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Assay Detail

CHEMBL4018361

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Functional
Agonist activity at human OTR expressed in CHO cells assessed as calcium mobilization measured after 30 mins by Fluo-4-AM dye based FLIPR assay
ChEMBL ↗
68
Total Activities
68
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Oxytocin receptor (CHEMBL2049) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Potent and selective oxytocin receptor agonists without disulfide bridges.
Adachi Y, Sakimura K, Shimizu Y, Nakayama M, Terao Y, Yano T, Asami T.
Bioorg Med Chem Lett (2017) 27 : 2331 -2335
PubMed 28438540 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 68 9.50 11.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4102192 — — 1 11.00
CHEMBL4095930 — — 1 10.89
CHEMBL4093931 — — 1 10.89
CHEMBL3277916 — — 1 10.89
CHEMBL4084223 — — 1 10.85
CHEMBL4078856 — — 1 10.82
CHEMBL4096848 — — 1 10.68
CHEMBL4065273 — — 1 10.57
CHEMBL4101771 — — 1 10.57
CHEMBL4094454 — — 1 10.52
CHEMBL4092971 — — 1 10.51
CHEMBL4080341 — — 1 10.38
CHEMBL4084795 — — 1 10.27
CHEMBL4063150 — — 1 10.25
CHEMBL3277915 — — 1 10.15
CHEMBL4101586 — — 1 10.14
CHEMBL4065416 — — 1 10.09
CHEMBL4066923 — — 1 9.96
CHEMBL4070577 — — 1 9.96
CHEMBL4093088 — — 1 9.92
CHEMBL4103942 — — 1 9.92
CHEMBL4075102 — — 1 9.92
CHEMBL4096331 — — 1 9.92
CHEMBL4092407 — — 1 9.72
CHEMBL4083700 — — 1 9.72
CHEMBL4100627 — — 1 9.62
CHEMBL4073891 — — 1 9.60
CHEMBL4072207 — — 1 9.59
CHEMBL4092242 — — 1 9.46
CHEMBL4099102 — — 1 9.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4102192 — EC50 = 0.01 nM 11.00
CHEMBL4095930 — EC50 = 0.013 nM 10.89
CHEMBL3277916 — EC50 = 0.013 nM 10.89
CHEMBL4093931 — EC50 = 0.013 nM 10.89
CHEMBL4084223 — EC50 = 0.014 nM 10.85
CHEMBL4078856 — EC50 = 0.015 nM 10.82
CHEMBL4096848 — EC50 = 0.021 nM 10.68
CHEMBL4065273 — EC50 = 0.027 nM 10.57
CHEMBL4101771 — EC50 = 0.027 nM 10.57
CHEMBL4094454 — EC50 = 0.03 nM 10.52
CHEMBL4092971 — EC50 = 0.031 nM 10.51
CHEMBL4080341 — EC50 = 0.042 nM 10.38
CHEMBL4084795 — EC50 = 0.054 nM 10.27
CHEMBL4063150 — EC50 = 0.056 nM 10.25
CHEMBL3277915 — EC50 = 0.07 nM 10.15
CHEMBL4101586 — EC50 = 0.072 nM 10.14
CHEMBL4065416 — EC50 = 0.082 nM 10.09
CHEMBL4066923 — EC50 = 0.11 nM 9.96
CHEMBL4070577 — EC50 = 0.11 nM 9.96
CHEMBL4093088 — EC50 = 0.12 nM 9.92
CHEMBL4103942 — EC50 = 0.12 nM 9.92
CHEMBL4075102 — EC50 = 0.12 nM 9.92
CHEMBL4096331 — EC50 = 0.12 nM 9.92
CHEMBL4092407 — EC50 = 0.19 nM 9.72
CHEMBL4083700 — EC50 = 0.19 nM 9.72
CHEMBL4100627 — EC50 = 0.24 nM 9.62
CHEMBL4073891 — EC50 = 0.25 nM 9.60
CHEMBL4072207 — EC50 = 0.26 nM 9.59
CHEMBL4092242 — EC50 = 0.35 nM 9.46
CHEMBL4099102 — EC50 = 0.53 nM 9.28
CHEMBL4094019 — EC50 = 0.78 nM 9.11
CHEMBL4063521 — EC50 = 1.2 nM 8.92
CHEMBL4086714 — EC50 = 1.4 nM 8.85
CHEMBL4070617 — EC50 = 1.5 nM 8.82
CHEMBL4083280 — EC50 = 1.6 nM 8.80
CHEMBL4061446 — EC50 = 1.6 nM 8.80
CHEMBL4074033 — EC50 = 3.4 nM 8.47
CHEMBL4102595 — EC50 = 3.6 nM 8.44
CHEMBL4061946 — EC50 = 4.4 nM 8.36
CHEMBL4085152 — EC50 = 5.1 nM 8.29
CHEMBL4094014 — EC50 = 9.5 nM 8.02
CHEMBL4103260 — EC50 = 12.0 nM 7.92
CHEMBL3246917 — EC50 = 13.0 nM 7.89
CHEMBL4104022 — EC50 = 17.0 nM 7.77
CHEMBL4074898 — EC50 = 22.0 nM 7.66
CHEMBL4091483 — EC50 = 40.0 nM 7.40
CHEMBL4075079 — EC50 = 89.0 nM 7.05
CHEMBL4073298 — EC50 > 100.0 nM -
CHEMBL4100142 — EC50 > 100.0 nM -
CHEMBL4074974 — EC50 = 0.0055 nM -