 5.0 -16982 21
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1038/s41467-023-40064-9
3157.0 1470 None 44 Human Functional pAC50 = 5.0 5.0 -16982 21
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1038/s41467-023-40064-9
7170 1470 None 44 Human Functional pAC50 = 5.0 5.0 -16982 21
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1038/s41467-023-40064-9
954 1470 None 44 Human Functional pAC50 = 5.0 5.0 -16982 21
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1038/s41467-023-40064-9
CHEMBL707 1470 None 44 Human Functional pAC50 = 5.0 5.0 -16982 21
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1038/s41467-023-40064-9
DB00590 1470 None 44 Human Functional pAC50 = 5.0 5.0 -16982 21
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1038/s41467-023-40064-9
3607 36392 None 50 Human Functional pAC50 = 5.0 5.0 -3 7
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 339 12 1 3 4.7 CCCCC(CC)CN1CN(CC(CC)CCCC)CC(C)(N)C1 10.1038/s41467-023-40064-9
CHEMBL144673 36392 None 50 Human Functional pAC50 = 5.0 5.0 -3 7
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 339 12 1 3 4.7 CCCCC(CC)CN1CN(CC(CC)CCCC)CC(C)(N)C1 10.1038/s41467-023-40064-9
9324 9240 None 40 Human Functional pAC50 = 5.0 5.0 -1 6
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 404 2 0 4 4.8 CC(=O)O[C@]1(C(C)=O)CC[C@H]2[C@@H]3C=C(Cl)C4=CC(=O)CC[C@]4(C)[C@H]3CC[C@@]21C 10.1038/s41467-023-40064-9
CHEMBL110691 9240 None 40 Human Functional pAC50 = 5.0 5.0 -1 6
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 404 2 0 4 4.8 CC(=O)O[C@]1(C(C)=O)CC[C@H]2[C@@H]3C=C(Cl)C4=CC(=O)CC[C@]4(C)[C@H]3CC[C@@]21C 10.1038/s41467-023-40064-9
1662 188812 None 53 Human Functional pAC50 = 5.0 5.0 1 3
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 162 4 3 3 -0.3 CC(O)(CC(=O)O)CC(=O)O 10.1038/s41467-023-40064-9
CHEMBL50444 188812 None 53 Human Functional pAC50 = 5.0 5.0 1 3
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 162 4 3 3 -0.3 CC(O)(CC(=O)O)CC(=O)O 10.1038/s41467-023-40064-9
2723 154135 None 63 Human Functional pAC50 = 5 5.0 -5 4
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 156 0 1 1 2.7 Cc1cc(O)cc(C)c1Cl 10.1038/s41467-023-40064-9
CHEMBL398440 154135 None 63 Human Functional pAC50 = 5 5.0 -5 4
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 156 0 1 1 2.7 Cc1cc(O)cc(C)c1Cl 10.1038/s41467-023-40064-9
133 2496 None 39 Human Functional pAC50 = 5 5.0 -25118 27
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 10.1038/s41467-023-40064-9
1723 2496 None 39 Human Functional pAC50 = 5 5.0 -25118 27
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 10.1038/s41467-023-40064-9
28693 2496 None 39 Human Functional pAC50 = 5 5.0 -25118 27
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 10.1038/s41467-023-40064-9
CHEMBL19215 2496 None 39 Human Functional pAC50 = 5 5.0 -25118 27
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 10.1038/s41467-023-40064-9
DB13520 2496 None 39 Human Functional pAC50 = 5 5.0 -25118 27
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 10.1038/s41467-023-40064-9
9927975 4190 None 0 Human Functional pEC50 = 9.7 9.7 10 2
Effective concentration required for stimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptorEffective concentration required for stimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptor
ChEMBL 341 3 0 5 3.5 C(#Cc1ccccc1)CSc1nsnc1[C@H]1CN2CCC[C@H]1C2 10.1016/s0960-894x(98)00509-5
CHEMBL100147 4190 None 0 Human Functional pEC50 = 9.7 9.7 10 2
Effective concentration required for stimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptorEffective concentration required for stimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptor
ChEMBL 341 3 0 5 3.5 C(#Cc1ccccc1)CSc1nsnc1[C@H]1CN2CCC[C@H]1C2 10.1016/s0960-894x(98)00509-5
24967746 16062 None 0 Human Functional pEC50 = 9.4 9.4 31 5
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 403 5 1 4 4.5 CCCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)[nH]c4cc(F)c(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223754 16062 None 0 Human Functional pEC50 = 9.4 9.4 31 5
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 403 5 1 4 4.5 CCCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)[nH]c4cc(F)c(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
42599070 16085 None 0 Human Functional pEC50 = 9.4 9.4 50 5
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 370 4 0 3 4.1 CCO[C@H]1CC[C@](C)(N2CCC(N3C(=O)Cc4ccc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223804 16085 None 0 Human Functional pEC50 = 9.4 9.4 50 5
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 370 4 0 3 4.1 CCO[C@H]1CC[C@](C)(N2CCC(N3C(=O)Cc4ccc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
44330081 210622 None 0 Human Functional pEC50 = 9.3 9.3 17 2
Stimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptorStimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptor
ChEMBL 325 3 0 5 2.8 C(#Cc1ccccc1)COc1nsnc1[C@H]1CN2CCC[C@H]1C2 10.1016/s0960-894x(98)00509-5
CHEMBL98255 210622 None 0 Human Functional pEC50 = 9.3 9.3 17 2
Stimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptorStimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptor
ChEMBL 325 3 0 5 2.8 C(#Cc1ccccc1)COc1nsnc1[C@H]1CN2CCC[C@H]1C2 10.1016/s0960-894x(98)00509-5
42598591 16084 None 0 Human Functional pEC50 = 9.3 9.3 39 5
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 384 5 0 3 4.5 CCCO[C@H]1CC[C@](C)(N2CCC(N3C(=O)Cc4ccc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223803 16084 None 0 Human Functional pEC50 = 9.3 9.3 39 5
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 384 5 0 3 4.5 CCCO[C@H]1CC[C@](C)(N2CCC(N3C(=O)Cc4ccc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
118724611 116525 None 0 Human Functional pEC50 = 9.2 9.2 - 1
Positive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assay
ChEMBL 373 3 1 5 3.4 Cn1cc(-c2ccc(Cn3cc4c(=O)[nH]nc-4c4ccccc43)c(F)c2)cn1 10.1016/j.bmcl.2014.11.011
CHEMBL3360954 116525 None 0 Human Functional pEC50 = 9.2 9.2 - 1
Positive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assay
ChEMBL 373 3 1 5 3.4 Cn1cc(-c2ccc(Cn3cc4c(=O)[nH]nc-4c4ccccc43)c(F)c2)cn1 10.1016/j.bmcl.2014.11.011
25110765 187124 None 0 Human Functional pEC50 = 9.1 9.1 - 1
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
ChEMBL 422 4 1 4 4.1 Cc1ccccc1CN1CCC(N2CCC(n3c(=O)[nH]c4ccc(F)cc43)CC2)CC1 10.1016/j.bmcl.2008.09.023
CHEMBL490797 187124 None 0 Human Functional pEC50 = 9.1 9.1 - 1
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
ChEMBL 422 4 1 4 4.1 Cc1ccccc1CN1CCC(N2CCC(n3c(=O)[nH]c4ccc(F)cc43)CC2)CC1 10.1016/j.bmcl.2008.09.023
46871844 6814 None 0 Human Functional pEC50 = 9.1 9.1 50 5
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 360 4 2 2 4.1 C[C@H]1CNCC[C@@H]1CNC(=O)c1c(F)cccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.127
CHEMBL1083925 6814 None 0 Human Functional pEC50 = 9.1 9.1 50 5
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 360 4 2 2 4.1 C[C@H]1CNCC[C@@H]1CNC(=O)c1c(F)cccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.127
25110764 193180 None 0 Human Functional pEC50 = 9.1 9.1 - 1
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
ChEMBL 422 4 1 4 4.1 Cc1ccccc1CN1CCC(N2CCC(n3c(=O)[nH]c4cc(F)ccc43)CC2)CC1 10.1016/j.bmcl.2008.09.023
CHEMBL522451 193180 None 0 Human Functional pEC50 = 9.1 9.1 - 1
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
ChEMBL 422 4 1 4 4.1 Cc1ccccc1CN1CCC(N2CCC(n3c(=O)[nH]c4cc(F)ccc43)CC2)CC1 10.1016/j.bmcl.2008.09.023
44329977 111473 None 0 Human Functional pEC50 = 9 9.0 10 2
Stimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptorStimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptor
ChEMBL 311 3 0 5 2.4 C(#Cc1ccccc1)COc1nsnc1[C@H]1CN2CCC1C2 10.1016/s0960-894x(98)00509-5
CHEMBL327269 111473 None 0 Human Functional pEC50 = 9 9.0 10 2
Stimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptorStimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptor
ChEMBL 311 3 0 5 2.4 C(#Cc1ccccc1)COc1nsnc1[C@H]1CN2CCC1C2 10.1016/s0960-894x(98)00509-5
46890906 7044 None 0 Human Functional pEC50 = 9 9.0 1 2
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 329 5 2 2 4.8 OC(CCC1CCNCC1)c1ccccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.127
CHEMBL1084850 7044 None 0 Human Functional pEC50 = 9 9.0 1 2
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 329 5 2 2 4.8 OC(CCC1CCNCC1)c1ccccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.127
42598358 16109 None 0 Human Functional pEC50 = 9 9.0 50 5
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 390 4 0 5 4.4 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4cc(F)c(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223860 16109 None 0 Human Functional pEC50 = 9 9.0 50 5
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 390 4 0 5 4.4 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4cc(F)c(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
44351242 118124 None 0 Human Functional pEC50 = 9 9.0 5 2
Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.
ChEMBL 285 5 0 6 2.5 CCCSc1nsnc1OC1CN2CCCC1C2 10.1021/jm970125n
CHEMBL340435 118124 None 0 Human Functional pEC50 = 9 9.0 5 2
Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.
ChEMBL 285 5 0 6 2.5 CCCSc1nsnc1OC1CN2CCCC1C2 10.1021/jm970125n
44330074 107263 None 0 Human Functional pEC50 = 9 9.0 - 1
Stimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptorStimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptor
ChEMBL 341 3 0 5 3.5 C(#Cc1ccccc1)CSc1nsnc1[C@@H]1CN2CCC[C@H]1C2 10.1016/s0960-894x(98)00509-5
CHEMBL316625 107263 None 0 Human Functional pEC50 = 9 9.0 - 1
Stimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptorStimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptor
ChEMBL 341 3 0 5 3.5 C(#Cc1ccccc1)CSc1nsnc1[C@@H]1CN2CCC[C@H]1C2 10.1016/s0960-894x(98)00509-5
44579457 186968 None 0 Human Functional pEC50 = 9.0 9.0 2570 2
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
ChEMBL 476 4 1 4 4.8 O=c1[nH]c2cc(F)ccc2n1C1CCN(C2CCN(Cc3ccccc3C(F)(F)F)CC2)CC1 10.1016/j.bmcl.2008.09.023
CHEMBL489576 186968 None 0 Human Functional pEC50 = 9.0 9.0 2570 2
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
ChEMBL 476 4 1 4 4.8 O=c1[nH]c2cc(F)ccc2n1C1CCN(C2CCN(Cc3ccccc3C(F)(F)F)CC2)CC1 10.1016/j.bmcl.2008.09.023
44579418 187088 None 0 Human Functional pEC50 = 9.0 9.0 - 1
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
ChEMBL 422 4 1 4 4.1 Cc1ccccc1CN1CCC(N2CCC(n3c(=O)[nH]c4c(F)cccc43)CC2)CC1 10.1016/j.bmcl.2008.09.023
CHEMBL490598 187088 None 0 Human Functional pEC50 = 9.0 9.0 - 1
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
ChEMBL 422 4 1 4 4.1 Cc1ccccc1CN1CCC(N2CCC(n3c(=O)[nH]c4c(F)cccc43)CC2)CC1 10.1016/j.bmcl.2008.09.023
187 255 None 24 Human Functional pEC50 = 9.0 9.0 -5 8
Agonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2012.05.048
187.0 255 None 24 Human Functional pEC50 = 9.0 9.0 -5 8
Agonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2012.05.048
294 255 None 24 Human Functional pEC50 = 9.0 9.0 -5 8
Agonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2012.05.048
65 255 None 24 Human Functional pEC50 = 9.0 9.0 -5 8
Agonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2012.05.048
8593 255 None 24 Human Functional pEC50 = 9.0 9.0 -5 8
Agonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2012.05.048
CHEMBL667 255 None 24 Human Functional pEC50 = 9.0 9.0 -5 8
Agonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2012.05.048
DB03128 255 None 24 Human Functional pEC50 = 9.0 9.0 -5 8
Agonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2012.05.048
187 255 None 24 Human Functional pEC50 = 9.0 9.0 -5 8
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm100697g
187.0 255 None 24 Human Functional pEC50 = 9.0 9.0 -5 8
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm100697g
294 255 None 24 Human Functional pEC50 = 9.0 9.0 -5 8
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm100697g
65 255 None 24 Human Functional pEC50 = 9.0 9.0 -5 8
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm100697g
8593 255 None 24 Human Functional pEC50 = 9.0 9.0 -5 8
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm100697g
CHEMBL667 255 None 24 Human Functional pEC50 = 9.0 9.0 -5 8
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm100697g
DB03128 255 None 24 Human Functional pEC50 = 9.0 9.0 -5 8
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm100697g
9883040 100591 None 0 Human Functional pEC50 = 9.0 9.0 3 3
In vitro functional agonism against M1 muscarinic receptor (PI)In vitro functional agonism against M1 muscarinic receptor (PI)
ChEMBL 307 8 0 5 3.2 CCCCCCSc1nccnc1O[C@H]1CN2CCC1C2 10.1016/s0960-894x(99)00313-3
CHEMBL291339 100591 None 0 Human Functional pEC50 = 9.0 9.0 3 3
In vitro functional agonism against M1 muscarinic receptor (PI)In vitro functional agonism against M1 muscarinic receptor (PI)
ChEMBL 307 8 0 5 3.2 CCCCCCSc1nccnc1O[C@H]1CN2CCC1C2 10.1016/s0960-894x(99)00313-3
CHEMBL542622 100591 None 0 Human Functional pEC50 = 9.0 9.0 3 3
In vitro functional agonism against M1 muscarinic receptor (PI)In vitro functional agonism against M1 muscarinic receptor (PI)
ChEMBL 307 8 0 5 3.2 CCCCCCSc1nccnc1O[C@H]1CN2CCC1C2 10.1016/s0960-894x(99)00313-3
68153829 116526 None 0 Human Functional pEC50 = 8.9 8.9 - 1
Positive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assay
ChEMBL 341 3 1 5 3.1 O=c1[nH]nc2c3ccccc3n(Cc3ccc(-n4cccn4)cc3)cc1-2 10.1016/j.bmcl.2014.11.011
CHEMBL3360955 116526 None 0 Human Functional pEC50 = 8.9 8.9 - 1
Positive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assay
ChEMBL 341 3 1 5 3.1 O=c1[nH]nc2c3ccccc3n(Cc3ccc(-n4cccn4)cc3)cc1-2 10.1016/j.bmcl.2014.11.011
42598828 16110 None 0 Human Functional pEC50 = 8.9 8.9 125 5
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 390 4 0 5 4.4 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4c(F)cc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223861 16110 None 0 Human Functional pEC50 = 8.9 8.9 125 5
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 390 4 0 5 4.4 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4c(F)cc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
302 2977 None 15 Human Functional pEC50 = 8.8 8.8 -3 8
Agonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assayAgonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assay
ChEMBL 206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1 10.1016/j.bmcl.2015.02.012
4630 2977 None 15 Human Functional pEC50 = 8.8 8.8 -3 8
Agonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assayAgonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assay
ChEMBL 206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1 10.1016/j.bmcl.2015.02.012
CHEMBL7634 2977 None 15 Human Functional pEC50 = 8.8 8.8 -3 8
Agonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assayAgonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assay
ChEMBL 206 2 0 2 0.7 O=C1CCCN1CC#CCN1CCCC1 10.1016/j.bmcl.2015.02.012
3652 4097 None 50 Human Functional pEC50 = 8.8 8.8 -18 15
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm100697g
57 4097 None 50 Human Functional pEC50 = 8.8 8.8 -18 15
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm100697g
60809 4097 None 50 Human Functional pEC50 = 8.8 8.8 -18 15
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm100697g
60809.0 4097 None 50 Human Functional pEC50 = 8.8 8.8 -18 15
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm100697g
CHEMBL21536 4097 None 50 Human Functional pEC50 = 8.8 8.8 -18 15
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm100697g
DB15357 4097 None 50 Human Functional pEC50 = 8.8 8.8 -18 15
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm100697g
44579419 192794 None 0 Human Functional pEC50 = 8.8 8.8 - 1
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
ChEMBL 476 4 1 4 4.8 O=c1[nH]c2c(F)cccc2n1C1CCN(C2CCN(Cc3ccccc3C(F)(F)F)CC2)CC1 10.1016/j.bmcl.2008.09.023
CHEMBL521914 192794 None 0 Human Functional pEC50 = 8.8 8.8 - 1
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
ChEMBL 476 4 1 4 4.8 O=c1[nH]c2c(F)cccc2n1C1CCN(C2CCN(Cc3ccccc3C(F)(F)F)CC2)CC1 10.1016/j.bmcl.2008.09.023
24751745 202311 None 0 Human Functional pEC50 = 8.8 8.8 - 1
Agonist activity at human muscarinic M1 acetylcholine receptor expressed CHO cells assessed as intracellular calcium mobilization after 1 hr by Fluo-4-AM based fluorescence assayAgonist activity at human muscarinic M1 acetylcholine receptor expressed CHO cells assessed as intracellular calcium mobilization after 1 hr by Fluo-4-AM based fluorescence assay
ChEMBL 345 4 1 4 3.0 COc1ccc(Cn2cc(C(=O)O)c(=O)c3c(F)ccc(F)c32)cc1 10.1021/jm400540b
CHEMBL594432 202311 None 0 Human Functional pEC50 = 8.8 8.8 - 1
Agonist activity at human muscarinic M1 acetylcholine receptor expressed CHO cells assessed as intracellular calcium mobilization after 1 hr by Fluo-4-AM based fluorescence assayAgonist activity at human muscarinic M1 acetylcholine receptor expressed CHO cells assessed as intracellular calcium mobilization after 1 hr by Fluo-4-AM based fluorescence assay
ChEMBL 345 4 1 4 3.0 COc1ccc(Cn2cc(C(=O)O)c(=O)c3c(F)ccc(F)c32)cc1 10.1021/jm400540b
22730942 18113 None 0 Human Functional pEC50 = 8.7 8.7 -2 2
Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.
ChEMBL 271 5 0 6 2.1 CCCSc1nsnc1OC1CN2CCC1C2 10.1021/jm970125n
CHEMBL126846 18113 None 0 Human Functional pEC50 = 8.7 8.7 -2 2
Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.
ChEMBL 271 5 0 6 2.1 CCCSc1nsnc1OC1CN2CCC1C2 10.1021/jm970125n
9809330 116063 None 0 Human Functional pEC50 = 8 8.0 -39 3
Agonist activity at human M1 receptor E170K mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M1 receptor E170K mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 552 16 0 13 2.3 CN1CCC=C(c2nsnc2OCCOCCOCCOCCOc2nsnc2C2=CCCN(C)C2)C1 10.1021/jm0606995
CHEMBL335542 116063 None 0 Human Functional pEC50 = 8 8.0 -39 3
Agonist activity at human M1 receptor E170K mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M1 receptor E170K mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 552 16 0 13 2.3 CN1CCC=C(c2nsnc2OCCOCCOCCOCCOc2nsnc2C2=CCCN(C)C2)C1 10.1021/jm0606995
46891179 6419 None 0 Human Functional pEC50 = 8 8.0 251 5
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 378 4 2 2 4.2 C[C@H]1CNCC[C@]1(F)CNC(=O)c1c(F)cccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.127
CHEMBL1082365 6419 None 0 Human Functional pEC50 = 8 8.0 251 5
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 378 4 2 2 4.2 C[C@H]1CNCC[C@]1(F)CNC(=O)c1c(F)cccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.127
46871665 6597 None 0 Human Functional pEC50 = 8 8.0 100 5
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 346 4 2 2 3.9 O=C(NCC1CCNCC1)c1ccccc1-c1cc(Cl)ccc1F 10.1016/j.bmcl.2010.04.128
CHEMBL1083108 6597 None 0 Human Functional pEC50 = 8 8.0 100 5
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 346 4 2 2 3.9 O=C(NCC1CCNCC1)c1ccccc1-c1cc(Cl)ccc1F 10.1016/j.bmcl.2010.04.128
25207745 16133 None 0 Human Functional pEC50 = 8 8.0 79 5
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 413 6 0 7 3.5 COCCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(C#N)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223941 16133 None 0 Human Functional pEC50 = 8 8.0 79 5
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 413 6 0 7 3.5 COCCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(C#N)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
46930343 16708 None 0 Human Functional pEC50 = 8 8.0 - 1
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 381 6 1 4 2.1 CCC(=O)NC1CCN(CCCN2C(=O)COc3cc(F)c(F)cc32)CC1 10.1021/jm100697g
CHEMBL1242925 16708 None 0 Human Functional pEC50 = 8 8.0 - 1
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 381 6 1 4 2.1 CCC(=O)NC1CCN(CCCN2C(=O)COc3cc(F)c(F)cc32)CC1 10.1021/jm100697g
264734 10112 None 58 Human Functional pEC50 = 8 8.0 - 1
Positive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assay
ChEMBL 237 2 0 2 2.4 O=C1C(=O)N(Cc2ccccc2)c2ccccc21 10.1016/j.bmcl.2014.11.011
CHEMBL115581 10112 None 58 Human Functional pEC50 = 8 8.0 - 1
Positive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assay
ChEMBL 237 2 0 2 2.4 O=C1C(=O)N(Cc2ccccc2)c2ccccc21 10.1016/j.bmcl.2014.11.011
118724612 116527 None 0 Human Functional pEC50 = 8 8.0 - 1
Positive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assay
ChEMBL 303 3 0 4 2.6 O=C1C(=O)N(Cc2ccc(-n3cccn3)cc2)c2ccccc21 10.1016/j.bmcl.2014.11.011
CHEMBL3360956 116527 None 0 Human Functional pEC50 = 8 8.0 - 1
Positive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assay
ChEMBL 303 3 0 4 2.6 O=C1C(=O)N(Cc2ccc(-n3cccn3)cc2)c2ccccc21 10.1016/j.bmcl.2014.11.011
44303018 204480 None 0 Human Functional pEC50 = 8.0 8.0 4 3
Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.
ChEMBL 343 3 0 5 2.4 Clc1cccc(C#CCOc2nsnc2C23CN4CC2C3C4)c1 10.1021/jm9910019
CHEMBL60833 204480 None 0 Human Functional pEC50 = 8.0 8.0 4 3
Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.
ChEMBL 343 3 0 5 2.4 Clc1cccc(C#CCOc2nsnc2C23CN4CC2C3C4)c1 10.1021/jm9910019
46891597 6400 None 0 Human Functional pEC50 = 7 7.0 - 1
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 362 4 2 2 4.4 O=C(NCC1CCNCC1)c1ccc(Cl)cc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.127
CHEMBL1082316 6400 None 0 Human Functional pEC50 = 7 7.0 - 1
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 362 4 2 2 4.4 O=C(NCC1CCNCC1)c1ccc(Cl)cc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.127
46890714 6619 None 0 Human Functional pEC50 = 7 7.0 - 1
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 362 4 2 2 4.4 O=C(NCC1CCNCC1)c1cc(Cl)ccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.127
CHEMBL1083277 6619 None 0 Human Functional pEC50 = 7 7.0 - 1
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 362 4 2 2 4.4 O=C(NCC1CCNCC1)c1cc(Cl)ccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.127
44207208 16726 None 0 Human Functional pEC50 = 7 7.0 - 1
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 423 7 1 4 3.3 O=C(Cc1ccccc1)NC1CCN(CCCN2C(=O)CSc3ccccc32)CC1 10.1021/jm100697g
CHEMBL1243138 16726 None 0 Human Functional pEC50 = 7 7.0 - 1
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 423 7 1 4 3.3 O=C(Cc1ccccc1)NC1CCN(CCCN2C(=O)CSc3ccccc32)CC1 10.1021/jm100697g
145984661 165474 None 0 Rat Functional pEC50 = 7 7.0 -8 2
Positive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assayPositive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assay
ChEMBL 448 5 2 7 3.2 Cn1ccc2c(Cc3ccc(-c4nccs4)cc3)cc(C(=O)N[C@@H]3CCOC[C@H]3O)nc21 10.1021/acsmedchemlett.8b00261
CHEMBL4237601 165474 None 0 Rat Functional pEC50 = 7 7.0 -8 2
Positive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assayPositive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assay
ChEMBL 448 5 2 7 3.2 Cn1ccc2c(Cc3ccc(-c4nccs4)cc3)cc(C(=O)N[C@@H]3CCOC[C@H]3O)nc21 10.1021/acsmedchemlett.8b00261
16094783 136654 None 0 Human Functional pEC50 = 6 6.0 -12 3
Agonist activity at human M1 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M1 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 399 10 0 11 1.6 COc1nsnc1OCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0606995
CHEMBL373888 136654 None 0 Human Functional pEC50 = 6 6.0 -12 3
Agonist activity at human M1 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M1 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 399 10 0 11 1.6 COc1nsnc1OCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0606995
70685587 74202 None 0 Human Functional pEC50 = 6 6.0 - 1
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
ChEMBL 351 6 2 5 2.2 CCOC(=O)N1[C@H]2CC[C@@H]1C[C@@H](NCCNC(=O)c1cccs1)C2 10.1016/j.bmcl.2012.03.088
CHEMBL2022948 74202 None 0 Human Functional pEC50 = 6 6.0 - 1
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
ChEMBL 351 6 2 5 2.2 CCOC(=O)N1[C@H]2CC[C@@H]1C[C@@H](NCCNC(=O)c1cccs1)C2 10.1016/j.bmcl.2012.03.088
76327871 103325 None 0 Human Functional pEC50 = 6 6.0 - 1
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
ChEMBL 351 6 2 4 2.1 CCOC(=O)N1C[C@@H]2CC[C@H](C1)[C@@H]2NCCNC(=O)C1CCCCC1 10.1016/j.bmcl.2012.03.088
CHEMBL3084452 103325 None 0 Human Functional pEC50 = 6 6.0 - 1
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
ChEMBL 351 6 2 4 2.1 CCOC(=O)N1C[C@@H]2CC[C@H](C1)[C@@H]2NCCNC(=O)C1CCCCC1 10.1016/j.bmcl.2012.03.088
46890718 6732 None 0 Human Functional pEC50 = 6 6.0 - 1
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 342 4 2 2 4.0 Cc1ccc(-c2cccc(Cl)c2)c(C(=O)NCC2CCNCC2)c1 10.1016/j.bmcl.2010.04.127
CHEMBL1083718 6732 None 0 Human Functional pEC50 = 6 6.0 - 1
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 342 4 2 2 4.0 Cc1ccc(-c2cccc(Cl)c2)c(C(=O)NCC2CCNCC2)c1 10.1016/j.bmcl.2010.04.127
46890972 6970 None 0 Human Functional pEC50 = 6 6.0 - 1
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 346 4 2 2 3.9 O=C(NCC1CCNCC1)c1ccccc1-c1cccc(Cl)c1F 10.1016/j.bmcl.2010.04.128
CHEMBL1084572 6970 None 0 Human Functional pEC50 = 6 6.0 - 1
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 346 4 2 2 3.9 O=C(NCC1CCNCC1)c1ccccc1-c1cccc(Cl)c1F 10.1016/j.bmcl.2010.04.128
46890907 7045 None 0 Human Functional pEC50 = 6 6.0 -79 2
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 311 4 1 1 5.4 Clc1cccc(-c2ccccc2/C=C/CC2CCNCC2)c1 10.1016/j.bmcl.2010.04.127
CHEMBL1084851 7045 None 0 Human Functional pEC50 = 6 6.0 -79 2
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 311 4 1 1 5.4 Clc1cccc(-c2ccccc2/C=C/CC2CCNCC2)c1 10.1016/j.bmcl.2010.04.127
20918653 116513 None 5 Human Functional pEC50 = 6 6.0 - 1
Positive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assay
ChEMBL 383 4 0 4 4.5 O=c1c2cn(Cc3ccccc3)c3ccccc3c-2nn1Cc1ccccc1F 10.1016/j.bmcl.2014.11.011
CHEMBL3360928 116513 None 5 Human Functional pEC50 = 6 6.0 - 1
Positive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assay
ChEMBL 383 4 0 4 4.5 O=c1c2cn(Cc3ccccc3)c3ccccc3c-2nn1Cc1ccccc1F 10.1016/j.bmcl.2014.11.011
187 255 None 24 Human Functional pEC50 = 4 4.0 -5 8
Agonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assayAgonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2015.02.012
187.0 255 None 24 Human Functional pEC50 = 4 4.0 -5 8
Agonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assayAgonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2015.02.012
294 255 None 24 Human Functional pEC50 = 4 4.0 -5 8
Agonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assayAgonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2015.02.012
65 255 None 24 Human Functional pEC50 = 4 4.0 -5 8
Agonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assayAgonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2015.02.012
8593 255 None 24 Human Functional pEC50 = 4 4.0 -5 8
Agonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assayAgonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2015.02.012
CHEMBL667 255 None 24 Human Functional pEC50 = 4 4.0 -5 8
Agonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assayAgonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2015.02.012
DB03128 255 None 24 Human Functional pEC50 = 4 4.0 -5 8
Agonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assayAgonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2015.02.012
163938 106974 None 7 Human Functional pEC50 = 4 4.0 -316 2
Effective concentration for HMPA (human muscarinic inositol phosphate accumulation) activity measured in CHO cells expressing Muscarinic acetylcholine receptor M1Effective concentration for HMPA (human muscarinic inositol phosphate accumulation) activity measured in CHO cells expressing Muscarinic acetylcholine receptor M1
ChEMBL 180 1 1 5 0.1 Nc1noc(C2CN3CCC2C3)n1 10.1016/S0960-894X(00)80538-7
CHEMBL314737 106974 None 7 Human Functional pEC50 = 4 4.0 -316 2
Effective concentration for HMPA (human muscarinic inositol phosphate accumulation) activity measured in CHO cells expressing Muscarinic acetylcholine receptor M1Effective concentration for HMPA (human muscarinic inositol phosphate accumulation) activity measured in CHO cells expressing Muscarinic acetylcholine receptor M1
ChEMBL 180 1 1 5 0.1 Nc1noc(C2CN3CCC2C3)n1 10.1016/S0960-894X(00)80538-7
117973690 137084 None 0 Human Functional pEC50 = 7 7.0 - 1
Positive allosteric modulation of human M1 receptor expressed in CHO cells assessed as acetylcholine-induced calcium mobilization by FLIPR assayPositive allosteric modulation of human M1 receptor expressed in CHO cells assessed as acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 415 5 2 6 3.3 O=C(N[C@H]1CCCC[C@@H]1O)c1cn(Cc2ccc(-n3cccn3)cc2)c2cccnc12 10.1016/j.bmcl.2015.11.053
CHEMBL3745973 137084 None 0 Human Functional pEC50 = 7 7.0 - 1
Positive allosteric modulation of human M1 receptor expressed in CHO cells assessed as acetylcholine-induced calcium mobilization by FLIPR assayPositive allosteric modulation of human M1 receptor expressed in CHO cells assessed as acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 415 5 2 6 3.3 O=C(N[C@H]1CCCC[C@@H]1O)c1cn(Cc2ccc(-n3cccn3)cc2)c2cccnc12 10.1016/j.bmcl.2015.11.053
20918653 116513 None 5 Human Functional pEC50 = 6 6.0 - 1
Positive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assay
ChEMBL 383 4 0 4 4.5 O=c1c2cn(Cc3ccccc3)c3ccccc3c-2nn1Cc1ccccc1F 10.1016/j.bmcl.2014.11.011
CHEMBL3360928 116513 None 5 Human Functional pEC50 = 6 6.0 - 1
Positive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assay
ChEMBL 383 4 0 4 4.5 O=c1c2cn(Cc3ccccc3)c3ccccc3c-2nn1Cc1ccccc1F 10.1016/j.bmcl.2014.11.011
15860348 118525 None 0 Human Functional pEC50 = 7.0 7.0 -4 2
Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.
ChEMBL 283 6 0 6 2.2 CCCCOc1nsnc1OC1CN2CCC1CC2 10.1021/jm970125n
CHEMBL341242 118525 None 0 Human Functional pEC50 = 7.0 7.0 -4 2
Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.
ChEMBL 283 6 0 6 2.2 CCCCOc1nsnc1OC1CN2CCC1CC2 10.1021/jm970125n
162659967 181368 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Positive allosteric modulation of human muscarinic M1 receptor stably expressed in CHO cells assessed as increase in Ach-induced intracellular calcium level preincubated for 10 mins followed by addition of Ach at EC20 concentration by Fluo-8AM dye based FLIPR TETRA methodPositive allosteric modulation of human muscarinic M1 receptor stably expressed in CHO cells assessed as increase in Ach-induced intracellular calcium level preincubated for 10 mins followed by addition of Ach at EC20 concentration by Fluo-8AM dye based FLIPR TETRA method
ChEMBL 434 5 2 6 2.7 Cc1c(Cc2ccc(-c3ccn(C)n3)cc2)cc(C(=O)N[C@H]2CCCC[C@@H]2O)c(=O)n1C 10.1021/acs.jmedchem.6b00544
CHEMBL4761922 181368 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Positive allosteric modulation of human muscarinic M1 receptor stably expressed in CHO cells assessed as increase in Ach-induced intracellular calcium level preincubated for 10 mins followed by addition of Ach at EC20 concentration by Fluo-8AM dye based FLIPR TETRA methodPositive allosteric modulation of human muscarinic M1 receptor stably expressed in CHO cells assessed as increase in Ach-induced intracellular calcium level preincubated for 10 mins followed by addition of Ach at EC20 concentration by Fluo-8AM dye based FLIPR TETRA method
ChEMBL 434 5 2 6 2.7 Cc1c(Cc2ccc(-c3ccn(C)n3)cc2)cc(C(=O)N[C@H]2CCCC[C@@H]2O)c(=O)n1C 10.1021/acs.jmedchem.6b00544
146216751 185429 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL 395 3 0 4 4.7 Cn1cc2cc(-c3cc(F)c(CN4Cc5sccc5C4=O)c(F)c3)ccc2n1 10.1016/j.bmcl.2021.128193
CHEMBL4859577 185429 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL 395 3 0 4 4.7 Cn1cc2cc(-c3cc(F)c(CN4Cc5sccc5C4=O)c(F)c3)ccc2n1 10.1016/j.bmcl.2021.128193
124415421 164748 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Positive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assayPositive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 300 1 1 2 4.3 C[C@@H]1N=C(c2ccccc2)c2cc(Cl)ccc2NC1=S 10.1016/j.bmcl.2017.11.008
CHEMBL4216615 164748 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Positive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assayPositive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 300 1 1 2 4.3 C[C@@H]1N=C(c2ccccc2)c2cc(Cl)ccc2NC1=S 10.1016/j.bmcl.2017.11.008
44579375 193339 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
ChEMBL 438 4 1 4 4.6 Cc1ccccc1CN1CCC(N2CCC(n3c(=O)[nH]c4cc(Cl)ccc43)CC2)CC1 10.1016/j.bmcl.2008.09.023
CHEMBL523657 193339 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
ChEMBL 438 4 1 4 4.6 Cc1ccccc1CN1CCC(N2CCC(n3c(=O)[nH]c4cc(Cl)ccc43)CC2)CC1 10.1016/j.bmcl.2008.09.023
44251558 7224 None 0 Rat Functional pEC50 = 6.0 6.0 1 2
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: PAM Calcium Assay Dose-Response with M1. Measurement of intracellular Ca2+ using Fluo-4 dye in CHO-K1 cells stably transfected with rat M1 (Class of assay: confirmatory) [Related pubchem assays: 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen [Primary Screening])]PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: PAM Calcium Assay Dose-Response with M1. Measurement of intracellular Ca2+ using Fluo-4 dye in CHO-K1 cells stably transfected with rat M1 (Class of assay: confirmatory) [Related pubchem assays: 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen [Primary Screening])]
ChEMBL 371 3 0 4 3.2 Cn1cc(-c2cc(F)c(CN3C(=O)C(=O)c4cccc(F)c43)c(F)c2)cn1 nan
CHEMBL1085686 7224 None 0 Rat Functional pEC50 = 6.0 6.0 1 2
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: PAM Calcium Assay Dose-Response with M1. Measurement of intracellular Ca2+ using Fluo-4 dye in CHO-K1 cells stably transfected with rat M1 (Class of assay: confirmatory) [Related pubchem assays: 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen [Primary Screening])]PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: PAM Calcium Assay Dose-Response with M1. Measurement of intracellular Ca2+ using Fluo-4 dye in CHO-K1 cells stably transfected with rat M1 (Class of assay: confirmatory) [Related pubchem assays: 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen [Primary Screening])]
ChEMBL 371 3 0 4 3.2 Cn1cc(-c2cc(F)c(CN3C(=O)C(=O)c4cccc(F)c43)c(F)c2)cn1 nan
139414093 163639 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Positive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assayPositive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 342 3 1 2 5.5 CCC[C@]1(C)N=C(c2ccccc2)c2cc(Cl)ccc2NC1=S 10.1016/j.bmcl.2017.11.008
CHEMBL4202915 163639 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Positive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assayPositive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 342 3 1 2 5.5 CCC[C@]1(C)N=C(c2ccccc2)c2cc(Cl)ccc2NC1=S 10.1016/j.bmcl.2017.11.008
122190997 123673 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 493 5 3 4 5.0 COc1ccc(N/C(C)=N/c2ccc3c(c2)[C@@H](NC(=O)c2ccc(Br)cc2)[C@H](O)C3)cc1 10.1016/j.bmcl.2015.08.011
CHEMBL3618439 123673 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 493 5 3 4 5.0 COc1ccc(N/C(C)=N/c2ccc3c(c2)[C@@H](NC(=O)c2ccc(Br)cc2)[C@H](O)C3)cc1 10.1016/j.bmcl.2015.08.011
117973690 137084 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Positive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as increase in ACh-induced intracellular calcium level preincubated for 10 mins followed by ACh addition measured every 2 secs for 80 secs by Fluo-4 dye-based FLIPR assayPositive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as increase in ACh-induced intracellular calcium level preincubated for 10 mins followed by ACh addition measured every 2 secs for 80 secs by Fluo-4 dye-based FLIPR assay
ChEMBL 415 5 2 6 3.3 O=C(N[C@H]1CCCC[C@@H]1O)c1cn(Cc2ccc(-n3cccn3)cc2)c2cccnc12 10.1016/j.bmcl.2018.04.054
CHEMBL3745973 137084 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Positive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as increase in ACh-induced intracellular calcium level preincubated for 10 mins followed by ACh addition measured every 2 secs for 80 secs by Fluo-4 dye-based FLIPR assayPositive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as increase in ACh-induced intracellular calcium level preincubated for 10 mins followed by ACh addition measured every 2 secs for 80 secs by Fluo-4 dye-based FLIPR assay
ChEMBL 415 5 2 6 3.3 O=C(N[C@H]1CCCC[C@@H]1O)c1cn(Cc2ccc(-n3cccn3)cc2)c2cccnc12 10.1016/j.bmcl.2018.04.054
44303396 203693 None 0 Human Functional pEC50 = 7.0 7.0 -1 3
Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.
ChEMBL 359 3 0 5 3.1 Clc1ccc(C#CCSc2nsnc2C23CN4CC2C3C4)cc1 10.1021/jm9910019
CHEMBL60374 203693 None 0 Human Functional pEC50 = 7.0 7.0 -1 3
Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.
ChEMBL 359 3 0 5 3.1 Clc1ccc(C#CCSc2nsnc2C23CN4CC2C3C4)cc1 10.1021/jm9910019
145962939 161430 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 445 4 2 5 3.0 O=C(N[C@H]1CCCC[C@@H]1O)C1CN(Cc2ccc(Br)nc2)c2ccccc2O1 10.1016/j.bmcl.2018.05.009
CHEMBL4125749 161430 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 445 4 2 5 3.0 O=C(N[C@H]1CCCC[C@@H]1O)C1CN(Cc2ccc(Br)nc2)c2ccccc2O1 10.1016/j.bmcl.2018.05.009
162475030 180029 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Positive allosteric modulation of recombinant human muscarinic M1 receptor co-expressing pCRE-Luc reporter gene in CHO cells assessed as stimulation of luciferase activity in presence of acetylcholine substrate measured after 4 hrs by luciferase reporter gene assayPositive allosteric modulation of recombinant human muscarinic M1 receptor co-expressing pCRE-Luc reporter gene in CHO cells assessed as stimulation of luciferase activity in presence of acetylcholine substrate measured after 4 hrs by luciferase reporter gene assay
ChEMBL 456 6 2 6 4.0 COc1ccc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCCC[C@H]4O)nn4cccc34)cc2)cn1 10.1021/acsmedchemlett.1c00118
CHEMBL4746155 180029 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Positive allosteric modulation of recombinant human muscarinic M1 receptor co-expressing pCRE-Luc reporter gene in CHO cells assessed as stimulation of luciferase activity in presence of acetylcholine substrate measured after 4 hrs by luciferase reporter gene assayPositive allosteric modulation of recombinant human muscarinic M1 receptor co-expressing pCRE-Luc reporter gene in CHO cells assessed as stimulation of luciferase activity in presence of acetylcholine substrate measured after 4 hrs by luciferase reporter gene assay
ChEMBL 456 6 2 6 4.0 COc1ccc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCCC[C@H]4O)nn4cccc34)cc2)cn1 10.1021/acsmedchemlett.1c00118
118663182 165316 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Positive allosteric modulation of human muscarinic M1 receptor stably expressed in CHO cells assessed as increase in Ach-induced intracellular calcium level preincubated for 10 mins followed by addition of Ach at EC20 concentration by Fluo-8AM dye based FLIPR TETRA methodPositive allosteric modulation of human muscarinic M1 receptor stably expressed in CHO cells assessed as increase in Ach-induced intracellular calcium level preincubated for 10 mins followed by addition of Ach at EC20 concentration by Fluo-8AM dye based FLIPR TETRA method
ChEMBL 392 5 2 6 2.0 Cc1cnc(C(=O)N[C@H]2CCOC[C@@H]2O)cc1Cc1ccc(-n2cccn2)cc1 10.1021/acs.jmedchem.6b00544
CHEMBL4229092 165316 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Positive allosteric modulation of human muscarinic M1 receptor stably expressed in CHO cells assessed as increase in Ach-induced intracellular calcium level preincubated for 10 mins followed by addition of Ach at EC20 concentration by Fluo-8AM dye based FLIPR TETRA methodPositive allosteric modulation of human muscarinic M1 receptor stably expressed in CHO cells assessed as increase in Ach-induced intracellular calcium level preincubated for 10 mins followed by addition of Ach at EC20 concentration by Fluo-8AM dye based FLIPR TETRA method
ChEMBL 392 5 2 6 2.0 Cc1cnc(C(=O)N[C@H]2CCOC[C@@H]2O)cc1Cc1ccc(-n2cccn2)cc1 10.1021/acs.jmedchem.6b00544
122186859 123041 None 0 Human Functional pEC50 = 8.0 8.0 1 2
Positive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as basal and acetylcholine-stimulated Ca2+ level by FLIPR assayPositive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as basal and acetylcholine-stimulated Ca2+ level by FLIPR assay
ChEMBL 431 5 2 7 2.4 Cn1cc(-c2ccc(Cn3cc(C(=O)N[C@H]4COCC[C@@H]4O)c4ncccc43)cc2)cn1 10.1021/acsmedchemlett.5b00185
CHEMBL3608419 123041 None 0 Human Functional pEC50 = 8.0 8.0 1 2
Positive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as basal and acetylcholine-stimulated Ca2+ level by FLIPR assayPositive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as basal and acetylcholine-stimulated Ca2+ level by FLIPR assay
ChEMBL 431 5 2 7 2.4 Cn1cc(-c2ccc(Cn3cc(C(=O)N[C@H]4COCC[C@@H]4O)c4ncccc43)cc2)cn1 10.1021/acsmedchemlett.5b00185
62707610 76381 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
ChEMBL 404 5 1 4 3.3 O=C1CCc2ccccc2N1CCCN1CCC(n2c(=O)[nH]c3ccccc32)CC1 10.1016/j.bmcl.2012.05.048
CHEMBL2059306 76381 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
ChEMBL 404 5 1 4 3.3 O=C1CCc2ccccc2N1CCCN1CCC(n2c(=O)[nH]c3ccccc32)CC1 10.1016/j.bmcl.2012.05.048
62705509 76398 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
ChEMBL 424 5 1 5 2.9 O=C1COc2ccccc2N1CCCN1CCC(n2c(=O)[nH]c3c(F)cccc32)CC1 10.1016/j.bmcl.2012.05.048
CHEMBL2059324 76398 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
ChEMBL 424 5 1 5 2.9 O=C1COc2ccccc2N1CCCN1CCC(n2c(=O)[nH]c3c(F)cccc32)CC1 10.1016/j.bmcl.2012.05.048
53303986 74366 None 0 Human Functional pEC50 = 7.0 7.0 20 3
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
ChEMBL 345 6 2 4 2.2 CCOC(=O)N1[C@H]2CC[C@@H]1C[C@H](NCCNC(=O)c1ccccc1)C2 10.1016/j.bmcl.2012.03.088
CHEMBL2024407 74366 None 0 Human Functional pEC50 = 7.0 7.0 20 3
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
ChEMBL 345 6 2 4 2.2 CCOC(=O)N1[C@H]2CC[C@@H]1C[C@H](NCCNC(=O)c1ccccc1)C2 10.1016/j.bmcl.2012.03.088
44207908 16741 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 357 6 1 4 1.8 O=C(NC1CCN(CCCN2C(=O)COc3ccccc32)CC1)C1CC1 10.1021/jm100697g
CHEMBL1243267 16741 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 357 6 1 4 1.8 O=C(NC1CCN(CCCN2C(=O)COc3ccccc32)CC1)C1CC1 10.1021/jm100697g
57391102 68276 None 5 Rat Functional pEC50 = 7.0 7.0 2 2
Agonist activity at rat muscarinic M1 receptor expressed in CHO cellsAgonist activity at rat muscarinic M1 receptor expressed in CHO cells
ChEMBL 373 4 1 4 2.8 CCOC(=O)N1CCC(N2CCC[C@@H](NC(=O)c3ccccc3C)C2)CC1 10.1016/j.bmcl.2011.08.084
CHEMBL1916224 68276 None 5 Rat Functional pEC50 = 7.0 7.0 2 2
Agonist activity at rat muscarinic M1 receptor expressed in CHO cellsAgonist activity at rat muscarinic M1 receptor expressed in CHO cells
ChEMBL 373 4 1 4 2.8 CCOC(=O)N1CCC(N2CCC[C@@H](NC(=O)c3ccccc3C)C2)CC1 10.1016/j.bmcl.2011.08.084
44209166 59575 None 0 Rat Functional pEC50 = 7.0 7.0 -7 2
Compound was tested in vitro for depolarizing response on the rat superior cervical ganglion (mediated by muscarinic acetylcholine receptor M1)Compound was tested in vitro for depolarizing response on the rat superior cervical ganglion (mediated by muscarinic acetylcholine receptor M1)
ChEMBL 193 1 0 4 1.0 Cc1noc(C2(C)CN3CCC2C3)n1 10.1021/jm00083a016
CHEMBL171721 59575 None 0 Rat Functional pEC50 = 7.0 7.0 -7 2
Compound was tested in vitro for depolarizing response on the rat superior cervical ganglion (mediated by muscarinic acetylcholine receptor M1)Compound was tested in vitro for depolarizing response on the rat superior cervical ganglion (mediated by muscarinic acetylcholine receptor M1)
ChEMBL 193 1 0 4 1.0 Cc1noc(C2(C)CN3CCC2C3)n1 10.1021/jm00083a016
46872059 68278 None 0 Rat Functional pEC50 = 7.0 7.0 - 1
Partial agonist activity at rat muscarinic M1 receptor expressed in CHO cells calcium responsePartial agonist activity at rat muscarinic M1 receptor expressed in CHO cells calcium response
ChEMBL 359 4 1 4 2.5 CCOC(=O)N1CCC(N2CCC[C@@H](NC(=O)c3ccccc3)C2)CC1 10.1016/j.bmcl.2012.10.132
CHEMBL1916226 68278 None 0 Rat Functional pEC50 = 7.0 7.0 - 1
Partial agonist activity at rat muscarinic M1 receptor expressed in CHO cells calcium responsePartial agonist activity at rat muscarinic M1 receptor expressed in CHO cells calcium response
ChEMBL 359 4 1 4 2.5 CCOC(=O)N1CCC(N2CCC[C@@H](NC(=O)c3ccccc3)C2)CC1 10.1016/j.bmcl.2012.10.132
10686494 100592 None 0 Human Functional pEC50 = 7.0 7.0 -14 3
Stimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptorStimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptor
ChEMBL 311 3 0 5 2.7 CN1CCC=C(c2nsnc2OCC#Cc2ccccc2)C1 10.1016/s0960-894x(98)00509-5
CHEMBL291351 100592 None 0 Human Functional pEC50 = 7.0 7.0 -14 3
Stimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptorStimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptor
ChEMBL 311 3 0 5 2.7 CN1CCC=C(c2nsnc2OCC#Cc2ccccc2)C1 10.1016/s0960-894x(98)00509-5
44303408 204403 None 0 Human Functional pEC50 = 7.0 7.0 -1 3
Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.
ChEMBL 361 3 0 5 2.6 Fc1cc(Cl)cc(C#CCOc2nsnc2C23CN4CC2C3C4)c1 10.1021/jm9910019
CHEMBL60777 204403 None 0 Human Functional pEC50 = 7.0 7.0 -1 3
Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.
ChEMBL 361 3 0 5 2.6 Fc1cc(Cl)cc(C#CCOc2nsnc2C23CN4CC2C3C4)c1 10.1021/jm9910019
10686494 100592 None 0 Human Functional pEC50 = 7.0 7.0 -14 3
Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.
ChEMBL 311 3 0 5 2.7 CN1CCC=C(c2nsnc2OCC#Cc2ccccc2)C1 10.1021/jm9910019
CHEMBL291351 100592 None 0 Human Functional pEC50 = 7.0 7.0 -14 3
Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.
