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Assay Detail

CHEMBL1786272

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Functional
Antagonist activity against human M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR
ChEMBL ↗
60
Total Activities
41
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 M3 (CHEMBL245) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis, and structure-activity relationship of tropane muscarinic acetylcholine receptor antagonists.
Lainé DI, Wan Z, Yan H, Zhu C, Xie H, Fu W, Busch-Petersen J, Neipp C, Davis R, Widdowson KL, Blaney FE, Foley J, Bacon AM, Webb EF, Luttmann MA, Burman M, Sarau HM, Salmon M, Palovich MR, Belmonte K.
J Med Chem (2009) 52 : 5241 -5252
PubMed 19630384 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 42 6.76 8.00
Kd 18 9.06 10.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2103803 — — 2 10.70
CHEMBL3084414 — — 2 10.00
CHEMBL3084413 — — 2 10.00
CHEMBL3084419 — — 2 10.00
CHEMBL3084409 — — 2 9.90
CHEMBL3084650 — — 2 9.50
CHEMBL3084658 — — 2 9.30
CHEMBL3084418 — — 2 9.00
CHEMBL3084417 — — 2 8.80
CHEMBL3084415 — — 2 8.70
CHEMBL3084396 — — 2 8.60
CHEMBL3084410 — — 2 8.60
CHEMBL3084662 — — 3 8.60
CHEMBL3084679 — — 2 8.40
CHEMBL3084643 — — 2 8.40
CHEMBL3084399 — — 2 8.30
CHEMBL3084398 — — 2 8.30
CHEMBL3084401 — — 2 8.00
CHEMBL3084411 — — 1 7.77
CHEMBL3084395 — — 1 7.72
CHEMBL3084416 — — 1 7.64
CHEMBL3084402 — — 1 7.60
CHEMBL3084406 — — 1 7.43
CHEMBL3084412 — — 1 7.19
CHEMBL3084405 — — 1 7.19
CHEMBL3084404 — — 1 7.13
CHEMBL3084407 — — 1 6.95
CHEMBL3084394 — — 1 6.87
CHEMBL3084397 — — 1 6.87
CHEMBL3084639 — — 1 6.69

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2103803 — Kd = 0.01995 nM 10.70
CHEMBL3084413 — Kd = 0.1 nM 10.00
CHEMBL3084419 — Kd = 0.1 nM 10.00
CHEMBL3084414 — Kd = 0.1 nM 10.00
CHEMBL3084409 — Kd = 0.1259 nM 9.90
CHEMBL3084650 — Kd = 0.3162 nM 9.50
CHEMBL3084658 — Kd = 0.5012 nM 9.30
CHEMBL3084418 — Kd = 1.0 nM 9.00
CHEMBL3084417 — Kd = 1.585 nM 8.80
CHEMBL3084415 — Kd = 1.995 nM 8.70
CHEMBL3084396 — Kd = 2.512 nM 8.60
CHEMBL3084410 — Kd = 2.512 nM 8.60
CHEMBL3084662 — Kd = 2.512 nM 8.60
CHEMBL3084679 — Kd = 3.981 nM 8.40
CHEMBL3084643 — Kd = 3.981 nM 8.40
CHEMBL3084398 — Kd = 5.012 nM 8.30
CHEMBL3084399 — Kd = 5.012 nM 8.30
CHEMBL3084401 — Kd = 10.0 nM 8.00
CHEMBL3084399 — IC50 = 10.0 nM 8.00
CHEMBL3084401 — IC50 = 11.0 nM 7.96
CHEMBL3084411 — IC50 = 17.0 nM 7.77
CHEMBL3084395 — IC50 = 19.0 nM 7.72
CHEMBL3084416 — IC50 = 23.0 nM 7.64
CHEMBL3084402 — IC50 = 25.0 nM 7.60
CHEMBL3084406 — IC50 = 37.0 nM 7.43
CHEMBL3084405 — IC50 = 65.0 nM 7.19
CHEMBL3084412 — IC50 = 65.0 nM 7.19
CHEMBL3084404 — IC50 = 74.0 nM 7.13
CHEMBL3084407 — IC50 = 112.0 nM 6.95
CHEMBL3084397 — IC50 = 135.0 nM 6.87
CHEMBL3084394 — IC50 = 134.0 nM 6.87
CHEMBL3084639 — IC50 = 206.0 nM 6.69
CHEMBL3084408 — IC50 = 290.0 nM 6.54
CHEMBL3084678 — IC50 = 687.0 nM 6.16
CHEMBL2308786 — IC50 = 839.0 nM 6.08
CHEMBL3084662 — IC50 = 973.0 nM 6.01
CHEMBL2306159 — IC50 = 1059.0 nM 5.97
CHEMBL2307674 — IC50 = 1338.0 nM 5.87
CHEMBL3084393 — IC50 = 1498.0 nM 5.82
CHEMBL3084663 — IC50 = 1939.0 nM 5.71
CHEMBL3084670 — IC50 = 2732.0 nM 5.56
CHEMBL3084674 — IC50 = 2895.0 nM 5.54
CHEMBL3084417 — IC50 < 10.0 nM -
CHEMBL3084662 — IC50 < 10.0 nM -
CHEMBL3084396 — IC50 < 10.0 nM -
CHEMBL3084658 — IC50 < 10.0 nM -
CHEMBL3084398 — IC50 < 10.0 nM -
CHEMBL3084400 — IC50 > 10000.0 nM -
CHEMBL3084403 — IC50 > 10000.0 nM -
CHEMBL3084410 — IC50 < 10.0 nM -