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Assay Detail

CHEMBL863355

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Binding
Displacement of [125I]OVTA antagonist from human oxytocin receptor expressed in HEK293-EBNA cells
ChEMBL ↗
67
Total Activities
67
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293-EBNA
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Discovery and development of a new class of potent, selective, orally active oxytocin receptor antagonists.
Quattropani A, Dorbais J, Covini D, Pittet PA, Colovray V, Thomas RJ, Coxhead R, Halazy S, Scheer A, Missotten M, Ayala G, Bradshaw C, De Raemy-Schenk AM, Nichols A, Cirillo R, Tos EG, Giachetti C, Golzio L, Marinelli P, Church DJ, Barberis C, Chollet A, Schwarz MK.
J Med Chem (2005) 48 : 7882 -7905
PubMed 16302826 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 67 7.27 9.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL445816 — — 1 9.19
CHEMBL2113181 — — 1 9.05
CHEMBL2113185 — — 1 9.05
CHEMBL2113201 — — 1 8.96
CHEMBL2113189 — — 1 8.80
CHEMBL2113203 — — 1 8.68
CHEMBL2113208 — — 1 8.52
CHEMBL2113198 — — 1 8.41
CHEMBL2113179 — — 1 8.39
CHEMBL2113211 — — 1 8.15
CHEMBL2113177 — — 1 8.15
CHEMBL2113207 — — 1 8.06
CHEMBL2113209 — — 1 8.00
CHEMBL1254117 — — 1 7.85
CHEMBL372122 — — 1 7.82
CHEMBL371223 — — 1 7.75
CHEMBL2113210 — — 1 7.75
CHEMBL2113215 — — 1 7.70
CHEMBL2113216 — — 1 7.68
CHEMBL382301 ATOSIBAN 4.0 1 7.57
CHEMBL2113212 — — 1 7.44
CHEMBL200403 — — 1 7.44
CHEMBL2113204 — — 1 7.43
CHEMBL200329 — — 1 7.22
CHEMBL2113213 — — 1 7.21
CHEMBL2113202 — — 1 7.19
CHEMBL115305 — — 1 7.17
CHEMBL200792 — — 1 7.17
CHEMBL1254116 — — 1 7.05
CHEMBL200415 — — 1 7.03

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL445816 — Ki = 0.65 nM 9.19
CHEMBL2113181 — Ki = 0.9 nM 9.05
CHEMBL2113185 — Ki = 0.9 nM 9.05
CHEMBL2113201 — Ki = 1.1 nM 8.96
CHEMBL2113189 — Ki = 1.6 nM 8.80
CHEMBL2113203 — Ki = 2.1 nM 8.68
CHEMBL2113208 — Ki = 3.0 nM 8.52
CHEMBL2113198 — Ki = 3.9 nM 8.41
CHEMBL2113179 — Ki = 4.1 nM 8.39
CHEMBL2113211 — Ki = 7.0 nM 8.15
CHEMBL2113177 — Ki = 7.0 nM 8.15
CHEMBL2113207 — Ki = 8.7 nM 8.06
CHEMBL2113209 — Ki = 10.0 nM 8.00
CHEMBL1254117 — Ki = 14.0 nM 7.85
CHEMBL372122 — Ki = 15.0 nM 7.82
CHEMBL371223 — Ki = 18.0 nM 7.75
CHEMBL2113210 — Ki = 18.0 nM 7.75
CHEMBL2113215 — Ki = 20.0 nM 7.70
CHEMBL2113216 — Ki = 21.0 nM 7.68
CHEMBL382301 ATOSIBAN Ki = 27.0 nM 7.57
CHEMBL2113212 — Ki = 36.0 nM 7.44
CHEMBL200403 — Ki = 36.0 nM 7.44
CHEMBL2113204 — Ki = 37.0 nM 7.43
CHEMBL200329 — Ki = 60.0 nM 7.22
CHEMBL2113213 — Ki = 61.0 nM 7.21
CHEMBL2113202 — Ki = 64.0 nM 7.19
CHEMBL200792 — Ki = 67.0 nM 7.17
CHEMBL115305 — Ki = 67.0 nM 7.17
CHEMBL1254116 — Ki = 90.0 nM 7.05
CHEMBL200415 — Ki = 93.0 nM 7.03
CHEMBL114302 — Ki = 100.0 nM 7.00
CHEMBL382515 — Ki = 104.0 nM 6.98
CHEMBL2113205 — Ki = 111.0 nM 6.96
CHEMBL2113195 — Ki = 109.0 nM 6.96
CHEMBL2113200 — Ki = 115.0 nM 6.94
CHEMBL373167 — Ki = 160.0 nM 6.80
CHEMBL196974 — Ki = 160.0 nM 6.80
CHEMBL2113206 — Ki = 174.0 nM 6.76
CHEMBL198630 — Ki = 237.0 nM 6.62
CHEMBL200729 — Ki = 239.0 nM 6.62
CHEMBL198622 — Ki = 320.0 nM 6.50
CHEMBL2113196 — Ki = 322.0 nM 6.49
CHEMBL2113194 — Ki = 448.0 nM 6.35
CHEMBL381433 — Ki = 470.0 nM 6.33
CHEMBL427190 — Ki = 500.0 nM 6.30
CHEMBL197378 — Ki = 510.0 nM 6.29
CHEMBL198780 — Ki = 620.0 nM 6.21
CHEMBL383149 — Ki = 770.0 nM 6.11
CHEMBL200682 — Ki = 800.0 nM 6.10
CHEMBL2113197 — Ki = 1376.0 nM 5.86