ChEMBL 311 3 0 5 2.7 CN1CCC=C(c2nsnc2OCC#Cc2ccccc2)C1 10.1021/jm9910019
70685678 74370 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
ChEMBL 359 6 2 4 2.5 CCOC(=O)N1[C@H]2CC[C@@H]1C[C@@H](NCCNC(=O)c1ccccc1C)C2 10.1016/j.bmcl.2012.03.088
CHEMBL2024418 74370 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
ChEMBL 359 6 2 4 2.5 CCOC(=O)N1[C@H]2CC[C@@H]1C[C@@H](NCCNC(=O)c1ccccc1C)C2 10.1016/j.bmcl.2012.03.088
46930074 16727 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 393 7 1 5 2.8 O=C(Cc1ccccc1)NC1CCN(CCCn2c(=O)oc3ccccc32)CC1 10.1021/jm100697g
CHEMBL1243139 16727 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 393 7 1 5 2.8 O=C(Cc1ccccc1)NC1CCN(CCCn2c(=O)oc3ccccc32)CC1 10.1021/jm100697g
44578977 189700 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
ChEMBL 469 5 1 6 4.2 O=c1[nH]c2cc(Cl)ccc2n1C1CCN(C2CCN(Cc3ccccc3[N+](=O)[O-])CC2)CC1 10.1016/j.bmcl.2008.09.023
CHEMBL514689 189700 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
ChEMBL 469 5 1 6 4.2 O=c1[nH]c2cc(Cl)ccc2n1C1CCN(C2CCN(Cc3ccccc3[N+](=O)[O-])CC2)CC1 10.1016/j.bmcl.2008.09.023
44251558 7224 None 0 Human Functional pEC50 = 6.0 6.0 -1 2
Potentiation of muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assayPotentiation of muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 371 3 0 4 3.2 Cn1cc(-c2cc(F)c(CN3C(=O)C(=O)c4cccc(F)c43)c(F)c2)cn1 10.1016/j.bmcl.2010.01.109
CHEMBL1085686 7224 None 0 Human Functional pEC50 = 6.0 6.0 -1 2
Potentiation of muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assayPotentiation of muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 371 3 0 4 3.2 Cn1cc(-c2cc(F)c(CN3C(=O)C(=O)c4cccc(F)c43)c(F)c2)cn1 10.1016/j.bmcl.2010.01.109
44589500 192687 None 0 Human Functional pEC50 = 5.0 5.0 - 1
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
ChEMBL 506 3 1 4 4.9 O=C(c1ccccc1C(F)(F)F)N1CCC(N2CCC(n3c(=O)[nH]c4cc(Cl)ccc43)CC2)CC1 10.1016/j.bmcl.2008.09.032
CHEMBL521388 192687 None 0 Human Functional pEC50 = 5.0 5.0 - 1
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
ChEMBL 506 3 1 4 4.9 O=C(c1ccccc1C(F)(F)F)N1CCC(N2CCC(n3c(=O)[nH]c4cc(Cl)ccc43)CC2)CC1 10.1016/j.bmcl.2008.09.032
127038325 137121 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Positive allosteric modulation of human M1 receptor expressed in CHO cells assessed as acetylcholine-induced calcium mobilization by FLIPR assayPositive allosteric modulation of human M1 receptor expressed in CHO cells assessed as acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 402 6 1 6 2.1 CN(C)C(=O)CNC(=O)c1cn(Cc2ccc(-n3cccn3)cc2)c2cccnc12 10.1016/j.bmcl.2015.11.053
CHEMBL3746514 137121 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Positive allosteric modulation of human M1 receptor expressed in CHO cells assessed as acetylcholine-induced calcium mobilization by FLIPR assayPositive allosteric modulation of human M1 receptor expressed in CHO cells assessed as acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 402 6 1 6 2.1 CN(C)C(=O)CNC(=O)c1cn(Cc2ccc(-n3cccn3)cc2)c2cccnc12 10.1016/j.bmcl.2015.11.053
146216735 186416 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL 463 5 0 6 4.1 Cn1cc2c(-c3cc(F)c(CN4Cc5cnn(CC6CCCO6)c5C4=O)c(F)c3)cccc2n1 10.1016/j.bmcl.2021.128193
CHEMBL4874580 186416 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL 463 5 0 6 4.1 Cn1cc2c(-c3cc(F)c(CN4Cc5cnn(CC6CCCO6)c5C4=O)c(F)c3)cccc2n1 10.1016/j.bmcl.2021.128193
118724608 116524 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assay
ChEMBL 459 5 0 6 5.2 Cc1ccc(Cn2nc3c4ccccc4n(Cc4ccc(-n5cccn5)cc4)cc-3c2=O)c(C)c1 10.1016/j.bmcl.2014.11.011
CHEMBL3360950 116524 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assay
ChEMBL 459 5 0 6 5.2 Cc1ccc(Cn2nc3c4ccccc4n(Cc4ccc(-n5cccn5)cc4)cc-3c2=O)c(C)c1 10.1016/j.bmcl.2014.11.011
162655325 180837 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Positive allosteric modulation of human muscarinic M1 receptor stably expressed in CHO cells assessed as increase in Ach-induced intracellular calcium level preincubated for 10 mins followed by addition of Ach at EC20 concentration by Fluo-8AM dye based FLIPR TETRA methodPositive allosteric modulation of human muscarinic M1 receptor stably expressed in CHO cells assessed as increase in Ach-induced intracellular calcium level preincubated for 10 mins followed by addition of Ach at EC20 concentration by Fluo-8AM dye based FLIPR TETRA method
ChEMBL 409 5 2 5 2.8 Cc1cc(F)c(C(=O)N[C@H]2CCOC[C@@H]2O)cc1Cc1ccc(-n2cccn2)cc1 10.1021/acs.jmedchem.6b00544
CHEMBL4755820 180837 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Positive allosteric modulation of human muscarinic M1 receptor stably expressed in CHO cells assessed as increase in Ach-induced intracellular calcium level preincubated for 10 mins followed by addition of Ach at EC20 concentration by Fluo-8AM dye based FLIPR TETRA methodPositive allosteric modulation of human muscarinic M1 receptor stably expressed in CHO cells assessed as increase in Ach-induced intracellular calcium level preincubated for 10 mins followed by addition of Ach at EC20 concentration by Fluo-8AM dye based FLIPR TETRA method
ChEMBL 409 5 2 5 2.8 Cc1cc(F)c(C(=O)N[C@H]2CCOC[C@@H]2O)cc1Cc1ccc(-n2cccn2)cc1 10.1021/acs.jmedchem.6b00544
118724608 116524 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assay
ChEMBL 459 5 0 6 5.2 Cc1ccc(Cn2nc3c4ccccc4n(Cc4ccc(-n5cccn5)cc4)cc-3c2=O)c(C)c1 10.1016/j.bmcl.2014.11.011
CHEMBL3360950 116524 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assay
ChEMBL 459 5 0 6 5.2 Cc1ccc(Cn2nc3c4ccccc4n(Cc4ccc(-n5cccn5)cc4)cc-3c2=O)c(C)c1 10.1016/j.bmcl.2014.11.011
126492039 161479 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 418 5 2 6 2.7 O=C(N[C@H]1CCC[C@@H]1O)C1CN(Cc2ccc(-n3cccn3)cc2)c2ccccc2O1 10.1016/j.bmcl.2018.05.009
CHEMBL4126348 161479 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 418 5 2 6 2.7 O=C(N[C@H]1CCC[C@@H]1O)C1CN(Cc2ccc(-n3cccn3)cc2)c2ccccc2O1 10.1016/j.bmcl.2018.05.009
122190995 123672 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 495 4 2 3 5.2 C/C(=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(Br)cc1)[C@H](O)C2)N(C)c1ccc(F)cc1 10.1016/j.bmcl.2015.08.011
CHEMBL3618437 123672 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 495 4 2 3 5.2 C/C(=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(Br)cc1)[C@H](O)C2)N(C)c1ccc(F)cc1 10.1016/j.bmcl.2015.08.011
62705172 76382 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
ChEMBL 405 5 1 5 2.7 O=C1CCc2ncccc2N1CCCN1CCC(n2c(=O)[nH]c3ccccc32)CC1 10.1016/j.bmcl.2012.05.048
CHEMBL2059307 76382 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
ChEMBL 405 5 1 5 2.7 O=C1CCc2ncccc2N1CCCN1CCC(n2c(=O)[nH]c3ccccc32)CC1 10.1016/j.bmcl.2012.05.048
71719475 87621 None 0 Human Functional pEC50 = 7.9 7.9 2 2
Partial agonist activity at human M1 receptor in CHO cells assessed as calcium mobilization after 60 mins by FLIPR assayPartial agonist activity at human M1 receptor in CHO cells assessed as calcium mobilization after 60 mins by FLIPR assay
ChEMBL 397 4 0 4 3.1 CCOC(=O)N1[C@H]2CC[C@@H]1C[C@@H](CN1CC[C@H](N3C(=O)Cc4ccccc43)C1)C2 10.1021/ml300372f
CHEMBL2336059 87621 None 0 Human Functional pEC50 = 7.9 7.9 2 2
Partial agonist activity at human M1 receptor in CHO cells assessed as calcium mobilization after 60 mins by FLIPR assayPartial agonist activity at human M1 receptor in CHO cells assessed as calcium mobilization after 60 mins by FLIPR assay
ChEMBL 397 4 0 4 3.1 CCOC(=O)N1[C@H]2CC[C@@H]1C[C@@H](CN1CC[C@H](N3C(=O)Cc4ccccc43)C1)C2 10.1021/ml300372f
145969354 165280 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Positive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as increase in ACh-induced intracellular calcium level preincubated for 10 mins followed by ACh addition measured every 2 secs for 80 secs by Fluo-4 dye-based FLIPR assayPositive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as increase in ACh-induced intracellular calcium level preincubated for 10 mins followed by ACh addition measured every 2 secs for 80 secs by Fluo-4 dye-based FLIPR assay
ChEMBL 422 5 4 6 1.5 Cc1[nH]c(=O)c(C(=O)N[C@H]2CC(O)CC[C@@H]2O)cc1Cc1ccc(-n2cccn2)cc1 10.1016/j.bmcl.2018.04.054
CHEMBL4228557 165280 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Positive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as increase in ACh-induced intracellular calcium level preincubated for 10 mins followed by ACh addition measured every 2 secs for 80 secs by Fluo-4 dye-based FLIPR assayPositive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as increase in ACh-induced intracellular calcium level preincubated for 10 mins followed by ACh addition measured every 2 secs for 80 secs by Fluo-4 dye-based FLIPR assay
ChEMBL 422 5 4 6 1.5 Cc1[nH]c(=O)c(C(=O)N[C@H]2CC(O)CC[C@@H]2O)cc1Cc1ccc(-n2cccn2)cc1 10.1016/j.bmcl.2018.04.054
46890977 6734 None 0 Human Functional pEC50 = 7.9 7.9 19 5
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 342 4 2 2 4.0 Cc1ccc(-c2ccccc2C(=O)NCC2CCNCC2)cc1Cl 10.1016/j.bmcl.2010.04.128
CHEMBL1083723 6734 None 0 Human Functional pEC50 = 7.9 7.9 19 5
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 342 4 2 2 4.0 Cc1ccc(-c2ccccc2C(=O)NCC2CCNCC2)cc1Cl 10.1016/j.bmcl.2010.04.128
42598359 16113 None 0 Human Functional pEC50 = 7.9 7.9 100 5
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 436 5 0 7 3.4 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(S(C)(=O)=O)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223864 16113 None 0 Human Functional pEC50 = 7.9 7.9 100 5
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 436 5 0 7 3.4 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(S(C)(=O)=O)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
44253016 80488 None 1 Human Functional pEC50 = 7.9 7.9 1 4
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assay
ChEMBL 299 2 1 3 3.3 O=c1[nH]c2ccccc2n1C1CCN(C2CCCCC2)CC1 10.1021/ml100105x
CHEMBL2146597 80488 None 1 Human Functional pEC50 = 7.9 7.9 1 4
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assay
ChEMBL 299 2 1 3 3.3 O=c1[nH]c2ccccc2n1C1CCN(C2CCCCC2)CC1 10.1021/ml100105x
46930073 16724 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 435 8 1 4 3.2 COc1ccc2c(c1)N(CCCN1CCC(NC(=O)Cc3ccccc3)CC1)C(=O)CC2 10.1021/jm100697g
CHEMBL1243109 16724 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 435 8 1 4 3.2 COc1ccc2c(c1)N(CCCN1CCC(NC(=O)Cc3ccccc3)CC1)C(=O)CC2 10.1021/jm100697g
44578976 182086 None 0 Human Functional pEC50 = 6.9 6.9 9 2
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
ChEMBL 435 5 1 6 3.5 O=c1[nH]c2ccccc2n1C1CCN(C2CCN(Cc3ccccc3[N+](=O)[O-])CC2)CC1 10.1016/j.bmcl.2008.09.023
CHEMBL478034 182086 None 0 Human Functional pEC50 = 6.9 6.9 9 2
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
ChEMBL 435 5 1 6 3.5 O=c1[nH]c2ccccc2n1C1CCN(C2CCN(Cc3ccccc3[N+](=O)[O-])CC2)CC1 10.1016/j.bmcl.2008.09.023
11734822 116699 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.
ChEMBL 550 14 0 10 6.4 CN1CCC=C(c2nsnc2SCCCCCCCCCSc2nsnc2C2=CCCN(C)C2)C1 10.1021/jm0102405
CHEMBL336933 116699 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.
ChEMBL 550 14 0 10 6.4 CN1CCC=C(c2nsnc2SCCCCCCCCCSc2nsnc2C2=CCCN(C)C2)C1 10.1021/jm0102405
145985917 165594 None 0 Human Functional pEC50 = 6.9 6.9 2 2
Positive allosteric modulation of human M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assayPositive allosteric modulation of human M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assay
ChEMBL 444 5 2 7 3.0 Cn1ccc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCCC[C@H]4O)nc4c3ccn4C)cn2)n1 10.1021/acsmedchemlett.8b00261
CHEMBL4240517 165594 None 0 Human Functional pEC50 = 6.9 6.9 2 2
Positive allosteric modulation of human M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assayPositive allosteric modulation of human M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assay
ChEMBL 444 5 2 7 3.0 Cn1ccc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCCC[C@H]4O)nc4c3ccn4C)cn2)n1 10.1021/acsmedchemlett.8b00261
62705331 76388 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
ChEMBL 407 5 1 6 2.2 O=C1COc2ccccc2N1CCCN1CCC(n2c(=O)[nH]c3ccncc32)CC1 10.1016/j.bmcl.2012.05.048
CHEMBL2059314 76388 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
ChEMBL 407 5 1 6 2.2 O=C1COc2ccccc2N1CCCN1CCC(n2c(=O)[nH]c3ccncc32)CC1 10.1016/j.bmcl.2012.05.048
70685670 74337 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
ChEMBL 359 5 1 4 2.4 CCOC(=O)N1CC[C@H]2[C@H](CCCN2CCNC(=O)c2ccccc2)C1 10.1016/j.bmcl.2012.03.088
CHEMBL2024328 74337 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
ChEMBL 359 5 1 4 2.4 CCOC(=O)N1CC[C@H]2[C@H](CCCN2CCNC(=O)c2ccccc2)C1 10.1016/j.bmcl.2012.03.088
70685676 74362 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
ChEMBL 371 4 1 4 2.6 CCOC(=O)N1C2CCC1CC(N1CC[C@H](NC(=O)c3ccccc3)C1)C2 10.1016/j.bmcl.2012.03.088
CHEMBL2024403 74362 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
ChEMBL 371 4 1 4 2.6 CCOC(=O)N1C2CCC1CC(N1CC[C@H](NC(=O)c3ccccc3)C1)C2 10.1016/j.bmcl.2012.03.088
53385831 74363 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
ChEMBL 385 4 1 4 3.0 CCOC(=O)N1C2CCC1CC(N1CC[C@@H](NC(=O)c3ccccc3C)C1)C2 10.1016/j.bmcl.2012.03.088
CHEMBL2024404 74363 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
ChEMBL 385 4 1 4 3.0 CCOC(=O)N1C2CCC1CC(N1CC[C@@H](NC(=O)c3ccccc3C)C1)C2 10.1016/j.bmcl.2012.03.088
53303986 74367 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human muscarinic M1 receptor by calcium mobilization assayAgonist activity at human muscarinic M1 receptor by calcium mobilization assay
ChEMBL 345 6 2 4 2.2 CCOC(=O)N1[C@H]2CC[C@@H]1C[C@@H](NCCNC(=O)c1ccccc1)C2 10.1016/j.bmcl.2012.03.088
CHEMBL2024408 74367 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human muscarinic M1 receptor by calcium mobilization assayAgonist activity at human muscarinic M1 receptor by calcium mobilization assay
ChEMBL 345 6 2 4 2.2 CCOC(=O)N1[C@H]2CC[C@@H]1C[C@@H](NCCNC(=O)c1ccccc1)C2 10.1016/j.bmcl.2012.03.088
145962939 161430 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 445 4 2 5 3.0 O=C(N[C@H]1CCCC[C@@H]1O)C1CN(Cc2ccc(Br)nc2)c2ccccc2O1 10.1016/j.bmcl.2018.05.009
CHEMBL4125749 161430 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 445 4 2 5 3.0 O=C(N[C@H]1CCCC[C@@H]1O)C1CN(Cc2ccc(Br)nc2)c2ccccc2O1 10.1016/j.bmcl.2018.05.009
126492039 161479 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 418 5 2 6 2.7 O=C(N[C@H]1CCC[C@@H]1O)C1CN(Cc2ccc(-n3cccn3)cc2)c2ccccc2O1 10.1016/j.bmcl.2018.05.009
CHEMBL4126348 161479 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 418 5 2 6 2.7 O=C(N[C@H]1CCC[C@@H]1O)C1CN(Cc2ccc(-n3cccn3)cc2)c2ccccc2O1 10.1016/j.bmcl.2018.05.009
44251559 7062 None 0 Human Functional pEC50 = 5.9 5.9 1 2
Potentiation of muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assayPotentiation of muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 371 3 0 4 3.2 Cn1cc(-c2ccc(CN3C(=O)C(=O)c4c(F)ccc(F)c43)c(F)c2)cn1 10.1016/j.bmcl.2010.01.109
CHEMBL1084940 7062 None 0 Human Functional pEC50 = 5.9 5.9 1 2
Potentiation of muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assayPotentiation of muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 371 3 0 4 3.2 Cn1cc(-c2ccc(CN3C(=O)C(=O)c4c(F)ccc(F)c43)c(F)c2)cn1 10.1016/j.bmcl.2010.01.109
44303424 202943 None 0 Human Functional pEC50 = 5.9 5.9 1 2
Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.
ChEMBL 376 3 0 4 4.6 Clc1cc(Cl)cc(C#CCOc2nsnc2C23CC4CC2C3C4)c1 10.1021/jm9910019
CHEMBL59862 202943 None 0 Human Functional pEC50 = 5.9 5.9 1 2
Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.
ChEMBL 376 3 0 4 4.6 Clc1cc(Cl)cc(C#CCOc2nsnc2C23CC4CC2C3C4)c1 10.1021/jm9910019
145983485 165576 None 0 Rat Functional pEC50 = 5.9 5.9 - 1
Agonist activity at rat M1 receptor expressed in CHO cells assessed as increase in calcium mobilization measured after 2.5 mins by Fluo-4-AM dye based assayAgonist activity at rat M1 receptor expressed in CHO cells assessed as increase in calcium mobilization measured after 2.5 mins by Fluo-4-AM dye based assay
ChEMBL 444 5 2 7 3.0 Cn1cc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCCC[C@H]4O)nc4c3ccn4C)cn2)cn1 10.1021/acsmedchemlett.8b00261
CHEMBL4240041 165576 None 0 Rat Functional pEC50 = 5.9 5.9 - 1
Agonist activity at rat M1 receptor expressed in CHO cells assessed as increase in calcium mobilization measured after 2.5 mins by Fluo-4-AM dye based assayAgonist activity at rat M1 receptor expressed in CHO cells assessed as increase in calcium mobilization measured after 2.5 mins by Fluo-4-AM dye based assay
ChEMBL 444 5 2 7 3.0 Cn1cc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCCC[C@H]4O)nc4c3ccn4C)cn2)cn1 10.1021/acsmedchemlett.8b00261
145983485 165576 None 0 Rat Functional pEC50 = 5.9 5.9 - 1
Agonist activity at rat M1 receptor expressed in CHO cells assessed as increase in calcium mobilization measured after 2.5 mins by Fluo-4-AM dye based assayAgonist activity at rat M1 receptor expressed in CHO cells assessed as increase in calcium mobilization measured after 2.5 mins by Fluo-4-AM dye based assay
ChEMBL 444 5 2 7 3.0 Cn1cc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCCC[C@H]4O)nc4c3ccn4C)cn2)cn1 10.1021/acsmedchemlett.8b00261
CHEMBL4240041 165576 None 0 Rat Functional pEC50 = 5.9 5.9 - 1
Agonist activity at rat M1 receptor expressed in CHO cells assessed as increase in calcium mobilization measured after 2.5 mins by Fluo-4-AM dye based assayAgonist activity at rat M1 receptor expressed in CHO cells assessed as increase in calcium mobilization measured after 2.5 mins by Fluo-4-AM dye based assay
ChEMBL 444 5 2 7 3.0 Cn1cc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCCC[C@H]4O)nc4c3ccn4C)cn2)cn1 10.1021/acsmedchemlett.8b00261
145985917 165594 None 0 Human Functional pEC50 = 6.9 6.9 2 2
Agonist activity at human M1 receptor expressed in CHO cells assessed as increase in calcium mobilization measured after 2.5 mins by Fluo-4-AM dye based assayAgonist activity at human M1 receptor expressed in CHO cells assessed as increase in calcium mobilization measured after 2.5 mins by Fluo-4-AM dye based assay
ChEMBL 444 5 2 7 3.0 Cn1ccc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCCC[C@H]4O)nc4c3ccn4C)cn2)n1 10.1021/acsmedchemlett.8b00261
CHEMBL4240517 165594 None 0 Human Functional pEC50 = 6.9 6.9 2 2
Agonist activity at human M1 receptor expressed in CHO cells assessed as increase in calcium mobilization measured after 2.5 mins by Fluo-4-AM dye based assayAgonist activity at human M1 receptor expressed in CHO cells assessed as increase in calcium mobilization measured after 2.5 mins by Fluo-4-AM dye based assay
ChEMBL 444 5 2 7 3.0 Cn1ccc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCCC[C@H]4O)nc4c3ccn4C)cn2)n1 10.1021/acsmedchemlett.8b00261
44251559 7062 None 0 Rat Functional pEC50 = 5.9 5.9 -1 2
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: PAM Calcium Assay Dose-Response with M1. Measurement of intracellular Ca2+ using Fluo-4 dye in CHO-K1 cells stably transfected with rat M1 (Class of assay: confirmatory) [Related pubchem assays: 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen [Primary Screening])]PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: PAM Calcium Assay Dose-Response with M1. Measurement of intracellular Ca2+ using Fluo-4 dye in CHO-K1 cells stably transfected with rat M1 (Class of assay: confirmatory) [Related pubchem assays: 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen [Primary Screening])]
ChEMBL 371 3 0 4 3.2 Cn1cc(-c2ccc(CN3C(=O)C(=O)c4c(F)ccc(F)c43)c(F)c2)cn1 nan
CHEMBL1084940 7062 None 0 Rat Functional pEC50 = 5.9 5.9 -1 2
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: PAM Calcium Assay Dose-Response with M1. Measurement of intracellular Ca2+ using Fluo-4 dye in CHO-K1 cells stably transfected with rat M1 (Class of assay: confirmatory) [Related pubchem assays: 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen [Primary Screening])]PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: PAM Calcium Assay Dose-Response with M1. Measurement of intracellular Ca2+ using Fluo-4 dye in CHO-K1 cells stably transfected with rat M1 (Class of assay: confirmatory) [Related pubchem assays: 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen [Primary Screening])]
ChEMBL 371 3 0 4 3.2 Cn1cc(-c2ccc(CN3C(=O)C(=O)c4c(F)ccc(F)c43)c(F)c2)cn1 nan
145961455 161483 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 447 5 2 7 2.7 Cn1nccc1-c1ccc(CN2CC(C(=O)N[C@H]3CCCC[C@@H]3O)Oc3ccccc32)cn1 10.1016/j.bmcl.2018.05.009
CHEMBL4126400 161483 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 447 5 2 7 2.7 Cn1nccc1-c1ccc(CN2CC(C(=O)N[C@H]3CCCC[C@@H]3O)Oc3ccccc32)cn1 10.1016/j.bmcl.2018.05.009
71540044 86392 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulator activity at human muscarinic M1 receptor by calcium mobilization assayPositive allosteric modulator activity at human muscarinic M1 receptor by calcium mobilization assay
ChEMBL 336 3 1 4 2.8 Cn1cc(-c2ccc(CN3C(=O)C(N)c4ccccc43)c(F)c2)cn1 10.1016/j.bmcl.2012.11.092
CHEMBL2313530 86392 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulator activity at human muscarinic M1 receptor by calcium mobilization assayPositive allosteric modulator activity at human muscarinic M1 receptor by calcium mobilization assay
ChEMBL 336 3 1 4 2.8 Cn1cc(-c2ccc(CN3C(=O)C(N)c4ccccc43)c(F)c2)cn1 10.1016/j.bmcl.2012.11.092
1476756 204446 None 50 Human Functional pEC50 = 6.9 6.9 - 1
Allosteric modulation of human muscarinic M1 acetylcholine receptor expressed CHO cells assessed as intracellular calcium mobilization after 1 hr by Fluo-4-AM based fluorescence assayAllosteric modulation of human muscarinic M1 acetylcholine receptor expressed CHO cells assessed as intracellular calcium mobilization after 1 hr by Fluo-4-AM based fluorescence assay
ChEMBL 309 4 1 4 2.8 COc1ccc(Cn2cc(C(=O)O)c(=O)c3ccccc32)cc1 10.1021/jm400540b
CHEMBL608112 204446 None 50 Human Functional pEC50 = 6.9 6.9 - 1
Allosteric modulation of human muscarinic M1 acetylcholine receptor expressed CHO cells assessed as intracellular calcium mobilization after 1 hr by Fluo-4-AM based fluorescence assayAllosteric modulation of human muscarinic M1 acetylcholine receptor expressed CHO cells assessed as intracellular calcium mobilization after 1 hr by Fluo-4-AM based fluorescence assay
ChEMBL 309 4 1 4 2.8 COc1ccc(Cn2cc(C(=O)O)c(=O)c3ccccc32)cc1 10.1021/jm400540b
44208359 16712 None 0 Human Functional pEC50 = 7.9 7.9 23 3
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 501 9 1 5 3.5 COc1ccc(CC(=O)NC2CCN(CCCN3C(=O)CCc4cc(F)c(F)cc43)CC2)cc1OC 10.1021/jm100697g
CHEMBL1242979 16712 None 0 Human Functional pEC50 = 7.9 7.9 23 3
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 501 9 1 5 3.5 COc1ccc(CC(=O)NC2CCN(CCCN3C(=O)CCc4cc(F)c(F)cc43)CC2)cc1OC 10.1021/jm100697g
145984808 165879 None 0 Rat Functional pEC50 = 7.9 7.9 - 1
Positive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assayPositive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assay
ChEMBL 446 5 2 8 1.8 Cn1ccc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCOC[C@H]4O)nc4c3ccn4C)cn2)n1 10.1021/acsmedchemlett.8b00261
CHEMBL4247625 165879 None 0 Rat Functional pEC50 = 7.9 7.9 - 1
Positive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assayPositive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assay
ChEMBL 446 5 2 8 1.8 Cn1ccc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCOC[C@H]4O)nc4c3ccn4C)cn2)n1 10.1021/acsmedchemlett.8b00261
122186859 123041 None 0 Rat Functional pEC50 = 7.9 7.9 -1 2
Positive allosteric modulation of rat muscarinic M1 receptor expressed in CHO cells assessed as basal and acetylcholine-stimulated Ca2+ level by FLIPR assayPositive allosteric modulation of rat muscarinic M1 receptor expressed in CHO cells assessed as basal and acetylcholine-stimulated Ca2+ level by FLIPR assay
ChEMBL 431 5 2 7 2.4 Cn1cc(-c2ccc(Cn3cc(C(=O)N[C@H]4COCC[C@@H]4O)c4ncccc43)cc2)cn1 10.1021/acsmedchemlett.5b00185
CHEMBL3608419 123041 None 0 Rat Functional pEC50 = 7.9 7.9 -1 2
Positive allosteric modulation of rat muscarinic M1 receptor expressed in CHO cells assessed as basal and acetylcholine-stimulated Ca2+ level by FLIPR assayPositive allosteric modulation of rat muscarinic M1 receptor expressed in CHO cells assessed as basal and acetylcholine-stimulated Ca2+ level by FLIPR assay
ChEMBL 431 5 2 7 2.4 Cn1cc(-c2ccc(Cn3cc(C(=O)N[C@H]4COCC[C@@H]4O)c4ncccc43)cc2)cn1 10.1021/acsmedchemlett.5b00185
44206730 16714 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 437 8 1 5 2.6 COc1cccc(CC(=O)NC2CCN(CCCN3C(=O)COc4ccccc43)CC2)c1 10.1021/jm100697g
CHEMBL1243010 16714 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 437 8 1 5 2.6 COc1cccc(CC(=O)NC2CCN(CCCN3C(=O)COc4ccccc43)CC2)c1 10.1021/jm100697g
46872059 68278 None 0 Rat Functional pEC50 = 6.9 6.9 - 1
Agonist activity at rat muscarinic M1 receptor expressed in CHO cellsAgonist activity at rat muscarinic M1 receptor expressed in CHO cells
ChEMBL 359 4 1 4 2.5 CCOC(=O)N1CCC(N2CCC[C@@H](NC(=O)c3ccccc3)C2)CC1 10.1016/j.bmcl.2011.08.084
CHEMBL1916226 68278 None 0 Rat Functional pEC50 = 6.9 6.9 - 1
Agonist activity at rat muscarinic M1 receptor expressed in CHO cellsAgonist activity at rat muscarinic M1 receptor expressed in CHO cells
ChEMBL 359 4 1 4 2.5 CCOC(=O)N1CCC(N2CCC[C@@H](NC(=O)c3ccccc3)C2)CC1 10.1016/j.bmcl.2011.08.084
172452791 196104 None 0 Human Functional pEC50 = 5.9 5.9 -2 2
Activation of human muscarinic M1 receptor expressed in HEK293 cells incubated for 3 mins by Calcium flux assayActivation of human muscarinic M1 receptor expressed in HEK293 cells incubated for 3 mins by Calcium flux assay
ChEMBL 404 4 0 5 2.0 COc1cc(F)ccc1C1CCN([C@@H]2COC3(C2)CN(C(=O)C2COC2)C3)CC1 10.1021/acsmedchemlett.3c00331
CHEMBL5416951 196104 None 0 Human Functional pEC50 = 5.9 5.9 -2 2
Activation of human muscarinic M1 receptor expressed in HEK293 cells incubated for 3 mins by Calcium flux assayActivation of human muscarinic M1 receptor expressed in HEK293 cells incubated for 3 mins by Calcium flux assay
ChEMBL 404 4 0 5 2.0 COc1cc(F)ccc1C1CCN([C@@H]2COC3(C2)CN(C(=O)C2COC2)C3)CC1 10.1021/acsmedchemlett.3c00331
57391102 68276 None 5 Human Functional pEC50 = 5.9 5.9 -2 2
Agonist activity at human recombinant muscarinic M1 receptor by HTS cell based assayAgonist activity at human recombinant muscarinic M1 receptor by HTS cell based assay
ChEMBL 373 4 1 4 2.8 CCOC(=O)N1CCC(N2CCC[C@@H](NC(=O)c3ccccc3C)C2)CC1 10.1016/j.bmcl.2011.08.084
CHEMBL1916224 68276 None 5 Human Functional pEC50 = 5.9 5.9 -2 2
Agonist activity at human recombinant muscarinic M1 receptor by HTS cell based assayAgonist activity at human recombinant muscarinic M1 receptor by HTS cell based assay
ChEMBL 373 4 1 4 2.8 CCOC(=O)N1CCC(N2CCC[C@@H](NC(=O)c3ccccc3C)C2)CC1 10.1016/j.bmcl.2011.08.084
46873654 68284 None 0 Rat Functional pEC50 = 5.9 5.9 - 1
Agonist activity at rat muscarinic M1 receptor expressed in CHO cellsAgonist activity at rat muscarinic M1 receptor expressed in CHO cells
ChEMBL 365 4 1 5 2.6 CCOC(=O)N1CCC(N2CCC[C@@H](NC(=O)c3cccs3)C2)CC1 10.1016/j.bmcl.2011.08.084
CHEMBL1916232 68284 None 0 Rat Functional pEC50 = 5.9 5.9 - 1
Agonist activity at rat muscarinic M1 receptor expressed in CHO cellsAgonist activity at rat muscarinic M1 receptor expressed in CHO cells
ChEMBL 365 4 1 5 2.6 CCOC(=O)N1CCC(N2CCC[C@@H](NC(=O)c3cccs3)C2)CC1 10.1016/j.bmcl.2011.08.084
57391102 68276 None 5 Rat Functional pEC50 = 5.9 5.9 2 2
Agonist activity at rat recombinant muscarinic M1 receptor by HTS cell based assayAgonist activity at rat recombinant muscarinic M1 receptor by HTS cell based assay
ChEMBL 373 4 1 4 2.8 CCOC(=O)N1CCC(N2CCC[C@@H](NC(=O)c3ccccc3C)C2)CC1 10.1016/j.bmcl.2011.08.084
CHEMBL1916224 68276 None 5 Rat Functional pEC50 = 5.9 5.9 2 2
Agonist activity at rat recombinant muscarinic M1 receptor by HTS cell based assayAgonist activity at rat recombinant muscarinic M1 receptor by HTS cell based assay
ChEMBL 373 4 1 4 2.8 CCOC(=O)N1CCC(N2CCC[C@@H](NC(=O)c3ccccc3C)C2)CC1 10.1016/j.bmcl.2011.08.084
145961455 161483 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 447 5 2 7 2.7 Cn1nccc1-c1ccc(CN2CC(C(=O)N[C@H]3CCCC[C@@H]3O)Oc3ccccc32)cn1 10.1016/j.bmcl.2018.05.009
CHEMBL4126400 161483 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 447 5 2 7 2.7 Cn1nccc1-c1ccc(CN2CC(C(=O)N[C@H]3CCCC[C@@H]3O)Oc3ccccc32)cn1 10.1016/j.bmcl.2018.05.009
71540044 86392 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulator activity at human muscarinic M1 receptor by calcium mobilization assayPositive allosteric modulator activity at human muscarinic M1 receptor by calcium mobilization assay
ChEMBL 336 3 1 4 2.8 Cn1cc(-c2ccc(CN3C(=O)C(N)c4ccccc43)c(F)c2)cn1 10.1016/j.bmcl.2012.11.092
CHEMBL2313530 86392 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulator activity at human muscarinic M1 receptor by calcium mobilization assayPositive allosteric modulator activity at human muscarinic M1 receptor by calcium mobilization assay
ChEMBL 336 3 1 4 2.8 Cn1cc(-c2ccc(CN3C(=O)C(N)c4ccccc43)c(F)c2)cn1 10.1016/j.bmcl.2012.11.092
2551 794 None 13 Human Functional pEC50 = 4.9 4.9 -27 13
Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0102405
2551.0 794 None 13 Human Functional pEC50 = 4.9 4.9 -27 13
Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0102405
298 794 None 13 Human Functional pEC50 = 4.9 4.9 -27 13
Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0102405
488 794 None 13 Human Functional pEC50 = 4.9 4.9 -27 13
Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0102405
CHEMBL965 794 None 13 Human Functional pEC50 = 4.9 4.9 -27 13
Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0102405
DB00411 794 None 13 Human Functional pEC50 = 4.9 4.9 -27 13
Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0102405
11072401 30786 None 0 Human Functional pEC50 = 4.9 4.9 -12882 2
Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.
ChEMBL 592 17 0 10 7.6 CN1CCC=C(c2nsnc2SCCCCCCCCCCCCSc2nsnc2C2=CCCN(C)C2)C1 10.1021/jm0102405
CHEMBL139603 30786 None 0 Human Functional pEC50 = 4.9 4.9 -12882 2
Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.
ChEMBL 592 17 0 10 7.6 CN1CCC=C(c2nsnc2SCCCCCCCCCCCCSc2nsnc2C2=CCCN(C)C2)C1 10.1021/jm0102405
72945087 120605 None 2 Human Functional pEC50 = 6.9 6.9 -2 2
Agonist activity at muscarinic M1 receptor (unknown origin) by calcium mobilization assayAgonist activity at muscarinic M1 receptor (unknown origin) by calcium mobilization assay
ChEMBL 429 3 0 5 2.8 CCOC(=O)N1CCC(CN2CCC3(CC2)CN(C(=O)N(C)C)c2ncccc23)CC1 10.1016/j.bmcl.2014.04.085
CHEMBL3310802 120605 None 2 Human Functional pEC50 = 6.9 6.9 -2 2
Agonist activity at muscarinic M1 receptor (unknown origin) by calcium mobilization assayAgonist activity at muscarinic M1 receptor (unknown origin) by calcium mobilization assay
ChEMBL 429 3 0 5 2.8 CCOC(=O)N1CCC(CN2CCC3(CC2)CN(C(=O)N(C)C)c2ncccc23)CC1 10.1016/j.bmcl.2014.04.085
CHEMBL3545481 120605 None 2 Human Functional pEC50 = 6.9 6.9 -2 2
Agonist activity at muscarinic M1 receptor (unknown origin) by calcium mobilization assayAgonist activity at muscarinic M1 receptor (unknown origin) by calcium mobilization assay
ChEMBL 429 3 0 5 2.8 CCOC(=O)N1CCC(CN2CCC3(CC2)CN(C(=O)N(C)C)c2ncccc23)CC1 10.1016/j.bmcl.2014.04.085
162475025 181586 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Positive allosteric modulation of recombinant human muscarinic M1 receptor co-expressing pCRE-Luc reporter gene in CHO cells assessed as stimulation of luciferase activity in presence of acetylcholine substrate measured after 4 hrs by luciferase reporter gene assayPositive allosteric modulation of recombinant human muscarinic M1 receptor co-expressing pCRE-Luc reporter gene in CHO cells assessed as stimulation of luciferase activity in presence of acetylcholine substrate measured after 4 hrs by luciferase reporter gene assay
ChEMBL 426 5 2 5 4.0 O=C(N[C@@H]1CCCC[C@H]1O)c1cc(Cc2ccc(-c3ccncc3)cc2)c2cccn2n1 10.1021/acsmedchemlett.1c00118
CHEMBL4764644 181586 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Positive allosteric modulation of recombinant human muscarinic M1 receptor co-expressing pCRE-Luc reporter gene in CHO cells assessed as stimulation of luciferase activity in presence of acetylcholine substrate measured after 4 hrs by luciferase reporter gene assayPositive allosteric modulation of recombinant human muscarinic M1 receptor co-expressing pCRE-Luc reporter gene in CHO cells assessed as stimulation of luciferase activity in presence of acetylcholine substrate measured after 4 hrs by luciferase reporter gene assay
ChEMBL 426 5 2 5 4.0 O=C(N[C@@H]1CCCC[C@H]1O)c1cc(Cc2ccc(-c3ccncc3)cc2)c2cccn2n1 10.1021/acsmedchemlett.1c00118
3652 4097 None 50 Human Functional pEC50 = 6.9 6.9 -18 15
Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm9910019
57 4097 None 50 Human Functional pEC50 = 6.9 6.9 -18 15
Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm9910019
60809 4097 None 50 Human Functional pEC50 = 6.9 6.9 -18 15
Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm9910019
60809.0 4097 None 50 Human Functional pEC50 = 6.9 6.9 -18 15
Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm9910019
CHEMBL21536 4097 None 50 Human Functional pEC50 = 6.9 6.9 -18 15
Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm9910019
DB15357 4097 None 50 Human Functional pEC50 = 6.9 6.9 -18 15
Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm9910019
10403330 17336 None 2 Human Functional pEC50 = 6.9 6.9 -61 2
Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.
ChEMBL 313 7 0 6 3.3 CCCCCSc1nsnc1OC1CN2CCC1CC2 10.1021/jm970125n
CHEMBL125732 17336 None 2 Human Functional pEC50 = 6.9 6.9 -61 2
Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.
