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Assay Detail

CHEMBL863357

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Displacement of [125I]LVA antagonist from human vasopressin 1a receptor expressed in HEK293-EBNA cells
ChEMBL ↗
63
Total Activities
63
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

Vasopressin V1a receptor (CHEMBL1889) ↗
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 63 6.23 9.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL382301 ATOSIBAN 4.0 1 9.20
CHEMBL445816 — — 1 7.38
CHEMBL2113201 — — 1 7.19
CHEMBL200682 — — 1 7.16
CHEMBL2113181 — — 1 7.03
CHEMBL373167 — — 1 6.94
CHEMBL2113185 — — 1 6.88
CHEMBL2113203 — — 1 6.75
CHEMBL114302 — — 1 6.52
CHEMBL381433 — — 1 6.49
CHEMBL2113215 — — 1 6.36
CHEMBL2113198 — — 1 6.33
CHEMBL2113204 — — 1 6.29
CHEMBL2113208 — — 1 6.29
CHEMBL198622 — — 1 6.24
CHEMBL2113177 — — 1 6.24
CHEMBL196816 — — 1 6.22
CHEMBL371223 — — 1 6.22
CHEMBL2113179 — — 1 6.21
CHEMBL2113200 — — 1 6.21
CHEMBL2113207 — — 1 6.21
CHEMBL372122 — — 1 6.19
CHEMBL2113189 — — 1 6.14
CHEMBL2113196 — — 1 5.96
CHEMBL2113211 — — 1 5.93
CHEMBL2113195 — — 1 5.89
CHEMBL2113209 — — 1 5.86
CHEMBL1254117 — — 1 5.85
CHEMBL197378 — — 1 5.80
CHEMBL383149 — — 1 5.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL382301 ATOSIBAN Ki = 0.63 nM 9.20
CHEMBL445816 — Ki = 42.0 nM 7.38
CHEMBL2113201 — Ki = 65.0 nM 7.19
CHEMBL200682 — Ki = 70.0 nM 7.16
CHEMBL2113181 — Ki = 94.0 nM 7.03
CHEMBL373167 — Ki = 115.0 nM 6.94
CHEMBL2113185 — Ki = 133.0 nM 6.88
CHEMBL2113203 — Ki = 176.0 nM 6.75
CHEMBL114302 — Ki = 300.0 nM 6.52
CHEMBL381433 — Ki = 325.0 nM 6.49
CHEMBL2113215 — Ki = 437.0 nM 6.36
CHEMBL2113198 — Ki = 471.0 nM 6.33
CHEMBL2113204 — Ki = 510.0 nM 6.29
CHEMBL2113208 — Ki = 511.0 nM 6.29
CHEMBL2113177 — Ki = 582.0 nM 6.24
CHEMBL198622 — Ki = 570.0 nM 6.24
CHEMBL196816 — Ki = 600.0 nM 6.22
CHEMBL371223 — Ki = 596.0 nM 6.22
CHEMBL2113179 — Ki = 615.0 nM 6.21
CHEMBL2113200 — Ki = 618.0 nM 6.21
CHEMBL2113207 — Ki = 611.0 nM 6.21
CHEMBL372122 — Ki = 650.0 nM 6.19
CHEMBL2113189 — Ki = 730.0 nM 6.14
CHEMBL2113196 — Ki = 1103.0 nM 5.96
CHEMBL2113211 — Ki = 1180.0 nM 5.93
CHEMBL2113195 — Ki = 1286.0 nM 5.89
CHEMBL2113209 — Ki = 1390.0 nM 5.86
CHEMBL1254117 — Ki = 1410.0 nM 5.85
CHEMBL197378 — Ki = 1600.0 nM 5.80
CHEMBL383149 — Ki = 1600.0 nM 5.80
CHEMBL427190 — Ki = 1800.0 nM 5.75
CHEMBL200368 — Ki = 1860.0 nM 5.73
CHEMBL2113212 — Ki = 2120.0 nM 5.67
CHEMBL200329 — Ki = 3215.0 nM 5.49
CHEMBL2113202 — Ki = 3610.0 nM 5.44
CHEMBL2113216 — Ki = 3730.0 nM 5.43
CHEMBL2113210 — Ki = 3980.0 nM 5.40
CHEMBL2113213 — Ki = 4940.0 nM 5.31
CHEMBL2113205 — Ki = 6880.0 nM 5.16
CHEMBL444879 — Ki > 10000.0 nM -
CHEMBL200498 — Ki > 10000.0 nM -
CHEMBL2113197 — Ki > 10000.0 nM -
CHEMBL2113194 — Ki > 10000.0 nM -
CHEMBL382515 — Ki > 10000.0 nM -
CHEMBL200738 — Ki > 10000.0 nM -
CHEMBL198430 — Ki > 10000.0 nM -
CHEMBL196974 — Ki > 10000.0 nM -
CHEMBL200415 — Ki > 10000.0 nM -
CHEMBL200904 — Ki > 10000.0 nM -
CHEMBL198630 — Ki > 10000.0 nM -