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Assay Detail

CHEMBL1686964

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

Binding
Displacement of [3H]AVP from human V1b receptor expressed in CHO cells co-expressing VIP-luciferase by whole cell binding assay
40
Total Activities
40
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Vasopressin V1b receptor (CHEMBL1921)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and SAR studies of novel 2-(4-oxo-2-aryl-quinazolin-3(4H)-yl)acetamide vasopressin V1b receptor antagonists.
Napier SE, Letourneau JJ, Ansari N, Auld DS, Baker J, Best S, Campbell-Wan L, Chan JH, Craighead M, Desai H, Goan KA, Ho KK, Hulskotte EG, MacSweeney CP, Milne R, Morphy JR, Neagu I, Ohlmeyer MH, Peeters AW, Presland J, Riviello C, Ruigt GS, Thomson FJ, Zanetakos HA, Zhao J, Webb ML.
Bioorg Med Chem Lett (2011) 21 : 1871 -1875
PubMed 21353540 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 40 6.82 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1684573 1 8.52
CHEMBL1684561 1 8.40
CHEMBL1684562 1 8.30
CHEMBL1684574 1 8.22
CHEMBL1684408 1 7.82
CHEMBL1684571 1 7.77
CHEMBL1684560 1 7.58
CHEMBL1684409 1 7.52
CHEMBL1684559 1 7.47
CHEMBL1684557 1 7.38
CHEMBL1684572 1 7.34
CHEMBL1684570 1 7.31
CHEMBL1684558 1 7.23
CHEMBL1684569 1 7.14
CHEMBL1684555 1 7.07
CHEMBL1684410 1 6.95
CHEMBL1684556 1 6.91
CHEMBL1684407 1 6.90
CHEMBL1684567 1 6.82
CHEMBL1684568 1 6.71
CHEMBL1684405 1 6.60
CHEMBL1684553 1 6.49
CHEMBL1684548 1 6.48
CHEMBL1684406 1 6.44
CHEMBL1684551 1 6.41
CHEMBL1684549 1 6.33
CHEMBL1684550 1 6.19
CHEMBL1684404 1 6.10
CHEMBL1684403 1 5.99
CHEMBL1684546 1 5.87

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1684573 IC50 = 3.0 nM 8.52
CHEMBL1684561 IC50 = 4.0 nM 8.40
CHEMBL1684562 IC50 = 5.0 nM 8.30
CHEMBL1684574 IC50 = 6.0 nM 8.22
CHEMBL1684408 IC50 = 15.0 nM 7.82
CHEMBL1684571 IC50 = 17.0 nM 7.77
CHEMBL1684560 IC50 = 26.0 nM 7.58
CHEMBL1684409 IC50 = 30.0 nM 7.52
CHEMBL1684559 IC50 = 34.0 nM 7.47
CHEMBL1684557 IC50 = 42.0 nM 7.38
CHEMBL1684572 IC50 = 46.0 nM 7.34
CHEMBL1684570 IC50 = 49.0 nM 7.31
CHEMBL1684558 IC50 = 59.0 nM 7.23
CHEMBL1684569 IC50 = 72.0 nM 7.14
CHEMBL1684555 IC50 = 86.0 nM 7.07
CHEMBL1684410 IC50 = 113.0 nM 6.95
CHEMBL1684556 IC50 = 122.0 nM 6.91
CHEMBL1684407 IC50 = 125.0 nM 6.90
CHEMBL1684567 IC50 = 152.0 nM 6.82
CHEMBL1684568 IC50 = 196.0 nM 6.71
CHEMBL1684405 IC50 = 250.0 nM 6.60
CHEMBL1684553 IC50 = 325.0 nM 6.49
CHEMBL1684548 IC50 = 328.0 nM 6.48
CHEMBL1684406 IC50 = 366.0 nM 6.44
CHEMBL1684551 IC50 = 387.0 nM 6.41
CHEMBL1684549 IC50 = 470.0 nM 6.33
CHEMBL1684550 IC50 = 644.0 nM 6.19
CHEMBL1684404 IC50 = 800.0 nM 6.10
CHEMBL1684403 IC50 = 1030.0 nM 5.99
CHEMBL1684546 IC50 = 1350.0 nM 5.87
CHEMBL1684402 IC50 = 1450.0 nM 5.84
CHEMBL1684566 IC50 = 2350.0 nM 5.63
CHEMBL1684552 IC50 = 2400.0 nM 5.62
CHEMBL1684565 IC50 = 2500.0 nM 5.60
CHEMBL1684547 IC50 = 3100.0 nM 5.51
CHEMBL1684554 IC50 = 6050.0 nM 5.22
CHEMBL1684564 IC50 > 20000.0 nM -
CHEMBL1684563 IC50 > 20000.0 nM -
CHEMBL1684575 IC50 > 20000.0 nM -
CHEMBL1684576 IC50 > 20000.0 nM -