ChEMBL 313 7 0 6 3.3 CCCCCSc1nsnc1OC1CN2CCC1CC2 10.1021/jm970125n
44475955 2566 None 17 Rat Functional pEC50 = 5.9 5.9 -1 2
Allosteric modulation at rat M1 receptor expressed in CHO cells by calcium mobilization assayAllosteric modulation at rat M1 receptor expressed in CHO cells by calcium mobilization assay
ChEMBL 505 6 1 6 4.3 Brc1ccc(c(c1)Cn1cc(c2c1cccc2)S(=O)(=O)CC(=O)Nc1noc(c1)C)F 10.1016/j.bmcl.2010.12.015
5437 2566 None 17 Rat Functional pEC50 = 5.9 5.9 -1 2
Allosteric modulation at rat M1 receptor expressed in CHO cells by calcium mobilization assayAllosteric modulation at rat M1 receptor expressed in CHO cells by calcium mobilization assay
ChEMBL 505 6 1 6 4.3 Brc1ccc(c(c1)Cn1cc(c2c1cccc2)S(=O)(=O)CC(=O)Nc1noc(c1)C)F 10.1016/j.bmcl.2010.12.015
CHEMBL1357815 2566 None 17 Rat Functional pEC50 = 5.9 5.9 -1 2
Allosteric modulation at rat M1 receptor expressed in CHO cells by calcium mobilization assayAllosteric modulation at rat M1 receptor expressed in CHO cells by calcium mobilization assay
ChEMBL 505 6 1 6 4.3 Brc1ccc(c(c1)Cn1cc(c2c1cccc2)S(=O)(=O)CC(=O)Nc1noc(c1)C)F 10.1016/j.bmcl.2010.12.015
122195090 124164 None 0 Human Functional pEC50 = 7.9 7.9 6 2
Agonist activity at human muscarinic M1 acetylcholine receptor expressed in CHO cells assessed as calcium mobilization by FLIPR assayAgonist activity at human muscarinic M1 acetylcholine receptor expressed in CHO cells assessed as calcium mobilization by FLIPR assay
ChEMBL 412 4 1 4 3.5 CCOC(=O)N1[C@H]2CC[C@@H]1C[C@@H](CN1CC[C@@H](N3Cc4ccccc4NC3=O)C1)C2 10.1016/j.bmcl.2015.09.032
CHEMBL3633184 124164 None 0 Human Functional pEC50 = 7.9 7.9 6 2
Agonist activity at human muscarinic M1 acetylcholine receptor expressed in CHO cells assessed as calcium mobilization by FLIPR assayAgonist activity at human muscarinic M1 acetylcholine receptor expressed in CHO cells assessed as calcium mobilization by FLIPR assay
ChEMBL 412 4 1 4 3.5 CCOC(=O)N1[C@H]2CC[C@@H]1C[C@@H](CN1CC[C@@H](N3Cc4ccccc4NC3=O)C1)C2 10.1016/j.bmcl.2015.09.032
145984808 165879 None 0 Rat Functional pEC50 = 7.9 7.9 - 1
Positive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assayPositive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assay
ChEMBL 446 5 2 8 1.8 Cn1ccc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCOC[C@H]4O)nc4c3ccn4C)cn2)n1 10.1021/acsmedchemlett.8b00261
CHEMBL4247625 165879 None 0 Rat Functional pEC50 = 7.9 7.9 - 1
Positive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assayPositive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assay
ChEMBL 446 5 2 8 1.8 Cn1ccc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCOC[C@H]4O)nc4c3ccn4C)cn2)n1 10.1021/acsmedchemlett.8b00261
135409468 2035 None 50 Human Functional pEC50 = 6.9 6.9 3 5
Agonist activity at human muscarinic M1 receptor Y381A mutant expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor Y381A mutant expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 10.1021/jm100697g
333 2035 None 50 Human Functional pEC50 = 6.9 6.9 3 5
Agonist activity at human muscarinic M1 receptor Y381A mutant expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor Y381A mutant expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 10.1021/jm100697g
CHEMBL845 2035 None 50 Human Functional pEC50 = 6.9 6.9 3 5
Agonist activity at human muscarinic M1 receptor Y381A mutant expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor Y381A mutant expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 10.1021/jm100697g
57398164 68279 None 0 Rat Functional pEC50 = 6.9 6.9 - 1
Agonist activity at rat muscarinic M1 receptor expressed in CHO cellsAgonist activity at rat muscarinic M1 receptor expressed in CHO cells
ChEMBL 377 4 1 4 2.6 CCOC(=O)N1CCC(N2CCC[C@@H](NC(=O)c3cccc(F)c3)C2)CC1 10.1016/j.bmcl.2011.08.084
CHEMBL1916227 68279 None 0 Rat Functional pEC50 = 6.9 6.9 - 1
Agonist activity at rat muscarinic M1 receptor expressed in CHO cellsAgonist activity at rat muscarinic M1 receptor expressed in CHO cells
ChEMBL 377 4 1 4 2.6 CCOC(=O)N1CCC(N2CCC[C@@H](NC(=O)c3cccc(F)c3)C2)CC1 10.1016/j.bmcl.2011.08.084
145961400 161746 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 450 5 2 6 3.2 O=C(N[C@H]1CCCC[C@@H]1O)C1CN(Cc2ccc(-n3cccn3)cc2)c2cccc(F)c2O1 10.1016/j.bmcl.2018.05.009
CHEMBL4130291 161746 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 450 5 2 6 3.2 O=C(N[C@H]1CCCC[C@@H]1O)C1CN(Cc2ccc(-n3cccn3)cc2)c2cccc(F)c2O1 10.1016/j.bmcl.2018.05.009
44589503 186624 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
ChEMBL 440 4 1 5 2.8 O=c1[nH]c2ccccc2n1C1CCN(C2CCN(S(=O)(=O)c3ccccc3)CC2)CC1 10.1016/j.bmcl.2008.09.032
CHEMBL487762 186624 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
ChEMBL 440 4 1 5 2.8 O=c1[nH]c2ccccc2n1C1CCN(C2CCN(S(=O)(=O)c3ccccc3)CC2)CC1 10.1016/j.bmcl.2008.09.032
145963674 161664 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 430 5 2 5 3.5 O=C(N[C@H]1CCCC[C@@H]1O)C1Cc2ccccc2N(Cc2ccc(-n3cccn3)cc2)C1 10.1016/j.bmcl.2018.05.009
CHEMBL4129005 161664 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 430 5 2 5 3.5 O=C(N[C@H]1CCCC[C@@H]1O)C1Cc2ccccc2N(Cc2ccc(-n3cccn3)cc2)C1 10.1016/j.bmcl.2018.05.009
145961400 161746 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 450 5 2 6 3.2 O=C(N[C@H]1CCCC[C@@H]1O)C1CN(Cc2ccc(-n3cccn3)cc2)c2cccc(F)c2O1 10.1016/j.bmcl.2018.05.009
CHEMBL4130291 161746 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 450 5 2 6 3.2 O=C(N[C@H]1CCCC[C@@H]1O)C1CN(Cc2ccc(-n3cccn3)cc2)c2cccc(F)c2O1 10.1016/j.bmcl.2018.05.009
118724597 116517 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assay
ChEMBL 411 4 0 4 5.2 Cc1ccc(Cn2nc3c4ccccc4n(Cc4cccc(F)c4)cc-3c2=O)c(C)c1 10.1016/j.bmcl.2014.11.011
CHEMBL3360939 116517 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assay
ChEMBL 411 4 0 4 5.2 Cc1ccc(Cn2nc3c4ccccc4n(Cc4cccc(F)c4)cc-3c2=O)c(C)c1 10.1016/j.bmcl.2014.11.011
118724597 116517 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assay
ChEMBL 411 4 0 4 5.2 Cc1ccc(Cn2nc3c4ccccc4n(Cc4cccc(F)c4)cc-3c2=O)c(C)c1 10.1016/j.bmcl.2014.11.011
CHEMBL3360939 116517 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assay
ChEMBL 411 4 0 4 5.2 Cc1ccc(Cn2nc3c4ccccc4n(Cc4cccc(F)c4)cc-3c2=O)c(C)c1 10.1016/j.bmcl.2014.11.011
44475955 2566 None 17 Rat Functional pEC50 = 5.9 5.9 -1 2
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: PAM Calcium Assay Dose-Response with M1. Measurement of intracellular Ca2+ using Fluo-4 dye in CHO-K1 cells stably transfected with rat M1 (Class of assay: confirmatory) [Related pubchem assays: 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen [Primary Screening])]PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: PAM Calcium Assay Dose-Response with M1. Measurement of intracellular Ca2+ using Fluo-4 dye in CHO-K1 cells stably transfected with rat M1 (Class of assay: confirmatory) [Related pubchem assays: 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen [Primary Screening])]
ChEMBL 505 6 1 6 4.3 Brc1ccc(c(c1)Cn1cc(c2c1cccc2)S(=O)(=O)CC(=O)Nc1noc(c1)C)F nan
5437 2566 None 17 Rat Functional pEC50 = 5.9 5.9 -1 2
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: PAM Calcium Assay Dose-Response with M1. Measurement of intracellular Ca2+ using Fluo-4 dye in CHO-K1 cells stably transfected with rat M1 (Class of assay: confirmatory) [Related pubchem assays: 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen [Primary Screening])]PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: PAM Calcium Assay Dose-Response with M1. Measurement of intracellular Ca2+ using Fluo-4 dye in CHO-K1 cells stably transfected with rat M1 (Class of assay: confirmatory) [Related pubchem assays: 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen [Primary Screening])]
ChEMBL 505 6 1 6 4.3 Brc1ccc(c(c1)Cn1cc(c2c1cccc2)S(=O)(=O)CC(=O)Nc1noc(c1)C)F nan
CHEMBL1357815 2566 None 17 Rat Functional pEC50 = 5.9 5.9 -1 2
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: PAM Calcium Assay Dose-Response with M1. Measurement of intracellular Ca2+ using Fluo-4 dye in CHO-K1 cells stably transfected with rat M1 (Class of assay: confirmatory) [Related pubchem assays: 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen [Primary Screening])]PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: PAM Calcium Assay Dose-Response with M1. Measurement of intracellular Ca2+ using Fluo-4 dye in CHO-K1 cells stably transfected with rat M1 (Class of assay: confirmatory) [Related pubchem assays: 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen [Primary Screening])]
ChEMBL 505 6 1 6 4.3 Brc1ccc(c(c1)Cn1cc(c2c1cccc2)S(=O)(=O)CC(=O)Nc1noc(c1)C)F nan
118663129 182869 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human muscarinic M1 receptor stably expressed in CHO cells assessed as increase in Ach-induced intracellular calcium level preincubated for 10 mins followed by addition of Ach at EC20 concentration by Fluo-8AM dye based FLIPR TETRA methodPositive allosteric modulation of human muscarinic M1 receptor stably expressed in CHO cells assessed as increase in Ach-induced intracellular calcium level preincubated for 10 mins followed by addition of Ach at EC20 concentration by Fluo-8AM dye based FLIPR TETRA method
ChEMBL 393 5 2 6 2.5 Cc1cnc(C(=O)N[C@H]2CCOC[C@@H]2O)cc1Cc1ccc(-c2cocn2)cc1 10.1021/acs.jmedchem.6b00544
CHEMBL4790220 182869 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human muscarinic M1 receptor stably expressed in CHO cells assessed as increase in Ach-induced intracellular calcium level preincubated for 10 mins followed by addition of Ach at EC20 concentration by Fluo-8AM dye based FLIPR TETRA methodPositive allosteric modulation of human muscarinic M1 receptor stably expressed in CHO cells assessed as increase in Ach-induced intracellular calcium level preincubated for 10 mins followed by addition of Ach at EC20 concentration by Fluo-8AM dye based FLIPR TETRA method
ChEMBL 393 5 2 6 2.5 Cc1cnc(C(=O)N[C@H]2CCOC[C@@H]2O)cc1Cc1ccc(-c2cocn2)cc1 10.1021/acs.jmedchem.6b00544
172443792 195072 None 0 Human Functional pEC50 = 5.8 5.8 -2 2
Activation of human muscarinic M1 receptor expressed in HEK293 cells incubated for 3 mins by Calcium flux assayActivation of human muscarinic M1 receptor expressed in HEK293 cells incubated for 3 mins by Calcium flux assay
ChEMBL 386 4 0 5 1.9 COc1ccccc1C1CCN([C@@H]2COC3(C2)CN(C(=O)C2COC2)C3)CC1 10.1021/acsmedchemlett.3c00331
CHEMBL5396126 195072 None 0 Human Functional pEC50 = 5.8 5.8 -2 2
Activation of human muscarinic M1 receptor expressed in HEK293 cells incubated for 3 mins by Calcium flux assayActivation of human muscarinic M1 receptor expressed in HEK293 cells incubated for 3 mins by Calcium flux assay
ChEMBL 386 4 0 5 1.9 COc1ccccc1C1CCN([C@@H]2COC3(C2)CN(C(=O)C2COC2)C3)CC1 10.1021/acsmedchemlett.3c00331
151866896 182703 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of recombinant human muscarinic M1 receptor co-expressing pCRE-Luc reporter gene in CHO cells assessed as stimulation of luciferase activity in presence of acetylcholine substrate measured after 4 hrs by luciferase reporter gene assayPositive allosteric modulation of recombinant human muscarinic M1 receptor co-expressing pCRE-Luc reporter gene in CHO cells assessed as stimulation of luciferase activity in presence of acetylcholine substrate measured after 4 hrs by luciferase reporter gene assay
ChEMBL 451 5 2 6 3.9 N#Cc1cncc(-c2ccc(Cc3cc(C(=O)N[C@H]4CCCC[C@@H]4O)nn4cccc34)cc2)c1 10.1021/acsmedchemlett.1c00118
CHEMBL4788148 182703 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of recombinant human muscarinic M1 receptor co-expressing pCRE-Luc reporter gene in CHO cells assessed as stimulation of luciferase activity in presence of acetylcholine substrate measured after 4 hrs by luciferase reporter gene assayPositive allosteric modulation of recombinant human muscarinic M1 receptor co-expressing pCRE-Luc reporter gene in CHO cells assessed as stimulation of luciferase activity in presence of acetylcholine substrate measured after 4 hrs by luciferase reporter gene assay
ChEMBL 451 5 2 6 3.9 N#Cc1cncc(-c2ccc(Cc3cc(C(=O)N[C@H]4CCCC[C@@H]4O)nn4cccc34)cc2)c1 10.1021/acsmedchemlett.1c00118
139414034 163900 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assayPositive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 380 2 1 2 5.8 Fc1ccccc1C1=N[C@@H](c2ccccc2)C(=S)Nc2ccc(Cl)cc21 10.1016/j.bmcl.2017.11.008
CHEMBL4206098 163900 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assayPositive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 380 2 1 2 5.8 Fc1ccccc1C1=N[C@@H](c2ccccc2)C(=S)Nc2ccc(Cl)cc21 10.1016/j.bmcl.2017.11.008
139414036 164841 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assayPositive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 370 3 1 2 6.0 CC(C)[C@@H]1N=C(c2ccccc2)c2cc(-c3ccccc3)ccc2NC1=S 10.1016/j.bmcl.2017.11.008
CHEMBL4217684 164841 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assayPositive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 370 3 1 2 6.0 CC(C)[C@@H]1N=C(c2ccccc2)c2cc(-c3ccccc3)ccc2NC1=S 10.1016/j.bmcl.2017.11.008
162475031 181181 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of recombinant human muscarinic M1 receptor co-expressing pCRE-Luc reporter gene in CHO cells assessed as stimulation of luciferase activity in presence of acetylcholine substrate measured after 4 hrs by luciferase reporter gene assayPositive allosteric modulation of recombinant human muscarinic M1 receptor co-expressing pCRE-Luc reporter gene in CHO cells assessed as stimulation of luciferase activity in presence of acetylcholine substrate measured after 4 hrs by luciferase reporter gene assay
ChEMBL 444 5 2 5 4.2 O=C(N[C@@H]1CCCC[C@H]1O)c1cc(Cc2ccc(-c3ccc(F)cn3)cc2)c2cccn2n1 10.1021/acsmedchemlett.1c00118
CHEMBL4759834 181181 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of recombinant human muscarinic M1 receptor co-expressing pCRE-Luc reporter gene in CHO cells assessed as stimulation of luciferase activity in presence of acetylcholine substrate measured after 4 hrs by luciferase reporter gene assayPositive allosteric modulation of recombinant human muscarinic M1 receptor co-expressing pCRE-Luc reporter gene in CHO cells assessed as stimulation of luciferase activity in presence of acetylcholine substrate measured after 4 hrs by luciferase reporter gene assay
ChEMBL 444 5 2 5 4.2 O=C(N[C@@H]1CCCC[C@H]1O)c1cc(Cc2ccc(-c3ccc(F)cn3)cc2)c2cccn2n1 10.1021/acsmedchemlett.1c00118
44208564 16710 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 441 7 1 3 3.5 O=C(Cc1ccccc1)NC1CCN(CCCN2C(=O)CCc3cc(F)c(F)cc32)CC1 10.1021/jm100697g
CHEMBL1242951 16710 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 441 7 1 3 3.5 O=C(Cc1ccccc1)NC1CCN(CCCN2C(=O)CCc3cc(F)c(F)cc32)CC1 10.1021/jm100697g
118732897 120935 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Partial agonist activity at human muscarinic M1 acetylcholine receptor expressed in CHO cells assessed as increase in IP1 accumulation incubated for 30 mins by FRET based HTRF assayPartial agonist activity at human muscarinic M1 acetylcholine receptor expressed in CHO cells assessed as increase in IP1 accumulation incubated for 30 mins by FRET based HTRF assay
ChEMBL 621 12 1 6 4.9 C[N+](C)(CC#CCOC1=NOCC1)CCCCCCNC(=O)c1cn(Cc2ccccc2)c2cc(Br)ccc2c1=O 10.1021/jm500860w
CHEMBL3414842 120935 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Partial agonist activity at human muscarinic M1 acetylcholine receptor expressed in CHO cells assessed as increase in IP1 accumulation incubated for 30 mins by FRET based HTRF assayPartial agonist activity at human muscarinic M1 acetylcholine receptor expressed in CHO cells assessed as increase in IP1 accumulation incubated for 30 mins by FRET based HTRF assay
ChEMBL 621 12 1 6 4.9 C[N+](C)(CC#CCOC1=NOCC1)CCCCCCNC(=O)c1cn(Cc2ccccc2)c2cc(Br)ccc2c1=O 10.1021/jm500860w
CHEMBL3559129 120935 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Partial agonist activity at human muscarinic M1 acetylcholine receptor expressed in CHO cells assessed as increase in IP1 accumulation incubated for 30 mins by FRET based HTRF assayPartial agonist activity at human muscarinic M1 acetylcholine receptor expressed in CHO cells assessed as increase in IP1 accumulation incubated for 30 mins by FRET based HTRF assay
ChEMBL 621 12 1 6 4.9 C[N+](C)(CC#CCOC1=NOCC1)CCCCCCNC(=O)c1cn(Cc2ccccc2)c2cc(Br)ccc2c1=O 10.1021/jm500860w
122186861 123043 None 0 Human Functional pEC50 = 7.8 7.8 1 2
Positive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as basal and acetylcholine-stimulated Ca2+ level by FLIPR assayPositive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as basal and acetylcholine-stimulated Ca2+ level by FLIPR assay
ChEMBL 449 5 2 7 2.5 Cn1cc(-c2ccc(Cn3cc(C(=O)N[C@H]4COCC[C@@H]4O)c4ncccc43)cc2F)cn1 10.1021/acsmedchemlett.5b00185
CHEMBL3608421 123043 None 0 Human Functional pEC50 = 7.8 7.8 1 2
Positive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as basal and acetylcholine-stimulated Ca2+ level by FLIPR assayPositive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as basal and acetylcholine-stimulated Ca2+ level by FLIPR assay
ChEMBL 449 5 2 7 2.5 Cn1cc(-c2ccc(Cn3cc(C(=O)N[C@H]4COCC[C@@H]4O)c4ncccc43)cc2F)cn1 10.1021/acsmedchemlett.5b00185
10426487 2841 None 7 Human Functional pEC50 = 7.8 7.8 3 2
Stimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptorStimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptor
ChEMBL 325 3 0 5 2.8 C1CN2CCC1C(C2)c1nsnc1OCC#Cc1ccccc1 10.1016/s0960-894x(98)00509-5
291 2841 None 7 Human Functional pEC50 = 7.8 7.8 3 2
Stimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptorStimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptor
ChEMBL 325 3 0 5 2.8 C1CN2CCC1C(C2)c1nsnc1OCC#Cc1ccccc1 10.1016/s0960-894x(98)00509-5
CHEMBL99521 2841 None 7 Human Functional pEC50 = 7.8 7.8 3 2
Stimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptorStimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptor
ChEMBL 325 3 0 5 2.8 C1CN2CCC1C(C2)c1nsnc1OCC#Cc1ccccc1 10.1016/s0960-894x(98)00509-5
46891595 6490 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 346 4 2 2 3.9 O=C(NCC1CCNCC1)c1c(F)cccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.127
CHEMBL1082680 6490 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 346 4 2 2 3.9 O=C(NCC1CCNCC1)c1c(F)cccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.127
289 242 None 13 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 301 8 0 2 4.9 CCCCC1CCN(CC1)CCCC(=O)c1ccccc1C 10.1021/jm100697g
9948320 242 None 13 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 301 8 0 2 4.9 CCCCC1CCN(CC1)CCCC(=O)c1ccccc1C 10.1021/jm100697g
CHEMBL1242950 242 None 13 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 301 8 0 2 4.9 CCCCC1CCN(CC1)CCCC(=O)c1ccccc1C 10.1021/jm100697g
46929965 16715 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 423 7 1 3 3.3 O=C(Cc1ccccc1)NC1CCN(CCCN2C(=O)CCc3c(F)cccc32)CC1 10.1021/jm100697g
CHEMBL1243011 16715 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 423 7 1 3 3.3 O=C(Cc1ccccc1)NC1CCN(CCCN2C(=O)CCc3c(F)cccc32)CC1 10.1021/jm100697g
70681453 74377 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
ChEMBL 351 6 2 4 2.4 CCOC(=O)N1[C@H]2CC[C@@H]1C[C@@H](NCCNC(=O)C1CCCCC1)C2 10.1016/j.bmcl.2012.03.088
CHEMBL2024426 74377 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
ChEMBL 351 6 2 4 2.4 CCOC(=O)N1[C@H]2CC[C@@H]1C[C@@H](NCCNC(=O)C1CCCCC1)C2 10.1016/j.bmcl.2012.03.088
44578928 191183 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
ChEMBL 492 4 1 4 5.3 O=c1[nH]c2cc(Cl)ccc2n1C1CCN(C2CCN(Cc3ccccc3C(F)(F)F)CC2)CC1 10.1016/j.bmcl.2008.09.023
CHEMBL518747 191183 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
ChEMBL 492 4 1 4 5.3 O=c1[nH]c2cc(Cl)ccc2n1C1CCN(C2CCN(Cc3ccccc3C(F)(F)F)CC2)CC1 10.1016/j.bmcl.2008.09.023
10952416 35159 None 0 Human Functional pEC50 = 5.8 5.8 -323 2
Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.
ChEMBL 578 16 0 10 7.2 CN1CCC=C(c2nsnc2SCCCCCCCCCCCSc2nsnc2C2=CCCN(C)C2)C1 10.1021/jm0102405
CHEMBL143466 35159 None 0 Human Functional pEC50 = 5.8 5.8 -323 2
Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.
ChEMBL 578 16 0 10 7.2 CN1CCC=C(c2nsnc2SCCCCCCCCCCCSc2nsnc2C2=CCCN(C)C2)C1 10.1021/jm0102405
146216732 185647 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL 423 5 1 6 2.9 Cn1cc2c(-c3cc(F)c(CN4Cc5cnn(CCO)c5C4=O)c(F)c3)cccc2n1 10.1016/j.bmcl.2021.128193
CHEMBL4862985 185647 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL 423 5 1 6 2.9 Cn1cc2c(-c3cc(F)c(CN4Cc5cnn(CCO)c5C4=O)c(F)c3)cccc2n1 10.1016/j.bmcl.2021.128193
122191005 123681 None 0 Human Functional pEC50 = 6.8 6.8 3 3
Agonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 509 5 2 3 5.2 C/C(=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(Br)cc1)[C@H](O)C2)N(C)Cc1ccc(F)cc1 10.1016/j.bmcl.2015.08.011
CHEMBL3618447 123681 None 0 Human Functional pEC50 = 6.8 6.8 3 3
Agonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 509 5 2 3 5.2 C/C(=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(Br)cc1)[C@H](O)C2)N(C)Cc1ccc(F)cc1 10.1016/j.bmcl.2015.08.011
118724604 116521 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assay
ChEMBL 394 4 0 5 4.4 Cc1ccc(Cn2nc3c4ccccc4n(Cc4ccncc4)cc-3c2=O)c(C)c1 10.1016/j.bmcl.2014.11.011
CHEMBL3360946 116521 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assay
ChEMBL 394 4 0 5 4.4 Cc1ccc(Cn2nc3c4ccccc4n(Cc4ccncc4)cc-3c2=O)c(C)c1 10.1016/j.bmcl.2014.11.011
118724604 116521 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assay
ChEMBL 394 4 0 5 4.4 Cc1ccc(Cn2nc3c4ccccc4n(Cc4ccncc4)cc-3c2=O)c(C)c1 10.1016/j.bmcl.2014.11.011
CHEMBL3360946 116521 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assay
ChEMBL 394 4 0 5 4.4 Cc1ccc(Cn2nc3c4ccccc4n(Cc4ccncc4)cc-3c2=O)c(C)c1 10.1016/j.bmcl.2014.11.011
3652 4097 None 50 Human Functional pEC50 = 6.8 6.8 -18 15
Agonist activity at human M1 receptor E170K mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M1 receptor E170K mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
57 4097 None 50 Human Functional pEC50 = 6.8 6.8 -18 15
Agonist activity at human M1 receptor E170K mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M1 receptor E170K mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
60809 4097 None 50 Human Functional pEC50 = 6.8 6.8 -18 15
Agonist activity at human M1 receptor E170K mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M1 receptor E170K mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
60809.0 4097 None 50 Human Functional pEC50 = 6.8 6.8 -18 15
Agonist activity at human M1 receptor E170K mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M1 receptor E170K mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
CHEMBL21536 4097 None 50 Human Functional pEC50 = 6.8 6.8 -18 15
Agonist activity at human M1 receptor E170K mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M1 receptor E170K mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
DB15357 4097 None 50 Human Functional pEC50 = 6.8 6.8 -18 15
Agonist activity at human M1 receptor E170K mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M1 receptor E170K mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
3652 4097 None 50 Human Functional pEC50 = 6.8 6.8 -18 15
Agonist activity at human M1 receptor Q185E mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M1 receptor Q185E mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
57 4097 None 50 Human Functional pEC50 = 6.8 6.8 -18 15
Agonist activity at human M1 receptor Q185E mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M1 receptor Q185E mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
60809 4097 None 50 Human Functional pEC50 = 6.8 6.8 -18 15
Agonist activity at human M1 receptor Q185E mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M1 receptor Q185E mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
60809.0 4097 None 50 Human Functional pEC50 = 6.8 6.8 -18 15
Agonist activity at human M1 receptor Q185E mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M1 receptor Q185E mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
CHEMBL21536 4097 None 50 Human Functional pEC50 = 6.8 6.8 -18 15
Agonist activity at human M1 receptor Q185E mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M1 receptor Q185E mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
DB15357 4097 None 50 Human Functional pEC50 = 6.8 6.8 -18 15
Agonist activity at human M1 receptor Q185E mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M1 receptor Q185E mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
46891142 6565 None 0 Human Functional pEC50 = 6.8 6.8 63 2
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 364 4 2 2 3.8 O=C(NC[C@H]1CCNC[C@H]1F)c1c(F)cccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.127
CHEMBL1083003 6565 None 0 Human Functional pEC50 = 6.8 6.8 63 2
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 364 4 2 2 3.8 O=C(NC[C@H]1CCNC[C@H]1F)c1c(F)cccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.127
46891143 6638 None 0 Human Functional pEC50 = 6.8 6.8 63 2
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 396 4 2 2 4.7 O=C(NCC1=C(F)CNCC1)c1c(-c2cccc(Cl)c2)ccc(Cl)c1F 10.1016/j.bmcl.2010.04.127
CHEMBL1083317 6638 None 0 Human Functional pEC50 = 6.8 6.8 63 2
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 396 4 2 2 4.7 O=C(NCC1=C(F)CNCC1)c1c(-c2cccc(Cl)c2)ccc(Cl)c1F 10.1016/j.bmcl.2010.04.127
46891031 6670 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 342 4 2 2 4.0 Cc1ccc(Cl)cc1-c1ccccc1C(=O)NCC1CCNCC1 10.1016/j.bmcl.2010.04.128
CHEMBL1083419 6670 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 342 4 2 2 4.0 Cc1ccc(Cl)cc1-c1ccccc1C(=O)NCC1CCNCC1 10.1016/j.bmcl.2010.04.128
46890717 6731 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 342 4 2 2 4.0 Cc1ccc(C(=O)NCC2CCNCC2)c(-c2cccc(Cl)c2)c1 10.1016/j.bmcl.2010.04.127
CHEMBL1083717 6731 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 342 4 2 2 4.0 Cc1ccc(C(=O)NCC2CCNCC2)c(-c2cccc(Cl)c2)c1 10.1016/j.bmcl.2010.04.127
46891077 6816 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 392 4 2 2 4.7 CC1CNCC=C1CNC(=O)c1c(-c2cccc(Cl)c2)ccc(Cl)c1F 10.1016/j.bmcl.2010.04.127
CHEMBL1083927 6816 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 392 4 2 2 4.7 CC1CNCC=C1CNC(=O)c1c(-c2cccc(Cl)c2)ccc(Cl)c1F 10.1016/j.bmcl.2010.04.127
46890962 7022 None 0 Human Functional pEC50 = 6.8 6.8 -1 2
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 328 4 2 2 3.4 O=C(Cc1ccccc1-c1cccc(Cl)c1)NC1CCNCC1 10.1016/j.bmcl.2010.04.127
CHEMBL1084804 7022 None 0 Human Functional pEC50 = 6.8 6.8 -1 2
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 328 4 2 2 3.4 O=C(Cc1ccccc1-c1cccc(Cl)c1)NC1CCNCC1 10.1016/j.bmcl.2010.04.127
145986042 165973 None 0 Rat Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assayPositive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assay
ChEMBL 444 6 1 7 3.1 Cn1ccc(-c2ccc(Cc3cc(C(=O)NCC4CCOCC4)nc4c3ccn4C)cn2)n1 10.1021/acsmedchemlett.8b00261
CHEMBL4249357 165973 None 0 Rat Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assayPositive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assay
ChEMBL 444 6 1 7 3.1 Cn1ccc(-c2ccc(Cc3cc(C(=O)NCC4CCOCC4)nc4c3ccn4C)cn2)n1 10.1021/acsmedchemlett.8b00261
46891029 6596 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 342 4 2 2 4.0 Cc1cc(Cl)cc(-c2ccccc2C(=O)NCC2CCNCC2)c1 10.1016/j.bmcl.2010.04.128
CHEMBL1083107 6596 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 342 4 2 2 4.0 Cc1cc(Cl)cc(-c2ccccc2C(=O)NCC2CCNCC2)c1 10.1016/j.bmcl.2010.04.128
46891019 6661 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 410 6 1 3 3.9 CS(=O)(=O)N(Cc1c(F)cccc1-c1cccc(Cl)c1)CC1CCNCC1 10.1016/j.bmcl.2010.04.127
CHEMBL1083401 6661 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 410 6 1 3 3.9 CS(=O)(=O)N(Cc1c(F)cccc1-c1cccc(Cl)c1)CC1CCNCC1 10.1016/j.bmcl.2010.04.127
145986042 165973 None 0 Rat Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assayPositive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assay
ChEMBL 444 6 1 7 3.1 Cn1ccc(-c2ccc(Cc3cc(C(=O)NCC4CCOCC4)nc4c3ccn4C)cn2)n1 10.1021/acsmedchemlett.8b00261
CHEMBL4249357 165973 None 0 Rat Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assayPositive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assay
ChEMBL 444 6 1 7 3.1 Cn1ccc(-c2ccc(Cc3cc(C(=O)NCC4CCOCC4)nc4c3ccn4C)cn2)n1 10.1021/acsmedchemlett.8b00261
2551 794 None 13 Human Functional pEC50 = 4.8 4.8 -27 13
Agonist activity at human M1 receptor E170K mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M1 receptor E170K mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0606995
2551.0 794 None 13 Human Functional pEC50 = 4.8 4.8 -27 13
Agonist activity at human M1 receptor E170K mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M1 receptor E170K mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0606995
298 794 None 13 Human Functional pEC50 = 4.8 4.8 -27 13
Agonist activity at human M1 receptor E170K mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M1 receptor E170K mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0606995
488 794 None 13 Human Functional pEC50 = 4.8 4.8 -27 13
Agonist activity at human M1 receptor E170K mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M1 receptor E170K mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0606995
CHEMBL965 794 None 13 Human Functional pEC50 = 4.8 4.8 -27 13
Agonist activity at human M1 receptor E170K mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M1 receptor E170K mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0606995
DB00411 794 None 13 Human Functional pEC50 = 4.8 4.8 -27 13
Agonist activity at human M1 receptor E170K mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M1 receptor E170K mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0606995
2551 794 None 13 Human Functional pEC50 = 4.8 4.8 -27 13
Agonist activity at human M1 receptor Q185E mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M1 receptor Q185E mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0606995
2551.0 794 None 13 Human Functional pEC50 = 4.8 4.8 -27 13
Agonist activity at human M1 receptor Q185E mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M1 receptor Q185E mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0606995
298 794 None 13 Human Functional pEC50 = 4.8 4.8 -27 13
Agonist activity at human M1 receptor Q185E mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M1 receptor Q185E mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0606995
488 794 None 13 Human Functional pEC50 = 4.8 4.8 -27 13
Agonist activity at human M1 receptor Q185E mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M1 receptor Q185E mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0606995
CHEMBL965 794 None 13 Human Functional pEC50 = 4.8 4.8 -27 13
Agonist activity at human M1 receptor Q185E mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M1 receptor Q185E mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0606995
DB00411 794 None 13 Human Functional pEC50 = 4.8 4.8 -27 13
Agonist activity at human M1 receptor Q185E mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M1 receptor Q185E mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm0606995
49799920 10545 None 0 Human Functional pEC50 = 6.8 6.8 6 2
Stimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptorStimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptor
ChEMBL 311 3 0 5 2.4 C(#Cc1ccccc1)COc1nsnc1[C@H]1CN2CC[C@@H]1C2 10.1016/s0960-894x(98)00509-5
CHEMBL1169506 10545 None 0 Human Functional pEC50 = 6.8 6.8 6 2
Stimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptorStimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptor
ChEMBL 311 3 0 5 2.4 C(#Cc1ccccc1)COc1nsnc1[C@H]1CN2CC[C@@H]1C2 10.1016/s0960-894x(98)00509-5
145969659 165055 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Positive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as increase in ACh-induced intracellular calcium level preincubated for 10 mins followed by ACh addition measured every 2 secs for 80 secs by Fluo-4 dye-based FLIPR assayPositive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as increase in ACh-induced intracellular calcium level preincubated for 10 mins followed by ACh addition measured every 2 secs for 80 secs by Fluo-4 dye-based FLIPR assay
ChEMBL 431 5 3 7 2.3 O=C(N[C@H]1CCC(O)C[C@@H]1O)c1cn(Cc2ccc(-n3cccn3)cc2)c2cccnc12 10.1016/j.bmcl.2018.04.054
CHEMBL4225188 165055 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Positive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as increase in ACh-induced intracellular calcium level preincubated for 10 mins followed by ACh addition measured every 2 secs for 80 secs by Fluo-4 dye-based FLIPR assayPositive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as increase in ACh-induced intracellular calcium level preincubated for 10 mins followed by ACh addition measured every 2 secs for 80 secs by Fluo-4 dye-based FLIPR assay
ChEMBL 431 5 3 7 2.3 O=C(N[C@H]1CCC(O)C[C@@H]1O)c1cn(Cc2ccc(-n3cccn3)cc2)c2cccnc12 10.1016/j.bmcl.2018.04.054
44215433 76380 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
ChEMBL 387 5 1 2 4.7 O=C1CCc2ccccc2N1CCCN1CCC(c2ccc3[nH]ccc3c2)CC1 10.1016/j.bmcl.2012.05.048
CHEMBL2059305 76380 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
ChEMBL 387 5 1 2 4.7 O=C1CCc2ccccc2N1CCCN1CCC(c2ccc3[nH]ccc3c2)CC1 10.1016/j.bmcl.2012.05.048
46930252 16743 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 371 6 1 4 2.2 O=C(NC1CCN(CCCN2C(=O)COc3ccccc32)CC1)C1CCC1 10.1021/jm100697g
CHEMBL1243295 16743 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 371 6 1 4 2.2 O=C(NC1CCN(CCCN2C(=O)COc3ccccc32)CC1)C1CCC1 10.1021/jm100697g
25010776 55971 None 1 Human Functional pEC50 = 5.8 5.8 1 5
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
ChEMBL 333 6 2 4 1.9 CCOC(=O)N1CCC(NCCNC(=O)c2ccccc2C)CC1 10.1016/j.bmcl.2012.03.088
CHEMBL1559151 55971 None 1 Human Functional pEC50 = 5.8 5.8 1 5
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
ChEMBL 333 6 2 4 1.9 CCOC(=O)N1CCC(NCCNC(=O)c2ccccc2C)CC1 10.1016/j.bmcl.2012.03.088
CHEMBL1624037 55971 None 1 Human Functional pEC50 = 5.8 5.8 1 5
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
ChEMBL 333 6 2 4 1.9 CCOC(=O)N1CCC(NCCNC(=O)c2ccccc2C)CC1 10.1016/j.bmcl.2012.03.088
44579416 187168 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
ChEMBL 449 4 1 5 4.2 N#Cc1ccccc1CN1CCC(N2CCC(n3c(=O)[nH]c4cc(Cl)ccc43)CC2)CC1 10.1016/j.bmcl.2008.09.023
CHEMBL491208 187168 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
ChEMBL 449 4 1 5 4.2 N#Cc1ccccc1CN1CCC(N2CCC(n3c(=O)[nH]c4cc(Cl)ccc43)CC2)CC1 10.1016/j.bmcl.2008.09.023
118124140 161509 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 450 5 2 6 3.2 O=C(N[C@H]1CCCC[C@@H]1O)C1CN(Cc2ccc(-n3cccn3)cc2F)c2ccccc2O1 10.1016/j.bmcl.2018.05.009
CHEMBL4126807 161509 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 450 5 2 6 3.2 O=C(N[C@H]1CCCC[C@@H]1O)C1CN(Cc2ccc(-n3cccn3)cc2F)c2ccccc2O1 10.1016/j.bmcl.2018.05.009
22730942 18113 None 0 Human Functional pEC50 = 6.8 6.8 -2 2
Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.
ChEMBL 271 5 0 6 2.1 CCCSc1nsnc1OC1CN2CCC1C2 10.1021/jm970125n
CHEMBL126846 18113 None 0 Human Functional pEC50 = 6.8 6.8 -2 2
Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.
ChEMBL 271 5 0 6 2.1 CCCSc1nsnc1OC1CN2CCC1C2 10.1021/jm970125n
145969333 165255 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as increase in ACh-induced intracellular calcium level preincubated for 10 mins followed by ACh addition measured every 2 secs for 80 secs by Fluo-4 dye-based FLIPR assayPositive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as increase in ACh-induced intracellular calcium level preincubated for 10 mins followed by ACh addition measured every 2 secs for 80 secs by Fluo-4 dye-based FLIPR assay
ChEMBL 425 5 3 7 2.3 Cc1cnc(C(=O)N[C@H]2CCOC(O)[C@@H]2O)cc1Cc1ccc(-c2cscn2)cc1 10.1016/j.bmcl.2018.04.054
CHEMBL4228097 165255 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as increase in ACh-induced intracellular calcium level preincubated for 10 mins followed by ACh addition measured every 2 secs for 80 secs by Fluo-4 dye-based FLIPR assayPositive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as increase in ACh-induced intracellular calcium level preincubated for 10 mins followed by ACh addition measured every 2 secs for 80 secs by Fluo-4 dye-based FLIPR assay
ChEMBL 425 5 3 7 2.3 Cc1cnc(C(=O)N[C@H]2CCOC(O)[C@@H]2O)cc1Cc1ccc(-c2cscn2)cc1 10.1016/j.bmcl.2018.04.054
122186858 123040 None 0 Rat Functional pEC50 = 6.8 6.8 -2 2
Positive allosteric modulation of rat muscarinic M1 receptor expressed in CHO cells assessed as basal and acetylcholine-stimulated Ca2+ level by FLIPR assayPositive allosteric modulation of rat muscarinic M1 receptor expressed in CHO cells assessed as basal and acetylcholine-stimulated Ca2+ level by FLIPR assay
ChEMBL 405 4 2 7 1.9 Cn1ncc2cc(Cn3cc(C(=O)N[C@H]4COCC[C@@H]4O)c4ncccc43)ccc21 10.1021/acsmedchemlett.5b00185
CHEMBL3608418 123040 None 0 Rat Functional pEC50 = 6.8 6.8 -2 2
Positive allosteric modulation of rat muscarinic M1 receptor expressed in CHO cells assessed as basal and acetylcholine-stimulated Ca2+ level by FLIPR assayPositive allosteric modulation of rat muscarinic M1 receptor expressed in CHO cells assessed as basal and acetylcholine-stimulated Ca2+ level by FLIPR assay
ChEMBL 405 4 2 7 1.9 Cn1ncc2cc(Cn3cc(C(=O)N[C@H]4COCC[C@@H]4O)c4ncccc43)ccc21 10.1021/acsmedchemlett.5b00185
126492034 161515 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 441 6 1 7 3.7 COc1cccnc1NC(=O)C1CN(Cc2ccc(-n3cccn3)cc2)c2ccccc2O1 10.1016/j.bmcl.2018.05.009
CHEMBL4126841 161515 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 441 6 1 7 3.7 COc1cccnc1NC(=O)C1CN(Cc2ccc(-n3cccn3)cc2)c2ccccc2O1 10.1016/j.bmcl.2018.05.009
127039038 137126 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human M1 receptor expressed in CHO cells assessed as acetylcholine-induced calcium mobilization by FLIPR assayPositive allosteric modulation of human M1 receptor expressed in CHO cells assessed as acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 414 5 2 5 3.9 O=C(N[C@H]1CCCC[C@@H]1O)c1cn(Cc2ccc(-n3cccn3)cc2)c2ccccc12 10.1016/j.bmcl.2015.11.053
CHEMBL3746599 137126 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human M1 receptor expressed in CHO cells assessed as acetylcholine-induced calcium mobilization by FLIPR assayPositive allosteric modulation of human M1 receptor expressed in CHO cells assessed as acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 414 5 2 5 3.9 O=C(N[C@H]1CCCC[C@@H]1O)c1cn(Cc2ccc(-n3cccn3)cc2)c2ccccc12 10.1016/j.bmcl.2015.11.053
9904307 19470 None 0 Human Functional pEC50 = 6.8 6.8 -6 2
Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.
ChEMBL 297 7 0 6 2.6 CCCCCOc1nsnc1OC1CN2CCC1CC2 10.1021/jm970125n
CHEMBL129764 19470 None 0 Human Functional pEC50 = 6.8 6.8 -6 2
Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.
ChEMBL 297 7 0 6 2.6 CCCCCOc1nsnc1OC1CN2CCC1CC2 10.1021/jm970125n
145964557 164314 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assayPositive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 344 2 1 2 4.8 Fc1ccccc1C1=N[C@@H](C2CC2)C(=S)Nc2ccc(Cl)cc21 10.1016/j.bmcl.2017.11.008
CHEMBL4211028 164314 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assayPositive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 344 2 1 2 4.8 Fc1ccccc1C1=N[C@@H](C2CC2)C(=S)Nc2ccc(Cl)cc21 10.1016/j.bmcl.2017.11.008
122189494 123401 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 461 6 2 4 4.4 COc1ccc(C(=O)N[C@@H]2c3cc(/N=C(\C)N(C)Cc4ccc(F)cc4)ccc3C[C@H]2O)cc1 10.1016/j.bmcl.2015.08.011
CHEMBL3616498 123401 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 461 6 2 4 4.4 COc1ccc(C(=O)N[C@@H]2c3cc(/N=C(\C)N(C)Cc4ccc(F)cc4)ccc3C[C@H]2O)cc1 10.1016/j.bmcl.2015.08.011
162648092 179997 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human muscarinic M1 receptor stably expressed in CHO cells assessed as increase in Ach-induced intracellular calcium level preincubated for 10 mins followed by addition of Ach at EC20 concentration by Fluo-8AM dye based FLIPR TETRA methodPositive allosteric modulation of human muscarinic M1 receptor stably expressed in CHO cells assessed as increase in Ach-induced intracellular calcium level preincubated for 10 mins followed by addition of Ach at EC20 concentration by Fluo-8AM dye based FLIPR TETRA method
ChEMBL 437 5 2 6 3.4 Cc1c(Cc2ccc(-c3cscn3)cc2)cc(C(=O)N[C@H]2CCCC[C@@H]2O)c(=O)n1C 10.1021/acs.jmedchem.6b00544
CHEMBL4745827 179997 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human muscarinic M1 receptor stably expressed in CHO cells assessed as increase in Ach-induced intracellular calcium level preincubated for 10 mins followed by addition of Ach at EC20 concentration by Fluo-8AM dye based FLIPR TETRA methodPositive allosteric modulation of human muscarinic M1 receptor stably expressed in CHO cells assessed as increase in Ach-induced intracellular calcium level preincubated for 10 mins followed by addition of Ach at EC20 concentration by Fluo-8AM dye based FLIPR TETRA method
ChEMBL 437 5 2 6 3.4 Cc1c(Cc2ccc(-c3cscn3)cc2)cc(C(=O)N[C@H]2CCCC[C@@H]2O)c(=O)n1C 10.1021/acs.jmedchem.6b00544
146216707 184564 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL 463 5 0 6 4.1 Cn1cc2cc(-c3cc(F)c(CN4Cc5cnn(CC6CCCO6)c5C4=O)c(F)c3)ccc2n1 10.1016/j.bmcl.2021.128193
CHEMBL4846688 184564 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL 463 5 0 6 4.1 Cn1cc2cc(-c3cc(F)c(CN4Cc5cnn(CC6CCCO6)c5C4=O)c(F)c3)ccc2n1 10.1016/j.bmcl.2021.128193
145969659 165055 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as increase in ACh-induced intracellular calcium level preincubated for 10 mins followed by ACh addition measured every 2 secs for 80 secs by Fluo-4 dye-based FLIPR assayPositive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as increase in ACh-induced intracellular calcium level preincubated for 10 mins followed by ACh addition measured every 2 secs for 80 secs by Fluo-4 dye-based FLIPR assay
ChEMBL 431 5 3 7 2.3 O=C(N[C@H]1CCC(O)C[C@@H]1O)c1cn(Cc2ccc(-n3cccn3)cc2)c2cccnc12 10.1016/j.bmcl.2018.04.054
CHEMBL4225188 165055 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as increase in ACh-induced intracellular calcium level preincubated for 10 mins followed by ACh addition measured every 2 secs for 80 secs by Fluo-4 dye-based FLIPR assayPositive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as increase in ACh-induced intracellular calcium level preincubated for 10 mins followed by ACh addition measured every 2 secs for 80 secs by Fluo-4 dye-based FLIPR assay
ChEMBL 431 5 3 7 2.3 O=C(N[C@H]1CCC(O)C[C@@H]1O)c1cn(Cc2ccc(-n3cccn3)cc2)c2cccnc12 10.1016/j.bmcl.2018.04.054
162658825 181106 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human muscarinic M1 receptor stably expressed in CHO cells assessed as increase in Ach-induced intracellular calcium level preincubated for 10 mins followed by addition of Ach at EC20 concentration by Fluo-8AM dye based FLIPR TETRA methodPositive allosteric modulation of human muscarinic M1 receptor stably expressed in CHO cells assessed as increase in Ach-induced intracellular calcium level preincubated for 10 mins followed by addition of Ach at EC20 concentration by Fluo-8AM dye based FLIPR TETRA method
ChEMBL 453 6 2 6 2.5 CO[C@@H]1CCN(c2ccc(Cc3cc(C(=O)N[C@H]4CCCC[C@@H]4O)c(=O)n(C)c3C)cc2)C1 10.1021/acs.jmedchem.6b00544
CHEMBL4758929 181106 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human muscarinic M1 receptor stably expressed in CHO cells assessed as increase in Ach-induced intracellular calcium level preincubated for 10 mins followed by addition of Ach at EC20 concentration by Fluo-8AM dye based FLIPR TETRA methodPositive allosteric modulation of human muscarinic M1 receptor stably expressed in CHO cells assessed as increase in Ach-induced intracellular calcium level preincubated for 10 mins followed by addition of Ach at EC20 concentration by Fluo-8AM dye based FLIPR TETRA method
ChEMBL 453 6 2 6 2.5 CO[C@@H]1CCN(c2ccc(Cc3cc(C(=O)N[C@H]4CCCC[C@@H]4O)c(=O)n(C)c3C)cc2)C1 10.1021/acs.jmedchem.6b00544
127049133 141121 None 0 Rat Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation at rat muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation at rat muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 393 3 0 4 3.7 Cn1cc2c(-c3cc(F)c(CN4C=CC5=NCCN5C4=O)c(F)c3)cccc2n1 10.1016/j.bmcl.2016.04.083
CHEMBL3823999 141121 None 0 Rat Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation at rat muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation at rat muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 393 3 0 4 3.7 Cn1cc2c(-c3cc(F)c(CN4C=CC5=NCCN5C4=O)c(F)c3)cccc2n1 10.1016/j.bmcl.2016.04.083
53385782 74339 None 0 Human Functional pEC50 = 7.8 7.8 56 3
Agonist activity at human muscarinic M1 receptor by calcium mobilization assayAgonist activity at human muscarinic M1 receptor by calcium mobilization assay
ChEMBL 399 4 1 4 3.3 CCOC(=O)N1C2CCC1CC(N1CCC[C@@H](NC(=O)c3ccccc3C)C1)C2 10.1016/j.bmcl.2012.03.088
CHEMBL2024331 74339 None 0 Human Functional pEC50 = 7.8 7.8 56 3
Agonist activity at human muscarinic M1 receptor by calcium mobilization assayAgonist activity at human muscarinic M1 receptor by calcium mobilization assay
ChEMBL 399 4 1 4 3.3 CCOC(=O)N1C2CCC1CC(N1CCC[C@@H](NC(=O)c3ccccc3C)C1)C2 10.1016/j.bmcl.2012.03.088
2166 3123 None 33 Human Functional pEC50 = 7.8 7.8 -3 10
Agonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assayAgonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assay
ChEMBL 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 10.1016/j.bmcl.2015.02.012
305 3123 None 33 Human Functional pEC50 = 7.8 7.8 -3 10
Agonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assayAgonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assay
ChEMBL 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 10.1016/j.bmcl.2015.02.012
5910 3123 None 33 Human Functional pEC50 = 7.8 7.8 -3 10
Agonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assayAgonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assay
ChEMBL 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 10.1016/j.bmcl.2015.02.012
5910.0 3123 None 33 Human Functional pEC50 = 7.8 7.8 -3 10
Agonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assayAgonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assay
ChEMBL 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 10.1016/j.bmcl.2015.02.012
CHEMBL550 3123 None 33 Human Functional pEC50 = 7.8 7.8 -3 10
Agonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assayAgonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assay
ChEMBL 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 10.1016/j.bmcl.2015.02.012
DB01085 3123 None 33 Human Functional pEC50 = 7.8 7.8 -3 10
Agonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assayAgonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assay
ChEMBL 208 3 0 4 1.2 CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C 10.1016/j.bmcl.2015.02.012
172456153 196244 None 0 Human Functional pEC50 = 6.8 6.8 -1 2
Activation of human muscarinic M1 receptor expressed in HEK293 cells incubated for 3 mins by Calcium flux assayActivation of human muscarinic M1 receptor expressed in HEK293 cells incubated for 3 mins by Calcium flux assay
ChEMBL 404 4 0 5 2.0 COc1ccc(F)cc1C1CCN([C@@H]2COC3(C2)CN(C(=O)C2COC2)C3)CC1 10.1021/acsmedchemlett.3c00331
CHEMBL5419622 196244 None 0 Human Functional pEC50 = 6.8 6.8 -1 2
Activation of human muscarinic M1 receptor expressed in HEK293 cells incubated for 3 mins by Calcium flux assayActivation of human muscarinic M1 receptor expressed in HEK293 cells incubated for 3 mins by Calcium flux assay
ChEMBL 404 4 0 5 2.0 COc1ccc(F)cc1C1CCN([C@@H]2COC3(C2)CN(C(=O)C2COC2)C3)CC1 10.1021/acsmedchemlett.3c00331
76335135 103321 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
ChEMBL 359 6 2 4 2.2 CCOC(=O)N1C[C@@H]2CC[C@H](C1)[C@@H]2NCCNC(=O)c1ccccc1C 10.1016/j.bmcl.2012.03.088
CHEMBL3084448 103321 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
ChEMBL 359 6 2 4 2.2 CCOC(=O)N1C[C@@H]2CC[C@H](C1)[C@@H]2NCCNC(=O)c1ccccc1C 10.1016/j.bmcl.2012.03.088
76331523 103328 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
ChEMBL 351 6 2 5 1.9 CCOC(=O)N1C[C@@H]2CC[C@H](C1)[C@@H]2NCCNC(=O)c1cccs1 10.1016/j.bmcl.2012.03.088
CHEMBL3084456 103328 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
ChEMBL 351 6 2 5 1.9 CCOC(=O)N1C[C@@H]2CC[C@H](C1)[C@@H]2NCCNC(=O)c1cccs1 10.1016/j.bmcl.2012.03.088
62705330 76387 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
ChEMBL 407 5 1 6 2.2 O=C1COc2ccccc2N1CCCN1CCC(n2c(=O)[nH]c3cccnc32)CC1 10.1016/j.bmcl.2012.05.048
CHEMBL2059313 76387 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
ChEMBL 407 5 1 6 2.2 O=C1COc2ccccc2N1CCCN1CCC(n2c(=O)[nH]c3cccnc32)CC1 10.1016/j.bmcl.2012.05.048
127050528 141076 None 0 Rat Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation at rat muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation at rat muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 393 3 0 5 3.4 Cn1cc2cc(-c3cc(F)c(CN4CCn5nccc5C4=O)c(F)c3)ccc2n1 10.1016/j.bmcl.2016.04.083
CHEMBL3823424 141076 None 0 Rat Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation at rat muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation at rat muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 393 3 0 5 3.4 Cn1cc2cc(-c3cc(F)c(CN4CCn5nccc5C4=O)c(F)c3)ccc2n1 10.1016/j.bmcl.2016.04.083
127049133 141121 None 0 Rat Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation at rat muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation at rat muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 393 3 0 4 3.7 Cn1cc2c(-c3cc(F)c(CN4C=CC5=NCCN5C4=O)c(F)c3)cccc2n1 10.1016/j.bmcl.2016.04.083
CHEMBL3823999 141121 None 0 Rat Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation at rat muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation at rat muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 393 3 0 4 3.7 Cn1cc2c(-c3cc(F)c(CN4C=CC5=NCCN5C4=O)c(F)c3)cccc2n1 10.1016/j.bmcl.2016.04.083
126492034 161515 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 441 6 1 7 3.7 COc1cccnc1NC(=O)C1CN(Cc2ccc(-n3cccn3)cc2)c2ccccc2O1 10.1016/j.bmcl.2018.05.009
CHEMBL4126841 161515 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 441 6 1 7 3.7 COc1cccnc1NC(=O)C1CN(Cc2ccc(-n3cccn3)cc2)c2ccccc2O1 10.1016/j.bmcl.2018.05.009
139414122 164406 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assayPositive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 362 2 1 2 5.6 CC(C)[C@@H]1N=C(c2cccc(Cl)c2)c2cc(Cl)ccc2NC1=S 10.1016/j.bmcl.2017.11.008
CHEMBL4212268 164406 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assayPositive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 362 2 1 2 5.6 CC(C)[C@@H]1N=C(c2cccc(Cl)c2)c2cc(Cl)ccc2NC1=S 10.1016/j.bmcl.2017.11.008
118729455 117914 None 0 Human Functional pEC50 = 4.8 4.8 - 1
Agonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assayAgonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assay
ChEMBL 182 1 1 4 0.3 CN1CCC=C(C2=NOC(O)C2)C1 10.1016/j.bmcl.2015.02.012
CHEMBL3402922 117914 None 0 Human Functional pEC50 = 4.8 4.8 - 1
Agonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assayAgonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assay
ChEMBL 182 1 1 4 0.3 CN1CCC=C(C2=NOC(O)C2)C1 10.1016/j.bmcl.2015.02.012
145982858 165894 None 0 Rat Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assayPositive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assay
ChEMBL 432 5 1 6 4.2 Cn1ccc2c(Cc3ccc(-c4nccs4)cc3)cc(C(=O)NC3CCOCC3)nc21 10.1021/acsmedchemlett.8b00261
CHEMBL4248069 165894 None 0 Rat Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assayPositive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assay
ChEMBL 432 5 1 6 4.2 Cn1ccc2c(Cc3ccc(-c4nccs4)cc3)cc(C(=O)NC3CCOCC3)nc21 10.1021/acsmedchemlett.8b00261
145982858 165894 None 0 Rat Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assayPositive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assay
ChEMBL 432 5 1 6 4.2 Cn1ccc2c(Cc3ccc(-c4nccs4)cc3)cc(C(=O)NC3CCOCC3)nc21 10.1021/acsmedchemlett.8b00261
CHEMBL4248069 165894 None 0 Rat Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assayPositive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assay
ChEMBL 432 5 1 6 4.2 Cn1ccc2c(Cc3ccc(-c4nccs4)cc3)cc(C(=O)NC3CCOCC3)nc21 10.1021/acsmedchemlett.8b00261
127042157 137176 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human M1 receptor expressed in CHO cells assessed as acetylcholine-induced calcium mobilization by FLIPR assayPositive allosteric modulation of human M1 receptor expressed in CHO cells assessed as acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 401 6 1 6 3.2 O=C(NC[C@@H]1CCCO1)c1cn(Cc2ccc(-n3cccn3)cc2)c2cccnc12 10.1016/j.bmcl.2015.11.053
CHEMBL3747254 137176 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human M1 receptor expressed in CHO cells assessed as acetylcholine-induced calcium mobilization by FLIPR assayPositive allosteric modulation of human M1 receptor expressed in CHO cells assessed as acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 401 6 1 6 3.2 O=C(NC[C@@H]1CCCO1)c1cn(Cc2ccc(-n3cccn3)cc2)c2cccnc12 10.1016/j.bmcl.2015.11.053
145986351 165322 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as increase in ACh-induced intracellular calcium level preincubated for 10 mins followed by ACh addition measured every 2 secs for 80 secs by Fluo-4 dye-based FLIPR assayPositive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as increase in ACh-induced intracellular calcium level preincubated for 10 mins followed by ACh addition measured every 2 secs for 80 secs by Fluo-4 dye-based FLIPR assay
ChEMBL 452 6 4 8 0.7 Cn1c(CO)c(Cc2ccc(-n3cccn3)cc2)cc(C(=O)N[C@H]2CCC(O)C[C@@H]2O)c1=O 10.1016/j.bmcl.2018.04.054
CHEMBL4229133 165322 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as increase in ACh-induced intracellular calcium level preincubated for 10 mins followed by ACh addition measured every 2 secs for 80 secs by Fluo-4 dye-based FLIPR assayPositive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as increase in ACh-induced intracellular calcium level preincubated for 10 mins followed by ACh addition measured every 2 secs for 80 secs by Fluo-4 dye-based FLIPR assay
ChEMBL 452 6 4 8 0.7 Cn1c(CO)c(Cc2ccc(-n3cccn3)cc2)cc(C(=O)N[C@H]2CCC(O)C[C@@H]2O)c1=O 10.1016/j.bmcl.2018.04.054
118732895 120934 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Partial agonist activity at human muscarinic M1 acetylcholine receptor expressed in CHO cells assessed as increase in IP1 accumulation incubated for 30 mins by FRET based HTRF assayPartial agonist activity at human muscarinic M1 acetylcholine receptor expressed in CHO cells assessed as increase in IP1 accumulation incubated for 30 mins by FRET based HTRF assay
ChEMBL 561 12 1 6 4.3 C[N+](C)(CC#CCOC1=NOCC1)CCCCCCNC(=O)c1cn(Cc2ccccc2)c2c(F)cccc2c1=O 10.1021/jm500860w
CHEMBL3414841 120934 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Partial agonist activity at human muscarinic M1 acetylcholine receptor expressed in CHO cells assessed as increase in IP1 accumulation incubated for 30 mins by FRET based HTRF assayPartial agonist activity at human muscarinic M1 acetylcholine receptor expressed in CHO cells assessed as increase in IP1 accumulation incubated for 30 mins by FRET based HTRF assay
ChEMBL 561 12 1 6 4.3 C[N+](C)(CC#CCOC1=NOCC1)CCCCCCNC(=O)c1cn(Cc2ccccc2)c2c(F)cccc2c1=O 10.1021/jm500860w
CHEMBL3559128 120934 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Partial agonist activity at human muscarinic M1 acetylcholine receptor expressed in CHO cells assessed as increase in IP1 accumulation incubated for 30 mins by FRET based HTRF assayPartial agonist activity at human muscarinic M1 acetylcholine receptor expressed in CHO cells assessed as increase in IP1 accumulation incubated for 30 mins by FRET based HTRF assay
ChEMBL 561 12 1 6 4.3 C[N+](C)(CC#CCOC1=NOCC1)CCCCCCNC(=O)c1cn(Cc2ccccc2)c2c(F)cccc2c1=O 10.1021/jm500860w
145962181 161591 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 447 5 2 7 2.7 Cn1cc(-c2ccc(CN3CC(C(=O)N[C@H]4CCCC[C@@H]4O)Oc4ccccc43)cn2)cn1 10.1016/j.bmcl.2018.05.009
CHEMBL4128022 161591 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 447 5 2 7 2.7 Cn1cc(-c2ccc(CN3CC(C(=O)N[C@H]4CCCC[C@@H]4O)Oc4ccccc43)cn2)cn1 10.1016/j.bmcl.2018.05.009
76313419 103320 None 0 Human Functional pEC50 = 7.8 7.8 69 2
Agonist activity at human muscarinic M1 receptor by calcium mobilization assayAgonist activity at human muscarinic M1 receptor by calcium mobilization assay
ChEMBL 345 6 2 4 1.9 CCOC(=O)N1C[C@@H]2CC[C@H](C1)[C@@H]2NCCNC(=O)c1ccccc1 10.1016/j.bmcl.2012.03.088
CHEMBL3084447 103320 None 0 Human Functional pEC50 = 7.8 7.8 69 2
Agonist activity at human muscarinic M1 receptor by calcium mobilization assayAgonist activity at human muscarinic M1 receptor by calcium mobilization assay
ChEMBL 345 6 2 4 1.9 CCOC(=O)N1C[C@@H]2CC[C@H](C1)[C@@H]2NCCNC(=O)c1ccccc1 10.1016/j.bmcl.2012.03.088
135409468 2035 None 50 Human Functional pEC50 = 7.8 7.8 3 5
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 10.1021/jm100697g
333 2035 None 50 Human Functional pEC50 = 7.8 7.8 3 5
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 10.1021/jm100697g
CHEMBL845 2035 None 50 Human Functional pEC50 = 7.8 7.8 3 5
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 10.1021/jm100697g
122186861 123043 None 0 Rat Functional pEC50 = 7.8 7.8 -1 2
Positive allosteric modulation of rat muscarinic M1 receptor expressed in CHO cells assessed as basal and acetylcholine-stimulated Ca2+ level by FLIPR assayPositive allosteric modulation of rat muscarinic M1 receptor expressed in CHO cells assessed as basal and acetylcholine-stimulated Ca2+ level by FLIPR assay
ChEMBL 449 5 2 7 2.5 Cn1cc(-c2ccc(Cn3cc(C(=O)N[C@H]4COCC[C@@H]4O)c4ncccc43)cc2F)cn1 10.1021/acsmedchemlett.5b00185
CHEMBL3608421 123043 None 0 Rat Functional pEC50 = 7.8 7.8 -1 2
Positive allosteric modulation of rat muscarinic M1 receptor expressed in CHO cells assessed as basal and acetylcholine-stimulated Ca2+ level by FLIPR assayPositive allosteric modulation of rat muscarinic M1 receptor expressed in CHO cells assessed as basal and acetylcholine-stimulated Ca2+ level by FLIPR assay
ChEMBL 449 5 2 7 2.5 Cn1cc(-c2ccc(Cn3cc(C(=O)N[C@H]4COCC[C@@H]4O)c4ncccc43)cc2F)cn1 10.1021/acsmedchemlett.5b00185
122186862 123044 None 0 Rat Functional pEC50 = 7.8 7.8 -1 2
Positive allosteric modulation of rat muscarinic M1 receptor expressed in CHO cells assessed as basal and acetylcholine-stimulated Ca2+ level by FLIPR assayPositive allosteric modulation of rat muscarinic M1 receptor expressed in CHO cells assessed as basal and acetylcholine-stimulated Ca2+ level by FLIPR assay
ChEMBL 408 5 3 6 1.3 CNC(=O)c1ccc(Cn2cc(C(=O)N[C@H]3COCC[C@@H]3O)c3ncccc32)cc1 10.1021/acsmedchemlett.5b00185
CHEMBL3608422 123044 None 0 Rat Functional pEC50 = 7.8 7.8 -1 2
Positive allosteric modulation of rat muscarinic M1 receptor expressed in CHO cells assessed as basal and acetylcholine-stimulated Ca2+ level by FLIPR assayPositive allosteric modulation of rat muscarinic M1 receptor expressed in CHO cells assessed as basal and acetylcholine-stimulated Ca2+ level by FLIPR assay
ChEMBL 408 5 3 6 1.3 CNC(=O)c1ccc(Cn2cc(C(=O)N[C@H]3COCC[C@@H]3O)c3ncccc32)cc1 10.1021/acsmedchemlett.5b00185
44207907 16734 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 331 5 1 4 1.4 CC(=O)NC1CCN(CCCN2C(=O)COc3ccccc32)CC1 10.1021/jm100697g
CHEMBL1243202 16734 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 331 5 1 4 1.4 CC(=O)NC1CCN(CCCN2C(=O)COc3ccccc32)CC1 10.1021/jm100697g
11124824 32255 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.
