Table 1.

Number and statistical analyses of chemical motifs and combinations

TotalInhibitors (<0.50)Activators (>1.60)
Classes Number Fraction Predicted Found P value Predicted Found P value 
Carboxyl (all) 2,298 23.36% 12.6 n.s. 16.8 38 P < 10−6 
Amide (all) 2,021 20.54% 11.1 n.s. 14.8 13 n.s. 
Biaryl amide (all) 733 7.45% 4.0 P = 0.015 5.4 17 P = 1.7 10−5 
Sulfonamide (all) 270 2.74% 1.5 n.s. 2.0 n.s. 
Biaryl sulfonamide (all) 605 6.15% 3.3 n.s. 4.4 n.s. 
Other 5,012 50.95% 27.5 40 P = 4 10−4 36.7 19 P = 1.9 10−5 
All combinations         
Carboxyl (only) 1,393 14.16% 7.6 n.s. 10.2 17 P = 0.022 
Amide (only) 1,304 13.25% 7.2 n.s. 9.5 n.s. 
Biaryl amide (only) 452 4.59% 2.5 n.s. 3.3 n.s. 
Sulfonamide (only) 132 1.34% 0.7 n.s. 1.0 n.s. 
Biaryl sulfonamide (only) 442 4.49% 2.4 n.s. 3.2 n.s. 
Carboxyl + amide 579 5.88% 3.2 n.s. 4.2 n.s. 
Carboxyl + biaryl amide 222 2.25% 1.2 n.s. 1.6 12 P < 10−6 
Carboxyl + sulfonamide 36 0.37% 0.2 n.s. 0.3 n.s. 
Carboxyl + biaryl sulfonamide 68 0.69% 0.4 n.s. 0.5 n.s. 
Amide + sulfonamide 95 0.97% 0.5 n.s. 0.7 n.s. 
Amide + biaryl sulfonamide 43 0.44% 0.2 n.s. 0.3 n.s. 
Sulfonamide + biaryl amide 0.07% 0.0 n.s. 0.1 n.s. 
Biaryl amide + biaryl sulfonamide 52 0.53% 0.3 n.s. 0.4 n.s. 
Other 5,012 50.95% 27.5 40 P = 4 10−4 36.7 19 P = 1.9 10−5 
Total 9,837 100.00% 54.0 54  72.0 72  
TotalInhibitors (<0.50)Activators (>1.60)
Classes Number Fraction Predicted Found P value Predicted Found P value 
Carboxyl (all) 2,298 23.36% 12.6 n.s. 16.8 38 P < 10−6 
Amide (all) 2,021 20.54% 11.1 n.s. 14.8 13 n.s. 
Biaryl amide (all) 733 7.45% 4.0 P = 0.015 5.4 17 P = 1.7 10−5 
Sulfonamide (all) 270 2.74% 1.5 n.s. 2.0 n.s. 
Biaryl sulfonamide (all) 605 6.15% 3.3 n.s. 4.4 n.s. 
Other 5,012 50.95% 27.5 40 P = 4 10−4 36.7 19 P = 1.9 10−5 
All combinations         
Carboxyl (only) 1,393 14.16% 7.6 n.s. 10.2 17 P = 0.022 
Amide (only) 1,304 13.25% 7.2 n.s. 9.5 n.s. 
Biaryl amide (only) 452 4.59% 2.5 n.s. 3.3 n.s. 
Sulfonamide (only) 132 1.34% 0.7 n.s. 1.0 n.s. 
Biaryl sulfonamide (only) 442 4.49% 2.4 n.s. 3.2 n.s. 
Carboxyl + amide 579 5.88% 3.2 n.s. 4.2 n.s. 
Carboxyl + biaryl amide 222 2.25% 1.2 n.s. 1.6 12 P < 10−6 
Carboxyl + sulfonamide 36 0.37% 0.2 n.s. 0.3 n.s. 
Carboxyl + biaryl sulfonamide 68 0.69% 0.4 n.s. 0.5 n.s. 
Amide + sulfonamide 95 0.97% 0.5 n.s. 0.7 n.s. 
Amide + biaryl sulfonamide 43 0.44% 0.2 n.s. 0.3 n.s. 
Sulfonamide + biaryl amide 0.07% 0.0 n.s. 0.1 n.s. 
Biaryl amide + biaryl sulfonamide 52 0.53% 0.3 n.s. 0.4 n.s. 
Other 5,012 50.95% 27.5 40 P = 4 10−4 36.7 19 P = 1.9 10−5 
Total 9,837 100.00% 54.0 54  72.0 72  

Number is the number of specific motifs or combinations among all studied compounds. The fraction is number/9,837. Predicted inhibitors is Fraction * 54 (total number of clear inhibitors). The predicted activators are Fraction * 72 (total number of clear activators). Found inhibitors/activators are from the experimental data. P value is the probability that the found value is different from the predicted value (see Materials and methods for calculations). Bold values denote that the found value is larger than the predicted value. Italic values denote that the found value is smaller than the predicted value.

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