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Assay Detail

CHEMBL998548

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Functional
Antagonist activity at human recombinant muscarinic M1 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced intracellular Ca2+ mobilization by FLIPR assay
ChEMBL ↗
54
Total Activities
54
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Muscarinic acetylcholine receptor M1 (CHEMBL216) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Muscarinic acetylcholine receptor antagonists: SAR and optimization of tyrosine ureas.
Jin J, Wang Y, Shi D, Wang F, Fu W, Davis RS, Jin Q, Foley JJ, Sarau HM, Morrow DM, Moore ML, Rivero RA, Palovich M, Salmon M, Belmonte KE, Busch-Petersen J.
Bioorg Med Chem Lett (2008) 18 : 5481 -5486
PubMed 18818072 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 45 6.54 8.00
Kd 9 7.44 8.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL553448 — — 1 8.60
CHEMBL554918 — — 1 8.00
CHEMBL495102 — — 1 7.90
CHEMBL540359 — — 1 7.80
CHEMBL540145 — — 1 7.80
CHEMBL540400 — — 1 7.60
CHEMBL540148 — — 1 7.50
CHEMBL466271 — — 1 7.50
CHEMBL540398 — — 1 7.40
CHEMBL555019 — — 1 7.40
CHEMBL550885 — — 1 7.40
CHEMBL555707 — — 1 7.30
CHEMBL555706 — — 1 7.10
CHEMBL538360 — — 1 7.10
CHEMBL539885 — — 1 7.10
CHEMBL555474 — — 1 7.00
CHEMBL554632 — — 1 7.00
CHEMBL527216 — — 1 7.00
CHEMBL540401 — — 1 6.90
CHEMBL540399 — — 1 6.80
CHEMBL540146 — — 1 6.80
CHEMBL540144 — — 1 6.70
CHEMBL553433 — — 1 6.60
CHEMBL521244 — — 1 6.60
CHEMBL555471 — — 1 6.60
CHEMBL480299 — — 1 6.30
CHEMBL471214 — — 1 6.20
CHEMBL551113 — — 1 6.20
CHEMBL518001 — — 1 6.10
CHEMBL479526 — — 1 6.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL553448 — Kd = 2.512 nM 8.60
CHEMBL554918 — IC50 = 10.0 nM 8.00
CHEMBL495102 — IC50 = 12.59 nM 7.90
CHEMBL540359 — Kd = 15.85 nM 7.80
CHEMBL540145 — Kd = 15.85 nM 7.80
CHEMBL540400 — IC50 = 25.12 nM 7.60
CHEMBL540148 — Kd = 31.62 nM 7.50
CHEMBL466271 — IC50 = 31.62 nM 7.50
CHEMBL540398 — IC50 = 39.81 nM 7.40
CHEMBL550885 — Kd = 39.81 nM 7.40
CHEMBL555019 — IC50 = 39.81 nM 7.40
CHEMBL555707 — IC50 = 50.12 nM 7.30
CHEMBL539885 — IC50 = 79.43 nM 7.10
CHEMBL538360 — Kd = 79.43 nM 7.10
CHEMBL555706 — Kd = 79.43 nM 7.10
CHEMBL555474 — IC50 = 100.0 nM 7.00
CHEMBL527216 — IC50 = 100.0 nM 7.00
CHEMBL554632 — IC50 = 100.0 nM 7.00
CHEMBL540401 — Kd = 125.89 nM 6.90
CHEMBL540399 — IC50 = 158.49 nM 6.80
CHEMBL540146 — Kd = 158.49 nM 6.80
CHEMBL540144 — IC50 = 199.53 nM 6.70
CHEMBL553433 — IC50 = 251.19 nM 6.60
CHEMBL521244 — IC50 = 251.19 nM 6.60
CHEMBL555471 — IC50 = 251.19 nM 6.60
CHEMBL480299 — IC50 = 501.19 nM 6.30
CHEMBL551113 — IC50 = 630.96 nM 6.20
CHEMBL471214 — IC50 = 630.96 nM 6.20
CHEMBL518001 — IC50 = 794.33 nM 6.10
CHEMBL479526 — IC50 = 1000.0 nM 6.00
CHEMBL486982 — IC50 = 1000.0 nM 6.00
CHEMBL486983 — IC50 = 1000.0 nM 6.00
CHEMBL451043 — IC50 = 1000.0 nM 6.00
CHEMBL526009 — IC50 = 1000.0 nM 6.00
CHEMBL519760 — IC50 = 1000.0 nM 6.00
CHEMBL501419 — IC50 = 1000.0 nM 6.00
CHEMBL480877 — IC50 = 1258.93 nM 5.90
CHEMBL553431 — IC50 = 1258.93 nM 5.90
CHEMBL553446 — IC50 = 1995.26 nM 5.70
CHEMBL480878 — IC50 = 1995.26 nM 5.70
CHEMBL505452 — IC50 = 1995.26 nM 5.70
CHEMBL517087 — IC50 = 2511.89 nM 5.60
CHEMBL507581 — IC50 > 3162.28 nM -
CHEMBL450093 — IC50 > 3162.28 nM -
CHEMBL513228 — IC50 > 3162.28 nM -
CHEMBL508556 — IC50 > 3162.28 nM -
CHEMBL443925 — IC50 > 3162.28 nM -
CHEMBL448904 — IC50 > 3162.28 nM -
CHEMBL458105 — IC50 > 3162.28 nM -
CHEMBL451040 — IC50 > 3162.28 nM -