ChEMBL 522 12 0 10 5.7 CN1CCC=C(c2nsnc2SCCCCCCCSc2nsnc2C2=CCCN(C)C2)C1 10.1021/jm0102405
CHEMBL140985 32255 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.
ChEMBL 522 12 0 10 5.7 CN1CCC=C(c2nsnc2SCCCCCCCSc2nsnc2C2=CCCN(C)C2)C1 10.1021/jm0102405
145985065 165825 None 0 Human Functional pEC50 = 6.8 6.8 2 2
Positive allosteric modulation of human M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assayPositive allosteric modulation of human M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assay
ChEMBL 443 5 2 6 3.6 Cn1ccc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCCC[C@H]4O)nc4c3ccn4C)cc2)n1 10.1021/acsmedchemlett.8b00261
CHEMBL4246159 165825 None 0 Human Functional pEC50 = 6.8 6.8 2 2
Positive allosteric modulation of human M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assayPositive allosteric modulation of human M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assay
ChEMBL 443 5 2 6 3.6 Cn1ccc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCCC[C@H]4O)nc4c3ccn4C)cc2)n1 10.1021/acsmedchemlett.8b00261
826706 41762 None 38 Human Functional pEC50 = 6.8 6.8 70 2
Positive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assayPositive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 286 1 1 2 4.2 SC1=Nc2ccc(Cl)cc2C(c2ccccc2)=NC1 10.1016/j.bmcl.2017.11.008
CHEMBL1492697 41762 None 38 Human Functional pEC50 = 6.8 6.8 70 2
Positive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assayPositive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 286 1 1 2 4.2 SC1=Nc2ccc(Cl)cc2C(c2ccccc2)=NC1 10.1016/j.bmcl.2017.11.008
145985065 165825 None 0 Rat Functional pEC50 = 6.8 6.8 -2 2
Positive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assayPositive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assay
ChEMBL 443 5 2 6 3.6 Cn1ccc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCCC[C@H]4O)nc4c3ccn4C)cc2)n1 10.1021/acsmedchemlett.8b00261
CHEMBL4246159 165825 None 0 Rat Functional pEC50 = 6.8 6.8 -2 2
Positive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assayPositive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assay
ChEMBL 443 5 2 6 3.6 Cn1ccc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCCC[C@H]4O)nc4c3ccn4C)cc2)n1 10.1021/acsmedchemlett.8b00261
44578975 189812 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
ChEMBL 458 4 1 4 4.9 O=c1[nH]c2cc(Cl)ccc2n1C1CCN(C2CCN(Cc3ccccc3Cl)CC2)CC1 10.1016/j.bmcl.2008.09.023
CHEMBL515489 189812 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
ChEMBL 458 4 1 4 4.9 O=c1[nH]c2cc(Cl)ccc2n1C1CCN(C2CCN(Cc3ccccc3Cl)CC2)CC1 10.1016/j.bmcl.2008.09.023
146487745 180938 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Positive allosteric modulation of recombinant human muscarinic M1 receptor co-expressing pCRE-Luc reporter gene in CHO cells assessed as stimulation of luciferase activity in presence of acetylcholine substrate measured after 4 hrs by luciferase reporter gene assayPositive allosteric modulation of recombinant human muscarinic M1 receptor co-expressing pCRE-Luc reporter gene in CHO cells assessed as stimulation of luciferase activity in presence of acetylcholine substrate measured after 4 hrs by luciferase reporter gene assay
ChEMBL 413 5 1 4 3.6 O=C(NCC1CCCO1)c1cc(Cc2ccc(Br)cc2)c2cccn2n1 10.1021/acsmedchemlett.1c00118
CHEMBL4756974 180938 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Positive allosteric modulation of recombinant human muscarinic M1 receptor co-expressing pCRE-Luc reporter gene in CHO cells assessed as stimulation of luciferase activity in presence of acetylcholine substrate measured after 4 hrs by luciferase reporter gene assayPositive allosteric modulation of recombinant human muscarinic M1 receptor co-expressing pCRE-Luc reporter gene in CHO cells assessed as stimulation of luciferase activity in presence of acetylcholine substrate measured after 4 hrs by luciferase reporter gene assay
ChEMBL 413 5 1 4 3.6 O=C(NCC1CCCO1)c1cc(Cc2ccc(Br)cc2)c2cccn2n1 10.1021/acsmedchemlett.1c00118
145985065 165825 None 0 Human Functional pEC50 = 6.7 6.7 2 2
Agonist activity at human M1 receptor expressed in CHO cells assessed as increase in calcium mobilization measured after 2.5 mins by Fluo-4-AM dye based assayAgonist activity at human M1 receptor expressed in CHO cells assessed as increase in calcium mobilization measured after 2.5 mins by Fluo-4-AM dye based assay
ChEMBL 443 5 2 6 3.6 Cn1ccc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCCC[C@H]4O)nc4c3ccn4C)cc2)n1 10.1021/acsmedchemlett.8b00261
CHEMBL4246159 165825 None 0 Human Functional pEC50 = 6.7 6.7 2 2
Agonist activity at human M1 receptor expressed in CHO cells assessed as increase in calcium mobilization measured after 2.5 mins by Fluo-4-AM dye based assayAgonist activity at human M1 receptor expressed in CHO cells assessed as increase in calcium mobilization measured after 2.5 mins by Fluo-4-AM dye based assay
ChEMBL 443 5 2 6 3.6 Cn1ccc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCCC[C@H]4O)nc4c3ccn4C)cc2)n1 10.1021/acsmedchemlett.8b00261
145985065 165825 None 0 Rat Functional pEC50 = 6.7 6.7 -2 2
Positive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assayPositive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assay
ChEMBL 443 5 2 6 3.6 Cn1ccc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCCC[C@H]4O)nc4c3ccn4C)cc2)n1 10.1021/acsmedchemlett.8b00261
CHEMBL4246159 165825 None 0 Rat Functional pEC50 = 6.7 6.7 -2 2
Positive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assayPositive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assay
ChEMBL 443 5 2 6 3.6 Cn1ccc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCCC[C@H]4O)nc4c3ccn4C)cc2)n1 10.1021/acsmedchemlett.8b00261
44303293 203883 None 0 Human Functional pEC50 = 5.7 5.7 -3 3
Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.
ChEMBL 393 3 0 5 3.8 Clc1cc(Cl)cc(C#CCSc2nsnc2C23CN4CC2C3C4)c1 10.1021/jm9910019
CHEMBL60479 203883 None 0 Human Functional pEC50 = 5.7 5.7 -3 3
Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.
ChEMBL 393 3 0 5 3.8 Clc1cc(Cl)cc(C#CCSc2nsnc2C23CN4CC2C3C4)c1 10.1021/jm9910019
146487799 182348 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Positive allosteric modulation of recombinant human muscarinic M1 receptor co-expressing pCRE-Luc reporter gene in CHO cells assessed as stimulation of luciferase activity in presence of acetylcholine substrate measured after 4 hrs by luciferase reporter gene assayPositive allosteric modulation of recombinant human muscarinic M1 receptor co-expressing pCRE-Luc reporter gene in CHO cells assessed as stimulation of luciferase activity in presence of acetylcholine substrate measured after 4 hrs by luciferase reporter gene assay
ChEMBL 415 5 1 6 3.2 Cn1cc(-c2ccc(Cc3cc(C(=O)NC4CCOCC4)nn4cccc34)cc2)cn1 10.1021/acsmedchemlett.1c00118
CHEMBL4783540 182348 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Positive allosteric modulation of recombinant human muscarinic M1 receptor co-expressing pCRE-Luc reporter gene in CHO cells assessed as stimulation of luciferase activity in presence of acetylcholine substrate measured after 4 hrs by luciferase reporter gene assayPositive allosteric modulation of recombinant human muscarinic M1 receptor co-expressing pCRE-Luc reporter gene in CHO cells assessed as stimulation of luciferase activity in presence of acetylcholine substrate measured after 4 hrs by luciferase reporter gene assay
ChEMBL 415 5 1 6 3.2 Cn1cc(-c2ccc(Cc3cc(C(=O)NC4CCOCC4)nn4cccc34)cc2)cn1 10.1021/acsmedchemlett.1c00118
122191003 123680 None 0 Human Functional pEC50 = 6.7 6.7 1 2
Agonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 509 6 3 3 4.9 C/C(=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(Br)cc1)[C@H](O)C2)NCCc1ccc(F)cc1 10.1016/j.bmcl.2015.08.011
CHEMBL3618446 123680 None 0 Human Functional pEC50 = 6.7 6.7 1 2
Agonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 509 6 3 3 4.9 C/C(=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(Br)cc1)[C@H](O)C2)NCCc1ccc(F)cc1 10.1016/j.bmcl.2015.08.011
145970842 165102 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Positive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as increase in ACh-induced intracellular calcium level preincubated for 10 mins followed by ACh addition measured every 2 secs for 80 secs by Fluo-4 dye-based FLIPR assayPositive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as increase in ACh-induced intracellular calcium level preincubated for 10 mins followed by ACh addition measured every 2 secs for 80 secs by Fluo-4 dye-based FLIPR assay
ChEMBL 459 6 2 8 2.2 Cn1ccc(-c2ccc(Cn3cc(C(=O)N[C@H]4CCOC[C@@H]4O)c4nc(C=O)ccc43)cc2)n1 10.1016/j.bmcl.2018.04.054
CHEMBL4225919 165102 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Positive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as increase in ACh-induced intracellular calcium level preincubated for 10 mins followed by ACh addition measured every 2 secs for 80 secs by Fluo-4 dye-based FLIPR assayPositive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as increase in ACh-induced intracellular calcium level preincubated for 10 mins followed by ACh addition measured every 2 secs for 80 secs by Fluo-4 dye-based FLIPR assay
ChEMBL 459 6 2 8 2.2 Cn1ccc(-c2ccc(Cn3cc(C(=O)N[C@H]4CCOC[C@@H]4O)c4nc(C=O)ccc43)cc2)n1 10.1016/j.bmcl.2018.04.054
139414055 164373 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assayPositive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 344 2 2 3 4.1 CC(C)(O)C1N=C(c2ccccc2)c2cc(Cl)ccc2NC1=S 10.1016/j.bmcl.2017.11.008
CHEMBL4211802 164373 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assayPositive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 344 2 2 3 4.1 CC(C)(O)C1N=C(c2ccccc2)c2cc(Cl)ccc2NC1=S 10.1016/j.bmcl.2017.11.008
127038317 137151 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Positive allosteric modulation of human M1 receptor expressed in CHO cells assessed as acetylcholine-induced calcium mobilization by FLIPR assayPositive allosteric modulation of human M1 receptor expressed in CHO cells assessed as acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 400 4 2 5 3.7 O=C(N[C@H]1CCCC[C@@H]1O)c1cn(Cc2ccc3ncccc3c2)c2cccnc12 10.1016/j.bmcl.2015.11.053
CHEMBL3746904 137151 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Positive allosteric modulation of human M1 receptor expressed in CHO cells assessed as acetylcholine-induced calcium mobilization by FLIPR assayPositive allosteric modulation of human M1 receptor expressed in CHO cells assessed as acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 400 4 2 5 3.7 O=C(N[C@H]1CCCC[C@@H]1O)c1cn(Cc2ccc3ncccc3c2)c2cccnc12 10.1016/j.bmcl.2015.11.053
44475948 61809 None 0 Rat Functional pEC50 = 5.7 5.7 - 1
Allosteric modulation at rat M1 receptor expressed in CHO cells by calcium mobilization assayAllosteric modulation at rat M1 receptor expressed in CHO cells by calcium mobilization assay
ChEMBL 511 7 2 7 4.1 Cc1cc(NC(=O)CS(=O)(=O)c2cn(Cc3cccc(-c4cn[nH]c4)c3)c3cc(F)cc(F)c23)no1 10.1016/j.bmcl.2010.12.015
CHEMBL1773111 61809 None 0 Rat Functional pEC50 = 5.7 5.7 - 1
Allosteric modulation at rat M1 receptor expressed in CHO cells by calcium mobilization assayAllosteric modulation at rat M1 receptor expressed in CHO cells by calcium mobilization assay
ChEMBL 511 7 2 7 4.1 Cc1cc(NC(=O)CS(=O)(=O)c2cn(Cc3cccc(-c4cn[nH]c4)c3)c3cc(F)cc(F)c23)no1 10.1016/j.bmcl.2010.12.015
145963718 161733 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 434 5 2 7 1.9 O=C(N[C@H]1CCOC[C@@H]1O)C1CN(Cc2ccc(-n3cccn3)cc2)c2ccccc2O1 10.1016/j.bmcl.2018.05.009
CHEMBL4130084 161733 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 434 5 2 7 1.9 O=C(N[C@H]1CCOC[C@@H]1O)C1CN(Cc2ccc(-n3cccn3)cc2)c2ccccc2O1 10.1016/j.bmcl.2018.05.009
139414015 163670 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Positive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assayPositive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 314 2 1 2 4.7 CC[C@@H]1N=C(c2ccccc2)c2cc(Cl)ccc2NC1=S 10.1016/j.bmcl.2017.11.008
CHEMBL4203218 163670 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Positive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assayPositive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 314 2 1 2 4.7 CC[C@@H]1N=C(c2ccccc2)c2cc(Cl)ccc2NC1=S 10.1016/j.bmcl.2017.11.008
169450433 196432 None 2 Human Functional pEC50 = 7.7 7.7 2 2
Activation of human muscarinic M1 receptor expressed in HEK293 cells incubated for 3 mins by Calcium flux assayActivation of human muscarinic M1 receptor expressed in HEK293 cells incubated for 3 mins by Calcium flux assay
ChEMBL 356 4 0 3 3.7 CCOc1ccccc1C1CCN([C@@H]2CCC3(C2)CN(C(C)=O)C3)CC1 10.1021/acsmedchemlett.3c00331
CHEMBL5423866 196432 None 2 Human Functional pEC50 = 7.7 7.7 2 2
Activation of human muscarinic M1 receptor expressed in HEK293 cells incubated for 3 mins by Calcium flux assayActivation of human muscarinic M1 receptor expressed in HEK293 cells incubated for 3 mins by Calcium flux assay
ChEMBL 356 4 0 3 3.7 CCOc1ccccc1C1CCN([C@@H]2CCC3(C2)CN(C(C)=O)C3)CC1 10.1021/acsmedchemlett.3c00331
44207904 16748 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 361 6 1 3 2.5 CCC(=O)NC1CCN(CCCN2C(=O)CCc3c(F)cccc32)CC1 10.1021/jm100697g
CHEMBL1243328 16748 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 361 6 1 3 2.5 CCC(=O)NC1CCN(CCCN2C(=O)CCc3c(F)cccc32)CC1 10.1021/jm100697g
46891075 6815 None 0 Human Functional pEC50 = 7.7 7.7 125 2
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 360 4 2 2 4.1 C[C@H]1CNCC[C@H]1CNC(=O)c1c(F)cccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.127
CHEMBL1083926 6815 None 0 Human Functional pEC50 = 7.7 7.7 125 2
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 360 4 2 2 4.1 C[C@H]1CNCC[C@H]1CNC(=O)c1c(F)cccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.127
46871666 7071 None 0 Human Functional pEC50 = 7.7 7.7 63 4
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 342 4 2 2 4.0 CC1CNCCC1CNC(=O)c1ccccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.128
CHEMBL1084993 7071 None 0 Human Functional pEC50 = 7.7 7.7 63 4
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 342 4 2 2 4.0 CC1CNCCC1CNC(=O)c1ccccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.128
145963718 161733 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 434 5 2 7 1.9 O=C(N[C@H]1CCOC[C@@H]1O)C1CN(Cc2ccc(-n3cccn3)cc2)c2ccccc2O1 10.1016/j.bmcl.2018.05.009
CHEMBL4130084 161733 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 434 5 2 7 1.9 O=C(N[C@H]1CCOC[C@@H]1O)C1CN(Cc2ccc(-n3cccn3)cc2)c2ccccc2O1 10.1016/j.bmcl.2018.05.009
70689865 74374 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
ChEMBL 381 6 2 4 2.4 CCOC(=O)N1[C@H]2CC[C@@H]1C[C@@H](NCCNC(=O)c1cc(F)cc(F)c1)C2 10.1016/j.bmcl.2012.03.088
CHEMBL2024423 74374 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
ChEMBL 381 6 2 4 2.4 CCOC(=O)N1[C@H]2CC[C@@H]1C[C@@H](NCCNC(=O)c1cc(F)cc(F)c1)C2 10.1016/j.bmcl.2012.03.088
10397356 120780 None 0 Human Functional pEC50 = 5.7 5.7 -1 3
Effective concentration for HMPA (human muscarinic inositol phosphate accumulation) activity measured in CHO cells expressing Muscarinic acetylcholine receptor M1Effective concentration for HMPA (human muscarinic inositol phosphate accumulation) activity measured in CHO cells expressing Muscarinic acetylcholine receptor M1
ChEMBL 178 2 0 3 0.7 CC#CCO/N=C1\CN2CCC1C2 10.1016/S0960-894X(00)80538-7
CHEMBL354738 120780 None 0 Human Functional pEC50 = 5.7 5.7 -1 3
Effective concentration for HMPA (human muscarinic inositol phosphate accumulation) activity measured in CHO cells expressing Muscarinic acetylcholine receptor M1Effective concentration for HMPA (human muscarinic inositol phosphate accumulation) activity measured in CHO cells expressing Muscarinic acetylcholine receptor M1
ChEMBL 178 2 0 3 0.7 CC#CCO/N=C1\CN2CCC1C2 10.1016/S0960-894X(00)80538-7
71555066 141051 None 19 Human Functional pEC50 = 5.7 5.7 1 2
Positive allosteric modulation at human muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation at human muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 322 3 0 4 2.8 Cn1cc(-c2ccc(CN3Cc4ncccc4C3=O)c(F)c2)cn1 10.1016/j.bmcl.2016.04.083
CHEMBL3823130 141051 None 19 Human Functional pEC50 = 5.7 5.7 1 2
Positive allosteric modulation at human muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation at human muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 322 3 0 4 2.8 Cn1cc(-c2ccc(CN3Cc4ncccc4C3=O)c(F)c2)cn1 10.1016/j.bmcl.2016.04.083
145961193 161744 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 432 7 2 6 2.9 CC(O)(CNC(=O)C1CN(Cc2ccc(-n3cccn3)cc2)c2ccccc2O1)C1CC1 10.1016/j.bmcl.2018.05.009
CHEMBL4130287 161744 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 432 7 2 6 2.9 CC(O)(CNC(=O)C1CN(Cc2ccc(-n3cccn3)cc2)c2ccccc2O1)C1CC1 10.1016/j.bmcl.2018.05.009
145961193 161744 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 432 7 2 6 2.9 CC(O)(CNC(=O)C1CN(Cc2ccc(-n3cccn3)cc2)c2ccccc2O1)C1CC1 10.1016/j.bmcl.2018.05.009
CHEMBL4130287 161744 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 432 7 2 6 2.9 CC(O)(CNC(=O)C1CN(Cc2ccc(-n3cccn3)cc2)c2ccccc2O1)C1CC1 10.1016/j.bmcl.2018.05.009
146216704 186299 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL 395 3 0 4 4.7 Cn1cc2c(-c3cc(F)c(CN4Cc5sccc5C4=O)c(F)c3)cccc2n1 10.1016/j.bmcl.2021.128193
CHEMBL4872836 186299 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL 395 3 0 4 4.7 Cn1cc2c(-c3cc(F)c(CN4Cc5sccc5C4=O)c(F)c3)cccc2n1 10.1016/j.bmcl.2021.128193
118724607 116523 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assay
ChEMBL 491 5 0 6 5.6 Cc1ccc(Cn2nc3c4ccccc4n(Cc4ccc(-c5cnn(C)c5)cc4F)cc-3c2=O)c(C)c1 10.1016/j.bmcl.2014.11.011
CHEMBL3360949 116523 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assay
ChEMBL 491 5 0 6 5.6 Cc1ccc(Cn2nc3c4ccccc4n(Cc4ccc(-c5cnn(C)c5)cc4F)cc-3c2=O)c(C)c1 10.1016/j.bmcl.2014.11.011
118724607 116523 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assay
ChEMBL 491 5 0 6 5.6 Cc1ccc(Cn2nc3c4ccccc4n(Cc4ccc(-c5cnn(C)c5)cc4F)cc-3c2=O)c(C)c1 10.1016/j.bmcl.2014.11.011
CHEMBL3360949 116523 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assay
ChEMBL 491 5 0 6 5.6 Cc1ccc(Cn2nc3c4ccccc4n(Cc4ccc(-c5cnn(C)c5)cc4F)cc-3c2=O)c(C)c1 10.1016/j.bmcl.2014.11.011
122190998 123675 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 507 6 3 4 4.7 COc1cccc(CN/C(C)=N/c2ccc3c(c2)[C@@H](NC(=O)c2ccc(Br)cc2)[C@H](O)C3)c1 10.1016/j.bmcl.2015.08.011
CHEMBL3618441 123675 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 507 6 3 4 4.7 COc1cccc(CN/C(C)=N/c2ccc3c(c2)[C@@H](NC(=O)c2ccc(Br)cc2)[C@H](O)C3)c1 10.1016/j.bmcl.2015.08.011
42598586 16130 None 0 Human Functional pEC50 = 6.7 6.7 1 4
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 450 6 0 7 3.8 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(S(=O)(=O)CC)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223938 16130 None 0 Human Functional pEC50 = 6.7 6.7 1 4
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 450 6 0 7 3.8 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(S(=O)(=O)CC)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
9913341 82189 None 4 Human Functional pEC50 = 5.7 5.7 -630 3
Agonist activity at human M1 receptor E170K mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M1 receptor E170K mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 487 16 0 13 1.6 COc1nsnc1OCCOCCOCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0606995
CHEMBL216927 82189 None 4 Human Functional pEC50 = 5.7 5.7 -630 3
Agonist activity at human M1 receptor E170K mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M1 receptor E170K mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 487 16 0 13 1.6 COc1nsnc1OCCOCCOCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0606995
CHEMBL553058 82189 None 4 Human Functional pEC50 = 5.7 5.7 -630 3
Agonist activity at human M1 receptor E170K mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M1 receptor E170K mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 487 16 0 13 1.6 COc1nsnc1OCCOCCOCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0606995
10104167 2059 None 2 Human Functional pEC50 = 8.7 8.7 -14 3
Partial agonist activity at human muscarinic M1 acetylcholine receptor expressed in CHO cells assessed as increase in IP1 accumulation incubated for 30 mins by FRET based HTRF assayPartial agonist activity at human muscarinic M1 acetylcholine receptor expressed in CHO cells assessed as increase in IP1 accumulation incubated for 30 mins by FRET based HTRF assay
ChEMBL 197 2 0 3 0.4 C[N+](CC#CCOC1=NOCC1)(C)C 10.1021/jm500860w
6937 2059 None 2 Human Functional pEC50 = 8.7 8.7 -14 3
Partial agonist activity at human muscarinic M1 acetylcholine receptor expressed in CHO cells assessed as increase in IP1 accumulation incubated for 30 mins by FRET based HTRF assayPartial agonist activity at human muscarinic M1 acetylcholine receptor expressed in CHO cells assessed as increase in IP1 accumulation incubated for 30 mins by FRET based HTRF assay
ChEMBL 197 2 0 3 0.4 C[N+](CC#CCOC1=NOCC1)(C)C 10.1021/jm500860w
CHEMBL3121473 2059 None 2 Human Functional pEC50 = 8.7 8.7 -14 3
Partial agonist activity at human muscarinic M1 acetylcholine receptor expressed in CHO cells assessed as increase in IP1 accumulation incubated for 30 mins by FRET based HTRF assayPartial agonist activity at human muscarinic M1 acetylcholine receptor expressed in CHO cells assessed as increase in IP1 accumulation incubated for 30 mins by FRET based HTRF assay
ChEMBL 197 2 0 3 0.4 C[N+](CC#CCOC1=NOCC1)(C)C 10.1021/jm500860w
22745278 187169 None 1 Human Functional pEC50 = 8.7 8.7 4 5
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
ChEMBL 372 3 1 5 2.6 CCOC(=O)N1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1 10.1016/j.bmcl.2008.09.023
CHEMBL491209 187169 None 1 Human Functional pEC50 = 8.7 8.7 4 5
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
ChEMBL 372 3 1 5 2.6 CCOC(=O)N1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1 10.1016/j.bmcl.2008.09.023
129456 209630 None 12 Rat Functional pEC50 = 8.6 8.6 -8 2
Compound was tested in vitro for depolarizing response on the rat superior cervical ganglion (mediated by Muscarinic M1 receptor)Compound was tested in vitro for depolarizing response on the rat superior cervical ganglion (mediated by Muscarinic M1 receptor)
ChEMBL 179 1 0 4 0.8 Cc1noc(C2CN3CCC2C3)n1 10.1021/jm00083a016
CHEMBL92421 209630 None 12 Rat Functional pEC50 = 8.6 8.6 -8 2
Compound was tested in vitro for depolarizing response on the rat superior cervical ganglion (mediated by Muscarinic M1 receptor)Compound was tested in vitro for depolarizing response on the rat superior cervical ganglion (mediated by Muscarinic M1 receptor)
ChEMBL 179 1 0 4 0.8 Cc1noc(C2CN3CCC2C3)n1 10.1021/jm00083a016
44303314 100987 None 0 Human Functional pEC50 = 8.6 8.6 10 3
Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.
ChEMBL 343 3 0 5 2.6 Fc1cccc(C#CCSc2nsnc2C23CN4CC2C3C4)c1 10.1021/jm9910019
CHEMBL293982 100987 None 0 Human Functional pEC50 = 8.6 8.6 10 3
Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.
ChEMBL 343 3 0 5 2.6 Fc1cccc(C#CCSc2nsnc2C23CN4CC2C3C4)c1 10.1021/jm9910019
42598360 16111 None 0 Human Functional pEC50 = 8.6 8.6 63 5
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 388 5 0 6 4.0 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(OC)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223862 16111 None 0 Human Functional pEC50 = 8.6 8.6 63 5
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 388 5 0 6 4.0 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(OC)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
42599071 16131 None 0 Human Functional pEC50 = 8.6 8.6 125 5
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 450 6 0 7 3.8 CCCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(S(C)(=O)=O)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223939 16131 None 0 Human Functional pEC50 = 8.6 8.6 125 5
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 450 6 0 7 3.8 CCCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(S(C)(=O)=O)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
25230693 16132 None 0 Human Functional pEC50 = 8.6 8.6 63 5
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 402 6 0 6 3.9 COCCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223940 16132 None 0 Human Functional pEC50 = 8.6 8.6 63 5
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 402 6 0 6 3.9 COCCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
62705175 76384 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
ChEMBL 405 5 1 5 2.7 O=C1CCc2cccnc2N1CCCN1CCC(n2c(=O)[nH]c3ccccc32)CC1 10.1016/j.bmcl.2012.05.048
CHEMBL2059310 76384 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
ChEMBL 405 5 1 5 2.7 O=C1CCc2cccnc2N1CCCN1CCC(n2c(=O)[nH]c3ccccc32)CC1 10.1016/j.bmcl.2012.05.048
46930342 16757 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 361 6 1 3 2.5 CCC(=O)NC1CCN(CCCN2C(=O)CCc3ccc(F)cc32)CC1 10.1021/jm100697g
CHEMBL1243358 16757 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 361 6 1 3 2.5 CCC(=O)NC1CCN(CCCN2C(=O)CCc3ccc(F)cc32)CC1 10.1021/jm100697g
44207447 16763 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 379 6 1 3 2.6 CCC(=O)NC1CCN(CCCN2C(=O)CCc3cc(F)c(F)cc32)CC1 10.1021/jm100697g
CHEMBL1243387 16763 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 379 6 1 3 2.6 CCC(=O)NC1CCN(CCCN2C(=O)CCc3cc(F)c(F)cc32)CC1 10.1021/jm100697g
162646208 179580 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Positive allosteric modulation of human muscarinic M1 receptor stably expressed in CHO cells assessed as increase in Ach-induced intracellular calcium level preincubated for 10 mins followed by addition of Ach at EC20 concentration by Fluo-8AM dye based FLIPR TETRA methodPositive allosteric modulation of human muscarinic M1 receptor stably expressed in CHO cells assessed as increase in Ach-induced intracellular calcium level preincubated for 10 mins followed by addition of Ach at EC20 concentration by Fluo-8AM dye based FLIPR TETRA method
ChEMBL 422 5 2 7 1.4 Cc1c(Cc2ccc(-n3cccn3)cc2)cc(C(=O)N[C@H]2CCOC[C@@H]2O)c(=O)n1C 10.1021/acs.jmedchem.6b00544
CHEMBL4740865 179580 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Positive allosteric modulation of human muscarinic M1 receptor stably expressed in CHO cells assessed as increase in Ach-induced intracellular calcium level preincubated for 10 mins followed by addition of Ach at EC20 concentration by Fluo-8AM dye based FLIPR TETRA methodPositive allosteric modulation of human muscarinic M1 receptor stably expressed in CHO cells assessed as increase in Ach-induced intracellular calcium level preincubated for 10 mins followed by addition of Ach at EC20 concentration by Fluo-8AM dye based FLIPR TETRA method
ChEMBL 422 5 2 7 1.4 Cc1c(Cc2ccc(-n3cccn3)cc2)cc(C(=O)N[C@H]2CCOC[C@@H]2O)c(=O)n1C 10.1021/acs.jmedchem.6b00544
11725107 100667 None 0 Human Functional pEC50 = 7.7 7.7 1 3
Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.
ChEMBL 345 3 0 5 2.1 Fc1cc(F)cc(C#CCOc2nsnc2C23CN4CC2C3C4)c1 10.1021/jm9910019
CHEMBL291872 100667 None 0 Human Functional pEC50 = 7.7 7.7 1 3
Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.
ChEMBL 345 3 0 5 2.1 Fc1cc(F)cc(C#CCOc2nsnc2C23CN4CC2C3C4)c1 10.1021/jm9910019
59654579 123674 None 0 Human Functional pEC50 = 7.7 7.7 3 3
Agonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 495 5 3 3 4.8 C/C(=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(Br)cc1)[C@H](O)C2)NCc1ccc(F)cc1 10.1016/j.bmcl.2015.08.011
CHEMBL3618440 123674 None 0 Human Functional pEC50 = 7.7 7.7 3 3
Agonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 495 5 3 3 4.8 C/C(=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(Br)cc1)[C@H](O)C2)NCc1ccc(F)cc1 10.1016/j.bmcl.2015.08.011
76335136 103324 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
ChEMBL 381 6 2 4 2.2 CCOC(=O)N1C[C@@H]2CC[C@H](C1)[C@@H]2NCCNC(=O)c1cc(F)cc(F)c1 10.1016/j.bmcl.2012.03.088
CHEMBL3084451 103324 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
ChEMBL 381 6 2 4 2.2 CCOC(=O)N1C[C@@H]2CC[C@H](C1)[C@@H]2NCCNC(=O)c1cc(F)cc(F)c1 10.1016/j.bmcl.2012.03.088
25010776 55971 None 1 Rat Functional pEC50 = 6.7 6.7 -1 5
Agonist activity at rat muscarinic M1 receptor expressed in CHO cellsAgonist activity at rat muscarinic M1 receptor expressed in CHO cells
ChEMBL 333 6 2 4 1.9 CCOC(=O)N1CCC(NCCNC(=O)c2ccccc2C)CC1 10.1016/j.bmcl.2011.08.084
CHEMBL1559151 55971 None 1 Rat Functional pEC50 = 6.7 6.7 -1 5
Agonist activity at rat muscarinic M1 receptor expressed in CHO cellsAgonist activity at rat muscarinic M1 receptor expressed in CHO cells
ChEMBL 333 6 2 4 1.9 CCOC(=O)N1CCC(NCCNC(=O)c2ccccc2C)CC1 10.1016/j.bmcl.2011.08.084
CHEMBL1624037 55971 None 1 Rat Functional pEC50 = 6.7 6.7 -1 5
Agonist activity at rat muscarinic M1 receptor expressed in CHO cellsAgonist activity at rat muscarinic M1 receptor expressed in CHO cells
ChEMBL 333 6 2 4 1.9 CCOC(=O)N1CCC(NCCNC(=O)c2ccccc2C)CC1 10.1016/j.bmcl.2011.08.084
3652 4097 None 50 Human Functional pEC50 = 6.7 6.7 -18 15
Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm970125n
57 4097 None 50 Human Functional pEC50 = 6.7 6.7 -18 15
Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm970125n
60809 4097 None 50 Human Functional pEC50 = 6.7 6.7 -18 15
Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm970125n
60809.0 4097 None 50 Human Functional pEC50 = 6.7 6.7 -18 15
Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm970125n
CHEMBL21536 4097 None 50 Human Functional pEC50 = 6.7 6.7 -18 15
Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm970125n
DB15357 4097 None 50 Human Functional pEC50 = 6.7 6.7 -18 15
Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm970125n
650899 54430 None 6 Rat Functional pEC50 = 6.7 6.7 4 5
Partial agonist activity at rat muscarinic M1 receptor expressed in CHO cells calcium responsePartial agonist activity at rat muscarinic M1 receptor expressed in CHO cells calcium response
ChEMBL 319 6 2 4 1.6 CCOC(=O)N1CCC(NCCNC(=O)c2ccccc2)CC1 10.1016/j.bmcl.2012.10.132
CHEMBL1535797 54430 None 6 Rat Functional pEC50 = 6.7 6.7 4 5
Partial agonist activity at rat muscarinic M1 receptor expressed in CHO cells calcium responsePartial agonist activity at rat muscarinic M1 receptor expressed in CHO cells calcium response
ChEMBL 319 6 2 4 1.6 CCOC(=O)N1CCC(NCCNC(=O)c2ccccc2)CC1 10.1016/j.bmcl.2012.10.132
CHEMBL1609153 54430 None 6 Rat Functional pEC50 = 6.7 6.7 4 5
Partial agonist activity at rat muscarinic M1 receptor expressed in CHO cells calcium responsePartial agonist activity at rat muscarinic M1 receptor expressed in CHO cells calcium response
ChEMBL 319 6 2 4 1.6 CCOC(=O)N1CCC(NCCNC(=O)c2ccccc2)CC1 10.1016/j.bmcl.2012.10.132
71737672 2576 None 21 Rat Functional pEC50 = 5.7 5.7 -3 6
Activity at rat muscarinic acetylcholine receptor subtype 1 expressed in CHO cells by calcium mobilization assayActivity at rat muscarinic acetylcholine receptor subtype 1 expressed in CHO cells by calcium mobilization assay
ChEMBL 494 6 1 4 4.0 CCN(C(=O)C1CCN(CC1)S(=O)(=O)c1ccc2c(c1)cn[nH]2)Cc1ccccc1C(F)(F)F 10.1021/jm500995y
8687 2576 None 21 Rat Functional pEC50 = 5.7 5.7 -3 6
Activity at rat muscarinic acetylcholine receptor subtype 1 expressed in CHO cells by calcium mobilization assayActivity at rat muscarinic acetylcholine receptor subtype 1 expressed in CHO cells by calcium mobilization assay
ChEMBL 494 6 1 4 4.0 CCN(C(=O)C1CCN(CC1)S(=O)(=O)c1ccc2c(c1)cn[nH]2)Cc1ccccc1C(F)(F)F 10.1021/jm500995y
CHEMBL3329755 2576 None 21 Rat Functional pEC50 = 5.7 5.7 -3 6
Activity at rat muscarinic acetylcholine receptor subtype 1 expressed in CHO cells by calcium mobilization assayActivity at rat muscarinic acetylcholine receptor subtype 1 expressed in CHO cells by calcium mobilization assay
ChEMBL 494 6 1 4 4.0 CCN(C(=O)C1CCN(CC1)S(=O)(=O)c1ccc2c(c1)cn[nH]2)Cc1ccccc1C(F)(F)F 10.1021/jm500995y
70687733 74201 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
ChEMBL 354 5 2 5 0.8 CCOC(=O)N1[C@H]2CC[C@@H]1C[C@@H](NCCNC(=O)N1CCOCC1)C2 10.1016/j.bmcl.2012.03.088
CHEMBL2022944 74201 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
ChEMBL 354 5 2 5 0.8 CCOC(=O)N1[C@H]2CC[C@@H]1C[C@@H](NCCNC(=O)N1CCOCC1)C2 10.1016/j.bmcl.2012.03.088
70687828 74368 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
ChEMBL 357 7 2 4 2.3 C=CCOC(=O)N1[C@H]2CC[C@@H]1C[C@@H](NCCNC(=O)c1ccccc1)C2 10.1016/j.bmcl.2012.03.088
CHEMBL2024410 74368 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
ChEMBL 357 7 2 4 2.3 C=CCOC(=O)N1[C@H]2CC[C@@H]1C[C@@H](NCCNC(=O)c1ccccc1)C2 10.1016/j.bmcl.2012.03.088
71717377 86598 None 0 Rat Functional pEC50 = 5.7 5.7 - 1
Partial agonist activity at rat muscarinic M1 receptor expressed in CHO cells calcium responsePartial agonist activity at rat muscarinic M1 receptor expressed in CHO cells calcium response
ChEMBL 437 4 1 4 3.3 CCOC(=O)N1CCC(N2CCC[C@@H](NC(=O)c3cccc(Br)c3)C2)CC1 10.1016/j.bmcl.2012.10.132
CHEMBL2315678 86598 None 0 Rat Functional pEC50 = 5.7 5.7 - 1
Partial agonist activity at rat muscarinic M1 receptor expressed in CHO cells calcium responsePartial agonist activity at rat muscarinic M1 receptor expressed in CHO cells calcium response
ChEMBL 437 4 1 4 3.3 CCOC(=O)N1CCC(N2CCC[C@@H](NC(=O)c3cccc(Br)c3)C2)CC1 10.1016/j.bmcl.2012.10.132
146216775 184638 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL 378 3 0 5 4.0 Cn1cc2cc(-c3ccc(CN4Cc5ncsc5C4=O)c(F)c3)ccc2n1 10.1016/j.bmcl.2021.128193
CHEMBL4847801 184638 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL 378 3 0 5 4.0 Cn1cc2cc(-c3ccc(CN4Cc5ncsc5C4=O)c(F)c3)ccc2n1 10.1016/j.bmcl.2021.128193
187 255 None 24 Human Functional pEC50 = 4.7 4.7 -5 8
Agonistic activity against M1 muscarinic receptor expressed in NIH 3T3 cells.Agonistic activity against M1 muscarinic receptor expressed in NIH 3T3 cells.
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm0102405
187.0 255 None 24 Human Functional pEC50 = 4.7 4.7 -5 8
Agonistic activity against M1 muscarinic receptor expressed in NIH 3T3 cells.Agonistic activity against M1 muscarinic receptor expressed in NIH 3T3 cells.
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm0102405
294 255 None 24 Human Functional pEC50 = 4.7 4.7 -5 8
Agonistic activity against M1 muscarinic receptor expressed in NIH 3T3 cells.Agonistic activity against M1 muscarinic receptor expressed in NIH 3T3 cells.
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm0102405
65 255 None 24 Human Functional pEC50 = 4.7 4.7 -5 8
Agonistic activity against M1 muscarinic receptor expressed in NIH 3T3 cells.Agonistic activity against M1 muscarinic receptor expressed in NIH 3T3 cells.
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm0102405
8593 255 None 24 Human Functional pEC50 = 4.7 4.7 -5 8
Agonistic activity against M1 muscarinic receptor expressed in NIH 3T3 cells.Agonistic activity against M1 muscarinic receptor expressed in NIH 3T3 cells.
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm0102405
CHEMBL667 255 None 24 Human Functional pEC50 = 4.7 4.7 -5 8
Agonistic activity against M1 muscarinic receptor expressed in NIH 3T3 cells.Agonistic activity against M1 muscarinic receptor expressed in NIH 3T3 cells.
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm0102405
DB03128 255 None 24 Human Functional pEC50 = 4.7 4.7 -5 8
Agonistic activity against M1 muscarinic receptor expressed in NIH 3T3 cells.Agonistic activity against M1 muscarinic receptor expressed in NIH 3T3 cells.
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm0102405
118724598 116518 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assay
ChEMBL 411 4 0 4 5.2 Cc1ccc(Cn2nc3c4ccccc4n(Cc4ccc(F)cc4)cc-3c2=O)c(C)c1 10.1016/j.bmcl.2014.11.011
CHEMBL3360940 116518 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assay
ChEMBL 411 4 0 4 5.2 Cc1ccc(Cn2nc3c4ccccc4n(Cc4ccc(F)cc4)cc-3c2=O)c(C)c1 10.1016/j.bmcl.2014.11.011
71717377 86598 None 0 Rat Functional pEC50 = 5.7 5.7 - 1
Partial agonist activity at rat muscarinic M1 receptor expressed in CHO cells calcium responsePartial agonist activity at rat muscarinic M1 receptor expressed in CHO cells calcium response
ChEMBL 437 4 1 4 3.3 CCOC(=O)N1CCC(N2CCC[C@@H](NC(=O)c3cccc(Br)c3)C2)CC1 10.1016/j.bmcl.2012.10.132
CHEMBL2315678 86598 None 0 Rat Functional pEC50 = 5.7 5.7 - 1
Partial agonist activity at rat muscarinic M1 receptor expressed in CHO cells calcium responsePartial agonist activity at rat muscarinic M1 receptor expressed in CHO cells calcium response
ChEMBL 437 4 1 4 3.3 CCOC(=O)N1CCC(N2CCC[C@@H](NC(=O)c3cccc(Br)c3)C2)CC1 10.1016/j.bmcl.2012.10.132
118724598 116518 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assay
ChEMBL 411 4 0 4 5.2 Cc1ccc(Cn2nc3c4ccccc4n(Cc4ccc(F)cc4)cc-3c2=O)c(C)c1 10.1016/j.bmcl.2014.11.011
CHEMBL3360940 116518 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assay
ChEMBL 411 4 0 4 5.2 Cc1ccc(Cn2nc3c4ccccc4n(Cc4ccc(F)cc4)cc-3c2=O)c(C)c1 10.1016/j.bmcl.2014.11.011
162654237 180690 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Positive allosteric modulation of human muscarinic M1 receptor stably expressed in CHO cells assessed as increase in Ach-induced intracellular calcium level preincubated for 10 mins followed by addition of Ach at EC20 concentration by Fluo-8AM dye based FLIPR TETRA methodPositive allosteric modulation of human muscarinic M1 receptor stably expressed in CHO cells assessed as increase in Ach-induced intracellular calcium level preincubated for 10 mins followed by addition of Ach at EC20 concentration by Fluo-8AM dye based FLIPR TETRA method
ChEMBL 391 5 2 5 2.7 Cc1ccc(C(=O)N[C@H]2CCOC[C@@H]2O)cc1Cc1ccc(-n2cccn2)cc1 10.1021/acs.jmedchem.6b00544
CHEMBL4754262 180690 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Positive allosteric modulation of human muscarinic M1 receptor stably expressed in CHO cells assessed as increase in Ach-induced intracellular calcium level preincubated for 10 mins followed by addition of Ach at EC20 concentration by Fluo-8AM dye based FLIPR TETRA methodPositive allosteric modulation of human muscarinic M1 receptor stably expressed in CHO cells assessed as increase in Ach-induced intracellular calcium level preincubated for 10 mins followed by addition of Ach at EC20 concentration by Fluo-8AM dye based FLIPR TETRA method
ChEMBL 391 5 2 5 2.7 Cc1ccc(C(=O)N[C@H]2CCOC[C@@H]2O)cc1Cc1ccc(-n2cccn2)cc1 10.1021/acs.jmedchem.6b00544
301 2534 None 15 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assayAgonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assay
ChEMBL 154 2 0 3 0.9 CO/N=C/C1=CCCN(C1)C 10.1016/j.bmcl.2015.02.012
9571002 2534 None 15 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assayAgonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assay
ChEMBL 154 2 0 3 0.9 CO/N=C/C1=CCCN(C1)C 10.1016/j.bmcl.2015.02.012
CHEMBL151938 2534 None 15 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assayAgonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assay
ChEMBL 154 2 0 3 0.9 CO/N=C/C1=CCCN(C1)C 10.1016/j.bmcl.2015.02.012
53303986 74366 None 0 Human Functional pEC50 = 6.7 6.7 20 3
Agonist activity at human muscarinic M1 receptor by calcium mobilization assayAgonist activity at human muscarinic M1 receptor by calcium mobilization assay
ChEMBL 345 6 2 4 2.2 CCOC(=O)N1[C@H]2CC[C@@H]1C[C@H](NCCNC(=O)c1ccccc1)C2 10.1016/j.bmcl.2012.03.088
CHEMBL2024407 74366 None 0 Human Functional pEC50 = 6.7 6.7 20 3
Agonist activity at human muscarinic M1 receptor by calcium mobilization assayAgonist activity at human muscarinic M1 receptor by calcium mobilization assay
ChEMBL 345 6 2 4 2.2 CCOC(=O)N1[C@H]2CC[C@@H]1C[C@H](NCCNC(=O)c1ccccc1)C2 10.1016/j.bmcl.2012.03.088
289 242 None 13 Human Functional pEC50 = 6.7 6.7 - 1
Partial agonist activity at EGFP-fused human full length M1 receptor expressed in HEK293 cells assessed as induction of calcium response by fluorescence assayPartial agonist activity at EGFP-fused human full length M1 receptor expressed in HEK293 cells assessed as induction of calcium response by fluorescence assay
ChEMBL 301 8 0 2 4.9 CCCCC1CCN(CC1)CCCC(=O)c1ccccc1C 10.1021/jm201348t
9948320 242 None 13 Human Functional pEC50 = 6.7 6.7 - 1
Partial agonist activity at EGFP-fused human full length M1 receptor expressed in HEK293 cells assessed as induction of calcium response by fluorescence assayPartial agonist activity at EGFP-fused human full length M1 receptor expressed in HEK293 cells assessed as induction of calcium response by fluorescence assay
ChEMBL 301 8 0 2 4.9 CCCCC1CCN(CC1)CCCC(=O)c1ccccc1C 10.1021/jm201348t
CHEMBL1242950 242 None 13 Human Functional pEC50 = 6.7 6.7 - 1
Partial agonist activity at EGFP-fused human full length M1 receptor expressed in HEK293 cells assessed as induction of calcium response by fluorescence assayPartial agonist activity at EGFP-fused human full length M1 receptor expressed in HEK293 cells assessed as induction of calcium response by fluorescence assay
ChEMBL 301 8 0 2 4.9 CCCCC1CCN(CC1)CCCC(=O)c1ccccc1C 10.1021/jm201348t
134817226 165330 None 5 Human Functional pEC50 = 6.7 6.7 - 1
Positive allosteric modulation of human muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization preincubated for 2.5 mins followed by acetylcholine addition measured after 1 min by Fluo-4AM-based FLIPR assayPositive allosteric modulation of human muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization preincubated for 2.5 mins followed by acetylcholine addition measured after 1 min by Fluo-4AM-based FLIPR assay
ChEMBL 465 5 2 6 3.8 Cn1cc(-c2ccc(Cn3cc(C(=O)N[C@@H]4CCCC[C@H]4O)c4c(F)cc(F)cc43)cn2)cn1 10.1021/acs.jmedchem.7b01812
CHEMBL4229203 165330 None 5 Human Functional pEC50 = 6.7 6.7 - 1
Positive allosteric modulation of human muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization preincubated for 2.5 mins followed by acetylcholine addition measured after 1 min by Fluo-4AM-based FLIPR assayPositive allosteric modulation of human muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization preincubated for 2.5 mins followed by acetylcholine addition measured after 1 min by Fluo-4AM-based FLIPR assay
ChEMBL 465 5 2 6 3.8 Cn1cc(-c2ccc(Cn3cc(C(=O)N[C@@H]4CCCC[C@H]4O)c4c(F)cc(F)cc43)cn2)cn1 10.1021/acs.jmedchem.7b01812
70692018 74338 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
ChEMBL 399 4 1 4 3.3 CCOC(=O)N1C2CCC1CC(N1CCC[C@H](NC(=O)c3ccccc3C)C1)C2 10.1016/j.bmcl.2012.03.088
CHEMBL2024329 74338 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
ChEMBL 399 4 1 4 3.3 CCOC(=O)N1C2CCC1CC(N1CCC[C@H](NC(=O)c3ccccc3C)C1)C2 10.1016/j.bmcl.2012.03.088
44589681 185394 None 0 Human Functional pEC50 = 5.7 5.7 -229 5
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
ChEMBL 387 5 2 6 1.5 NC(=O)OCCN1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1 10.1016/j.bmcl.2008.09.032
CHEMBL485913 185394 None 0 Human Functional pEC50 = 5.7 5.7 -229 5
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
ChEMBL 387 5 2 6 1.5 NC(=O)OCCN1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1 10.1016/j.bmcl.2008.09.032
10952349 35142 None 0 Human Functional pEC50 = 5.7 5.7 -3467 2
Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.
