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Assay Detail

CHEMBL812860

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Binding
Inhibition of radioligand [3H]AVP binding to the vasopressin V1 receptor in rat liver tissue
ChEMBL ↗
163
Total Activities
159
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Vasopressin V1 receptor (CHEMBL2095221) ↗
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Nanomolar-affinity, non-peptide oxytocin receptor antagonists.
Evans BE, Lundell GF, Gilbert KF, Bock MG, Rittle KE, Carroll LA, Williams PD, Pawluczyk JM, Leighton JL, Young MB.
J Med Chem (1993) 36 : 3993 -4005
PubMed 8258821 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 163 5.75 7.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL337889 — — 1 7.17
CHEMBL130891 — — 1 6.96
CHEMBL339524 — — 1 6.92
CHEMBL433662 — — 1 6.80
CHEMBL127445 — — 1 6.54
CHEMBL436189 — — 1 6.51
CHEMBL339756 — — 1 6.50
CHEMBL341049 — — 1 6.43
CHEMBL128258 — — 1 6.39
CHEMBL341289 — — 3 6.38
CHEMBL132389 — — 1 6.37
CHEMBL339498 — — 1 6.36
CHEMBL131477 — — 1 6.36
CHEMBL338118 — — 1 6.33
CHEMBL335182 — — 1 6.32
CHEMBL130905 — — 1 6.31
CHEMBL128219 — — 1 6.31
CHEMBL340388 — — 1 6.30
CHEMBL339768 — — 1 6.30
CHEMBL128383 — — 1 6.30
CHEMBL128749 — — 1 6.28
CHEMBL335944 — — 1 6.28
CHEMBL338984 — — 1 6.28
CHEMBL132391 — — 1 6.19
CHEMBL337853 — — 1 6.17
CHEMBL338576 — — 1 6.16
CHEMBL128712 — — 1 6.15
CHEMBL339155 — — 1 6.15
CHEMBL405016 — — 1 6.11
CHEMBL128423 — — 1 6.08

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL337889 — IC50 = 67.0 nM 7.17
CHEMBL130891 — IC50 = 110.0 nM 6.96
CHEMBL339524 — IC50 = 120.0 nM 6.92
CHEMBL433662 — IC50 = 160.0 nM 6.80
CHEMBL127445 — IC50 = 290.0 nM 6.54
CHEMBL436189 — IC50 = 310.0 nM 6.51
CHEMBL339756 — IC50 = 320.0 nM 6.50
CHEMBL341049 — IC50 = 370.0 nM 6.43
CHEMBL128258 — IC50 = 410.0 nM 6.39
CHEMBL341289 — IC50 = 420.0 nM 6.38
CHEMBL132389 — IC50 = 430.0 nM 6.37
CHEMBL131477 — IC50 = 440.0 nM 6.36
CHEMBL339498 — IC50 = 440.0 nM 6.36
CHEMBL338118 — IC50 = 470.0 nM 6.33
CHEMBL335182 — IC50 = 480.0 nM 6.32
CHEMBL128219 — IC50 = 490.0 nM 6.31
CHEMBL130905 — IC50 = 490.0 nM 6.31
CHEMBL128383 — IC50 = 500.0 nM 6.30
CHEMBL340388 — IC50 = 500.0 nM 6.30
CHEMBL339768 — IC50 = 500.0 nM 6.30
CHEMBL338984 — IC50 = 530.0 nM 6.28
CHEMBL335944 — IC50 = 530.0 nM 6.28
CHEMBL128749 — IC50 = 530.0 nM 6.28
CHEMBL341289 — IC50 = 580.0 nM 6.24
CHEMBL341289 — IC50 = 600.0 nM 6.22
CHEMBL132391 — IC50 = 640.0 nM 6.19
CHEMBL337853 — IC50 = 680.0 nM 6.17
CHEMBL338576 — IC50 = 700.0 nM 6.16
CHEMBL339155 — IC50 = 710.0 nM 6.15
CHEMBL128712 — IC50 = 710.0 nM 6.15
CHEMBL405016 — IC50 = 770.0 nM 6.11
CHEMBL128423 — IC50 = 830.0 nM 6.08
CHEMBL2112666 — IC50 = 890.0 nM 6.05
CHEMBL131551 — IC50 = 890.0 nM 6.05
CHEMBL435019 — IC50 = 910.0 nM 6.04
CHEMBL338177 — IC50 = 950.0 nM 6.02
CHEMBL339132 — IC50 = 960.0 nM 6.02
CHEMBL130993 — IC50 = 1000.0 nM 6.00
CHEMBL128328 — IC50 = 1000.0 nM 6.00
CHEMBL130887 — IC50 = 1100.0 nM 5.96
CHEMBL2112663 — IC50 = 1100.0 nM 5.96
CHEMBL338383 — IC50 = 1100.0 nM 5.96
CHEMBL129983 — IC50 = 1100.0 nM 5.96
CHEMBL337667 — IC50 = 1200.0 nM 5.92
CHEMBL128489 — IC50 = 1200.0 nM 5.92
CHEMBL338711 — IC50 = 1200.0 nM 5.92
CHEMBL340676 — IC50 = 1300.0 nM 5.89
CHEMBL339124 — IC50 = 1400.0 nM 5.85
CHEMBL131239 — IC50 = 1500.0 nM 5.82
CHEMBL341311 — IC50 = 1500.0 nM 5.82