Ki Summary

Reaction Details

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Target

Muscarinic acetylcholine receptor M1

Ligand

BDBM50228399

Substrate/Competitor

n/a

Meas. Tech.

ChEMBL_452481 (CHEMBL902718)

IC50

1129±n/a nM

Citation

Eckhardt, M; Langkopf, E; Mark, M; Tadayyon, M; Thomas, L; Nar, H; Pfrengle, W; Guth, B; Lotz, R; Sieger, P; Fuchs, H; Himmelsbach, F 8-(3-(R)-aminopiperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydropurine-2,6-dione (BI 1356), a highly potent, selective, long-acting, and orally bioavailable DPP-4 inhibitor for the treatment of type 2 diabetes. J Med Chem50:6450-3 (2007) [PubMed] Article

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Muscarinic acetylcholine receptor M1

Name:

Muscarinic acetylcholine receptor M1

Synonyms:

ACM1_HUMAN | CHRM1 | Cholinergic receptor, muscarinic 1 | Cholinergic, muscarinic M1

Type:

Protein

Mol. Mass.:

51442.54

Organism:

Homo sapiens (Human)

Description:

P11229

Residue:

460

Sequence:

MNTSAPPAVSPNITVLAPGKGPWQVAFIGITTGLLSLATVTGNLLVLISFKVNTELKTVN
NYFLLSLACADLIIGTFSMNLYTTYLLMGHWALGTLACDLWLALDYVASNASVMNLLLIS
FDRYFSVTRPLSYRAKRTPRRAALMIGLAWLVSFVLWAPAILFWQYLVGERTVLAGQCYI
QFLSQPIITFGTAMAAFYLPVTVMCTLYWRIYRETENRARELAALQGSETPGKGGGSSSS
SERSQPGAEGSPETPPGRCCRCCRAPRLLQAYSWKEEEEEDEGSMESLTSSEGEEPGSEV
VIKMPMVDPEAQAPTKQPPRSSPNTVKRPTKKGRDRAGKGQKPRGKEQLAKRKTFSLVKE
KKAARTLSAILLAFILTWTPYNIMVLVSTFCKDCVPETLWELGYWLCYVNSTINPMCYAL
CNKAFRDTFRLLLLCRWDKRRWRKIPKRPGSVHRTPSRQC

BDBM50228399

n/a

Name

BDBM50228399

Synonyms:

8-((S)-3-amino-piperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(2-oxo-2-phenyl-ethyl)-3,7-dihydro-purine-2,6-dione | CHEMBL237288

Type

Small organic molecule

Emp. Form.

C23H26N6O3

Mol. Mass.

434.4909

SMILES

CC#CCn1c(nc2n(C)c(=O)n(CC(=O)c3ccccc3)c(=O)c12)N1CCC[C@H](N)C1

Structure