ChEMBL 564 15 0 10 6.8 CN1CCC=C(c2nsnc2SCCCCCCCCCCSc2nsnc2C2=CCCN(C)C2)C1 10.1021/jm0102405
CHEMBL143434 35142 None 0 Human Functional pEC50 = 5.7 5.7 -3467 2
Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.
ChEMBL 564 15 0 10 6.8 CN1CCC=C(c2nsnc2SCCCCCCCCCCSc2nsnc2C2=CCCN(C)C2)C1 10.1021/jm0102405
118124039 161555 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 431 5 2 5 3.7 O=C(N[C@H]1CCCC[C@@H]1O)C1CN(Cc2ccc(-n3cccc3)cc2)c2ccccc2O1 10.1016/j.bmcl.2018.05.009
CHEMBL4127506 161555 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 431 5 2 5 3.7 O=C(N[C@H]1CCCC[C@@H]1O)C1CN(Cc2ccc(-n3cccc3)cc2)c2ccccc2O1 10.1016/j.bmcl.2018.05.009
127039042 137155 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Positive allosteric modulation of human M1 receptor expressed in CHO cells assessed as acetylcholine-induced calcium mobilization by FLIPR assayPositive allosteric modulation of human M1 receptor expressed in CHO cells assessed as acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 445 5 2 7 2.7 Cc1cnc2c(C(=O)N[C@H]3CCOC[C@@H]3O)cn(Cc3ccc(-c4ccn(C)n4)cc3)c2c1 10.1016/j.bmcl.2015.11.053
CHEMBL3747004 137155 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Positive allosteric modulation of human M1 receptor expressed in CHO cells assessed as acetylcholine-induced calcium mobilization by FLIPR assayPositive allosteric modulation of human M1 receptor expressed in CHO cells assessed as acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 445 5 2 7 2.7 Cc1cnc2c(C(=O)N[C@H]3CCOC[C@@H]3O)cn(Cc3ccc(-c4ccn(C)n4)cc3)c2c1 10.1016/j.bmcl.2015.11.053
44590188 179188 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
ChEMBL 452 3 1 4 4.2 Cc1cccc(C(=O)N2CCC(N3CCC(n4c(=O)[nH]c5cc(Cl)ccc54)CC3)CC2)c1 10.1016/j.bmcl.2008.09.032
CHEMBL471636 179188 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
ChEMBL 452 3 1 4 4.2 Cc1cccc(C(=O)N2CCC(N3CCC(n4c(=O)[nH]c5cc(Cl)ccc54)CC3)CC2)c1 10.1016/j.bmcl.2008.09.032
118124169 161742 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 446 6 2 6 2.7 O=C(NCC(O)C(F)(F)F)C1CN(Cc2ccc(-n3cccn3)cc2)c2ccccc2O1 10.1016/j.bmcl.2018.05.009
CHEMBL4130246 161742 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 446 6 2 6 2.7 O=C(NCC(O)C(F)(F)F)C1CN(Cc2ccc(-n3cccn3)cc2)c2ccccc2O1 10.1016/j.bmcl.2018.05.009
127039040 137093 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Positive allosteric modulation of human M1 receptor expressed in CHO cells assessed as acetylcholine-induced calcium mobilization by FLIPR assayPositive allosteric modulation of human M1 receptor expressed in CHO cells assessed as acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 416 5 2 7 2.7 O=C(N[C@H]1CCCC[C@@H]1O)c1nn(Cc2ccc(-n3cccn3)cc2)c2cccnc12 10.1016/j.bmcl.2015.11.053
CHEMBL3746104 137093 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Positive allosteric modulation of human M1 receptor expressed in CHO cells assessed as acetylcholine-induced calcium mobilization by FLIPR assayPositive allosteric modulation of human M1 receptor expressed in CHO cells assessed as acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 416 5 2 7 2.7 O=C(N[C@H]1CCCC[C@@H]1O)c1nn(Cc2ccc(-n3cccn3)cc2)c2cccnc12 10.1016/j.bmcl.2015.11.053
14851833 164571 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assayPositive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 396 1 1 2 4.0 Fc1ccccc1C1=NCC(=S)Nc2ccc(I)cc21 10.1016/j.bmcl.2017.11.008
CHEMBL4214189 164571 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assayPositive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 396 1 1 2 4.0 Fc1ccccc1C1=NCC(=S)Nc2ccc(I)cc21 10.1016/j.bmcl.2017.11.008
146216719 185419 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL 395 3 0 4 4.7 Cn1cc2c(-c3cc(F)c(CN4Cc5ccsc5C4=O)c(F)c3)cccc2n1 10.1016/j.bmcl.2021.128193
CHEMBL4859477 185419 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL 395 3 0 4 4.7 Cn1cc2c(-c3cc(F)c(CN4Cc5ccsc5C4=O)c(F)c3)cccc2n1 10.1016/j.bmcl.2021.128193
139414008 164456 None 0 Rat Functional pEC50 = 6.7 6.7 -1 3
Positive allosteric modulation of rat M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assayPositive allosteric modulation of rat M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 346 2 1 2 5.1 CC(C)[C@@H]1N=C(c2ccccc2F)c2cc(Cl)ccc2NC1=S 10.1016/j.bmcl.2017.11.008
CHEMBL4212760 164456 None 0 Rat Functional pEC50 = 6.7 6.7 -1 3
Positive allosteric modulation of rat M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assayPositive allosteric modulation of rat M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 346 2 1 2 5.1 CC(C)[C@@H]1N=C(c2ccccc2F)c2cc(Cl)ccc2NC1=S 10.1016/j.bmcl.2017.11.008
145960875 161539 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 450 5 2 6 3.2 O=C(N[C@H]1CCCC[C@@H]1O)C1CN(Cc2ccc(-n3cccn3)cc2)c2ccc(F)cc2O1 10.1016/j.bmcl.2018.05.009
CHEMBL4127356 161539 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 450 5 2 6 3.2 O=C(N[C@H]1CCCC[C@@H]1O)C1CN(Cc2ccc(-n3cccn3)cc2)c2ccc(F)cc2O1 10.1016/j.bmcl.2018.05.009
9308 17761 None 16 Rat Functional pEC50 = 6.7 6.7 -11 9
Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M1Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M1
ChEMBL 174 2 1 2 0.2 C[C@@H]1O[C@H](C[N+](C)(C)C)C[C@H]1O 10.1021/jm9705115
CHEMBL1255785 17761 None 16 Rat Functional pEC50 = 6.7 6.7 -11 9
Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M1Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M1
ChEMBL 174 2 1 2 0.2 C[C@@H]1O[C@H](C[N+](C)(C)C)C[C@H]1O 10.1021/jm9705115
CHEMBL12587 17761 None 16 Rat Functional pEC50 = 6.7 6.7 -11 9
Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M1Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M1
ChEMBL 174 2 1 2 0.2 C[C@@H]1O[C@H](C[N+](C)(C)C)C[C@H]1O 10.1021/jm9705115
CHEMBL292911 17761 None 16 Rat Functional pEC50 = 6.7 6.7 -11 9
Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M1Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M1
ChEMBL 174 2 1 2 0.2 C[C@@H]1O[C@H](C[N+](C)(C)C)C[C@H]1O 10.1021/jm9705115
44216759 61807 None 0 Rat Functional pEC50 = 5.7 5.7 - 1
Allosteric modulation at rat M1 receptor expressed in CHO cells by calcium mobilization assayAllosteric modulation at rat M1 receptor expressed in CHO cells by calcium mobilization assay
ChEMBL 475 7 2 7 3.8 Cc1cc(NC(=O)CS(=O)(=O)c2cn(Cc3cccc(-c4cn[nH]c4)c3)c3ccccc23)no1 10.1016/j.bmcl.2010.12.015
CHEMBL1773100 61807 None 0 Rat Functional pEC50 = 5.7 5.7 - 1
Allosteric modulation at rat M1 receptor expressed in CHO cells by calcium mobilization assayAllosteric modulation at rat M1 receptor expressed in CHO cells by calcium mobilization assay
ChEMBL 475 7 2 7 3.8 Cc1cc(NC(=O)CS(=O)(=O)c2cn(Cc3cccc(-c4cn[nH]c4)c3)c3ccccc23)no1 10.1016/j.bmcl.2010.12.015
44350993 168366 None 0 Human Functional pEC50 = 7.7 7.7 -6 2
Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.
ChEMBL 299 6 0 6 2.9 CCCCSc1nsnc1OC1CN2CCC1CC2 10.1021/jm970125n
CHEMBL433867 168366 None 0 Human Functional pEC50 = 7.7 7.7 -6 2
Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.
ChEMBL 299 6 0 6 2.9 CCCCSc1nsnc1OC1CN2CCC1CC2 10.1021/jm970125n
5441 2426 None 12 Human Functional pEC50 = 7.6 7.6 30 3
Agonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 507 6 2 3 6.1 O[C@@H]1Cc2c([C@H]1NC(=O)c1ccc(cc1)c1ccccc1)cc(cc2)N=C(N(Cc1ccc(cc1)F)C)C 10.1016/j.bmcl.2015.08.011
9893054 2426 None 12 Human Functional pEC50 = 7.6 7.6 30 3
Agonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 507 6 2 3 6.1 O[C@@H]1Cc2c([C@H]1NC(=O)c1ccc(cc1)c1ccccc1)cc(cc2)N=C(N(Cc1ccc(cc1)F)C)C 10.1016/j.bmcl.2015.08.011
CHEMBL3616501 2426 None 12 Human Functional pEC50 = 7.6 7.6 30 3
Agonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 507 6 2 3 6.1 O[C@@H]1Cc2c([C@H]1NC(=O)c1ccc(cc1)c1ccccc1)cc(cc2)N=C(N(Cc1ccc(cc1)F)C)C 10.1016/j.bmcl.2015.08.011
145962181 161591 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 447 5 2 7 2.7 Cn1cc(-c2ccc(CN3CC(C(=O)N[C@H]4CCCC[C@@H]4O)Oc4ccccc43)cn2)cn1 10.1016/j.bmcl.2018.05.009
CHEMBL4128022 161591 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 447 5 2 7 2.7 Cn1cc(-c2ccc(CN3CC(C(=O)N[C@H]4CCCC[C@@H]4O)Oc4ccccc43)cn2)cn1 10.1016/j.bmcl.2018.05.009
70689864 74365 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
ChEMBL 357 4 1 4 2.3 CCOC(=O)N1C2CCC1CC(N1CC(NC(=O)c3ccccc3)C1)C2 10.1016/j.bmcl.2012.03.088
CHEMBL2024406 74365 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
ChEMBL 357 4 1 4 2.3 CCOC(=O)N1C2CCC1CC(N1CC(NC(=O)c3ccccc3)C1)C2 10.1016/j.bmcl.2012.03.088
145960875 161539 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 450 5 2 6 3.2 O=C(N[C@H]1CCCC[C@@H]1O)C1CN(Cc2ccc(-n3cccn3)cc2)c2ccc(F)cc2O1 10.1016/j.bmcl.2018.05.009
CHEMBL4127356 161539 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 450 5 2 6 3.2 O=C(N[C@H]1CCCC[C@@H]1O)C1CN(Cc2ccc(-n3cccn3)cc2)c2ccc(F)cc2O1 10.1016/j.bmcl.2018.05.009
118124169 161742 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 446 6 2 6 2.7 O=C(NCC(O)C(F)(F)F)C1CN(Cc2ccc(-n3cccn3)cc2)c2ccccc2O1 10.1016/j.bmcl.2018.05.009
CHEMBL4130246 161742 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 446 6 2 6 2.7 O=C(NCC(O)C(F)(F)F)C1CN(Cc2ccc(-n3cccn3)cc2)c2ccccc2O1 10.1016/j.bmcl.2018.05.009
145982857 165893 None 0 Rat Functional pEC50 = 5.7 5.7 -2 2
Agonist activity at rat M1 receptor expressed in CHO cells assessed as increase in calcium mobilization measured after 2.5 mins by Fluo-4-AM dye based assayAgonist activity at rat M1 receptor expressed in CHO cells assessed as increase in calcium mobilization measured after 2.5 mins by Fluo-4-AM dye based assay
ChEMBL 445 5 2 7 2.4 Cn1ccc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCOC[C@H]4O)nc4c3ccn4C)cc2)n1 10.1021/acsmedchemlett.8b00261
CHEMBL4248057 165893 None 0 Rat Functional pEC50 = 5.7 5.7 -2 2
Agonist activity at rat M1 receptor expressed in CHO cells assessed as increase in calcium mobilization measured after 2.5 mins by Fluo-4-AM dye based assayAgonist activity at rat M1 receptor expressed in CHO cells assessed as increase in calcium mobilization measured after 2.5 mins by Fluo-4-AM dye based assay
ChEMBL 445 5 2 7 2.4 Cn1ccc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCOC[C@H]4O)nc4c3ccn4C)cc2)n1 10.1021/acsmedchemlett.8b00261
145961235 161481 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 431 5 2 6 3.0 NC1CCCCC1NC(=O)C1CN(Cc2ccc(-n3cccn3)cc2)c2ccccc2O1 10.1016/j.bmcl.2018.05.009
CHEMBL4126393 161481 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 431 5 2 6 3.0 NC1CCCCC1NC(=O)C1CN(Cc2ccc(-n3cccn3)cc2)c2ccccc2O1 10.1016/j.bmcl.2018.05.009
118123991 161522 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 407 5 2 5 3.1 O=C(N[C@H]1CCCC[C@@H]1O)C1CN(Cc2ccc(C3CC3)nc2)c2ccccc2O1 10.1016/j.bmcl.2018.05.009
CHEMBL4127046 161522 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 407 5 2 5 3.1 O=C(N[C@H]1CCCC[C@@H]1O)C1CN(Cc2ccc(C3CC3)nc2)c2ccccc2O1 10.1016/j.bmcl.2018.05.009
146487687 183676 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Positive allosteric modulation of recombinant human muscarinic M1 receptor co-expressing pCRE-Luc reporter gene in CHO cells assessed as stimulation of luciferase activity in presence of acetylcholine substrate measured after 4 hrs by luciferase reporter gene assayPositive allosteric modulation of recombinant human muscarinic M1 receptor co-expressing pCRE-Luc reporter gene in CHO cells assessed as stimulation of luciferase activity in presence of acetylcholine substrate measured after 4 hrs by luciferase reporter gene assay
ChEMBL 460 5 2 5 4.7 O=C(N[C@H]1CCCC[C@@H]1O)c1cc(Cc2ccc(-c3ccnc(Cl)c3)cc2)c2cccn2n1 10.1021/acsmedchemlett.1c00118
CHEMBL4800374 183676 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Positive allosteric modulation of recombinant human muscarinic M1 receptor co-expressing pCRE-Luc reporter gene in CHO cells assessed as stimulation of luciferase activity in presence of acetylcholine substrate measured after 4 hrs by luciferase reporter gene assayPositive allosteric modulation of recombinant human muscarinic M1 receptor co-expressing pCRE-Luc reporter gene in CHO cells assessed as stimulation of luciferase activity in presence of acetylcholine substrate measured after 4 hrs by luciferase reporter gene assay
ChEMBL 460 5 2 5 4.7 O=C(N[C@H]1CCCC[C@@H]1O)c1cc(Cc2ccc(-c3ccnc(Cl)c3)cc2)c2cccn2n1 10.1021/acsmedchemlett.1c00118
145982857 165893 None 0 Rat Functional pEC50 = 5.7 5.7 -2 2
Agonist activity at rat M1 receptor expressed in CHO cells assessed as increase in calcium mobilization measured after 2.5 mins by Fluo-4-AM dye based assayAgonist activity at rat M1 receptor expressed in CHO cells assessed as increase in calcium mobilization measured after 2.5 mins by Fluo-4-AM dye based assay
ChEMBL 445 5 2 7 2.4 Cn1ccc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCOC[C@H]4O)nc4c3ccn4C)cc2)n1 10.1021/acsmedchemlett.8b00261
CHEMBL4248057 165893 None 0 Rat Functional pEC50 = 5.7 5.7 -2 2
Agonist activity at rat M1 receptor expressed in CHO cells assessed as increase in calcium mobilization measured after 2.5 mins by Fluo-4-AM dye based assayAgonist activity at rat M1 receptor expressed in CHO cells assessed as increase in calcium mobilization measured after 2.5 mins by Fluo-4-AM dye based assay
ChEMBL 445 5 2 7 2.4 Cn1ccc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCOC[C@H]4O)nc4c3ccn4C)cc2)n1 10.1021/acsmedchemlett.8b00261
44351073 18001 None 0 Human Functional pEC50 = 6.7 6.7 -15 2
Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.
ChEMBL 327 8 0 6 3.7 CCCCCCSc1nsnc1OC1CN2CCC1CC2 10.1021/jm970125n
CHEMBL126237 18001 None 0 Human Functional pEC50 = 6.7 6.7 -15 2
Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.
ChEMBL 327 8 0 6 3.7 CCCCCCSc1nsnc1OC1CN2CCC1CC2 10.1021/jm970125n
137701968 165492 None 11 Rat Functional pEC50 = 6.6 6.6 1 2
Positive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assayPositive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assay
ChEMBL 430 5 1 7 2.9 Cn1cc(-c2ccc(Cc3cc(C(=O)NC4CCOCC4)nc4c3ccn4C)cn2)cn1 10.1021/acsmedchemlett.8b00261
CHEMBL4238059 165492 None 11 Rat Functional pEC50 = 6.6 6.6 1 2
Positive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assayPositive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assay
ChEMBL 430 5 1 7 2.9 Cn1cc(-c2ccc(Cc3cc(C(=O)NC4CCOCC4)nc4c3ccn4C)cn2)cn1 10.1021/acsmedchemlett.8b00261
145985917 165594 None 0 Rat Functional pEC50 = 5.6 5.6 -2 2
Agonist activity at rat M1 receptor expressed in CHO cells assessed as increase in calcium mobilization measured after 2.5 mins by Fluo-4-AM dye based assayAgonist activity at rat M1 receptor expressed in CHO cells assessed as increase in calcium mobilization measured after 2.5 mins by Fluo-4-AM dye based assay
ChEMBL 444 5 2 7 3.0 Cn1ccc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCCC[C@H]4O)nc4c3ccn4C)cn2)n1 10.1021/acsmedchemlett.8b00261
CHEMBL4240517 165594 None 0 Rat Functional pEC50 = 5.6 5.6 -2 2
Agonist activity at rat M1 receptor expressed in CHO cells assessed as increase in calcium mobilization measured after 2.5 mins by Fluo-4-AM dye based assayAgonist activity at rat M1 receptor expressed in CHO cells assessed as increase in calcium mobilization measured after 2.5 mins by Fluo-4-AM dye based assay
ChEMBL 444 5 2 7 3.0 Cn1ccc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCCC[C@H]4O)nc4c3ccn4C)cn2)n1 10.1021/acsmedchemlett.8b00261
145985917 165594 None 0 Rat Functional pEC50 = 5.6 5.6 -2 2
Agonist activity at rat M1 receptor expressed in CHO cells assessed as increase in calcium mobilization measured after 2.5 mins by Fluo-4-AM dye based assayAgonist activity at rat M1 receptor expressed in CHO cells assessed as increase in calcium mobilization measured after 2.5 mins by Fluo-4-AM dye based assay
ChEMBL 444 5 2 7 3.0 Cn1ccc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCCC[C@H]4O)nc4c3ccn4C)cn2)n1 10.1021/acsmedchemlett.8b00261
CHEMBL4240517 165594 None 0 Rat Functional pEC50 = 5.6 5.6 -2 2
Agonist activity at rat M1 receptor expressed in CHO cells assessed as increase in calcium mobilization measured after 2.5 mins by Fluo-4-AM dye based assayAgonist activity at rat M1 receptor expressed in CHO cells assessed as increase in calcium mobilization measured after 2.5 mins by Fluo-4-AM dye based assay
ChEMBL 444 5 2 7 3.0 Cn1ccc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCCC[C@H]4O)nc4c3ccn4C)cn2)n1 10.1021/acsmedchemlett.8b00261
126492036 161536 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 429 5 1 6 3.8 O=C(Nc1ncccc1F)C1CN(Cc2ccc(-n3cccn3)cc2)c2ccccc2O1 10.1016/j.bmcl.2018.05.009
CHEMBL4127312 161536 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 429 5 1 6 3.8 O=C(Nc1ncccc1F)C1CN(Cc2ccc(-n3cccn3)cc2)c2ccccc2O1 10.1016/j.bmcl.2018.05.009
9815331 205565 None 1 Rat Functional pEC50 = 7.6 7.6 -6 5
Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M1Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M1
ChEMBL 169 1 1 3 0.8 CC(=O)OC1CC2CCCC1N2 10.1021/jm9705115
CHEMBL64000 205565 None 1 Rat Functional pEC50 = 7.6 7.6 -6 5
Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M1Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M1
ChEMBL 169 1 1 3 0.8 CC(=O)OC1CC2CCCC1N2 10.1021/jm9705115
137701968 165492 None 11 Rat Functional pEC50 = 6.6 6.6 1 2
Positive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assayPositive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assay
ChEMBL 430 5 1 7 2.9 Cn1cc(-c2ccc(Cc3cc(C(=O)NC4CCOCC4)nc4c3ccn4C)cn2)cn1 10.1021/acsmedchemlett.8b00261
CHEMBL4238059 165492 None 11 Rat Functional pEC50 = 6.6 6.6 1 2
Positive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assayPositive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assay
ChEMBL 430 5 1 7 2.9 Cn1cc(-c2ccc(Cc3cc(C(=O)NC4CCOCC4)nc4c3ccn4C)cn2)cn1 10.1021/acsmedchemlett.8b00261
70694062 74371 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
ChEMBL 379 6 2 4 2.8 CCOC(=O)N1[C@H]2CC[C@@H]1C[C@@H](NCCNC(=O)c1ccccc1Cl)C2 10.1016/j.bmcl.2012.03.088
CHEMBL2024419 74371 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
ChEMBL 379 6 2 4 2.8 CCOC(=O)N1[C@H]2CC[C@@H]1C[C@@H](NCCNC(=O)c1ccccc1Cl)C2 10.1016/j.bmcl.2012.03.088
25010776 55971 None 1 Human Functional pEC50 = 5.6 5.6 1 5
Agonist activity at human recombinant muscarinic M1 receptor by HTS cell based assayAgonist activity at human recombinant muscarinic M1 receptor by HTS cell based assay
ChEMBL 333 6 2 4 1.9 CCOC(=O)N1CCC(NCCNC(=O)c2ccccc2C)CC1 10.1016/j.bmcl.2011.08.084
CHEMBL1559151 55971 None 1 Human Functional pEC50 = 5.6 5.6 1 5
Agonist activity at human recombinant muscarinic M1 receptor by HTS cell based assayAgonist activity at human recombinant muscarinic M1 receptor by HTS cell based assay
ChEMBL 333 6 2 4 1.9 CCOC(=O)N1CCC(NCCNC(=O)c2ccccc2C)CC1 10.1016/j.bmcl.2011.08.084
CHEMBL1624037 55971 None 1 Human Functional pEC50 = 5.6 5.6 1 5
Agonist activity at human recombinant muscarinic M1 receptor by HTS cell based assayAgonist activity at human recombinant muscarinic M1 receptor by HTS cell based assay
ChEMBL 333 6 2 4 1.9 CCOC(=O)N1CCC(NCCNC(=O)c2ccccc2C)CC1 10.1016/j.bmcl.2011.08.084
44589594 185302 None 0 Human Functional pEC50 = 5.6 5.6 1 2
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
ChEMBL 458 4 1 5 3.0 O=c1[nH]c2cc(F)ccc2n1C1CCN(C2CCN(S(=O)(=O)c3ccccc3)CC2)CC1 10.1016/j.bmcl.2008.09.032
CHEMBL485755 185302 None 0 Human Functional pEC50 = 5.6 5.6 1 2
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
ChEMBL 458 4 1 5 3.0 O=c1[nH]c2cc(F)ccc2n1C1CCN(C2CCN(S(=O)(=O)c3ccccc3)CC2)CC1 10.1016/j.bmcl.2008.09.032
25010776 55971 None 1 Rat Functional pEC50 = 5.6 5.6 -1 5
Agonist activity at rat recombinant muscarinic M1 receptor by HTS cell based assayAgonist activity at rat recombinant muscarinic M1 receptor by HTS cell based assay
ChEMBL 333 6 2 4 1.9 CCOC(=O)N1CCC(NCCNC(=O)c2ccccc2C)CC1 10.1016/j.bmcl.2011.08.084
CHEMBL1559151 55971 None 1 Rat Functional pEC50 = 5.6 5.6 -1 5
Agonist activity at rat recombinant muscarinic M1 receptor by HTS cell based assayAgonist activity at rat recombinant muscarinic M1 receptor by HTS cell based assay
ChEMBL 333 6 2 4 1.9 CCOC(=O)N1CCC(NCCNC(=O)c2ccccc2C)CC1 10.1016/j.bmcl.2011.08.084
CHEMBL1624037 55971 None 1 Rat Functional pEC50 = 5.6 5.6 -1 5
Agonist activity at rat recombinant muscarinic M1 receptor by HTS cell based assayAgonist activity at rat recombinant muscarinic M1 receptor by HTS cell based assay
ChEMBL 333 6 2 4 1.9 CCOC(=O)N1CCC(NCCNC(=O)c2ccccc2C)CC1 10.1016/j.bmcl.2011.08.084
145961235 161481 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 431 5 2 6 3.0 NC1CCCCC1NC(=O)C1CN(Cc2ccc(-n3cccn3)cc2)c2ccccc2O1 10.1016/j.bmcl.2018.05.009
CHEMBL4126393 161481 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 431 5 2 6 3.0 NC1CCCCC1NC(=O)C1CN(Cc2ccc(-n3cccn3)cc2)c2ccccc2O1 10.1016/j.bmcl.2018.05.009
126492036 161536 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 429 5 1 6 3.8 O=C(Nc1ncccc1F)C1CN(Cc2ccc(-n3cccn3)cc2)c2ccccc2O1 10.1016/j.bmcl.2018.05.009
CHEMBL4127312 161536 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 429 5 1 6 3.8 O=C(Nc1ncccc1F)C1CN(Cc2ccc(-n3cccn3)cc2)c2ccccc2O1 10.1016/j.bmcl.2018.05.009
44251557 6613 None 0 Human Functional pEC50 = 5.6 5.6 1 2
Potentiation of muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assayPotentiation of muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 353 3 0 4 3.1 Cn1cc(-c2ccc(CN3C(=O)C(=O)c4cccc(F)c43)c(F)c2)cn1 10.1016/j.bmcl.2010.01.109
CHEMBL1083205 6613 None 0 Human Functional pEC50 = 5.6 5.6 1 2
Potentiation of muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assayPotentiation of muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 353 3 0 4 3.1 Cn1cc(-c2ccc(CN3C(=O)C(=O)c4cccc(F)c43)c(F)c2)cn1 10.1016/j.bmcl.2010.01.109
44251554 7063 None 0 Human Functional pEC50 = 5.6 5.6 1 4
Potentiation of muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assayPotentiation of muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 317 3 0 4 2.8 Cn1cc(-c2ccc(CN3C(=O)C(=O)c4ccccc43)cc2)cn1 10.1016/j.bmcl.2010.01.109
CHEMBL1084941 7063 None 0 Human Functional pEC50 = 5.6 5.6 1 4
Potentiation of muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assayPotentiation of muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
ChEMBL 317 3 0 4 2.8 Cn1cc(-c2ccc(CN3C(=O)C(=O)c4ccccc43)cc2)cn1 10.1016/j.bmcl.2010.01.109
139414071 164038 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Positive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assayPositive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 378 3 1 3 5.2 CC(C)[C@@H]1N=C(c2ccccc2)c2cc(OC(F)(F)F)ccc2NC1=S 10.1016/j.bmcl.2017.11.008
CHEMBL4207635 164038 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Positive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assayPositive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 378 3 1 3 5.2 CC(C)[C@@H]1N=C(c2ccccc2)c2cc(OC(F)(F)F)ccc2NC1=S 10.1016/j.bmcl.2017.11.008
44251557 6613 None 0 Rat Functional pEC50 = 5.6 5.6 -1 2
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: PAM Calcium Assay Dose-Response with M1. Measurement of intracellular Ca2+ using Fluo-4 dye in CHO-K1 cells stably transfected with rat M1 (Class of assay: confirmatory) [Related pubchem assays: 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen [Primary Screening])]PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: PAM Calcium Assay Dose-Response with M1. Measurement of intracellular Ca2+ using Fluo-4 dye in CHO-K1 cells stably transfected with rat M1 (Class of assay: confirmatory) [Related pubchem assays: 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen [Primary Screening])]
ChEMBL 353 3 0 4 3.1 Cn1cc(-c2ccc(CN3C(=O)C(=O)c4cccc(F)c43)c(F)c2)cn1 nan
CHEMBL1083205 6613 None 0 Rat Functional pEC50 = 5.6 5.6 -1 2
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: PAM Calcium Assay Dose-Response with M1. Measurement of intracellular Ca2+ using Fluo-4 dye in CHO-K1 cells stably transfected with rat M1 (Class of assay: confirmatory) [Related pubchem assays: 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen [Primary Screening])]PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: PAM Calcium Assay Dose-Response with M1. Measurement of intracellular Ca2+ using Fluo-4 dye in CHO-K1 cells stably transfected with rat M1 (Class of assay: confirmatory) [Related pubchem assays: 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen [Primary Screening])]
ChEMBL 353 3 0 4 3.1 Cn1cc(-c2ccc(CN3C(=O)C(=O)c4cccc(F)c43)c(F)c2)cn1 nan
139414044 164619 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Positive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assayPositive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 328 3 1 2 5.1 CCC[C@@H]1N=C(c2ccccc2)c2cc(Cl)ccc2NC1=S 10.1016/j.bmcl.2017.11.008
CHEMBL4214867 164619 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Positive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assayPositive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 328 3 1 2 5.1 CCC[C@@H]1N=C(c2ccccc2)c2cc(Cl)ccc2NC1=S 10.1016/j.bmcl.2017.11.008
71533547 86390 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Positive allosteric modulator activity at human muscarinic M1 receptor by calcium mobilization assayPositive allosteric modulator activity at human muscarinic M1 receptor by calcium mobilization assay
ChEMBL 321 3 0 3 3.3 Cn1cc(-c2ccc(CN3C(=O)Cc4ccccc43)c(F)c2)cn1 10.1016/j.bmcl.2012.11.092
CHEMBL2313520 86390 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Positive allosteric modulator activity at human muscarinic M1 receptor by calcium mobilization assayPositive allosteric modulator activity at human muscarinic M1 receptor by calcium mobilization assay
ChEMBL 321 3 0 3 3.3 Cn1cc(-c2ccc(CN3C(=O)Cc4ccccc43)c(F)c2)cn1 10.1016/j.bmcl.2012.11.092
76324307 103323 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
ChEMBL 375 7 2 5 1.9 CCOC(=O)N1C[C@@H]2CC[C@H](C1)[C@@H]2NCCNC(=O)c1cccc(OC)c1 10.1016/j.bmcl.2012.03.088
CHEMBL3084450 103323 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
ChEMBL 375 7 2 5 1.9 CCOC(=O)N1C[C@@H]2CC[C@H](C1)[C@@H]2NCCNC(=O)c1cccc(OC)c1 10.1016/j.bmcl.2012.03.088
71533547 86390 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Positive allosteric modulator activity at human muscarinic M1 receptor by calcium mobilization assayPositive allosteric modulator activity at human muscarinic M1 receptor by calcium mobilization assay
ChEMBL 321 3 0 3 3.3 Cn1cc(-c2ccc(CN3C(=O)Cc4ccccc43)c(F)c2)cn1 10.1016/j.bmcl.2012.11.092
CHEMBL2313520 86390 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Positive allosteric modulator activity at human muscarinic M1 receptor by calcium mobilization assayPositive allosteric modulator activity at human muscarinic M1 receptor by calcium mobilization assay
ChEMBL 321 3 0 3 3.3 Cn1cc(-c2ccc(CN3C(=O)Cc4ccccc43)c(F)c2)cn1 10.1016/j.bmcl.2012.11.092
44251554 7063 None 0 Rat Functional pEC50 = 5.6 5.6 -1 4
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: PAM Calcium Assay Dose-Response with M1. Measurement of intracellular Ca2+ using Fluo-4 dye in CHO-K1 cells stably transfected with rat M1 (Class of assay: confirmatory) [Related pubchem assays: 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen [Primary Screening])]PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: PAM Calcium Assay Dose-Response with M1. Measurement of intracellular Ca2+ using Fluo-4 dye in CHO-K1 cells stably transfected with rat M1 (Class of assay: confirmatory) [Related pubchem assays: 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen [Primary Screening])]
ChEMBL 317 3 0 4 2.8 Cn1cc(-c2ccc(CN3C(=O)C(=O)c4ccccc43)cc2)cn1 nan
CHEMBL1084941 7063 None 0 Rat Functional pEC50 = 5.6 5.6 -1 4
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: PAM Calcium Assay Dose-Response with M1. Measurement of intracellular Ca2+ using Fluo-4 dye in CHO-K1 cells stably transfected with rat M1 (Class of assay: confirmatory) [Related pubchem assays: 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen [Primary Screening])]PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: PAM Calcium Assay Dose-Response with M1. Measurement of intracellular Ca2+ using Fluo-4 dye in CHO-K1 cells stably transfected with rat M1 (Class of assay: confirmatory) [Related pubchem assays: 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen [Primary Screening])]
ChEMBL 317 3 0 4 2.8 Cn1cc(-c2ccc(CN3C(=O)C(=O)c4ccccc43)cc2)cn1 nan
68176440 116528 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Positive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assay
ChEMBL 355 3 0 6 3.1 Cn1nc2c3ccccc3n(Cc3ccc(-n4cccn4)cc3)cc-2c1=O 10.1016/j.bmcl.2014.11.011
CHEMBL3360958 116528 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Positive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assay
ChEMBL 355 3 0 6 3.1 Cn1nc2c3ccccc3n(Cc3ccc(-n4cccn4)cc3)cc-2c1=O 10.1016/j.bmcl.2014.11.011
146216715 185953 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL 395 3 0 4 4.7 Cn1cc2cc(-c3cc(F)c(CN4Cc5ccsc5C4=O)c(F)c3)ccc2n1 10.1016/j.bmcl.2021.128193
CHEMBL4867614 185953 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL 395 3 0 4 4.7 Cn1cc2cc(-c3cc(F)c(CN4Cc5ccsc5C4=O)c(F)c3)ccc2n1 10.1016/j.bmcl.2021.128193
127038678 137075 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Positive allosteric modulation of human M1 receptor expressed in CHO cells assessed as acetylcholine-induced calcium mobilization by FLIPR assayPositive allosteric modulation of human M1 receptor expressed in CHO cells assessed as acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 429 6 2 6 3.6 O=C(N[C@H]1CC[C@H](CO)CC1)c1cn(Cc2ccc(-n3cccn3)cc2)c2cccnc12 10.1016/j.bmcl.2015.11.053
CHEMBL3745855 137075 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Positive allosteric modulation of human M1 receptor expressed in CHO cells assessed as acetylcholine-induced calcium mobilization by FLIPR assayPositive allosteric modulation of human M1 receptor expressed in CHO cells assessed as acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 429 6 2 6 3.6 O=C(N[C@H]1CC[C@H](CO)CC1)c1cn(Cc2ccc(-n3cccn3)cc2)c2cccnc12 10.1016/j.bmcl.2015.11.053
46891140 6712 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 380 4 2 2 4.5 O=C(NCC1CCNCC1)c1c(-c2cccc(Cl)c2)ccc(Cl)c1F 10.1016/j.bmcl.2010.04.127
CHEMBL1083621 6712 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 380 4 2 2 4.5 O=C(NCC1CCNCC1)c1c(-c2cccc(Cl)c2)ccc(Cl)c1F 10.1016/j.bmcl.2010.04.127
46890975 7028 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 346 4 2 2 3.9 O=C(NCC1CCNCC1)c1ccccc1-c1ccc(F)c(Cl)c1 10.1016/j.bmcl.2010.04.128
CHEMBL1084818 7028 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 346 4 2 2 3.9 O=C(NCC1CCNCC1)c1ccccc1-c1ccc(F)c(Cl)c1 10.1016/j.bmcl.2010.04.128
25199525 16088 None 0 Human Functional pEC50 = 7.6 7.6 5 3
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 358 4 0 5 4.0 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccccc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223807 16088 None 0 Human Functional pEC50 = 7.6 7.6 5 3
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 358 4 0 5 4.0 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccccc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
117937675 123037 None 0 Human Functional pEC50 = 7.6 7.6 2 2
Positive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as basal and acetylcholine-stimulated Ca2+ level by FLIPR assayPositive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as basal and acetylcholine-stimulated Ca2+ level by FLIPR assay
ChEMBL 448 5 2 7 3.1 Cn1cc(-c2ccc(Cn3nc(C(=O)N[C@H]4CCCC[C@@H]4O)c4ncccc43)c(F)c2)cn1 10.1021/acsmedchemlett.5b00185
CHEMBL3608415 123037 None 0 Human Functional pEC50 = 7.6 7.6 2 2
Positive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as basal and acetylcholine-stimulated Ca2+ level by FLIPR assayPositive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as basal and acetylcholine-stimulated Ca2+ level by FLIPR assay
ChEMBL 448 5 2 7 3.1 Cn1cc(-c2ccc(Cn3nc(C(=O)N[C@H]4CCCC[C@@H]4O)c4ncccc43)c(F)c2)cn1 10.1021/acsmedchemlett.5b00185
187 255 None 24 Human Functional pEC50 = 7.6 7.6 -5 8
Agonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2015.08.011
187.0 255 None 24 Human Functional pEC50 = 7.6 7.6 -5 8
Agonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2015.08.011
294 255 None 24 Human Functional pEC50 = 7.6 7.6 -5 8
Agonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2015.08.011
65 255 None 24 Human Functional pEC50 = 7.6 7.6 -5 8
Agonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2015.08.011
8593 255 None 24 Human Functional pEC50 = 7.6 7.6 -5 8
Agonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2015.08.011
CHEMBL667 255 None 24 Human Functional pEC50 = 7.6 7.6 -5 8
Agonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2015.08.011
DB03128 255 None 24 Human Functional pEC50 = 7.6 7.6 -5 8
Agonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2015.08.011
2551 794 None 13 Human Functional pEC50 = 6.6 6.6 -27 13
Agonist activity at EGFP-fused human M1 receptor N-terminal truncated at 17 residues expressed in HEK293 cells assessed as induction of calcium response by fluorescence assayAgonist activity at EGFP-fused human M1 receptor N-terminal truncated at 17 residues expressed in HEK293 cells assessed as induction of calcium response by fluorescence assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm201348t
2551.0 794 None 13 Human Functional pEC50 = 6.6 6.6 -27 13
Agonist activity at EGFP-fused human M1 receptor N-terminal truncated at 17 residues expressed in HEK293 cells assessed as induction of calcium response by fluorescence assayAgonist activity at EGFP-fused human M1 receptor N-terminal truncated at 17 residues expressed in HEK293 cells assessed as induction of calcium response by fluorescence assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm201348t
298 794 None 13 Human Functional pEC50 = 6.6 6.6 -27 13
Agonist activity at EGFP-fused human M1 receptor N-terminal truncated at 17 residues expressed in HEK293 cells assessed as induction of calcium response by fluorescence assayAgonist activity at EGFP-fused human M1 receptor N-terminal truncated at 17 residues expressed in HEK293 cells assessed as induction of calcium response by fluorescence assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm201348t
488 794 None 13 Human Functional pEC50 = 6.6 6.6 -27 13
Agonist activity at EGFP-fused human M1 receptor N-terminal truncated at 17 residues expressed in HEK293 cells assessed as induction of calcium response by fluorescence assayAgonist activity at EGFP-fused human M1 receptor N-terminal truncated at 17 residues expressed in HEK293 cells assessed as induction of calcium response by fluorescence assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm201348t
CHEMBL965 794 None 13 Human Functional pEC50 = 6.6 6.6 -27 13
Agonist activity at EGFP-fused human M1 receptor N-terminal truncated at 17 residues expressed in HEK293 cells assessed as induction of calcium response by fluorescence assayAgonist activity at EGFP-fused human M1 receptor N-terminal truncated at 17 residues expressed in HEK293 cells assessed as induction of calcium response by fluorescence assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm201348t
DB00411 794 None 13 Human Functional pEC50 = 6.6 6.6 -27 13
Agonist activity at EGFP-fused human M1 receptor N-terminal truncated at 17 residues expressed in HEK293 cells assessed as induction of calcium response by fluorescence assayAgonist activity at EGFP-fused human M1 receptor N-terminal truncated at 17 residues expressed in HEK293 cells assessed as induction of calcium response by fluorescence assay
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm201348t
57399810 68280 None 0 Rat Functional pEC50 = 6.6 6.6 - 1
Agonist activity at rat muscarinic M1 receptor expressed in CHO cellsAgonist activity at rat muscarinic M1 receptor expressed in CHO cells
ChEMBL 389 5 1 5 2.5 CCOC(=O)N1CCC(N2CCC[C@@H](NC(=O)c3cccc(OC)c3)C2)CC1 10.1016/j.bmcl.2011.08.084
CHEMBL1916228 68280 None 0 Rat Functional pEC50 = 6.6 6.6 - 1
Agonist activity at rat muscarinic M1 receptor expressed in CHO cellsAgonist activity at rat muscarinic M1 receptor expressed in CHO cells
ChEMBL 389 5 1 5 2.5 CCOC(=O)N1CCC(N2CCC[C@@H](NC(=O)c3cccc(OC)c3)C2)CC1 10.1016/j.bmcl.2011.08.084
118124117 4050 None 12 Human Functional pEC50 = 6.6 6.6 -2 2
Positive allosteric modulation of human muscarinic acetylcholine M1 receptorPositive allosteric modulation of human muscarinic acetylcholine M1 receptor
ChEMBL 432 5 2 6 3.1 C1CC[C@@H]([C@H](C1)NC(=O)[C@H]1CN(c2ccccc2O1)Cc1ccc(cc1)n1cccn1)O 10.1016/j.bmcl.2018.05.009
12305 4050 None 12 Human Functional pEC50 = 6.6 6.6 -2 2
Positive allosteric modulation of human muscarinic acetylcholine M1 receptorPositive allosteric modulation of human muscarinic acetylcholine M1 receptor
ChEMBL 432 5 2 6 3.1 C1CC[C@@H]([C@H](C1)NC(=O)[C@H]1CN(c2ccccc2O1)Cc1ccc(cc1)n1cccn1)O 10.1016/j.bmcl.2018.05.009
CHEMBL4127762 4050 None 12 Human Functional pEC50 = 6.6 6.6 -2 2
Positive allosteric modulation of human muscarinic acetylcholine M1 receptorPositive allosteric modulation of human muscarinic acetylcholine M1 receptor
ChEMBL 432 5 2 6 3.1 C1CC[C@@H]([C@H](C1)NC(=O)[C@H]1CN(c2ccccc2O1)Cc1ccc(cc1)n1cccn1)O 10.1016/j.bmcl.2018.05.009
118124117 4050 None 12 Rat Functional pEC50 = 6.6 6.6 2 2
Positive allosteric modulation of rat muscarinic acetylcholine M1 receptorPositive allosteric modulation of rat muscarinic acetylcholine M1 receptor
ChEMBL 432 5 2 6 3.1 C1CC[C@@H]([C@H](C1)NC(=O)[C@H]1CN(c2ccccc2O1)Cc1ccc(cc1)n1cccn1)O 10.1016/j.bmcl.2018.05.009
12305 4050 None 12 Rat Functional pEC50 = 6.6 6.6 2 2
Positive allosteric modulation of rat muscarinic acetylcholine M1 receptorPositive allosteric modulation of rat muscarinic acetylcholine M1 receptor
ChEMBL 432 5 2 6 3.1 C1CC[C@@H]([C@H](C1)NC(=O)[C@H]1CN(c2ccccc2O1)Cc1ccc(cc1)n1cccn1)O 10.1016/j.bmcl.2018.05.009
CHEMBL4127762 4050 None 12 Rat Functional pEC50 = 6.6 6.6 2 2
Positive allosteric modulation of rat muscarinic acetylcholine M1 receptorPositive allosteric modulation of rat muscarinic acetylcholine M1 receptor
ChEMBL 432 5 2 6 3.1 C1CC[C@@H]([C@H](C1)NC(=O)[C@H]1CN(c2ccccc2O1)Cc1ccc(cc1)n1cccn1)O 10.1016/j.bmcl.2018.05.009
70681454 74378 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
ChEMBL 380 5 2 4 2.7 CCOC(=O)N1[C@H]2CC[C@@H]1C[C@@H](NCCNC(=O)N1[C@@H](C)CCC[C@H]1C)C2 10.1016/j.bmcl.2012.03.088
CHEMBL2024427 74378 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
ChEMBL 380 5 2 4 2.7 CCOC(=O)N1[C@H]2CC[C@@H]1C[C@@H](NCCNC(=O)N1[C@@H](C)CCC[C@H]1C)C2 10.1016/j.bmcl.2012.03.088
118123991 161522 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 407 5 2 5 3.1 O=C(N[C@H]1CCCC[C@@H]1O)C1CN(Cc2ccc(C3CC3)nc2)c2ccccc2O1 10.1016/j.bmcl.2018.05.009
CHEMBL4127046 161522 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 407 5 2 5 3.1 O=C(N[C@H]1CCCC[C@@H]1O)C1CN(Cc2ccc(C3CC3)nc2)c2ccccc2O1 10.1016/j.bmcl.2018.05.009
139414069 164262 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Positive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assayPositive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 340 3 1 2 5.1 S=C1Nc2ccc(Cl)cc2C(c2ccccc2)=N[C@H]1CC1CC1 10.1016/j.bmcl.2017.11.008
CHEMBL4210455 164262 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Positive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assayPositive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 340 3 1 2 5.1 S=C1Nc2ccc(Cl)cc2C(c2ccccc2)=N[C@H]1CC1CC1 10.1016/j.bmcl.2017.11.008
9913341 82189 None 4 Human Functional pEC50 = 6.6 6.6 -630 3
Agonist activity at human M1 receptor Q185E mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M1 receptor Q185E mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 487 16 0 13 1.6 COc1nsnc1OCCOCCOCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0606995
CHEMBL216927 82189 None 4 Human Functional pEC50 = 6.6 6.6 -630 3
Agonist activity at human M1 receptor Q185E mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M1 receptor Q185E mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 487 16 0 13 1.6 COc1nsnc1OCCOCCOCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0606995
CHEMBL553058 82189 None 4 Human Functional pEC50 = 6.6 6.6 -630 3
Agonist activity at human M1 receptor Q185E mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M1 receptor Q185E mutant expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 487 16 0 13 1.6 COc1nsnc1OCCOCCOCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0606995
44418764 82190 None 0 Human Functional pEC50 = 6.6 6.6 1 4
Agonist activity at human M1 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M1 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 487 16 0 13 1.8 COc1nsc(OCCOCCOCCOCCOc2nsnc2C2C=CCCN2C)n1 10.1021/jm0606995
CHEMBL216928 82190 None 0 Human Functional pEC50 = 6.6 6.6 1 4
Agonist activity at human M1 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M1 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 487 16 0 13 1.8 COc1nsc(OCCOCCOCCOCCOc2nsnc2C2C=CCCN2C)n1 10.1021/jm0606995
16094788 142002 None 0 Human Functional pEC50 = 6.6 6.6 1 3
Agonist activity at human M1 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M1 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 531 19 0 14 1.6 COc1nsnc1OCCOCCOCCOCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0606995
CHEMBL386983 142002 None 0 Human Functional pEC50 = 6.6 6.6 1 3
Agonist activity at human M1 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M1 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 531 19 0 14 1.6 COc1nsnc1OCCOCCOCCOCCOCCOc1nsnc1C1=CCCN(C)C1 10.1021/jm0606995
46891376 6410 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 361 4 1 4 3.7 O=C(NCC12CCN(CC1)CC2)c1ccccc1-c1nc(Cl)cs1 10.1016/j.bmcl.2010.04.128
CHEMBL1082341 6410 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 361 4 1 4 3.7 O=C(NCC12CCN(CC1)CC2)c1ccccc1-c1nc(Cl)cs1 10.1016/j.bmcl.2010.04.128
46891375 6806 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 335 4 2 4 3.2 O=C(NCC1CCNCC1)c1ccccc1-c1nc(Cl)cs1 10.1016/j.bmcl.2010.04.127
46891375 6806 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 335 4 2 4 3.2 O=C(NCC1CCNCC1)c1ccccc1-c1nc(Cl)cs1 10.1016/j.bmcl.2010.04.128
CHEMBL1083911 6806 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 335 4 2 4 3.2 O=C(NCC1CCNCC1)c1ccccc1-c1nc(Cl)cs1 10.1016/j.bmcl.2010.04.127
CHEMBL1083911 6806 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 335 4 2 4 3.2 O=C(NCC1CCNCC1)c1ccccc1-c1nc(Cl)cs1 10.1016/j.bmcl.2010.04.128
10092649 193182 None 43 Human Functional pEC50 = 6.6 6.6 -2 11
Partial agonist activity at human muscarinic M1 receptor expressed in CHO cells calcium responsePartial agonist activity at human muscarinic M1 receptor expressed in CHO cells calcium response
ChEMBL 404 4 1 4 3.9 Cc1ccccc1CN1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1 10.1016/j.bmcl.2012.10.132
CHEMBL522460 193182 None 43 Human Functional pEC50 = 6.6 6.6 -2 11
Partial agonist activity at human muscarinic M1 receptor expressed in CHO cells calcium responsePartial agonist activity at human muscarinic M1 receptor expressed in CHO cells calcium response
ChEMBL 404 4 1 4 3.9 Cc1ccccc1CN1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1 10.1016/j.bmcl.2012.10.132
127039041 137062 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Positive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as increase in ACh-induced intracellular calcium level preincubated for 10 mins followed by ACh addition measured every 2 secs for 80 secs by Fluo-4 dye-based FLIPR assayPositive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as increase in ACh-induced intracellular calcium level preincubated for 10 mins followed by ACh addition measured every 2 secs for 80 secs by Fluo-4 dye-based FLIPR assay
ChEMBL 445 5 2 7 2.7 Cc1ccc2c(n1)c(C(=O)N[C@H]1CCOC[C@@H]1O)cn2Cc1ccc(-c2ccn(C)n2)cc1 10.1016/j.bmcl.2018.04.054
CHEMBL3745724 137062 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Positive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as increase in ACh-induced intracellular calcium level preincubated for 10 mins followed by ACh addition measured every 2 secs for 80 secs by Fluo-4 dye-based FLIPR assayPositive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as increase in ACh-induced intracellular calcium level preincubated for 10 mins followed by ACh addition measured every 2 secs for 80 secs by Fluo-4 dye-based FLIPR assay
ChEMBL 445 5 2 7 2.7 Cc1ccc2c(n1)c(C(=O)N[C@H]1CCOC[C@@H]1O)cn2Cc1ccc(-c2ccn(C)n2)cc1 10.1016/j.bmcl.2018.04.054
10092649 193182 None 43 Human Functional pEC50 = 6.6 6.6 -2 11
Partial agonist activity at human muscarinic M1 receptor expressed in CHO cells calcium responsePartial agonist activity at human muscarinic M1 receptor expressed in CHO cells calcium response
ChEMBL 404 4 1 4 3.9 Cc1ccccc1CN1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1 10.1016/j.bmcl.2012.10.132
CHEMBL522460 193182 None 43 Human Functional pEC50 = 6.6 6.6 -2 11
Partial agonist activity at human muscarinic M1 receptor expressed in CHO cells calcium responsePartial agonist activity at human muscarinic M1 receptor expressed in CHO cells calcium response
ChEMBL 404 4 1 4 3.9 Cc1ccccc1CN1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1 10.1016/j.bmcl.2012.10.132
145984780 165801 None 0 Rat Functional pEC50 = 6.6 6.6 - 1
Positive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assayPositive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assay
ChEMBL 430 5 2 7 2.6 Cn1ccc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCC[C@H]4O)nc4c3ccn4C)cn2)n1 10.1021/acsmedchemlett.8b00261
CHEMBL4245556 165801 None 0 Rat Functional pEC50 = 6.6 6.6 - 1
Positive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assayPositive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assay
ChEMBL 430 5 2 7 2.6 Cn1ccc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCC[C@H]4O)nc4c3ccn4C)cn2)n1 10.1021/acsmedchemlett.8b00261
127038679 137207 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Positive allosteric modulation of human M1 receptor expressed in CHO cells assessed as acetylcholine-induced calcium mobilization by FLIPR assayPositive allosteric modulation of human M1 receptor expressed in CHO cells assessed as acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 397 5 1 7 3.3 Cn1ccc(NC(=O)c2cn(Cc3ccc(-n4cccn4)cc3)c3cccnc23)n1 10.1016/j.bmcl.2015.11.053
CHEMBL3747724 137207 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Positive allosteric modulation of human M1 receptor expressed in CHO cells assessed as acetylcholine-induced calcium mobilization by FLIPR assayPositive allosteric modulation of human M1 receptor expressed in CHO cells assessed as acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 397 5 1 7 3.3 Cn1ccc(NC(=O)c2cn(Cc3ccc(-n4cccn4)cc3)c3cccnc23)n1 10.1016/j.bmcl.2015.11.053
44214356 18016 None 0 Human Functional pEC50 = 6.6 6.6 -11 2
Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.
ChEMBL 311 8 0 6 3.0 CCCCCCOc1nsnc1OC1CN2CCC1CC2 10.1021/jm970125n
CHEMBL126332 18016 None 0 Human Functional pEC50 = 6.6 6.6 -11 2
Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.
ChEMBL 311 8 0 6 3.0 CCCCCCOc1nsnc1OC1CN2CCC1CC2 10.1021/jm970125n
156246132 196237 None 3 Human Functional pEC50 = 7.6 7.6 -4 3
Activation of human muscarinic M1 receptor expressed in HEK293 cells incubated for 3 mins by Calcium flux assayActivation of human muscarinic M1 receptor expressed in HEK293 cells incubated for 3 mins by Calcium flux assay
ChEMBL 398 5 0 4 3.3 CCOc1ccccc1C1CCN([C@@H]2CCC3(C2)CN(C(=O)C2COC2)C3)CC1 10.1021/acsmedchemlett.3c00331
CHEMBL5419462 196237 None 3 Human Functional pEC50 = 7.6 7.6 -4 3
Activation of human muscarinic M1 receptor expressed in HEK293 cells incubated for 3 mins by Calcium flux assayActivation of human muscarinic M1 receptor expressed in HEK293 cells incubated for 3 mins by Calcium flux assay
ChEMBL 398 5 0 4 3.3 CCOc1ccccc1C1CCN([C@@H]2CCC3(C2)CN(C(=O)C2COC2)C3)CC1 10.1021/acsmedchemlett.3c00331
10251795 181928 None 1 Human Functional pEC50 = 6.6 6.6 7 2
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
ChEMBL 424 4 1 4 4.3 O=c1[nH]c2ccccc2n1C1CCN(C2CCN(Cc3ccccc3Cl)CC2)CC1 10.1016/j.bmcl.2008.09.023
CHEMBL477821 181928 None 1 Human Functional pEC50 = 6.6 6.6 7 2
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
ChEMBL 424 4 1 4 4.3 O=c1[nH]c2ccccc2n1C1CCN(C2CCN(Cc3ccccc3Cl)CC2)CC1 10.1016/j.bmcl.2008.09.023
145984780 165801 None 0 Rat Functional pEC50 = 6.6 6.6 - 1
Positive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assayPositive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assay
ChEMBL 430 5 2 7 2.6 Cn1ccc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCC[C@H]4O)nc4c3ccn4C)cn2)n1 10.1021/acsmedchemlett.8b00261
CHEMBL4245556 165801 None 0 Rat Functional pEC50 = 6.6 6.6 - 1
Positive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assayPositive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assay
ChEMBL 430 5 2 7 2.6 Cn1ccc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCC[C@H]4O)nc4c3ccn4C)cn2)n1 10.1021/acsmedchemlett.8b00261
25010776 55971 None 1 Human Functional pEC50 = 5.6 5.6 1 5
Agonist activity at human muscarinic M1 receptor by calcium mobilization assayAgonist activity at human muscarinic M1 receptor by calcium mobilization assay
ChEMBL 333 6 2 4 1.9 CCOC(=O)N1CCC(NCCNC(=O)c2ccccc2C)CC1 10.1016/j.bmcl.2012.03.088
CHEMBL1559151 55971 None 1 Human Functional pEC50 = 5.6 5.6 1 5
Agonist activity at human muscarinic M1 receptor by calcium mobilization assayAgonist activity at human muscarinic M1 receptor by calcium mobilization assay
ChEMBL 333 6 2 4 1.9 CCOC(=O)N1CCC(NCCNC(=O)c2ccccc2C)CC1 10.1016/j.bmcl.2012.03.088
CHEMBL1624037 55971 None 1 Human Functional pEC50 = 5.6 5.6 1 5
Agonist activity at human muscarinic M1 receptor by calcium mobilization assayAgonist activity at human muscarinic M1 receptor by calcium mobilization assay
ChEMBL 333 6 2 4 1.9 CCOC(=O)N1CCC(NCCNC(=O)c2ccccc2C)CC1 10.1016/j.bmcl.2012.03.088
44589593 185950 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
ChEMBL 458 4 1 5 3.0 O=c1[nH]c2c(F)cccc2n1C1CCN(C2CCN(S(=O)(=O)c3ccccc3)CC2)CC1 10.1016/j.bmcl.2008.09.032
CHEMBL486758 185950 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
ChEMBL 458 4 1 5 3.0 O=c1[nH]c2c(F)cccc2n1C1CCN(C2CCN(S(=O)(=O)c3ccccc3)CC2)CC1 10.1016/j.bmcl.2008.09.032
46873655 68286 None 0 Rat Functional pEC50 = 5.6 5.6 - 1
Agonist activity at rat muscarinic M1 receptor expressed in CHO cellsAgonist activity at rat muscarinic M1 receptor expressed in CHO cells
ChEMBL 393 4 1 4 3.2 CCOC(=O)N1CCC(N2CCC[C@@H](NC(=O)c3ccccc3Cl)C2)CC1 10.1016/j.bmcl.2011.08.084
CHEMBL1916234 68286 None 0 Rat Functional pEC50 = 5.6 5.6 - 1
Agonist activity at rat muscarinic M1 receptor expressed in CHO cellsAgonist activity at rat muscarinic M1 receptor expressed in CHO cells
ChEMBL 393 4 1 4 3.2 CCOC(=O)N1CCC(N2CCC[C@@H](NC(=O)c3ccccc3Cl)C2)CC1 10.1016/j.bmcl.2011.08.084
3652 4097 None 50 Human Functional pEC50 = 5.6 5.6 -18 15
Agonistic activity against M1 muscarinic receptor expressed in NIH 3T3 cellsAgonistic activity against M1 muscarinic receptor expressed in NIH 3T3 cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0102405
57 4097 None 50 Human Functional pEC50 = 5.6 5.6 -18 15
Agonistic activity against M1 muscarinic receptor expressed in NIH 3T3 cellsAgonistic activity against M1 muscarinic receptor expressed in NIH 3T3 cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0102405
60809 4097 None 50 Human Functional pEC50 = 5.6 5.6 -18 15
Agonistic activity against M1 muscarinic receptor expressed in NIH 3T3 cellsAgonistic activity against M1 muscarinic receptor expressed in NIH 3T3 cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0102405
60809.0 4097 None 50 Human Functional pEC50 = 5.6 5.6 -18 15
Agonistic activity against M1 muscarinic receptor expressed in NIH 3T3 cellsAgonistic activity against M1 muscarinic receptor expressed in NIH 3T3 cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0102405
CHEMBL21536 4097 None 50 Human Functional pEC50 = 5.6 5.6 -18 15
Agonistic activity against M1 muscarinic receptor expressed in NIH 3T3 cellsAgonistic activity against M1 muscarinic receptor expressed in NIH 3T3 cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0102405
DB15357 4097 None 50 Human Functional pEC50 = 5.6 5.6 -18 15
Agonistic activity against M1 muscarinic receptor expressed in NIH 3T3 cellsAgonistic activity against M1 muscarinic receptor expressed in NIH 3T3 cells
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0102405
145963344 161441 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 430 5 1 6 3.3 O=C(N[C@H]1CCCCC1=O)C1CN(Cc2ccc(-n3cccn3)cc2)c2ccccc2O1 10.1016/j.bmcl.2018.05.009
CHEMBL4125860 161441 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 430 5 1 6 3.3 O=C(N[C@H]1CCCCC1=O)C1CN(Cc2ccc(-n3cccn3)cc2)c2ccccc2O1 10.1016/j.bmcl.2018.05.009
145975401 163896 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Positive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assayPositive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 344 2 1 2 5.0 CC(C)C1C(=O)N(c2ccccc2)c2cc(Cl)ccc2NC1=S 10.1016/j.bmcl.2017.11.008
CHEMBL4206066 163896 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Positive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assayPositive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 344 2 1 2 5.0 CC(C)C1C(=O)N(c2ccccc2)c2cc(Cl)ccc2NC1=S 10.1016/j.bmcl.2017.11.008
46930250 16737 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 345 6 1 4 1.8 CCC(=O)NC1CCN(CCCN2C(=O)COc3ccccc32)CC1 10.1021/jm100697g
CHEMBL1243232 16737 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 345 6 1 4 1.8 CCC(=O)NC1CCN(CCCN2C(=O)COc3ccccc32)CC1 10.1021/jm100697g
145963344 161441 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 430 5 1 6 3.3 O=C(N[C@H]1CCCCC1=O)C1CN(Cc2ccc(-n3cccn3)cc2)c2ccccc2O1 10.1016/j.bmcl.2018.05.009
CHEMBL4125860 161441 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 430 5 1 6 3.3 O=C(N[C@H]1CCCCC1=O)C1CN(Cc2ccc(-n3cccn3)cc2)c2ccccc2O1 10.1016/j.bmcl.2018.05.009
187 255 None 24 Human Functional pEC50 = 4.6 4.6 -5 8
Agonist activity at human muscarinic M1 receptor Y381A mutant expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human muscarinic M1 receptor Y381A mutant expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2012.05.048
187.0 255 None 24 Human Functional pEC50 = 4.6 4.6 -5 8
Agonist activity at human muscarinic M1 receptor Y381A mutant expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human muscarinic M1 receptor Y381A mutant expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2012.05.048
294 255 None 24 Human Functional pEC50 = 4.6 4.6 -5 8
Agonist activity at human muscarinic M1 receptor Y381A mutant expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human muscarinic M1 receptor Y381A mutant expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2012.05.048
65 255 None 24 Human Functional pEC50 = 4.6 4.6 -5 8
Agonist activity at human muscarinic M1 receptor Y381A mutant expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human muscarinic M1 receptor Y381A mutant expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2012.05.048
8593 255 None 24 Human Functional pEC50 = 4.6 4.6 -5 8
Agonist activity at human muscarinic M1 receptor Y381A mutant expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human muscarinic M1 receptor Y381A mutant expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2012.05.048
CHEMBL667 255 None 24 Human Functional pEC50 = 4.6 4.6 -5 8
Agonist activity at human muscarinic M1 receptor Y381A mutant expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human muscarinic M1 receptor Y381A mutant expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2012.05.048
DB03128 255 None 24 Human Functional pEC50 = 4.6 4.6 -5 8
Agonist activity at human muscarinic M1 receptor Y381A mutant expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human muscarinic M1 receptor Y381A mutant expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1016/j.bmcl.2012.05.048
187 255 None 24 Human Functional pEC50 = 4.6 4.6 -5 8
Agonist activity at human muscarinic M1 receptor Y381A mutant expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor Y381A mutant expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm100697g
187.0 255 None 24 Human Functional pEC50 = 4.6 4.6 -5 8
Agonist activity at human muscarinic M1 receptor Y381A mutant expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor Y381A mutant expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm100697g
294 255 None 24 Human Functional pEC50 = 4.6 4.6 -5 8
Agonist activity at human muscarinic M1 receptor Y381A mutant expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor Y381A mutant expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm100697g
65 255 None 24 Human Functional pEC50 = 4.6 4.6 -5 8
Agonist activity at human muscarinic M1 receptor Y381A mutant expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor Y381A mutant expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm100697g
8593 255 None 24 Human Functional pEC50 = 4.6 4.6 -5 8
Agonist activity at human muscarinic M1 receptor Y381A mutant expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor Y381A mutant expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm100697g
CHEMBL667 255 None 24 Human Functional pEC50 = 4.6 4.6 -5 8
Agonist activity at human muscarinic M1 receptor Y381A mutant expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor Y381A mutant expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm100697g
DB03128 255 None 24 Human Functional pEC50 = 4.6 4.6 -5 8
Agonist activity at human muscarinic M1 receptor Y381A mutant expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor Y381A mutant expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm100697g
10419574 58112 None 0 Human Functional pEC50 = 4.6 4.6 -2 2
Effective concentration for HMPA (human muscarinic inositol phosphate accumulation) activity measured in CHO cells expressing Muscarinic acetylcholine receptor M1Effective concentration for HMPA (human muscarinic inositol phosphate accumulation) activity measured in CHO cells expressing Muscarinic acetylcholine receptor M1
ChEMBL 168 3 0 3 1.1 CCCO/N=C1\CN2CCC1C2 10.1016/S0960-894X(00)80538-7
CHEMBL167438 58112 None 0 Human Functional pEC50 = 4.6 4.6 -2 2
Effective concentration for HMPA (human muscarinic inositol phosphate accumulation) activity measured in CHO cells expressing Muscarinic acetylcholine receptor M1Effective concentration for HMPA (human muscarinic inositol phosphate accumulation) activity measured in CHO cells expressing Muscarinic acetylcholine receptor M1
ChEMBL 168 3 0 3 1.1 CCCO/N=C1\CN2CCC1C2 10.1016/S0960-894X(00)80538-7
44590186 179187 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
ChEMBL 452 3 1 4 4.2 Cc1ccccc1C(=O)N1CCC(N2CCC(n3c(=O)[nH]c4cc(Cl)ccc43)CC2)CC1 10.1016/j.bmcl.2008.09.032
CHEMBL471635 179187 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
ChEMBL 452 3 1 4 4.2 Cc1ccccc1C(=O)N1CCC(N2CCC(n3c(=O)[nH]c4cc(Cl)ccc43)CC2)CC1 10.1016/j.bmcl.2008.09.032
127038318 137158 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Positive allosteric modulation of human M1 receptor expressed in CHO cells assessed as acetylcholine-induced calcium mobilization by FLIPR assayPositive allosteric modulation of human M1 receptor expressed in CHO cells assessed as acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 492 6 2 7 4.4 O=C(N[C@H]1CCCC[C@@H]1O)c1cn(Cc2ccc(-n3cc(-c4ccncc4)cn3)cc2)c2cccnc12 10.1016/j.bmcl.2015.11.053
CHEMBL3747037 137158 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Positive allosteric modulation of human M1 receptor expressed in CHO cells assessed as acetylcholine-induced calcium mobilization by FLIPR assayPositive allosteric modulation of human M1 receptor expressed in CHO cells assessed as acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 492 6 2 7 4.4 O=C(N[C@H]1CCCC[C@@H]1O)c1cn(Cc2ccc(-n3cc(-c4ccncc4)cn3)cc2)c2cccnc12 10.1016/j.bmcl.2015.11.053
145963886 164358 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Positive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assayPositive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 329 2 1 3 4.4 CC(C)[C@@H]1N=C(c2cccnc2)c2cc(Cl)ccc2NC1=S 10.1016/j.bmcl.2017.11.008
CHEMBL4211618 164358 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Positive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assayPositive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 329 2 1 3 4.4 CC(C)[C@@H]1N=C(c2cccnc2)c2cc(Cl)ccc2NC1=S 10.1016/j.bmcl.2017.11.008
117686764 141130 None 0 Rat Functional pEC50 = 5.6 5.6 - 1
Positive allosteric modulation at rat muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation at rat muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 403 3 0 6 3.7 Cn1cc2cc(-c3cc(F)c(Cn4c(=O)cnc5ncccc54)c(F)c3)ccc2n1 10.1016/j.bmcl.2016.04.083
CHEMBL3824114 141130 None 0 Rat Functional pEC50 = 5.6 5.6 - 1
Positive allosteric modulation at rat muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation at rat muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 403 3 0 6 3.7 Cn1cc2cc(-c3cc(F)c(Cn4c(=O)cnc5ncccc54)c(F)c3)ccc2n1 10.1016/j.bmcl.2016.04.083
146216774 186118 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL 377 3 0 4 4.6 Cn1cc2cc(-c3ccc(CN4Cc5sccc5C4=O)c(F)c3)ccc2n1 10.1016/j.bmcl.2021.128193
CHEMBL4870412 186118 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL 377 3 0 4 4.6 Cn1cc2cc(-c3ccc(CN4Cc5sccc5C4=O)c(F)c3)ccc2n1 10.1016/j.bmcl.2021.128193
71460588 81982 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Antagonist activity at human muscarinic M1 receptorAntagonist activity at human muscarinic M1 receptor
ChEMBL 326 4 0 2 2.9 CN1CCN(C(=O)C(F)(Cc2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2012.09.011
CHEMBL2164910 81982 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Antagonist activity at human muscarinic M1 receptorAntagonist activity at human muscarinic M1 receptor
ChEMBL 326 4 0 2 2.9 CN1CCN(C(=O)C(F)(Cc2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2012.09.011
44330080 107776 None 0 Human Functional pEC50 = 7.6 7.6 8 2
Stimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptorStimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptor
ChEMBL 325 3 0 5 2.8 C(#Cc1ccccc1)COc1nsnc1[C@@H]1CN2CCC[C@H]1C2 10.1016/s0960-894x(98)00509-5
CHEMBL319109 107776 None 0 Human Functional pEC50 = 7.6 7.6 8 2
Stimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptorStimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptor
ChEMBL 325 3 0 5 2.8 C(#Cc1ccccc1)COc1nsnc1[C@@H]1CN2CCC[C@H]1C2 10.1016/s0960-894x(98)00509-5
117937644 123036 None 0 Human Functional pEC50 = 7.5 7.5 2 2
Positive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as basal and acetylcholine-stimulated Ca2+ level by FLIPR assayPositive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as basal and acetylcholine-stimulated Ca2+ level by FLIPR assay
ChEMBL 449 5 2 7 2.5 Cn1cc(-c2ccc(Cn3cc(C(=O)N[C@H]4CCOC[C@@H]4O)c4ncccc43)c(F)c2)cn1 10.1021/acsmedchemlett.5b00185
CHEMBL3608414 123036 None 0 Human Functional pEC50 = 7.5 7.5 2 2
Positive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as basal and acetylcholine-stimulated Ca2+ level by FLIPR assayPositive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as basal and acetylcholine-stimulated Ca2+ level by FLIPR assay
ChEMBL 449 5 2 7 2.5 Cn1cc(-c2ccc(Cn3cc(C(=O)N[C@H]4CCOC[C@@H]4O)c4ncccc43)c(F)c2)cn1 10.1021/acsmedchemlett.5b00185
117686764 141130 None 0 Rat Functional pEC50 = 5.6 5.6 - 1
Positive allosteric modulation at rat muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation at rat muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 403 3 0 6 3.7 Cn1cc2cc(-c3cc(F)c(Cn4c(=O)cnc5ncccc54)c(F)c3)ccc2n1 10.1016/j.bmcl.2016.04.083
CHEMBL3824114 141130 None 0 Rat Functional pEC50 = 5.6 5.6 - 1
Positive allosteric modulation at rat muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation at rat muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 403 3 0 6 3.7 Cn1cc2cc(-c3cc(F)c(Cn4c(=O)cnc5ncccc54)c(F)c3)ccc2n1 10.1016/j.bmcl.2016.04.083
145961841 161740 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 466 5 2 6 3.7 O=C(N[C@H]1CCCC[C@@H]1O)C1CN(Cc2ccc(-n3cccn3)cc2)c2cc(Cl)ccc2O1 10.1016/j.bmcl.2018.05.009
CHEMBL4130215 161740 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 466 5 2 6 3.7 O=C(N[C@H]1CCCC[C@@H]1O)C1CN(Cc2ccc(-n3cccn3)cc2)c2cc(Cl)ccc2O1 10.1016/j.bmcl.2018.05.009
145961106 161597 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 433 5 2 7 2.5 O=C(N[C@H]1CCCC[C@@H]1O)C1CN(Cc2ccc(-n3ccnc3)nc2)c2ccccc2O1 10.1016/j.bmcl.2018.05.009
CHEMBL4128093 161597 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 433 5 2 7 2.5 O=C(N[C@H]1CCCC[C@@H]1O)C1CN(Cc2ccc(-n3ccnc3)nc2)c2ccccc2O1 10.1016/j.bmcl.2018.05.009
146216742 185858 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL 395 3 0 4 4.7 Cn1cnc2ccc(-c3cc(F)c(CN4Cc5sccc5C4=O)c(F)c3)cc21 10.1016/j.bmcl.2021.128193
CHEMBL4866266 185858 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL 395 3 0 4 4.7 Cn1cnc2ccc(-c3cc(F)c(CN4Cc5sccc5C4=O)c(F)c3)cc21 10.1016/j.bmcl.2021.128193
10092649 193182 None 43 Human Functional pEC50 = 6.5 6.5 -2 11
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
ChEMBL 404 4 1 4 3.9 Cc1ccccc1CN1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1 10.1016/j.bmcl.2008.09.023
10092649 193182 None 43 Human Functional pEC50 = 6.5 6.5 -2 11
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
ChEMBL 404 4 1 4 3.9 Cc1ccccc1CN1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1 10.1016/j.bmcl.2008.09.032
CHEMBL522460 193182 None 43 Human Functional pEC50 = 6.5 6.5 -2 11
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
ChEMBL 404 4 1 4 3.9 Cc1ccccc1CN1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1 10.1016/j.bmcl.2008.09.023
CHEMBL522460 193182 None 43 Human Functional pEC50 = 6.5 6.5 -2 11
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
ChEMBL 404 4 1 4 3.9 Cc1ccccc1CN1CCC(N2CCC(n3c(=O)[nH]c4ccccc43)CC2)CC1 10.1016/j.bmcl.2008.09.032
145971391 164734 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assayPositive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 329 2 1 3 4.4 CC(C)[C@@H]1N=C(c2ccccn2)c2cc(Cl)ccc2NC1=S 10.1016/j.bmcl.2017.11.008
CHEMBL4216319 164734 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assayPositive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 329 2 1 3 4.4 CC(C)[C@@H]1N=C(c2ccccn2)c2cc(Cl)ccc2NC1=S 10.1016/j.bmcl.2017.11.008
145970395 165170 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Positive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as increase in ACh-induced intracellular calcium level preincubated for 10 mins followed by ACh addition measured every 2 secs for 80 secs by Fluo-4 dye-based FLIPR assayPositive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as increase in ACh-induced intracellular calcium level preincubated for 10 mins followed by ACh addition measured every 2 secs for 80 secs by Fluo-4 dye-based FLIPR assay
ChEMBL 420 5 2 6 2.5 Cc1c(Cc2ccc(-n3cccn3)cc2)cc(C(=O)N[C@H]2CCCC[C@@H]2O)c(=O)n1C 10.1016/j.bmcl.2018.04.054
CHEMBL4226889 165170 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Positive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as increase in ACh-induced intracellular calcium level preincubated for 10 mins followed by ACh addition measured every 2 secs for 80 secs by Fluo-4 dye-based FLIPR assayPositive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as increase in ACh-induced intracellular calcium level preincubated for 10 mins followed by ACh addition measured every 2 secs for 80 secs by Fluo-4 dye-based FLIPR assay
ChEMBL 420 5 2 6 2.5 Cc1c(Cc2ccc(-n3cccn3)cc2)cc(C(=O)N[C@H]2CCCC[C@@H]2O)c(=O)n1C 10.1016/j.bmcl.2018.04.054
145970395 165170 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Positive allosteric modulation of human muscarinic M1 receptor stably expressed in CHO cells assessed as increase in Ach-induced intracellular calcium level preincubated for 10 mins followed by addition of Ach at EC20 concentration by Fluo-8AM dye based FLIPR TETRA methodPositive allosteric modulation of human muscarinic M1 receptor stably expressed in CHO cells assessed as increase in Ach-induced intracellular calcium level preincubated for 10 mins followed by addition of Ach at EC20 concentration by Fluo-8AM dye based FLIPR TETRA method
ChEMBL 420 5 2 6 2.5 Cc1c(Cc2ccc(-n3cccn3)cc2)cc(C(=O)N[C@H]2CCCC[C@@H]2O)c(=O)n1C 10.1021/acs.jmedchem.6b00544
CHEMBL4226889 165170 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Positive allosteric modulation of human muscarinic M1 receptor stably expressed in CHO cells assessed as increase in Ach-induced intracellular calcium level preincubated for 10 mins followed by addition of Ach at EC20 concentration by Fluo-8AM dye based FLIPR TETRA methodPositive allosteric modulation of human muscarinic M1 receptor stably expressed in CHO cells assessed as increase in Ach-induced intracellular calcium level preincubated for 10 mins followed by addition of Ach at EC20 concentration by Fluo-8AM dye based FLIPR TETRA method
ChEMBL 420 5 2 6 2.5 Cc1c(Cc2ccc(-n3cccn3)cc2)cc(C(=O)N[C@H]2CCCC[C@@H]2O)c(=O)n1C 10.1021/acs.jmedchem.6b00544
46929968 16720 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 423 7 1 3 3.3 O=C(Cc1ccccc1)NC1CCN(CCCN2C(=O)CCc3cccc(F)c32)CC1 10.1021/jm100697g
CHEMBL1243074 16720 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 423 7 1 3 3.3 O=C(Cc1ccccc1)NC1CCN(CCCN2C(=O)CCc3cccc(F)c32)CC1 10.1021/jm100697g
9809330 116063 None 0 Human Functional pEC50 = 6.5 6.5 -39 3
Agonistic activity against M1 muscarinic receptor expressed in NIH 3T3 cellsAgonistic activity against M1 muscarinic receptor expressed in NIH 3T3 cells
ChEMBL 552 16 0 13 2.3 CN1CCC=C(c2nsnc2OCCOCCOCCOCCOc2nsnc2C2=CCCN(C)C2)C1 10.1021/jm0102405
CHEMBL335542 116063 None 0 Human Functional pEC50 = 6.5 6.5 -39 3
Agonistic activity against M1 muscarinic receptor expressed in NIH 3T3 cellsAgonistic activity against M1 muscarinic receptor expressed in NIH 3T3 cells
ChEMBL 552 16 0 13 2.3 CN1CCC=C(c2nsnc2OCCOCCOCCOCCOc2nsnc2C2=CCCN(C)C2)C1 10.1021/jm0102405
145961106 161597 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 433 5 2 7 2.5 O=C(N[C@H]1CCCC[C@@H]1O)C1CN(Cc2ccc(-n3ccnc3)nc2)c2ccccc2O1 10.1016/j.bmcl.2018.05.009
CHEMBL4128093 161597 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 433 5 2 7 2.5 O=C(N[C@H]1CCCC[C@@H]1O)C1CN(Cc2ccc(-n3ccnc3)nc2)c2ccccc2O1 10.1016/j.bmcl.2018.05.009
146216736 185649 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL 475 6 0 5 4.6 Cn1cc2c(-c3cc(F)c(CN4Cc5ccn(CCN6CCCC6)c5C4=O)c(F)c3)cccc2n1 10.1016/j.bmcl.2021.128193
CHEMBL4863018 185649 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL 475 6 0 5 4.6 Cn1cc2c(-c3cc(F)c(CN4Cc5ccn(CCN6CCCC6)c5C4=O)c(F)c3)cccc2n1 10.1016/j.bmcl.2021.128193
127039041 137062 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulation of human M1 receptor expressed in CHO cells assessed as acetylcholine-induced calcium mobilization by FLIPR assayPositive allosteric modulation of human M1 receptor expressed in CHO cells assessed as acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 445 5 2 7 2.7 Cc1ccc2c(n1)c(C(=O)N[C@H]1CCOC[C@@H]1O)cn2Cc1ccc(-c2ccn(C)n2)cc1 10.1016/j.bmcl.2015.11.053
CHEMBL3745724 137062 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulation of human M1 receptor expressed in CHO cells assessed as acetylcholine-induced calcium mobilization by FLIPR assayPositive allosteric modulation of human M1 receptor expressed in CHO cells assessed as acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 445 5 2 7 2.7 Cc1ccc2c(n1)c(C(=O)N[C@H]1CCOC[C@@H]1O)cn2Cc1ccc(-c2ccn(C)n2)cc1 10.1016/j.bmcl.2015.11.053
46891076 6710 None 0 Human Functional pEC50 = 8.5 8.5 398 5
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 344 4 2 2 3.8 O=C(NCC1=CCNCC1)c1c(F)cccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.127
CHEMBL1083618 6710 None 0 Human Functional pEC50 = 8.5 8.5 398 5
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 344 4 2 2 3.8 O=C(NCC1=CCNCC1)c1c(F)cccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.127
42599068 16086 None 0 Human Functional pEC50 = 8.5 8.5 39 5
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 356 3 0 3 3.7 CO[C@H]1CC[C@](C)(N2CCC(N3C(=O)Cc4ccc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223805 16086 None 0 Human Functional pEC50 = 8.5 8.5 39 5
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 356 3 0 3 3.7 CO[C@H]1CC[C@](C)(N2CCC(N3C(=O)Cc4ccc(C)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
42598357 16112 None 0 Human Functional pEC50 = 8.5 8.5 125 5
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 383 4 0 6 3.8 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(C#N)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
CHEMBL1223863 16112 None 0 Human Functional pEC50 = 8.5 8.5 125 5
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on calcium mobilization by FLIPR assay
ChEMBL 383 4 0 6 3.8 CCO[C@H]1CC[C@](C)(N2CCC(n3c(=O)oc4ccc(C#N)cc43)CC2)CC1 10.1016/j.bmcl.2010.07.097
156246105 195266 None 3 Human Functional pEC50 = 8.5 8.5 -1 4
Activation of human muscarinic M1 receptor expressed in HEK293 cells incubated for 3 mins by Calcium flux assayActivation of human muscarinic M1 receptor expressed in HEK293 cells incubated for 3 mins by Calcium flux assay
ChEMBL 402 4 0 4 3.0 COc1ccc(F)cc1C1CCN([C@@H]2CCC3(C2)CN(C(=O)C2COC2)C3)CC1 10.1021/acsmedchemlett.3c00331
CHEMBL5399732 195266 None 3 Human Functional pEC50 = 8.5 8.5 -1 4
Activation of human muscarinic M1 receptor expressed in HEK293 cells incubated for 3 mins by Calcium flux assayActivation of human muscarinic M1 receptor expressed in HEK293 cells incubated for 3 mins by Calcium flux assay
ChEMBL 402 4 0 4 3.0 COc1ccc(F)cc1C1CCN([C@@H]2CCC3(C2)CN(C(=O)C2COC2)C3)CC1 10.1021/acsmedchemlett.3c00331
156246205 195343 None 2 Human Functional pEC50 = 7.5 7.5 -4 3
Activation of human muscarinic M1 receptor expressed in HEK293 cells incubated for 3 mins by Calcium flux assayActivation of human muscarinic M1 receptor expressed in HEK293 cells incubated for 3 mins by Calcium flux assay
ChEMBL 384 4 0 4 2.9 COc1ccccc1C1CCN(C2CCC3(C2)CN(C(=O)C2COC2)C3)CC1 10.1021/acsmedchemlett.3c00331
CHEMBL5401679 195343 None 2 Human Functional pEC50 = 7.5 7.5 -4 3
Activation of human muscarinic M1 receptor expressed in HEK293 cells incubated for 3 mins by Calcium flux assayActivation of human muscarinic M1 receptor expressed in HEK293 cells incubated for 3 mins by Calcium flux assay
ChEMBL 384 4 0 4 2.9 COc1ccccc1C1CCN(C2CCC3(C2)CN(C(=O)C2COC2)C3)CC1 10.1021/acsmedchemlett.3c00331
117937652 123039 None 0 Human Functional pEC50 = 7.5 7.5 1 2
Positive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as basal and acetylcholine-stimulated Ca2+ level by FLIPR assayPositive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as basal and acetylcholine-stimulated Ca2+ level by FLIPR assay
ChEMBL 449 5 2 7 2.5 Cn1cc(-c2ccc(Cn3cc(C(=O)N[C@H]4COCC[C@@H]4O)c4ncccc43)c(F)c2)cn1 10.1021/acsmedchemlett.5b00185
CHEMBL3608417 123039 None 0 Human Functional pEC50 = 7.5 7.5 1 2
Positive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as basal and acetylcholine-stimulated Ca2+ level by FLIPR assayPositive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as basal and acetylcholine-stimulated Ca2+ level by FLIPR assay
ChEMBL 449 5 2 7 2.5 Cn1cc(-c2ccc(Cn3cc(C(=O)N[C@H]4COCC[C@@H]4O)c4ncccc43)c(F)c2)cn1 10.1021/acsmedchemlett.5b00185
62705505 76394 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
ChEMBL 422 5 1 4 3.5 O=C1CCc2cccc(F)c2N1CCCN1CCC(n2c(=O)[nH]c3ccccc32)CC1 10.1016/j.bmcl.2012.05.048
CHEMBL2059320 76394 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
ChEMBL 422 5 1 4 3.5 O=C1CCc2cccc(F)c2N1CCCN1CCC(n2c(=O)[nH]c3ccccc32)CC1 10.1016/j.bmcl.2012.05.048
118732899 120936 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Partial agonist activity at human muscarinic M1 acetylcholine receptor expressed in CHO cells assessed as increase in IP1 accumulation incubated for 30 mins by FRET based HTRF assayPartial agonist activity at human muscarinic M1 acetylcholine receptor expressed in CHO cells assessed as increase in IP1 accumulation incubated for 30 mins by FRET based HTRF assay
ChEMBL 595 12 1 6 5.0 C[N+](C)(CC#CCOC1=NOCC1)CCCCCCNC(=O)c1cn(Cc2ccccc2)c2cc(Cl)c(F)cc2c1=O 10.1021/jm500860w
CHEMBL3414843 120936 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Partial agonist activity at human muscarinic M1 acetylcholine receptor expressed in CHO cells assessed as increase in IP1 accumulation incubated for 30 mins by FRET based HTRF assayPartial agonist activity at human muscarinic M1 acetylcholine receptor expressed in CHO cells assessed as increase in IP1 accumulation incubated for 30 mins by FRET based HTRF assay
ChEMBL 595 12 1 6 5.0 C[N+](C)(CC#CCOC1=NOCC1)CCCCCCNC(=O)c1cn(Cc2ccccc2)c2cc(Cl)c(F)cc2c1=O 10.1021/jm500860w
CHEMBL3559130 120936 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Partial agonist activity at human muscarinic M1 acetylcholine receptor expressed in CHO cells assessed as increase in IP1 accumulation incubated for 30 mins by FRET based HTRF assayPartial agonist activity at human muscarinic M1 acetylcholine receptor expressed in CHO cells assessed as increase in IP1 accumulation incubated for 30 mins by FRET based HTRF assay
ChEMBL 595 12 1 6 5.0 C[N+](C)(CC#CCOC1=NOCC1)CCCCCCNC(=O)c1cn(Cc2ccccc2)c2cc(Cl)c(F)cc2c1=O 10.1021/jm500860w
54585946 61812 None 0 Rat Functional pEC50 = 5.5 5.5 - 1
Allosteric modulation at rat M1 receptor expressed in CHO cells by calcium mobilization assayAllosteric modulation at rat M1 receptor expressed in CHO cells by calcium mobilization assay
ChEMBL 493 7 2 7 3.9 Cc1cc(NC(=O)CS(=O)(=O)c2cn(Cc3cc(-c4cn[nH]c4)ccc3F)c3ccccc23)no1 10.1016/j.bmcl.2010.12.015
CHEMBL1773115 61812 None 0 Rat Functional pEC50 = 5.5 5.5 - 1
Allosteric modulation at rat M1 receptor expressed in CHO cells by calcium mobilization assayAllosteric modulation at rat M1 receptor expressed in CHO cells by calcium mobilization assay
ChEMBL 493 7 2 7 3.9 Cc1cc(NC(=O)CS(=O)(=O)c2cn(Cc3cc(-c4cn[nH]c4)ccc3F)c3ccccc23)no1 10.1016/j.bmcl.2010.12.015
145960540 161734 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 450 5 2 6 3.2 O=C(N[C@H]1CCCC[C@@H]1O)C1CN(Cc2ccc(-n3cccn3)cc2)c2cc(F)ccc2O1 10.1016/j.bmcl.2018.05.009
CHEMBL4130089 161734 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 450 5 2 6 3.2 O=C(N[C@H]1CCCC[C@@H]1O)C1CN(Cc2ccc(-n3cccn3)cc2)c2cc(F)ccc2O1 10.1016/j.bmcl.2018.05.009
145962519 161463 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 450 5 2 6 3.2 O=C(N[C@H]1CCCC[C@@H]1O)C1CN(Cc2ccc(-n3cccn3)cc2)c2c(F)cccc2O1 10.1016/j.bmcl.2018.05.009
CHEMBL4126120 161463 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 450 5 2 6 3.2 O=C(N[C@H]1CCCC[C@@H]1O)C1CN(Cc2ccc(-n3cccn3)cc2)c2c(F)cccc2O1 10.1016/j.bmcl.2018.05.009
156246208 197020 None 3 Human Functional pEC50 = 7.5 7.5 -3 2
Activation of human muscarinic M1 receptor expressed in HEK293 cells incubated for 3 mins by Calcium flux assayActivation of human muscarinic M1 receptor expressed in HEK293 cells incubated for 3 mins by Calcium flux assay
ChEMBL 402 4 0 4 3.0 COc1cc(F)ccc1C1CCN([C@@H]2CCC3(C2)CN(C(=O)C2COC2)C3)CC1 10.1021/acsmedchemlett.3c00331
CHEMBL5436967 197020 None 3 Human Functional pEC50 = 7.5 7.5 -3 2
Activation of human muscarinic M1 receptor expressed in HEK293 cells incubated for 3 mins by Calcium flux assayActivation of human muscarinic M1 receptor expressed in HEK293 cells incubated for 3 mins by Calcium flux assay
ChEMBL 402 4 0 4 3.0 COc1cc(F)ccc1C1CCN([C@@H]2CCC3(C2)CN(C(=O)C2COC2)C3)CC1 10.1021/acsmedchemlett.3c00331
10444753 117913 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assayAgonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assay
ChEMBL 249 2 0 4 1.0 CN1CCC=C(C2=NOC(N3CCCC3=O)C2)C1 10.1016/j.bmcl.2015.02.012
CHEMBL3402921 117913 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assayAgonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assay
ChEMBL 249 2 0 4 1.0 CN1CCC=C(C2=NOC(N3CCCC3=O)C2)C1 10.1016/j.bmcl.2015.02.012
122191008 123684 None 0 Human Functional pEC50 = 7.5 7.5 2 3
Agonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 465 5 2 3 5.0 C/C(=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(Cl)cc1)[C@H](O)C2)N(C)Cc1ccc(F)cc1 10.1016/j.bmcl.2015.08.011
CHEMBL3618450 123684 None 0 Human Functional pEC50 = 7.5 7.5 2 3
Agonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 465 5 2 3 5.0 C/C(=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(Cl)cc1)[C@H](O)C2)N(C)Cc1ccc(F)cc1 10.1016/j.bmcl.2015.08.011
46891022 6664 None 0 Human Functional pEC50 = 7.5 7.5 39 2
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 380 4 2 2 4.5 O=C(NCC1CCNCC1)c1c(F)cccc1-c1cc(Cl)ccc1Cl 10.1016/j.bmcl.2010.04.127
CHEMBL1083404 6664 None 0 Human Functional pEC50 = 7.5 7.5 39 2
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 380 4 2 2 4.5 O=C(NCC1CCNCC1)c1c(F)cccc1-c1cc(Cl)ccc1Cl 10.1016/j.bmcl.2010.04.127
24751745 202311 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Allosteric modulation of human muscarinic M1 acetylcholine receptor expressed CHO cells assessed as intracellular calcium mobilization after 1 hr by Fluo-4-AM based fluorescence assayAllosteric modulation of human muscarinic M1 acetylcholine receptor expressed CHO cells assessed as intracellular calcium mobilization after 1 hr by Fluo-4-AM based fluorescence assay
ChEMBL 345 4 1 4 3.0 COc1ccc(Cn2cc(C(=O)O)c(=O)c3c(F)ccc(F)c32)cc1 10.1021/jm400540b
CHEMBL594432 202311 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Allosteric modulation of human muscarinic M1 acetylcholine receptor expressed CHO cells assessed as intracellular calcium mobilization after 1 hr by Fluo-4-AM based fluorescence assayAllosteric modulation of human muscarinic M1 acetylcholine receptor expressed CHO cells assessed as intracellular calcium mobilization after 1 hr by Fluo-4-AM based fluorescence assay
ChEMBL 345 4 1 4 3.0 COc1ccc(Cn2cc(C(=O)O)c(=O)c3c(F)ccc(F)c32)cc1 10.1021/jm400540b
44207445 16762 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 361 6 1 3 2.5 CCC(=O)NC1CCN(CCCN2C(=O)CCc3cccc(F)c32)CC1 10.1021/jm100697g
CHEMBL1243386 16762 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 361 6 1 3 2.5 CCC(=O)NC1CCN(CCCN2C(=O)CCc3cccc(F)c32)CC1 10.1021/jm100697g
149505732 186337 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at muscarinic M1 receptor (unknown origin) expressed in CHO cellsAgonist activity at muscarinic M1 receptor (unknown origin) expressed in CHO cells
ChEMBL 321 1 1 3 4.6 Cc1ccc2c(c1)N=C(C1=CCN(C)CC1)c1cc(F)ccc1N2 10.1016/j.bmcl.2021.127911
CHEMBL4873426 186337 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at muscarinic M1 receptor (unknown origin) expressed in CHO cellsAgonist activity at muscarinic M1 receptor (unknown origin) expressed in CHO cells
ChEMBL 321 1 1 3 4.6 Cc1ccc2c(c1)N=C(C1=CCN(C)CC1)c1cc(F)ccc1N2 10.1016/j.bmcl.2021.127911
57394608 68281 None 0 Rat Functional pEC50 = 6.5 6.5 - 1
Agonist activity at rat muscarinic M1 receptor expressed in CHO cellsAgonist activity at rat muscarinic M1 receptor expressed in CHO cells
ChEMBL 395 4 1 4 2.8 CCOC(=O)N1CCC(N2CCC[C@@H](NC(=O)c3ccc(F)c(F)c3)C2)CC1 10.1016/j.bmcl.2011.08.084
CHEMBL1916229 68281 None 0 Rat Functional pEC50 = 6.5 6.5 - 1
Agonist activity at rat muscarinic M1 receptor expressed in CHO cellsAgonist activity at rat muscarinic M1 receptor expressed in CHO cells
ChEMBL 395 4 1 4 2.8 CCOC(=O)N1CCC(N2CCC[C@@H](NC(=O)c3ccc(F)c(F)c3)C2)CC1 10.1016/j.bmcl.2011.08.084
139414132 164670 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assayPositive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 368 2 1 2 5.3 FC(F)(F)C[C@@H]1N=C(c2ccccc2)c2cc(Cl)ccc2NC1=S 10.1016/j.bmcl.2017.11.008
CHEMBL4215404 164670 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assayPositive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 368 2 1 2 5.3 FC(F)(F)C[C@@H]1N=C(c2ccccc2)c2cc(Cl)ccc2NC1=S 10.1016/j.bmcl.2017.11.008
3652 4097 None 50 Human Functional pEC50 = 6.5 6.5 -18 15
Agonist activity at human M1 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M1 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
57 4097 None 50 Human Functional pEC50 = 6.5 6.5 -18 15
Agonist activity at human M1 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M1 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
60809 4097 None 50 Human Functional pEC50 = 6.5 6.5 -18 15
Agonist activity at human M1 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M1 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
60809.0 4097 None 50 Human Functional pEC50 = 6.5 6.5 -18 15
Agonist activity at human M1 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M1 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
CHEMBL21536 4097 None 50 Human Functional pEC50 = 6.5 6.5 -18 15
Agonist activity at human M1 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M1 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
DB15357 4097 None 50 Human Functional pEC50 = 6.5 6.5 -18 15
Agonist activity at human M1 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M1 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1021/jm0606995
16094810 137973 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at human M1 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M1 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 467 16 0 12 3.1 COc1nsnc1OCCCOCCCOCCCOc1nsnc1-c1cccnc1 10.1021/jm0606995
CHEMBL376295 137973 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at human M1 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysisAgonist activity at human M1 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis
ChEMBL 467 16 0 12 3.1 COc1nsnc1OCCCOCCCOCCCOc1nsnc1-c1cccnc1 10.1021/jm0606995
46890846 7361 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 342 5 2 2 4.1 O=C(NCCC1CCNCC1)c1ccccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.127
CHEMBL1086298 7361 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 342 5 2 2 4.1 O=C(NCCC1CCNCC1)c1ccccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.127
20449980 164165 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assayPositive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 303 1 1 1 5.1 Fc1ccccc1C1=CCC(=S)Nc2ccc(Cl)cc21 10.1016/j.bmcl.2017.11.008
CHEMBL4209299 164165 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assayPositive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 303 1 1 1 5.1 Fc1ccccc1C1=CCC(=S)Nc2ccc(Cl)cc21 10.1016/j.bmcl.2017.11.008
139414027 164311 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assayPositive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 342 3 1 2 5.3 CC(C)C[C@@H]1N=C(c2ccccc2)c2cc(Cl)ccc2NC1=S 10.1016/j.bmcl.2017.11.008
CHEMBL4210984 164311 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assayPositive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 342 3 1 2 5.3 CC(C)C[C@@H]1N=C(c2ccccc2)c2cc(Cl)ccc2NC1=S 10.1016/j.bmcl.2017.11.008
3081966 164940 None 15 Human Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assayPositive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 304 1 1 2 4.1 Fc1ccccc1C1=NCC(=S)Nc2ccc(Cl)cc21 10.1016/j.bmcl.2017.11.008
CHEMBL4218941 164940 None 15 Human Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assayPositive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 304 1 1 2 4.1 Fc1ccccc1C1=NCC(=S)Nc2ccc(Cl)cc21 10.1016/j.bmcl.2017.11.008
145962519 161463 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 450 5 2 6 3.2 O=C(N[C@H]1CCCC[C@@H]1O)C1CN(Cc2ccc(-n3cccn3)cc2)c2c(F)cccc2O1 10.1016/j.bmcl.2018.05.009
CHEMBL4126120 161463 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 450 5 2 6 3.2 O=C(N[C@H]1CCCC[C@@H]1O)C1CN(Cc2ccc(-n3cccn3)cc2)c2c(F)cccc2O1 10.1016/j.bmcl.2018.05.009
71528459 194709 None 4 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human M1 receptorAgonist activity at human M1 receptor
ChEMBL 365 4 1 4 2.8 CCOC(=O)N1CCC[C@H](N2CCC(C(=O)NC3(C)CCC3)CC2)CC1 10.1021/acs.jmedchem.2c01827
CHEMBL5314959 194709 None 4 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human M1 receptorAgonist activity at human M1 receptor
ChEMBL 365 4 1 4 2.8 CCOC(=O)N1CCC[C@H](N2CCC(C(=O)NC3(C)CCC3)CC2)CC1 10.1021/acs.jmedchem.2c01827
118732893 120930 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Partial agonist activity at human muscarinic M1 acetylcholine receptor expressed in CHO cells assessed as increase in IP1 accumulation incubated for 30 mins by FRET based HTRF assayPartial agonist activity at human muscarinic M1 acetylcholine receptor expressed in CHO cells assessed as increase in IP1 accumulation incubated for 30 mins by FRET based HTRF assay
ChEMBL 567 10 1 6 4.2 C[N+](C)(CC#CCOC1=NOCC1)CCCCNC(=O)c1cn(Cc2ccccc2)c2cc(Cl)c(F)cc2c1=O 10.1021/jm500860w
CHEMBL3414840 120930 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Partial agonist activity at human muscarinic M1 acetylcholine receptor expressed in CHO cells assessed as increase in IP1 accumulation incubated for 30 mins by FRET based HTRF assayPartial agonist activity at human muscarinic M1 acetylcholine receptor expressed in CHO cells assessed as increase in IP1 accumulation incubated for 30 mins by FRET based HTRF assay
ChEMBL 567 10 1 6 4.2 C[N+](C)(CC#CCOC1=NOCC1)CCCCNC(=O)c1cn(Cc2ccccc2)c2cc(Cl)c(F)cc2c1=O 10.1021/jm500860w
CHEMBL3559070 120930 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Partial agonist activity at human muscarinic M1 acetylcholine receptor expressed in CHO cells assessed as increase in IP1 accumulation incubated for 30 mins by FRET based HTRF assayPartial agonist activity at human muscarinic M1 acetylcholine receptor expressed in CHO cells assessed as increase in IP1 accumulation incubated for 30 mins by FRET based HTRF assay
ChEMBL 567 10 1 6 4.2 C[N+](C)(CC#CCOC1=NOCC1)CCCCNC(=O)c1cn(Cc2ccccc2)c2cc(Cl)c(F)cc2c1=O 10.1021/jm500860w
53385877 74364 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
ChEMBL 371 4 1 4 2.6 CCOC(=O)N1C2CCC1CC(N1CC[C@@H](NC(=O)c3ccccc3)C1)C2 10.1016/j.bmcl.2012.03.088
CHEMBL2024405 74364 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
ChEMBL 371 4 1 4 2.6 CCOC(=O)N1C2CCC1CC(N1CC[C@@H](NC(=O)c3ccccc3)C1)C2 10.1016/j.bmcl.2012.03.088
137701968 165492 None 11 Human Functional pEC50 = 6.5 6.5 -1 2
Positive allosteric modulation of human M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assayPositive allosteric modulation of human M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assay
ChEMBL 430 5 1 7 2.9 Cn1cc(-c2ccc(Cc3cc(C(=O)NC4CCOCC4)nc4c3ccn4C)cn2)cn1 10.1021/acsmedchemlett.8b00261
CHEMBL4238059 165492 None 11 Human Functional pEC50 = 6.5 6.5 -1 2
Positive allosteric modulation of human M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assayPositive allosteric modulation of human M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assay
ChEMBL 430 5 1 7 2.9 Cn1cc(-c2ccc(Cc3cc(C(=O)NC4CCOCC4)nc4c3ccn4C)cn2)cn1 10.1021/acsmedchemlett.8b00261
145960540 161734 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 450 5 2 6 3.2 O=C(N[C@H]1CCCC[C@@H]1O)C1CN(Cc2ccc(-n3cccn3)cc2)c2cc(F)ccc2O1 10.1016/j.bmcl.2018.05.009
CHEMBL4130089 161734 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 450 5 2 6 3.2 O=C(N[C@H]1CCCC[C@@H]1O)C1CN(Cc2ccc(-n3cccn3)cc2)c2cc(F)ccc2O1 10.1016/j.bmcl.2018.05.009
44158142 188777 None 42 Rat Functional pEC50 = 5.5 5.5 -1 4
Activation of rat muscarinic M1 receptor expressed in CHO cells co-expressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of rat muscarinic M1 receptor expressed in CHO cells co-expressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 339 2 0 2 4.1 O=C1C(=O)N(Cc2ccc(C(F)(F)F)cc2)c2c(Cl)cccc21 10.1021/jm900286j
CHEMBL503735 188777 None 42 Rat Functional pEC50 = 5.5 5.5 -1 4
Activation of rat muscarinic M1 receptor expressed in CHO cells co-expressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of rat muscarinic M1 receptor expressed in CHO cells co-expressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 339 2 0 2 4.1 O=C1C(=O)N(Cc2ccc(C(F)(F)F)cc2)c2c(Cl)cccc21 10.1021/jm900286j
CHEMBL4571199 216488 None 5 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at human M1 receptorAgonist activity at human M1 receptor
ChEMBL None None None CCOC(=O)N1CCC(N2CCC(C(N)=O)CC2)CC1 10.1021/acs.jmedchem.2c01827
70683564 74336 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
ChEMBL 359 5 1 4 2.4 CCOC(=O)N1CC[C@H]2[C@@H](CCCN2CCNC(=O)c2ccccc2)C1 10.1016/j.bmcl.2012.03.088
CHEMBL2024327 74336 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
ChEMBL 359 5 1 4 2.4 CCOC(=O)N1CC[C@H]2[C@@H](CCCN2CCNC(=O)c2ccccc2)C1 10.1016/j.bmcl.2012.03.088
44158142 188777 None 42 Rat Functional pEC50 = 5.5 5.5 -1 4
Agonist activity at rat muscarinic M1 expressed in CHO cells assessed as stimulation of calcium mobilizationAgonist activity at rat muscarinic M1 expressed in CHO cells assessed as stimulation of calcium mobilization
ChEMBL 339 2 0 2 4.1 O=C1C(=O)N(Cc2ccc(C(F)(F)F)cc2)c2c(Cl)cccc21 10.1016/j.bmcl.2009.11.089
CHEMBL503735 188777 None 42 Rat Functional pEC50 = 5.5 5.5 -1 4
Agonist activity at rat muscarinic M1 expressed in CHO cells assessed as stimulation of calcium mobilizationAgonist activity at rat muscarinic M1 expressed in CHO cells assessed as stimulation of calcium mobilization
ChEMBL 339 2 0 2 4.1 O=C1C(=O)N(Cc2ccc(C(F)(F)F)cc2)c2c(Cl)cccc21 10.1016/j.bmcl.2009.11.089
71555066 141051 None 19 Rat Functional pEC50 = 5.5 5.5 -1 2
Positive allosteric modulation at rat muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation at rat muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 322 3 0 4 2.8 Cn1cc(-c2ccc(CN3Cc4ncccc4C3=O)c(F)c2)cn1 10.1016/j.bmcl.2016.04.083
CHEMBL3823130 141051 None 19 Rat Functional pEC50 = 5.5 5.5 -1 2
Positive allosteric modulation at rat muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation at rat muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 322 3 0 4 2.8 Cn1cc(-c2ccc(CN3Cc4ncccc4C3=O)c(F)c2)cn1 10.1016/j.bmcl.2016.04.083
71540493 86388 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Positive allosteric modulator activity at human muscarinic M1 receptor by calcium mobilization assayPositive allosteric modulator activity at human muscarinic M1 receptor by calcium mobilization assay
ChEMBL 353 3 0 4 3.9 Cn1cc(-c2ccc(CN3C(=O)CSc4ccccc43)c(F)c2)cn1 10.1016/j.bmcl.2012.11.092
CHEMBL2313515 86388 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Positive allosteric modulator activity at human muscarinic M1 receptor by calcium mobilization assayPositive allosteric modulator activity at human muscarinic M1 receptor by calcium mobilization assay
ChEMBL 353 3 0 4 3.9 Cn1cc(-c2ccc(CN3C(=O)CSc4ccccc43)c(F)c2)cn1 10.1016/j.bmcl.2012.11.092
54585945 61805 None 0 Rat Functional pEC50 = 5.5 5.5 - 1
Allosteric modulation at rat M1 receptor expressed in CHO cells by calcium mobilization assayAllosteric modulation at rat M1 receptor expressed in CHO cells by calcium mobilization assay
ChEMBL 489 7 1 8 3.8 Cc1cc(NC(=O)CS(=O)(=O)c2cn(Cc3cccc(-c4cnn(C)c4)c3)c3ccccc23)no1 10.1016/j.bmcl.2010.12.015
CHEMBL1773099 61805 None 0 Rat Functional pEC50 = 5.5 5.5 - 1
Allosteric modulation at rat M1 receptor expressed in CHO cells by calcium mobilization assayAllosteric modulation at rat M1 receptor expressed in CHO cells by calcium mobilization assay
ChEMBL 489 7 1 8 3.8 Cc1cc(NC(=O)CS(=O)(=O)c2cn(Cc3cccc(-c4cnn(C)c4)c3)c3ccccc23)no1 10.1016/j.bmcl.2010.12.015
146216756 186395 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL 427 5 0 6 3.2 Cc1nn(C)cc1-c1cc(F)c(CN2Cc3cnn(CC4CCCO4)c3C2=O)c(F)c1 10.1016/j.bmcl.2021.128193
CHEMBL4874253 186395 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL 427 5 0 6 3.2 Cc1nn(C)cc1-c1cc(F)c(CN2Cc3cnn(CC4CCCO4)c3C2=O)c(F)c1 10.1016/j.bmcl.2021.128193
137701968 165492 None 11 Human Functional pEC50 = 6.5 6.5 -1 2
Agonist activity at human M1 receptor expressed in CHO cells assessed as increase in calcium mobilization measured after 2.5 mins by Fluo-4-AM dye based assayAgonist activity at human M1 receptor expressed in CHO cells assessed as increase in calcium mobilization measured after 2.5 mins by Fluo-4-AM dye based assay
ChEMBL 430 5 1 7 2.9 Cn1cc(-c2ccc(Cc3cc(C(=O)NC4CCOCC4)nc4c3ccn4C)cn2)cn1 10.1021/acsmedchemlett.8b00261
CHEMBL4238059 165492 None 11 Human Functional pEC50 = 6.5 6.5 -1 2
Agonist activity at human M1 receptor expressed in CHO cells assessed as increase in calcium mobilization measured after 2.5 mins by Fluo-4-AM dye based assayAgonist activity at human M1 receptor expressed in CHO cells assessed as increase in calcium mobilization measured after 2.5 mins by Fluo-4-AM dye based assay
ChEMBL 430 5 1 7 2.9 Cn1cc(-c2ccc(Cc3cc(C(=O)NC4CCOCC4)nc4c3ccn4C)cn2)cn1 10.1021/acsmedchemlett.8b00261
145985065 165825 None 0 Rat Functional pEC50 = 5.5 5.5 -2 2
Agonist activity at rat M1 receptor expressed in CHO cells assessed as increase in calcium mobilization measured after 2.5 mins by Fluo-4-AM dye based assayAgonist activity at rat M1 receptor expressed in CHO cells assessed as increase in calcium mobilization measured after 2.5 mins by Fluo-4-AM dye based assay
ChEMBL 443 5 2 6 3.6 Cn1ccc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCCC[C@H]4O)nc4c3ccn4C)cc2)n1 10.1021/acsmedchemlett.8b00261
CHEMBL4246159 165825 None 0 Rat Functional pEC50 = 5.5 5.5 -2 2
Agonist activity at rat M1 receptor expressed in CHO cells assessed as increase in calcium mobilization measured after 2.5 mins by Fluo-4-AM dye based assayAgonist activity at rat M1 receptor expressed in CHO cells assessed as increase in calcium mobilization measured after 2.5 mins by Fluo-4-AM dye based assay
ChEMBL 443 5 2 6 3.6 Cn1ccc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCCC[C@H]4O)nc4c3ccn4C)cc2)n1 10.1021/acsmedchemlett.8b00261
71540493 86388 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Positive allosteric modulator activity at human muscarinic M1 receptor by calcium mobilization assayPositive allosteric modulator activity at human muscarinic M1 receptor by calcium mobilization assay
ChEMBL 353 3 0 4 3.9 Cn1cc(-c2ccc(CN3C(=O)CSc4ccccc43)c(F)c2)cn1 10.1016/j.bmcl.2012.11.092
CHEMBL2313515 86388 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Positive allosteric modulator activity at human muscarinic M1 receptor by calcium mobilization assayPositive allosteric modulator activity at human muscarinic M1 receptor by calcium mobilization assay
ChEMBL 353 3 0 4 3.9 Cn1cc(-c2ccc(CN3C(=O)CSc4ccccc43)c(F)c2)cn1 10.1016/j.bmcl.2012.11.092
145985065 165825 None 0 Rat Functional pEC50 = 5.5 5.5 -2 2
Agonist activity at rat M1 receptor expressed in CHO cells assessed as increase in calcium mobilization measured after 2.5 mins by Fluo-4-AM dye based assayAgonist activity at rat M1 receptor expressed in CHO cells assessed as increase in calcium mobilization measured after 2.5 mins by Fluo-4-AM dye based assay
ChEMBL 443 5 2 6 3.6 Cn1ccc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCCC[C@H]4O)nc4c3ccn4C)cc2)n1 10.1021/acsmedchemlett.8b00261
CHEMBL4246159 165825 None 0 Rat Functional pEC50 = 5.5 5.5 -2 2
Agonist activity at rat M1 receptor expressed in CHO cells assessed as increase in calcium mobilization measured after 2.5 mins by Fluo-4-AM dye based assayAgonist activity at rat M1 receptor expressed in CHO cells assessed as increase in calcium mobilization measured after 2.5 mins by Fluo-4-AM dye based assay
ChEMBL 443 5 2 6 3.6 Cn1ccc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCCC[C@H]4O)nc4c3ccn4C)cc2)n1 10.1021/acsmedchemlett.8b00261
44589595 185426 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
ChEMBL 458 4 1 5 3.0 O=c1[nH]c2ccc(F)cc2n1C1CCN(C2CCN(S(=O)(=O)c3ccccc3)CC2)CC1 10.1016/j.bmcl.2008.09.032
CHEMBL485953 185426 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
ChEMBL 458 4 1 5 3.0 O=c1[nH]c2ccc(F)cc2n1C1CCN(C2CCN(S(=O)(=O)c3ccccc3)CC2)CC1 10.1016/j.bmcl.2008.09.032
10220392 208463 None 0 Human Functional pEC50 = 5.5 5.5 6 2
Effective concentration for HMPA (human muscarinic inositol phosphate accumulation) activity measured in CHO cells expressing Muscarinic acetylcholine receptor M1Effective concentration for HMPA (human muscarinic inositol phosphate accumulation) activity measured in CHO cells expressing Muscarinic acetylcholine receptor M1
ChEMBL 240 2 0 3 1.7 C(#Cc1ccccc1)CO/N=C1\CN2CCC1C2 10.1016/S0960-894X(00)80538-7
CHEMBL84893 208463 None 0 Human Functional pEC50 = 5.5 5.5 6 2
Effective concentration for HMPA (human muscarinic inositol phosphate accumulation) activity measured in CHO cells expressing Muscarinic acetylcholine receptor M1Effective concentration for HMPA (human muscarinic inositol phosphate accumulation) activity measured in CHO cells expressing Muscarinic acetylcholine receptor M1
ChEMBL 240 2 0 3 1.7 C(#Cc1ccccc1)CO/N=C1\CN2CCC1C2 10.1016/S0960-894X(00)80538-7
71540148 86382 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Positive allosteric modulator activity at human muscarinic M1 receptor by calcium mobilization assayPositive allosteric modulator activity at human muscarinic M1 receptor by calcium mobilization assay
ChEMBL 405 3 1 4 3.5 Cn1cc(-c2ccc(CN3C(=O)C(O)(C(F)(F)F)c4ccccc43)c(F)c2)cn1 10.1016/j.bmcl.2012.11.092
CHEMBL2313498 86382 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Positive allosteric modulator activity at human muscarinic M1 receptor by calcium mobilization assayPositive allosteric modulator activity at human muscarinic M1 receptor by calcium mobilization assay
ChEMBL 405 3 1 4 3.5 Cn1cc(-c2ccc(CN3C(=O)C(O)(C(F)(F)F)c4ccccc43)c(F)c2)cn1 10.1016/j.bmcl.2012.11.092
71540267 86383 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Positive allosteric modulator activity at human muscarinic M1 receptor by calcium mobilization assayPositive allosteric modulator activity at human muscarinic M1 receptor by calcium mobilization assay
ChEMBL 419 4 1 4 4.0 CCn1cc(-c2ccc(CN3C(=O)C(O)(C(F)(F)F)c4ccccc43)c(F)c2)cn1 10.1016/j.bmcl.2012.11.092
CHEMBL2313499 86383 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Positive allosteric modulator activity at human muscarinic M1 receptor by calcium mobilization assayPositive allosteric modulator activity at human muscarinic M1 receptor by calcium mobilization assay
ChEMBL 419 4 1 4 4.0 CCn1cc(-c2ccc(CN3C(=O)C(O)(C(F)(F)F)c4ccccc43)c(F)c2)cn1 10.1016/j.bmcl.2012.11.092
71540148 86382 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Positive allosteric modulator activity at human muscarinic M1 receptor by calcium mobilization assayPositive allosteric modulator activity at human muscarinic M1 receptor by calcium mobilization assay
ChEMBL 405 3 1 4 3.5 Cn1cc(-c2ccc(CN3C(=O)C(O)(C(F)(F)F)c4ccccc43)c(F)c2)cn1 10.1016/j.bmcl.2012.11.092
CHEMBL2313498 86382 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Positive allosteric modulator activity at human muscarinic M1 receptor by calcium mobilization assayPositive allosteric modulator activity at human muscarinic M1 receptor by calcium mobilization assay
ChEMBL 405 3 1 4 3.5 Cn1cc(-c2ccc(CN3C(=O)C(O)(C(F)(F)F)c4ccccc43)c(F)c2)cn1 10.1016/j.bmcl.2012.11.092
71540267 86383 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Positive allosteric modulator activity at human muscarinic M1 receptor by calcium mobilization assayPositive allosteric modulator activity at human muscarinic M1 receptor by calcium mobilization assay
ChEMBL 419 4 1 4 4.0 CCn1cc(-c2ccc(CN3C(=O)C(O)(C(F)(F)F)c4ccccc43)c(F)c2)cn1 10.1016/j.bmcl.2012.11.092
CHEMBL2313499 86383 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Positive allosteric modulator activity at human muscarinic M1 receptor by calcium mobilization assayPositive allosteric modulator activity at human muscarinic M1 receptor by calcium mobilization assay
ChEMBL 419 4 1 4 4.0 CCn1cc(-c2ccc(CN3C(=O)C(O)(C(F)(F)F)c4ccccc43)c(F)c2)cn1 10.1016/j.bmcl.2012.11.092
10027177 182583 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
ChEMBL 458 4 1 4 4.7 O=c1[nH]c2ccccc2n1C1CCN(C2CCN(Cc3ccccc3C(F)(F)F)CC2)CC1 10.1016/j.bmcl.2008.09.032
CHEMBL478662 182583 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
ChEMBL 458 4 1 4 4.7 O=c1[nH]c2ccccc2n1C1CCN(C2CCN(Cc3ccccc3C(F)(F)F)CC2)CC1 10.1016/j.bmcl.2008.09.032
145968533 165063 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as increase in ACh-induced intracellular calcium level preincubated for 10 mins followed by ACh addition measured every 2 secs for 80 secs by Fluo-4 dye-based FLIPR assayPositive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as increase in ACh-induced intracellular calcium level preincubated for 10 mins followed by ACh addition measured every 2 secs for 80 secs by Fluo-4 dye-based FLIPR assay
ChEMBL 408 6 3 7 1.2 O=C(N[C@H]1CCOC[C@@H]1O)c1cc(Cc2ccc(-n3cccn3)cc2)c(CO)cn1 10.1016/j.bmcl.2018.04.054
CHEMBL4225344 165063 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as increase in ACh-induced intracellular calcium level preincubated for 10 mins followed by ACh addition measured every 2 secs for 80 secs by Fluo-4 dye-based FLIPR assayPositive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as increase in ACh-induced intracellular calcium level preincubated for 10 mins followed by ACh addition measured every 2 secs for 80 secs by Fluo-4 dye-based FLIPR assay
ChEMBL 408 6 3 7 1.2 O=C(N[C@H]1CCOC[C@@H]1O)c1cc(Cc2ccc(-n3cccn3)cc2)c(CO)cn1 10.1016/j.bmcl.2018.04.054
145968558 165108 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Positive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as increase in ACh-induced intracellular calcium level preincubated for 10 mins followed by ACh addition measured every 2 secs for 80 secs by Fluo-4 dye-based FLIPR assayPositive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as increase in ACh-induced intracellular calcium level preincubated for 10 mins followed by ACh addition measured every 2 secs for 80 secs by Fluo-4 dye-based FLIPR assay
ChEMBL 431 5 2 6 3.4 O=C(N[C@H]1CCCC[C@@H]1O)c1cn(Cc2ccc([N+]3([O-])C=CC=N3)cc2)c2cccnc12 10.1016/j.bmcl.2018.04.054
CHEMBL4225950 165108 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Positive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as increase in ACh-induced intracellular calcium level preincubated for 10 mins followed by ACh addition measured every 2 secs for 80 secs by Fluo-4 dye-based FLIPR assayPositive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as increase in ACh-induced intracellular calcium level preincubated for 10 mins followed by ACh addition measured every 2 secs for 80 secs by Fluo-4 dye-based FLIPR assay
ChEMBL 431 5 2 6 3.4 O=C(N[C@H]1CCCC[C@@H]1O)c1cn(Cc2ccc([N+]3([O-])C=CC=N3)cc2)c2cccnc12 10.1016/j.bmcl.2018.04.054
117937642 123035 None 0 Rat Functional pEC50 = 7.5 7.5 -3 2
Positive allosteric modulation of rat muscarinic M1 receptor expressed in CHO cells assessed as basal and acetylcholine-stimulated Ca2+ level by FLIPR assayPositive allosteric modulation of rat muscarinic M1 receptor expressed in CHO cells assessed as basal and acetylcholine-stimulated Ca2+ level by FLIPR assay
ChEMBL 447 5 2 6 3.7 Cn1cc(-c2ccc(Cn3cc(C(=O)N[C@H]4CCCC[C@@H]4O)c4ncccc43)c(F)c2)cn1 10.1021/acsmedchemlett.5b00185
CHEMBL3608413 123035 None 0 Rat Functional pEC50 = 7.5 7.5 -3 2
Positive allosteric modulation of rat muscarinic M1 receptor expressed in CHO cells assessed as basal and acetylcholine-stimulated Ca2+ level by FLIPR assayPositive allosteric modulation of rat muscarinic M1 receptor expressed in CHO cells assessed as basal and acetylcholine-stimulated Ca2+ level by FLIPR assay
ChEMBL 447 5 2 6 3.7 Cn1cc(-c2ccc(Cn3cc(C(=O)N[C@H]4CCCC[C@@H]4O)c4ncccc43)c(F)c2)cn1 10.1021/acsmedchemlett.5b00185
122186860 123042 None 0 Human Functional pEC50 = 7.5 7.5 2 2
Positive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as basal and acetylcholine-stimulated Ca2+ level by FLIPR assayPositive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as basal and acetylcholine-stimulated Ca2+ level by FLIPR assay
ChEMBL 432 5 2 8 1.8 Cn1cc(-c2ccc(Cn3cc(C(=O)N[C@H]4COCC[C@@H]4O)c4ncccc43)cn2)cn1 10.1021/acsmedchemlett.5b00185
CHEMBL3608420 123042 None 0 Human Functional pEC50 = 7.5 7.5 2 2
Positive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as basal and acetylcholine-stimulated Ca2+ level by FLIPR assayPositive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as basal and acetylcholine-stimulated Ca2+ level by FLIPR assay
ChEMBL 432 5 2 8 1.8 Cn1cc(-c2ccc(Cn3cc(C(=O)N[C@H]4COCC[C@@H]4O)c4ncccc43)cn2)cn1 10.1021/acsmedchemlett.5b00185
9937709 34106 None 0 Human Functional pEC50 = 6.5 6.5 -239 2
Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.
ChEMBL 560 17 0 10 6.2 CN1CCC=C(c2nsnc2OCCCCCCCCCCCCOc2nsnc2C2=CCCN(C)C2)C1 10.1021/jm0102405
CHEMBL142538 34106 None 0 Human Functional pEC50 = 6.5 6.5 -239 2
Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.
ChEMBL 560 17 0 10 6.2 CN1CCC=C(c2nsnc2OCCCCCCCCCCCCOc2nsnc2C2=CCCN(C)C2)C1 10.1021/jm0102405
162656728 180947 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulation of recombinant human muscarinic M1 receptor co-expressing pCRE-Luc reporter gene in CHO cells assessed as stimulation of luciferase activity in presence of acetylcholine substrate measured after 4 hrs by luciferase reporter gene assayPositive allosteric modulation of recombinant human muscarinic M1 receptor co-expressing pCRE-Luc reporter gene in CHO cells assessed as stimulation of luciferase activity in presence of acetylcholine substrate measured after 4 hrs by luciferase reporter gene assay
ChEMBL 415 6 1 6 3.2 Cn1cc(-c2ccc(Cc3cc(C(=O)NCC4CCCO4)nn4cccc34)cc2)cn1 10.1021/acsmedchemlett.1c00118
CHEMBL4757070 180947 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulation of recombinant human muscarinic M1 receptor co-expressing pCRE-Luc reporter gene in CHO cells assessed as stimulation of luciferase activity in presence of acetylcholine substrate measured after 4 hrs by luciferase reporter gene assayPositive allosteric modulation of recombinant human muscarinic M1 receptor co-expressing pCRE-Luc reporter gene in CHO cells assessed as stimulation of luciferase activity in presence of acetylcholine substrate measured after 4 hrs by luciferase reporter gene assay
ChEMBL 415 6 1 6 3.2 Cn1cc(-c2ccc(Cc3cc(C(=O)NCC4CCCO4)nn4cccc34)cc2)cn1 10.1021/acsmedchemlett.1c00118
44247544 49529 None 0 Rat Functional pEC50 = 5.5 5.5 - 1
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: PAM Calcium Assay Dose-Response with M1. Measurement of intracellular Ca2+ using Fluo-4 dye in CHO-K1 cells stably transfected with rat M1 (Class of assay: confirmatory) [Related pubchem assays: 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen [Primary Screening])]PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: PAM Calcium Assay Dose-Response with M1. Measurement of intracellular Ca2+ using Fluo-4 dye in CHO-K1 cells stably transfected with rat M1 (Class of assay: confirmatory) [Related pubchem assays: 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen [Primary Screening])]
ChEMBL 489 7 1 8 3.8 Cc1cc(NC(=O)CS(=O)(=O)c2cn(Cc3cccc(-c4ccn(C)n4)c3)c3ccccc23)no1 nan
CHEMBL1565295 49529 None 0 Rat Functional pEC50 = 5.5 5.5 - 1
PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: PAM Calcium Assay Dose-Response with M1. Measurement of intracellular Ca2+ using Fluo-4 dye in CHO-K1 cells stably transfected with rat M1 (Class of assay: confirmatory) [Related pubchem assays: 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen [Primary Screening])]PUBCHEM_BIOASSAY: Discovery of novel allosteric modulators of the M1 muscarinic receptor: PAM Calcium Assay Dose-Response with M1. Measurement of intracellular Ca2+ using Fluo-4 dye in CHO-K1 cells stably transfected with rat M1 (Class of assay: confirmatory) [Related pubchem assays: 626 (Discovery of Novel Allosteric Modulators of the M1 Muscarinic Receptor: Agonist Primary Screen [Primary Screening])]
ChEMBL 489 7 1 8 3.8 Cc1cc(NC(=O)CS(=O)(=O)c2cn(Cc3cccc(-c4ccn(C)n4)c3)c3ccccc23)no1 nan
145965599 164527 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assayPositive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 344 2 1 2 4.5 CC(C)C1C(=S)Nc2ccc(Cl)cc2C(c2ccccc2)=[N+]1[O-] 10.1016/j.bmcl.2017.11.008
CHEMBL4213699 164527 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assayPositive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 344 2 1 2 4.5 CC(C)C1C(=S)Nc2ccc(Cl)cc2C(c2ccccc2)=[N+]1[O-] 10.1016/j.bmcl.2017.11.008
53385783 74340 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human muscarinic M1 receptor by calcium mobilization assayAgonist activity at human muscarinic M1 receptor by calcium mobilization assay
ChEMBL 385 4 1 4 3.0 CCOC(=O)N1C2CCC1CC(N1CCC[C@@H](NC(=O)c3ccccc3)C1)C2 10.1016/j.bmcl.2012.03.088
CHEMBL2024332 74340 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human muscarinic M1 receptor by calcium mobilization assayAgonist activity at human muscarinic M1 receptor by calcium mobilization assay
ChEMBL 385 4 1 4 3.0 CCOC(=O)N1C2CCC1CC(N1CCC[C@@H](NC(=O)c3ccccc3)C1)C2 10.1016/j.bmcl.2012.03.088
46930253 16744 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 385 6 1 4 2.6 O=C(NC1CCN(CCCN2C(=O)COc3ccccc32)CC1)C1CCCC1 10.1021/jm100697g
CHEMBL1243296 16744 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 385 6 1 4 2.6 O=C(NC1CCN(CCCN2C(=O)COc3ccccc32)CC1)C1CCCC1 10.1021/jm100697g
147230103 180259 None 0 Human Functional pEC50 = 6.5 6.5 1 2
Agonist activity at muscarinic M1 receptor (unknown origin) expressed in CHO cellsAgonist activity at muscarinic M1 receptor (unknown origin) expressed in CHO cells
ChEMBL 323 1 1 3 4.8 CN1CC=C(C2=Nc3cc(Cl)ccc3Nc3ccccc32)CC1 10.1016/j.bmcl.2021.127911
CHEMBL4748915 180259 None 0 Human Functional pEC50 = 6.5 6.5 1 2
Agonist activity at muscarinic M1 receptor (unknown origin) expressed in CHO cellsAgonist activity at muscarinic M1 receptor (unknown origin) expressed in CHO cells
ChEMBL 323 1 1 3 4.8 CN1CC=C(C2=Nc3cc(Cl)ccc3Nc3ccccc32)CC1 10.1016/j.bmcl.2021.127911
9912392 116743 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.
ChEMBL 466 8 0 10 4.1 CN1CCC=C(c2nsnc2SCCCSc2nsnc2C2=CCCN(C)C2)C1 10.1021/jm0102405
CHEMBL337131 116743 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.
ChEMBL 466 8 0 10 4.1 CN1CCC=C(c2nsnc2SCCCSc2nsnc2C2=CCCN(C)C2)C1 10.1021/jm0102405
290 2473 None 4 Human Functional pEC50 = 5.5 5.5 -7 5
Effective concentration for HMPA (human muscarinic inositol phosphate accumulation) activity measured in CHO cells expressing Muscarinic acetylcholine receptor M1Effective concentration for HMPA (human muscarinic inositol phosphate accumulation) activity measured in CHO cells expressing Muscarinic acetylcholine receptor M1
ChEMBL 316 3 1 2 -0.4 O=C(Nc1cccc(c1)Cl)OCC#CC[N+](C)(C)C.[Cl-] 10.1016/S0960-894X(00)80538-7
4022 2473 None 4 Human Functional pEC50 = 5.5 5.5 -7 5
Effective concentration for HMPA (human muscarinic inositol phosphate accumulation) activity measured in CHO cells expressing Muscarinic acetylcholine receptor M1Effective concentration for HMPA (human muscarinic inositol phosphate accumulation) activity measured in CHO cells expressing Muscarinic acetylcholine receptor M1
ChEMBL 316 3 1 2 -0.4 O=C(Nc1cccc(c1)Cl)OCC#CC[N+](C)(C)C.[Cl-] 10.1016/S0960-894X(00)80538-7
5926 2473 None 4 Human Functional pEC50 = 5.5 5.5 -7 5
Effective concentration for HMPA (human muscarinic inositol phosphate accumulation) activity measured in CHO cells expressing Muscarinic acetylcholine receptor M1Effective concentration for HMPA (human muscarinic inositol phosphate accumulation) activity measured in CHO cells expressing Muscarinic acetylcholine receptor M1
ChEMBL 316 3 1 2 -0.4 O=C(Nc1cccc(c1)Cl)OCC#CC[N+](C)(C)C.[Cl-] 10.1016/S0960-894X(00)80538-7
CHEMBL40554 2473 None 4 Human Functional pEC50 = 5.5 5.5 -7 5
Effective concentration for HMPA (human muscarinic inositol phosphate accumulation) activity measured in CHO cells expressing Muscarinic acetylcholine receptor M1Effective concentration for HMPA (human muscarinic inositol phosphate accumulation) activity measured in CHO cells expressing Muscarinic acetylcholine receptor M1
ChEMBL 316 3 1 2 -0.4 O=C(Nc1cccc(c1)Cl)OCC#CC[N+](C)(C)C.[Cl-] 10.1016/S0960-894X(00)80538-7
CHEMBL74300 2473 None 4 Human Functional pEC50 = 5.5 5.5 -7 5
Effective concentration for HMPA (human muscarinic inositol phosphate accumulation) activity measured in CHO cells expressing Muscarinic acetylcholine receptor M1Effective concentration for HMPA (human muscarinic inositol phosphate accumulation) activity measured in CHO cells expressing Muscarinic acetylcholine receptor M1
ChEMBL 316 3 1 2 -0.4 O=C(Nc1cccc(c1)Cl)OCC#CC[N+](C)(C)C.[Cl-] 10.1016/S0960-894X(00)80538-7
73672762 112087 None 0 Human Functional pEC50 = 6.5 6.5 -3 2
Agonist activity at human muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as calcium mobilization by FLIPR assayAgonist activity at human muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as calcium mobilization by FLIPR assay
ChEMBL 436 4 0 6 2.1 CCOC(=O)N1CCC(CN2CCC3(CC2)CN(S(C)(=O)=O)c2ncccc23)CC1 10.1016/j.bmcl.2014.04.083
CHEMBL3289440 112087 None 0 Human Functional pEC50 = 6.5 6.5 -3 2
Agonist activity at human muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as calcium mobilization by FLIPR assayAgonist activity at human muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as calcium mobilization by FLIPR assay
ChEMBL 436 4 0 6 2.1 CCOC(=O)N1CCC(CN2CCC3(CC2)CN(S(C)(=O)=O)c2ncccc23)CC1 10.1016/j.bmcl.2014.04.083
139413966 164065 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assayPositive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 344 3 1 3 4.3 COC(C)C1N=C(c2ccccc2)c2cc(Cl)ccc2NC1=S 10.1016/j.bmcl.2017.11.008
CHEMBL4207900 164065 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assayPositive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 344 3 1 3 4.3 COC(C)C1N=C(c2ccccc2)c2cc(Cl)ccc2NC1=S 10.1016/j.bmcl.2017.11.008
146216716 185782 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL 463 5 0 6 4.1 Cn1cc2c(-c3cc(F)c(CN4Cc5cn(CC6CCCO6)nc5C4=O)c(F)c3)cccc2n1 10.1016/j.bmcl.2021.128193
CHEMBL4865056 185782 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL 463 5 0 6 4.1 Cn1cc2c(-c3cc(F)c(CN4Cc5cn(CC6CCCO6)nc5C4=O)c(F)c3)cccc2n1 10.1016/j.bmcl.2021.128193
44579417 187087 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
ChEMBL 424 4 1 4 4.3 O=c1[nH]c2cc(Cl)ccc2n1C1CCN(C2CCN(Cc3ccccc3)CC2)CC1 10.1016/j.bmcl.2008.09.023
CHEMBL490597 187087 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
ChEMBL 424 4 1 4 4.3 O=c1[nH]c2cc(Cl)ccc2n1C1CCN(C2CCN(Cc3ccccc3)CC2)CC1 10.1016/j.bmcl.2008.09.023
146216708 184875 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL 424 5 0 5 3.9 Cc1cc(-c2cc(F)c(CN3Cc4cnn(CC5CCCO5)c4C3=O)c(F)c2)ccn1 10.1016/j.bmcl.2021.128193
CHEMBL4851192 184875 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL 424 5 0 5 3.9 Cc1cc(-c2cc(F)c(CN3Cc4cnn(CC5CCCO5)c4C3=O)c(F)c2)ccn1 10.1016/j.bmcl.2021.128193
122189496 123403 None 0 Human Functional pEC50 = 7.4 7.4 4 3
Agonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 499 5 2 3 5.4 C/C(=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(C(F)(F)F)cc1)[C@H](O)C2)N(C)Cc1ccc(F)cc1 10.1016/j.bmcl.2015.08.011
CHEMBL3616500 123403 None 0 Human Functional pEC50 = 7.4 7.4 4 3
Agonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 499 5 2 3 5.4 C/C(=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(C(F)(F)F)cc1)[C@H](O)C2)N(C)Cc1ccc(F)cc1 10.1016/j.bmcl.2015.08.011
146487777 181639 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Positive allosteric modulation of recombinant human muscarinic M1 receptor co-expressing pCRE-Luc reporter gene in CHO cells assessed as stimulation of luciferase activity in presence of acetylcholine substrate measured after 4 hrs by luciferase reporter gene assayPositive allosteric modulation of recombinant human muscarinic M1 receptor co-expressing pCRE-Luc reporter gene in CHO cells assessed as stimulation of luciferase activity in presence of acetylcholine substrate measured after 4 hrs by luciferase reporter gene assay
ChEMBL 469 6 3 6 3.1 NC(=O)c1cncc(-c2ccc(Cc3cc(C(=O)N[C@H]4CCCC[C@@H]4O)nn4cccc34)cc2)c1 10.1021/acsmedchemlett.1c00118
CHEMBL4765183 181639 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Positive allosteric modulation of recombinant human muscarinic M1 receptor co-expressing pCRE-Luc reporter gene in CHO cells assessed as stimulation of luciferase activity in presence of acetylcholine substrate measured after 4 hrs by luciferase reporter gene assayPositive allosteric modulation of recombinant human muscarinic M1 receptor co-expressing pCRE-Luc reporter gene in CHO cells assessed as stimulation of luciferase activity in presence of acetylcholine substrate measured after 4 hrs by luciferase reporter gene assay
ChEMBL 469 6 3 6 3.1 NC(=O)c1cncc(-c2ccc(Cc3cc(C(=O)N[C@H]4CCCC[C@@H]4O)nn4cccc34)cc2)c1 10.1021/acsmedchemlett.1c00118
145983789 165748 None 0 Rat Functional pEC50 = 6.4 6.4 - 1
Positive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assayPositive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assay
ChEMBL 446 5 2 6 4.3 Cn1ccc2c(Cc3ccc(-c4nccs4)cc3)cc(C(=O)N[C@@H]3CCCC[C@H]3O)nc21 10.1021/acsmedchemlett.8b00261
CHEMBL4244259 165748 None 0 Rat Functional pEC50 = 6.4 6.4 - 1
Positive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assayPositive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assay
ChEMBL 446 5 2 6 4.3 Cn1ccc2c(Cc3ccc(-c4nccs4)cc3)cc(C(=O)N[C@@H]3CCCC[C@H]3O)nc21 10.1021/acsmedchemlett.8b00261
70683569 74373 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
ChEMBL 375 7 2 5 2.2 CCOC(=O)N1[C@H]2CC[C@@H]1C[C@@H](NCCNC(=O)c1cccc(OC)c1)C2 10.1016/j.bmcl.2012.03.088
CHEMBL2024422 74373 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
ChEMBL 375 7 2 5 2.2 CCOC(=O)N1[C@H]2CC[C@@H]1C[C@@H](NCCNC(=O)c1cccc(OC)c1)C2 10.1016/j.bmcl.2012.03.088
76313420 103327 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
ChEMBL 337 6 2 4 1.7 CCOC(=O)N1C[C@@H]2CC[C@H](C1)[C@@H]2NCCNC(=O)C1CCCC1 10.1016/j.bmcl.2012.03.088
CHEMBL3084454 103327 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
ChEMBL 337 6 2 4 1.7 CCOC(=O)N1C[C@@H]2CC[C@H](C1)[C@@H]2NCCNC(=O)C1CCCC1 10.1016/j.bmcl.2012.03.088
44589646 186735 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
ChEMBL 553 4 2 5 5.9 O=C(Nc1cccc(SC(F)(F)F)c1)N1CCC(N2CCC(n3c(=O)[nH]c4cc(Cl)ccc43)CC2)CC1 10.1016/j.bmcl.2008.09.032
CHEMBL487986 186735 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
ChEMBL 553 4 2 5 5.9 O=C(Nc1cccc(SC(F)(F)F)c1)N1CCC(N2CCC(n3c(=O)[nH]c4cc(Cl)ccc43)CC2)CC1 10.1016/j.bmcl.2008.09.032
145983789 165748 None 0 Rat Functional pEC50 = 6.4 6.4 - 1
Positive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assayPositive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assay
ChEMBL 446 5 2 6 4.3 Cn1ccc2c(Cc3ccc(-c4nccs4)cc3)cc(C(=O)N[C@@H]3CCCC[C@H]3O)nc21 10.1021/acsmedchemlett.8b00261
CHEMBL4244259 165748 None 0 Rat Functional pEC50 = 6.4 6.4 - 1
Positive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assayPositive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assay
ChEMBL 446 5 2 6 4.3 Cn1ccc2c(Cc3ccc(-c4nccs4)cc3)cc(C(=O)N[C@@H]3CCCC[C@H]3O)nc21 10.1021/acsmedchemlett.8b00261
126492033 161518 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 435 4 2 5 3.3 O=C(N[C@H]1CCCC[C@@H]1O)C1CN(Cc2ccc(C(F)(F)F)nc2)c2ccccc2O1 10.1016/j.bmcl.2018.05.009
CHEMBL4126902 161518 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 435 4 2 5 3.3 O=C(N[C@H]1CCCC[C@@H]1O)C1CN(Cc2ccc(C(F)(F)F)nc2)c2ccccc2O1 10.1016/j.bmcl.2018.05.009
118724603 116520 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Positive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assay
ChEMBL 394 4 0 5 4.4 Cc1ccc(Cn2nc3c4ccccc4n(Cc4cccnc4)cc-3c2=O)c(C)c1 10.1016/j.bmcl.2014.11.011
CHEMBL3360945 116520 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Positive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assay
ChEMBL 394 4 0 5 4.4 Cc1ccc(Cn2nc3c4ccccc4n(Cc4cccnc4)cc-3c2=O)c(C)c1 10.1016/j.bmcl.2014.11.011
11535022 11811 None 0 Human Functional pEC50 = 4.4 4.4 -14791 2
Potency at muscarinic receptor M1 in rabbit vas deferensPotency at muscarinic receptor M1 in rabbit vas deferens
ChEMBL 574 13 0 3 4.8 CC(C)(CN1C(=O)c2cccc3cccc(c23)C1=O)C[N+](C)(C)CCCCCC[N+](C)(C)CC#CCN1CCCC1=O 10.1021/jm050769s
CHEMBL1181943 11811 None 0 Human Functional pEC50 = 4.4 4.4 -14791 2
Potency at muscarinic receptor M1 in rabbit vas deferensPotency at muscarinic receptor M1 in rabbit vas deferens
ChEMBL 574 13 0 3 4.8 CC(C)(CN1C(=O)c2cccc3cccc(c23)C1=O)C[N+](C)(C)CCCCCC[N+](C)(C)CC#CCN1CCCC1=O 10.1021/jm050769s
CHEMBL199636 11811 None 0 Human Functional pEC50 = 4.4 4.4 -14791 2
Potency at muscarinic receptor M1 in rabbit vas deferensPotency at muscarinic receptor M1 in rabbit vas deferens
ChEMBL 574 13 0 3 4.8 CC(C)(CN1C(=O)c2cccc3cccc(c23)C1=O)C[N+](C)(C)CCCCCC[N+](C)(C)CC#CCN1CCCC1=O 10.1021/jm050769s
118724603 116520 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Positive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assay
ChEMBL 394 4 0 5 4.4 Cc1ccc(Cn2nc3c4ccccc4n(Cc4cccnc4)cc-3c2=O)c(C)c1 10.1016/j.bmcl.2014.11.011
CHEMBL3360945 116520 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Positive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assay
ChEMBL 394 4 0 5 4.4 Cc1ccc(Cn2nc3c4ccccc4n(Cc4cccnc4)cc-3c2=O)c(C)c1 10.1016/j.bmcl.2014.11.011
5377745 164332 None 1 Human Functional pEC50 = 5.4 5.4 - 1
Positive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assayPositive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 266 1 1 2 3.6 Cc1ccc2c(c1)C(c1ccccc1)=NCC(=S)N2 10.1016/j.bmcl.2017.11.008
CHEMBL4211235 164332 None 1 Human Functional pEC50 = 5.4 5.4 - 1
Positive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assayPositive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 266 1 1 2 3.6 Cc1ccc2c(c1)C(c1ccccc1)=NCC(=S)N2 10.1016/j.bmcl.2017.11.008
126492033 161518 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 435 4 2 5 3.3 O=C(N[C@H]1CCCC[C@@H]1O)C1CN(Cc2ccc(C(F)(F)F)nc2)c2ccccc2O1 10.1016/j.bmcl.2018.05.009
CHEMBL4126902 161518 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 435 4 2 5 3.3 O=C(N[C@H]1CCCC[C@@H]1O)C1CN(Cc2ccc(C(F)(F)F)nc2)c2ccccc2O1 10.1016/j.bmcl.2018.05.009
127038319 137083 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Positive allosteric modulation of human M1 receptor expressed in CHO cells assessed as acetylcholine-induced calcium mobilization by FLIPR assayPositive allosteric modulation of human M1 receptor expressed in CHO cells assessed as acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 427 5 2 6 3.6 O=C(N[C@H]1CCCC[C@@H]1O)c1cn(Cc2ccc(-c3cncnc3)cc2)c2cccnc12 10.1016/j.bmcl.2015.11.053
CHEMBL3745962 137083 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Positive allosteric modulation of human M1 receptor expressed in CHO cells assessed as acetylcholine-induced calcium mobilization by FLIPR assayPositive allosteric modulation of human M1 receptor expressed in CHO cells assessed as acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 427 5 2 6 3.6 O=C(N[C@H]1CCCC[C@@H]1O)c1cn(Cc2ccc(-c3cncnc3)cc2)c2cccnc12 10.1016/j.bmcl.2015.11.053
187 255 None 24 Human Functional pEC50 = 6.4 6.4 -5 8
Partial agonist activity at human muscarinic M1 acetylcholine receptor expressed in CHO cells assessed as increase in IP1 accumulation incubated for 30 mins by FRET based HTRF assayPartial agonist activity at human muscarinic M1 acetylcholine receptor expressed in CHO cells assessed as increase in IP1 accumulation incubated for 30 mins by FRET based HTRF assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm500860w
187.0 255 None 24 Human Functional pEC50 = 6.4 6.4 -5 8
Partial agonist activity at human muscarinic M1 acetylcholine receptor expressed in CHO cells assessed as increase in IP1 accumulation incubated for 30 mins by FRET based HTRF assayPartial agonist activity at human muscarinic M1 acetylcholine receptor expressed in CHO cells assessed as increase in IP1 accumulation incubated for 30 mins by FRET based HTRF assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm500860w
294 255 None 24 Human Functional pEC50 = 6.4 6.4 -5 8
Partial agonist activity at human muscarinic M1 acetylcholine receptor expressed in CHO cells assessed as increase in IP1 accumulation incubated for 30 mins by FRET based HTRF assayPartial agonist activity at human muscarinic M1 acetylcholine receptor expressed in CHO cells assessed as increase in IP1 accumulation incubated for 30 mins by FRET based HTRF assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm500860w
65 255 None 24 Human Functional pEC50 = 6.4 6.4 -5 8
Partial agonist activity at human muscarinic M1 acetylcholine receptor expressed in CHO cells assessed as increase in IP1 accumulation incubated for 30 mins by FRET based HTRF assayPartial agonist activity at human muscarinic M1 acetylcholine receptor expressed in CHO cells assessed as increase in IP1 accumulation incubated for 30 mins by FRET based HTRF assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm500860w
8593 255 None 24 Human Functional pEC50 = 6.4 6.4 -5 8
Partial agonist activity at human muscarinic M1 acetylcholine receptor expressed in CHO cells assessed as increase in IP1 accumulation incubated for 30 mins by FRET based HTRF assayPartial agonist activity at human muscarinic M1 acetylcholine receptor expressed in CHO cells assessed as increase in IP1 accumulation incubated for 30 mins by FRET based HTRF assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm500860w
CHEMBL667 255 None 24 Human Functional pEC50 = 6.4 6.4 -5 8
Partial agonist activity at human muscarinic M1 acetylcholine receptor expressed in CHO cells assessed as increase in IP1 accumulation incubated for 30 mins by FRET based HTRF assayPartial agonist activity at human muscarinic M1 acetylcholine receptor expressed in CHO cells assessed as increase in IP1 accumulation incubated for 30 mins by FRET based HTRF assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm500860w
DB03128 255 None 24 Human Functional pEC50 = 6.4 6.4 -5 8
Partial agonist activity at human muscarinic M1 acetylcholine receptor expressed in CHO cells assessed as increase in IP1 accumulation incubated for 30 mins by FRET based HTRF assayPartial agonist activity at human muscarinic M1 acetylcholine receptor expressed in CHO cells assessed as increase in IP1 accumulation incubated for 30 mins by FRET based HTRF assay
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1021/jm500860w
44247542 61840 None 0 Rat Functional pEC50 = 5.4 5.4 - 1
Allosteric modulation at rat M1 receptor expressed in CHO cells by calcium mobilization assayAllosteric modulation at rat M1 receptor expressed in CHO cells by calcium mobilization assay
ChEMBL 487 6 1 6 4.2 Cc1cc(NC(=O)CS(=O)(=O)c2cn(Cc3cccc(Br)c3)c3ccccc23)no1 10.1016/j.bmcl.2010.12.015
CHEMBL1773272 61840 None 0 Rat Functional pEC50 = 5.4 5.4 - 1
Allosteric modulation at rat M1 receptor expressed in CHO cells by calcium mobilization assayAllosteric modulation at rat M1 receptor expressed in CHO cells by calcium mobilization assay
ChEMBL 487 6 1 6 4.2 Cc1cc(NC(=O)CS(=O)(=O)c2cn(Cc3cccc(Br)c3)c3ccccc23)no1 10.1016/j.bmcl.2010.12.015
118724602 116519 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Positive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assay
ChEMBL 394 4 0 5 4.4 Cc1ccc(Cn2nc3c4ccccc4n(Cc4ccccn4)cc-3c2=O)c(C)c1 10.1016/j.bmcl.2014.11.011
CHEMBL3360944 116519 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Positive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assay
ChEMBL 394 4 0 5 4.4 Cc1ccc(Cn2nc3c4ccccc4n(Cc4ccccn4)cc-3c2=O)c(C)c1 10.1016/j.bmcl.2014.11.011
162669110 182699 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Positive allosteric modulation of human muscarinic M1 receptor stably expressed in CHO cells assessed as increase in Ach-induced intracellular calcium level preincubated for 10 mins followed by addition of Ach at EC20 concentration by Fluo-8AM dye based FLIPR TETRA methodPositive allosteric modulation of human muscarinic M1 receptor stably expressed in CHO cells assessed as increase in Ach-induced intracellular calcium level preincubated for 10 mins followed by addition of Ach at EC20 concentration by Fluo-8AM dye based FLIPR TETRA method
ChEMBL 421 5 2 6 3.0 Cc1c(Cc2ccc(-c3cocn3)cc2)cc(C(=O)N[C@H]2CCCC[C@@H]2O)c(=O)n1C 10.1021/acs.jmedchem.6b00544
CHEMBL4788101 182699 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Positive allosteric modulation of human muscarinic M1 receptor stably expressed in CHO cells assessed as increase in Ach-induced intracellular calcium level preincubated for 10 mins followed by addition of Ach at EC20 concentration by Fluo-8AM dye based FLIPR TETRA methodPositive allosteric modulation of human muscarinic M1 receptor stably expressed in CHO cells assessed as increase in Ach-induced intracellular calcium level preincubated for 10 mins followed by addition of Ach at EC20 concentration by Fluo-8AM dye based FLIPR TETRA method
ChEMBL 421 5 2 6 3.0 Cc1c(Cc2ccc(-c3cocn3)cc2)cc(C(=O)N[C@H]2CCCC[C@@H]2O)c(=O)n1C 10.1021/acs.jmedchem.6b00544
145982857 165893 None 0 Rat Functional pEC50 = 7.4 7.4 -2 2
Positive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assayPositive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assay
ChEMBL 445 5 2 7 2.4 Cn1ccc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCOC[C@H]4O)nc4c3ccn4C)cc2)n1 10.1021/acsmedchemlett.8b00261
CHEMBL4248057 165893 None 0 Rat Functional pEC50 = 7.4 7.4 -2 2
Positive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assayPositive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assay
ChEMBL 445 5 2 7 2.4 Cn1ccc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCOC[C@H]4O)nc4c3ccn4C)cc2)n1 10.1021/acsmedchemlett.8b00261
145962138 161526 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 410 5 2 6 2.3 CN(C)c1ccc(CN2CC(C(=O)N[C@H]3CCCC[C@@H]3O)Oc3ccccc32)cn1 10.1016/j.bmcl.2018.05.009
CHEMBL4127118 161526 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 410 5 2 6 2.3 CN(C)c1ccc(CN2CC(C(=O)N[C@H]3CCCC[C@@H]3O)Oc3ccccc32)cn1 10.1016/j.bmcl.2018.05.009
145962138 161526 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 410 5 2 6 2.3 CN(C)c1ccc(CN2CC(C(=O)N[C@H]3CCCC[C@@H]3O)Oc3ccccc32)cn1 10.1016/j.bmcl.2018.05.009
CHEMBL4127118 161526 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 410 5 2 6 2.3 CN(C)c1ccc(CN2CC(C(=O)N[C@H]3CCCC[C@@H]3O)Oc3ccccc32)cn1 10.1016/j.bmcl.2018.05.009
118724602 116519 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Positive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assay
ChEMBL 394 4 0 5 4.4 Cc1ccc(Cn2nc3c4ccccc4n(Cc4ccccn4)cc-3c2=O)c(C)c1 10.1016/j.bmcl.2014.11.011
CHEMBL3360944 116519 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Positive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assay
ChEMBL 394 4 0 5 4.4 Cc1ccc(Cn2nc3c4ccccc4n(Cc4ccccn4)cc-3c2=O)c(C)c1 10.1016/j.bmcl.2014.11.011
2551 794 None 13 Human Functional pEC50 = 5.4 5.4 -27 13
Stimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptorStimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptor
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/s0960-894x(98)00509-5
2551.0 794 None 13 Human Functional pEC50 = 5.4 5.4 -27 13
Stimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptorStimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptor
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/s0960-894x(98)00509-5
298 794 None 13 Human Functional pEC50 = 5.4 5.4 -27 13
Stimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptorStimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptor
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/s0960-894x(98)00509-5
488 794 None 13 Human Functional pEC50 = 5.4 5.4 -27 13
Stimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptorStimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptor
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/s0960-894x(98)00509-5
CHEMBL965 794 None 13 Human Functional pEC50 = 5.4 5.4 -27 13
Stimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptorStimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptor
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/s0960-894x(98)00509-5
DB00411 794 None 13 Human Functional pEC50 = 5.4 5.4 -27 13
Stimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptorStimulation of phosphoinositide hydrolysis in A9L cells expressing human m1 receptor
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1016/s0960-894x(98)00509-5
46891141 6564 None 0 Human Functional pEC50 = 7.4 7.4 251 2
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 374 5 2 2 4.5 CC[C@H]1CNCC[C@@H]1CNC(=O)c1c(F)cccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.127
CHEMBL1083002 6564 None 0 Human Functional pEC50 = 7.4 7.4 251 2
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 374 5 2 2 4.5 CC[C@H]1CNCC[C@@H]1CNC(=O)c1c(F)cccc1-c1cccc(Cl)c1 10.1016/j.bmcl.2010.04.127
46891030 6598 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 362 4 2 2 4.4 O=C(NCC1CCNCC1)c1ccccc1-c1cc(Cl)ccc1Cl 10.1016/j.bmcl.2010.04.128
CHEMBL1083109 6598 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 362 4 2 2 4.4 O=C(NCC1CCNCC1)c1ccccc1-c1cc(Cl)ccc1Cl 10.1016/j.bmcl.2010.04.128
122191007 123683 None 0 Human Functional pEC50 = 6.4 6.4 -1 3
Agonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 449 5 2 3 4.5 C/C(=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(F)cc1)[C@H](O)C2)N(C)Cc1ccc(F)cc1 10.1016/j.bmcl.2015.08.011
CHEMBL3618449 123683 None 0 Human Functional pEC50 = 6.4 6.4 -1 3
Agonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 449 5 2 3 4.5 C/C(=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(F)cc1)[C@H](O)C2)N(C)Cc1ccc(F)cc1 10.1016/j.bmcl.2015.08.011
162646270 179745 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Positive allosteric modulation of human muscarinic M1 receptor stably expressed in CHO cells assessed as increase in Ach-induced intracellular calcium level preincubated for 10 mins followed by addition of Ach at EC20 concentration by Fluo-8AM dye based FLIPR TETRA methodPositive allosteric modulation of human muscarinic M1 receptor stably expressed in CHO cells assessed as increase in Ach-induced intracellular calcium level preincubated for 10 mins followed by addition of Ach at EC20 concentration by Fluo-8AM dye based FLIPR TETRA method
ChEMBL 392 5 2 6 2.0 Cc1ncc(C(=O)N[C@H]2CCOC[C@@H]2O)cc1Cc1ccc(-n2cccn2)cc1 10.1021/acs.jmedchem.6b00544
CHEMBL4742964 179745 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Positive allosteric modulation of human muscarinic M1 receptor stably expressed in CHO cells assessed as increase in Ach-induced intracellular calcium level preincubated for 10 mins followed by addition of Ach at EC20 concentration by Fluo-8AM dye based FLIPR TETRA methodPositive allosteric modulation of human muscarinic M1 receptor stably expressed in CHO cells assessed as increase in Ach-induced intracellular calcium level preincubated for 10 mins followed by addition of Ach at EC20 concentration by Fluo-8AM dye based FLIPR TETRA method
ChEMBL 392 5 2 6 2.0 Cc1ncc(C(=O)N[C@H]2CCOC[C@@H]2O)cc1Cc1ccc(-n2cccn2)cc1 10.1021/acs.jmedchem.6b00544
146216712 185703 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL 437 6 0 6 3.5 COCCn1ncc2c1C(=O)N(Cc1c(F)cc(-c3cccc4nn(C)cc34)cc1F)C2 10.1016/j.bmcl.2021.128193
CHEMBL4863755 185703 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL 437 6 0 6 3.5 COCCn1ncc2c1C(=O)N(Cc1c(F)cc(-c3cccc4nn(C)cc34)cc1F)C2 10.1016/j.bmcl.2021.128193
146216726 185605 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL 377 3 0 4 4.6 Cn1cc2c(-c3ccc(CN4Cc5sccc5C4=O)c(F)c3)cccc2n1 10.1016/j.bmcl.2021.128193
CHEMBL4862413 185605 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assayPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
ChEMBL 377 3 0 4 4.6 Cn1cc2c(-c3ccc(CN4Cc5sccc5C4=O)c(F)c3)cccc2n1 10.1016/j.bmcl.2021.128193
46890911 7395 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 356 5 1 2 4.4 CC(=O)N(Cc1ccccc1-c1cccc(Cl)c1)CC1CCNCC1 10.1016/j.bmcl.2010.04.127
CHEMBL1086479 7395 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium level by FLIPR assay
ChEMBL 356 5 1 2 4.4 CC(=O)N(Cc1ccccc1-c1cccc(Cl)c1)CC1CCNCC1 10.1016/j.bmcl.2010.04.127
44204999 63838 None 4 Human Functional pEC50 = 6.4 6.4 -7 3
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assay
ChEMBL 369 6 1 4 3.6 O=c1[nH]c2ccccc2n1C1CCN(CCCOc2ccc(F)cc2)CC1 10.1021/ml100105x
CHEMBL1802360 63838 None 4 Human Functional pEC50 = 6.4 6.4 -7 3
Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as intracellular calcium mobilization after 10 to 15 mins by FLIPR assay
ChEMBL 369 6 1 4 3.6 O=c1[nH]c2ccccc2n1C1CCN(CCCOc2ccc(F)cc2)CC1 10.1021/ml100105x
71540384 86385 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Positive allosteric modulator activity at human muscarinic M1 receptor by calcium mobilization assayPositive allosteric modulator activity at human muscarinic M1 receptor by calcium mobilization assay
ChEMBL 387 3 1 4 3.4 Cn1cc(-c2ccc(CN3C(=O)C(O)(C(F)(F)F)c4ccccc43)cc2)cn1 10.1016/j.bmcl.2012.11.092
CHEMBL2313507 86385 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Positive allosteric modulator activity at human muscarinic M1 receptor by calcium mobilization assayPositive allosteric modulator activity at human muscarinic M1 receptor by calcium mobilization assay
ChEMBL 387 3 1 4 3.4 Cn1cc(-c2ccc(CN3C(=O)C(O)(C(F)(F)F)c4ccccc43)cc2)cn1 10.1016/j.bmcl.2012.11.092
145976302 163741 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Positive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assayPositive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 328 2 1 2 5.0 CC(C)[C@@H]1N=C(c2ccccc2)c2ccc(Cl)cc2NC1=S 10.1016/j.bmcl.2017.11.008
CHEMBL4204098 163741 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Positive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assayPositive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 328 2 1 2 5.0 CC(C)[C@@H]1N=C(c2ccccc2)c2ccc(Cl)cc2NC1=S 10.1016/j.bmcl.2017.11.008
44157160 178888 None 2 Rat Functional pEC50 = 5.4 5.4 -2 2
Activation of rat muscarinic M1 receptor expressed in CHO cells co-expressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of rat muscarinic M1 receptor expressed in CHO cells co-expressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 333 2 0 2 3.3 O=C1C(=O)N(Cc2ccc(Br)cc2)c2c(F)cccc21 10.1021/jm900286j
CHEMBL468925 178888 None 2 Rat Functional pEC50 = 5.4 5.4 -2 2
Activation of rat muscarinic M1 receptor expressed in CHO cells co-expressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilizationActivation of rat muscarinic M1 receptor expressed in CHO cells co-expressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
ChEMBL 333 2 0 2 3.3 O=C1C(=O)N(Cc2ccc(Br)cc2)c2c(F)cccc21 10.1021/jm900286j
44303323 163337 None 0 Human Functional pEC50 = 8.4 8.4 4 3
Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.
ChEMBL 343 3 0 5 2.6 Fc1ccc(C#CCSc2nsnc2C23CN4CC2C3C4)cc1 10.1021/jm9910019
CHEMBL418491 163337 None 0 Human Functional pEC50 = 8.4 8.4 4 3
Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.
ChEMBL 343 3 0 5 2.6 Fc1ccc(C#CCSc2nsnc2C23CN4CC2C3C4)cc1 10.1021/jm9910019
10019339 102681 None 0 Human Functional pEC50 = 8.3 8.3 4 3
Compound was tested for its ability to stimulate phosphoinositol (PI) hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1 (100 uM concentration)Compound was tested for its ability to stimulate phosphoinositol (PI) hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1 (100 uM concentration)
ChEMBL 327 3 0 5 1.9 Fc1cccc(C#CCOc2nsnc2C23CN4CC2C3C4)c1 10.1021/jm9910019
CHEMBL304247 102681 None 0 Human Functional pEC50 = 8.3 8.3 4 3
Compound was tested for its ability to stimulate phosphoinositol (PI) hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1 (100 uM concentration)Compound was tested for its ability to stimulate phosphoinositol (PI) hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1 (100 uM concentration)
ChEMBL 327 3 0 5 1.9 Fc1cccc(C#CCOc2nsnc2C23CN4CC2C3C4)c1 10.1021/jm9910019
145969714 165150 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Positive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as increase in ACh-induced intracellular calcium level preincubated for 10 mins followed by ACh addition measured every 2 secs for 80 secs by Fluo-4 dye-based FLIPR assayPositive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as increase in ACh-induced intracellular calcium level preincubated for 10 mins followed by ACh addition measured every 2 secs for 80 secs by Fluo-4 dye-based FLIPR assay
ChEMBL 436 6 3 7 1.7 Cn1c(CO)c(Cc2ccc(-n3cccn3)cc2)cc(C(=O)N[C@H]2CCCC[C@@H]2O)c1=O 10.1016/j.bmcl.2018.04.054
CHEMBL4226420 165150 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Positive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as increase in ACh-induced intracellular calcium level preincubated for 10 mins followed by ACh addition measured every 2 secs for 80 secs by Fluo-4 dye-based FLIPR assayPositive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as increase in ACh-induced intracellular calcium level preincubated for 10 mins followed by ACh addition measured every 2 secs for 80 secs by Fluo-4 dye-based FLIPR assay
ChEMBL 436 6 3 7 1.7 Cn1c(CO)c(Cc2ccc(-n3cccn3)cc2)cc(C(=O)N[C@H]2CCCC[C@@H]2O)c1=O 10.1016/j.bmcl.2018.04.054
145983485 165576 None 0 Rat Functional pEC50 = 7.4 7.4 - 1
Positive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assayPositive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assay
ChEMBL 444 5 2 7 3.0 Cn1cc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCCC[C@H]4O)nc4c3ccn4C)cn2)cn1 10.1021/acsmedchemlett.8b00261
CHEMBL4240041 165576 None 0 Rat Functional pEC50 = 7.4 7.4 - 1
Positive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assayPositive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assay
ChEMBL 444 5 2 7 3.0 Cn1cc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCCC[C@H]4O)nc4c3ccn4C)cn2)cn1 10.1021/acsmedchemlett.8b00261
145982857 165893 None 0 Rat Functional pEC50 = 7.4 7.4 -2 2
Positive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assayPositive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assay
ChEMBL 445 5 2 7 2.4 Cn1ccc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCOC[C@H]4O)nc4c3ccn4C)cc2)n1 10.1021/acsmedchemlett.8b00261
CHEMBL4248057 165893 None 0 Rat Functional pEC50 = 7.4 7.4 -2 2
Positive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assayPositive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assay
ChEMBL 445 5 2 7 2.4 Cn1ccc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCOC[C@H]4O)nc4c3ccn4C)cc2)n1 10.1021/acsmedchemlett.8b00261
44204999 63838 None 4 Human Functional pEC50 = 6.4 6.4 -7 3
Agonist activity at human M1 muscarinic receptor expressed in CHO cells assessed as inhibition of carbachol-stimulated phosphatidyl-inositol hydrolysis by cell-based functional assayAgonist activity at human M1 muscarinic receptor expressed in CHO cells assessed as inhibition of carbachol-stimulated phosphatidyl-inositol hydrolysis by cell-based functional assay
ChEMBL 369 6 1 4 3.6 O=c1[nH]c2ccccc2n1C1CCN(CCCOc2ccc(F)cc2)CC1 10.1021/jm200371q
CHEMBL1802360 63838 None 4 Human Functional pEC50 = 6.4 6.4 -7 3
Agonist activity at human M1 muscarinic receptor expressed in CHO cells assessed as inhibition of carbachol-stimulated phosphatidyl-inositol hydrolysis by cell-based functional assayAgonist activity at human M1 muscarinic receptor expressed in CHO cells assessed as inhibition of carbachol-stimulated phosphatidyl-inositol hydrolysis by cell-based functional assay
ChEMBL 369 6 1 4 3.6 O=c1[nH]c2ccccc2n1C1CCN(CCCOc2ccc(F)cc2)CC1 10.1021/jm200371q
68634 76379 None 27 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
ChEMBL 337 5 1 4 3.0 O=c1[nH]c2ccccc2n1C1CCN(CCOc2ccccc2)CC1 10.1016/j.bmcl.2012.05.048
CHEMBL2059304 76379 None 27 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
ChEMBL 337 5 1 4 3.0 O=c1[nH]c2ccccc2n1C1CCN(CCOc2ccccc2)CC1 10.1016/j.bmcl.2012.05.048
1726 2497 None 8 Rat Functional pEC50 = 6.4 6.4 -12 8
Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M1Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M1
ChEMBL 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 10.1021/jm9705115
1993 2497 None 8 Rat Functional pEC50 = 6.4 6.4 -12 8
Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M1Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M1
ChEMBL 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 10.1021/jm9705115
1993.0 2497 None 8 Rat Functional pEC50 = 6.4 6.4 -12 8
Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M1Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M1
ChEMBL 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 10.1021/jm9705115
7438 2497 None 8 Rat Functional pEC50 = 6.4 6.4 -12 8
Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M1Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M1
ChEMBL 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 10.1021/jm9705115
CHEMBL978 2497 None 8 Rat Functional pEC50 = 6.4 6.4 -12 8
Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M1Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M1
ChEMBL 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 10.1021/jm9705115
DB06709 2497 None 8 Rat Functional pEC50 = 6.4 6.4 -12 8
Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M1Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M1
ChEMBL 160 3 0 2 0.6 CC(C[N+](C)(C)C)OC(=O)C 10.1021/jm9705115
71540384 86385 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Positive allosteric modulator activity at human muscarinic M1 receptor by calcium mobilization assayPositive allosteric modulator activity at human muscarinic M1 receptor by calcium mobilization assay
ChEMBL 387 3 1 4 3.4 Cn1cc(-c2ccc(CN3C(=O)C(O)(C(F)(F)F)c4ccccc43)cc2)cn1 10.1016/j.bmcl.2012.11.092
CHEMBL2313507 86385 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Positive allosteric modulator activity at human muscarinic M1 receptor by calcium mobilization assayPositive allosteric modulator activity at human muscarinic M1 receptor by calcium mobilization assay
ChEMBL 387 3 1 4 3.4 Cn1cc(-c2ccc(CN3C(=O)C(O)(C(F)(F)F)c4ccccc43)cc2)cn1 10.1016/j.bmcl.2012.11.092
146487737 179924 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Positive allosteric modulation of recombinant human muscarinic M1 receptor co-expressing pCRE-Luc reporter gene in CHO cells assessed as stimulation of luciferase activity in presence of acetylcholine substrate measured after 4 hrs by luciferase reporter gene assayPositive allosteric modulation of recombinant human muscarinic M1 receptor co-expressing pCRE-Luc reporter gene in CHO cells assessed as stimulation of luciferase activity in presence of acetylcholine substrate measured after 4 hrs by luciferase reporter gene assay
ChEMBL 400 6 2 5 3.5 CC(C)(O)CNC(=O)c1cc(Cc2ccc(-c3ccncc3)cc2)c2cccn2n1 10.1021/acsmedchemlett.1c00118
CHEMBL4745001 179924 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Positive allosteric modulation of recombinant human muscarinic M1 receptor co-expressing pCRE-Luc reporter gene in CHO cells assessed as stimulation of luciferase activity in presence of acetylcholine substrate measured after 4 hrs by luciferase reporter gene assayPositive allosteric modulation of recombinant human muscarinic M1 receptor co-expressing pCRE-Luc reporter gene in CHO cells assessed as stimulation of luciferase activity in presence of acetylcholine substrate measured after 4 hrs by luciferase reporter gene assay
ChEMBL 400 6 2 5 3.5 CC(C)(O)CNC(=O)c1cc(Cc2ccc(-c3ccncc3)cc2)c2cccn2n1 10.1021/acsmedchemlett.1c00118
334 236 None 29 Human Functional pEC50 = 7.4 7.4 24 4
Agonist activity at human muscarinic M1 receptor by calcium mobilization assayAgonist activity at human muscarinic M1 receptor by calcium mobilization assay
ChEMBL 348 7 0 3 3.8 CCCCC1CCN(CC1)CCCN1C(=O)COc2c1ccc(c2)F 10.1016/j.bmcl.2012.03.088
9928284 236 None 29 Human Functional pEC50 = 7.4 7.4 24 4
Agonist activity at human muscarinic M1 receptor by calcium mobilization assayAgonist activity at human muscarinic M1 receptor by calcium mobilization assay
ChEMBL 348 7 0 3 3.8 CCCCC1CCN(CC1)CCCN1C(=O)COc2c1ccc(c2)F 10.1016/j.bmcl.2012.03.088
CHEMBL2022960 236 None 29 Human Functional pEC50 = 7.4 7.4 24 4
Agonist activity at human muscarinic M1 receptor by calcium mobilization assayAgonist activity at human muscarinic M1 receptor by calcium mobilization assay
ChEMBL 348 7 0 3 3.8 CCCCC1CCN(CC1)CCCN1C(=O)COc2c1ccc(c2)F 10.1016/j.bmcl.2012.03.088
146487795 180107 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Positive allosteric modulation of recombinant human muscarinic M1 receptor co-expressing pCRE-Luc reporter gene in CHO cells assessed as stimulation of luciferase activity in presence of acetylcholine substrate measured after 4 hrs by luciferase reporter gene assayPositive allosteric modulation of recombinant human muscarinic M1 receptor co-expressing pCRE-Luc reporter gene in CHO cells assessed as stimulation of luciferase activity in presence of acetylcholine substrate measured after 4 hrs by luciferase reporter gene assay
ChEMBL 440 5 2 5 4.3 Cc1cccc(-c2ccc(Cc3cc(C(=O)N[C@H]4CCCC[C@@H]4O)nn4cccc34)cc2)n1 10.1021/acsmedchemlett.1c00118
CHEMBL4747042 180107 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Positive allosteric modulation of recombinant human muscarinic M1 receptor co-expressing pCRE-Luc reporter gene in CHO cells assessed as stimulation of luciferase activity in presence of acetylcholine substrate measured after 4 hrs by luciferase reporter gene assayPositive allosteric modulation of recombinant human muscarinic M1 receptor co-expressing pCRE-Luc reporter gene in CHO cells assessed as stimulation of luciferase activity in presence of acetylcholine substrate measured after 4 hrs by luciferase reporter gene assay
ChEMBL 440 5 2 5 4.3 Cc1cccc(-c2ccc(Cc3cc(C(=O)N[C@H]4CCCC[C@@H]4O)nn4cccc34)cc2)n1 10.1021/acsmedchemlett.1c00118
145983485 165576 None 0 Rat Functional pEC50 = 7.4 7.4 - 1
Positive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assayPositive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assay
ChEMBL 444 5 2 7 3.0 Cn1cc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCCC[C@H]4O)nc4c3ccn4C)cn2)cn1 10.1021/acsmedchemlett.8b00261
CHEMBL4240041 165576 None 0 Rat Functional pEC50 = 7.4 7.4 - 1
Positive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assayPositive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assay
ChEMBL 444 5 2 7 3.0 Cn1cc(-c2ccc(Cc3cc(C(=O)N[C@@H]4CCCC[C@H]4O)nc4c3ccn4C)cn2)cn1 10.1021/acsmedchemlett.8b00261
10027177 182583 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
ChEMBL 458 4 1 4 4.7 O=c1[nH]c2ccccc2n1C1CCN(C2CCN(Cc3ccccc3C(F)(F)F)CC2)CC1 10.1016/j.bmcl.2008.09.023
CHEMBL478662 182583 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
ChEMBL 458 4 1 4 4.7 O=c1[nH]c2ccccc2n1C1CCN(C2CCN(Cc3ccccc3C(F)(F)F)CC2)CC1 10.1016/j.bmcl.2008.09.023
70687825 74335 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
ChEMBL 331 6 2 4 1.4 CCOC(=O)N1C[C@H]2C(NCCNC(=O)c3ccccc3C)[C@H]2C1 10.1016/j.bmcl.2012.03.088
CHEMBL2024326 74335 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
ChEMBL 331 6 2 4 1.4 CCOC(=O)N1C[C@H]2C(NCCNC(=O)c3ccccc3C)[C@H]2C1 10.1016/j.bmcl.2012.03.088
44589596 192646 None 0 Human Functional pEC50 = 5.4 5.4 -1 2
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
ChEMBL 474 4 1 5 3.5 O=c1[nH]c2cc(Cl)ccc2n1C1CCN(C2CCN(S(=O)(=O)c3ccccc3)CC2)CC1 10.1016/j.bmcl.2008.09.032
CHEMBL521030 192646 None 0 Human Functional pEC50 = 5.4 5.4 -1 2
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
ChEMBL 474 4 1 5 3.5 O=c1[nH]c2cc(Cl)ccc2n1C1CCN(C2CCN(S(=O)(=O)c3ccccc3)CC2)CC1 10.1016/j.bmcl.2008.09.032
139414075 164532 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Positive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assayPositive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 334 2 1 2 5.5 CC(C)[C@@H]1N=C(C2CCCCC2)c2cc(Cl)ccc2NC1=S 10.1016/j.bmcl.2017.11.008
CHEMBL4213762 164532 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Positive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assayPositive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 334 2 1 2 5.5 CC(C)[C@@H]1N=C(C2CCCCC2)c2cc(Cl)ccc2NC1=S 10.1016/j.bmcl.2017.11.008
139414129 163652 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Positive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assayPositive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 346 2 1 2 5.1 CC(C)[C@H]1N=C(c2ccccc2F)c2cc(Cl)ccc2NC1=S 10.1016/j.bmcl.2017.11.008
CHEMBL4203058 163652 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Positive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assayPositive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 346 2 1 2 5.1 CC(C)[C@H]1N=C(c2ccccc2F)c2cc(Cl)ccc2NC1=S 10.1016/j.bmcl.2017.11.008
122191004 123400 None 0 Human Functional pEC50 = 6.4 6.4 -1 3
Agonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 521 7 3 4 4.7 COc1ccc(CCN/C(C)=N/c2ccc3c(c2)[C@@H](NC(=O)c2ccc(Br)cc2)[C@H](O)C3)cc1 10.1016/j.bmcl.2015.08.011
CHEMBL3616497 123400 None 0 Human Functional pEC50 = 6.4 6.4 -1 3
Agonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assayAgonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
ChEMBL 521 7 3 4 4.7 COc1ccc(CCN/C(C)=N/c2ccc3c(c2)[C@@H](NC(=O)c2ccc(Br)cc2)[C@H](O)C3)cc1 10.1016/j.bmcl.2015.08.011
127049132 141079 None 0 Rat Functional pEC50 = 5.4 5.4 - 1
Positive allosteric modulation at rat muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation at rat muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 404 3 0 4 4.1 Cn1cc2c(-c3cc(F)c(CN4CCc5ncccc5C4=O)c(F)c3)cccc2n1 10.1016/j.bmcl.2016.04.083
CHEMBL3823474 141079 None 0 Rat Functional pEC50 = 5.4 5.4 - 1
Positive allosteric modulation at rat muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation at rat muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 404 3 0 4 4.1 Cn1cc2c(-c3cc(F)c(CN4CCc5ncccc5C4=O)c(F)c3)cccc2n1 10.1016/j.bmcl.2016.04.083
44350994 116880 None 0 Human Functional pEC50 = 6.4 6.4 -54 2
Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.
ChEMBL 285 5 0 6 2.5 CCCSc1nsnc1OC1CN2CCC1CC2 10.1021/jm970125n
CHEMBL337925 116880 None 0 Human Functional pEC50 = 6.4 6.4 -54 2
Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.
ChEMBL 285 5 0 6 2.5 CCCSc1nsnc1OC1CN2CCC1CC2 10.1021/jm970125n
127049132 141079 None 0 Rat Functional pEC50 = 5.4 5.4 - 1
Positive allosteric modulation at rat muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation at rat muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 404 3 0 4 4.1 Cn1cc2c(-c3cc(F)c(CN4CCc5ncccc5C4=O)c(F)c3)cccc2n1 10.1016/j.bmcl.2016.04.083
CHEMBL3823474 141079 None 0 Rat Functional pEC50 = 5.4 5.4 - 1
Positive allosteric modulation at rat muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation at rat muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 404 3 0 4 4.1 Cn1cc2c(-c3cc(F)c(CN4CCc5ncccc5C4=O)c(F)c3)cccc2n1 10.1016/j.bmcl.2016.04.083
10403330 17336 None 2 Human Functional pEC50 = 6.4 6.4 -61 2
Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.
ChEMBL 313 7 0 6 3.3 CCCCCSc1nsnc1OC1CN2CCC1CC2 10.1021/jm970125n
CHEMBL125732 17336 None 2 Human Functional pEC50 = 6.4 6.4 -61 2
Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.
ChEMBL 313 7 0 6 3.3 CCCCCSc1nsnc1OC1CN2CCC1CC2 10.1021/jm970125n
62705507 76396 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
ChEMBL 424 5 1 5 2.9 O=C1COc2ccccc2N1CCCN1CCC(n2c(=O)[nH]c3ccc(F)cc32)CC1 10.1016/j.bmcl.2012.05.048
CHEMBL2059322 76396 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based stainingAgonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
ChEMBL 424 5 1 5 2.9 O=C1COc2ccccc2N1CCCN1CCC(n2c(=O)[nH]c3ccc(F)cc32)CC1 10.1016/j.bmcl.2012.05.048
70692024 74372 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
ChEMBL 379 6 2 4 2.8 CCOC(=O)N1[C@H]2CC[C@@H]1C[C@@H](NCCNC(=O)c1cccc(Cl)c1)C2 10.1016/j.bmcl.2012.03.088
CHEMBL2024421 74372 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
ChEMBL 379 6 2 4 2.8 CCOC(=O)N1[C@H]2CC[C@@H]1C[C@@H](NCCNC(=O)c1cccc(Cl)c1)C2 10.1016/j.bmcl.2012.03.088
10962438 119238 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.
ChEMBL 452 7 0 10 3.7 CN1CCC=C(c2nsnc2SCCSc2nsnc2C2=CCCN(C)C2)C1 10.1021/jm0102405
CHEMBL343055 119238 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.
ChEMBL 452 7 0 10 3.7 CN1CCC=C(c2nsnc2SCCSc2nsnc2C2=CCCN(C)C2)C1 10.1021/jm0102405
44589643 186733 None 0 Human Functional pEC50 = 5.4 5.4 -1 2
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
ChEMBL 518 4 1 5 3.6 O=c1[nH]c2cc(Br)ccc2n1C1CCN(C2CCN(S(=O)(=O)c3ccccc3)CC2)CC1 10.1016/j.bmcl.2008.09.032
CHEMBL487984 186733 None 0 Human Functional pEC50 = 5.4 5.4 -1 2
Agonist activity at muscarinic M1 receptorAgonist activity at muscarinic M1 receptor
ChEMBL 518 4 1 5 3.6 O=c1[nH]c2cc(Br)ccc2n1C1CCN(C2CCN(S(=O)(=O)c3ccccc3)CC2)CC1 10.1016/j.bmcl.2008.09.032
54583035 61811 None 0 Rat Functional pEC50 = 5.4 5.4 - 1
Allosteric modulation at rat M1 receptor expressed in CHO cells by calcium mobilization assayAllosteric modulation at rat M1 receptor expressed in CHO cells by calcium mobilization assay
ChEMBL 493 7 2 7 3.9 Cc1cc(NC(=O)CS(=O)(=O)c2cn(Cc3cccc(-c4cn[nH]c4)c3F)c3ccccc23)no1 10.1016/j.bmcl.2010.12.015
CHEMBL1773114 61811 None 0 Rat Functional pEC50 = 5.4 5.4 - 1
Allosteric modulation at rat M1 receptor expressed in CHO cells by calcium mobilization assayAllosteric modulation at rat M1 receptor expressed in CHO cells by calcium mobilization assay
ChEMBL 493 7 2 7 3.9 Cc1cc(NC(=O)CS(=O)(=O)c2cn(Cc3cccc(-c4cn[nH]c4)c3F)c3ccccc23)no1 10.1016/j.bmcl.2010.12.015
1979 77355 None 47 Human Functional pEC50 = 5.4 5.4 -30 7
Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.
ChEMBL 169 1 0 3 0.6 CC(=O)OC1CN2CCC1CC2 10.1021/jm970125n
CHEMBL20835 77355 None 47 Human Functional pEC50 = 5.4 5.4 -30 7
Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.
ChEMBL 169 1 0 3 0.6 CC(=O)OC1CN2CCC1CC2 10.1021/jm970125n
118663155 3066 None 18 Human Functional pEC50 = 6.4 6.4 - 1
Positive allosteric modulation of muscarinic M1 receptor (unknown origin) expressed in CHO cells assessed as increase in Ach-induced accumulation of inositol phosphate accumulation measured after 30 mins by HTRF assayPositive allosteric modulation of muscarinic M1 receptor (unknown origin) expressed in CHO cells assessed as increase in Ach-induced accumulation of inositol phosphate accumulation measured after 30 mins by HTRF assay
ChEMBL 409 5 2 6 3.0 O[C@H]1COCC[C@@H]1NC(=O)c1ncc(c(c1)Cc1ccc(cc1)c1cscn1)C 10.1021/acs.jmedchem.6b00544
9228 3066 None 18 Human Functional pEC50 = 6.4 6.4 - 1
Positive allosteric modulation of muscarinic M1 receptor (unknown origin) expressed in CHO cells assessed as increase in Ach-induced accumulation of inositol phosphate accumulation measured after 30 mins by HTRF assayPositive allosteric modulation of muscarinic M1 receptor (unknown origin) expressed in CHO cells assessed as increase in Ach-induced accumulation of inositol phosphate accumulation measured after 30 mins by HTRF assay
ChEMBL 409 5 2 6 3.0 O[C@H]1COCC[C@@H]1NC(=O)c1ncc(c(c1)Cc1ccc(cc1)c1cscn1)C 10.1021/acs.jmedchem.6b00544
CHEMBL4097569 3066 None 18 Human Functional pEC50 = 6.4 6.4 - 1
Positive allosteric modulation of muscarinic M1 receptor (unknown origin) expressed in CHO cells assessed as increase in Ach-induced accumulation of inositol phosphate accumulation measured after 30 mins by HTRF assayPositive allosteric modulation of muscarinic M1 receptor (unknown origin) expressed in CHO cells assessed as increase in Ach-induced accumulation of inositol phosphate accumulation measured after 30 mins by HTRF assay
ChEMBL 409 5 2 6 3.0 O[C@H]1COCC[C@@H]1NC(=O)c1ncc(c(c1)Cc1ccc(cc1)c1cscn1)C 10.1021/acs.jmedchem.6b00544
5378491 164360 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Positive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assayPositive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 297 2 1 4 3.2 O=[N+]([O-])c1ccc2c(c1)C(c1ccccc1)=NCC(=S)N2 10.1016/j.bmcl.2017.11.008
CHEMBL4211633 164360 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Positive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assayPositive allosteric modulation of human wild type M1 receptor assessed as increase in acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 297 2 1 4 3.2 O=[N+]([O-])c1ccc2c(c1)C(c1ccccc1)=NCC(=S)N2 10.1016/j.bmcl.2017.11.008
289 242 None 13 Human Functional pEC50 = 6.4 6.4 - 1
Partial agonist activity at EGFP-fused human M1 receptor N-terminal truncated at 17 residues expressed in HEK293 cells assessed as induction of calcium response by fluorescence assayPartial agonist activity at EGFP-fused human M1 receptor N-terminal truncated at 17 residues expressed in HEK293 cells assessed as induction of calcium response by fluorescence assay
ChEMBL 301 8 0 2 4.9 CCCCC1CCN(CC1)CCCC(=O)c1ccccc1C 10.1021/jm201348t
9948320 242 None 13 Human Functional pEC50 = 6.4 6.4 - 1
Partial agonist activity at EGFP-fused human M1 receptor N-terminal truncated at 17 residues expressed in HEK293 cells assessed as induction of calcium response by fluorescence assayPartial agonist activity at EGFP-fused human M1 receptor N-terminal truncated at 17 residues expressed in HEK293 cells assessed as induction of calcium response by fluorescence assay
ChEMBL 301 8 0 2 4.9 CCCCC1CCN(CC1)CCCC(=O)c1ccccc1C 10.1021/jm201348t
CHEMBL1242950 242 None 13 Human Functional pEC50 = 6.4 6.4 - 1
Partial agonist activity at EGFP-fused human M1 receptor N-terminal truncated at 17 residues expressed in HEK293 cells assessed as induction of calcium response by fluorescence assayPartial agonist activity at EGFP-fused human M1 receptor N-terminal truncated at 17 residues expressed in HEK293 cells assessed as induction of calcium response by fluorescence assay
ChEMBL 301 8 0 2 4.9 CCCCC1CCN(CC1)CCCC(=O)c1ccccc1C 10.1021/jm201348t
127039039 137109 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Positive allosteric modulation of human M1 receptor expressed in CHO cells assessed as acetylcholine-induced calcium mobilization by FLIPR assayPositive allosteric modulation of human M1 receptor expressed in CHO cells assessed as acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 415 5 2 6 3.3 O=C(N[C@H]1CCCC[C@@H]1O)c1nn(Cc2ccc(-n3cccn3)cc2)c2ccccc12 10.1016/j.bmcl.2015.11.053
CHEMBL3746322 137109 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Positive allosteric modulation of human M1 receptor expressed in CHO cells assessed as acetylcholine-induced calcium mobilization by FLIPR assayPositive allosteric modulation of human M1 receptor expressed in CHO cells assessed as acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 415 5 2 6 3.3 O=C(N[C@H]1CCCC[C@@H]1O)c1nn(Cc2ccc(-n3cccn3)cc2)c2ccccc12 10.1016/j.bmcl.2015.11.053
44206959 16738 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 359 6 1 4 2.0 CC(C)C(=O)NC1CCN(CCCN2C(=O)COc3ccccc32)CC1 10.1021/jm100697g
CHEMBL1243233 16738 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assayAgonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
ChEMBL 359 6 1 4 2.0 CC(C)C(=O)NC1CCN(CCCN2C(=O)COc3ccccc32)CC1 10.1021/jm100697g
44303294 203613 None 0 Human Functional pEC50 = 7.3 7.3 3 3
Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.
ChEMBL 377 3 0 5 3.3 Fc1cc(Cl)cc(C#CCSc2nsnc2C23CN4CC2C3C4)c1 10.1021/jm9910019
CHEMBL60331 203613 None 0 Human Functional pEC50 = 7.3 7.3 3 3
Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.
ChEMBL 377 3 0 5 3.3 Fc1cc(Cl)cc(C#CCSc2nsnc2C23CN4CC2C3C4)c1 10.1021/jm9910019
2551 794 None 13 Human Functional pEC50 = 5.3 5.3 -27 13
Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9910019
2551.0 794 None 13 Human Functional pEC50 = 5.3 5.3 -27 13
Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9910019
298 794 None 13 Human Functional pEC50 = 5.3 5.3 -27 13
Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9910019
488 794 None 13 Human Functional pEC50 = 5.3 5.3 -27 13
Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9910019
CHEMBL965 794 None 13 Human Functional pEC50 = 5.3 5.3 -27 13
Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9910019
DB00411 794 None 13 Human Functional pEC50 = 5.3 5.3 -27 13
Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1021/jm9910019
76324306 103322 None 0 Human Functional pEC50 = 7.3 7.3 61 2
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
ChEMBL 379 6 2 4 2.5 CCOC(=O)N1C[C@@H]2CC[C@H](C1)[C@@H]2NCCNC(=O)c1cccc(Cl)c1 10.1016/j.bmcl.2012.03.088
CHEMBL3084449 103322 None 0 Human Functional pEC50 = 7.3 7.3 61 2
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
ChEMBL 379 6 2 4 2.5 CCOC(=O)N1C[C@@H]2CC[C@H](C1)[C@@H]2NCCNC(=O)c1cccc(Cl)c1 10.1016/j.bmcl.2012.03.088
122186857 123038 None 0 Human Functional pEC50 = 7.3 7.3 1 2
Positive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as basal and acetylcholine-stimulated Ca2+ level by FLIPR assayPositive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as basal and acetylcholine-stimulated Ca2+ level by FLIPR assay
ChEMBL 463 5 2 7 2.9 Cn1cc(-c2ccc(Cn3cc(C(=O)N[C@H]4CCOC[C@@]4(C)O)c4ncccc43)c(F)c2)cn1 10.1021/acsmedchemlett.5b00185
CHEMBL3608416 123038 None 0 Human Functional pEC50 = 7.3 7.3 1 2
Positive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as basal and acetylcholine-stimulated Ca2+ level by FLIPR assayPositive allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as basal and acetylcholine-stimulated Ca2+ level by FLIPR assay
ChEMBL 463 5 2 7 2.9 Cn1cc(-c2ccc(Cn3cc(C(=O)N[C@H]4CCOC[C@@]4(C)O)c4ncccc43)c(F)c2)cn1 10.1021/acsmedchemlett.5b00185
70689860 74333 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
ChEMBL 377 6 2 4 2.6 CCOC(=O)N1[C@H]2CC[C@@H]1CC(NCCNC(=O)c1ccc(C)c(F)c1)C2 10.1016/j.bmcl.2012.03.088
CHEMBL2024324 74333 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at human muscarinic M1 receptorAgonist activity at human muscarinic M1 receptor
ChEMBL 377 6 2 4 2.6 CCOC(=O)N1[C@H]2CC[C@@H]1CC(NCCNC(=O)c1ccc(C)c(F)c1)C2 10.1016/j.bmcl.2012.03.088
137284323 184959 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Agonist activity at muscarinic M1 receptor (unknown origin) expressed in CHO cellsAgonist activity at muscarinic M1 receptor (unknown origin) expressed in CHO cells
ChEMBL 341 1 1 3 4.9 CN1CC=C(C2=Nc3cc(Cl)ccc3Nc3ccc(F)cc32)CC1 10.1016/j.bmcl.2021.127911
CHEMBL4852403 184959 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Agonist activity at muscarinic M1 receptor (unknown origin) expressed in CHO cellsAgonist activity at muscarinic M1 receptor (unknown origin) expressed in CHO cells
ChEMBL 341 1 1 3 4.9 CN1CC=C(C2=Nc3cc(Cl)ccc3Nc3ccc(F)cc32)CC1 10.1016/j.bmcl.2021.127911
9990434 106395 None 0 Human Functional pEC50 = 5.3 5.3 -1 3
Effective concentration for HMPA (human muscarinic inositol phosphate accumulation) activity measured in CHO cells expressing Muscarinic acetylcholine receptor M1Effective concentration for HMPA (human muscarinic inositol phosphate accumulation) activity measured in CHO cells expressing Muscarinic acetylcholine receptor M1
ChEMBL 202 2 0 3 0.7 C#CCC#CCO/N=C1\CN2CCC1C2 10.1016/S0960-894X(00)80538-7
CHEMBL313918 106395 None 0 Human Functional pEC50 = 5.3 5.3 -1 3
Effective concentration for HMPA (human muscarinic inositol phosphate accumulation) activity measured in CHO cells expressing Muscarinic acetylcholine receptor M1Effective concentration for HMPA (human muscarinic inositol phosphate accumulation) activity measured in CHO cells expressing Muscarinic acetylcholine receptor M1
ChEMBL 202 2 0 3 0.7 C#CCC#CCO/N=C1\CN2CCC1C2 10.1016/S0960-894X(00)80538-7
117680178 141023 None 0 Rat Functional pEC50 = 5.3 5.3 - 1
Positive allosteric modulation at rat muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation at rat muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 402 3 0 5 4.3 Cn1cc2c(-c3cc(F)c(Cn4cnc5ccccc5c4=O)c(F)c3)cccc2n1 10.1016/j.bmcl.2016.04.083
CHEMBL3822763 141023 None 0 Rat Functional pEC50 = 5.3 5.3 - 1
Positive allosteric modulation at rat muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation at rat muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 402 3 0 5 4.3 Cn1cc2c(-c3cc(F)c(Cn4cnc5ccccc5c4=O)c(F)c3)cccc2n1 10.1016/j.bmcl.2016.04.083
86298473 141112 None 0 Rat Functional pEC50 = 5.3 5.3 -2 2
Positive allosteric modulation at rat muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation at rat muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 403 3 0 6 3.7 Cn1cc2c(-c3cc(F)c(Cn4cnc5cnccc5c4=O)c(F)c3)cccc2n1 10.1016/j.bmcl.2016.04.083
CHEMBL3823885 141112 None 0 Rat Functional pEC50 = 5.3 5.3 -2 2
Positive allosteric modulation at rat muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation at rat muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 403 3 0 6 3.7 Cn1cc2c(-c3cc(F)c(Cn4cnc5cnccc5c4=O)c(F)c3)cccc2n1 10.1016/j.bmcl.2016.04.083
9154093 48592 None 9 Human Functional pEC50 = 6.3 6.3 - 1
Positive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assay
ChEMBL 393 4 0 4 5.0 Cc1ccc(C)c(Cn2nc3c4ccccc4n(Cc4ccccc4)cc-3c2=O)c1 10.1016/j.bmcl.2014.11.011
CHEMBL1556989 48592 None 9 Human Functional pEC50 = 6.3 6.3 - 1
Positive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assayPositive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assay
ChEMBL 393 4 0 4 5.0 Cc1ccc(C)c(Cn2nc3c4ccccc4n(Cc4ccccc4)cc-3c2=O)c1 10.1016/j.bmcl.2014.11.011
117937665 137086 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Positive allosteric modulation of human M1 receptor expressed in CHO cells assessed as acetylcholine-induced calcium mobilization by FLIPR assayPositive allosteric modulation of human M1 receptor expressed in CHO cells assessed as acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 374 4 2 5 3.0 N#Cc1ccc(Cn2cc(C(=O)N[C@H]3CCCC[C@@H]3O)c3ncccc32)cc1 10.1016/j.bmcl.2015.11.053
CHEMBL3745995 137086 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Positive allosteric modulation of human M1 receptor expressed in CHO cells assessed as acetylcholine-induced calcium mobilization by FLIPR assayPositive allosteric modulation of human M1 receptor expressed in CHO cells assessed as acetylcholine-induced calcium mobilization by FLIPR assay
ChEMBL 374 4 2 5 3.0 N#Cc1ccc(Cn2cc(C(=O)N[C@H]3CCCC[C@@H]3O)c3ncccc32)cc1 10.1016/j.bmcl.2015.11.053
145960766 161723 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 432 5 2 6 3.1 O=C(N[C@H]1CCCC[C@@H]1O)C1CN(Cc2ccc(-n3cccc3)nc2)c2ccccc2O1 10.1016/j.bmcl.2018.05.009
CHEMBL4130009 161723 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilizationPositive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
ChEMBL 432 5 2 6 3.1 O=C(N[C@H]1CCCC[C@@H]1